Imipenem/cilastatin

antibiotic ( carbapenem). Carbapenems are antibacterial agents (broad-spectrum antibiotics, reserve antibiotics), which are characterized by a broad anti-catabolic spectrum of activity in the gram-positive and gram-negative range. They belong to the reserve antibiotics and are approved for the treatment of severe infections in hospital patients. Carbapenems are not absorbed orally and must be administered parenterally. Imipenem is only administered in a fixed 1:1 combination with cilastatin (e.g. imipenem/cilastatin, meropenem). Cilastatin is an inhibitor of dihydropeptidase in the proximal renal tubules, otherwise imipenem in the kidneys is inactivated very effectively. Ertapenem is also cultivated by this enzyme so that ineffective metabolites appear in the urine. All representatives are resistant to most ß-lactamases.

Reserve antibiotic for severe skin and soft tissue infections, infections of the respiratory tract, kidneys and urinary tract, genital organs, sepsis, fever of unknown origin in granulocytopenic patients.

• 1.5-4 g/day i.v. in 3-4 ED
• Children > 3 months: 60 mg/kg bw/day, max. 2 g/day

The most common clinical side effects were local experiences related to the location of the intravenous infusion.

Gastrointestinal ADRs (examination in 3470 patients treated with imipenem / cilastatib)

• Nausea
• Vomiting or diarrhea.
• Pseudomembranous colitis: frequency is low (0 x 1%)

Dermatological UAWs:

• The most common clinical side effects are local changes at the site of intravenous infusion.
• Exanthema
• Itching
• Hematological ADRs: The most common laboratory changes were temporarily elevated liver function values
• Eosinophilia
• positive Coombs test (not associated with haemolysis) and increased platelet counts

Nephrogenic ADRs: High doses have a nephrotoxic effect. Loop diuretics and aminoglycosides increase nephrotoxicity.

Zienam®

1. Calandra GB et al (1986) The safety profile of imipenem/cilastatin: worldwide clinical experience based on 3470 patients. J Antimicrob Chemother 18 Suppl E:193-202.

2. Yanagihara K et al (2006) Clinical comparative study of sulbactam/ampicillin and imipenem/cilastatin in elderly patients with community-acquired pneumonia. Internal Med 45: 995-999