imipenem cilastatin (Primaxin)
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Introduction
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
- 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
Table
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
elimination via kidney
elimination by hemodialysis = +
1/2life = 0.25 hours
Antimicrobial activity
- Streptococcus
- Streptococcus pneumonia
- Streptococcus viridans, milleri
- Enterococcus faecalis
- Enterococcus faecium (+/-)
- Staphylococcus aureus (MSSA)
- Staphylococcus epidermidis
- Listeria monocytogenes
- 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]
- Actinomyces
- Bacteroides fragilis
- Bacteroides melaninogenicus
- Clostridium difficile
- Clostridium species
- Peptostreptococcus species
Adverse effects
- dose-related neurotoxicity in the elderly
- accumulates in patients with renal insufficiency
- superinfection with Xanthomonas maltophilia
Drug interactions
- coadministration of ganciclovir increases likelihood of seizures
- drug interaction(s) anticonvulsants with anti-bacterial agents
- drug interaction(s) of antibiotics with warfarin
Laboratory
More general terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill pg 1092
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Sanford Guide to antimicrobial therapy 1997, 2001
- ↑ 4.0 4.1 4.2 4.3 Deprecated Reference
- ↑ Department of Veterans Affairs, VA National Formulary
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=53032
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=47317
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=104838
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5282372
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5288621
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3694
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3695