Země: Kanada
Jazyk: angličtina
Zdroj: Health Canada
IMIPENEM; CILASTATIN (CILASTATIN SODIUM)
METHAPHARM INC
J01DH51
IMIPENEM AND CILASTATIN
250MG; 250MG
POWDER FOR SOLUTION
IMIPENEM 250MG; CILASTATIN (CILASTATIN SODIUM) 250MG
INTRAVENOUS
100
Prescription
CARBAPENEMS
Active ingredient group (AIG) number: 0218820002; AHFS:
CANCELLED PRE MARKET
2018-04-23
Page 1 of 48 PRODUCT MONOGRAPH IMIPENEM AND CILASTATIN FOR INJECTION, USP Imipenem 250 mg and Cilastatin 250 mg (as cilastatin sodium) per vial Imipenem 500 mg and Cilastatin 500 mg (as cilastatin sodium) per vial Sterile Powder for intravenous Infusion ANTIBIOTIC Methapharm Inc. Date of Revision: April 10, 2015 Brantford, Ontario, Canada Control: 174843 Page 2 of 48 IMIPENEM AND CILASTATIN FOR INJECTION, USP THERAPEUTIC CLASSIFICATION Antibiotic ACTION Imipenem exerts a bactericidal action by inhibiting cell wall synthesis in aerobic and anaerobic gram-positive and gram-negative bacteria. IMIPENEM AND CILASTATIN FOR INJECTION, USP (imipenem and cilastatin sodium) consists of two components: (1) imipenem, a derivative of thienamycin, a carbapenem antibiotic; and (2) cilastatin sodium, a specific inhibitor of dehydropeptidase-I a renal enzyme which metabolizes and inactivates imipenem. Cilastatin blocks the metabolism of imipenem in the kidney, so that concomitant administration of imipenem and cilastatin allows antibacterial levels of imipenem to be attained in the urine. Inhibition of cell-wall synthesis is achieved in gram-negative bacteria by the binding of imipenem to penicillin binding proteins (PBPs). In the case of _Escherichia coli _ and selected strains of _Pseudomonas aeruginosa_ , imipenem has been shown to have highest affinity for PBP- 2, PBP-1a and PBP-1b, with lower activity against PBP-3. The preferential binding of imipenem on PBP-2 and PBP-1b leads to direct conversion of the individual cell to a spheroplast resulting in rapid lysis and cell death without filament formation. When imipenem is removed prior to complete killing of gram-negative species, the remaining viable cells show a measurable lag, termed a "post-antibiotic effect" (PAE), prior to resumption of new growth. INDICATIONS AND CLINICAL USE IMIPENEM AND CILASTATIN FOR INJECTION, USP (imipenem and cilastatin sodium) may be indicated in the treatment of serious infections when caused by sensitive strains of bacteria. Where considered n Přečtěte si celý dokument