Imipenem
Latin: Imipenemum
- 64221-86-9
- 74431-23-5 (monohydrate)
J01DH51
White to almost white or pale yellow powder
β -lactam antibiotics, carbapenem
Inhibition of cell wall synthesis
1972 mg · kg -1 ( LD50, rat, i.v.)
Template: Infobox chemical / molecular formula search available
Imipenem is an antibiotic effective drug and belongs chemically to the group of carbapenems.
Pharmacology
Imipenem is a β -lactam antibiotic which is effective against bacteria by inhibiting bacterial cell wall synthesis. Since the substance is rapidly degraded by renal dipeptidase in the proximal tubular cells of the kidneys, imipenem is administered exclusively in combination with cilastatin. Cilastatin inhibits the dipeptidase and allows therapeutically effective concentrations of Imipenems.
Spectrum
The spectrum of activity is broad in the gram-positive, gram-negative, aerobic and anaerobic. Effect gaps exist for Clostridium difficile, Enterococcus faecium, Legionella, Mycoplasma, MRSA, Stenotrophomonas maltophilia and only moderate activity against Pseudomonas.
Pharmacokinetics
Imipenem is not absorbed and therefore must be given parenterally. The plasma half-life is one hour, the volume of distribution of 0.2 l / kg, the plasma protein binding is 25%. Imipenem is excreted 70 % unchanged by the kidney ( renal ), 30 % are metabolized by the liver ( hepatic metabolism ). Imipenem is dialysable.
Areas of application
Indications for imipenem are severe polymicrobial infections or sepsis.
Side effects
Possible side effects include rash, gastrointestinal intolerance, dizziness, convulsions, seizures, venous irritation, brown discolouration of the tongue and blood count changes, such as eosinophilia, leukopenia, thrombocytopenia, thrombocytosis, and rarely agranulocytosis. Increase of transaminases, alkaline phosphatase and creatinine are possible.