Ivermectin (Molecule of the Month for March 2007)
Avermectin, Stromectol, Mectizan
Ivermectin is an anti-parasite medication and is effective against most common intestinal worms (except tapeworms), most mites, and some lice. While normally used to treat animals, it is also prescribed to humans to treat infections of Strongyloides stercoralis and onchocerciasis (river blindness). Ivermectin is derived from the bacterium Streptomyces avermitilis and kill by interfering with the target animal's nervous system. Ivermectin is a mixture of two compounds 22,23-dihydroavermectin B1a and 22,23-dihydroavermectin B1b, which differ by a single ethyl or methyl side group. In General Use Pesticide (GUP) formulations, Ivermectin is classified by the United States' Environmental Protection Agency as toxicity category IV, or very low. This means that although highly poisonous to insects, mammals should not generally be adversely affected by normal use of ivermectin pesticide formulations.
Ivermectin is an antihelmintic used mainly in the treatment of onchocerciasis in humans, and also for strongyloidiasis, ascariasis, trichuriasis and enterobiasis. It is being used in mass treatment of programmes in endemic regions. Ivermectin is an antiparasitic agent with a broad spectrum of activity against nematode worms and ectoparasites in animals, and has been in use for nearly a decade. It can also be used off-label for the treatment of topical cream resistant mites
Ivermectin inactivates parasitic nematodes, arachnids, and insects. It binds to glutamate gated chloride channels (GABA mediated, present in nerves and muscle cells). This binding promotes increased membrane permeability to chloride ions which cases hyperpolarization of the nerve or muscle cell. This results in neuro-muscular paralysis which may lead to death.
Formal Chemical Name (IUPAC)
Update by Karl Harrison
(Molecule of the Month for March 2007 )