Amoxiclav radar instructions for use. Radar station radar. Structural diagram and principle of operation of a ship radar Which is better - Bisoprolol or Concor
The 250 mg/125 mg tablets contain active ingredients amoxicillin(trihydrate form) and clavulanic acid(a form of potassium salt). The tablets also contain auxiliary components: MCC sodium croscarmellose.
Tablets Amoxiclav 2X 625 mg and 1000 mg contain the active ingredients amoxicillin and clavulanic acid, as well as additional components: anhydrous colloidal silicon dioxide, flavorings, aspartame, yellow iron oxide, talc, hydrogenated castor oil, silicated MCC.
Amoxiclav Quiktab 500 mg and 875 mg tablets contain the active ingredients amoxicillin and clavulanic acid, as well as additional components: anhydrous colloidal silicon dioxide, flavorings, aspartame, yellow iron oxide, talc, hydrogenated Castor oil, MCC silicated.
The powder from which the Amoxiclav suspension is prepared also contains amoxicillin and clavulanic acid, and also contains sodium citrate, MCC, sodium benzoate, mannitol, and sodium saccharin as inactive components.
The powder for preparing Amoxiclav IV infusion contains amoxicillin and clavulanic acid.
Release form
The drug is produced in the form of tablets. Amoxiclav 250 mg/125 mg – film-coated tablets, package contains 15 pieces.
Amoxiclav 2X (500 mg/125 mg; 875 mg/125 mg) - coated tablets, the package may contain 10 or 14 pieces.
Amoxiclav Quiktab (500 mg/125 mg; 875 mg/125 mg) is available as dispersed tablets, there are 10 such tablets in a package.
The product is also produced in the form of a powder from which a suspension is made; the bottle contains powder for preparing 100 ml of the product.
A powder is also produced, from which a solution is made, which is administered intravenously. The bottle holds 600 mg of the product (amoxicillin 500 mg, clavulanic acid 100 mg), 1.2 g bottles are also available (amoxicillin 1000 mg, clavulanic acid 200 mg), the package holds 5 bottles.
pharmachologic effect
The abstract provides information that antibiotic Amoxiclav (INN Amoksiklav) is a broad-spectrum agent. Group of antibiotics: broad-spectrum penicillins. The medicine contains amoxicillin (semi-synthetic penicillin) and clavulanic acid (β-lactamase inhibitor). The presence of clavulanic acid in the composition of the drug ensures the resistance of amoxicillin to the action of β-lactamases produced by microorganisms.
The structure of clavulanic acid is similar to beta-lactam antibiotics, this substance also has an antibacterial effect. Amoxiclav is active against strains that demonstrate sensitivity to amoxicillin. This is a series gram-positive bacteria, aerobic gram-negative bacteria, gram-positive and gram-negative anaerobes.
Pharmacokinetics and pharmacodynamics
As the Vidal drug reference book informs, after oral administration, both substances are actively absorbed from the gastrointestinal tract; the absorption of the components is not affected by food intake, so it does not matter how you take it - before or after meals. Highest concentration in blood observed one hour after the drug was taken. Both active ingredients of the drug are distributed in fluids and tissues. Amoxicillin also enters the liver, synovial fluid, prostate, tonsils, gallbladder, muscle tissue, saliva, bronchial secretions.
If the membranes of the brain are not inflamed, both active substances do not penetrate through the BBB. At the same time, the active components penetrate the placental barrier, and traces of them are detected in breast milk. They bind to blood proteins to a small extent.
In the body, amoxicillin undergoes partial metabolism, clavulanic acid is metabolized intensively. It is excreted from the body through the kidneys; small particles of active substances are excreted by the intestines and lungs. The half-life of amoxicillin and clavulanic acid is 1-1.5 hours.
Indications for use of Amoxiclav
Amoxiclav is prescribed for infectious and inflammatory diseases that develop due to the influence of microorganisms sensitive to this medicine. The following indications for the use of this drug are determined:
- infections of the ENT organs, as well as infectious diseases of the upper respiratory tract (otitis media, retropharyngeal abscess, sinusitis, pharyngitis, tonsillitis);
- urinary tract infections (with cystitis, at prostatitis and etc.);
- infectious diseases of the lower respiratory tract (pneumonia, bronchitis acute and chronic);
- gynecological diseases of an infectious nature;
- connective and bone tissue infections;
- infectious diseases of soft tissues, skin (including consequences of bites);
- biliary tract infections (cholangitis, cholecystitis);
- odontogenic infections.
What else Amoxiclav helps with, you should ask a specialist during an individual consultation.
Contraindications
When determining why tablets and other forms of the drug help, you should also take into account existing contraindications:
- Infectious mononucleosis;
- previously past illnesses liver or cholestatic jaundice when taking clavulanic acid or amoxicillin;
- lymphocytic leukemia;
- high sensitivity to antibiotic drugs from the group of cephalosporins, penicillins, as well as other beta-lactam antibiotics;
- high sensitivity to the active components of the drug.
It is prescribed with caution to people suffering from liver failure and people with severe kidney disease.
Side effects
When taking this antibiotic, patients may experience the following side effects:
- Digestive system: deterioration appetite, vomiting, nausea, diarrhea; in rare cases, abdominal pain and liver dysfunction may occur; isolated manifestations - hepatitis, jaundice, pseudomembranous colitis.
- Hematopoietic system: in rare cases - reversible leukopenia, thrombocytopenia; in very rare cases - eosinophilia, pancytopenia.
- Allergic manifestations: itching, erythematous rash, hives; in rare cases - anaphylactic shock, exudative erythema, edema, allergic vasculitis; isolated manifestations - Stevens-Johnson syndrome, pustulosis, exfoliative dermatitis.
- Functions of the nervous system: dizziness, headache; in rare cases - convulsions, anxiety, hyperactivity, insomnia.
- Urinary system: crystalluria, interstitial nephritis.
- In rare cases, superinfection may occur.
It is noted that such treatment, as a rule, does not provoke significant side effects.
Instructions for use of Amoxiclav (Method and dosage of Amoxiclav for adults)
Medicine in tablets is not prescribed to children under 12 years of age. When prescribing the drug, it should be taken into account that the permissible dose per day of clavulanic acid is 600 mg (adults) and 10 mg per 1 kg of weight (child). The permissible daily dose of amoxicillin is 6 g for an adult and 45 mg per 1 kg of weight for a child.
The agent for parenteral administration is prepared by dissolving the contents of the vial in water for injection. To dissolve 600 mg of the product, you need 10 mol of water, to dissolve 1.2 g of the product - 20 ml of water. The solution should be administered slowly over 3-4 minutes. Intravenous infusion should continue for 30-40 minutes. The solution must not be frozen.
Before anesthesia, to prevent purulent complications, 1.2 g of drugs should be administered intravenously. If there is a risk of complications, the drug is administered intravenously or taken orally in the period after surgery. The duration of the appointment is determined by the doctor.
Amoxiclav tablets, instructions for use
As a rule, adults and children (who weigh more than 40 kg) receive 1 tablet every eight hours. (375 mg), provided the infection is mild or moderate. Another acceptable treatment regimen in this case is to take 1 tablet every 12 hours. (500 mg+125 mg). For severe infectious diseases, as well as for infectious diseases of the respiratory tract, taking 1 tablet every eight hours is recommended. (500 mg+125 mg) or taken every 12 hours 1 tablet. (875 mg+125 mg). Depending on the disease, you need to take an antibiotic from five to fourteen days, but the doctor must individually prescribe a treatment regimen.
Patients with odontogenic infections should take 1 tablet every 8 hours. (250 mg + 125 mg) or once 12 hours, 1 tablet. (500 mg + 125 mg) for five days.
People suffering from moderate renal failure, the use of 1 table is indicated. (500 mg + 125 mg) every twelve hours. Severe renal failure is a reason to increase the interval between doses to 24 hours.
Amoxiclav suspension, instructions for use
Childhood The patient's dose involves calculating the dose taking into account the child's weight. Before preparing the syrup, shake the bottle well. In two doses you need to add 86 ml of water to the bottle, each time you need to shake its contents well. Please note that the measuring spoon contains 5 ml of product. Prescribed in a dose depending on the age and weight of the child.
Instructions for use Amoxiclav for children
Children from birth to three months are prescribed the drug at the rate of 30 mg per 1 kg of weight (dose per day), this dose should be divided equally and administered at equal intervals. From the age of three months, Amoxiclav is prescribed at a dose of 25 mg per 1 kg of weight, which is similarly divided equally into two administrations. For infectious diseases of moderate severity, the dose is prescribed at the rate of 20 mg per 1 kg of weight, divided into three administrations. For severe infectious diseases, the dose is prescribed at the rate of 45 mg per 1 kg of weight, divided into two doses per day.
Instructions for use Amoxiclav Quiktab
Before taking, the tablet must be dissolved in 100 ml of water (the amount of water may be more). Before taking, you need to stir the contents well. You can also chew the tablet; it is better to take the drug before meals. Adults and children after reaching 12 years of age should take 1 tablet per day. 625 mg 2-3 times a day. For severe infectious diseases, 1 tablet is prescribed. 1000 mg 2 times a day. Treatment should not last more than 2 weeks.
Sometimes a doctor may prescribe analogues of the drug, for example, Flemoclav Solutab, etc.
Amoxiclav for sore throat
The drug Amoxiclav for sore throat an adult is prescribed 1 tablet. 325 mg once every 8 hours. Another treatment regimen involves taking 1 tablet once every 12 hours. A doctor may prescribe a higher dose of an antibiotic if the disease in an adult is severe. Treatment of sore throat in children involves the use of a suspension. As a rule, 1 spoon is prescribed (a dosage spoon is 5 ml). The frequency of administration is determined by the doctor, whose recommendations are important to follow. How to take Amoxiclav for children with sore throat depends on the severity of the disease.
Dosage of Amoxiclav for sinusitis
Does Amoxiclav help with sinusitis, depends on the causes and characteristics of the course of the disease. The dosage is determined by the otolaryngologist. It is recommended to take 500 mg tablets three times a day. How many days to take the medicine depends on the severity of the disease. But after the symptoms disappear, you need to take the drug for two more days.
Overdose
To avoid overdose, the prescribed dosage for children and the dosage of Amoxiclav for adults must be strictly observed. It is recommended to carefully study the instructions or watch a video on how to dilute the suspension.
Wikipedia indicates that with an overdose of the drug, a number of manifestations are possible: unpleasant symptoms, however, there is no data on the patient’s life-threatening conditions. Due to an overdose, the appearance of abdominal pain, vomiting, diarrhea, excitement. In severe cases, seizures may occur.
If the drug has been taken recently, gastric lavage is indicated. Activated carbon . The patient must be monitored by a doctor. In this case it is effective hemodialysis.
Interaction
When taking the drug simultaneously with some drugs, undesirable manifestations may occur, which is why tablets, syrup and intravenous administration of the drug should not be used in parallel with a number of drugs.
Simultaneous use of drugs with Glucosamine, antacids, aminoglycosides, laxatives slow down the absorption of Amoxiclav when taken simultaneously with Ascorbic acid– absorption accelerates.
With simultaneous treatment with Phenylbutazone, diuretics, NSAIDs, Allopurinol and other drugs that block tubular secretion, the concentration of amoxicillin increases.
If anticoagulants and Amoxiclav are taken simultaneously, the prothrombin time increases. Therefore, drugs in such a combination must be prescribed with caution.
Amoxiclav increases toxicity Methotrexate when taken simultaneously.
When taking Amoxiclav and Allopurinol the likelihood of exanthema occurring increases.
Should not be taken at the same time Disulfiram and Amoxiclav.
Antagonists when taken together are amoxicillin and Rifampicin. The drugs mutually weaken the antibacterial effect.
You should not take Amoxiclav and bacteriostatic antibiotics (tetracyclines, macrolides), as well as sulfonamides at the same time, as these drugs can reduce the effectiveness of Amoxiclav.
Probenecid increases the concentration of amoxicillin and slows down its elimination.
When using Amoxiclav, the effectiveness of oral contraceptives may decrease.
Terms of sale
In pharmacies, Amoxiclav is sold by prescription; a specialist issues a prescription in Latin.
Storage conditions
The medicine belongs to list B. It must be stored in a place inaccessible to children, at a temperature of no more than 25°C.
Best before date
special instructions
Since the majority of people suffering from lymphocytic leukemia and infectious mononucleosis and receiving Ampicillin, subsequently noted the manifestation of an erythematous rash; such people are not recommended to take ampicillin antibiotics.
Prescribed with caution to people with a tendency to allergies.
If a course of treatment with the drug is prescribed for adults or children, it is important to monitor the functions of the kidneys, liver, and the process of hematopoiesis.
People who have impaired renal function need a dose adjustment of the drug or an increase in the interval between taking the drug.
It is optimal to take the product during meals to reduce the likelihood of side effects from the digestive system.
Patients undergoing treatment with Amoxiclav may experience a false-positive reaction when determining glucose levels in urine when using Felling's solution or Benedict's reagent.
There is no data on the negative impact of Amoxiclav on the ability to drive vehicles and work with precision machinery.
Patients who are interested in whether Amoxiclav is an antibiotic or not should keep in mind that the product is an antibacterial drug.
If Amoxiclav is prescribed, the patient's childhood age must be taken into account when prescribing the medication form and dosage.
Analogues of Amoxiclav Level 4 ATX code matches:
There are a number of analogues of this drug. The price of analogues depends, first of all, on the manufacturer of the drug. There are analogues on sale that are cheaper than Amoxiclav. For patients interested in what can replace this antibiotic, experts offer a large list of medications. These are the means Moxiclave, Co-Amoxiclav, Augmentin, Clavocin, Flemoklav, Honeyclave, Bactoclav, Ranklav, Amowycombe etc. However, any substitute should only be prescribed by a doctor. You can choose a cheaper analogue in tablets, for example, Augmentin. You can also choose a Russian analogue, for example, Amoxicillin.
Flemoklav Solutab and Amoxiclav: the difference between the drugs
The active components of the drugs are similar. The difference between drugs is in the dosage of the active components in the release forms of these drugs. Both drugs fall into approximately the same price category.
Which is better: Amoxiclav or Augmentin?
What is the composition of Amoxiclav and Augmentin, what is the difference between these drugs? Both of these products contain similar active ingredients, that is, in fact they are the same thing. Respectively, pharmachologic effect The drugs are almost identical, as are the side effects. Only the manufacturers of these drugs differ.
Which is better: Sumamed or Amoxiclav?
Sumamed contains azithromycin, which is a broad-spectrum antibiotic. Before prescribing any of the drugs, it is important to check the sensitivity of the microflora to their action.
Which is better: Flemoxin Solutab or Amoxiclav?
In the composition of the product Flemoxin contains only amoxicillin. Accordingly, its spectrum of influence is less than that of the drug Amoxiclav, which also contains clavulonic acid.
Amoxiclav for children
Children should take antibiotics only after a doctor's prescription. It is important to adhere to the specified dosage. Children under 12 years of age are usually prescribed a suspension. The dosage of Amoxiclav suspension for children depends on the severity of the disease and diagnosis. As a rule, children under 2 years of age are prescribed a dose of 62.5 mg, from 2 to 7 years of age - 125 mg, from 7 to 12 years of age - 250 mg.
Amoxiclav and alcohol
This drug should not be combined with alcohol. When taken simultaneously, the load on the liver increases significantly, and the likelihood of a number of negative effects also increases.
Amoxiclav during pregnancy and lactation
Amoxiclav at pregnancy can be used if the expected effect exceeds the possible harm to the fetus. It is undesirable to use the drug Amoxiclav in the early stages of pregnancy. The 2nd trimester and 3rd trimester are more preferable, but even during this period, the dosage of Amoxiclav during pregnancy must be observed very precisely. Amoxiclav at breastfeeding are not prescribed, since the active components of the drug penetrate into breast milk.
Reviews about Amoxiclav
In the process of discussing the drug Amoxiclav, reviews from doctors and patients are predominantly positive. It is noted that the antibiotic is effective in the treatment of respiratory tract diseases, and it is suitable for both adults and children. Reviews mention the effectiveness of the product for sinusitis, otitis media, and genital tract infections. As a rule, adult patients take 875 mg + 125 mg tablets; if the dosage is correct, relief occurs quickly. The reviews note that after a course of antibiotic treatment, it is advisable to take drugs that restore normal microflora.
Reviews of the Amoxiclav suspension are also positive. Parents write that it is convenient to give the product to children, as it has a pleasant taste and is normally perceived by children.
Amoxiclav price, where to buy
The price of Amoxiclav tablets 250 mg + 125 mg is on average 230 rubles for 15 pieces. You can buy an antibiotic 500 mg + 125 mg at a price of 360 – 400 rubles for 15 pcs. How much 875 mg + 125 mg tablets cost depends on the place of sale. On average, their cost is 420 – 470 rubles for 14 pieces.
Price Amoxiclav Quiktab 625 mg – from 420 rubles for 14 pcs.
The price of Amoxiclav suspension for children is 290 rubles (100 ml).
Price Amoxiclav 1000 mg in Ukraine (Kyiv, Kharkov, etc.) – from 200 hryvnia for 14 pieces.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
WER.RU
Amoxiclav powder 400 mg+57 mg 17.5 g 70 ml Lek d. d.
Amoxiclav tablets 375 mg 15 pcs. Lek d. d.
Amoxiclav powder 25 g 100 ml 20 doses
Amoxiclav powder 35 g
ZdravZone
Amoxiclav powder for injection 600 mg No. 5 bottle Lek D.D.
Amoxiclav powder for injection 1200 mg No. 5 bottle Lek D.D.
Amoxiclav Quiktab 1000 mg No. 14 tablets Lek D.D.
Amoxiclav Quiktab 625 mg No. 14 tablets Lek D.D.
Amoxiclav 375 mg No. 15 tablets Lek D.D.
Pharmacy IFC
AmoksiklavLek, Slovenia
AmoksiklavLek, Slovenia
AmoksiklavLek, Slovenia
Amoxiclav QuiktabLek, Slovenia
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Pharmacy24
AmoxiclavLek (Slovenia)
Amoxiclav1
Amoxiclav 2x14
Amoxiclav 2x14
Amoxiclav quiktab dispersible tablets 875 mg/125 mg No. 10 Sandoz
PaniPharmacy
Amoxiclav 2 tablets p/o 875/125 mg No. 14 Sandoz
Amoxiclav 2 tablets p/o 875/125 mg No. 14 Sandoz
Amoxiclav 2 tablets p/o 875/125 mg No. 14 Sandoz
Amoxiclav 2 tablets p/o 875/125 mg No. 14 Sandoz
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BIOSPHERE
Amoxiclav 375 mg No. 15 tablet p.p.o.
Amoxiclav 156.25 mg/5 ml 100 ml portions/susp. for oral administrationLek Pharmaceuticals d.d. (Slovenia)
Amoxiclav 312.5 mg/5 ml 100 ml portions/susp. for oral administration
Amoxiclav 625 mg No. 15 tablet p.p.o.
Amoxiclav 2X 625 mg No. 14 tablet p.p.o.
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NOTE! Information about medications on the site is for reference and general information, collected from publicly available sources and cannot serve as a basis for making a decision on the use of medications in the course of treatment. Before use medicinal product For amoxiclav, be sure to consult your doctor.
INSTRUCTIONS
on the use of the drug
for medical use
Read these instructions carefully before you start taking/using this medicine.
Save the instructions, you may need them again.
If you have any questions, consult your doctor.
This medicine is prescribed for you personally and should not be given to others because it may harm them even if they have the same symptoms as you.
Registration number
Tradename
Amoxiclav®
Group name
amoxicillin + clavulanic acid
Dosage form
Film-coated tablets
Compound
Active substances (core): each 250 mg + 125 mg tablet contains 250 mg of amoxicillin in the form of trihydrate and 125 mg of clavulanic acid in the form of potassium salt;
each 500 mg + 125 mg tablet contains 500 mg of amoxicillin in the form of trihydrate and 125 mg of clavulanic acid in the form of potassium salt;
Each 875 mg + 125 mg tablet contains 875 mg of amoxicillin in the form of trihydrate and 125 mg of clavulanic acid in the form of potassium salt.
Excipients (respectively for each dosage): colloidal silicon dioxide 5.40 mg/9.00 mg/12.00 mg, crospovidone 27.40 mg/45.00 mg/61.00 mg, croscarmellose sodium 27.40 mg/ 35.00 mg/47.00, magnesium stearate 12.00 mg/20.00 mg/17.22 mg, talc 13.40 mg (for dosage 250 mg + 125 mg), microcrystalline cellulose up to 650 mg/up to 1060 mg/up 1435 mg;
film coating tablets 250 mg + 125 mg - hypromellose 14.378 mg, ethylcellulose 0.702 mg, polysorbate 80 - 0.780 mg, triethyl citrate 0.793 mg, titanium dioxide 7.605 mg, talc 1.742 mg;
film coating tablets 500 mg + 125 mg - hypromellose 17.696 mg, ethylcellulose 0.864 mg, polysorbate 80 - 0.960 mg, triethyl citrate 0.976 mg, titanium dioxide 9.360 mg, talc 2.144 mg;
film coating tablets 875 mg + 125 mg - hypromellose 23.226 mg, ethylcellulose 1.134 mg, polysorbate 80 - 1.260 mg, triethyl citrate 1.280 mg, titanium dioxide 12.286 mg, talc 2.814 mg.
Description
250 mg + 125 mg tablets: white or off-white, oblong, octagonal, biconvex, film-coated tablets, imprinted “250/125” on one side and “AMC” on the other side.
Tablets 500 mg + 125 mg: white or almost white, oval, biconvex film-coated tablets.
Tablets 875 mg + 125 mg: white or off-white, oblong, biconvex, film-coated tablets, scored and imprinted “875/125” on one side and “AMC” on the other side.
Fracture appearance: yellowish mass.
Pharmacotherapeutic group
Antibiotic – semi-synthetic penicillin + beta-lactamase inhibitor
ATX code: J01CR02.
Pharmacological properties
Pharmacodynamics
Mechanism of action
Amoxicillin is a semisynthetic penicillin that is active against many gram-positive and gram-negative microorganisms. Amoxicillin disrupts the biosynthesis of peptidoglycan, which is a structural component of the bacterial cell wall. Violation of peptidoglycan synthesis leads to loss of cell wall strength, which causes lysis and death of microorganism cells. At the same time, amoxicillin is susceptible to destruction by beta-lactamases, and therefore the spectrum of activity of amoxicillin does not extend to microorganisms that produce this enzyme.
Clavulanic acid is a beta-lactamase inhibitor, structurally related to penicillins, has the ability to inactivate wide range beta-lactamases found in microorganisms resistant to penicillins and cephalosporins. Clavulanic acid is sufficiently effective against plasmid beta-lactamases, which most often cause bacterial resistance, and is not effective against type I chromosomal beta-lactamases, which are not inhibited by clavulanic acid.
The presence of clavulanic acid in the drug protects amoxicillin from destruction by enzymes - beta-lactamases, which allows expanding the antibacterial spectrum of amoxicillin.
Below is the activity of the combination of amoxicillin and clavulanic acid in vitro.
| Bacteria, usually sensitive |
| Gram-positive aerobes: Bacillus anthracis, Enterococcus faecalis, Listeria monocytogenes, Nocardia asteroides, Streptococcus pyogenes and other beta-hemolytic streptococci1,2, Streptococcus agalactiae1,2, Staphylococcus aureus (sensitive to methicillin)1, Staphylococcus saprophyticus (sensitive to methicillin), coagu lase-negative staphylococci (methicillin sensitive). Gram-negative aerobes: Bordetella pertussis, Haemophilus influenzae1, Helicobacter pylori, Moraxella catarrhalis1, Neisseria gonorrhoeae, Pasteurella multocida, Vibrio cholerae. Other: Borrelia burgdorferi, Leptospira icterohaemorrhagiae, Treponema pallidum. Gram-positive anaerobes: species of the genus Clostridium, Peptococcus niger, Peptostreptococcus magnus, Peptostreptococcus micros, species of the genus Peptostreptococcus. Gram-negative anaerobes: Bacteroides fragilis, species of the genus Bacteroides, species of the genus Capnocytophaga, Eikenella corrodens, Fusobacterium nucleatum, species of the genus Fusobacterium, species of the genus Porphyromonas, species of the genus Prevotella. |
| Bacteria for which acquired resistance is likely to a combination of amoxicillin and clavulanic acid |
| Gram-negative aerobes: Escherichia сoli1, Klebsiella oxytoca, Klebsiella pneumoniae, species of the genus Klebsiella, Proteus mirabilis, Proteus vulgaris, species of the genus Proteus, species of the genus Salmonella, species of the genus Shigella. Gram-positive aerobes: species of the genus Corynebacterium, Enterococcus faecium, Streptococcus pneumoniae1,2, streptococci of the Viridans group. |
| Naturally resistant bacteria to a combination of amoxicillin and clavulanic acid |
| Gram-negative aerobes: species of the genus Acinetobacter, Citrobacter freundii, species of the genus Enterobacter, Hafnia alvei, Legionella pneumophila, Morganella morganii, species of the genus Providencia, species of the genus Pseudomonas, species of the genus Serratia, Stenotrophomonas maltophilia, Yersinia enterocolitica. Other: Chlamydophila pneumoniae, Chlamydophila psittaci, species of the genus Chlamydia, Coxiella burnetii, species of the genus Mycoplasma. 1 For these bacteria, the clinical effectiveness of the combination of amoxicillin with clavulanic acid has been demonstrated in clinical studies. 2 strains of these bacterial species do not produce beta-lactamases. Sensitivity during amoxicillin monotherapy suggests similar sensitivity to the combination of amoxicillin and clavulanic acid. |
Pharmacokinetics
The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and clavulanic acid are highly soluble in aqueous solutions with physiological significance pH and after taking the drug Amoxiclav® orally are quickly and completely absorbed from the gastrointestinal tract (GIT). Absorption of the active substances amoxicillin and clavulanic acid is optimal when taken at the beginning of a meal.
The bioavailability of amoxicillin and clavulanic acid after oral administration is about 70%.
The following are the pharmacokinetic parameters of amoxicillin and clavulanic acid after administration at a dose of 875 mg/125 mg and 500 mg/125 mg twice daily, 250 mg/125 mg three times daily in healthy volunteers.
| Mean (±SD) pharmacokinetic parameters | |||||
| Active substances Amoxicillin/ clavulanic acid |
One-time dose (mg) |
Cmax (µg/ml) |
Tmax (hour) |
AUC (0-24h) (mcg.hour/ml) |
T1/2 (hour) |
| Amoxicillin | |||||
| 875 mg/125 mg | 875 | 11.64±2.78 | 1.50 (1.0-2.5) | 53.52±12.31 | 1.19±0.21 |
| 500 mg/125 mg | 500 | 7.19±2.26 | 1.50 (1.0-2.5) | 53.5±8.87 | 1.15±0.20 |
| 250 mg/125 mg | 250 | 3.3±1.12 | 1,5 (1,0-2,0) | 26.7±4.56 | 1.36±0.56 |
| Clavulanic acid | |||||
| 875 mg/125 mg | 125 | 2.18±0.99 | 1.25 (1.0-2.0) | 10.16±3.04 | 0.96±0.12 |
| 500 mg/125 mg | 125 | 2.40±0.83 | 1.5 (1.0-2.0) | 15.72±3.86 | 0.98±0.12 |
| 250 mg/125 mg | 125 | 1.5±0.70 | 1,2 (1,0-2,0) | 12.6±3.25 | 1.01±0.11 |
Cmax – maximum concentration in blood plasma;
Tmax – time to reach maximum concentration in blood plasma;
AUC – area under the concentration-time curve;
T1/2 – half-life
Distribution
Both components are characterized by a good volume of distribution in various organs, tissues and fluids of the body (including the lungs, abdominal organs; adipose, bone and muscle tissues; pleural, synovial and peritoneal fluids; skin, bile, urine, purulent discharge, sputum, interstitial fluid).
Plasma protein binding is moderate: 25% for clavulanic acid and 18% for amoxicillin.
The volume of distribution is approximately 0.3-0.4 l/kg for amoxicillin and approximately 0.2 l/kg for clavulanic acid.
Amoxicillin and clavulanic acid do not penetrate the blood-brain barrier in non-inflammatory conditions. meninges.
Amoxicillin (like most penicillins) is excreted in breast milk. Trace amounts of clavulanic acid are also found in breast milk. Amoxicillin and clavulanic acid penetrate the placental barrier.
Metabolism
About 10-25% of the initial dose of amoxicillin is excreted by the kidneys in the form of inactive penicillic acid. Clavulanic acid in the human body undergoes intensive metabolism with the formation of 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butan-2-one and is excreted by the kidneys, through the gastrointestinal tract, and also with exhaled air in the form of carbon dioxide.
Removal
Amoxicillin is eliminated primarily by the kidneys, while clavulanic acid is eliminated through both renal and extrarenal mechanisms. After a single oral dose of one tablet of 250 mg/125 mg or 500 mg/125 mg, approximately 60-70% of amoxicillin and 40-65% of clavulanic acid are excreted unchanged by the kidneys during the first 6 hours.
The average half-life (T1/2) of amoxicillin/clavulanic acid is approximately one hour, and the average total clearance is approximately 25 L/h in healthy patients.
The largest amount of clavulanic acid is excreted during the first 2 hours after administration.
Patients with impaired renal function
The total clearance of amoxicillin/clavulanic acid decreases in proportion to the decrease in renal function. The decrease in clearance is more pronounced for amoxicillin than for clavulanic acid, because Most amoxicillin is excreted by the kidneys. Doses of the drug for renal failure should be selected taking into account the undesirability of amoxicillin accumulation while maintaining normal level clavulanic acid.
Patients with liver dysfunction
In patients with impaired liver function, the drug is used with caution; continuous monitoring of liver function is necessary.
Both components are removed by hemodialysis and minor amounts by peritoneal dialysis.
Indications for use
Infections caused by sensitive strains of microorganisms:
infections of the upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);
lower respiratory tract infections (including acute bronchitis with bacterial superinfection, Chronical bronchitis, pneumonia);
urinary tract infections;
infections in gynecology;
skin and soft tissue infections, as well as wounds from human and animal bites;
infections of bone and connective tissue;
biliary tract infections (cholecystitis, cholangitis);
odontogenic infections.
Contraindications
Hypersensitivity to the components of the drug;
history of hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics;
cholestatic jaundice and/or other liver dysfunction caused by a history of taking amoxicillin/clavulanic acid;
infectious mononucleosis and lymphocytic leukemia;
children under 12 years of age or with a body weight of less than 40 kg.
Carefully
History of pseudomembranous colitis, diseases of the gastrointestinal tract, liver failure, severe renal dysfunction, pregnancy, lactation, when used simultaneously with anticoagulants.
Use during pregnancy and breastfeeding
Animal studies have not revealed any evidence of harm from taking the drug during pregnancy or its effect on the embryonic development of the fetus.
One study in women with premature rupture of membranes found that prophylactic use of amoxicillin/clavulanic acid may be associated with an increased risk of neonatal necrotizing enterocolitis.
During pregnancy and lactation, the drug is used only if the expected benefit to the mother outweighs the potential risk to the fetus and child.
Amoxicillin and clavulanic acid pass into breast milk in small quantities.
In infants receiving breast-feeding, possible development of sensitization, diarrhea, candidiasis of the mucous membranes of the oral cavity. When taking Amoxiclav®, it is necessary to decide whether to stop breastfeeding.
Directions for use and doses
Inside.
The dosage regimen is set individually depending on the age, body weight, kidney function of the patient, as well as the severity of the infection.
Amoxiclav® is recommended to be taken at the beginning of a meal for optimal absorption and to reduce possible side effects from the digestive system.
A course of treatment is 5-14 days. The duration of treatment is determined by the attending physician. Treatment should not be continued for more than 14 days without repeated medical examination.
Adults and children 12 years and older or weighing 40 kg or more:
For the treatment of mild to moderate infections - 1 tablet 250 mg + 125 mg every 8 hours (3 times a day).
For the treatment of severe infections and respiratory infections - 1 tablet 500 mg + 125 mg every 8 hours (3 times a day) or 1 tablet 875 mg + 125 mg every 12 hours (2 times a day).
Since amoxicillin and clavulanic acid combination tablets of 250 mg + 125 mg and 500 mg + 125 mg contain the same amount of clavulanic acid - 125 mg, then 2 tablets of 250 mg + 125 mg are not equivalent to 1 tablet of 500 mg + 125 mg.
Patients with impaired renal function
Dose adjustments are based on the maximum recommended dose of amoxicillin and are based on creatinine clearance (CC) values.
| QC | Amoxiclav® dosage regimen |
| >30 ml/min | No dosage adjustment required |
| 10-30 ml/min | 1 tablet 500 mg + 125 mg 2 times a day or 1 tablet 250 mg + 125 mg 2 times a day (depending on the severity of the disease). |
| 30 ml/min. Patients with liver dysfunction Amoxiclav® should be taken with caution. It is necessary to regularly monitor liver function. Does not require adjustment of the dosage regimen for elderly patients. In elderly patients with impaired renal function, the dose should be adjusted as for adult patients with impaired renal function. Side effect According to World Organization Health (WHO) adverse effects are classified according to their frequency of development as follows: very often (≥1/10), often (≥1/100, Amoxiclav - new instructions for use of the drug, you can see contraindications, side effects, prices in pharmacies for Amoxiclav. Reviews about Amoxiclav - A broad-spectrum penicillin antibiotic with a beta-lactamase inhibitor. Amoxiclav release form, drug packaging and composition.Powder for the preparation of a solution for intravenous administration from white to yellowish white. Powder for preparing a solution for intravenous administration 1 fl. amoxicillin (in the form sodium salt) 500 mg clavulanic acid (as potassium salt) 100 mg The description of the drug is based on the officially approved instructions for use. Pharmacological action AmoxiclavBroad-spectrum antibiotic; contains semisynthetic penicillin amoxicillin and β-lactamase inhibitor clavulanic acid. Clavulanic acid forms a stable inactivated complex with β-lactamases and ensures the resistance of amoxicillin to their effects. Pharmacokinetics of the drug.The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and clavulanic acid in combination do not affect each other. Pharmacokinetics of the drug.in special clinical cases Indications for use:Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug: The drug is administered intravenously. Dosage and method of administration of the drug.>0.5 ml/s (>30 ml/min) no dose adjustment required 0.166-0.5 ml/s (10-30 ml/min) first dose - 1.2 g (1000 mg + 200 mg), and then 600 mg (500 mg+100 mg) IV every 12 hours
Excipients Film shell composition: 15 pcs. - dark glass bottles (1) - cardboard packs. Film-coated tablets white or almost white, oval, biconvex. Excipients: colloidal silicon dioxide, crospovidone, croscarmellose sodium, magnesium stearate, talc, microcrystalline cellulose. Film shell composition: hypromellose, ethylcellulose, diethyl phthalate, macrogol 6000, titanium dioxide.
Film-coated tablets white or almost white, oblong, biconvex, with the imprint “AMC” on one side, with a notch and imprint “875” and “125” on the other. Excipients: colloidal silicon dioxide, crospovidone, croscarmellose sodium, magnesium stearate, talc, microcrystalline cellulose. Film shell composition: hypromellose, ethylcellulose, povidone, triethyl citrate, titanium dioxide, talc. 5 pieces. - blisters (2) - cardboard packs. |
During experiments on radio communications between ships, he discovered the phenomenon of reflection of radio waves from the ship. The radio transmitter was installed on the upper bridge of the transport "Europe", which was at anchor, and the radio receiver was installed on the cruiser "Africa". In the report of the commission appointed to conduct these experiments, A. S. Popov wrote:
The influence of the ship's environment is reflected in the following: all metal objects (masts, pipes, gear) must interfere with the operation of instruments both at the sending station and at the receiving station, because when they get in the way of the electromagnetic wave, they disrupt its correctness, partly similar to how a breakwater acts on an ordinary wave propagating over the surface of water, partly due to the interference of the waves excited in them with the waves of the source, that is, they influence unfavorably.
...The influence of the intermediate vessel was also observed. So, during the experiments, the cruiser “Lieutenant Ilyin” got between “Europe” and “Africa”, and if this happened at large distances, then the interaction of the instruments stopped until the ships left the same straight line.
During Operation Bruneval Conducted by English commandos on the French coast in the province of Seine-Maritime (Haute-Normandy), the secret of German radars was revealed. To jam radars, the Allies used transmitters that emitted interference in a certain frequency band with an average frequency of 560 megahertz. At first, bombers were equipped with such transmitters. When German pilots learned to guide fighters to jamming signals, as if to radio beacons, huge American Tuba transmitters were placed along the southern coast of England ( Project Tuba), developed in Harvard University Radio Laboratory. Their powerful signals blinded German fighters in Europe, and Allied bombers, having gotten rid of their pursuers, calmly flew home across the English Channel.
IN THE USSR
In the Soviet Union, awareness of the need for aircraft detection means free from the disadvantages of sound and optical surveillance led to the development of research in the field of radar. The idea proposed by the young artilleryman Pavel Oshchepkov received the approval of the high command: the People's Commissar of Defense of the USSR K. E. Voroshilov and his deputy, M. N. Tukhachevsky.
In 1946, American experts Raymond and Hacherton, former employees of the US Embassy in Moscow, wrote: “Soviet scientists successfully developed the theory of radar several years before radar was invented in England.”
Much attention in the air defense system is paid to solving the problem of timely detection of low-flying air targets (English).
Classification
According to the scope of application there are:
- military radars;
- civil radars.
By purpose:
- detection radar;
- Control and tracking radar;
- panoramic radars;
- Side-view radar;
- weather radars;
- Target designation radar;
- Situation surveillance radar.
By the nature of the carrier:
- coastal radars;
- maritime radars;
- airborne radars;
- mobile radars.
By type of action:
- primary, or passive;
- secondary, or active;
- combined.
By method of action:
- over-horizon radar;
By wave range:
- meter;
- decimeter;
- centimeter;
- millimeter.
Primary radar
Primary (passive) radar mainly serves to detect targets by illuminating them with an electromagnetic wave and then receiving the reflections (echoes) of this wave from the target. Since the speed of electromagnetic waves is constant (the speed of light), it becomes possible to determine the distance to the target based on the measurement of various signal propagation parameters.
A radar station is based on three components: transmitter, antenna and receiver.
Transmitter(transmitting device) is a source of high power electromagnetic signal. It can be a powerful pulse generator. For centimeter-range pulsed radars, it is usually a magnetron or a pulse generator operating according to the following scheme: the master oscillator is a powerful amplifier, most often using a traveling wave lamp (TWT) as a generator, and for meter-range radars a triode lamp is often used. Radars that use magnetrons are incoherent or pseudo-coherent, unlike TWT-based radars. Depending on the design, the transmitter operates either in pulse mode, generating repeating short powerful electromagnetic pulses, or emits a continuous electromagnetic signal.
Antenna performs focusing of the transmitter signal and formation of the radiation pattern, as well as receiving the signal reflected from the target and transmitting this signal to the receiver. Depending on the implementation, the reflected signal can be received either by the same antenna or by another, which can sometimes be located at a considerable distance from the transmitting device. If transmission and reception are combined in one antenna, these two actions are performed alternately, and so that the powerful signal leaking from the transmitting transmitter to the receiver does not blind the weak echo receiver, a special device is placed in front of the receiver that closes the receiver input at the moment of emission of the probing signal .
Receiver(receiving device) performs amplification and processing of the received signal. In the very simple case the resulting signal is fed to a beam tube (screen), which displays an image synchronized with the movement of the antenna.
Different radars are based on different methods for measuring the parameters of the reflected signal:
Frequency method
The frequency range measurement method is based on the use of frequency modulation of emitted continuous signals. In this method, a frequency is emitted over a period that varies linearly from f1 to f2. The reflected signal will arrive modulated linearly at a time instant preceding the present by the delay time. That. the frequency of the reflected signal received at the radar will depend proportionally on time. The delay time is determined by a sharp change in the frequency of the difference signal.
Advantages:
- allows you to measure very short ranges;
- a low-power transmitter is used.
Flaws:
- two antennas are required;
- deterioration in the sensitivity of the receiver due to leakage through the antenna into the receiving path of the transmitter radiation, subject to random changes;
- high requirements for linearity of frequency changes.
Phase method
The phase (coherent) radar method is based on isolating and analyzing the phase difference between the sent and reflected signals, which arises due to the Doppler effect when the signal is reflected from a moving object. In this case, the transmitting device can operate both continuously and in pulse mode. The main advantage of this method is that it “allows you to observe only moving objects, and this eliminates interference from stationary objects located between the receiving equipment and the target or behind it.”
Since ultrashort waves are used, the unambiguous range of range measurement is on the order of several meters. Therefore, in practice, more complex circuits are used, in which two or more frequencies are present.
Advantages:
- low-power radiation, as undamped oscillations are generated;
- accuracy does not depend on the Doppler frequency shift of the reflection;
- a fairly simple device.
Flaws:
- lack of range resolution;
- deterioration in the sensitivity of the receiver due to penetration through the antenna into the receiving path of the transmitter radiation, subject to random changes.
Pulse method
Modern tracking radars are built as pulse radars. Pulse radar transmits the transmit signal only for a very short time, in a short pulse (usually about a microsecond), after which it goes into receive mode and listens for the echo reflected from the target while the radiated pulse propagates through space.
Since the pulse travels far from the radar at a constant speed, there is a direct relationship between the time elapsed from the moment the pulse is sent until the echo response is received and the distance to the target. The next pulse can be sent only after some time, namely after the pulse comes back (this depends on the radar detection range, transmitter power, antenna gain, receiver sensitivity). If the pulse is sent earlier, the echo of the previous pulse from a distant target may be confused with the echo of a second pulse from a close target. The time interval between pulses is called pulse repetition interval(English) Pulse Repetition Interval, PRI), its inverse is an important parameter called pulse repetition rate(ChPI, English) Pulse Repetition Frequency, PRF). Long-range low-frequency radars typically have a repetition interval of several hundred pulses per second. Pulse repetition rate is one of the distinctive features, by which it is possible to remotely determine the radar model.
Advantages of the pulse range measurement method:
- the ability to build a radar with one antenna;
- simplicity of the indicator device;
- Convenience of measuring the range of several targets;
- simplicity of emitted pulses, lasting a very short time, and received signals.
Flaws:
- the need to use high transmitter pulse powers;
- inability to measure short ranges;
- large dead zone.
Removing Passive Interference
One of the main problems of pulse radars is getting rid of the signal reflected from stationary objects: the earth's surface, high hills, etc. If, for example, an airplane is located against the backdrop of a high hill, the reflected signal from this hill will completely block the signal from the airplane. For ground-based radars, this problem manifests itself when working with low-flying objects. For airborne pulse radars, it is expressed in the fact that reflection from the earth's surface obscures all objects lying below the aircraft with the radar.
Methods for eliminating interference use, one way or another, the Doppler effect (the frequency of the wave reflected from an approaching object increases, and from a departing object it decreases).
The simplest radar that can detect a target in interference is radar with moving target selection(PDS) - a pulse radar that compares reflections from more than two or more pulse repetition intervals. Any target that moves relative to the radar produces a change in the signal parameter (stage in the serial SDS), while the interference remains unchanged. Elimination of interference occurs by subtracting reflections from two consecutive intervals. In practice, noise elimination can be carried out in special devices - through-period compensators or algorithms in software.
A fatal drawback of SDCs operating with constant PRF is the inability to detect targets with specific circular velocities (targets that produce phase changes of exactly 360 degrees). The speed at which a target becomes invisible to the radar depends on the station's operating frequency and PRF. To eliminate the shortcoming, modern SDCs emit several pulses with different PRFs. PRFs are selected in such a way that the number of “invisible” speeds is minimal.
Pulse-Doppler radars, unlike radars with SDC, they use a different, more the hard way getting rid of interference. The received signal, containing information about targets and interference, is transmitted to the input of the Doppler filter block. Each filter passes a signal of a certain frequency. At the output of the filters, derivatives of the signals are calculated. The method helps to find targets with given speeds, can be implemented in hardware or software, and does not allow (without modifications) to determine distances to targets. To determine distances to targets, you can divide the pulse repetition interval into segments (called range segments) and apply a signal to the input of the Doppler filter bank during this range segment. It is possible to calculate the distance only when multiple repetitions pulses at different frequencies (the target appears at different range segments at different PRFs).
An important property of pulse-Doppler radars is signal coherence, the phase dependence of sent and received (reflected) signals.
Pulse-Doppler radars, in contrast to radars with SDC, are more successful in detecting low-flying targets. On modern fighters, these radars are used for airborne interception and fire control (AN/APG-63, 65, 66, 67 and 70 radars). Modern implementations are mainly software: the signal is digitized and sent to a separate processor for processing. Often a digital signal is converted into a form convenient for other algorithms using a fast Fourier transform. Using software implementation compared to hardware has a number of advantages:
- the ability to select algorithms from among those available;
- the ability to change algorithm parameters;
- the ability to add/change algorithms (by changing the firmware).
The listed advantages, along with the ability to store data in ROM) allow, if necessary, to quickly adapt to the technique of jamming the enemy.
Elimination of active interference
The most effective method of combating active interference is the use of a digital antenna array in the radar, which allows the formation of dips in the radiation pattern in the directions of the jammers. . .
Secondary radar
Secondary radar is used in aviation for identification. The main feature is the use of an active transponder on aircraft.
The operating principle of the secondary radar is somewhat different from that of the primary radar. The Secondary Radar Station is based on the following components: transmitter, antenna, azimuth marker generators, receiver, signal processor, indicator and aircraft transponder with antenna.
Transmitter serves to generate request pulses in the antenna at a frequency of 1030 MHz.
Antenna serves to emit request pulses and receive the reflected signal. According to ICAO standards for secondary radar, the antenna emits at 1030 MHz and receives at 1090 MHz.
Azimuth marker generators serve to generate azimuth marks(eng. Azimuth Change Pulse, ACP) and North marks(English Azimuth Reference Pulse, ARP). For one rotation of the radar antenna, 4096 low azimuth marks (for older systems) or 16384 improved low azimuth marks (English) are generated. Improved Azimuth Change pulse, IACP- for new systems), as well as one North mark. The north mark comes from the azimuth mark generator when the antenna is in such a position when it is directed to the North, and small azimuth marks are used to count the antenna rotation angle.
Receiver serves to receive pulses at a frequency of 1090 MHz.
Signal processor serves to process received signals.
Indicator serves to display processed information.
Aircraft transponder with antenna serves to transmit a pulse radio signal containing additional information back to the radar upon request.
The principle of operation of the secondary radar is to use the energy of the aircraft transponder to determine the position of the aircraft. The radar irradiates the surrounding space with interrogation pulses P1 and P3, as well as a suppression pulse P2 at a frequency of 1030 MHz. Aircraft equipped with transponders located in the range of the interrogation beam, upon receiving interrogation pulses, if the condition P1, P3> P2 is in effect, respond to the requesting radar with a series of coded pulses at a frequency of 1090 MHz, which contain additional information about the aircraft number, altitude, and so on . The response of the aircraft transponder depends on the radar request mode, and the request mode is determined by the time interval between the request pulses P1 and P3, for example, in request mode A (mode A), the time interval between the station request pulses P1 and P3 is 8 microseconds and upon receiving such a request the transponder the aircraft encodes its aircraft number in the response pulses.
In request mode C (mode C), the time interval between station request pulses is 21 microseconds and upon receipt of such a request, the aircraft transponder encodes its altitude in the response pulses. The radar can also send a request in a mixed mode, for example, Mode A, Mode C, Mode A, Mode C. The azimuth of the aircraft is determined by the angle of rotation of the antenna, which, in turn, is determined by calculating small azimuth marks.
The range is determined by the delay of the received response. If the aircraft is in the range of the side lobes, and not the main beam, or is located behind the antenna, then the aircraft transponder, when receiving a request from the radar, will receive at its input the condition that pulses P1, P3 The signal received from the transponder is processed by the radar receiver, then goes to the signal processor, which processes the signals and provides information to the end user and (or) to the control indicator. Pros of a secondary radar: The article discusses the operating principle and general structural diagram of a ship's radar. The operation of radar stations (radars) is based on the use of the phenomenon of reflection of radio waves from various obstacles located in the path of their propagation, i.e. in radar, the phenomenon of echo is used to determine the position of objects. For this purpose, the radar has a transmitter, a receiver, a special antenna-waveguide device and an indicator with a screen for visual observation of echo signals. Thus, the operation of a radar station can be represented as follows: the radar transmitter generates high-frequency oscillations of a certain shape, which are sent into space in a narrow beam that continuously rotates along the horizon. Reflected vibrations from any object in the form of an echo signal are received by the receiver and displayed on the indicator screen, while it is possible to immediately determine on the screen the direction (bearing) to the object and its distance from the ship. The magnetron generates a probing pulse with a power of 70-80 kW, wavelength 1 = 3.2 cm, frequency /s = 9400 MHz. The magnetron pulse is supplied to the antenna through an antenna switch (AS) through a special waveguide and radiated into space in a narrow directed beam. The beam width in the horizontal plane is 1-2°, and in the vertical plane about 20°. The antenna, rotating around a vertical axis at a speed of 12-30 rpm, irradiates the entire space surrounding the vessel. One Bisoprolol tablet contains 0.005 or 0.01 g bisoprolol fumarate, as well as auxiliary components: magnesium stearate (Magnesium stearate), colloidal silicon dioxide (Silicon dioxide colloidal), crospovidone (Crospovidone), corn starch (Amylum maydis), microcrystalline cellulose (Cellulose microcrystalline). To make the film shell covering the tablet, the following are used: polyvinyl alcohol, titanium dioxide, talc, macrogol, dyes (iron oxide yellow, quinoline yellow, orange yellow). The drug is produced in the form of film-coated tablets, packaged in blister packs, 20, 30 or 50 pieces in a cardboard box. The tablets are round, biconvex, their color varies from beige to beige with a yellowish tint, at the break - from white to almost white. Bisoprolol (INN - Bisoprolol) belongs to the clinical-pharmacological group “ β1-blockers" Its action is aimed at relieving symptoms of myocardial ischemia(antianginal effect), normalization of the disturbed rhythm of contractions of the heart muscle(antiarrhythmic effect), as well as on decrease in blood pressure readings(antihypertensive effect). Bisoprolol is selective β1-blocker and does not have internal sympathomimetic and membrane-stabilizing activity. Under the influence of low doses of the active substance bisoprolol fumarate in a patient: According to the annotation, Bisoprolol in a dosage significantly higher than the therapeutic one (0.2 grams or more) can cause blockade, including β2-adrenergic receptors mainly in bronchi And smooth muscles of vascular walls. The drug is absorbed by approximately 80-90%, and the level of absorption does not depend on food intake. The concentration of the active substance in plasma reaches maximum value 60-180 minutes after taking the tablet. Bisoprolol fumarate binds to blood plasma proteins by approximately 30%. The substance has the ability to a small extent: Approximately half of the dose taken is metabolized into liver, resulting in the formation of inactive metabolites. The half-life varies from 10 to 12 hours. About 98% is eliminated from the body unchanged in the urine, up to 2% is excreted in bile. What are Bisoprolol tablets for? Indications for the use of Bisoprolol are arterial hypertension(persistently elevated blood pressure), stable angina pectoris(IHD), chronic heart failure (CHF). The drug Bisoprolol is produced by a fairly large number of pharmaceutical companies, however, regardless of where and by whom they are produced, the tablets have the same indications for use: that is, the indications for use of Bisoprolol-Pran are identical to the indications for use of the drug produced, for example, by Lugansk Chemical Pharmaceutical Plant or the Israeli company Teva. The use of Bisoprolol is contraindicated in: Due to the fact that there is not enough data on the safety and effectiveness of the drug for patients under 18 years of age, Bisoprolol is not used in pediatrics. In addition, the drug is not prescribed to patients undergoing treatment MAO inhibitors(the exception is cases when the patient is prescribed B-type monoamine oxidase inhibitors). Taking Bisoprolol may be accompanied by: In some cases, the course may worsen heart failure with the development of peripheral edema. In patients with impaired blood supply to the lower extremities, which is accompanied by intermittent claudication, as well as in patients diagnosed with Raynaud's syndrome, the main symptoms of these diseases may intensify. Also, the possibility of decreased glucose tolerance cannot be ruled out, mainly in patients with concomitant diabetes mellitus(including but not limited to hidden (latent) diabetes, which is characterized by the complete absence of any manifestations of this disease). The dosage of the drug is selected individually. The tablets are taken in the morning, before meals, without chewing. The course of treatment begins by prescribing 0.005 grams to the patient, which is taken once. Patients who have arterial pressure increased slightly, the starting dose is 0.0025 grams per day. In cases where this is necessary, the dose is doubled. The dosage regimen remains the same. The highest daily dose is 0.02 grams; for patients with kidney dysfunction, which is characterized by a decrease in creatinine clearance (CC) below a level of 20 ml per minute, the highest dose should be half that (0.01 grams per day). Exceeding the prescribed average daily dose is allowed in extreme cases. The drug is usually used for a long time. Elderly patients do not need dose adjustment. Instructions for use Bisoprolol-Ratiopharm identical to instructions for use Bisoprolol-Lugal and instructions for use Bisoprolol-Teva. According to the same scheme they take Bisoprolol-Prana and other bisoprolol preparations. An overdose of the drug is accompanied by the following symptoms: Treatment involves performing a gastric lavage procedure, taking adsorbent medicines
and prescription of symptomatic therapy: Inadmissible combinations with Bisoprolol: The drug is prescribed with caution with: Allowed combinations: To purchase the drug, a prescription in Latin is required. Bisoprolol is included in List B. It is recommended to store it in a dry place, protected from light, at room temperature (no more than 25 degrees Celsius). Keep away from children. 36 months. The drug should be prescribed with caution: Patients who have been diagnosed with pheochromocytoma”, the drug is prescribed only after completing a course of treatment α-blockers. Sudden withdrawal of the drug is unacceptable; the course of its use is completed gradually, gradually reducing the prescribed dose (it is considered optimal to reduce it by halving the dose daily). Structural analogues of Bisoprolol (synonyms) are drugs Biprol, Bisogamma, Niperten, Bisoprolol-Prana, Bisoprolol-Lugal, Bisoprolol-Ratiopharm, Bisoprolol-Teva, Concor, Concor Cor, Bisomore, Bioscard, Corbis, Bidop, Aritel Kor, Bisomore. Analogs of the drug according to the mechanism of action are Atenolol, Betacard, Betalok, Binelol, Cordanum, Lidalok, Lokren, Metozok, Metoprolol, Metocore, Nebivator, Nebilong, Nebilet, OD-Sky, Egilok, Estekor. Which is better - Bisoprolol or Concor? Concor is the brand name under which the original bisoprolol is produced. The manufacturer of the drug is the German pharmaceutical company Merck KGaA. However, the patent on this drug has long expired, so there are currently only a large number of more affordable generic bisoprolol. It is believed that all of them are not inferior in quality to the original drug, however, there is not enough official data to confirm this today. Bisoprolol is not recommended for the treatment of pregnant and lactating women. However, in situations where the benefits to the mother potentially outweigh the likely risks to the developing fetus, the drug may still be prescribed. IN exceptional cases When the medicine is used during pregnancy, it should be discontinued no later than 72 hours before the expected date of birth. Otherwise, there is a high likelihood that the newborn baby will develop hypoglycemia, arterial hypotension, bradycardia, and respiratory depression. When withdrawal is not possible, constant monitoring of the baby's condition is necessary during the first 72 hours after birth. If it is necessary to prescribe Bisoprolol to a nursing woman, it is necessary to resolve the issue of terminating lactation. Most often, the topic of drug withdrawal is discussed on relevant forums. Reviews about Bisoprolol left by patients and doctors are mainly related to withdrawal syndrome, which occurs against the background of abrupt cessation of treatment with this drug. Its particular manifestations are increased heart rate And seizures arterial hypertension
. Some patients note that during treatment with the drug they have significantly vision decreased. However, since Bisoprolol is prescribed for a long period of time (for some patients even for life), visual impairment and medication intake may be unrelated phenomena. Taking Bisoprolol may be accompanied by side effects. Some patients practically do not notice them in themselves, while in others, if you believe the reviews, they are quite pronounced. In connection with all of the above, neither treatment nor discontinuation of the use of this drug should be an independent decision of the patient. In each specific case, the treatment regimen and dosage regimen are determined solely by the doctor who is caring for the patient. The price of Bisoprolol depends on which pharmaceutical company produced the drug. For example, the average price of Bisoprolol-Ratiopharm 0.005 grams is 55 UAH (in Russian pharmacies you can buy it for about 345 rubles), but the price of Bisoprolol-Astrapharm starts from 8 UAH. The price of analogues of the drug on the Russian pharmaceutical market is from 32 rubles (the average package of Bisoprolol-Prana 0.005 grams costs the buyer this amount). Bisoprolol-Prana tablets 5 mg 30 pcs.Pranafarm Bisoprolol-Teva tablets 10 mg 30 pcs. Teva Bisoprolol-Teva tablets 5 mg 30 pcs. Teva Bisoprolol tablets 2.5 mg 30 pcs.Vertex Bisoprolol-Prana tablets 10 mg 30 pcs.Pranafarm Bisoprolol 10 mg No. 30 tablets /ozone/Ozone LLC Bisoprolol 5mg No. 30 tablets /ozone/Ozone LLC Bisoprolol-prana 10 mg No. 30 tabletsPranafarm LLC Bisoprolol-Teva 10 mg No. 30 tabletsTeva Pharmaceutical Bisoprolol-Teva 10 mg No. 50 tabletsTeva Pharmaceutical Bisoprolol-TevaTeva, Israel Bisoprolol-TevaTeva, Israel Bisoprolol-TevaTeva, Israel Bisoprolol-TevaTeva, Israel BisoprololSevernaya Zvezda JSC, Russia Bisoprolol Bisoprolol30 Bisoprolol30 Bisoprolol-Apo tablet. 10mg No. 30Apotex (Canada) Bisoprolol-Apo tablet. 10mg No. 60Apotex (Canada) Bisoprolol 10 mg No. 30 tablet p.o. Lekpharm LLC (Belarus) Bisoprolol 5 mg No. 30 tablet p.o. Lekpharm LLC (Belarus) Bisoprolol 10 mg No. 50 tablet p.o. Lekpharm LLC (Belarus) Bisoprolol 5 mg No. 50 tablet p.o. Lekpharm LLC (Belarus) Bisoprolol-ratiopharm 5 mg No. 50 tab. LSR-007326/10-290710 Tradename: Bisoprolol -Teva International nonproprietary name (INN): bisoprolol film-coated tablets Compound Round, biconvex, film-coated tablets, white or almost white, with engraving on one side: “BISOPROLOL 5” (dosage 5 mg) or “BISOPROLOL 10” (dosage 10 mg). Beta1-adrenergic blocker selective ATX Code:С07АВ07 Pharmacological properties Pharmacodynamics Bisoprolol is a selective beta 1-blocker, without its own sympathomimetic activity, and does not have a membrane-stabilizing effect. As with other beta1-blockers, the mechanism of action in hypertension is unclear. At the same time, it is known that bisoprolol reduces the activity of renin in the blood plasma, reduces the myocardial oxygen demand, and reduces the heart rate (HR). It has hypotensive, antiarrhythmic and antianginal effects. By blocking beta 1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP), reduces the intracellular current of calcium ions, inhibits all cardiac functions, reduces atrioventricular (AV) conductivity and excitability. When the therapeutic dose is exceeded, it has a beta2-adrenergic blocking effect. Total peripheral vascular resistance at the beginning of drug use, in the first 24 hours, increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), after 1-3 days it returns to its original value, and with prolonged use it decreases. Pharmacokinetics Bisoprolol is almost completely absorbed from the gastrointestinal tract; food intake does not affect absorption. The first pass effect through the liver is negligible, resulting in high bioavailability (90%). Bisoprolol is metabolized via the oxidative pathway without subsequent conjugation. All metabolites have strong polarity and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not exhibit pharmacological activity. Data obtained from in vitro experiments with human liver microsomes indicate that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%), with the CYP2D6 isoenzyme playing only a minor role. Indications for use Contraindications Carefully Use during pregnancy and breastfeeding Pregnancy Bisoprolol does not have direct cytotoxic, mutagenic or teratogenic effects, but has pharmacological effects that may have a harmful effect on the course of pregnancy and/or on the fetus or newborn. Typically, beta blockers reduce placental perfusion, leading to reduced fetal growth, intrauterine fetal death, miscarriage, or premature birth. The fetus and newborn child may experience pathological reactions, such as intrauterine growth retardation, hypoglycemia, bradycardia. Bisoprolol-Teva should not be used during pregnancy; use is possible if the benefit to the mother outweighs the risk of side effects in the fetus and/or child. In the event that treatment with Bisoprolol-Teva is considered necessary, blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored, and in the event of adverse events in relation to pregnancy and/or the fetus, alternative methods should be taken therapy. The newborn should be carefully examined after birth. Symptoms of hypoglycemia and bradycardia usually occur during the first 3 days of life. Breastfeeding period There is no data on the penetration of bisoprolol into breast milk. Therefore, taking the drug Bisoprolol-Teva is not recommended for women during breastfeeding. If it is necessary to use the drug during lactation, breastfeeding should be stopped. Directions for use and doses Side effect Overdose Interaction with other drugs special instructions In smokers, the effectiveness of beta-blockers is lower. Impact on the ability to drive vehicles and work with equipment that requires increased concentration. The use of the drug Bisoprolol-Teva does not affect the ability to drive vehicles, according to the results of a study in patients with coronary artery disease. However, due to individual reactions, the ability to drive vehicles or operate technically complex mechanisms may be impaired. This should be noted Special attention at the beginning of treatment, after changing the dose, and also with simultaneous use of alcohol. Release form Storage conditions Best before date Conditions for dispensing from pharmacies Owner ru: Manufacturer Pharmaceutical plant Teva Private Co. Ltd., N-4042, Debrecen, st. Pallagi 13, Hungary Address for receiving complaints: Russia, Moscow, 119049, st. Shabolovka, 10, Business Center "Concord" Trade name of the drug: Bisoprolol Active substance: Bisoprolol (Bisoprololum) Attention! Below is a description of the active substance. The decision about the possibility of using the described drug cannot be made on the basis of this information. Contraindications of the drugBisoprolol:
Hypersensitivity, sinus bradycardia (less than 45–50 beats/min), sick sinus syndrome, sinoatrial and AV block II–III degree, cardiogenic shock, acute and refractory to treatment severe heart failure, acute myocardial infarction, arterial hypotension (SBP below 90 mm Hg), severe obstructive respiratory failure, pregnancy, breastfeeding. Bisoprololduring pregnancy and breastfeeding: It is possible if the expected effect of therapy in the mother exceeds the potential risk to the fetus and child (adequate and strictly controlled studies of the safety of use in pregnant and lactating women have not been conducted). Since there is a risk of bradycardia, hypotension, hypoglycemia and respiratory distress (neonatal asphyxia) in newborns, treatment with bisoprolol fumarate should be discontinued 48–72 hours before delivery. If this cannot be done, the newborn should be under close medical observation for 48–72 hours after birth. The excretion of bisoprolol fumarate into human milk has not been studied, but since it is secreted into breast milk in rats (less than 2%), infants should be under medical supervision. Side effect of the drugBisoprolol:
The frequency of side effects is indicated when prescribing doses not exceeding 40 mg. From the nervous system and sensory organs: dizziness (3.5%), insomnia (2.5%), asthenia (1.5%), hypoesthesia (1.5%), depression (0.2%), drowsiness, anxiety, paresthesia (a feeling of coldness in the extremities), hallucinations, disturbances in thinking, concentration, orientation in time and space, balance, emotional lability, tinnitus, conjunctivitis, visual disturbances, decreased secretion of tear fluid, convulsions. From the outside of cardio-vascular system and blood (hematopoiesis, hemostasis): bradycardia (0.5%), arrhythmia, palpitations, AV block, hypotension, heart failure, impaired microcirculation in the myocardium and extremities, intermittent claudication, vasculitis, agranulocytosis, thrombocytopenia, thrombocytopenic purpura. From the gastrointestinal tract: diarrhea (3.5%), nausea (2.2%), vomiting (1.5%), dry mouth (1.3%), dyspeptic symptoms, constipation, ischemic colitis, mesenteric artery thrombosis . From the respiratory system: cough (2.5%), shortness of breath (1.5%), broncho- and laryngospasm, pharyngitis (2.2%), rhinitis (4%), sinusitis (2.2%), respiratory infections pathways (5%), respiratory distress syndrome. From the genitourinary system: peripheral edema (3%), decreased libido, impotence, Peyronie's disease, cystitis, renal colic. From the skin: rash, acne, eczema-like reactions, prurigo, redness of the skin, hyperhidrosis, dermatitis, alopecia. On the metabolic side: increased concentrations of liver enzymes (AST, ALT), hyperglycemia or increased glucose tolerance, hyperuricemia, changes in potassium concentration in the blood. Other: pain syndrome (headache - 10.9%, arthralgia - 2.7%, myalgia, pain in the abdomen, chest - 1.5%, eyes, ears), weight gain. Special instructions: It is possible that test results may change during laboratory tests. Precautionary measures: The possibility of masking the symptoms of hypoglycemia and thyrotoxicosis during treatment should be taken into account. It is possible that the severity of hypersensitivity reactions and the lack of effect from usual doses of adrenaline may increase against the background of a burdened allergic history. In case of severe liver dysfunction, acute renal failure (Cl creatinine less than 20 ml/min), patients on hemo- or peritoneal dialysis, the dose must be reduced. For pheochromocytoma, it should not be prescribed without additional administration of alpha-blockers. Bisoprolol reduces compensatory cardiovascular reactions in response to the use of general anesthetics and iodinated contrast agents. It is necessary to discontinue the drug 48 hours before anesthesia or choose anesthetic with the least negative inotropic effect. Treatment should be stopped gradually over a period of about 2 weeks (withdrawal syndrome is possible). Use with caution while working for vehicle drivers and people whose profession involves increased concentration. It is necessary to avoid the consumption of alcoholic beverages during treatment (risk of orthostatic hypotension). Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children. Best before date: 3 years. Attention: This information may not be current at the time of reading. Always look for the latest versions of the radar in the package with the drug. Clinical and pharmacological group Beta1 blocker Film-coated tablets
from beige-yellow to beige, round, biconvex; on the fracture, white or almost white. Excipients: croscarmellose sodium (primellose), povidone (medium molecular weight polyvinylpyrrolidone), pregelatinized starch (starch 1500), colloidal silicon dioxide (Aerosil), talc, microcrystalline cellulose, lactose (milk sugar), magnesium stearate. Film shell composition: opadry II (polyvinyl alcohol, partially hydrolyzed, titanium dioxide, talc, macrogol (polyethylene glycol 3350), iron (II) oxide dye). 10 pieces. - contour cell packaging (3) - cardboard packs. pharmachologic effect A selective beta1-blocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. Reduces plasma renin activity, reduces myocardial oxygen demand, and reduces heart rate (at rest and during exercise). It has hypotensive, antiarrhythmic and antianginal effects. By blocking beta1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, bathmo- and inotropic effect, inhibits the conductivity and excitability of the myocardium, and reduces AV conductivity. When increasing the dose above the therapeutic one, it has a beta2-adrenergic blocking effect. OPSS at the beginning of drug use, in the first 24 hours, increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and the elimination of stimulation of beta2-adrenergic receptors), which after 1-3 days returns to the original level, and with long-term administration decreases. The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure and an effect on the central nervous system .
In case of arterial hypertension, the effect occurs after 2-5 days, stable effect - after 1-2 months. The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate and decreased contractility, prolongation of diastole, and improved myocardial perfusion. By increasing end-diastolic pressure in the left ventricle and increasing the stretch of ventricular muscle fibers, it can increase oxygen demand, especially in patients with chronic heart failure. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions via the AV node) and along additional paths. When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause delay sodium ions (Na+) in the body; the severity of the atherogenic effect does not differ from the effect of propranolol. Pharmacokinetics Suction and distribution Absorption - 80-90%, food intake does not affect absorption. Cmax in blood plasma is observed after 1-3 hours. Communication with blood plasma proteins is about 30%. Passes through the BBB and the placental barrier to an insignificant extent, and is excreted in breast milk in small quantities. Metabolism and excretion 50% of the dose is metabolized in the liver to form inactive metabolites. T1/2 - 10-12 hours. About 98% is excreted in the urine - 50% unchanged, less than 2% -
with bile. Indications Arterial hypertension; IHD: prevention of angina attacks. Contraindications Shock (including cardiogenic); Collapse; Pulmonary edema; Acute heart failure; Chronic heart failure in the stage of decompensation; AV block II and III degrees; Sinoatrial block; Severe bradycardia; Prinzmetal's angina; Cardiomegaly (without signs of heart failure); Arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with myocardial infarction); History of severe forms of bronchial asthma and chronic obstructive pulmonary disease; Concomitant use of MAO inhibitors (except MAO-B); Late stages of peripheral circulatory disorders, Raynaud's disease; Pheochromocytoma (without simultaneous use of alpha-blockers); Metabolic acidosis; Age up to 18 years (efficacy and safety have not been established); Hypersensitivity to the components of the drug and other beta-blockers. WITH caution the drug should be prescribed for liver failure, chronic renal failure, myasthenia gravis, thyrotoxicosis, diabetes mellitus, first degree AV blockade, depression (including a history), psoriasis, as well as for elderly patients. Dosage The drug is taken orally, in the morning, on an empty stomach, without chewing, at an initial dose of 5 mg 1 time/day. If necessary, the dose is increased to 10 mg 1 time / day. The maximum daily dose is 20 mg/day. In patients with impaired renal function with CC less than 20 ml/min or with severe liver dysfunction the maximum daily dose should be 10 mg. Dose adjustments for elderly patients not required. Side effects From the side of the central nervous system: increased fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia, paresthesia in the limbs (in patients with intermittent claudication and Raynaud's syndrome), tremor. From the senses: blurred vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis. From the cardiovascular system: sinus bradycardia, palpitations, myocardial conduction disturbances, AV block (up to the development of complete transverse block and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (worsening) of chronic heart failure (swelling of the ankles, feet, shortness of breath), decreased blood pressure, orthostatic hypotension, manifestation of vasospasm (increased peripheral circulatory disorders, coldness of the lower extremities, Raynaud's syndrome), chest pain. From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver dysfunction (dark urine, yellowness of the sclera or skin, cholestasis), changes in taste. From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity) and/or in predisposed patients - laryngo- and bronchospasm. From the endocrine system: hyperglycemia (in patients with non-insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroid state. Allergic reactions: skin itching, rash, urticaria. Dermatological reactions: increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions, exacerbation of psoriasis symptoms. From the laboratory parameters: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, changes in the activity of liver enzymes (increased ALT, AST), bilirubin levels, triglycerides. Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia. Others: back pain, arthralgia, weakened libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure). Overdose Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, chronic heart failure, cyanosis of fingernails or palms, difficulty breathing, bronchospasm, dizziness, fainting, convulsions. Treatment: gastric lavage and administration of adsorbents; symptomatic therapy: in case of developed AV block - intravenous administration of 1-2 mg of atropine, epinephrine or installation of a temporary pacemaker; for ventricular extrasystole - lidocaine (class IA drugs are not used); when blood pressure decreases, the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - intravenous plasma-substituting solutions, if ineffective - administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic effects and eliminate a pronounced decrease in blood pressure); for heart failure - cardiac glycosides, diuretics, glucagon; for convulsions - intravenous diazepam; for bronchospasm, beta-agonists by inhalation. Drug interactions Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol. Phenytoin, when administered intravenously, and drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of a decrease in blood pressure. Changes the effectiveness of insulin and oral hypoglycemic drugs, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure). Reduces the clearance of lidocaine and xanthines (except diphylline) and increases their concentration in plasma, especially in patients with initially increased clearance of theophylline under the influence of smoking. The hypotensive effect is weakened by NSAIDs (Na+ retention and blockade of prostaglandin synthesis by the kidneys), corticosteroids and estrogens (Na+ ion retention). Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), amiodorone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure. Prolongs the effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins. Tri- and tetracyclic antidepressants, antipsychotic drugs (neuroleptics), ethanol, sedatives and hypnotics increase CNS depression. Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect; the break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders. Ergotamine increases the risk of developing peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in plasma; Rifampin shortens the half-life. special instructions Monitoring of patients taking Bisoprolol should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), conducting an ECG, determining blood glucose levels in patients with diabetes mellitus (once every 4-5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months). The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min. In approximately 20% of patients with angina, beta blockers are ineffective. Main reasons - severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats/min) and increased end-diastolic volume of the left ventricle, disrupting subendocardial blood flow. In smoking patients, the effectiveness of beta-blockers is lower. Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease. When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective alpha-blockade is not previously achieved). In case of thyrotoxicosis, Bisoprolol can mask certain clinical signs of thyrotoxicosis, for example, tachycardia. Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels. When taking clonidine concomitantly, it can be discontinued only a few days after discontinuation of Bisoprolol. It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from the usual doses of zpinephrine against the background of a burdened allergy history. If planned surgical treatment is necessary, the drug should be discontinued 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should select a drug for general anesthesia with minimal negative inotropic effect. Reciprocal activation of the vagus nerve can be eliminated by intravenous atropine (1-2 mg). Medicines that reduce the reserves of catecholamines (including reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia. Patients with bronchospastic diseases can be prescribed cardioselective adrenergic blockers in case of intolerance and/or ineffectiveness of other antihypertensive drugs. An overdose is dangerous due to the development of bronchospasm. If increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), or AV blockade is detected in elderly patients, it is necessary to reduce the dose or stop treatment. Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days). It should be discontinued before testing the content of catecholamines, normetanephrine and vanillinmandelic acid in the blood and urine, and titers of antinuclear antibodies. Impact on the ability to drive vehicles and operate machinery During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Pregnancy and lactation Use during pregnancy and lactation is possible if the benefit to the mother outweighs the risk of side effects in the fetus and child. The drug is available with a prescription. List B. The drug should be stored in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C. Shelf life - 3 years. Tenofovir disoproxil fumarate is a salt of fumaric acid and a bisisopropoxycarbonyloxymethyl ester, a derivative of tenofovir. In vivo it is converted to tenofovir, an analogue of the nucleoside monophosphate (nucleotide) adenosine monophosphate. Tenofovir is subsequently converted into an active metabolite - tenofovir diphosphate. Tenofovir is a nucleotide reverse transcriptase inhibitor, has specific activity yu in relation to the human immunodeficiency virus (HIV-1 and HIV-2) and hepatitis B virus. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases. In in vitro tests, tenofovir at concentrations up to 300 µmol/l had no effect on the synthesis of mitochondrial DNA and formation of lactic acid. When using tenofovir in vitro, antiviral activity was observed. In studies of the combined use of the drug with HIV protease inhibitors and with nucleoside and non-nucleoside analogues of HIV-1 reverse transcriptase inhibitors, additive or synergistic effects were noted. The antiviral activity of tenofovir against laboratory and clinical isolates of HIV-1 was assessed in lymphoblastoid cell lines, primary monocytes/macrophages, and peripheral blood lymphocytes. EC50 (half-maximal effective concentration) was 0.04 – 8.5 µmol. In cell culture, tenofovir showed antiviral activity against HIV-1 subtypes A, B, C, D, E, F, G, O (EC50 was in the range of 0.5 - 2.2 μmol), as well as an inhibitory effect on some strains HIV-2 (EC50 was in the range of 1.6 – 4.9 µmol). The antiviral activity of tenofovir against the hepatitis B virus was assessed on the HepG2 2.2.15 cell line. The effective concentration of tenofovir was in the range of 0.14 to 1.5 µmol with an effective cytotoxic concentration of >100 µmol. In cell cultures, studies of the antiviral activity of combinations of tenofovir with nucleoside Reverse transcriptase inhibitors acting on the hepatitis B virus (emtricitabine, entecavir, lamivudine and telbivudine) did not antagonize the activities of the drugs. In in vitro studies and in some patients infected with HIV-1, resistance to tenofovir was observed, the occurrence of which was caused by mutations (substitution type) M184V/I and K65R, respectively. No other mechanisms of resistance to tenofovir have been identified. No hepatitis B virus mutations associated with tenofovir resistance were identified. Following oral administration to HIV-infected patients, tenofovir disoproxil fumarate is rapidly absorbed and converted to tenofovir. Peak serum concentrations of tenofovir were observed one hour after dosing on an empty stomach and two hours after dosing with food; the bioavailability of tenofovir from tenofovir disoproxil fumarate after oral administration on an empty stomach was approximately 25%. When tenofovir disoproxil fumarate was administered with food, oral bioavailability was increased, with an increase in the area under the concentration-time curve and mean maximum concentration of tenofovir by approximately 40% and 14%. After the first dose of tenofovir disoproxil fumarate with food, the maximum serum concentration ranges from 213 to 375 mg/ml. The volume of distribution at steady state after intravenous administration of tenofovir was approximately 800 ml/kg. The binding of tenofovir disoproxil fumarate to human plasma proteins in vitro is less than 0.7% and 7.2% depending on the concentration of tenofovir from 0.01 to 25 μg/ ml. It has been proven that neither tenofovir disoproxil fumarate nor tenofovir inhibit human cytochrome P450 enzymes. Moreover, at concentrations significantly higher than therapeutic (more than 300 times), tenofovir does not affect metabolic processes involving other cytochrome P450 isoenzymes (cytochrome P3A4, P2D6, P2C9 , P2E1, etc.). Tenofovir disoproxil fumarate does not affect cytochrome P450 isoenzymes with the exception of PIA1/2, where small but statistically significant changes were observed (6%). Tenofovir is eliminated primarily through the kidneys via glomerular filtration and active tubular secretion. After a single oral dose, the half-life (T1/2) of tenofovir is approximately 17 hours. The pharmacokinetics of tenofovir does not depend on the dose of tenofovir disoproxil fumarate (with a dosing regimen of 75 to 600 mg), as well as in cases of repeated administration of the drug at different dosing regimens. Tenofovir disoproxil fumarate did not show significant carcinogenic activity in long-term studies in rats when administered orally. There was a low incidence of duodenal tumors in mice, which were considered likely to be related to high concentrations of tenofovir disoproxil fumarate in the gastrointestinal tract when administered at a relatively high dose of 600 mg/kg. Limited data on the pharmacokinetics of tenofovir in women indicate no significant sex differences. No pharmacokinetic studies have been conducted in children, adolescents under 18 years of age, or elderly people over 65 years of age. Specific pharmacokinetic studies have not been conducted in different ethnic groups. A drug Tenofovir-TL created for: – Treatment of HIV-1 infection in adults in combination therapy with other antiretroviral drugs. – Treatment of chronic viral hepatitis B in adults with compensated liver failure, signs of active viral replication, constant increased activity serum alanine aminotransferase (ALT), histological evidence of active inflammatory process and/or fibrosis. Tenofovir-TL take orally, during meals or with a small amount of food. Treatment of HIV-1 infection: adults 300 mg (1 tablet) per day. For the treatment of chronic hepatitis B: adults: 300 mg (1 tablet) per day. In HBeAg-positive patients without cirrhosis, treatment should be continued for at least 6-12 months after confirmation of HBe seroconversion (disappearance of HBeAg or disappearance of hepatitis B virus DNA with detection of anti-HBe), or until HBs seroconversion, and until loss of effectiveness. To identify any delayed virological relapses after the end of treatment, it is necessary to regularly measure the levels of ALT and hepatitis B virus DNA in the blood serum. In HBeAg-negative patients without cirrhosis, treatment should be continued at least until HBs seroconversion or loss of efficacy. For prolonged treatment beyond 2 years, it is recommended that the patient be regularly monitored to confirm that the drug selected for the individual patient treatment remains adequate. Select the dose with caution in elderly patients, given the high incidence of liver, kidney or cardiac dysfunction, as well as concomitant diseases or taking other medications. From the blood system and hematopoietic organs: frequency unknown - neutropenia, anemia. Metabolism: very often – hypophosphatemia; not often – hyperglycemia, hypokalemia, hyperkalemia. From the nervous system: very often - dizziness, headache, insomnia, depression. From the respiratory system: very rarely - shortness of breath. From the gastrointestinal tract (GIT): very often – diarrhea, vomiting, nausea; often - flatulence, increased amylase concentration, abdominal pain, bloating; rarely – pancreatitis, dyspepsia, increased lipase activity. From the liver and biliary tract: rarely - increased activity of liver transaminases (most often aspartate aminotransferase, alanine aminotransferase, gamma-glutamyl transpeptidase); very rarely - hepatic steatosis, hyperbilirubinemia, exacerbation of hepatitis both during treatment and after cessation. From the side of the track and popliteal tissue: very often - skin rash, sometimes accompanied by itching (maculopapular rash, urticaria, vesicular bullous, pustular rash); rarely - angioedema, change in skin color (mainly on the palms and/or soles of the feet). From the musculoskeletal system: uncommon – rhabdomyolysis, muscle weakness; rarely - osteomalacia (manifested by pain in the bones, occasionally leading to fractures), myopathy. From the urinary system: not often - increased creatinine levels; rarely - renal dysfunction, including acute renal failure, acute tubular necrosis; very rarely - renal tubulopathy of the proximal type, including Fanconi syndrome; frequency unknown - nephritis, including interstitial nephritis, nephrogenic diabetes insipidus, proteinuria, polyuria. Others: often - asthenia; not often – fatigue. The following non-adversarial reactions can occur with both mono and combination retroviral therapy. Renal failure - symptoms are similar to monotherapy. Metabolic disorders - hypertriglyceridemia, hypercholesterolemia, insulin resistance, hyperlactatemia, lipodystrophy, including loss of peripheral and facial subcutaneous fat, increase in intra-abdominal and visceral fat, mammary hypertrophy, dorsocervical obesity (buffalo hump). Immune reconstitution syndrome – may occur inflammatory reactions in response to asymptomatic or residual opportunistic infections such as cytomegalovirus retinitis, generalized and/or focal mycobacterial infection and pneumonia, autoimmune disorders such as Graves' disease, which may occur several months after the start of treatment. Osteonecrosis – Cases of osteonecrosis have been reported, especially in patients with risk factors or during long-term combination antiviral therapy. If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor. Contraindications to the use of the drug Tenofovir-TL are: – Hypersensitivity to tenofovir and any component of the drug. – Children under 18 years of age. – Patients with creatinine clearance less than 30 ml/min, as well as patients who require hemodialysis. – Lactase deficiency, lactose intolerance, glucose-lactose malabsorption, since the drug contains lactose. – Concomitant use with other drugs containing tenofovir; with didanosine, adefovir. – Renal failure with creatinine clearance greater than 30 ml/min and less than 50 ml/min. – Elderly people over 65 years of age. A drug Tenofovir-TL should be used during pregnancy only if the expected benefit from treatment for the mother outweighs the potential risk to the fetus. Breastfeeding is not recommended for HIV-infected mothers receiving therapy with Tenofovir-TL to prevent the risk of postnatal transmission of HIV. Women of childbearing age during During treatment, reliable methods of contraception should be used. Nursing HIV-infected mothers should be instructed not to breastfeed. A drug Tenofovir-TL should not be used concomitantly with drugs containing tenofovir. Didanosine. When taking tenofovir with didanosine simultaneously, the systemic exposure of didanosine increases by 40-60%, which increases the risk of side effects of didanosine (such as pancreatitis, lactic acidosis, including death). Co-administration of tenofovir and didanosine at a dose of 400 mg per day led to a decrease in the number of SP4 lymphocytes (probably due to intracellular interaction, didanosine phosphorylation increases). The combined use of tenofovir and didanosine is not recommended. Adefovir. Tenofovir should not be used concomitantly with adefovir, as in vitro studies have shown almost identical antiviral effect tenofovir and adefovir. Eitecavir. When tenofovir was co-administered with entecavir, no significant drug interactions were identified. Atazanavir/ritonavir. Atazanavir has shown the ability to increase the concentration of tenofovir. The mechanism of this interaction has not been established. It is necessary to carefully monitor the condition of patients who receive atazanavir together with tenofovir in case of adverse events associated with taking tenofovir. When co-administered with tenofovir, it is recommended to take atazanavir 300 mg together with ritonavir 100 mg. Trenofovir should not be taken concomitantly with atazanavir without ritonavir. In studies in healthy volunteers, no clinically significant interactions were observed when tenofovir was used concomitantly with abacavir, efavirenz, emtricitabine, lamivudine, indinavir, lopinavir/ritonavir, nelfinavir, oral contraceptives, ribavirin, saquinavir/ritonavir. Nephrotoxic drugs. Tenofovir is primarily eliminated from the body through the kidneys. Concomitant use of tenofovir with drugs that reduce renal function or reduce/cessate active tubular secretion may lead to increased serum concentrations of tenofovir and/or increased concentrations of other drugs eliminated by the kidney. Necessary Avoid use of tenofovir concomitantly or after recent treatment with nephrotoxic drugs such as aminoglycosides, amphotericin B, foscarnet, pentamidine, vancomycin, tacrolimus, cidofovir, or interleukin-2. Ganciclovir, valganciclovir and cidofovir compete with tenofovir for active tubular secretion by the kidneys, resulting in increased concentrations of tenofovir. Darunavir: increases the concentration of tenofovir by 20-25%. The drugs should be used in standard doses, and the nephrotoxic effect of tenofovir must be carefully monitored. Symptoms of drug overdose Tenofovir-TL: signs of toxicity, such phenomena as lactic acidosis: nausea, diarrhea, vomiting, abdominal pain; neurological symptoms: dizziness, headache, impaired consciousness. To avoid overdose, the patient should be under medical supervision. Treatment: There is no antidote for tenofovir, therefore, in intensive care conditions, standard supportive therapy is carried out until the general condition normalizes. To replenish the water and electrolyte balance, eliminate the symptoms of vomiting, detoxification therapy and normalize cardiac activity, you can use: trace elements, antiemetic drugs, parenteral nutrition drugs , adsorbents, drugs that stimulate cardiac activity, antiallergic drugs. If the above symptoms cannot be dealt with, the patient is referred for hemodialysis. Approximately 10% of a dose of tenofovir disoproxil fumarate is eliminated by hemodialysis. In a dry place, protected from light, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Tenofovir-TL – film-coated tablets, 300 mg. 10 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil. 30 or 60 tablets in a polymer jar (bottle) for medicines or a plastic jar (bottle) for medicines. The free space in the jar (bottle) is filled with medical absorbent cotton. Each jar (bottle), 3 or 6 blister packs, along with instructions for use, is placed in a box of cardboard. 1 tablet Tenofovir-TL contains the active ingredient: tenofovir disoproxil fumarate. 300.0 mg. Lactose monohydrate. 90.0 mg Corn starch. 150.0 mg Pregelatinized starch. 11.0 mg Microcrystalline cellulose. 80.0 mg Croscarmellose sodium. 60.0 mg Magnesium stearate. 7.0 mg Silicon dioxide colloidal. 2.0 mg Film shell Aquarius Prime blue [hypromellose – 62.5%, titanium dioxide – 23.62%, macrogol 3350 – 6%, medium chain triglycerides – 6.5%, indigo carmine dye aluminum varnish – 0.5%, brilliant blue dye aluminum varnish – 0.85%, quinoline yellow dye aluminum varnish – 0.03%]. 30.0 mg.Radar ranges
Designation
/ITUEtymology
Frequencies
Wavelength
Notes
HF
English high frequency
3-30 MHz
10-100 m
Coast Guard radars, “over-the-horizon” radars
P
English previous
< 300 МГц
> 1 m
Used in early radars
VHF
English very high frequency
50-330 MHz
0.9-6 m
Long range detection, Earth exploration
UHF
English ultra high frequency
300-1000 MHz
0.3-1 m
Detection at long ranges (for example, artillery shelling), exploration of forests, the Earth's surface
L
English Long
1-2 GHz
15-30 cm
air traffic surveillance and control
S
English Short
2-4 GHz
7.5-15 cm
air traffic control, meteorology, maritime radar
C
English Compromise
4-8 GHz
3.75-7.5 cm
meteorology, satellite broadcasting, intermediate range between X and S
X
8-12 GHz
2.5-3.75 cm
weapons control, missile guidance, maritime radar, weather, medium resolution mapping; in the USA, the 10.525 GHz ± 25 MHz band is used in airport radars
K u
English under K
12-18 GHz
1.67-2.5 cm
high resolution mapping, satellite altimetry
K
German kurz - “short”
18-27 GHz
1.11-1.67 cm
use is limited due to strong absorption by water vapor, so the K u and K a ranges are used. K-band is used for cloud detection, in police traffic radars (24.150 ± 0.100 GHz).
K a
English above K
27-40 GHz
0.75-1.11 cm
Mapping, short range air traffic control, special radars controlling traffic cameras (34.300 ± 0.100 GHz)
mm
40-300 GHz
1-7.5 mm
millimeter waves, divided into the following two ranges
V
40-75 GHz
4.0-7.5 mm
EHF medical devices used for physiotherapy
W
75-110 GHz
2.7-4.0 mm
sensors in experimental automated vehicles, high-precision weather research
Designations of frequency ranges adopted by the US Armed Forces and NATO since.
Designation
Frequencies, MHz
Wavelength, cm
Examples
A
< 100-250
120 - >300
Early warning and air traffic control radars, e.g. Radar 1Л13 “NEBO-SV”
B
250 - 500
60 - 120
C
500 −1 000
30 - 60
D
1 000 - 2 000
15 - 30
E
2 000 - 3 000
10 - 15
F
3 000 - 4 000
7.5 - 10
G
4 000 - 6 000
5 - 7.5
H
6 000 - 8 000
3.75 - 5.00
I
8 000 - 10 000
3.00 - 3.75
Airborne multifunctional radars (BRLS)
J
10 000 - 20 000
1.50 - 3.00
Target guidance and illumination radar (RPN), e.g. 30N6, 9S32
K
20 000 - 40 000
0.75 - 1.50
L
40 000 - 60 000
0.50 - 0.75
M
60 000-100 000
0.30 - 0.50
see also
Radar station on Wikimedia Commons
Radar station in Wikinews
Notes
The bearing to an object is determined by the direction of a narrow radar beam, which is currently falling on the object and is reflected from it.
The distance to the object can be obtained by measuring short time intervals between the sending of the probing pulse and the moment of receiving the reflected pulse, provided that the radio pulses propagate at a speed c = 3 X 108 m/sec. Ship radars have all-round indicators (PSI), on the screen of which an image of the navigation environment surrounding the ship is formed.
Coastal radars installed in ports, on their approaches and on canals or on complex fairways are widely used. With their help, it became possible to bring ships into the port, control the movement of ships along the fairway, channel in conditions of poor visibility, as a result of which the downtime of ships is significantly reduced. These stations in some ports are supplemented with special television transmitting equipment, which transmits images from the screen of the radar station to ships approaching the port. The transmitted images are received on the ship by a conventional television receiver, which greatly facilitates the task of entering the ship into port in poor visibility for the navigator.
Coastal (port) radars can also be used by the port dispatcher to monitor the movement of ships located in the port waters or on the approaches to it.
Let's consider the principle of operation of a ship's radar with an all-round visibility indicator. Let's use a simplified block diagram of a radar to explain its operation (Fig. 1).
The triggering pulse generated by the SI generator launches (synchronizes) all radar units.
When triggering pulses arrive at the transmitter, the modulator (Mod) generates a rectangular pulse with a duration of several tenths of microseconds, which is fed to the magnetron generator (MG).
The reflected signals are received by the same antenna, so the AP alternately connects the antenna first to the transmitter and then to the receiver. The reflected pulse is fed through an antenna switch to a mixer to which a klystron oscillator (KG) is connected. The latter generates low-power oscillations with a frequency f Г=946 0 MHz.
In the mixer, as a result of the addition of oscillations, an intermediate frequency fPR=fГ-fС=60 MHz is released, which then goes to an intermediate frequency amplifier (IFA), which amplifies the reflected pulses. Using a detector located at the output of the amplifier, the amplified pulses are converted into video pulses, which are fed through a video mixer (VS) to a video amplifier. Here they are amplified and sent to the cathode of a cathode ray tube (CRT).
A cathode ray tube is a specially designed vacuum tube (see Fig. 1).
It consists of three main parts: an electron gun with a focusing device, a deflecting magnetic system and a glass bulb with a screen that has an afterglow property.
The electron gun 1-2 and the focusing device 4 form a dense, well-focused beam of electrons, and the deflection system 5 serves to control this electron beam.
After passing through the deflection system, the electron beam hits screen 8, which is coated with a special substance that has the ability to glow when bombarded with electrons. The inner side of the wide part of the tube is coated with a special conductive layer (graphite). This layer is the main anode of the tube 7 and has a contact to which a high positive voltage is applied. Anode 3 is an accelerating electrode.
The brightness of the luminous point on the CRT screen is regulated by changing the negative voltage on control electrode 2 using the “Brightness” potentiometer. In the normal state, the tube is locked with negative voltage at control electrode 2.
The image of the surrounding environment on the screen of the all-round visibility indicator is obtained as follows.
Simultaneously with the start of radiation by the probe pulse transmitter, a sweep generator is started, consisting of a multivibrator (MB) and a sawtooth current generator (RCG), which generates sawtooth pulses. These pulses are fed to the deflecting system 5, which has a rotation mechanism that is connected to the receiving synchronizer 6.
At the same time, a rectangular positive voltage pulse is applied to control electrode 2 and unlocks it. With the appearance of an increasing (sawtooth) current in the CRT deflection system, the electron beam begins to smoothly deviate from the center to the edge of the tube and a luminous scanning radius appears on the screen. The radial movement of the beam across the screen is very faintly visible. At the moment the reflected signal arrives, the potential between the grid and the control cathode increases, the tube is unlocked and a point corresponding to the current position of the beam performing radial movement begins to glow on the screen. The distance from the center of the screen to the luminous point will be proportional to the distance to the object. The deflection system has a rotational movement.
The rotation mechanism of the deflection system is connected by synchronous transmission to the synchronous sensor of the antenna 9, so the deflection coil rotates around the neck of the CRT synchronously and in phase with the antenna 12. As a result, a rotating scan radius appears on the CRT screen.
When the antenna is rotated, the scan line rotates and new areas begin to light up on the indicator screen, corresponding to pulses reflected from various objects located at different bearings. Behind full turn antenna, the entire surface of the CRT screen is covered with many radial scan lines, which are illuminated only if there are reflective objects on the corresponding bearings. Thus, a complete picture of the situation surrounding the ship is reproduced on the tube screen.
For approximate measurement of distances to various objects, scale rings (fixed range circles) are applied on the CRT screen using electronic illumination generated in the PCD unit. To more accurately measure distance, the radar uses a special rangefinder device with a so-called moving range circle (MRC).
To measure the distance to any target on the CRT screen, it is necessary to rotate the rangefinder handle, align the PCD with the target mark and take a reading in miles and tenths from a counter mechanically connected to the rangefinder handle.
In addition to echo signals and distance rings, heading mark 10 is illuminated on the CRT screen (see Fig. 1). This is achieved by applying a positive pulse to the CRT control grid at the moment when the maximum radiation from the antenna passes in a direction coinciding with the centerline plane of the vessel.
The image on the CRT screen can be oriented relative to the ship's DP (heading stabilization) or relative to the true meridian (north stabilization). In the latter case, the deflection system of the tube also has a synchronous connection with the gyrocompass.
Rp.: Tab. Bisoprololi 0.005 No. 20
D.S. 1 tab. per day (AH, IHD)Registration number:
1 film-coated tablet contains:
active substance: bisoprolol fumarate 5.00 or 10.00 mg;
excipients: microcrystalline cellulose, mannitol, croscarmellose sodium, magnesium stearate;
shell: hypromellose, titanium dioxide, macrogol-6000.
The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the sympathoadrenal system (SAS) (of great importance for patients with initial renin hypersecretion), restoration of sensitivity in response to a decrease in blood pressure (BP) and an effect on the central nervous system (CNS). In case of arterial hypertension, the effect develops after 2-5 days, a stable effect is observed after 1-2 months.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of decreased contractility and other myocardial functions, prolongation of diastole, and improved myocardial perfusion. Due to increased end-diastolic pressure in the left ventricle and increased stretch of ventricular muscle fibers, oxygen demand may increase, especially in patients with chronic heart failure (CHF).
When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism; does not cause sodium ion retention in the body; the severity of the atherogenic effect does not differ from the effect of propranolol.
Communication with blood plasma proteins is about 30%. Volume of distribution - 3.5 l/kg. Total ground clearance is approximately 15 l/h. The maximum concentration in blood plasma is determined after 2-3 hours. Permeability through the blood-brain barrier and placental barrier is low.
The plasma half-life (10-12 hours) ensures effectiveness for up to 24 hours after a single daily dose.
Bisoprolol is excreted from the body in two ways; 50% of the dose is metabolized in the liver with the formation of inactive metabolites. About 98% is excreted by the kidneys, of which 50% is excreted unchanged; less than 2% - through the intestines (with bile).
Since elimination occurs equally in the kidneys and liver, no dosage adjustment is required in patients with impaired liver function or renal failure. The pharmacokinetics of bisoprolol is linear and does not depend on age.
In patients with CHF, plasma concentrations of bisoprolol are higher and the half-life is longer compared to healthy volunteers.
Psoriasis, depression (including history), diabetes mellitus (may mask symptoms of hypoglycemia), allergic reactions (history), bronchospasm (history), desensitization therapy, Prinzmetal's angina, 1st degree AV block, severe renal dysfunction (creatinine clearance (CC) less than 20 ml/min); severe liver dysfunction; thyrotoxicosis, old age.
The drug Bisoprolol-Teva is taken orally, in the morning on an empty stomach, 1 time per day with a small amount of liquid, in the morning before, during or after breakfast. The tablets should not be chewed or crushed into powder.
In all cases, the doctor selects the dosage regimen and dose individually for each patient, in particular, taking into account the heart rate and condition of the patient. For arterial hypertension and coronary heart disease, the drug is prescribed 5 mg 1 time per day. If necessary, the dose is increased to 10 mg 1 time per day. In the treatment of arterial hypertension and angina pectoris, the maximum daily dose is 20 mg 1 time / day.
For patients with severely impaired renal function (creatinine clearance less than 20 ml/min.) or with severely impaired liver function, the maximum daily dose is 10 mg 1 time per day. Increasing the dose in such patients must be carried out with extreme caution. No dose adjustment is required in elderly patients.
The frequency of adverse reactions listed below was determined according to the following (World Health Organization classification): very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages.
From the heart and blood vessels: very often - decrease in heart rate (bradycardia, especially in patients with CHF); sensation of heartbeat, often - a pronounced decrease in blood pressure (especially in patients with CHF), manifestation of vasospasm (increased peripheral circulatory disorders, a feeling of cold in the extremities (paresthesia); infrequently - impaired AV conduction (up to the development of complete transverse block and cardiac arrest), arrhythmias , orthostatic hypotension, worsening CHF with the development of peripheral edema (swelling of the ankles, feet; shortness of breath), chest pain.
From the nervous system: often - dizziness, headache, asthenia, increased fatigue, sleep disturbances, depression, anxiety; rarely - confusion or short-term memory loss, nightmares, hallucinations, myasthenia gravis, tremors, muscle cramps. Typically, these phenomena are mild in nature and usually disappear within 1-2 weeks after the start of treatment.
From the senses: rarely - blurred vision, decreased lacrimation (should be taken into account when wearing contact lenses), tinnitus, hearing loss, ear pain; very rarely - dry and sore eyes, conjunctivitis, taste disturbances.
From the respiratory system: infrequently - bronchospasm in patients with bronchial asthma or obstructive airway diseases; rarely - allergic rhinitis; nasal congestion.
From the digestive system: often - nausea, vomiting, diarrhea, constipation, dry oral mucosa, abdominal pain; rarely - hepatitis, increased activity of liver enzymes (alanine aminotransferase, aspartate aminotransferase), increased bilirubin concentration, change in taste.
From the musculoskeletal system: infrequently - arthralgia, back pain.
From the genitourinary system: very rarely - impaired potency, weakened libido.
Laboratory indicators: rarely - increased concentration of triglycerides in the blood; in some cases - thrombocytopenia, agranulocytosis, leukopenia.
Allergic reactions: rarely - itching, rash, urticaria
From the outside skin: rarely - increased sweating, skin hyperemia, exanthema, psoriasis-like skin reactions; very rarely - alopecia; beta-blockers can aggravate the course of psoriasis.
Other: withdrawal syndrome (increased frequency of angina attacks, increased blood pressure).
Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV block, marked decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.
Treatment: if an overdose occurs, first of all you need to stop taking the drug, perform gastric lavage, prescribe adsorbents, and carry out symptomatic therapy.
For severe bradycardia, intravenous atropine is administered. If the effect is insufficient, a drug with a positive chronotropic effect can be administered with caution. Sometimes temporary placement of an artificial pacemaker may be necessary.
With a pronounced decrease in blood pressure, intravenous administration of plasma-substituting solutions and vasopressors.
For hypoglycemia, intravenous glucagon or intravenous dextrose (glucose) may be indicated.
For AV block: Patients should be closely monitored and treated with beta-agonists such as epinephrine. If necessary, install an artificial pacemaker.
In case of exacerbation of CHF, intravenous administration of diuretics, drugs with positive inotropic effects, as well as vasodilators. For bronchospasm, prescribe bronchodilators, including beta2-adrenergic agonists and/or aminophylline.
The effectiveness and tolerability of drugs may be affected by concomitant use of other drugs. This interaction can also occur when two drugs are taken within a short period of time. The doctor must be informed about the use of other medications, even if used without a prescription.
Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.
Class III antiarrhythmic drugs (eg, amiodarone) may worsen AV conduction disturbances.
The effect of beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).
Parasympathomimetics, when used simultaneously with bisoprolol, may increase AV conduction disturbances and increase the risk of developing bradycardia. The simultaneous use of Bisoprolol-Teva with beta-agonists (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs.
The combination of bisoprolol with adrenergic agonists that affect beta and alpha adrenergic receptors (for example, norepinephrine, epinephrine) may enhance the vasoconstrictor effects of these drugs that occur with the participation of alpha adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers. Mefloquine, when used simultaneously with bisoprolol, may increase the risk of bradycardia.
Allergens used for immunotherapy or allergen extracts for skin testing increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol. Iodine-containing radiopaque diagnostic agents for intravenous administration increase the risk of developing anaphylactic reactions. Phenytoin, when administered intravenously, and agents for inhalation anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure.
The effectiveness of insulin and hypoglycemic agents for oral administration may change during treatment with bisoprolol (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).
The clearance of lidocaine and xanthines (except theophylline) may be reduced due to a possible increase in their concentration in the blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking. The hypotensive effect is weakened by non-steroidal anti-inflammatory drugs (NSAIDs) (sodium ion retention and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids and estrogens (sodium ion retention). Cardiac glycosides, methyldopa, reserpine and guanfacine, “slow” blockers calcium channels(verapamil, diltiazem), amiodarone and others antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV block, cardiac arrest and heart failure. Nifedipine can lead to a significant decrease in blood pressure. Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol. Tricyclic and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase depression of the central nervous system.
Concomitant use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. The treatment break between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Ergotamine increases the risk of developing peripheral circulatory disorders. Sulfasalazine increases the concentration of bisoprolol in the blood plasma. Rifampin shortens the half-life of bisoprolol.
Monitoring the condition of patients taking the drug Bisoprolol-Teva should include measuring heart rate and blood pressure, conducting an ECG, and determining blood glucose concentrations in patients with diabetes mellitus (once every 4-5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months).
The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.
Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a burdened bronchopulmonary history.
Patients who use contact lenses should take into account that during treatment with the drug, the production of tear fluid may decrease.
When using the drug Bisoprolol-Teva in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective blockade of alpha-adrenergic receptors is not previously achieved).
In thyrotoxicosis, bisoprolol can mask certain Clinical signs thyrotoxicosis (for example, tachycardia). Abrupt withdrawal of the drug in patients with thyrotoxicosis is contraindicated, as it can increase symptoms.
In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal values.
When using clonidine simultaneously, its use can be discontinued only a few days after discontinuation of the drug Bisoprolol-Teva. There may be an increase in the severity of the hypersensitivity reaction and no effect from usual doses epinephrine against the background of a burdened allergic history.
If it is necessary to carry out a planned surgical treatment the drug should be discontinued 48 hours before general anesthesia. If the patient took the drug before surgical intervention, he should choose a drug for general anesthesia with minimal negative inotropic effect.
Reciprocal activation vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that deplete catecholamine stores (including reserpine) may enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a significant decrease in blood pressure or bradycardia.
Patients with bronchospastic diseases may be prescribed cardioselective beta-blockers with caution in case of intolerance and/or ineffectiveness of other antihypertensive drugs. While taking beta-blockers in patients with concomitant bronchial asthma, airway resistance may increase. If the dose of Bisoprolol-Teva is exceeded in such patients, there is a risk of developing bronchospasm. If increasing bradycardia (heart rate less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure less than 100 mm Hg), or AV block is detected in patients, it is necessary to reduce the dose or stop treatment. It is recommended to discontinue therapy with Bisoprolol-Teva if depression develops.
Treatment should not be abruptly interrupted due to the risk of developing severe arrhythmias and myocardial infarction. The drug is discontinued gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days).
The drug should be discontinued before testing the concentrations of catecholamines, normetanephrine, vanillinmandelic acid, and antinuclear antibody titers in the blood and urine.
Film-coated tablets 5 mg and 10 mg 10 tablets in a PVC / aluminum blister. 3 or 5 blisters along with instructions for use in a cardboard box.
At a temperature not exceeding 25° C. Keep out of the reach of children.
2 years.
Do not use after the expiration date stated on the package.
On prescription.
Teva Pharmaceutical Enterprises Ltd., IsraelInstructions for use, contraindications, composition, price, photo
It is prohibited to use site materials without consulting a specialist.
30 pcs. - dark glass jars (1) - cardboard packs.
30 pcs. - polymer jars (1) - cardboard packs.
30 pcs. - polymer bottles (1) - cardboard packs.