Sunday, August 06, 2006

Carbapenems

Carbapenems

Carbapenems are a class of beta-lactam antibiotics.

The following drugs belong to the carbapenem class:

Imipenem (often given as part of Imipenem/cilastatin)
Meropenem
Ertapenem
Faropenem
Doripenem


External Links

Structure Activity Relationships "Antibacterial Agents; Structure Activity Relationships," André Bryskier MD; beginning at pp131
Carbapenems

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Carbapenems

Imipenem/Cilastatin(Primaxin)

Mechanism of action

Inhibits bacterial cell wall synthesis. Cilastatin blocks metabolism of imipenem.

Spectrum of activity

Gram-negative (including P aeruginosa); Gram-positive (including some enterococci); not MRSA; Anaerobes including Bacteroides fragilis

Half-life

1 h

Metabolism

In kidney by dehydropeptidase. Blocked by cilastatin

Excretion

70% unchanged in urine

Clinical Side effects

GI, phlebitis, neurologic (seizures <>

Laboratory abnormalities

Increased LFTs, other rare events

Mechanism of drug interactions

No CYP-450 interactions. Probenecid increases levels

Other considerations

Significant dosage adjustment in renal insufficincy

Approved indications

Intra-abdominal infection, lower respiratory tract infection, UTI, gynecologic infection, bacterial septicemia, bone, joint, and skin infections, endocarditis, polymicrobic infections

Usual Dose

500 mg q6h, adjusted for renal function

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Meropenem(Merrem)

Mechanism of action

Inhibits bacterial cell wall synthesis

Spectrum of activity

Gram-negative (including P aeruginosa); Gram-positive (including some enterococci); not MRSA; Anaerobes including Bacteriodes fragilis

Half-life

1-1.5 h

Metabolism

Minor hepatic to inactive metabolite

Excretion

75% unchanged in urine

Clinical Side effects

Headache, rash, GI, phlebitis, hypotension

Laboratory abnormalities

Increased LFTs, other rare events

Mechanism of drug interactions

No CYP-450 interactions. Probenecid increases levels

Other considerations

Dose adjustment necessary in renal insufficiency

Approved indications

Intra-abdominal infection, bacterial meningitis

Usual Dose

1 g q8h, adjusted for renal function

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Ertapenem(Invanz)

Mechanism of action

Inhibits bacterial cell wall synthesis

Spectrum of activity

Gram-negative—not P aeruginosa;Gram-positive, not enterococci, not MRSA; Anaerobes including Bacteriodes fragilis

Half-life

4h

Metabolism

Minor hepatic to inactive metabolite

Excretion

38% unchanged in urine; 37% inactive metabolite; 10% feces

Clinical Side effects

Headache, rash, GI, phlebitis, hypotension

Laboratory abnormalities

Increased LFTs, other rare events

Mechanism of drug interactions

No CYP-450 interactions. Probenecid increases levels.

Other considerations

Minor dose adjustment necessary in renal insufficiency

Approved indications

Intra-abdominal infection, skin and skin structure, community-acquired pneumonia, UTI, pelvic infections

Usual Dose

1 g once daily, adjusted for renal function

Cleveland Clinic