Abstract
Modes of action of anthelmintic drugs are described. Some anthelmintic drugs act rapidly and selectively on neuromuscular transmission of nematodes. Levamisole, pyrantel and morantel are agonists at nicotinic acetylcholine receptors of nematode muscle and cause spastic paralysis. Dichlorvos and haloxon are organophosphorus cholinesterase antagonists. Piperazine is a GABA (gamma-amino-butyric acid) agonist at receptors on nematode muscles and causes flaccid paralysis. The avermectins increase the opening of glutamate-gated chloride (GluCl) channels and produce paralysis of pharyngeal pumping. Praziquantel has a selective effect on the tegument of trematodes and increases permeability of calcium. Other anthelmintics have a biochemical mode of action. The benzimidazole drugs bind selectively to beta-tubulin of nematodes, cestodes and fluke, and inhibit microtubule formation. The salicylanilides: rafoxanide, oxyclozanide, brotianide and closantel and the substituted phenol, nitroxynil, are proton ionophores. Clorsulon is a selective antagonist of fluke phosphoglycerate kinase and mutase. Diethylcarbamazine blocks host, and possibly parasite, enzymes involved in arachidonic acid metabolism, and enhances the innate, nonspecific immune system.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Anthelmintics / chemistry
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Anthelmintics / pharmacology*
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Anthelmintics / therapeutic use
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Calcium Channel Agonists / chemistry
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Calcium Channel Agonists / pharmacology
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Calcium Channel Agonists / therapeutic use
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Cholinesterase Inhibitors / pharmacology
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Cholinesterase Inhibitors / therapeutic use
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Diethylcarbamazine / chemistry
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Diethylcarbamazine / pharmacology
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Diethylcarbamazine / therapeutic use
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Drug Resistance / genetics
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Drug Resistance / physiology
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GABA Agonists / chemistry
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GABA Agonists / pharmacology
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GABA Agonists / therapeutic use
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Helminthiasis / drug therapy
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Helminthiasis / physiopathology
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Helminthiasis, Animal
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Helminths / drug effects*
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Helminths / physiology
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Ionophores / chemistry
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Ionophores / pharmacology
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Ionophores / therapeutic use
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Microtubules / drug effects
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Microtubules / metabolism
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Microtubules / physiology
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Nicotinic Agonists / chemistry
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Nicotinic Agonists / pharmacology
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Nicotinic Agonists / therapeutic use
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Phosphoglycerate Kinase / antagonists & inhibitors
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Phosphoglycerate Mutase / antagonists & inhibitors
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Structure-Activity Relationship
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Tubulin / metabolism
Substances
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Anthelmintics
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Calcium Channel Agonists
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Cholinesterase Inhibitors
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GABA Agonists
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Ionophores
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Nicotinic Agonists
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Tubulin
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Phosphoglycerate Kinase
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Phosphoglycerate Mutase
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Diethylcarbamazine