Natural products : Avermectins (Mectizan) - Synthesis and Drug Profile
Natural products
Mode of action: Avermectins specifically open the chloride
channels in the invertebrate system distinct from the GABA-gated and
glutamate-gated chloride channels.
Metabolism: It is metabolized and it gives
3-O-demethyl-22,23-dihydroavermectin B1α monosaccharide.
Properties and uses: Avermectins are macrocyclic lactones with broad
antinematocidal activity. This class of compound was isolated from a
fermentation broth of a soil actinomycetics (Streptomycin avermitils). The drug avermectin is now effectively being used to treat
and control onchocera volvulus, the
filarial infection responsible for liver
blindness. Ivermectin is a mixture of B1a and B1b (80:20) and is prepared by
catalytic reduction of ivermectin B1 (Abamectin)
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