Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects

Avermectins are a group of drugs that occurs naturally as a product of fermenting Streptomyces avermitilis, an actinomycetes, isolated from the soil. Eight different structures, including ivermectin, abamectin, doramectin, eprinomectin, moxidectin, and selamectin, were isolated and divided into four...

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Published inPharmaceuticals (Basel, Switzerland) Vol. 13; no. 8; p. 196
Main Authors El-Saber Batiha, Gaber, Alqahtani, Ali, Ilesanmi, Omotayo B., Saati, Abdullah A., El-Mleeh, Amany, Hetta, Helal F., Magdy Beshbishy, Amany
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 17.08.2020
MDPI
Subjects
Animals
antihelminthic
avermectins
Biological activity
Biosynthesis
Drug dosages
Enzymes
insecticidal
Laboratories
Metabolites
Pharmacokinetics
Review
Streptomyces avermitilis
pharmacokinetics
avermectins
antihelminthic
Streptomyces avermitilis
insecticidal
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Summary:Avermectins are a group of drugs that occurs naturally as a product of fermenting Streptomyces avermitilis, an actinomycetes, isolated from the soil. Eight different structures, including ivermectin, abamectin, doramectin, eprinomectin, moxidectin, and selamectin, were isolated and divided into four major components (A1a, A2a, B1a and B2a) and four minor components (A1b, A2b, B1b, and B2b). Avermectins are generally used as a pesticide for the treatment of pests and parasitic worms as a result of their anthelmintic and insecticidal properties. Additionally, they possess anticancer, anti-diabetic, antiviral, antifungal, and are used for treatment of several metabolic disorders. Avermectin generally works by preventing the transmission of electrical impulse in the muscle and nerves of invertebrates, by amplifying the glutamate effects on the invertebrates-specific gated chloride channel. Avermectin has unwanted effects or reactions, especially when administered indiscriminately, which include respiratory failure, hypotension, and coma. The current review examines the mechanism of actions, biosynthesis, safety, pharmacokinetics, biological toxicity and activities of avermectins.
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These authors contributed equally to this work.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph13080196