Antinematodal Drugs Carlos E. Lanusse, Juan M. Sallovitz, Sergio F. Sanchez Bruni, and Luis I. Alvarez The economic importance of helminth infections in livestock has long been recognized and it is probably for this reason that the most important advances in the chemotherapy of helminthiasis have come from the animal health area Horton, Anthelmintics are used in all animal species and man.
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See other articles in PMC that cite the published article. Abstract Anthelmintics are some of the most widely used drugs in veterinary medicine. Here we review the mechanism of action of these compounds on nematode parasites. Included are the older classes of compounds; the benzimidazoles, cholinergic agonists and macrocyclic lactones. We also consider newer anthelmintics, including emodepside, derquantel and tribendimidine.
In the absence of vaccines for most parasite species, control of nematode parasites will continue to rely on anthelmintic drugs.
As a consequence, vigilance in detecting drug resistance in parasite populations is required. Since resistance development appears almost inevitable, there is a continued and pressing need to fully understand the mode of action of these compounds. It is also necessary to identify new drug targets and drugs for the continued effective control of nematode parasites. Keywords: anthelmintic, parasite, benzimidazoles, avermectins, cholinergic, emodepside, derquantel Introduction Anthelmintics are drugs that are used to treat infections caused by parasitic worms helminths [ 1 ].
There are three major groups of helminths namely: nematodes roundworms , trematodes flukes and cestodes tapeworms. These groups of helminths are divided into two phyla; nematodes roundworms and platyhelminths trematodes and cestodes [ 2 ]. Anthelmintics either kill worms or cause their expulsion from the body, without causing any significant damage to the host [ 3 ].
Although there is a high prevalence of parasitic worms, the progress of anthelmintic drug discovery and development by pharmaceutical companies has been slow over the years. One contributing factor is that the majority of those suffering from helminth infections live in developing nations who lack the resources to support a profitable drug market [ 4 ]. Development of new anthelmintics is limited by high costs and modest global markets for antiparasitic drugs and chemicals.
Many anthelmintic drugs used to treat humans were first developed and marketed as veterinary drugs [ 9 — 11 ]. There are only a few classes of anthelmintics including; benzimidazoles, imidazothiazoles, tetrahydopyrimidines, macrocyclic lactones, amino-acetonitrile derivatives, spiroindoles and cyclooctadepsipeptides.
Here we review the mode of action of several classes of drug used to treat infections with parasitic nematodes. Benzimidazoles BZs Thiabendazole was the first benzimidazole anthelmintic agent produced. Since the introduction of thiabendazole in , a number of benzimidazoles with improved efficacy and extended spectrum of action have been developed [ 12 ].
These include mebendazole, albendazole and flubendazole Figure 1. The initial mode of action of benzimidazoles was thought to be inhibition of various parasite metabolic enzymes including fumarate reductase and malate dehydrogenase [ 13 , 14 ].
This results in the destruction of cell structure and consequent death of the parasite [ 15 ].
A BRIEF REVIEW ON THE MODE OF ACTION OF ANTINEMATODAL DRUGS
Its commercial introduction into the U. It is effective against a wide variety of parasites. IM to horses: Gasterophilus intestinalis, Parascaris equorum, Strongylus vulgaris, Strongylus edentatus, Oxyuris equi, Habronema muscae. Adult Trichostrongylus Benzimidazoles Eight benzimidazoles are available for clinical use including: thiabendazole, mebendazole, fenbendazole, cambendazole, oxibendazole, flubendazole, oxfendazole, and albendazole. In addition, there are pro-benzimidazoles.