Benzylpenicillin preparation for oral administration. Benzylpenicillin - instructions, indications, composition, method of application. Side effects of the substance benzylpenicillin

1 bottle includes 500,000 IU or 1,000,000 IU sodium salt of benzylpenicillin ( ).

Release form

The company "Sintez" produces the drug in the form of a powder for the manufacture of injections, in bottles No. 1; No. 5; #10 or #50 per pack.

pharmachologic effect

Antibacterial.

Pharmacodynamics and pharmacokinetics

Benzylpenicillin is biosynthetic and included in the group . The bactericidal efficacy of the drug is manifested due to its ability to inhibit the synthesis of walls bacterial cells .

The effect of the drug is detrimental to gram-positive microorganisms: staphylococci , pathogens and anthrax , streptococci ; Gram-negative bacteria: pathogens and ; spore-forming anaerobic rods; as well as spirochete and actinomycete .

Insensitive to impact benzylpenicillin strains staphylococci that produce penicillinase .

With the introduction of the drug in / m TCmax in plasma is observed after 20-30 minutes. Binding to plasma proteins occurs by 60%. Antibiotic it has good penetration into tissues, biological fluids and organs of the human body, with the exception of liquor , prostate and eye tissues, passes through GEB . Excretion is carried out in unchanged form by the kidneys. T1 / 2 fluctuates between 30-60 minutes, with can increase up to 4-10 hours or even more.

Indications for use

Benzylpenicillin is indicated for the treatment of diseases caused by microorganisms sensitive to its effects:

focal/croupous pneumonia ;
pleural empyema;
sepsis;
septicemia;
erysipelas;
pyemia ;
anthrax ;
septic (subacute and acute);
actinomycosis;
ENT infections;
infections of the biliary and urinary tract;
blennorea ;
infections of the mucous membranes and soft tissues;
skin purulent infections;
purulent-inflammatory infections in gynecologists.

Contraindications

Absolutely prohibited introduction benzylpenicillin with personal hypersensitivity (including other penicillin antibiotics ) and (for endolumbar injections). It is also not recommended to use this drug for breastfeeding and pregnancy .

Side effects

There may be effects associated with the chemotherapeutic effects of drugs, including oral cavity and/or vagina .

From the gastrointestinal tract observed a feeling nausea , , sometimes vomit .

From the side of the central nervous system, especially when using high doses of the drug or when injecting endolumbally, it is possible to form neurotoxic events , such as an increase in reflex excitability, convulsions , nausea, symptoms meningism , vomit, .

In this situation, stop further injections and prescribe symptomatic treatment, including . In this case, special attention is paid to the water-electrolyte state.

Interaction

Combined appointment with bacteriostatic antibiotics (Tetracycline ), reduces the bactericidal effectiveness benzylpenicillin .

Parallel use with reduces tubular secretion benzylpenicillin , which affects the increase in its plasma concentration and increases T1 / 2.

Terms of sale

Benzylpenicillin is marketed as a prescription drug.

Storage conditions

The powder should be stored in the original sealed vial at temperatures up to 20°C.

Best before date

From the date of manufacture - 3 years.

special instructions

Benzylpenicillin administered with extreme caution to patients with , heart failure , allergy sufferers (especially with ), as well as hypersensitivity to cephalosporins (because of the possible formation of cross-reactions).

In the case of a zero effect of therapy carried out for 3-5 days, the possibility of a combination with other drugs or the appointment of other drugs should be considered. antibiotics .It is better to avoid drinking drinks with alcohol.

During pregnancy and lactation

Purpose benzylpenicillin when allowed only in extreme cases, with a comprehensive assessment of the benefits / risks.

If necessary, use benzylpenicillin at the time of lactation stop.

powder for preparation. r-ra d / in / in and / m injections of 500 thousand units: fl. 1 or 50 pcs. Reg. No.: LS-001481

Clinico-pharmacological group:

Antibiotic of the penicillin group, destroyed by penicillinase

Release form, composition and packaging

bottles (1) - cardboard boxes.
bottles (50) - cardboard boxes.

Description of the active ingredients of the drug Benzylpenicillin»

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.

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, infections of the urinary and biliary tract, tonsillitis, purulent infections of the skin, soft tissues and mucous membranes, erysipelas, diphtheria, scarlet fever, anthrax, actinomycosis, treatment of pyoinflammatory 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 units. 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, the daily dose can be increased to 200,000-300,000 IU / kg, according to vital indications - up to 500,000 IU / kg. Multiplicity of introduction 4-6 times / day.

Depending on the disease and the severity of the course, endolumbar injection is administered to adults - 5000-10,000 IU, to children - 2000-5000 IU. The drug is diluted in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1 thousand units / ml. Before injection (depending on the level of intracranial pressure), 5-10 ml of CSF is removed and added 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 IU. Children under the age of 1 year - 50,000-100,000 U / kg / day, over 1 year - 50,000 U / kg / day. Multiplicity of introduction 3-4 times / 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.

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.

active substance: benzylpenicillin;

1 bottle contains sterile benzylpenicillin sodium salt - 500,000 IU or 1,000,000 IU.

Dosage form. Powder for solution for injection.

Basic physical and chemical properties: white or almost white crystalline powder.

Pharmacotherapeutic group.

Antimicrobial agents for systemic use. Penicillins sensitive to the action of β-lactamases.

ATX code J01C E01.

Pharmacological properties

Pharmacodynamics.

The drug is a water-soluble benzylpenicillin, which has a bactericidal effect on sensitive microorganisms by inhibiting cell wall biosynthesis. The spectrum of action of benzylpenicillin extends to streptococci of groups A, B, C, G, H, L and M, Streptococcus pneumoniae, Streptococcus viridans, enterococci, penicillin-azone-non-producing strains of staphylococci, as well as Neisseriae, corynebacteria, Bacillus anthracis, actinomycetes, Pasteurella multocida, varieties of spirochetes, for example Leptospira, Treponema, Borrelia and other spirochetes, as well as numerous microorganisms (Peptococcus, Peptostreptococcus, Fusobacteria, Clostridia). In high concentrations, the drug is also active against other gram-negative microorganisms, for example Escherichia coli, Proteus mirabilis, salmonella, shigella, Enterobacter aerogenes and Alcaligenes faecalis. In infections caused by staphylococci, enterococci, E. coli or E. aerogenes, it is recommended to carry out bacteriological studies, including sensitivity tests. The production of penicillinase (for example, by staphylococci) causes resistance.

Pharmacokinetics.

After the use of penicillin in high doses, therapeutic concentrations are also achieved in hard-to-reach tissues, such as heart valves, bones and cerebrospinal fluid. Peak plasma levels of 150-200 IU/mL are reached 15-30 minutes after intramuscular injection of 10 million MO of the drug. After short-term infusions (30 minutes), the level can reach a maximum of 500 IU / ml. Plasma protein binding is approximately 55% of the total dose. Most of the administered dose (50-80%) is excreted unchanged by the kidneys (85-95%). Excretion of the active substance with bile is limited to a small part of the dose (about 5%).

Since the functions of the kidneys and liver in premature children and infants are still undeveloped, the half-life in the blood serum is approximately 3 hours. Therefore, the interval between doses should be at least 8-12 hours (depending on the degree of maturity of the organ). There may also be delayed elimination of the drug in elderly patients.

To increase the interval between doses, the drug can be combined with penicillin preparations that form a depot.

clinical characteristics.

Indications

Infectious diseases caused by penicillin-sensitive microorganisms: sepsis, wound infections and skin infections, diphtheria (in addition to antitoxin), pneumonia, empyema, erysipeloid, pericarditis, bacterial endocarditis, mediastinitis, peritonitis, meningitis, brain abscesses, arthritis, osteomyelitis; infections of the genital tract caused by fusobacteria; and also when specific infections: anthrax; infections caused by Clostridium, including tetanus, listeriosis, pasteurellosis; fever caused by rat bites; fusospirochetosis, actinomycosis; treatment of complications caused by gonorrhea and syphilis; Lyme borreliosis after the first stage of the disease.

Contraindications

Hypersensitivity to benzylpenicillin or other β-lactam antibiotics (penicillins, cephalosporins, carbapenems). Newborns whose mothers are hypersensitive to antibiotics of the penicillin group. Epilepsy (with intralumbar injection). Severe allergic reactions or bronchial asthma or urticaria, history of hay fever.

Interaction with other medicinal products and other forms of interaction. Penicillin preparations with bactericidal action should not be used in combination with bacteriostatic antibiotics. Combination with other antibiotics is advisable only when a synergistic effect or any additional effect is possible. The individual components of the therapeutic combination should be administered at full dose (the dose of the more toxic component may be reduced if a synergistic effect is shown).

Bactericidal antibiotics used in combination with the drug include isoxazolylpenicillins, such as flucloxacillin and other narrow-spectrum beta-lactam antibiotics, aminopenicillins, aminoglycosides. They should be administered by slow intravenous injection prior to the administration of benzylpenicillin. If possible, aminoglycosides should be given IM separately. It should be borne in mind the possibility of competitive inhibition of the excretion process from the body with the simultaneous use of benzylpenicillin with anti-inflammatory, antirheumatic and antipyretic drugs (indomethacin, phenylbutazone, salicylates in high doses). Aspirin, probenecid, thiazide diuretics, furosemide, ethacrynic acid increase the half-life of benzylpenicillin, increasing its concentration in the blood plasma, thereby increasing the risk of developing its toxic effect by influencing tubular secretion of the kidneys. Allopurinol increases the risk of developing allergic reactions (skin rashes). The use of benzylpenicillin may in some cases lead to a decrease in the effectiveness of oral contraceptives.

Avoid simultaneous use with chloramphenicol, erythromycin, tetracycline, sulfonamides.

With simultaneous use with methotrexate, the excretion of the latter decreases and the risk of its toxicity increases.

Application features

Before starting treatment, it is necessary to conduct a preliminary test for the possibility of a hypersensitivity reaction to penicillins and cephalosporins. In patients with known hypersensitivity to cephalosporins, the possibility of cross-allergy should be considered.

Severe and sometimes fatal cases of hypersensitivity (anaphylactic reaction) have been observed in patients treated with penicillin. Such reactions occur more frequently in patients with a known history of severe allergic reactions. Treatment with the drug must be discontinued and replaced with another appropriate treatment. Symptoms of an anaphylactic reaction may need to be treated, such as immediate adrenaline, intravenous steroids, and emergency treatment for respiratory failure.

3 special care should be used in patients with hay fever, urticaria and other allergic diseases.

Penicillin is not recommended for the treatment of patients with acute lymphocytic leukemia or infectious mononucleosis due to an increased risk of erythematous skin rashes. It should be borne in mind that in patients with diabetes mellitus, the absorption of the active substance from intramuscular depots may be reduced.

Patients who use the drug in high doses for more than 5 days should monitor the electrolyte balance, blood count and kidney function.

In severe disorders of kidney function, large doses of penicillin can cause cerebral disorders, convulsions, coma.

Caution should be exercised when using the drug in infants, patients with severe cardiopathy, hypovolemia, epilepsy, impaired renal or hepatic function.

With the on / in the introduction of the drug in high doses (more than 10 million IU / day), the injection sites should be changed every 2 days to prevent the development of superinfection and thrombophlebitis.

With intramuscular administration of the drug to infants, the development of serious local reactions is possible, so preference should be given to intravenous administration.

Prolonged use of the drug may lead to the development of colonization of resistant microorganisms or yeast. Superinfection may occur, which requires careful monitoring of such patients.

If severe diarrhea occurs, characteristic of pseudomembranous colitis (in most cases caused by Clostridium difficile), it is recommended to discontinue the use of the drug and take appropriate measures. The use of agents that inhibit peristalsis is contraindicated. In the treatment of sexually transmitted diseases with suspected syphilis, serological studies should be carried out before the start of therapy and within 4 months after its completion.

To suppress or alleviate the Jarisch-Herxheimer reaction, at the first use of the drug, administer 50 mg of prednisolone or its equivalent. In patients with syphilis at the stage of cardiovascular, vascular, and meningeal syphilis, Jarisch-Herxheimer reactions can be prevented by prednisone 50 mg daily or an equivalent steroid for 1 to 2 weeks.

Freshly prepared solutions for injection or infusion should be used immediately. Even when stored in a refrigerator, aqueous solutions of the sodium salt of benzylpenicillin decompose to the formation of degradation products and metabolites.

Use during pregnancy or lactation

Benzylpenicillin crosses the placental barrier and its concentration in the blood plasma of the fetus 1-2 hours after administration corresponds to the concentration in the mother's blood serum. Available data on the use of the drug during pregnancy indicate the absence of a negative effect on the fetus / newborn. The use of the drug during pregnancy is possible only after a thorough assessment of the benefit / risk ratio.

Benzylpenicillin penetrates in small amounts into breast milk, so the risk of developing hypersensitivity in a child cannot be excluded. The use of the drug during lactation is possible only when the expected benefit to the mother outweighs the potential risk to the child.

The ability to influence the reaction rate when driving vehicles or operating other mechanisms. There was no negative effect on the reaction rate when driving vehicles or working with other mechanisms.

Dosage and administration

The drug is administered intramuscularly, subcutaneously, intravenously (by jet and drip), intrathecally, into the body cavity. The most common intramuscular route of administration.

Intravenously: with infections of moderate severity, a single dose of the drug for adults is usually 250,000-500,000 IU, daily - 1,000,000-2,000,000 IU, for severe infections, administer up to 10,000,000-20,000,000 IU per day, with gas gangrene - up to 40,000,000-60,000,000 units Usually the daily dose for children under the age of 1 year is 50,000-100,000 U / kg, at the age of 1 year - 50,000 U / kg, if necessary, the 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 of the drug is 4-6 times a day. Benzylpenicillin solution should be prepared immediately before its use. For intravenous jet injection, a single dose (1,000,000-2,000,000 IU) of the drug should be dissolved in 5-10 ml of sterile water for injection or 0.9% sodium chloride solution and administered slowly over 3-5 minutes. For intravenous drip, dissolve 2,000,000-5,000,000 IU of the antibiotic in 100-200 ml of 0.9% sodium chloride solution or 5% glucose solution and inject at a rate of 60-80 drops per 1 minute.

Intravenously, the drug is administered 1-2 times a day, combined with intramuscular injections.

Intramuscularly: for infections of moderate severity, a single dose of the drug for adults is usually 250,000-500,000 IU, daily - 1,000,000-2,000,000 IU, for severe infections, up to 10,000,000-20,000,000 IU per day, with gas gangrene - up to 40,000,000- 60,000,000 units Usually the daily dose for children under the age of 1 year is 50,000-100,000 U / kg, at the age of 1 year - 50,000 U / kg, if necessary, the 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 of the drug is 4-6 times a day. For intramuscular injection, add 1-3 ml of sterile water for injection or 0.9% sodium chloride solution, or 0.5% novocaine solution to the contents of the vial. The resulting solution is injected deep into the muscle in the upper outer quadrant of the buttock.

Subcutaneously: Benzylpenicillin is used for chipping infiltrates at a concentration of 100,000-200,000 IU in 1 ml of a 0.25-0.5% novocaine solution. In the cavity (abdominal, pleural), a solution of Benzylpenicillin should be administered to adults at a concentration of 10,000-20,000 IU per 1 ml, for children - 2,000-5,000 IU per 1 ml. Dissolve in sterile water for injection or 0.9% sodium chloride solution. Duration of treatment - 5-7 days, followed by the transition to intramuscular injection.

Intrathecal: the drug is administered for purulent diseases of the brain, spinal cord, meninges. For adults, prescribe at a dose of 5,000-10,000 IU, for children over the age of 1 year - 2,000-5,000 IU, administer slowly - 1 ml per minute 1 time per day. Dilute the drug in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1,000 IU per 1 ml. Before injection, remove 5-10 ml of cerebrospinal fluid from the spinal canal and add it to the antibiotic solution in equal proportions. Injections are repeated for 2-3 days, after which they switch to intramuscular injection.

Treatment of patients with syphilis, gonorrhea should be carried out according to specially developed schemes. Depending on the form and severity of the disease, benzylpenicillin should be used from 7-10 days to 2 months or more (sepsis, septic endocarditis).

Children.

Apply to children from birth. With extreme caution, the drug should be used in children under 2 years of age.

Overdose

Symptoms of an overdose largely correspond to the nature of the side effects. Gastrointestinal disorders and disturbances in water and electrolyte balance are possible.

Treatment: there is no specific antidote. Treatment includes hemodialysis, gastric lavage and symptomatic therapy; special attention should be paid to the water-electrolyte balance.

Adverse reactions

From the blood and lymphatic system: eosinophilia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis, pancytopenia. Hemolytic anemia, a clotting disorder, and a positive Coombs test result are also possible.

From the side of the immune system: allergic reactions, including urticaria, erythema multiforme, exfoliative dermatitis, contact dermatitis, angioedema, fever, joint pain, anaphylactic or anaphylactoid reactions (bronchial asthma, thrombocytopenic purpura, gastrointestinal symptoms).

From the side of the nervous system: when infused with a high dose (adults more than 20 million IU), the risk of seizures is especially high in patients with severe renal dysfunction, epilepsy, meningitis, cerebral edema, or when using an extracorporeal circulation device; neurotoxic reactions, including hyperreflexia, myoclonic twitches; coma, symptoms of meningism, paresthesia.

Metabolism and eating disorders: electrolyte imbalance, which is possible with the rapid introduction of a dose of more than 10 million IU, an increase in the level of nitrogen in the blood serum.

From the digestive tract: stomatitis, glossitis, black coloration of the tongue, nausea, vomiting, diarrhea.

From the digestive system: hepatitis, bile stasis.

From the side of the kidneys and urinary system: interstitial nephritis, nephropathy (with a / in the introduction of a dose of more than 10 million IU), albuminuria, cylindruria and hematuria. Oliguria or anuria, as a rule, disappear 48 hours after discontinuation of therapy. Diuresis can be restored after the application of a 10% mannitol solution.

Other: reactions at the injection site; with intravenous administration, the development of phlebitis or thrombophlebitis is possible; severe local reactions with i / m administration to infants; prolonged use of antibiotics can lead to the development of secondary superinfection caused by resistant microorganisms; candidiasis; in the treatment of syphilis or other infectious diseases caused by spirochetes, the bacterial lysis process can cause the Jarisch-Herxheimer reaction, which is characterized by the following symptoms: fever, chills, myalgia, headache, exacerbation of skin symptoms, tachycardia, vasodilation with changes in arterial pressure; hypersensitivity reactions (itching, laryngospasm, bronchospasm, arterial hypotension, vascular collapse); serum sickness (including manifestations such as fever, weakness, arthralgia, abdominal pain, rash (all types)); high doses of the drug can lead to the development of congestive heart failure.

Best before date

Storage conditions

In original packaging at a temperature not exceeding 25 ºС.

Keep out of the reach of children.

Incompatibility. To prevent unwanted chemical reactions, two drugs for injection or infusion should not be mixed in one container, and solutions containing glucose should not be used.

The drug is incompatible with metal ions, especially copper, mercury, zinc and zinc compounds, which may be part of the rubber stoppers of infusion bottles. Substances with oxidizing and reducing properties, alcohol, glycerin, macrogols and other hydroxyl compounds can also inactivate it. In slightly alkaline solutions, the drug is quickly inactivated by cysteine and other aminothiol compounds. Sympathomimetic amines are also incompatible with benzylpenicillin.

The drug should not be used in glucose solution.

Do not mix with other injection solutions containing cimetidine, cytarabine, chlorpromazine, dopamine, heparin, hydroxyzine, lactate, lincomycin, metaraminol, sodium bicarbonate, oxytetracycline, pentobarbital, tetracycline, sodium thiopental, vancomycin. Benzylpenicillin is incompatible in solution with a complex of vitamins of group B and ascorbic acid.

Package

500,000 IU or 1,000,000 IU in vials; in bottles No. 10 in a pack.

Manufacturer

PJSC "Kyivmedpreparat"

The location of the manufacturer and its address of the place of business.

Ukraine, 01032, Kyiv, st. Saksaganskogo, 139.

Producer: Arterium (Arterium) Ukraine

ATC code: J01CE01

Farm group:

Release form: Liquid dosage forms. Injection.

General characteristics. Compound:

Active ingredient: benzylpenicillin;
1 bottle contains sterile benzylpenicillin sodium salt - 500,000 units or 1,000,000 units.

Pharmacological properties:

Pharmacodynamics. Benzylpenicillin has an antimicrobial bactericidal effect. Mechanism
actions: the drug prevents the formation of peptide bonds due to the inhibition of transpeptidase, disrupts the later stages of the synthesis of peptidoglycan of the cell wall, which leads to lysis of dividing cells. The drug is active against gram-positive bacteria Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis, some
gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), anaerobic spore-forming rods, as well as Actinomyces spp., Spirochaetaceae. The drug is not active against most gram-negative bacteria, rickettsiae, viruses, protozoa, fungi. Destroyed by penicillinase. In recent years, there has been a change in the sensitivity of gonococci, hemolytic streptococci, staphylococci and pneumococci to benzylpenicillin.

Pharmacokinetics. With intramuscular injection, the maximum concentration of the drug in the blood is created after 30-60 minutes, after 3-4 hours after a single injection, traces of the antibiotic are present in the blood. With subcutaneous administration, the rate of absorption is less constant, usually the maximum concentration in the blood is observed after 60 minutes. The concentration and duration of circulation of benzylpenicillin in the blood depend on the administered dose. It binds to blood proteins by 60%. The antibiotic penetrates well into organs, tissues and body fluids, with the exception of cerebrospinal fluid, eye and prostate tissues, but with inflammation of the meninges, its concentration in the cerebrospinal fluid increases.
The half-life is 30-60 minutes, in case of impaired renal function - 4-10 hours, and with simultaneous impaired liver and kidney function - up to 16-30 hours. It is rapidly excreted from the body by the kidneys (glomerular filtration and tubular secretion) unchanged. It is excreted in small amounts with saliva, sweat, breast milk, and bile. Does not have a cumulative effect.
pharmaceutical characteristics.
Basic physical and chemical properties: white or almost white crystalline powder.
Incompatibility.
Benzylpenicillin must not be mixed in the same container with other drugs.
It is not recommended to use Ringer's solution or other sodium-containing solutions that contain glucose as a solvent. The drug is incompatible with metal ions and sympathomimetic amines.

Indications for use:

Infections caused by susceptible microorganisms:
- infections of the respiratory tract and ENT organs: tonsillitis, purulent, lungs;
-:, salpingo-oophoritis;
- infections of the organ of vision:,;
- purulent infections of the skin and soft tissues;
- septic,;
- ;
- wound infections;
- ;
- ;
- ;
- ;
- infections of the biliary tract.

Important! Get to know the treatment

Dosage and administration:

Before administration, it is necessary to conduct a preliminary skin test for the tolerance of the drug and novocaine, provided that it is used for dilution, in the absence of contraindications to its implementation. The drug is administered intramuscularly, subcutaneously, intravenously (stream and drip),
intrathecally, in the body cavity. The most common intramuscular route of administration.
Intravenously: for infections of moderate severity, a single dose of the drug for adults is usually 250,000-500,000 IU, daily - 1,000,000-2,000,000 IU, for severe infections, up to 10,000,000-20,000,000 IU per day, with gas gangrene - up to 40,000,000-60,000,000 units. Usually the daily dose for children under the age of 1 year is 50,000-100,000 U / kg, over 1 year - 50,000 U / kg, if necessary, the daily dose can be increased to 200,000-300,000 U / kg, according to health indications - up to 500,000 units / kg. The frequency of administration of the drug - 4-6 times a day. A solution of benzylpenicillin is prepared immediately before its use. For intravenous jet administration, a single dose (1,000,000-
2,000,000 IU) of the drug is dissolved in 5-10 ml of sterile water for injection or 0.9% sodium chloride solution and injected slowly over 3-5 minutes. For intravenous drip, 2,000,000-5,000,000 IU of the antibiotic is dissolved in 100-200 ml of 0.9% sodium chloride solution or 5% glucose solution and administered at a rate of 60-80 drops per 1 minute.
Intravenously, the drug is administered 1-2 times a day, combined with intramuscular injections. Intramuscularly: for infections of moderate severity, a single dose of the drug for adults is usually 250,000-500,000 IU, daily - 1,000,000-2,000,000 IU, for severe infections, up to 10,000,000-20,000,000 IU per day are administered, with gas gangrene - up to 40,000,000-60,000,000 units. Usually the daily dose for children under the age of 1 year is 50,000-100,000 U / kg, over 1 year - 50,000 U / kg, if necessary, the 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 of the drug - 4-6 times a day. For intramuscular injection, add 1-3 ml of sterile water for injection or 0.9% sodium chloride solution, or 0.5% novocaine solution to the contents of the vial. The resulting solution is injected deep into the muscle in the upper outer quadrant of the buttock. Subcutaneously: Benzylpenicillin is used for chipping infiltrates at a concentration of 100,000-200,000 IU in 1 ml of a 0.25-0.5% novocaine solution. In the cavity (abdominal, pleural, etc.), a solution of Benzylpenicillin is administered to adults at a concentration of 10,000-20,000 IU per 1 ml, for children - 2,000-5,000 IU per 1 ml. Dissolve in
sterile water for injection or 0.9% sodium chloride solution. Duration of treatment - 5-7 days, followed by the transition to intramuscular injection. Intrathecal: the drug is administered for purulent diseases of the brain, spinal cord, meninges. Adults are prescribed in a dose of 5,000-10,000 IU, children over 1 year old - 2,000-5,000 IU, administered slowly - 1 ml per minute 1 time per day. The drug is diluted in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1,000 IU per 1 ml. Before injection, 5-10 ml of cerebrospinal fluid is removed from the spinal canal and added to the antibiotic solution in equal proportions. Injections are repeated for 2-3 days, after which they switch to intramuscular injection. Treatment of patients with syphilis, gonorrhea is carried out according to specially designed schemes. Depending on the form and severity of the disease, benzylpenicillin is used from 7-10 days to 2 months or more (sepsis, septic endocarditis, etc.).

Application Features:

Use during pregnancy or lactation. Use during pregnancy is possible only if the expected benefit to the woman outweighs the potential risk to the fetus. If necessary, the use of the drug should stop breastfeeding. Children. With extreme caution, the drug should be used in children under the age of 2 years.

Before starting treatment, patients should be checked for hypersensitivity. After the examination and administration of the drug for 30 minutes, you need to be ready for the introduction of adrenaline. Patients should be warned about the possibility of allergic reactions, and if necessary, report them to the doctor. Those who develop allergic reactions to the drug should stop treatment and prescribe symptomatic therapy with epinephrine, antihistamines and corticosteroids. Benzylpenicillin solutions are used immediately after preparation. Application
the drug is possible only in pathological processes caused by microorganisms sensitive to it. With the appearance of resistance of pathogens to the drug, it is replaced with other antibiotics. If the effect of the use of the drug is absent after
3-5 days after the start of treatment, it is necessary to switch to the use of other antibiotics or combine benzylpenicillin with other antibiotics or synthetic chemotherapeutic agents. In this case, the possibility of increasing side effects should be taken into account. Patients over 60 years of age and pregnant women are not recommended to prescribe large doses (above 10,000,000 IU per day). With long-term treatment, electrolyte balance, blood count and kidney function should be monitored. With a special
the drug should be used with caution in infants, patients with syphilis, severe cardiomyopathy, allergic diathesis, bronchial asthma, hypovolemia, epilepsy, patients with impaired renal and hepatic function, as well as patients with diabetes mellitus. In patients with known hypersensitivity to cephalosporins, cross-allergy is possible. Prolonged severe may lead to suspicion regarding development. This condition is life-threatening, so the drug must be urgently canceled with subsequent complex treatment. When dissolving benzylpenicillin in a solution of novocaine, a cloudy
solution due to the formation of novocaine salt of benzylpenicillin, which is not an obstacle to intramuscular administration of the drug. The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Does not affect the ability to drive vehicles and work with other complex mechanisms.

Side effects:

Hypersensitivity reactions: , itching, fever, edema, erythema multiforme exudative, exfoliative, Quincke's angioedema,.
From the side of the respiratory system: .
From the side of the central and peripheral nervous system:,. Endolumbar administration can cause neurotoxicosis (nausea, symptoms of meningism, agrunolocytosis.
Other: in debilitated patients, newborns, the elderly with long-term treatment, superinfection caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms) may occur. Patients being treated for syphilis may develop Jarisch-Herxheimer cancer secondary to bacteriolysis.

Interaction with other drugs:

In combination with aminoglycazides, macrolides, sulfa drugs, benzylpenicillin exhibits a synergistic effect. The effect of the drug is reduced by bacteriostatic drugs (chloramphenicol), and beta-lactamase inhibitors increase its activity. It is not recommended to combine benzylpenicillin with non-steroidal anti-inflammatory drugs, ethinyl estradiol, the drug increases the effectiveness of indirect anticoagulants. Diuretics, allopurinol, blockers of tubular secretion, non-steroidal anti-inflammatory drugs block tubular secretion, as a result of which the concentration of benzylpenicillin in the blood plasma increases, its half-life increases and the risk of toxic effects increases. When combined with allopurinol, the risk of developing a skin rash increases. Benzylpenicillin reduces clearance and increases the toxicity of methotrexate, may reduce the effect of oral contraceptives.

Contraindications:

Hypersensitivity to benzylpenicillin and other β-lactam antibiotics (penicillins, cephalosporins, carbapenems);
- ;
- ;
- urticaria and other allergic diseases;
- (for endolumbar injection);
- period of breastfeeding.

Overdose:

It is manifested by a toxic effect on the central nervous system (more often with endolumbar administration). There is a reflex excitation, headache, nausea, vomiting, convulsions, arthralgia, symptoms of meningism, coma. In such cases, the administration of the drug should be discontinued. Treatment is symptomatic, which includes, special attention should be paid to the water and electrolyte balance.

Storage conditions:

Shelf life 3 years. Store in the original packaging at a temperature not exceeding 25 ° C, out of the reach of
children place.

Leave conditions:

On prescription

Package:

500,000 IU or 1,000,000 IU in vials; in bottles No. 10 in a pack.

Benzylpenicillin INN

International name: Benzylpenicillin
Dosage form: powder for solution for intravenous and intramuscular injection, powder for solution for intramuscular injection, powder for solution for intramuscular and subcutaneous injection, powder for preparation

Chemical Name:
(2S - (2alpha, 5alpha, 6beta) (- 3, 3 - dimethyl - 7 - oxo - 6 - ((phenylacetyl) amino ( - 4 - thia - 1 - aza bicycloheptane - 2 - carboxylic acid (as sodium or potassium salt)

Pharmachologic effect:
Bactericidal antibiotic from the group of biosynthetic ("natural") penicillins. Suppresses the synthesis of the cell wall of microorganisms. Active against gram-positive pathogens: staphylococci (non-forming penicillinase), streptococci, pneumococci, diphtheria corynebacteria, anaerobic spore-forming rods, anthrax rods, Actinomyces spp .; gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, as well as against Treponema spp., gonococci, meningococci and against spirochetes. Inactive against most gram-negative bacteria, rickettsiae, viruses, protozoa. Penicillinase-forming strains of microorganisms are resistant to the action of the drug. Decomposes in an acidic environment. The procaine salt of benzylpenicillin, in comparison with the potassium and sodium salts, is characterized by a longer duration of action.

Pharmacokinetics:
TCmax with i / m administration - 20-30 minutes. T1 / 2 30-60 minutes, with renal failure - 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, tissues of the eye and prostate with inflammation of the meningeal membranes, penetrates through the BBB. Excreted by the kidneys unchanged.

Indications:
Bacterial infections caused by susceptible pathogens: lobar and focal pneumonia, pleural empyema, bronchitis; sepsis, septic endocarditis (acute and subacute), peritonitis; meningitis; osteomyelitis; infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, blennorrhea, syphilis, cervicitis), biliary tract (cholangitis, cholecystitis); wound infection, skin and soft tissue infections: erysipelas, impetigo, secondarily infected dermatoses; diphtheria; scarlet fever; anthrax; actinomycosis; infections of the ENT organs and infections of the eyeball.

Contraindications:
Hypersensitivity; epilepsy (for endolumbar administration), hyperkalemia, arrhythmias (for potassium salt). Caution. Pregnancy, lactation.

Dosing regimen:
Benzylpenicillin sodium salt is administered intramuscularly, intravenously, s / c, endolumbally, intratracheally. In the moderate course of the disease (infection of the lower respiratory tract, urinary and biliary tract, soft tissue infection, etc.) - 4-6 million IU / day for 4 injections. In severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units / day; with gas gangrene - up to 40-60 million units / day. The daily dose for children under the age of 1 year is 50-100 thousand U / kg, over 1 year - 50 thousand U / kg; if necessary - 200-300 thousand U / kg, according to "vital" indications - an increase to 500 thousand U / kg. The frequency of administration is 4-6 times a day, i / v - 1-2 times a day in combination with i / m injections. Endolumbalno injected with purulent diseases of the brain and spinal cord and meninges. Depending on the disease and the severity of its course: adults - 5-10 thousand IU, children - 2-5 thousand IU 1 time per day for 2-3 days in / in, then prescribed in / m. For intravenous jet injection, a single dose (1-2 million units) is dissolved in 5-10 ml of sterile water for injection or 0.9% NaCl solution and injected slowly over 3-5 minutes. For intravenous drip, 2-5 million units are diluted with 100-200 ml of 0.9% NaCl solution or 5-10% dextrose solution and administered at a rate of 60-80 drops / min. When administered dropwise to children, a 5-10% dextrose solution is used as a solvent (30-100 ml, depending on the dose and age). Solutions are used immediately after preparation, avoiding the addition of other drugs to them. P / c is used for chipping infiltrates - 100-200 thousand units in 1 ml of a 0.25-0.5% solution of procaine. Endolumbal. The drug is diluted in sterile water for injection or in 0.9% NaCl solution at the rate of 1 thousand units / ml. Before injection (depending on intracranial pressure), 5-10 ml of CSF is removed and added to the antibiotic solution in equal proportions. Enter slowly (1 ml / min), usually 1 time per day for 2-3 days, then go to / in or / m injections. With suppurative processes in the lungs, a solution of the drug is administered intratracheally (after thorough anesthesia of the pharynx, larynx and trachea). Usually 100 thousand units are used in 10 ml of 0.9% NaCl solution. In eye diseases (acute conjunctivitis, corneal ulcer, gonoblenorrhea, etc.), eye drops containing 20-100 thousand units in 1 ml of 0.9% NaCl solution or distilled water are sometimes prescribed. Enter 1-2 drops 6-8 times a day. For ear drops or nose drops, solutions containing 10-100 thousand units / ml are used. Benzylpenicillin potassium salt is administered only in / m and s / c, in the same doses as benzylpenicillin sodium salt. Benzylpenicillin procaine salt is administered only in / m. The average therapeutic dose for adults: single - 300 thousand units, daily - 600 thousand units. The highest daily dose for adults is 1.2 million units. Children under the age of 1 year are prescribed 50-100 thousand U / kg / day, older than 1 year - 50 thousand U / kg / day. Frequency rate of introduction 1-2 times a day. The duration of treatment with benzylpenicillin, depending on the form and severity of the course of the disease, is 7-10 days.

Side effects:
Allergic reactions (hyperthermia, urticaria, skin rash, rash on mucous membranes, arthralgia, eosinophilia, angioedema, interstitial nephritis, bronchospasm); rarely - anaphylactic shock. At the beginning of the course of treatment (especially in the treatment of congenital syphilis), rarely - fever, chills, increased sweating, exacerbation of the disease, the Yarisch-Herxheimer reaction. For sodium salt - a decrease in the pumping function of the myocardium; for potassium salt - arrhythmias, cardiac arrest, hyperkalemia. With endolumbar administration - neurotoxic reactions: nausea, vomiting, increased reflex excitability, meningeal symptoms, convulsions, coma. Local reactions: soreness and induration at the injection site. With prolonged use: dysbacteriosis, the development of superinfection.

Special instructions:
Solutions of the drug for i / m administration are prepared ex tempore. If after 2-3 days (maximum 5 days) after the start of the drug, there is no effect, you should switch to the use of other antibiotics or combination therapy. In connection with the possibility of developing fungal infections, it is advisable to prescribe vitamins of group B and vitamin C, and, if necessary, nystatin and levorin during long-term treatment with benzylpenicillin. It should be borne in mind that the use of insufficient doses of the drug or too early termination of treatment often leads to the emergence of resistant strains of pathogens.

Interaction:
Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the prothrombin index); reduces the effectiveness of oral contraceptives, drugs, during the metabolism of which PABA is formed, ethinyl estradiol - the risk of bleeding "breakthrough". Diuretics, allopurinol, blockers of tubular secretion, phenylbutazone, NSAIDs, reducing tubular secretion, increase the concentration of benzylpenicillin. Allopurinol increases the risk of developing allergic reactions (skin rash).