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Ivermectin

Ivermectin is an oral macrocyclic lactone with broad activity against onchocerciasis, strongyloidiasis, lymphatic filariasis, scabies, head lice and several other parasites. It is a core drug in mass administration programmes. It must not be given in areas where loiasis is endemic without testing, because heavy Loa loa infection can cause serious brain illness.

Class. Antiparasitic; macrocyclic lactone.

Mechanism. Binds glutamate-gated chloride channels in invertebrate nerve and muscle cells, causing paralysis and death of the parasite. It has little effect in humans because these channels are absent.

Pharmacokinetics. Oral absorption increased by food. Half life about 18 hours. Metabolised by CYP3A4; excreted in faeces. It is a P-glycoprotein substrate.

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