Benzathine Penicillin

Indications
 Intramuscular
Syphilis
Adult: Early syphilis: A single dose of 1.8 g, usually as 2 inj in separate sites. Late syphilis: 1.8 g at wkly intervals for 3 consecutive wk.
Intramuscular
Treponemal infections
Adult: 900 mg as a single dose.
Child: 450 mg as a single dose.
Intramuscular
Streptococcal pharyngitis
Adult: 900 mg as a single dose. To prevent recurrences of acute rheumatic fever: 900 mg every 3-4 wk.
Child: <30 kg: 225-675 mg as a single dose. To prevent recurrences of acute rheumatic fever: <30 kg: 450 mg every 3-4 wk.
Intramuscular
Primary prophylaxis of rheumatic fever
Adult: 900 mg as a single dose. To prevent recurrences of acute rheumatic fever: 900 mg every 3-4 wk.
Child: <30 kg: 225-675 mg as a single dose. To prevent recurrences of acute rheumatic fever: <30 kg: 450 mg every 3-4 wk.
Intramuscular
Congenital syphilis
Child: Infants up to 2 yr: 37.5 mg/kg/day as a single dose.
Contraindications
 Hypersensitivity to penicillins or cephalosporins. IM inj (ischaemic reactions may occur).
Warnings / Precautions
 Very high doses in poor renal function (risk of neurotoxicity) or heart failure. Avoid contact, skin sensitization may occur. Monitor serum potassium concentration, renal and haematological status. Spirochete infections particularly syphilis; suprainfection with penicillin-resistant organisms with prolonged use; avoid intrathecal route.
Adverse Reactions
 Hypersensitivity reactions including uticaria; fever; joint pains; rashes; angioedema; serum sickness-like reactions; haemolytic anaemia; interstitial nephritis; neutropenia; thrombocytopenia; CNS toxicity including convulsions; diarrhoea; antibiotic-associated colitis.
Potentially Fatal: Anaphylaxis.
Drug Interactions
 Probenecid prolongs T1/2 of benzathine benzylpenicillin. Bacteriostatic drugs e.g. chloramphenicol, tetracyclines; other antibacterials; anticoagulants.
See Below for More benzathine benzylpenicillin Drug Interactions
Lab Interactions
 May interfere with diagnostic tests for urinary glucose using copper sulfate, direct Coomb's test, and test for urinary or serum proteins. May interfere with diagnostic tests that use bacteria.
Mechanism of Actions
 Benzathine benzylpenicillin has the same antimicrobial action as benzylpenicillin which exerts its bactericidal action on growing and dividing bacteria by inhibiting bacterial cell wall synthesis. IM admin results in a prolonged effect, but because of its relatively low blood concentrations, its use should be restricted to microorganisms that are highly susceptible to it.
Absorption: Forms a depot which is slowly released and hydrolysed to benzylpenicillin after IM admin.
Distribution: Poor penetration into CSF.
Excretion: Detected in the urine for up to 12 wk after a single dose.
ATC Classification
 J01CE08 - benzathine benzylpenicillin ; Belongs to the class of beta-lactamase sensitive penicillins. Used in the systemic treatment of infections.
Available As
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