Penicillin is one of the main representatives of the group of antibiotics, the drug has a wide range of bacteriostatic and bactericidal action (of penicillin preparations, benzylpenicillin is the most active).

Indications and dosage:

The use of penicillin is indicated:

• With sepsis (especially streptococcal)
• In all sulfanilamide-resistant cases of relevant infections (pneumococcal, gonococcal, meningococcal infection and etc.)
• With extensive and deeply localized infectious processes(osteomyelitis, severe phlegmon, gas gangrene)
• After injuries with involvement in the process and infection of large musculoskeletal arrays
• In the postoperative period for the prevention of purulent complications
• For infected third and fourth degree burns
• For soft tissue injuries
• For chest injuries
• With purulent meningitis
• For brain abscesses
• With erysipelas
• With gonorrhea and its sulfanilamide-resistant forms
• With syphilis
• With severe furunculosis
• With sycosis
• With various inflammations of the eye and ear

In the clinic of internal diseases, Penicillin is used to treat lobar pneumonia(together with sulfanilamide drugs), focal pneumonia, acute sepsis, cholecystitis and cholangitis, protracted septic endocarditis, as well as for the prevention and treatment of rheumatism.

In children Penicillin is used: for umbilical sepsis, septicopyemia and septic-toxic diseases of newborns, pneumonia in newborns and infants and young children, otitis media in infants and young children, septic form of scarlet fever, septic-toxic form of diphtheria (necessarily in combination with a special serum ), pleuropulmonary processes that are not amenable to the action of sulfanilamide drugs, purulent pleurisy and purulent meningitis, with gonorrhea.

The antimicrobial effect of Penicillin is achieved both with resorptive and with its local action.

Penicillin preparations can be administered intramuscularly, subcutaneously and intravenously, into cavities, into the spinal canal, by inhalation, sublingually (under the tongue), inside; locally - in the form of eye and nasal drops, rinses, washes.

When administered intramuscularly, penicillin is rapidly absorbed into the blood, but after 3-4 hours, penicillin almost completely disappears from it. For the effectiveness of therapy in 1 ml of blood should be 0.1-0.3 IU of penicillin, therefore, to maintain the therapeutic concentration of the drug in the blood, it should be administered every 3-4 hours.

The use of Penicillin for the treatment of gonorrhea, syphilis, pneumonia, cerebrospinal meningitis is carried out according to special instructions.

Overdose:

Not described.

Side effects:

Treatment with benzylpenicillins, bicillins and other penicillin-containing drugs may be accompanied by side effects, most often of an allergic nature.

The occurrence of allergic reactions to penicillin preparations is usually associated with sensitization of the body to them as a result of the previous use of these drugs, as well as as a result of their long-term exposure: professional sensitization of nurses, people working in the production of antibiotics.

Less commonly, allergic reactions are observed upon first contact with penicillin. They occur predominantly in people with allergic diseases(urticaria, bronchial asthma). Allergic reactions to penicillin from the skin are expressed in erythema, limited or widespread rashes, urticaria and urticaria-like rashes, macular, vesicular, pustular rashes, sometimes life threatening exfoliative dermatitis. Numerous cases have been reported contact dermatitis (medical staff medical institutions).

Contact dermatitis and reactions from the skin and mucous membranes are observed both with general exposure and with topical application Penicillin in the form of ointments, lotions, drops for the nose and eyes.

• On the part of the respiratory organs, rhinitis, pharyngitis, laryngopharyngitis, asthmatic bronchitis, bronchial asthma are noted.
• From the side gastrointestinal tract allergic reactions are expressed in stomatitis, nausea, vomiting, diarrhea.

In some cases, the distinction between toxic and allergic genesis of side effects is difficult. The allergic origin of these phenomena is indicated by their combination with skin rashes, under the influence of penicillin, the development of agranulocytosis is also possible.

If allergic reactions occur on the skin, respiratory tract, gastrointestinal tract, treatment with penicillin should be stopped or its dose reduced, the patient should be prescribed Diphenhydramine, Pipolfen, Suprastin, calcium chloride, vitamin B1.

It should be remembered about the possibility of sensitization of the body even in the prenatal period during the treatment of pregnant women with penicillin preparations.

Contraindications:

The use of penicillin is contraindicated in:

• stock hypersensitivity to penicillin
• Bronchial asthma
• Urticaria
• Hay fever and other allergic diseases
• Hypersensitivity of patients to antibiotics, sulfonamides and other drugs

Possible sensitization of the body to penicillin during fetal development in the treatment of pregnant women with its antibiotics, penicillin preparations.

Interaction with other drugs and alcohol:

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Care must be taken when combining penicillins active against Pseudomonas aeruginosa with anticoagulants and antiplatelet agents (potential risk of increased bleeding). It is not recommended to combine penicillins with thrombolytics. When combined with sulfonamides, the bactericidal effect may be weakened. Oral penicillins may reduce the effectiveness of oral contraceptives due to impaired enterohepatic estrogen circulation. Penicillins can slow down the excretion of methotrexate from the body (inhibit its tubular secretion). The combination of ampicillin with allopurinol increases the likelihood of a skin rash. The use of high doses of the potassium salt of benzylpenicillin in combination with potassium-sparing diuretics, potassium preparations or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.

Drinking alcohol during treatment with penicillin preparations is strictly contraindicated.

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Penicillin instructions for use, analogues, contraindications, composition and prices in pharmacies

Shelf life of penicillin: The shelf life of penicillin is 5 years.

Storage conditions of the drug: Store at a temperature not exceeding 25 degrees, in a dry place.

Terms of dispensing from pharmacies: By prescription

Composition, form of release, Pharmacological action of penicillin

Ingredients of Penicillin

The composition of drugs that are related to antibiotics groups penicillins depends on which drug is being discussed.

Currently, four groups are used:

• natural penicillins;
• semi-synthetic penicillins;
• aminopenicillins, which have an extended spectrum of action;
• penicillins with a wide antibacterial spectrum of influence.

Release form of penicillin

Injectable preparations are produced, as well as penicillin tablets.

Means for injections are produced in glass bottles, which are closed with rubber stoppers and metal caps. The vials contain different doses of penicillin. It is dissolved before administration.

Penicillin-ecmolin tablets are also produced, intended for resorption and for oral administration. Sucking tablets contain 5000 units of penicillin. In tablets for oral administration - 50,000 units.

Tablets of penicillin with sodium citrate may contain 50,000 and 100,000 units.

Pharmacological action of penicillin

Penicillin is the first antimicrobial agent that has been obtained using the waste products of microorganisms as the basis. The history of this drug begins in 1928, when Alexander Fleming, the inventor of the antibiotic, isolated it from a strain of the fungus Penicillium notatum. In the chapter that describes the history of the discovery of penicillin, Wikipedia indicates that the antibiotic was discovered by accident, after entering the culture of bacteria from external environment mold fungus, its bactericidal effect was noted. Later, the formula of penicillin was determined, and other specialists began to study how to get penicillin. However, the answer to the questions, in what year this remedy was invented, and who invented the antibiotic, is unequivocal.

The further description of penicillin on Wikipedia testifies to who created and improved the drugs. In the forties of the twentieth century, scientists in the USA and Great Britain worked on the process of producing penicillin in industry. For the first time the use of this antibacterial drug for the purpose of therapy bacterial infections happened in 1941. And in 1945, for the invention of penicillin, the Nobel Prize was awarded to its creator Fleming (the one who invented penicillin), as well as scientists who worked on its further improvement - Flory and Chain.

Speaking about who discovered penicillin in Russia, it should be noted that the first samples of the antibiotic were obtained in the Soviet Union in 1942 by microbiologists Balezina and Yermolyeva. Further, the industrial production of the antibiotic began in the country. In the late fifties, synthetic penicillins appeared.

When this medicine was invented, for a long time it remained the main antibiotic used clinically throughout the world. And even after other antibiotics without penicillin were invented, this antibiotic remained important drug for the treatment of infectious diseases. There is a claim that the medicine is obtained with the help of cap mushrooms, but today there is different methods its production. Currently, the so-called protected penicillins are widely used.

The chemical composition of penicillin indicates that the agent is an acid, from which various salts are subsequently obtained. To penicillin antibiotics include Phenoxymethylpenicillin (penicillin V), Benzylpenicillin (penicillin G), etc. The classification of penicillins involves their division into natural and semi-synthetic.

Biosynthetic penicillins provide a bactericidal and bacteriostatic effect by inhibiting the synthesis of the cell wall of microorganisms. They act on some gram-positive bacteria (Streptococcus spp., Staphylococcus spp., Bacillus anthracis, Corynebacterium diphtheria), some gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae), anaerobic spore-forming bacilli (Spirochaetaceae Actinomyces spp.), etc.

The most active of penicillin preparations is Benzylpenicillin. Resistance to the influence of benzylpenicillin is demonstrated by strains of Staphylococcus spp., which produce penicillinase.

Penicillin is not effective tool in relation to bacteria of the enteric-typhoid-dysenteric group, pathogens of tularemia, brucellosis, plague, cholera, as well as pertussis, tuberculosis, Friedlander, Pseudomonas aeruginosa and viruses, rickettsiae, fungi, protozoa.

Indications for the use of penicillin

Indications for the use of penicillin are:

Antibiotics of the penicillin group, the names of which will be prompted directly by the attending physician, are used to treat diseases provoked by microorganisms sensitive to penicillin:

• pneumonia (croupous and focal);
• pleural empyema;
• septic endocarditis in acute and subacute form;
• sepsis;
• pyemia;
• septicemia;
• osteomyelitis in acute and chronic form;
• meningitis;
• infectious diseases biliary and urinary tract;
• purulent infectious diseases of the skin, mucous membranes, soft tissues;
• angina;
• scarlet fever;
• erysipelas;
• anthrax;
• actinomycosis;
• diphtheria;
• gynecological purulent-inflammatory diseases;
• ENT diseases;
• eye diseases;
• gonorrhea, syphilis, blennorrhea.

Contraindications to the use of penicillin

Contraindications to the use of the drug penicillin are:

Tablets and injections are not used in such cases:

• with high sensitivity to this antibiotic;
• with urticaria, hay fever, bronchial asthma and other allergic manifestations;
• with the manifestation in patients of high sensitivity to sulfonamides, antibiotics, as well as to other drugs.

penicillin - instructions for use

Antimicrobial action is observed with local and resorptive action of penicillin.

Instructions for the use of penicillin in injections

The drug can be administered subcutaneously, intramuscularly, intravenously. Also, the drug is injected into the spinal canal. In order for the therapy to be as effective as possible, it is necessary to calculate the dose so that 0.1–0.3 IU of penicillin is in 1 ml of blood. Therefore, the drug is administered every 3-4 hours.

For the treatment of pneumonia, syphilis, cerebrospinal meningitis, etc., a doctor prescribes a special scheme.

Instructions for use of penicillin tablets

The dosage of penicillin tablets depends on the disease and on the treatment regimen prescribed by the attending physician. As a rule, patients are prescribed 250-500 mg, the drug should be taken every 8 hours. If necessary, the dose is increased to 750 mg. It is recommended to take the tablets half an hour before a meal or two hours after a meal. The duration of treatment depends on the disease.

Side effects

In the process of application, the patient must understand what penicillin is, and what side effects he can provoke. In the course of treatment, allergy symptoms sometimes appear. As a rule, such manifestations are associated with sensitization of the body due to more early application these drugs. Also, allergies can occur due to prolonged use of the drug. At the first use of the drug, allergies are less common. There is a possibility of fetal sensitization during pregnancy if a woman takes penicillin.

Also, during the course of treatment, the following may develop: side effects:

• Digestive system: nausea, diarrhea, vomiting.
• Central nervous system: neurotoxic reactions, signs of meningism, coma, convulsions.
• Allergy: urticaria, fever, rash on the mucous membranes and on the skin, eosinophilia, edema. Cases recorded anaphylactic shock and fatal outcome. With such manifestations, adrenaline should be administered intravenously immediately.
• Manifestations associated with chemotherapeutic influence: oral candidiasis, vaginal candidiasis.

penicillin - analogues of the drug

Analogues of the drug penicillin are:

penicillin with alcohol

penicillin during pregnancy and lactation

No data

penicillin for children

It is used to treat children only after a doctor's prescription and under his supervision.

special instructions

Before using penicillin, it is important to conduct tests and determine the sensitivity to the antibiotic.

Carefully prescribe the drug to people who have impaired renal function, as well as patients with acute heart failure, people who have a tendency to allergic manifestations or severe sensitivity to cephalosporins.

If after 3-5 days after the start of treatment there is no improvement in the patient's condition, it is important to consult a doctor who will prescribe other antibiotics or combined treatment.

Since there is a high likelihood of fungal superinfection during antibiotic use, it is important to take antifungal agents during treatment. It is also important to consider that with the use of subtherapeutic doses of the drug or with an incomplete course of therapy, resistant strains of pathogens may appear.

When taking the drug inside, you need to drink it with plenty of liquid. It is important to strictly follow the instructions on how to dilute the product.

In the process of treatment with penicillins, it is necessary to follow the prescribed treatment regimen very precisely and not to skip doses. If a dose is missed, the dose should be taken as soon as possible. You can not interrupt the course of treatment.

Since the medicine expired storage may be toxic, it should not be taken.

The active ingredients are listed in alphabetical order.

Preparations containing Ampicillin (Ampicillin, ATC code (ATC) J01CA01)
Name	Release form	Packing, pcs	Producing country	Price in Moscow, r	Offers in Moscow
Ampicillin (Ampicillin)		1	Russia, Biochemist	9-(middle 11)-24	210↘
Ampicillin (Ampicillin)	tablets 250mg	20	Russia, various	7-(middle 10)-52	106↘
Ampicillin-AKOS	powder for injections 1g in vial	1	Russia, AKOS	9-(medium 11)-15	219↗
Ampicillin sodium salt		1	Various	5-(medium 6)-21	250
Ampicillin trihydrate	tablets 250mg	10, 20, 24 and 40	Various	7-(medium 22)-58	108↘
Ampicillin trihydrate	capsules 250mg	10, 20, 24	Russia, various	6-(medium 10)-60	505↗
Ampicillin (Ampicillin)	powder for injection 500mg in vial	1	Russia, various	6-(medium 7)-10	74↗
Ampicillin-AKOS	tablets 250mg	24	Russia, Synthesis	12-(medium 13)-25	28↘
Ampicillin-AKOS	tablets 500mg	24	Russia, Synthesis	7-(medium 10)-12	14↘
Zetsil (Zetsyl)	powder for injection 500mg in vial	1	India, Aurobil	No	No
Standacillin (Standacillin)	capsules 500mg	12	Austria, Biochemi	No	No
Upsampi	powder for oral administration 250mg/5ml 60ml	1	Italy, BMS	No	No
Preparations containing a combination of Ampicillin + Oxacillin
Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packing, pcs	Producing country	Price in Moscow, r	Offers in Moscow
Oksamp (Oxamp)	capsules 250mg	20	Russia, Synthesis	32- (average 58↗) -90	92↘
Rare and discontinued forms of release (less than 100 offers in Moscow pharmacies)
Ampiox (Ampiox)	capsules 250mg	20	Russia, Bryntsalov	No	No
Ampiox sodium	powder for injection 500mg	5 and 10	Russia, Bryntsalov	No	No
Oxamp sodium	powder for injection 500mg	1	Russia, various	No	No
Preparations containing Benzylpenicillin (Benzylpenicillin, ATC code (ATC) J01CE01)
Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packing, pcs	Producing country	Price in Moscow, r	Offers in Moscow
Benzyl penicillin sodium salt	powder for injection 1 million units	1	Russia, various	4-(medium 6)-15	250↘
Preparations containing Benzathine Benzylpenicillin (Benzathine Benzylpenicillin, ATC code (ATC) J01CE08)
Rare forms of release (less than 100 offers in Moscow pharmacies)
Bicillin-1	powder for injections 600 thousand and 1 million 200 thousand units	1	Russia, Synthesis	7-(medium 8)-12	9↘
Retarpen	powder for injections 2 million 400 thousand units	1	Austria, Biochemi	950	1↘
Extencillin (Extencillin)		1	France, Rhone Poulenc	No	No
Extencillin (Extencillin)		1	France, Rhone Poulenc	No	No
Preparations containing benzylpenicillin and benzathine benzylpenicillin (benzathine benzylpenicillin + benzylpenicillin, ATC code J01CE30)
Common forms of release (more than 100 offers in Moscow pharmacies)
Bicillin-3	powder for injections 600 thousand units	1	Russia, Synthesis	1-(medium 8)-25	402↗
Bicillin-5	powder for injection 1 million 500 thousand (1 million 200 thousand + 300 thousand) units	1	Russia, Synthesis	5-(medium 13)-20	197↘
Bicillin-3	powder for injections 1 million 200 thousand units	1	Russia, Synthesis	6-(medium 12)-22	77↗
Rare forms of release of drugs containing Phenoxymethylpenicillin (Phenoxymethylpenicillin, code (ATC) J01CE02)
Rare forms of release (less than 100 offers in Moscow pharmacies
Name	Release form	Packing, pcs	Producing country	Price in Moscow, r	Offers in Moscow
Phenoxymethyl penicillin	tablets 250mg	10	Russia, Synthesis	13-(middle 17)-31	75↗

Ampicillin - instructions for use. Prescription drug, information intended for healthcare professionals only!

Clinico-pharmacological group:

Antibiotic of the penicillin group a wide range action, destroyed by penicillinase.

pharmachologic effect

An antibiotic of the group of semi-synthetic penicillins with a wide spectrum of action. It has a bactericidal effect by inhibiting the synthesis of the bacterial cell wall.

Active against gram-positive aerobic bacteria: Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp. (including Enterococcus spp.), Listeria monocytogenes; gram-negative aerobic bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Bordetella pertussis, some strains of Haemophilus influenzae.

Destroyed by penicillinase. Acid resistant.

Pharmacokinetics

Suction

After oral administration, it is well absorbed from the gastrointestinal tract, without being destroyed in the acidic environment of the stomach. After parenteral administration (in / m and / in) is found in plasma in high concentrations.

Distribution

It penetrates well into tissues and biological fluids of the body, is found in therapeutic concentrations in pleural, peritoneal and synovial fluids. Penetrates through the placental barrier. Poorly penetrates the blood-brain barrier, however, with inflammation of the membranes of the brain, the permeability of the BBB increases dramatically.

Metabolism

30% of ampicillin is metabolized in the liver.

breeding

T1 / 2 - 1-1.5 hours. It is excreted mainly in the urine, and very high concentrations of unchanged drug are created in the urine. Partially excreted in bile.

With repeated injections does not accumulate.

Indications for use of the drug AMPICILLIN

Infectious and inflammatory diseases caused by microorganisms sensitive to ampicillin, including:

• respiratory infections (including bronchitis, pneumonia, lung abscess);
• infections of ENT organs (including tonsillitis);
• biliary tract infections (including cholecystitis, cholangitis);
• urinary tract infections (including pyelitis, pyelonephritis, cystitis);
• gastrointestinal infections (including salmonella carriers);
• gynecological infections;
• skin and soft tissue infections;
• peritonitis;
• sepsis, septic endocarditis;
• meningitis;
• rheumatism;
• erysipelas;
• scarlet fever;
• gonorrhea.

Dosing regimen

Set individually depending on the severity of the course, the localization of the infection and the sensitivity of the pathogen.

When taken orally, a single dose for adults is 250-500 mg, the daily dose is 1-3 g. The maximum daily dose is 4 g.

For children, the drug is prescribed in a daily dose of 50-100 mg / kg, for children weighing up to 20 kg - 12.5-25 mg / kg.

The daily dose is divided into 4 doses. The duration of treatment depends on the severity of the infection and the effectiveness of the treatment.

Tablets are taken orally, regardless of the meal.

To prepare the suspension, 62 ml of distilled water is added to the vial with the powder. The finished suspension is dosed with a special spoon having 2 marks: the lower one corresponds to 2.5 ml (125 mg), the upper one - 5 ml (250 mg). The suspension should be taken with water.

At parenteral administration(in / m, in / in a stream or in / in a drip) a single dose for adults is 250-500 mg, a daily dose is 1-3 g; in severe infections, the daily dose may be increased to 10 g or more.

For newborns, the drug is prescribed in a daily dose of 100 mg / kg, for children of other age groups - 50 mg / kg. At severe course infections, the indicated doses may be doubled.

The daily dose is divided into 4-6 injections with an interval of 4-6 hours. The duration of the intramuscular injection is 7-14 days. The duration of the / in the application of 5-7 days, followed by the transition (if necessary) to the / m administration.

A solution for intramuscular injection is prepared by adding 2 ml of water for injection to the contents of the vial.

For intravenous jet administration single dose the drug (not more than 2 g) is dissolved in 5-10 ml of water for injection or isotonic solution sodium chloride and injected slowly over 3-5 minutes (1-2 g over 10-15 minutes). With a single dose exceeding 2 g, the drug is administered intravenously. To do this, a single dose of the drug (2-4 g) is dissolved in 7.5-15 ml of water for injection, then the resulting solution is added to 125-250 ml of isotonic sodium chloride solution or 5-10% glucose solution and injected at a rate of 60-80 drops. /min When administered intravenously to children, a 5-10% glucose solution (30-50 ml, depending on age) is used as a solvent.

Solutions are used immediately after preparation.

Side effect

Allergic reactions: skin rash, urticaria, angioedema, itching, exfoliative dermatitis, erythema multiforme; in rare cases - anaphylactic shock.

From the side digestive system: nausea, vomiting, diarrhea, glossitis, stomatitis, pseudomembranous colitis, intestinal dysbacteriosis, increased activity of hepatic transaminases.

From the hematopoietic system: anemia, leukopenia, thrombocytopenia, agranulocytosis.

Effects due to chemotherapeutic action: oral candidiasis, vaginal candidiasis.

Contraindications to the use of the drug AMPICILLIN

• hypersensitivity to antibiotics from the penicillin group and other beta-lactam antibiotics;
• severe liver dysfunction (for parenteral use).

The use of the drug AMPICILLIN during pregnancy and lactation

It is possible to use the drug during pregnancy according to indications in cases where the benefit to the mother outweighs the potential risk to the fetus.

Ampicillin is excreted in breast milk in low concentrations. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

Parenteral use is contraindicated in severe liver dysfunction.

Use in children

When administered orally to children, the drug is prescribed in a daily dose of 50-100 mg / kg, for children weighing up to 20 kg - 12.5-25 mg / kg. Parenterally for newborns, the drug is prescribed in a daily dose of 100 mg / kg, for children of other age groups - 50 mg / kg. In severe infections, these doses may be doubled.

special instructions

With caution and against the background of the simultaneous use of desensitizing agents, the drug should be prescribed for bronchial asthma, hay fever and other allergic diseases.

In the process of using Ampicillin, systematic monitoring of the function of the kidneys, liver and peripheral blood is necessary.

At liver failure the drug should be used only under the control of liver function.

Patients with impaired renal function require adjustment of the dosing regimen depending on the CC.

When using the drug in high doses in patients with renal insufficiency, it is possible toxic effect on the CNS.

When using the drug for the treatment of sepsis, a bacteriolysis reaction (the Jarisch-Herxheimer reaction) is possible.

If allergic reactions occur during the use of Ampicillin, the drug should be discontinued and desensitizing therapy prescribed.

In debilitated patients with prolonged use of the drug, superinfection caused by ampicillin-resistant microorganisms may develop.

To prevent the development of candidiasis, nystatin or levorin, as well as vitamins of groups B and C, should be prescribed simultaneously with Ampicillin.

Overdose

Currently, cases of overdose of the drug Ampicillin have not been reported.

drug interaction

Probenecid at simultaneous application with Ampicillin reduces the tubular secretion of ampicillin, resulting in an increase in its concentration in the blood plasma and an increased risk of toxic effects.

With the simultaneous use of Ampicillin with allopurinol, the likelihood of a skin rash increases.

With simultaneous use with Ampicillin, the effectiveness of estrogen-containing oral contraceptives decreases.

With simultaneous use with Ampicillin, the effectiveness of anticoagulants and aminoglycoside antibiotics increases.

Terms and conditions of storage

List B. The drug should be stored in a dry, dark place; tablets and powder for suspension - at a temperature of 15 ° to 25 ° C, powder for solution for injection - at a temperature not exceeding 20 ° C. The shelf life of tablets, powder for suspension and powder for solution for injection is 2 years.

The prepared suspension should be stored in the refrigerator or at room temperature for no more than 8 days. Prepared solutions for intramuscular and intravenous administration are not subject to storage.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Benzylpenicillin sodium salt - instructions for use. Prescription drug, information intended for healthcare professionals only!

pharmachologic effect

Antibiotic of the biosynthetic penicillin group. It has a bactericidal effect by inhibiting the synthesis of the cell wall of microorganisms.

Active against gram-positive bacteria: Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis; anaerobic spore-forming rods; as well as Actinomyces spp., Spirochaetaceae.

The strains of Staphylococcus spp., which produce penicillinase, are resistant to the action of benzylpenicillin. Decomposes in an acidic environment.

Novocaine salt of benzylpenicillin compared with potassium and sodium salts is characterized by a longer duration of action.

Pharmacokinetics

After i / m administration, it is rapidly absorbed from the injection site. Widely distributed in tissues and body fluids. Benzylpenicillin penetrates well through the placental barrier, the BBB during inflammation of the meninges.

T1/2 - 30 min. Excreted with urine.

Indications

Treatment of diseases caused by microorganisms sensitive to benzylpenicillin: lobar and focal pneumonia, pleural empyema, sepsis, septicemia, pyemia, acute and subacute septic endocarditis, meningitis, acute and chronic osteomyelitis, urinary tract and biliary tract, tonsillitis, purulent infections of the skin, soft tissues and mucous membranes, erysipelas, diphtheria, scarlet fever, anthrax, actinomycosis, treatment of purulent inflammatory diseases in obstetric and gynecological practice, ENT diseases, eye diseases, gonorrhea, blennorrhea, syphilis.

Dosing regimen

Individual. Enter in / m, in / in, s / c, endolumbally.

With the / m and / in the introduction of adults, the daily dose varies from 250,000 to 60 million. The daily dose for children under the age of 1 year is 50,000-100,000 IU / kg, over 1 year - 50,000 IU / kg; if necessary daily dose can be increased to 200,000-300,000 U/kg, according to vital indications - up to 500,000 U/kg. The frequency of administration is 4-6 times a day.

Depending on the disease and the severity of the course, it is administered endolumbally for adults - 5000-10,000 IU, for children - 2000-5000 The drug is diluted in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1 thousand U / ml. Before injection (depending on the level intracranial pressure) extract 5-10 ml of CSF and add it to the antibiotic solution in equal proportions.

S / c benzylpenicillin is used for chipping infiltrates (100,000-200,000 IU in 1 ml of a 0.25% -0.5% solution of novocaine).

Benzylpenicillin potassium salt is used only in / m and s / c, in the same doses as benzylpenicillin sodium salt.

Benzylpenicillin novocaine salt is used only in / m. The average therapeutic dose for adults: single - 300,000 IU, daily - 600,000. Children under the age of 1 year - 50,000-100,000 IU / kg / day, over 1 year - 50,000 IU / kg / day. The frequency of administration is 3-4 times a day.

The duration of treatment with benzylpenicillin, depending on the form and severity of the course of the disease, can range from 7-10 days to 2 months or more.

Side effect

From the digestive system: diarrhea, nausea, vomiting.

Effects due to chemotherapeutic action: vaginal candidiasis, oral candidiasis.

From the side of the central nervous system: when using benzylpenicillin in high doses, especially with endolumbar administration, neurotoxic reactions may develop: nausea, vomiting, increased reflex excitability, symptoms of meningism, convulsions, coma.

Allergic reactions: fever, urticaria, skin rash, rash on mucous membranes, joint pain, eosinophilia, angioedema. Cases of anaphylactic shock with a fatal outcome are described.

Contraindications

Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins. Endolumbar administration is contraindicated in patients suffering from epilepsy.

Use during pregnancy and lactation

Use during pregnancy is possible only if the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

If necessary, use during lactation should decide on the termination of breastfeeding.

Application for violations of kidney function

Use with caution in patients with impaired renal function.

special instructions

Use with caution in patients with impaired renal function, with heart failure, a predisposition to allergic reactions (especially with drug allergies), with hypersensitivity to cephalosporins (due to the possibility of cross-allergy).

If after 3-5 days after the start of the application of the effect is not observed, you should switch to the use of other antibiotics or combination therapy.

In connection with the possibility of developing fungal superinfection, it is advisable to prescribe antifungal drugs in the treatment with benzylpenicillin.

It should be borne in mind that the use of benzylpenicillin in subtherapeutic doses or early termination of treatment often leads to the emergence of resistant strains of pathogens.

drug interaction

Probenecid reduces the tubular secretion of benzylpenicillin, resulting in an increase in the concentration of the latter in the blood plasma, and an increase in the half-life.

With simultaneous use with antibiotics that have a bacteriostatic effect (tetracycline), the bactericidal effect of benzylpenicillin decreases.

AT field conditions soldiers were dying en masse from seemingly simple infections, and humanity was getting closer and closer to solving the problem. Both Soviet and British laboratories conducted research on a green mold fungus called Penicillium notatum. At first, its ability to destroy staphylococci in cell culture was established, then significant amounts of the first penicillin from the culture of Penicillium notatum were isolated in pure form, and over time for clinical use virtually unlimited quantities of benzylpenicillin became available.

Penicillin is the backbone of drugs such as antibiotics. Even today, when mankind knows a wide variety of its derivatives and antibiotics of alternative origin, use of penicillin still popular.

What do we know today about use of penicillin, about this "firstborn" antibiotic therapy? How does it affect the human body? Why is it so relevant? And when is it better to forget about it and resort to other achievements of antibacterial treatment?

Description of penicillins

If in the middle of the twentieth century a medicinal substance isolated from the green mold Penicillium notatum was called penicillin, then science did not stop there. To date, penicillins are a whole group of beta-lactam antibiotics, the production of which involves a wide variety of molds of the same genus, as well as some semi-synthetic agents. . The resulting medicinal substance is active against most gram-positive and some gram-negative microorganisms. In addition to penicillins, cephalosporins, carbapenems, and monobactams were subsequently classified as beta-lactam antibiotics. It is the most widely used in clinical practice a group of antimicrobial agents united due to the presence of a four-membered beta-lactam ring in the structure of the molecules of the substances.

In the classification of antibiotics, penicillins occupy the following positions:

• according to the mechanism of action - inhibitors of the synthesis of the cell wall of the microorganism;
• on chemical structure- beta lactams;
• according to the type of impact on the microbial cell - bactericidal;
• by spectrum antimicrobial action- active against gram-positive and gram-negative cocci (staphylococci, streptococci, meningococci, gonococci), some gram-positive microbes (corynebacterium, clostridia) and spirochetes; Semi-synthetic penicillins are broad-spectrum drugs.

Among themselves, penicillins are classified as follows:

• natural penicillins - active against gram-positive bacteria and cocci
• benzylpenicillins,
• bicillins,
• phenoxymethylpenicillin;
• isoxazolpenicillins - active mainly against staphylococci
• oxacillin is used against penicillinase-forming staphylococci that are resistant to natural penicillins and resistant to other antibiotics
• cloxacillin,
• flucloxacillin;
• amidinopenicillins - active against gram-negative enterobacteria
• amdinocillin,
• pivamdinocillin,
• bacamdinocillin,
• acidocillin;
• aminopenicillins - rated as broad spectrum
• ampicillin,
• amoxicillin,
• talampicillin,
• bacampicillin,
• pivampicillin;
• carboxypenicillins - active against Pseudomonas aeruginosa and indole-positive Proteus species
• carbenicillin,
• carfecillin,
• carindacillin,
• ticarcillin;
• ureidopenicillins - even more active against Pseudomonas aeruginosa, they are also used against Klebsiella spp
• azlocillin,
• mezlocillin,
• piperacillin.

Mechanism of action of penicillin

The mechanism of action of the drug is based on use of penicillin. Any drug is used not at all in order for a new biochemical reaction to occur or physiological process. The role of the drug in stimulating, simulating, inhibiting or completely blocking the action of internal mediators responsible for signals between various organs and systems through biological substrates.

So, penicillins, in particular, are involved in the synthesis of the cell wall, and more precisely in the synthesis of a glycopeptide. This is a very complex biochemical process, the violation of which causes cell lysis or the appearance of areas without a cell wall at all. This is something analogous to growing microorganisms without essential amino acids, primarily without lysine or its precursor, diaminopimelic acid.

Being a beta-lactam antibiotic, penicillin has the ability to interfere with glycopeptide synthesis and cause lysis of exposed cytoplasm and cell death. This is the basis of the mechanism of action of penicillin.

The use of penicillin makes it possible to prevent the construction of cell membranes by microbes, blocking the final stage of the synthesis of the bacterial wall.

The action of penicillin is estimated as bactericidal and bacteriostatic. It demonstrates effectiveness in relation to:

• streptococcus,
• gonococcus,
• pneumococcus,
• meningococcus,
• tetanus pathogens,
• anthrax pathogens,
• causative agents of gas gangrene,
• diphtheria pathogens,
  
• some strains of pathogenic staphylococci,
• some strains of Proteus.

It is useless to use penicillin in relation to:

• bacteria of the enterotyphoid-dysenteric group,
• pertussis pathogens,
• mycobacterium tuberculosis,
• friedlander sticks,
• Pseudomonas aeruginosa and so on.

Indications for the use of penicillin

So, it was named against which microorganisms penicillins are active, but what diseases can they cure? The list of those is:

• sepsis,
• septic endocarditis ,
• pneumococcal, meningococcal, gonococcal and other infections, often extensive and deeply localized,
• croupous and focal pneumonia,
• pleuropulmonary processes, in particular purulent pleurisy,
• large wounds, severe burns and in the period after operations for the prevention of complications,
• furunculosis,
• brain abscesses and purulent meningitis,
• gonorrhea,
• syphilis,
• sycosis,
• inflammation of the eye and ear, otitis,
• cholecystitis,
• cholangitis,
• rheumatism,
• umbilical sepsis, septicopyemia and septic-toxic diseases in newborns and infants,
• scarlet fever,
• diphtheria.

Depending on the expected localization of the infectious agent use of penicillin administered intramuscularly, subcutaneously and intravenously. Also practiced is the introduction of a medicinal substance into the cavity, the spinal canal, sublingually. The use of penicillin may be in the form of inhalations, rinses, washes, drops for the eyes and nose.

Particularly effective is demonstrated by intramuscular use of penicillin. So it quickly enters the bloodstream, where a peak is detected already after 30-60 minutes. then the spread of penicillin throughout the body affects the muscles, lungs, joint cavities. It reaches the cerebrospinal fluid in minimal amounts, and therefore in the treatment of meningitis and encephalitis use of penicillin should be intramuscular and endolumbar.

The ability of penicillin to penetrate is noted. At the same time, numerous studies have shown the safety of penicillin for the fetus and pregnant woman. It is easily excreted from the body by the kidneys.

Usually within 3-4 hours, penicillin is excreted from the body in the urine. To maintain a stable required level of drug concentration in the blood, its repeated administration is prescribed taking into account this period.

Contraindications to the use of penicillin

Although the invention of antibiotics has become a revolutionary breakthrough in medicine, the use of these drugs is necessarily associated with side effects. The use of penicillin is, of course, no exception.

First of all, penicillin poses a danger to persons with high sensitivity to him. Usually sensitivity to penicillin is associated with high susceptibility to sulfonamides and similar antibiotics. Sensitization to medicinal substance can also occur during pregnancy, despite the fact that penicillin is one of the few antibiotics allowed during pregnancy.

Contraindications to use of penicillin it is also bronchial asthma, and urticaria, and hay fever, and many.

• Usually allergic manifestations side effects from penicillin occur in people with allergies. Most often, these are skin manifestations - erythema, urticaria, urticaria-like rashes, as well as macular, vesicular and pustular rashes, and even life-threatening exfoliative dermatitis.
• In the work of the respiratory organs, side effects from the use of penicillin can manifest as rhinitis, laryngopharyngitis and pharyngitis, bronchial asthma and asthmatic bronchitis.
• Penicillin can affect the functioning of the gastrointestinal tract with nausea and vomiting, stomatitis and diarrhea. Also, during treatment with penicillin, as with any other antibiotics, dysbacteriosis can develop, because penicillin equally affects both pathogenic and beneficial bacteria.

Serious complications in the process of using penicillin preparations can be anaphylactic shock and impaired liver function.

When prescribing penicillins, the physician should weigh the potential risk and the expected benefit, taking into account all anamnestic data on the use of penicillin and reactions to it. And, of course, use of penicillins should not occur as part of self-medication.

AT modern medicine antibiotics of the penicillin group are widely used in standard forms of inflammatory diseases. Although in recent times semi-synthetic penicillins are more commonly used, a simple variant of this medicinal product not infrequently it turns out to be indispensable, otitis media, cystitis and tonsillitis in children.

The antibiotic penicillin is one of the first forms antibacterial agents directional action invented by man. At the time of its discovery, it was a powerful drug that helped save the lives of patients with pneumonia and. Before the invention of penicillin, inflammation of the lungs was almost 90% fatal. dangerous disease. But, a few years later, doctors began to notice a decrease in the activity of the antibiotic penicillin against the vast majority of pathogens. This was the impetus for developing the latest antibacterial agents.

However, with each new generation, antibiotics acquired not only powerful antibacterial properties, but also strongest side effects. at the same time, simple, completely natural penicillin was gradually forgotten. To date, the use of first-generation penicillin is recommended by all foreign microbiologists. The essence of this is simple. Immediately after the invention of penicillin, a gradual decrease in its activity began to manifest itself due to mutations in bacteria. They began to adapt to this antibiotic, to develop a kind of immunity against it. Later this process progressed. Man invented new, bacteria - new forms of adaptation.

According to recent microbiological studies, resistance to the antibiotic penicillin in bacteria is low. This means that it can be successfully used in the treatment of bacterial infections caused by bacteria sensitive to this drug.

Main pharmachologic effect penicillin is aimed at disrupting protein synthesis in bacterial cells. As a result of violation of the permeability of the cell membrane causes the destruction and death of bacteria. This causes its rapid bactericidal action. Unlike other antibiotics, it does not slow down the reproduction of pathogens, but provokes their disappearance.

Experimentally proven low resistance to penicillin in:

1. gram positive bacteria causing inflammation respiratory and urinary system;
2. gram-negative bacteria of the cocci group, including those causing meningitis, gonorrhea, syphilis;
3. bacteria of the actinomycete group.

Maximum concentration in biological environments human body achieved with intramuscular injection of the drug. In this case, the increase in the percentage begins 5 minutes after the injection of penicillin and reaches its maximum after 30 minutes. The antibiotic penicillin freely penetrates into the blood, urine, bile, binding to plasma proteins. Not available for him cerebrospinal fluid, tissues in the eye area and the prostate gland. Therefore, in the treatment of gonorrhea in men, penicillin is used in combination with other drugs.

The antibiotic penicillin is available in tablets and vials for injection in the form of a dry powder. Before use, it is diluted with saline sodium chloride or novocaine.

Where is penicillin used?

Penicillin is used in the treatment of inflammatory bacterial infections of the upper respiratory tract. In particular, good performance it gives in the treatment of catarrhal and lacunar tonsillitis. The drug is effective in combination with sulfonamides in the treatment of uncomplicated forms of pneumonia. Used in the treatment of pyelonephritis, consequences urolithiasis, cystitis in combination with drugs of the nitrofuran series.

Other indications for the use of penicillin include:

• inflammation and purulent lesions of the epidermis, including erysipelas;
• otitis and sinusitis;
• chronic and sharp forms pleurisy with effusion;
• endocarditis, pericarditis, rheumatic heart disease;
• some sexually transmitted infections (syphilis, ureaplasmosis, toxicoplasmosis);
• infectious diseases, among which scarlet fever and anthrax are most successfully treated with penicillin.

Penicillin is not effective for intestinal infections, in particular with dysentery, salmonellosis. This drug is not stable in an acidic environment and is rapidly destroyed in the intestine by penicillinase.

Treatment of inflammatory diseases with penicillin

For effective treatment penicillin inflammatory diseases are important two factors. it correct selection the method of administration and the exact determination of the daily and single dosage. A course of treatment is recommended for acute conditions and severe disease, start with intramuscular injection. The half-life of penicillin in tissues and body fluids is just over 4 hours. Therefore, to maintain the maximum concentration, injections should be done at intervals of 4 hours. Those. 6 times daily administration of penicillin is necessary to obtain a qualitative result of treatment.

The dosage is calculated based on the weight of the patient, the severity of his condition and the type of pathogen. Approximate dosages can be seen in the table below, the course of treatment is at least 10 days.

Is it possible for children to have penicillin?

Penicillin can be prescribed to children from 1 year. In more early age this drug can have an otogenic effect, which in the future will negatively affect the development of hearing in a baby. Penicillin injections for children can only be done in a hospital setting. At home, only oral administration of the drug is allowed.

The use of penicillin during pregnancy and lactation

During pregnancy, penicillin is strictly prohibited for intramuscular and internal use. It is allowed to use in the form of an ointment on limited areas of the skin.

During lactation, penicillin should also be excluded. It easily penetrates breast milk and has an extremely negative effect on the infant.

Allergy to penicillin

Allergy to penicillin is quite common. Wherein allergic reaction after intramuscular injection, it often develops according to the type of anaphylactic shock, which is dangerous for the patient's life. Therefore, before the appointment of penicillin, a mandatory skin test is necessary.

To do this, the nurse makes a small scratch on inside patient's forearm. A solution of penicillin prepared for injection is applied to the wound surface. After 30 minutes, the reaction is checked. If there is even a scratch at the site slight redness, penicillin should not be used in this patient.

To reduce the level of local irritation before injection, penicillin should be diluted with a solution of novocaine. Although dilution with sodium chloride solution is usually recommended.