Stromectol
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This article includes a list of references or external links, but its sources remain unclear because it has insufficient inline citations. Please help to improve this article by introducing more precise citations where appropriate. (March 2009)IvermectinSystematic (IUPAC) nameIvermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b)IdentifiersCAS number70288-86-7 71827-03-7ATC codeP02CF01PubChem6474909DrugBankAPRD01058Chemical dataFormulaC48H74O14 (22,23-dihydroavermectin B=1a)C47H72O14 (22,23-dihydroavermectin B=1b) Mol. mass875.10 g/molPharmacokinetic dataBioavailability ?Protein binding93%Metabolismliver; CYP450Half life18 hoursExcretionfeces; <1% urineTherapeutic considerationsPregnancy cat.CLegal statusRoutesOralIvermectin (22,23-dihydroavermectin B1a + 22,23-dihydroavermectin B1b) is a broad-spectrum antiparasitic medication.It is sold under brand names Stromectol in the United States, Mectizan in Canada by Merck and Ivexterm in Mexico by Valeant Pharmaceuticals International.// UsesIt is traditionally used against worms (except tapeworms), but more recently found to be effective against mites and some lice too.Mectizan is currently being used to help eliminate river blindness (onchocerciasis) in the Americas and stop transmission of lymphatic filariasis around the world. PharmacodynamicsIvermectin and the related avermectin (an insecticide most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission.The drug binds and activates glutamate-gated chloride channels (GluCls) present in neurons and myocytes. PharmacokineticsIvermectin can be given either per os or parenterally. It does not readily cross the blood-brain barrier of mammals, although crossing may still become significant if ivermectin is given at high doses (in which case, brain levels peak 2-5 hours after administration). ToxicityThe main concern is neurotoxicity, which in most mammalian species may manifest as CNS depression, and consequent ataxia, as might be expected from potentiation of inhibitory GABA-ergic synapses EcotoxicityField studies have demonstrated that the dung of animals treated with ivermectin supports a significantly reduced diversity of invertebrates, and that the dung persists for longer. Indications for use HumansIvermectin is a broad-spectrum antiparasitic agent. It is mainly used in humans in the treatment of onchocerciasis, but is also effective against other worm infestations (such as strongyloidiasis, ascariasis, trichuriasis and enterobiasis). More recent evidence supports its off-label use in the treatment of mites such as scabies, usually limited to cases that prove resistant to topical treatments and/or who present in advanced state (such as Norwegian scabies).
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