देश: कनाडा
भाषा: अंग्रेज़ी
स्रोत: Health Canada
CILASTATIN (CILASTATIN SODIUM); IMIPENEM
PFIZER CANADA ULC
J01DH51
IMIPENEM AND CILASTATIN
500MG; 500MG
POWDER FOR SOLUTION
CILASTATIN (CILASTATIN SODIUM) 500MG; IMIPENEM 500MG
INTRAVENOUS
20ML VIAL
Prescription
CARBAPENEMS
Active ingredient group (AIG) number: 0218820001; AHFS:
CANCELLED POST MARKET
2019-06-28
PRODUCT MONOGRAPH PR IMIPENEM AND CILASTATIN FOR INJECTION Imipenem and Cilastatin Sodium, 250 mg / 250 mg for injection Imipenem and Cilastatin Sodium, 500 mg / 500 mg for injection Sterile Powder for intravenous Infusion Pfizer Standard ANTIBIOTIC Pfizer Canada Inc. 17300 Trans-Canada Highway Kirkland, Québec H9J 2M5 Date of revision: May 31, 2018 Submission Control No. 215175 _Product Monograph – _ _Pr_ _Imipenem and Cilastatin for Injection _ _Page 2 of 52 _ PR IMIPENEM AND CILASTATIN FOR INJECTION Imipenem and Cilastatin Sodium, 250 mg / 250 mg for injection Imipenem and Cilastatin Sodium, 500 mg / 500 mg for injection Sterile Powder for Intravenous Infusion 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 (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), pri पूरा दस्तावेज़ पढ़ें