Lastinem-500 (Imipenem and Cilastatin Powder for Solution for Infusion 500 mg 500mg)

Nazione: Malesia

Lingua: inglese

Fonte: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)

Principio attivo:

CILASTATIN SODIUM; IMIPENEM

Commercializzato da:

UNIMED SDN BHD

INN (Nome Internazionale):

CILASTATIN SODIUM; IMIPENEM

Confezione:

1 Vials

Prodotto da:

Venus Remedies Limited

Scheda tecnica

LASTINEM-500 (IMIPENEM AND CILASTATIN POWDER FOR SOLUTION FOR INFUSION
500 MG/ 500MG)
DESCRIPTION
Before Reconstitution: White to pale yellow crystalline powder filled
in glass vial.
After Reconstitution: Clear Solution. Appropriate diluents can be used
for reconstitution are 0.9% Sodium Chloride Injection, 5% Dextrose
Injection
COMPOSITION
LASTINEM-500 (IMIPENEM AND CILASTATIN POWDER FOR SOLUTION FOR INFUSION
500 MG/ 500MG)
Each vial contains:
Sterile Imipenem USP equivalent to Anhydrous Imipenem 500 mg
Sterile Cilastatin Sodium USP equivalent to Cilastatin 500 mg
Sterile Sodium bicarbonate is used as a buffer.
PHARMACODYNAMICS
Imipenem, also referred to as N-formimidoyl-thienamycin, is a
semi-synthetic derivative of thienamycin, the parent compound produced
by the filamentous
bacterium Streptomyces cattleya. Imipenem exerts its bactericidal
activity by inhibiting bacterial cell wall synthesis in Gram-positive
and Gram-negative
bacteria through binding to penicillin-binding proteins (PBPs).
Cilastatin sodium is a competitive, reversible and specific inhibitor
of dehydropeptidase-I, the renal enzyme which metabolizes and
inactivates imipenem. It is
devoid of intrinsic antibacterial activity and does not affect the
antibacterial activity of imipenem.
PHARMACOKINETIC/PHARMACODYNAMIC (PK/PD) RELATIONSHIP
Similar to other beta-lactam antibacterial agents, the time that
imipenem concentrations exceed the MIC (T>MIC) has been shown to best
correlate with
efficacy.
MECHANISM OF RESISTANCE
Resistance to imipenem may be due to the following:
•
Decreased permeability of the outer membrane of Gram-negative bacteria
(due to diminished production of porins)
•
Imipenem may be actively removed from the cell with an efflux pump.
•
Reduced affinity of PBPs to imipenem
•
Imipenem is stable to hydrolysis by most beta-lactamases, including
penicillinases and cephalosporinases produced by gram-positive and
gram-negative
bacteria, with the exception of relatively rare carbapenem hydrolysing
beta-lactamases. Species resistant t