Avermectins
Avermectins are macrocyclic lactones produced as
fermentation products of Streptomycesavermitilis.
Structurally similar to the macrolide antibiotics, they are effective at extremelylow
concentration against a wide variety of nematodes and arthropods. The
avermectins appear to induce neuromuscular paralysis by acting on a receptor of
the parasites-peripheral neurotransmitter, gamma-aminobutyric acid (GABA). In
mammals, GABA is confined to the central nervous system, and because the
avermectins do not cross the blood–brain barrier in significant concentration,
they do not appear to produce significant untoward effects in the mammalian
host. Ivermectin, a derivative of avermectin B1, is currently the drug of
choice for the treatment of onchocerciasis and is undergoing evalua-tion for
the treatment of other human filarial infections. Its usefulness in other
parasitic infections of humans remains to be established.
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