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Primaxin I.V.
Clinical Pharmacology
Primaxin I.V.
Imipenem-cilastatin sodium is hemodialyzable. However, usefulness of this procedure in the overdosage setting is questionable. (See OVERDOSAGE.)
Microbiology
The bactericidal activity of imipenem results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B.
Imipenem has a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases produced by gram-negative and gram-positive bacteria. It is a potent inhibitor of beta-lactamases from certain gram-negative bacteria which are inherently resistant to most beta-lactam antibiotics, e.g., Pseudomonas aeruginosa, Serratia spp., and Enterobacter spp.
Imipenem has in vitro activity against a wide range of gram-positive and gram-negative organisms. Imipenem has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections treated with the intravenous formulation of imipenem-cilastatin sodium as described in the INDICATIONS AND USAGE section.
Gram-positive aerobes
Enterococcus faecalis (formerly S.faecalis) (NOTE:
Imipenem is inactive in vitro against
Enterococcus faecium [formerly S.faecium].)
Staphylococcus aureus including penicillinase-producing strains
Staphylococcus epidermidis including penicillinase-producing
strains (NOTE: Methicillin-resistant staphylococci should be reported as resistant
to imipenem.)
Streptococcus agalactiae (Group B streptococci)
Streptococcus pneumoniae
Streptococcus pyogenes
Gram-negative aerobes
Acinetobacter spp.
Citrobacter spp.
Enterobacter spp.
Escherichia coli
Gardnerella vaginalis
Haemophilus influenzae
Haemophilus parainfluenzae
Klebsiella spp.
Morganella morganii
Proteus vulgaris
Providencia rettgeri
Pseudomonas aeruginosa(NOTE: Imipenem is inactive in vitro
against Xanthomonas (Pseudomonas) maltophilia and some strains of P.
cepacia.)
Serratia spp., including S. marcescens
Gram-positive anaerobes
Bifidobacterium spp.
Clostridium spp.
Eubacterium spp.
Peptococcus spp.
Peptostreptococcus spp.
Propionibacterium spp.
Gram-negative anaerobes
Bacteroides spp., includingB.fragilis
Fusobacterium spp.
The following in vitro data are available, but their clinical significance is unknown.
Imipenem exhibits in vitro minimum inhibitory concentrations (MICs) of 4 μg/mL or less against most ( ≥ 90%) strains of the following microorganisms; however, the safety and effectiveness of imipenem in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.
Gram-positive aerobes
Bacillus spp.
Listeria monocytogenes
Nocardia spp.
Staphylococcus saprophyticus
Group C streptococci
Group G streptococci
Viridans group streptococci
Gram-negative aerobes
Aeromonas hydrophila
Alcaligenes spp.
Capnocytophaga spp.
Haemophilus ducreyi
Neisseria gonorrhoeae including penicillinase-producing
strains
Pasteurella spp.
Providencia stuartii
Gram-negative anaerobes
Prevotella bivia
Prevotella disiens
Prevotella melaninogenica
Veillonella spp.
Generic Name: Imipenem and Cilastatin for Injection
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