Penicillin (penicillinase-resistant penicillin)
Staphylococcus spp., Streptococcal spp.
Exerts bactericidal activity via inhibition of bacterial cell wall synthesis by binding one or more of the penicillin binding proteins (PBPs). Exerts bacterial autolytic effect by inhibition of certain PBPs related to the activation of a bacterial autolytic process.
Penicillins produce time-dependent killing
Distribution: total protein binding 28 to 49%; Metabolism: liver (20 to 40%); Excretion: renal (62 to 80%); Volume of distribution: 22 L/kg
Renal: interstitial nephritis, nephrotoxicity
Hematologic: neutropenia, inhibition of platelet aggregation, thrombocytopenia
CNS: seizures
Hepatic: transient increases in transaminases
Other: thrombophlebitis, Jarisch-Herxheimer Reaction (fever, chills, sweating, tachycardia, hyperventilation, flushing, and myalgia)
Adult: Susceptible infections: 1-2 g IV every 4-6 hr; 1 g IM every 4-6 hr
Pediatric: Susceptible infections:
· neonates less than 7 days of age, 50-75 mg/kg/day IV/IM divided every 8-12 hr; neonates 7 days of age and older, 75-100 mg/kg/day IV/IM divided every 6-8 hr
· infants and children, 100-200 mg/kg/day IV/IM divided every 6 hr; maximum 12 g/day
Disease state based dosing:
Renal failure: Dosage intervals should be increased for patients with renal failure.
Mild renal failure: GFR > 50 mL/min: normal dose every 4 to 6 hours
Moderate renal failure: GFR 10 to 50 mL/min: normal dose every 6 to 8 hours
Severe renal failure: GFR < 10 mL/min: normal dose every 8 to 12 hours.
Hepatic failure: No dosing adjustment necessary.
Contraindications/Warnings/Precautions:
Contraindications: Anaphylaxis to methicillin or other penicillins
Precautions: Cephalosporin hypersensitivity
Pregnancy:
Category B: No evidence of risk in humans but studies inadequate.
Monitoring Requirements:
Therapeutic: Culture and sensitivities, signs and symptoms of infection
Toxic: Periodic CBC, urinalysis, BUN, SCr, AST and ALT
Brand names/Manufacturer:
· CELBENIN (Beecham Research, UK)
· CHIBRO-FLABELLINE (Merck Sharp & Dohme-Chibret - FRANCE)
· LUCOPENIN (Durascan - DENMARK)
· METIN (CSL - AUSTRALIA)
· METIN (CSL - AUSTRALIA)
· STAFICYN (Firma - ITALY)
· STAPHCILLIN (Apothecon - USA)