Benzylpenicillin novocaine (Powder) Instructions for Use

Marketing Authorization Holder

Sintez PJSC (Russia)

ATC Code

J01CE09 (Benzylpenicillin procaine)

Active Substance

Procaine benzylpenicillin

Dosage Form

Benzylpenicillin novocaine

Powder for suspension for intramuscular administration 600,000 IU: vial 1 or 10 pcs.

Dosage Form, Packaging, and Composition

Powder for preparation of suspension for intramuscular administration white in color, prone to clumping.

* benzylpenicillin procaine (benzylpenicillin novocaine salt).

Colorless glass vials (1) – cardboard packs.
Colorless glass vials (10) – cardboard packs.

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

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

Pharmacological Action

Bactericidal antibiotic from the group of biosynthetic penicillins. It suppresses 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.

It is not active against most gram-negative bacteria, rickettsiae, viruses, protozoa. Strains of microorganisms that produce penicillinase are resistant to the action of procaine 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, T_max is 20-30 min. T_1/2 is 30-60 min, in renal failure – 4-10 h or more. Plasma protein binding is 60%. It penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissue and prostate. It penetrates the blood-brain barrier when the meninges are inflamed. It is excreted by the kidneys unchanged.

Indications

Infectious and inflammatory diseases 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, infections of the skin and soft tissues: erysipelas, impetigo, secondarily infected dermatoses; diphtheria; scarlet fever; anthrax; actinomycosis; ENT diseases, eye diseases.

ICD codes

Dosage Regimen

It is administered intramuscularly.

Intravenous and endolumbar administration is prohibited.

The average therapeutic dose for adults: single – 300,000 IU, daily – 600,000 IU. The maximum daily dose for adults is 1,200,000 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 1-2 times/day.

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

Adverse Reactions

Allergic reactions hyperthermia, urticaria, skin rash, rash on mucous membranes, arthralgia, eosinophilia, angioedema, interstitial nephritis, bronchospasm; rarely – anaphylactic shock

Local reactions: pain and induration at the injection site.

If it enters the vascular bed tinnitus, visual impairment, fear, dizziness, short-term loss of consciousness.

When administered in high doses neurotoxic phenomena are possible – nausea, vomiting, increased reflex excitability, symptoms of meningism, convulsions, coma.

Contraindications

Hypersensitivity to the group of penicillins, allergy to procaine.

Use in Pregnancy and Lactation

Use with caution during pregnancy and during lactation (breastfeeding).

Use in Hepatic Impairment

The drug is approved for use in impaired liver function

Special Precautions

With caution: bronchial asthma, hay fever and other allergic diseases, decreased blood clotting activity, pregnancy, lactation period, renal failure.

If no effect is noted 2-3 days (maximum 5 days) after starting the drug, it is necessary to switch to the use of other antibiotics or combination therapy.

Due to the possibility of developing fungal lesions, it is advisable during long-term treatment with benzylpenicillin to prescribe B vitamins and vitamin C, and if necessary, nystatin and levorin.

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

When treating venereal diseases, if syphilis is suspected, before starting therapy and then for 4 months, it is necessary to conduct microscopic and serological studies.

If any allergic reaction occurs, immediate discontinuation of treatment is required.

Drug Interactions

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) act synergistically with procaine benzylpenicillin. Bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect.

It increases the effectiveness of indirect anticoagulants (by suppressing the intestinal microflora, it 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, NSAIDs, by reducing tubular secretion, increase the concentration of benzylpenicillin.

Allopurinol increases the risk of allergic reactions (skin rash).

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.