Benzylpenicillin (Powder) Instructions for Use

ATC Code

J01CE01 (Benzylpenicillin)

Active Substance

Benzylpenicillin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Systemic antibacterial agents; beta-lactam antibacterial agents, penicillins; beta-lactamase sensitive penicillins

Pharmacological Action

An antibiotic from the group of biosynthetic penicillins. It exerts a bactericidal effect by inhibiting the synthesis of the microbial cell wall.

It is 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.

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

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

Pharmacokinetics

After intramuscular administration, it is rapidly absorbed from the injection site. It is widely distributed in body tissues and fluids. Benzylpenicillin penetrates well through the placental barrier and the blood-brain barrier when the meninges are inflamed.

The half-life (T_1/2) is 30 minutes. It is excreted in the urine.

Indications

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

ICD codes

Dosage Regimen

Powder

The dosage is individualized. It is administered intramuscularly, intravenously, subcutaneously, and intrathecally.

For intramuscular and intravenous administration in adults, the daily dose ranges from 250,000 to 60 million IU. The daily dose for children under 1 year of age 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, and for vital indications – up to 500,000 IU/kg. The frequency of administration is 4-6 times a day.

For intrathecal administration, depending on the disease and severity, adults receive 5,000-10,000 IU, children – 2,000-5,000 IU. The drug is dissolved in sterile water for injection or in 0.9% sodium chloride solution at the rate of 1 thousand IU/ml. Before injection (depending on the level of intracranial pressure), 5-10 ml of cerebrospinal fluid is withdrawn and added to the antibiotic solution in an equal ratio.

Subcutaneously, Benzylpenicillin is used for infiltrate block (100,000-200,000 IU in 1 ml of 0.25%-0.5% procaine solution).

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

The procaine salt of Benzylpenicillin is used only intramuscularly. The average therapeutic dose for adults: single dose – 300,000 IU, daily dose – 600,000 IU. For children under 1 year of age – 50,000-100,000 IU/kg/day, over 1 year – 50,000 IU/kg/day. The frequency of administration is 3-4 times a day.

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

Adverse Reactions

From the digestive system: diarrhea, nausea, vomiting.

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

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

Contraindications

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

Use in Pregnancy and Lactation

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

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

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Can be used in children according to indications.

Special Precautions

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

If no effect is observed 3-5 days after starting use, a switch to other antibiotics or combination therapy should be made.

Due to the possibility of fungal superinfection, it is advisable to prescribe antifungal drugs during treatment with benzylpenicillin.

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

Drug Interactions

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

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

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.