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Imipenem/cilastatin
Combination of
Imipenem Carbapenem antibiotic
Cilastatin Dehydropeptidase inhibitor
Identifiers
CAS number 92309-29-0
ATC code J01DH51
PubChem 11954222
Therapeutic considerations
Pregnancy cat. C(US)
Legal status POM (UK) -only (US)
Routes Intravenous, intramuscular

Imipenem/cilastatin is a broad spectrum beta-lactam antibiotic containing equal quantities of imipenem and cilastatin. It is related to the penicillin/cephalosporin family of antibiotics but is classified as belonging to the carbapenem class.

Contents

Mechanism

It has the ability to kill a wide variety of bacteria. It works by interfering with their ability to form cell walls, and therefore the bacteria break up and die.

  • Imipenem, the active antibacterial agent, is rapidly degraded by the renal enzyme dehydropeptidase if administered alone (making it less effective).
  • Cilastatin is a dehydropeptidase inhibitor, with no intrinsic antibacterial activity, and must be co-administered with imipenem to ensure its efficacy. Cilastatin blocks the effects of the renal enzyme. Cilastatin has no antibacterial effects and does not affect the antibacterial activity of the imipenim.

Administration

The usual dose for adults equal or over 70kg is 250mg every 6 hours for mild infection, and 500mg every 8 hours OR 1g every 6-8 hours for moderate infection. In severe, fully susceptible infection 500mg every 6 hours is recommended. This drug is given by injection or infusion. It's nine FDA indications are lower respiratory tract infections, urinary tract infections, intra-abdominal infections, gynecologic infections, bacterial septicemia, bone and joint infections, skin and skin structure infections, endocarditis, and polymicrobic infections. [1]It may be less likely to cause an allergic reaction in people who have had an allergic reaction to a penicillin in the past. It is particularly effective against Enterobacter species.

Production

Imipenem/cilastatin is marketed by Merck & Co. under the trade names Primaxin ,Tienam and Zienam. The combination is also marketed by Ranbaxy Laboratories in India under the brand name Cilanem.

Imipenem/cilastatin is marketed by Highnoon Laboratories Ltd. in Pakistan under the trade name "Prepenem". Prepenem was launched by Highnoon in May 2007 and was the first generic brand after the research brand Tienam.

References

  1. ^ US Food and Drug Administration. [http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/050587s065,050630s028lbl.pdf "Primaxin FDA label"], Food and Drug Administration. Oct 2006.
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