Imipenem and Cilastatin
- Atc Codes:J01DH
- CAS Codes:74431-23-5#64221-86-9#81129-83-1#82009-34-5
- PHARMGKB ID:74431-23-5#64221-86-9#81129-83-1#82009-34-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Cilanem, Imipenem/Cilastatin, Xedine, Zienam; Belgium: Tienam; Cyprus: Tienam; Czech Republic: Cilanem, Imipenem/Cilastatin, Tienam; Estonia: Tienam; Finland: Tienam; France: Imipenem/Cilastatine, Tienam; Germany: Imipenem/Cilastatin, Zienam; Greece: Primagal, Primaxin; Hungary: Imipenem/Cilastatin, Tienam; Ireland: Primaxin; Italy: Tenacid, Tienam; Latvia: Imipenem/Cilastatin, Tienam; Lithuania: Imipenem/Cilastatin, Tienam; Luxembourg: Tienam; Malta: Primaxin; Netherlands: Imipenem/Cilastatine, Tienam; Poland: Tienam; Portugal: Imipenem/Cilastatina, Tienam; Romania: Cilopen, Imipenem/Cilastatin, Tienam; Slovakia: Imipenem/Cilastatin, Tienam; Spain: Tienam; Sweden: Imicilast, Imipenem/Cilastatin, Tienam; UK: Primaxin.
North America
Canada: Primaxin; USA: Primaxin.
Latin America
Argentina: Dixabiox, Imipecil, Imipenem, Imipenem-Cilastatina, Imistatin, Klonam, Zienam; Brazil: Imipenem-Cilastatina, Tienam; Mexico: Iminen, Lemibet, Tienam.
Asia
Japan: Chiecool, Imistan, Indast, Tienam.
Drug combinations
Chemistry
Imipenen: C~12~H~17~N~3~O~4~S H~2~O. Mw: 317.36. (1) 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 6-(1-hydroxyethyl)-3-[[2-[iminomethyl)amino]ethyl]thio]-7-oxo-, monohydrate, [5R-[5α,6α(R*)]]-; (2)(5R,6S)-3-[[2-(Formimidoylamino)ethyl]thio]-6-[(R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate. CAS-74431-23-5; CAS-64221-86-9 (anhydrous)(1983).
Cilastatin Sodium: C~16~H~25~N~2~NaO~5~S. Mw: 380.43. (1) 2-Heptenoic acid, 7-[2-amino-2-carboxyethyl)thio]-2-[[2,2-dimethylcyclopropyl)carbonyl]amino]-, monosodium salt, [R-[R*,S*-(Z)]]-; (2) Sodium (Z)-7-[[(R)-2-amino-2-carboxyethyl]thio]-2-[(S)-2,2-dimethylcyclopropanecarboxamido]-2-heptenoate. CAS-81129-83-1; CAS-82009-34-5 (cilastatin)(1984).
Pharmacologic Category
Antibacterials; Miscellaneous β-Lactams; Carbapenems. (ATC-Code: J01DH).
Mechanism of action
Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins, thus inhibiting bacterial cell wall biosynthesis. Cilastatin prevents renal metabolism of imipenem by competitive inhibition of dehydropeptidase along brush border of renal tubules.
Therapeutic use
Treatment of lower respiratory tract, urinary tract, intra-abdominal, gynecologic, bone and joint, skin and skin structure, and polymicrobic infections as well as bacterial septicemia and endocarditis. Antibacterial activity includes resistant Gram-negative bacilli (Pseudomonas aeruginosa and Enterobacter spp.), Gram-positive bacteria (methicillin-sensitive Staphylococcus aureus and Streptococcus spp.) and anaerobes.
Pregnancy and lactiation implications
Imipemem and cilastatin should be used during pregnancy only if potential benefit justifies potential risk to mother and fetus. Use caution during lactation.
Unlabeled use
Hepatic abscess, neutropenic fever, melioidosis.
Contraindications
Hypersensitivity to imipenem/cilastatin or any component of the formulation. Hypersensitivity to amide-type anesthetics. Severe shock or heart block in I.M. formulation due to lidocaine diluent.
Warnings and precautions
Serious hypersensitivity reactions, including anaphylaxis reported (some without history of previous allergic reactions to β-lactams). Associated with CNS adverse effects, including confusional states and seizures (myoclonic). Use caution with CNS disorders (e.g. brain lesions, history of seizures or renal impairment). Incidence of seizures may be higher than with other carbapenems. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea. Use with caution in renal impairment. Increased seizure risk and thrombocytopenia reported in significant renal dysfunction. I.V. and I.M. preparations cannot be interchanged. Doses for I.M. administration mixed with lidocaine.