Merop Mechanism of Action

Antibacterial.
Pharmacology: Pharmacodynamics: Mode of Action: Meropenem Trihydrate (MEROP) Injection is a carbapenem antibiotic structurally similar to imipenem for parenteral use, that is relatively stable to human dehydropeptidase-1 (DHP-1) and therefore does not require the addition of an inhibitor of DHP-1. Meropenem Trihydrate (MEROP) Injection exerts its bactericidal action by interfering with vital bacterial cell wall synthesis. The ease with which it penetrates bacterial cell walls, its high level of stability to all serine beta-lactamases and its marked affinity for the Penicillin Binding Proteins (PBPs) explain the potent bactericidal action of Meropenem Trihydrate (MEROP) Injection against a broad spectrum of aerobic and anaerobic bacteria.
Minimum bactericidal concentrations (MBC) are commonly the same as the minimum inhibitory concentrations (MIC). For 76% of the bacteria tested, the MBC: MIC ratios were 2 or less. The in vitro antibacterial spectrum of Meropenem Trihydrate (MEROP) Injection includes the majority of clinically significant Gram-positive and Gram-negative, aerobic and anaerobic strains of H bacteria, as shown as follows: Gram-positive aerobes: Bacillus spp., Corynebacterium diphtheriae, Enterococcus faecalis, Lactobacillus spp., Staphylococcus aureus (penicillinase negative and positive), Staphylococci-coagulase-negative; including Staphylococcus epidermis, Staphylococcus saprophyticus, Staphylococcus intermedius, Streptococcus pneumoniae (penicillin susceptible and resistant), Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus bovis, Streptococcus viridans.
Gram-negative aerobes: Acinetobacter baumannii, Campylobacter coli, Campylobacter jejuni, Citrobacter freundii, Citrobacter diversus, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae (including beta-lactamase positive and ampicillin resistant strains), Haemophilus parainfluenzae, Helicobacter pylori, Neisseria gonorrhoeae (including beta-lactamase positive, penicillin resistant and spectinomycin resistant strains), Klebsiella pneumoniae, Klebsiella aerogenes, Moraxella catarrhalis, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Salmonella spp., Vibrio cholerae.
Anaerobic bacteria: Bacteroides fragilis, Bacteroides coagulans, Bacteroides uniformis, Clostridium perfringens, Clostridium sporogenes, Clostridium innocuum, Fusobacterium mortiferum, Fusobacterium varium, Peptostreptococcus anaerobius, Peptostreptococcus micros, Peptococcus saccharolyticus, Propionibacterium acnes, Propionibacterium avidum, Enterococcus faecium and methicillin-resistant staphylococci have been found to be resistant to meropenem.
Pharmacokinetics: A 30-minute intravenous infusion of a single dose of Meropenem Trihydrate (MEROP) Injection in healthy volunteers results in peak plasma levels of approximately 23 microgram/mL for the 500 mg dose and 49 microgram/mL for the 1 g dose.
After an IV dose of 500 mg, plasma levels of Meropenem Trihydrate (MEROP) Injection decline to values of 1 microgram/mL or less, 6 hours after administration.
When multiple doses are administered at 8 hourly intervals to subjects with normal renal function, accumulation of Meropenem Trihydrate (MEROP) Injection does not occur. In subjects with normal renal function, Meropenem Trihydrate (MEROP) Injection's elimination half-life is approximately 1 hour. Plasma protein binding of Meropenem Trihydrate (MEROP) Injection is approximately 2%.
Meropenem Trihydrate (MEROP) Injection penetrates well into most body fluids and tissues including cerebrospinal fluid of patients with bacterial meningitis, achieving concentrations in excess of those required to inhibit most bacteria.
Studies in children have shown that the pharmacokinetics of Meropenem Trihydrate (MEROP) Injection in children is similar to those in adults. The elimination half-life for Meropenem Trihydrate (MEROP) Injection was approximately 1.5 hours in pediatric patients of age 3 months to 2 years and the pharmacokinetics are linear over the dose range of 10 to 40 mg/kg. Pharmacokinetic studies in patients with renal insufficiency have shown the plasma clearance of Meropenem Trihydrate (MEROP) Injection correlates with creatinine clearance. Dosage adjustments are necessary in subjects with renal impairment. Pharmacokinetic studies in the elderly have shown a reduction in plasma clearance of Meropenem Trihydrate (MEROP) Injection, which correlated with age-associated reduction in creatinine clearance. Pharmacokinetic studies in patients with liver disease have shown no effects of liver disease on the pharmacokinetics of Meropenem Trihydrate (MEROP) Injection.