Benzathine benzylpenicillin

Generic Medicine Info
Indications and Dosage
Adult: Primary, secondary and latent: 1.8 g (2.4 MIU) as a single dose. Late (tertiary and neurosyphilis): 1.8 g (2.4 MIU) once wkly for 3 doses.

Streptococcal pharyngitis
Adult: 900 mg (1.2 MIU) as a single dose.
Child: <27 kg: 225-450 mg (300,000-600,000 U) as a single dose; ≥27 kg: 675 mg (900,000 U) as a single dose.

Treponemal infections
Adult: 900 mg (1.2 MIU) as a single dose.
Child: 450 mg (600,000 U) as a single dose.

Congenital syphilis
Child: Normal CSF: <2 yr 37.5 mg/kg (50,000 U/kg) as a single dose; 2-12 yr Adjust dosage based on adult dosage schedule.

Primary prophylaxis of rheumatic fever
Adult: 900 mg (1.2 MIU) as a single dose. Prevention of recurrence of acute attack: 900 mg (1.2 MIU) once every 3 or 4 wk or 450 mg (600,000 U) once every 2 wk.
Child: <27 kg: 225-450 mg (300,000-600,000 U) as a single dose; ≥27 kg: 675 mg (900,000 U) as a single dose. Prevention of recurrence of acute attack: <27 kg: 450 mg (600,000 U) once every 3 or 4 wk; ≥27 kg: 900 mg (1.2 MIU) once every 3 or 4 wk.
Hypersensitivity to penicillins.
Special Precautions
Patient w/ previous hypersensitivity reactions to cephalosporins, history of allergy, asthma, seizure disorder. Not intended for IV or intra-arterial admin or inj near major peripheral nerves of blood vessels. Prolonged use may result in bacterial or fungal superinfection. Renal impairment.
Adverse Reactions
Hypersensitivity reactions including skin eruptions, urticaria, laryngeal oedema, serum sickness-like reactions, allergic vasculitis, pruritus, fatigue, asthenia, pain, headache; fever; haemolytic anaemia, leucopenia, thrombocytopenia; neuropathy; nephropathy; hypotension, tachycardia, palpitations, pulmonary HTN, pulmonary embolism, vasodilation, vasovagal reaction, cerebrovascular accident, syncope; nausea, vomiting, intestinal necrosis, blood in stool, intestinal necrosis; lymphadenopathy; inj site reactions (e.g. pain, inflammation), joint disorder, periostitis, exacerbation of arthritis, myoglobinuria, rhabdomyolysis; nervousness, tremors, dizziness, somnolence, confusion, anxiety, euphoria, transverse myelitis, seizures, coma; hypoxia, apnoea, dyspnoea; diaphoresis; blurred vision, blindness; neurogenic bladder, haematuria, proteinuria, renal failure, impotence, priapism.
Potentially Fatal: Anaphylaxis, antibiotic-associated pseudomembranous colitis.
Monitoring Parameters
Periodic evaluation of renal and haematopoietic functions. Assess culture and sensitivity test prior to initiation of therapy. Monitor for hypersensitivity reactions and opportunistic infections.
Drug Interactions
Bactericidal effect may be antagonised by tetracycline. Decreased rate of excretion and increased serum concentration when used w/ probenecid.
Lab Interference
May cause false-positive result in urinary and/or serum protein test, false positive or negative result for glycosuria test using copper sulfate reagent method, positive Coombs’ test.
Mechanism of Action: Benzathine benzylpenicillin interferes w/ bacterial cell wall synthesis during active multiplication causing cell wall death and resultant bactericidal activity against susceptible bacteria.
Duration: 1-4 wk.
Absorption: Slowly absorbed from the site of inj. Time to peak plasma concentration: W/in 12-24 hr.
Distribution: Distributed throughout body tissues; CSF (minimal amount). Plasma protein binding: Approx 60%.
Metabolism: Hydrolysed to benzylpenicillin.
Excretion: Via urine.
Chemical Structure

Chemical Structure Image
Benzathine benzylpenicillin

Source: National Center for Biotechnology Information. PubChem Database. Benzathine benzylpenicillin, CID=15232, (accessed on Jan. 21, 2020)

Store between 2-8°C. Do not freeze.
MIMS Class
ATC Classification
J01CE08 - benzathine benzylpenicillin ; Belongs to the class of beta-lactamase sensitive penicillins. Used in the systemic treatment of infections.
Anon. Penicillin G Benzathine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 05/09/2016.

Bicillin L-A Injection (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. Accessed 05/09/2016.

Buckingham R (ed). Benzathine Benzylpenicillin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 05/09/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Penicillin G Benzathine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). Accessed 05/09/2016.

Pfizer New Zealand Ltd. Bicillin L-A Injection data sheet 8 June 2012. Medsafe. Accessed 05/09/2016.

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