eneric name: metronidazole Brand name: Triconex Forte 500 mg tablet Category: antiprotozoal/ amoebicide Formulation: each tablet

contains: metronidazole 500mg Pharmacodynamic properties: Metronidazole is an anti-infective agent belonging to the 5-nitroimidazole group . The antimicrobial spectrum of Metronidazole concerns exclusively anaerobic mic roorganisms. Susceptible species: more than 90% are susceptible. Bacteroides sp., Fusobacteri um Clostridium sp., C. perfringes, Bacteroides fragilis, Fusobacterium, Peptostr eptococcus The antiparasitic activity concerns: trichomonas vaginalis, Giardia intestinalis , Entamoeba histolytica Pharmacokinetic properties: Absorption: Metronidazole is rapidly absorbed following oral administration, at least 80% in less than one hour. The peak serum concentrations achieved following oral admin istration are similar to those obtained following intravenous administration of equivalent doses. The oral bioavailability is 100% and is not modified by simult aneous ingestion of food. Distribution: Approximately one hour after a single dose administration of 500 mg of Metronida zole, the peak serum concentration is on average 10 mcg/mL. The plasma half-life is between 8 to 10 hours. The protein binding is low: <20%. The volume of distr ibution is large, on average 40 L (i.e. 0.66L/kg). Diffusion of the drug is rapi d and extensive with concentrations close to serum levels in the lungs, kidneys, liver, skin, bile, CSF, saliva, seminal fluid and vaginal secretion. Metronidaz ole crosses the placenta barrier and is excreted in breast milk. Metabolism: Metronidazole is primarily metabolized in the liver. Oxidation yields two main m etabolites: -the alcoholic metabolites, the primary metabolites, with a bactericidal activit y 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 approxima tely equal to 5% of that of Metronidazole. Elimination: High liver and biliary concentration. Low concentration in the colon. Little fec al elimination. Excretion is primarily urinary, shown by the fact that the Metro nidazole and its oxidation metabolites excreted in the urine account for approxi mately 35 to 85% of the administered dose. Indication: The indications are based on the anti-parasitic and antibacterial activity, and on the pharmacokinetic characteristics of Metronidazole. They are restricted to infections caused by the microorganism defined above as susceptible to Metronida zole: Urethritis and vaginitis caused by Trichomonas vaginalis. -intestinal and hepatic amoebiasis -Giardia intestinalis (Lambilasis_ -infections caused by anaerobic bacteria -amoebiasis -urogenital trichomoniasis -non-specific vaginalis -Giardiasis -curative treatment of medico-surgical infections due to susceptible anaerobic p athogens -prophylaxis against infections caused susceptible anaerobic pathogens in high r isk surgical contents

-conversion from prophylais or curative injectable treatment of infection due to susceptible anaerobic contents. Metronidazole is also indicated in the treatment of trichomoniasis in both male and female patients when the presence of trichomonas has been demonstrated by we t smear or culture and for sexual partners of those patients who have recurrence of infections. Trichomonal infection is demonstrated for other protozoa includi ng Entamoeba histolytica, giardiasis and liver abscess. Contraindication: It should not be administered to patients with active neurological disorders or history of blood dyscrasias, hypothyroidism and hypoadrenalism. Precaution: When there is clinical evidence of a trichomonal infection, the sexual partner s hould be treated, concomitantly to avoid re-infestations. Although no persistent hematologic abnormalities have been reported in clinical studies, total and dif ferential leukocytes counts should be made before and after treatment especially if a second course of therapy is needed. Treatment should be discontinued if at axia or any symptoms CNS occur. Metronidazole has been shown to be carcinogenic in mice. Unnecessary use of the drug should be reserved for conditions described in the indications. The use of this drug in the first trimester of pregnancy should be avoided. Duri ng the second trimester of pregnancy, its use should be restricted to those pati ents in whom topical measures have been proven inadequate. Metronidazole is secr eted in the breast milk when administered to nursing mothers. Its use should avo ided although there is no reported effect to the newborn. Drug Interactions: When given with alcohol, Metronidazole may provoke a disulfiram-like reaction in some patients. Concomitant administration of Metronidazole and disulfiram, have caused acute psychoses or confusion. Metronidazole can enhance the anticoagulan t effects of Warfarin. Metronidazole is also reported to impair the metabolism o f excretion of the following drugs, with the consequent potential for an increas ed risk of adverse effects: phenytoin, lithium, and fluorouracil. Adverse effects: Infrequent and minor adverse effects include metallic taste, furred tongue and d ry mouth, gastrointestinal disturbances such as diarrhea, anorexia, vomiting, ep igastric distress, constipation, occasional flushing, and headaches, especially with concomitant ingestion with alcohol, dizziness and rarely incoordination and ataxia have been reported. Occasionally patients have complained of numbness or paresthesia of extremities, fleeting joint pains have been experienced, as have confusion, irritability, depression, urticaria, pruritus, dysuria, cystitis, ur ethral discomfort and darkening of the urine have occurred in patients receiving the drug. Dosage: Adult dose to be taken with or after meals, or as prescribed by a physician. Amoebiasis, Balantidiasis and Blastocystitis hominis infection: 1 tablet three t imes daily for 5 to 10 days or 3 to 5 tablets as a single dose daily for 2 or 3 days. Giardiasis: 4 tablets once daily for 3 successive days or 1 tablet twice daily f or 7 to 10 days. Trichomoniasis: 4 tablets once daily or 1 tablet twice daily for 7 days. Bacterial vaginosis: 4 tablets once daily or 1 tablet twice daily for 5 to 7 day s. Anaerobic bacterial infections: 1 tablet every 8 hours Prevention of postoperative anaerobic bacterial infections: 1 tablet every 8 hou rs before surgery followed postoperatively by intravenous or rectal administrati on until oral therapy is possible. Cautions: foods, drugs, devices and cosmetics act prohibits dispensing without p rescription Availability: box of 100s; foil strip of 10 s Store at temperatures not exceeding 30 degrees Celsius.