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imipenem cilastatin (Primaxin)

Imipenem is derived from a compound produced by Streptomyces cattleya. The compound thienamycin is unstable, but the N-formimidoyl derivative imipenem is stable. Imipenem is the most active non-penicillin, non-cephalosporin antibiotic against a wide variety of bacteria. It is marketed in combination with cilastatin, a drug that inhibits the degradation of imipenem with formation of a nephrotoxic metabolite by a renal tubular dipeptidase. Indications: - bacterial infections due to susceptible organisms - cutaneous anthrax, inhalation anthrax [4] - intra-abdominal infection - gastrointestinal infections - bacterial peritonitis - abdominal abscess - urogenital infection - pelvic inflammatory disease - endometritis - respiratory tract infections - lower respiratory tract infections - pneumonia - meliodosis - skin or soft tissue infection - diabetic foot infection - infectious arthritis, osteomyelitis - endocarditis - empiric treatment for fever of unknown origin - empiric treatment of febrile neutropenia [4] Dosage: 0.5 g IV every 6 hours Dosage adjustment in renal failure: creatinine clearance dosage > 50-90 mL/min 250-500 mg every 6-8 hours 10-50 mL/min* 250 mg every 8-12 hours < 10 mL/min# 125-250 mg every 12 hours * same dose for continuous arteriovenous hemofiltration # dose after hemodialysis Pharmacokinetics: 1/2life 0.25 hours Antimicrobial activity: Gram positive - Streptococcus - Streptococcus group A - Streptococcus group B - Streptococcus group C - Streptococcus group G - Streptococcus pneumonia - Streptococcus viridans, milleri - Enterococcus faecalis - Enterococcus faecium (+/-) - Staphylococcus aureus (MSSA) - Staphylococcus epidermidis - Listeria monocytogenes Gram negative - Neisseria gonorrhoeae - Neisseria meningitidis - Moraxella catarrhalis - Haemophilus influenzae - Escherichia coli - Klebsiella species - Enterobacter species - Serratia species - Salmonella species - Shigella species - Proteus mirabilis - Proteus vulgaris - Providencia species - Morganella species - Citrobacter species - Aeromonas species - Acinetobacter species - Pseudomonas aeruginosa - Pseudomonas cepacia - Yersinia enterocolitica - Pasteurella multocida - Campylobacter fetus [4] Anaerobes - Actinomyces - Bacteroides fragilis - Bacteroides melaninogenicus - Clostridium difficile - Clostridium species - Peptostreptococcus species Adverse effects: 1) dose-related neurotoxicity in the elderly - seizures 2) accumulates in patients with renal insufficiency 3) superinfection with Xanthomonas maltophilia Drug interactions: - coadministration of ganciclovir increases likelihood of seizures Laboratory: - antibiotic susceptibility imipenem

Interactions

drug interactions

Related

cilastatin

General

carbapenem (thienamycin)

Properties

MISC-INFO: elimination route KIDNEY elimination by hemodialysis + 1/2life 0.25 HOURS

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 1092
  2. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
  3. Sanford Guide to antimicrobial therapy 1997, 2001
  4. Deprecated Reference
  5. Department of Veterans Affairs, VA National Formulary

Component-of

cilastatin/imipenem imipenem cilastatin/relebactam (Recarbrio)