benzathine penicillin (Bicillin L-A)
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Introduction
Tradename: Bicillin L-A. 1st generation penicillin.
Indications
- active against most gram positive organisms, especially Streptococcus species
- active against Neisseria gonorrhoeae
- active against some anaerobes
- active against some spirochetes
- treatment of mild to moderately severe infections
- prophylaxis against susceptible organisms
Dosage
- adults:
- group A streptococcal respiratory tract infection: 1.2 x 10E6 U IM as a single dose
- prophylaxis of recurrent rheumatic fever: 1.2 x 10E6 U IM every 3-4 weeks, or 600,000 U IM every 2 weeks
- early syphilis: 2.4 x 10E6 U IM as a single dose
- syphilis of more than 1 year duration: 2.4 x 10E6 U IM weekly for 3 doses
- infants & children
- group A streptococcal respiratory tract infection: 25,000 U/kg IM as a single dose; maximum 1.2 x 10E6 U
- prophylaxis of recurrent rheumatic fever: 25,000 U/kg IM every 3-4 weeks; maximum 1.2 x 10E6 U
- early syphilis: 50,000 U/kg IM as a single dose; maximum 2.4 x 10E6 U
- syphilis of more than 1 year duration: 50,000 U/kg IM weekly for 3 doses; maximum 2.4 x 10E6 U/dose
- neonates > 1200 g: 50,000 U IM as a single dose
Injection: 600,000 U/mL (2 mL)
Pharmacokinetics
- slowly absorbed following IM administration
- time to peak serum concentration within 12-24 hours
elimination via kidney
Adverse effects
- not common (1-10%)
- local pain
- uncommon (< 1%)
- thrombophlebitis, convulsions, confusion, drowsiness, fever, rash, electrolyte imbalance, hemolytic anemia, positive direct antiglobulin (Coomb's) test (DAT), myoclonus, acute interstitial nephritis, Jarisch- Herxheimer reaction, hypersensitivity reaction, anaphylaxis