Benzylpenicillin dilution. Benzylpenicillin - instructions for use

Benzylpenicillin- antimicrobial agent for systemic use,
antibacterial, bactericidal.
Violates the synthesis of peptidoglycan of the cell wall and causes lysis of microorganisms.
Active against gram-positive bacteria (Staphylococcus spp. strains that do not form penicillinase, Streptococcus spp., including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods, anthrax rods, Actinomyces spp., as well as against gram-negative cocci (Neisseria meningitidis, Neisseria gonorrhoeae ), Treponema spp., Spirochaeta spp. Not effective against most gram-negative bacteria, rickettsiae, viruses, protozoa, fungi.
With the / m administration of sodium and potassium salts of benzylpenicillin, Cmax in the blood is reached after 30-60 minutes, after 3-4 hours traces of the antibiotic are found in the blood. Benzylpenicillin novocaine salt is slowly absorbed and has a prolonged effect; after a single injection in the form of a suspension, the therapeutic concentration of penicillin in the blood lasts up to 12 hours. Binding to blood proteins is 60%. It penetrates well into organs, tissues and biological fluids, with the exception of cerebrospinal fluid, prostate. With inflammation of the meninges, it passes through the BBB. When instilled into the conjunctival sac in therapeutic concentrations, it is found in the stroma of the cornea (practically does not penetrate into the moisture of the anterior chamber when applied topically). Therapeutic concentrations in the cornea and moisture of the anterior chamber are created with subconjunctival administration (in this case, the concentration in the vitreous body does not reach the therapeutic level). With intravitreal administration, T1 / 2 is about 3 hours. It is excreted by the kidneys by glomerular filtration (approximately 10%) and tubular secretion (90%) unchanged. In newborns and infants, excretion slows down, with renal failure T1 / 2 increases to 4-10 hours.

Indications for use

Mode of application

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.).

Side effects

Contraindications

Pregnancy

Interaction with other drugs

Overdose

Storage conditions

Release form:
Benzylpenicillin - powder for solution for injection. 500,000 IU or 1,000,000 IU in vials; in bottles No. 10 in a pack.

Compound

Main settings

Structural formula

Russian name

Latin name of the substance benzylpenicillin

chemical name

3,3-Dimethyl-7-oxo-6-[(phenylacetyl)amino]-4-thia-1-azabicycloheptane-2-carboxylic acid (and as sodium, potassium or novocaine salt)

Gross formula

Pharmacological group of the substance Benzylpenicillin

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Benzylpenicillin

Natural antibiotic of the penicillin group. Acid-resistant, destroyed by beta-lactamase (penicillinase).

In medical practice, benzylpenicillin sodium, potassium and novocaine salt are used.

Benzylpenicillin sodium salt is a white, finely crystalline powder with a bitter taste. Slightly hygroscopic. Very easily soluble in water, soluble in ethanol and methanol. Easily destroyed by acids, alkalis and oxidizing agents. Introduced in / m, in / in, s / c, endolumbally, intratracheally.

Benzylpenicillin potassium salt is a white, finely crystalline powder with a bitter taste. Hygroscopic. Very easily soluble in water, soluble in ethanol and methanol. Easily destroyed by acids, alkalis, oxidizing agents. Enter in / m, s / c.

Benzylpenicillin novocaine salt is a white, odorless, finely crystalline powder, bitter in taste. Hygroscopic. Slightly soluble in water, ethanol and methanol. We will hardly dissolve in chloroform. Forms a thin suspension with water. Resistant to light. Easily destroyed by the action of acids and alkalis. Enter only in / m.

Pharmacology

Violates the synthesis of peptidoglycan of the cell wall and causes lysis of microorganisms.

Active against gram-positive bacteria (strains Staphylococcus spp. do not form penicillinase, Streptococcus spp., including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods, anthrax rods, Actinomyces spp., as well as in relation to gram-negative cocci ( Neisseria meningitidis, Neisseria gonorrhoeae), Treponema spp., Spirochaeta spp. Not effective against most gram-negative bacteria, rickettsiae, viruses, protozoa, fungi.

With the / m administration of sodium and potassium salts of benzylpenicillin, Cmax in the blood is reached after 30-60 minutes, after 3-4 hours traces of the antibiotic are found in the blood. Benzylpenicillin novocaine salt is slowly absorbed and has a prolonged effect; after a single injection in the form of a suspension, the therapeutic concentration of penicillin in the blood lasts up to 12 hours. Binding to blood proteins is 60%. It penetrates well into organs, tissues and biological fluids, with the exception of cerebrospinal fluid, prostate. With inflammation of the meninges, it passes through the BBB. When instilled into the conjunctival sac in therapeutic concentrations, it is found in the stroma of the cornea (practically does not penetrate into the moisture of the anterior chamber when applied topically). Therapeutic concentrations in the cornea and moisture of the anterior chamber are created with subconjunctival administration (in this case, the concentration in the vitreous body does not reach the therapeutic level). With intravitreal administration, T 1/2 is about 3 hours. It is excreted by the kidneys by glomerular filtration (approximately 10%) and tubular secretion (90%) unchanged. In newborns and infants, excretion slows down, with renal failure T 1/2 increases to 4-10 hours.

Application of the substance Benzylpenicillin

Bacterial infections caused by susceptible pathogens: lobar and focal pneumonia, pleural empyema, bronchitis; septic endocarditis (acute and subacute), wound infection, purulent infections of the skin, soft tissues and mucous membranes (including erysipelas, impetigo, secondarily infected dermatoses), purulent pleurisy, peritonitis, sepsis, osteomyelitis, infections of ENT organs (angina ), meningitis, diphtheria, gas gangrene, scarlet fever, gonorrhea, leptospirosis, syphilis, anthrax, lung actinomycosis, infections of the urinary and biliary tract, treatment of pyoinflammatory diseases in obstetric and gynecological practice, eye diseases (including acute gonococcal conjunctivitis, corneal ulcer, gonoblenorrhea).

Contraindications

Hypersensitivity, incl. to other penicillins; epilepsy (for endolumbar administration), hyperkalemia, arrhythmia (for potassium salt).

Application restrictions

Bronchial asthma, pollinosis, renal failure.

Use during pregnancy and lactation

During pregnancy, it is possible if the intended benefit to the mother outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Side effects of the substance benzylpenicillin

Allergic reactions: anaphylactic shock, urticaria, angioedema, fever/chills, headache, arthralgia, eosinophilia, interstitial nephritis, bronchospasm, skin rashes.

Others: for sodium salt - violation of myocardial contractility; for potassium salt - arrhythmia, cardiac arrest, hyperkalemia.

With endolumbar administration - neurotoxic reactions: nausea, vomiting; increased reflex excitability, meningeal symptoms, convulsions, coma.

Interaction

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) - synergistic action, bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonism. Diuretics, allopurinol, blockers of tubular secretion, NSAIDs reduce tubular secretion, increase the concentration of benzylpenicillin. Allopurinol increases the risk of developing allergic reactions (skin rash).

Overdose

Symptoms: convulsions, impaired consciousness.

Treatment: drug withdrawal, symptomatic therapy.

Routes of administration

In / m, in / in, s / c, endolumbally, in the cavity, intratracheally; instillations into the conjunctival sac, subconjunctival, intravitreal.

Precautions of substance Benzylpenicillin

In / in, endolumbally and into the cavity is administered only in a hospital setting.

It is necessary to use benzylpenicillin preparations only as directed and under medical supervision. It must be remembered that the use of insufficient doses of benzylpenicillin (as well as other antibiotics) or too early termination of treatment often leads to the development of resistant strains of microorganisms. If resistance occurs, treatment with another antibiotic should be continued.

Benzylpenicillin novocaine salt is administered only in / m. In / in and endolumbar introduction is not allowed. Of all benzylpenicillin preparations, only the sodium salt is administered endolumbally.

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 the 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 administration, 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.

Shelf life

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.

Instructions for medical use

medicinal product

Benzylpenicillin

Tradename

Benzylpenicillin

International non-proprietary name

Benzylpenicillin

Dosage form

Powder for solution for intravenous and intramuscular administration 1000000 IU

Compound

One vial contains:

Description

White or almost white fine crystalline powder with a slight characteristic odor.

Pharmacotherapeutic group

Beta-lactam antibiotics - penicillins.

Penicillins penicillinase - sensitive. Benzylpenicillin

ATX code J01SE01

Pharmacological properties

Pharmacokinetics

The maximum concentration in blood plasma when administered intramuscularly is reached after 20-30 minutes. The half-life of the drug is 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, eye tissues and prostate. With inflammation of the meningeal membranes, the permeability

across the blood-brain barrier increases. Passes through the placenta and passes into breast milk. Excreted by the kidneys unchanged.

Pharmacodynamics

Bactericidal antibiotic from the group of biosynthetic ("natural") penicillins. Inhibits the synthesis of the cell wall of microorganisms.

Active against gram-positive pathogens: Staphylococcus spp. (non-forming penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis, Actinomyces spp.; gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, as well as against Treponema spp .. Inactive against most gram-negative bacteria, rickettsia, viruses, protozoa.

Penicillinase-forming strains of microorganisms are resistant to the action of the drug. Decomposes in an acidic environment.

Indications for use

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 infections (cholangitis, cholecystitis)
• wound infection
• skin and soft tissue infections: erysipelas, impetigo, secondarily infected dermatoses
• diphtheria
• scarlet fever
• anthrax
• actinomycosis
• ENT infections
• eyeball infections

Dosage and administration

The drug is intended for intramuscular, intravenous, subcutaneous, endolumbar and intratracheal administration.

In the moderate course of the disease (infections of the lower respiratory tract, urinary and biliary tract, soft tissue infections, etc.) - 4-6 million units / day for 4 injections.

In severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units per day; with gas gangrene - up to 40-60 million units.

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 - 200,000-300,000 U / kg, according to vital indications - an increase to 500,000 U / kg. The frequency of administration - 4-6 times a day, intravenously - 1 - 2 times a day in combination with intramuscular 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 units, children - 2-5 thousand units 1 time per day for 2-3 days intravenously, then administered intramuscularly.

For intravenous jet administration, a single dose (1-2 million units) 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 administration of 2-5 million units, dilute 100-200 ml of 0.9% sodium chloride solution or 5-10% dextrose solution and inject at a rate of 60-80 drops / min.

With drip administration to children, a 5-10% dextrose solution is used as a solvent (100-300 ml, depending on the dose and age).

A solution of the drug for intramuscular administration is prepared immediately before administration by adding 1-3 ml of water for injection or 0.9% sodium chloride solution or 0.5% novocaine solution to the contents of the vial.

Solutions are used immediately after preparation, avoiding the addition of other drugs to them.

Subcutaneously, the drug is used for chipping infiltrates at a concentration of 100-200 thousand units in 1 ml of 0.25-0.5% novocaine solution.

Preparation of a solution of the drug for endolumbar use: dilute the drug in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1 thousand units / ml. Before injection (depending on intracranial pressure), 5-10 ml of cerebrospinal fluid 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 proceed to intravenous or intramuscular injections.

In 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% sodium chloride solution.

For eye diseases (acute conjunctivitis, corneal ulcer, gonoblenorrhea and others), eye drops containing 20-100 thousand units in 1 ml of 0.9% sodium chloride solution or distilled water are 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.

The duration of treatment with the drug, depending on the form and severity of the course of the disease, is from 7-10 days to 2 months or more (for example, with sepsis, septic endocarditis).

Side effects

Arrhythmias, cardiac arrest, congestive heart failure (because high doses may cause hypernatremia)

Nausea, vomiting, stomatitis, glossitis, abnormal liver function

Impaired kidney function

Anemia, leukopenia, thrombocytopenia

Increased reflex excitability, meningeal symptoms, convulsions, coma

- allergic reactions: hyperthermia, urticaria, skin rash, fever, chills, increased sweating, rash on mucous membranes, arthralgia, eosinophilia, angioedema, interstitial nephritis, bronchospasm, angioedema

Rarely

Anaphylactic shock

Superinfection caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms)

- local reactions: soreness and induration at the site of intramuscular injection

Contraindications

Hypersensitivity (including to other β-lactam

antibiotics) to the drug

Urticaria, bronchial asthma

Endolumbar injection in epilepsy.

Carefully

• kidney failure.

Drug Interactions

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, in the process of metabolism of which para-aminobenzoic acid is formed, ethinyl estradiol - the risk of developing breakthrough bleeding.

Diuretics, allopurinol, tubular secretion blockers, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing tubular secretion, increase the concentration of benzylpenicillin.

Allopurinol, when used together, increases the risk of developing allergic reactions (skin rash).

special instructions

Solutions of the drug for all routes of administration are prepared ex tempore.

If after 2-3 (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 debilitated patients, newborns, people

the elderly with long-term treatment may develop superinfection caused by drug-resistant microflora (yeast-like

fungi, Gram-negative bacteria).

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. If resistance occurs, treatment with another antibiotic should be continued.

Pregnancy and lactation

Use during pregnancy is possible if the intended benefit to the mother outweighs the potential risk to the fetus.

If necessary, use during lactation should decide on the termination of breastfeeding (penetrates into breast milk in low concentrations).

Features of the influence of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

Does not affect.

Overdose

Benzylpenicillin is an antibiotic from the group of biosynthetic penicillins. The drug has a bactericidal effect, inhibiting the synthesis of the cell wall of microorganisms.

Release form and composition

Benzylpenicillin is available in the form of a white crystalline powder for solution for injection. The powder has a slight characteristic odor. One vial contains benzylpenicillin sodium salt 125,000, 250,000, 500,000 or 1,000,000 IU.

Indications for use

The drug is prescribed for diseases caused by microorganisms that are sensitive to benzylpenicillin:

• Sepsis;
• Focal and croupous pneumonia;
• Pyemia;
• Septicemia;
• Pleural empyema;
• Meningitis;
• Septic endocarditis (acute and subacute);
• Infections of the biliary and urinary tract;
• Chronic and acute osteomyelitis;
• Angina;
• Diphtheria;
• erysipelas;
• Scarlet fever;
• actinomycosis;
• Gonorrhea;
• Syphilis;
• Blennorea;
• ENT diseases;
• Anthrax;
• eye diseases;
• Purulent infections of soft tissues, skin and mucous membranes;
• Purulent-inflammatory diseases in obstetric and gynecological practice.

Contraindications

A contraindication to the use of benzylpenicillin is hypersensitivity to the drug and other antibiotics from the group of cephalosporins and penicillins.

In patients with epilepsy, benzylpenicillin should not be administered endolumbally.

Method of application and dosage

The dosage regimen of the drug is individual. According to the instructions, Benzylpenicillin is administered intravenously, intramuscularly, subcutaneously and endolumbally.

The daily dose for adults (with intramuscular and intravenous administration) varies in the range of 250,000-60,000,000 IU, for babies up to a year - from 50,000 to 100,000 IU / kg, for children over one year old - 50,000 IU / kg of body weight. If necessary, you can increase the daily dose to 200,000-300,000 IU / kg, and for health reasons, up to 500,000 IU / kg. As a rule, the frequency of administration of the drug varies from 4 to 6 times a day.

The dosage of benzylpenicillin with the endolumbar route of administration depends on the disease and the severity of its course. Adults are prescribed 5000-10000 IU, children - from 2000 to 5000 IU. The powder is diluted in 0.9% NaCl solution or in special sterile water for injection at the rate of 1000 IU / ml. Immediately before the injection, 5 to 10 ml of cerebrospinal fluid is removed, which is added to the antibiotic solution in a 1:1 ratio.

For chipping infiltrates, Benzylpenicillin is used subcutaneously at the rate of 100,000-200,000 IU per 1 ml of novocaine solution of 0.25-0.5% concentration.

The duration of treatment depends on the severity of the course and the form of the disease. On average, it ranges from 7-10 days to two months, and sometimes more.

Side effects

When using benzylpenicillin, the following side effects may occur:

• Nausea, vomiting and diarrhea from the digestive system;
• Candidiasis of the oral cavity and vagina, due to the chemotherapeutic effect of the drug;
• Increased reflex excitability, symptoms of meningism, convulsive conditions and even coma from the side of the central nervous system;
• Rash on the skin and mucous membranes, joint pain, fever, urticaria, angioedema, eosinophilia and other allergic reactions up to fatal anaphylactic shock.

special instructions

Caution requires the use of benzylpenicillin in persons with heart failure and impaired renal function, as well as with a predisposition to allergies (especially medicinal).

In the absence of a therapeutic effect, 3-5 days after the start of treatment, you should turn to combination therapy or change the antibiotic.

When using benzylpenicillin, it is advisable to prescribe antifungal drugs because of the high likelihood of developing fungal superinfection.

It is necessary to strictly adhere to the dosages and duration of treatment indicated in the instructions for benzylpenicillin, since subtherapeutic doses or early termination of therapy can lead to the emergence of resistant strains of microorganisms.

Analogues

Structural analogues of the drug are:

• Benzylpenicillin novocaine salt;
• Penicillin G sodium salt;
• Benzylpenicillin-KMP.

Terms and conditions of storage

According to the instructions, benzylpenicillin should be stored in a dry place, protected from direct sunlight, at a temperature not exceeding 10 ° C. The shelf life of the antibiotic is 2 years.