Active ingredient: Mebendazole 100 mg PHARMACEUTICAL FORM: Tablet Off white to creamy flat rounded uncoated scored tablet. Scoring is non functional. Tablets should be swallowed whole. Mebendazole induces in vitro and in vivo inhibition of the glucose uptake by parasitic helminths; this is associated with glycogen depletion and a decrease in the generation of ATP, leading to inhibition of larval development. There is no evidence that mebendazole is effective in the treatment of cysticercosis. Absorption: Following oral administration, < 10% of the dose reaches the systemic circulation, due to incomplete absorption and extensive pre-systemic metabolism (first-pass effect). Maximum plasma concentrations are generally seen 2 to 4 hours after administration. Dosing with a high-fat meal leads to a modest increase in the bioavailability of mebendazole. Distribution: The plasma protein binding of mebendazole is 90 to 95%. The volume of distribution is 1 to 2 L/kg, indicating that mebendazole penetrates areas outside the vascular space. This is supported by data in patients on chronic mebendazole therapy (e.g., 40 mg/kg/day for 3–21 months) that show drug levels in tissue. Metabolism: Orally administered mebendazole is extensively metabolized primarily by the liver. Plasma concentrations of its major metabolites (amino and hydroxylated amino forms of mebendazole) are substantially higher than those of mebendazole. Impaired hepatic function, impaired metabolism, or impaired biliary elimination may lead to higher plasma levels of mebendazole. Elimination: Mebendazole, the conjugated forms of mebendazole, and its metabolites likely undergo some degree of enterohepatic recirculation and are excreted in the urine and bile. The apparent elimination half-life after an oral dose ranges from 3 to 6 hours in most patients. Steady-state Pharmacokinetics: During chronic dosing (e.g., 40 mg/kg/day for 3–21 months), plasma concentrations of mebendazole and its major metabolites increase, resulting in approximately three-fold higher exposure to steady-state compared to single dosing. INDICATIONS AND CLINICAL USE Mebendazole has a broad spectrum of anthelmintic activity and is effective in the treatment of single or mixed helminthic infestations. Clinical studies have shown it to be effective in the treatment of Enterobius vermicularis (pinworm); Ascaris lumbricoides (roundworm); Trichuris trichiura (whipworm); Ancylostoma duodenale and Necator americanus (hookworm). It has also been used to treat infestations due to Strongyloides stercoralis (threadworm) and Taenia solium (large tapeworms). CONTRAINDICATIONS VERMIN is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation. For a complete listing, see the Composition section.
