Benzylpenicillin - description of the drug, instructions for use, reviews

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Manufacturers: Biosynthesis

Active ingredients

• Benzylpenicillin

Disease class

• Acute and subacute endocarditis
• Nonspecific lymphadenitis
• Acute upper respiratory tract infection of multiple and unspecified localization
• Abscess of the lung and mediastinum
• Syndrome of staphylococcal skin lesions in the form of burn-like blisters
• Skin abscess, boil and carbuncle
• Other local infections of the skin and subcutaneous tissue
• Infectious myositis
• Tendon sheath abscess
• Other infectious (teno)synovitis
• Abscess of the bursa
• Other infectious bursitis
• Osteomyelitis
• Pleurisy
• Detection of other specified substances not normally present in the blood
• anthrax
• Other forms of tetanus
• Septicemia, unspecified
• Erysipelas
• Syphilis, unspecified
• Gonococcal infection
• Other and unspecified infectious diseases
• Inflammatory diseases of the female pelvic organs caused by syphilis (A51.4, A52.7)
• Gonococcal inflammatory diseases of the female pelvic organs

Clinical and pharmacological group

• Antibiotics of the penicillin group

Pharmacological action

• Antibacterial
• Bactericidal

Pharmacological group

• Penicillins

pharmachologic effect

Antibiotic of the group of biosynthetic penicillins. 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 bacilli, as well as Actinomyces spp., Spirochaetaceae.

Strains of Staphylococcus spp. that produce penicillinase are resistant to the action of benzylpenicillin. Destroys in an acidic environment.

The novocaine salt of benzylpenicillin, compared to the potassium and sodium salts, is characterized by a longer duration of action.

Drug interactions

Probenecid inhibits the tubular secretion of benzylpenicillin, thereby increasing the level of the latter in the blood plasma and increasing the half-life.

When combined with antibiotics that have a bacteriostatic effect (tetracycline, macrolides, lincosamides, chloramphenicol), the bactericidal effect of benzylpenicillin is reduced.

The drug enhances the effectiveness of indirect anticoagulants by reducing the prothrombin index and inhibiting intestinal microflora and makes the use of ethinyl estradiol less effective (risk of breakthrough bleeding), drugs in which the end product of metabolism is para-aminobenzoic acid, and oral contraceptives.

Nonsteroidal anti-inflammatory drugs, diuretics, phenylbutazone, tubular secretion blockers, allopurinol suppress tubular secretion, thereby increasing the concentration of benzylpenicillin when used together.

The combination of the drug with allopurinol increases the risk of allergic reactions (skin rashes). The combination of benzylpenicillin and bactericidal antibiotics (including aminoglycosides, cephalosporins, rifampicin, vancomycin) has a synergistic effect.

Contraindications

Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins.

Endolumbar administration is contraindicated in patients with epilepsy.

Carefully:

Renal dysfunction.

Heart failure.

Predisposition to allergic reactions (especially with drug allergies).

Hypersensitivity to cephalosporins (due to the possibility of developing cross-allergy).

Use during pregnancy and breastfeeding.

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

If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.

Indications for use of Benzylpenicillin

The instructions for benzylpenicillin indicate that the drug is indicated for infectious and inflammatory diseases such as:

• pleural empyema, community-acquired pneumonia, bronchitis - respiratory diseases;
• diseases of the ENT organs;
• cholecystitis, cholangitis - biliary tract;
• pyelitis, cervicitis, pyelonephritis, urethritis, cystitis - genitourinary system;
• impetigo, wound infection, secondary infected dermatoses, erysipelas - soft tissues and skin;
• peritonitis;
• ulcer of the cornea, gonoblennorrhea - organs of vision;
• acute and subacute septic endocarditis, sepsis;
• syphilis and gonorrhea;
• osteomyelitis;
• anthrax;
• diphtheria;
• actinomycosis;
• meningitis;
• scarlet fever.

special instructions

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

If no effect is observed 3-5 days after the start of use, you should move on to the use of other antibiotics or combination therapy.

Due to the possibility of developing fungal superinfection, it is advisable to prescribe antifungal drugs when treating with benzylpenicillin.

It must be taken into account that the use of benzylpenicillin in subtherapeutic doses or early cessation of treatment often leads to the emergence of resistant strains of pathogens.

Pharmacodynamics and pharmacokinetics

Benzylpenicillin is a biosynthetic antibiotic and belongs to the group of penicillins . The bactericidal effectiveness of the drug is manifested due to its ability to inhibit the synthesis of bacterial cell .

The effect of the drug is detrimental to gram-positive microorganisms: staphylococci , causative agents of diphtheria and anthrax , streptococci ; gram-negative bacteria: pathogens of gonorrhea and meningococcal infection ; spore-forming anaerobic rods; as well as spirochetes and actinomycetes .

Strains of staphylococci that produce penicillinase are not sensitive to the effects of benzylpenicillin .

When the drug is administered intramuscularly, TCmax in plasma is observed after 20-30 minutes. Binding to plasma proteins occurs by 60%. The antibiotic has good penetration into tissues, biological fluids and organs of the human body, with the exception of cerebrospinal fluid , prostate gland and eye tissues, and passes through the BBB . Excretion is carried out in unchanged form by the kidneys. T1/2 fluctuates between 30-60 minutes, with kidney pathologies it can increase to 4-10 hours or even more.

Directions for use and doses

Individual. Injected intramuscularly, intravenously, subcutaneously, endolumbarally.

When administered intramuscularly and intravenously to adults, the daily dose varies from 250,000 to 60 million units. The daily dose for children under 1 year of age is 50,000-100,000 units/kg, over 1 year - 50,000 units/kg, if necessary, the daily dose can be increased to 200,000-300,000 units/kg, for health reasons - up to 500,000 units/kg. Frequency of administration 4-6 times/day.

Depending on the disease and severity, adults are administered endolumbarally - 5000-10,000 units, children - 2000-5000 units. 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.

Subcutaneous benzylpenicillin is used to inject infiltrates (100,000-200,000 units in 1 ml of 0.25%-0.5% novocaine solution).

Benzylpenicillin potassium salt is used only intramuscularly and subcutaneously, in the same doses as benzylpenicillin sodium salt.

Benzylpenicillin novocaine salt is used only intramuscularly. Average therapeutic dose for adults: single - 300,000 units, daily - 600,000 units. Children under 1 year of age - 50,000-100,000 units/kg/day, over 1 year of age - 50,000 units/kg/day. Frequency of administration 3-4 times/day.

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

Instructions for use of Benzylpenicillin: method and dosage

The dosage of benzylpenicillin is determined by the type and severity of the infection.

Approximate recommended doses:

• Adults: 1800-3600 mg (3-6 million IU) per day, divided into 4-6 doses. For severe infections (septicemia, meningitis), the dosage is calculated based on weight - up to 200-300 mg/kg (330-500 thousand IU/kg) per day. In this case, therapy should begin with a slow intravenous injection or with a rapid infusion, using 5% glucose as a diluent;
• Children: at the rate of 30-90 mg/kg (50-150 thousand IU/kg) per day in 4-6 divided doses. For severe infections, the dosage can be increased to 300 mg/kg (500 thousand IU/kg).

Benzylpenicillin can also be used intramuscularly, diluting the drug immediately before use, since its activity in infusion solutions quickly decreases. The duration of therapy is determined by the indications and clinical picture.

Recommended dosages for specific diseases are:

• Septicemia and meningitis caused by meningococci: for at least 5 days as a slow intravenous injection or infusion of 180-240 mg/kg (300-400 thousand IU/kg) per day in 4-6 divided doses;
• Septicemia and meningitis caused by pneumococci: for at least 10 days as a slow intravenous injection or infusion of 240-300 mg/kg (400-500 thousand IU/kg) per day in 4-6 divided doses;
• Infections caused by clostridia: for 7 days as an addition to antitoxin therapy, 9,000-12,000 mg (15-20 million IU) per day for adults and 180 mg/kg (300 thousand IU/kg) for children;
• Streptococcal endocarditis: for 14-28 days, 6,000-12,000 mg (10-20 million IU) per day for adults and 180 mg/kg (300 thousand IU/kg) for children;
• Congenital syphilis: in 2 doses for 14 days, intramuscularly or intravenously, 30 mg/kg (50 thousand IU/kg) per day.

Side effects

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 fatal outcome have been described.

Overdose

In case of overdose of benzylpenicillin, its toxic effect on the central nervous system was noted (mainly when administered endolumbarally). The observed symptoms were manifested by reflex agitation , nausea, headaches , myalgia , vomiting, convulsions , meningism , arthralgia, coma .

In this situation, further injections are stopped and symptomatic treatment is prescribed, including hemodialysis . In this case, special attention is paid to the water-electrolyte state.

Pharmacological properties of the drug Benzylpenicillin

Pharmacodynamics. Benzylpenicillin has a bactericidal effect. Mechanism of action: the drug prevents the formation of peptide bonds by inhibiting transpeptidase, disrupts the late stages of cell wall peptidoglycan synthesis, which leads to lysis of dividing bacterial cells. Active against gram-positive microorganisms ( Staphylococcus spp., Streptococcus spp ., including S. pneumoniae; Corynebacterium diphtheriae, Bacillus anthracis, some gram-negative microorganisms, including Neisseria gonorrhoeae, N. meningitidis ), anaerobic spore-forming bacilli, as well as Actinomeces spp ., Spirochaetaceae . The drug is inactive against most gram-negative bacteria, rickettsia, viruses, protozoa, and 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 administration, the maximum concentration of the drug in the blood is achieved after 30–60 minutes; 3–4 hours after a single injection, trace concentrations of the antibiotic are determined 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. Binding to blood proteins is 60%. The antibiotic penetrates well into organs, tissues and body fluids, with the exception of cerebrospinal fluid, eye tissue and prostate, but with inflammation of the meninges, its concentration in the CSF increases. The half-life is 30-60 minutes, in case of impaired renal function - 4-10 hours, and in case of simultaneous impairment of liver and kidney function - up to 16-30 hours. It is quickly excreted from the body by the kidneys by glomerular filtration and tubular secretion unchanged. It is excreted in small quantities with saliva, sweat, milk, and bile. Does not have a cumulative effect.

Side effects of the drug Benzylpenicillin

When the drug is administered, allergic reactions are possible - skin rash, urticaria, fever, chills, headache, arthralgia, eosinophilia, Quincke's edema, interstitial nephritis, impaired pumping function of the myocardium. In some cases, anaphylactic shock may develop. Endolumbar administration may be accompanied by neurotoxic effects (nausea, vomiting, symptoms of meningism, convulsions). In weakened patients, newborns, and the elderly, during long-term treatment, superinfection may occur caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms).

Benzylpenicillin

Pharmacological properties

Pharmacodynamics

Benzylpenicillin has a bactericidal effect. Mechanism of action: the drug prevents the formation of peptide bonds by inhibiting transpeptidase, disrupts the late stages of cell wall peptidoglycan synthesis, which leads to lysis of dividing bacterial cells.

Active against gram-positive microorganisms ( Staphylococcus spp., Streptococcus spp

., including
S. pneumoniae;
Corynebacterium diphtheriae, Bacillus anthracis, some gram-negative microorganisms, including
Neisseria gonorrhoeae, N. meningitidis
), anaerobic spore-forming rods, as well as
Actinomeces spp., Spirochaetaceae
.

The drug is inactive against most gram-negative bacteria, rickettsia, viruses, protozoa, and 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 administration, the maximum concentration of the drug in the blood is achieved after 30–60 minutes; 3–4 hours after a single injection, trace concentrations of the antibiotic are determined 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. Binding to blood proteins is 60%. The antibiotic penetrates well into organs, tissues and body fluids, with the exception of cerebrospinal fluid, eye tissue and prostate, but with inflammation of the meninges, its concentration in the CSF increases. The half-life is 30-60 minutes, in case of impaired renal function - 4-10 hours, and in case of simultaneous impairment of liver and kidney function - up to 16-30 hours. It is quickly excreted from the body by the kidneys by glomerular filtration and tubular secretion unchanged. It is excreted in small quantities with saliva, sweat, milk, and bile. Does not have a cumulative effect.

Indications

Infections caused by sensitive microorganisms: tonsillitis, pneumonia, septic endocarditis, purulent pleurisy, peritonitis, cystitis, sepsis, meningitis, osteomyelitis, urinary and biliary tract infections, wound infections, purulent infections of the skin, soft tissues, diphtheria, scarlet fever, erysipelas, anthrax, syphilis, gonorrhea, pulmonary actinomycosis, colpitis, endocervicitis, endometritis, adnexitis, salpingo-oophoritis, conjunctivitis, blepharitis, dacryocystitis.

Application

Before administration, it is necessary to conduct an intradermal test to determine the tolerability of the drug, provided there are no contraindications to its implementation.

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

IV: for moderate infections, a single dose of the drug for adults is usually 250,000–500,000 units, daily - 1,000,000–2,000,000 units; for severe infections, up to 10,000,000–20,000,000 units/day are administered, with gas gangrene - up to 40,000,000–60,000,000 units. Typically, the daily dose for children under 1 year of age is 50,000–100,000 units/kg, over 1 year of age - 50,000 units/kg, if necessary, the daily dose can be increased to 200,000–300,000 units/kg, according to vital signs - up to 500,000 units/kg. The frequency of administration of the drug is 4–6 times a day.

Benzylpenicillin solution is prepared immediately before its use.

For IV jet administration

a single dose (1,000,000–2,000,000 units) of the drug is 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 administration, 2,000,000–5,000,000 units of antibiotic are 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 minute.

The drug is administered intravenously 1–2 times a day, combined with intramuscular administration.

V/m

: for moderate infections, a single dose of the drug for adults is usually 250,000-500,000 units, daily - 1,000,000-2,000,000 units, for severe infections up to 10,000,000-20,000,000 units per day are administered, for gas gangrene - up to 40,000,000–60,000,000 units. Typically, the daily dose for children under 1 year of age is 50,000–100,000 units/kg, over 1 year of age - 50,000 units/kg, if necessary, the daily dose can be increased to 200,000–300,000 units/kg, according to vital signs - up to 500,000 units/kg. The frequency of administration of the drug is 4–6 times a day.

For intramuscular administration, add 1–3 ml of sterile water for injection or 0.9% sodium chloride solution, or 0.5% procaine solution to the contents of the bottle. The resulting solution is injected deep into the muscle in the upper outer quadrant of the buttock.

PC:

Benzylpenicillin is used to inoculate infiltrates at a concentration of 100,000–200,000 units in 1 ml of 0.25–0.5% procaine solution.

In the cavity (abdominal, pleural, etc.), benzylpenicillin solution is administered to adults at a concentration of 10,000–20,000 units per 1 ml, for children - 2000–5,000 units per 1 ml. Dissolve in sterile water for injection or 0.9% sodium chloride solution. The duration of treatment is 5–7 days, followed by a transition to intramuscular administration.

Intrathecal (endolumbar)

: the drug is administered for purulent diseases of the brain, spinal cord, meninges. Adults are prescribed a dose of 5000–10,000 units; children over 1 year of age - 2000-5000 units, administered slowly - 1 ml/min 1 time per day. The drug is diluted in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1000 units per 1 ml. Before injection, 5–10 ml of CSF 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 administration.

Treatment of patients with syphilis and gonorrhea is carried out according to specially developed regimens.

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.).

Contraindications

Patients with hypersensitivity to beta-lactam antibiotics, asthma, hay fever, urticaria and other allergic diseases. Epilepsy is a contraindication for endolumbar administration.

Side effects

When the drug is administered, allergic reactions are possible - skin rash, urticaria, fever, chills, headache, arthralgia, eosinophilia, Quincke's edema, interstitial nephritis, impaired pumping function of the myocardium. In some cases, anaphylactic shock may develop. Endolumbar administration may be accompanied by neurotoxic effects (nausea, vomiting, symptoms of meningism, convulsions).

In weakened patients, newborns, and the elderly, during long-term treatment, superinfection may occur caused by drug-resistant microflora (yeast-like fungi, gram-negative microorganisms).

special instructions

Benzylpenicillin solutions are used immediately after preparation. It is not allowed to add any other medicines to the drug solutions. The use of the drug is possible only in pathological processes caused by microorganisms sensitive to it. When pathogen resistance to the drug appears, it is replaced with other antibiotics. If there is no effect from the use of the drug 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 the severity of side effects should be taken into account. Patients over 60 years of age and pregnant women are not recommended to prescribe the drug in high doses.

When benzylpenicillin is dissolved in a procaine solution, a cloudy solution may form due to the formation of benzylpenicillin procaine salt, which is not an obstacle to intramuscular administration of the drug.

During pregnancy and breastfeeding. During pregnancy

use is possible only when the intended therapeutic effect for the mother outweighs the potential risk to the fetus. If it is necessary to use it during breastfeeding, the issue of stopping breastfeeding should be decided.

The drug does not affect the ability to drive vehicles.

Interactions

The effect of the drug is weakened by antimicrobial agents that have a bacteriostatic effect (tetracycline). Probenecid reduces the tubular secretion of benzylpenicillin, thereby increasing the concentration of the latter in the blood plasma and increasing the half-life.

Overdose

It manifests itself as a toxic effect on the central nervous system (more often with endolumbar administration). Convulsions, headache, myalgia, arthralgia occur. In such cases, administration of the drug should be stopped. Treatment is symptomatic.

Storage conditions

In a dry place at a temperature of 15–20 °C.

Price, where to buy

The price for benzylpenicillin sodium salt, 1,000,000 units, is 6-7 rubles per bottle.

• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

PaniPharmacy

• Benzylpenicillin bottle Benzylpenicillin sodium salt powder for injection 1000000IU Ukraine, Kievmedpreparat OJSC
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Reviews

On various Internet resources you can find both negative and positive reviews about benzylpenicillin sodium salt . When the drug is used against microorganisms , the treatment almost always shows good results and, on the contrary, when using Benzylpenicillin to destroy strains of bacteria , at best, it is wasted. In this regard, for any bacterial infection causative agent before starting therapy and only then prescribe an antibiotic .