IMIPENEM AND CILASTATIN FOR INJECTION, USP POWDER FOR SOLUTION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

IMIPENEM; CILASTATIN (CILASTATIN SODIUM)

Available from:

METHAPHARM INC

ATC code:

J01DH51

INN (International Name):

IMIPENEM AND CILASTATIN

Dosage:

500MG; 500MG

Pharmaceutical form:

POWDER FOR SOLUTION

Composition:

IMIPENEM 500MG; CILASTATIN (CILASTATIN SODIUM) 500MG

Administration route:

INTRAVENOUS

Units in package:

100

Prescription type:

Prescription

Therapeutic area:

CARBAPENEMS

Product summary:

Active ingredient group (AIG) number: 0218820001; AHFS:

Authorization status:

CANCELLED PRE MARKET

Authorization date:

2018-04-23

Summary of Product characteristics

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