IMIPENEM AND CILASTATIN FOR INJECTION POWDER FOR SOLUTION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

IMIPENEM; CILASTATIN (CILASTATIN SODIUM)

Available from:

PFIZER CANADA ULC

ATC code:

J01DH51

INN (International Name):

IMIPENEM AND CILASTATIN

Dosage:

250MG; 250MG

Pharmaceutical form:

POWDER FOR SOLUTION

Composition:

IMIPENEM 250MG; CILASTATIN (CILASTATIN SODIUM) 250MG

Administration route:

INTRAVENOUS

Units in package:

20ML VIAL

Prescription type:

Prescription

Therapeutic area:

CARBAPENEMS

Product summary:

Active ingredient group (AIG) number: 0218820002; AHFS:

Authorization status:

CANCELLED PRE MARKET

Authorization date:

2019-06-28

Summary of Product characteristics

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