Ivermectin

Ivermectin (Mectizan) acts on parasite-specific inhibitory glutamate-gated chloride channels that are phylogenetically related to vertebrate GABA-gated chloride channels. Ivermectin causes hyperpolarization of the parasite cell membrane and muscle paralysis. At higher doses it can potentiate GABA-gated chloride channels. It does not cross the blood-brain barrier and therefore has no paralytic action in mammals, since GABA-regulated transmission occurs only in the central nervous system (CNS). Ivermectin is administered by the oral and subcutaneous routes. It is rapidly absorbed. Most of the drug is excreted unaltered in the feces. The half-life is approximately 12 hours.

Ivermectin has broad-spectrum activity in that it can affect nematodes, insects, and acarine parasites. It is the drug of choice in onchocerciasis and is quite useful in the treatment of other forms of filariasis, strongyloidia-sis, ascariasis, loiasis, and cutaneous larva migrans. It is also highly active against various mites. It is the drug of choice in treating humans infected with Onchocerca volvulus, acting as a microfilaricidal drug against the skin-dwelling larvae (microfilaria). Annual treatment can prevent blindness from ocular onchocerciasis. Ivermectin is clearly more effective than diethylcarba-mazine in bancroftian filariasis, and it reduces microfi-laremia to near zero levels. In brugian filariasis diethyl-carbamazine-induced clearance may be superior. It also is used to treat cutaneous larva migrans and disseminated strongyloidiasis. Its safe use in pregnancy has not been fully established.

The side effects are minimal, with pruritus, fever, and tender lymph nodes occasionally seen. The side effects are considerably less than those associated with di-ethylcarbamazine administration.

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