Ivermectin

Ivermectin
Ivermectin is an antiparasitic agent derived from avermectins used to treat infestations which include head lice, scabies, onchocerciasis, tropical pulmonary eosinophilia and lymphatic filariasis. It comes as both topical and oral preparations. In veterinary medicine, ivermectin is used to prevent and treat parasitic worms.

Ivermectin was first discovered in 1975 and has been used since 1981. A Nobel Prize was awarded to William Campbell and Satoshi Ōmura for its discovery and its applications. It is a key part of the World Health Organisation’s Onchocerciasis Eradication Program.

Ivermectin causes paralysis of the parasite’s musculature by binding to glutamate-gated chloride channels in the invertebrate nerve and muscle cells, opening the channels and increasing cell wall permeability. This increases the flow of chloride ions to hyperpolarize the cell membranes resulting in the paralysis.

It is metabolized in the liver by CYP450-3A47 with a plasma half-life of 16 hours and excreted almost exclusively in the faeces over an estimated 12 days.

Side effects include a transient tachycardia, fever, nausea, itching, and skin rash (when taken orally); red eyes, dry skin, and burning skin (when used topically for head lice)

Brand names: Heartgard (USA), Sklice (USA) and Stromectol (USA, NZ), Mectizan (Merck, Canada)
Chemical formula: C48H74O14

Page last updated: Nov 4, 2021 @ 3:44 am

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