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Review

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

by
Gaber El-Saber Batiha
1,*,†,
Ali Alqahtani
2,
Omotayo B. Ilesanmi
3,
Abdullah A. Saati
4,
Amany El-Mleeh
5,
Helal F. Hetta
6,7 and
Amany Magdy Beshbishy
8,*,†
1
Department of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, Egypt
2
Department of Pharmacology, College of Pharmacy, King Khalid University, Guraiger, Abha 62529, Saudi Arabia
3
Department of Biochemistry, Faculty of Science, Federal University Otuoke, Otuoke 561, Nigeria
4
Department of Community Medicine & Pilgrims Healthcare, Faculty of Medicine, Umm Al-Qura University Makkah, Mecca 24382, Saudi Arabia
5
Department of Pharmacology, Faculty of Veterinary Medicine, Menoufia University, Shibin Al Kawm 32511, Egypt
6
Department of Medical Microbiology and Immunology, Faculty of Medicine, Assiut University, Assiut 71515, Egypt
7
Department of Internal Medicine, University of Cincinnati College of Medicine, Cincinnati, OH 45221, USA
8
National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Nishi 2-13, Inada-cho, Obihiro 080-8555, Hokkaido, Japan
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceuticals 2020, 13(8), 196; https://doi.org/10.3390/ph13080196
Submission received: 19 July 2020 / Revised: 9 August 2020 / Accepted: 13 August 2020 / Published: 17 August 2020
(This article belongs to the Special Issue Antiparasitics)

Abstract

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.
Keywords: avermectins; antihelminthic; insecticidal; pharmacokinetics; Streptomyces avermitilis avermectins; antihelminthic; insecticidal; pharmacokinetics; Streptomyces avermitilis
Graphical Abstract

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MDPI and ACS Style

El-Saber Batiha, G.; Alqahtani, A.; Ilesanmi, O.B.; Saati, A.A.; El-Mleeh, A.; Hetta, H.F.; Magdy Beshbishy, A. Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals 2020, 13, 196. https://doi.org/10.3390/ph13080196

AMA Style

El-Saber Batiha G, Alqahtani A, Ilesanmi OB, Saati AA, El-Mleeh A, Hetta HF, Magdy Beshbishy A. Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals. 2020; 13(8):196. https://doi.org/10.3390/ph13080196

Chicago/Turabian Style

El-Saber Batiha, Gaber, Ali Alqahtani, Omotayo B. Ilesanmi, Abdullah A. Saati, Amany El-Mleeh, Helal F. Hetta, and Amany Magdy Beshbishy. 2020. "Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects" Pharmaceuticals 13, no. 8: 196. https://doi.org/10.3390/ph13080196

APA Style

El-Saber Batiha, G., Alqahtani, A., Ilesanmi, O. B., Saati, A. A., El-Mleeh, A., Hetta, H. F., & Magdy Beshbishy, A. (2020). Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals, 13(8), 196. https://doi.org/10.3390/ph13080196

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