Triconex Mechanism of Action

Pharmacology: Pharmacodynamics: Metronidazole is an anti-infective agent belonging to the 5-nitroimidazole group. The antimicrobial spectrum of Metronidazole concerns exclusively anaerobic microorganisms.
Susceptible species: More than 90% are susceptible: Bacteroides sp., Fusobacterium, Clostridium sp., Bacteroides sp., C. perfringens, Bacteroides fragilis, Fusobacterium, Peptostreptococcus.
The antiparasitic activity concerns: Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica.
Pharmacokinetics: Absorption: Metronidazole is rapidly absorbed following oral administration, at least 80% in less than one hour. The peak serum concentration achieved following oral administration are similar to those obtained following intravenous administration of equivalent doses. The oral bioavailability is 100% and is not modified by simultaneous ingestion of food.
Distribution: Approximately one hour after a single dose administration of 500 mg of Metronidazole, the peak serum concentration is on average 10 µg/mL. The plasma half-life is between 8 to 10 hours. The protein binding is low: <20%. The volume of distribution is large, on average 40 L (i.e. 0.66 L/kg). Diffusion of the drug is rapid and extensive with concentrations close to serum levels in the lungs, kidneys, liver, skin, bile, CSF, saliva, seminal fluid and vaginal secretion. Metronidazole crosses the placental barrier and is excreted in breast milk.
Metabolism: Metronidazole is primarily metabolized in the liver. Oxidation yields two main metabolites: the alcoholic metabolites, the primary metabolite, with a bactericidal activity against anaerobic bacteria equal to approximately 30% of that of Metronidazole; and with an elimination half-life of 11 hours.
The acid metabolite, in small amounts, and with bactericidal activity approximately equal to 5% of that of Metronidazole.
Elimination: High liver and biliary concentration. Low concentration in the colon. Little fecal elimination. Excretion is primarily urinary, shown by the fact that the Metronidazole and its oxidation metabolites excreted in the urine account for approximately 35 to 85% of the administered dose.