Moxidectin: a review of chemistry, pharmacokinetics and use in horses

Abstract

This article reviews the current knowledge of the use of moxidectin (MOX) in horses, including its mode of action, pharmacokinetic and pharmacodynamic properties, efficacy, safety and resistance profile. Moxidectin is a second generation macrocyclic lactone (ML) with potent endectocide activity. It is used for parasite control in horses in an oral gel formulation.The principal mode of action of MOX and of other MLs is binding to gamma-aminobutyric (GABA) and glutamate-gated chloride channels. Moxidectin is different from other MLs in that it is a poor substrate for P-glycoproteins (P-gps) and therefore less susceptible to elimination from parasite cells through this mechanism. Due to its unique physico-chemical and pharmacokinetic characteristics, MOX provides broad distribution into tissues, long half-life, significant residual antiparasitic activity, and high efficacy against encysted cyathostomin larvae. These characteristics allow for high efficacy and longer treatment interval against all important nematodes, when compared to other equine anthelmintics. A combination of MOX with praziquantel provides expanded spectrum of activity by adding activity against cestodes.Appropriate use of MOX allows for the development of strategic anthelmintic programmes that are different from those with conventional anthelmintics. Fewer treatments are required over a period of time, and therefore impose less frequent selection pressure for resistance.

The Anthelmintic Ingredient Moxidectin Negatively Affects Seed Germination of Three Temperate Grassland Species

“…noncyanogenus [30]. Moxidectin is applied worldwide to domestic ungulate species against endo- and ectoparasites [2].…”

“…Macrocyclic lactones bind to glutamate-gated chloride channels and enhance permeability for chloride ions through membranes of nerve and muscle cells of invertebrates [5]. The influx of chloride ions leads to paralysis and death of the parasite [30]. However, the mode of action of macrocyclic lactones is still not completely understood [2, 4].…”

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

“…The mode of action of milbemycins is not well understood compared to avermectin although its anti-parasitic properties have been discovered and described more than two decades ago [62]. Nemadectin is the most potent milbemycin that has unsaturated long-chain C at its 25-position.…”

Penggunaan Antiparasit Ivermectin pada Ternak: Antara Manfaat dan Risiko

“…Kondisi tersebut mengakibatkan adanya kecenderungan Ivermectin akan terakumulasi dalam jaringan lemak yang berfungsi sebagai reservoir obat sehingga konsentrasi ivermectin tertinggi terdapat pada hati dan jaringan lemak serta terendah pada otak (Juarez et al, 2018). Saat ini Ivermectin memiliki banyak famili seperti doramectin dari strain mutan Streptomyces avermitilis, selamycin (derivat doramectin), nemadectin (Streptomyces cyanogriseus)., moxidectin (derivat nemadectin), milbemycin oxime yang berasal dari makrosiklik lactone milbemycin dan eprinomycin yang merupakan derivat ivermectin (Shoop et al, 2001;Cobb and Boeckh, 2009;Xiang et al, 2010;Prichard et al, 2012;Lespine, 2013).…”