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Anthelmintics

Topic updated on 12/11/15 10:36pm

Overview
 
Microtubule Assembly Inhibitors 
 Name of Drug Mechanism of Action
Indications
Albendazole, mebendazole
  • Inhibits tubulin polymerization resulting in inability to form microtubules and impaires glucose uptake
  • Ascaris lumbricoides
  • Necator americanus 
  • Trichinella spiralis 
  • Enterobius vermicularis 
  • Trichuris trichiuria 
  • Echinicoccus
  • Strongyloides stercoralis
  • Taenia solium
  • Microsporidia
Thiabendazole
  • Unknown but may inhibit helminth-specific fumarate reductase
Paralyzing Agents via Depolarization
Pyrantel pamoate
  • Acts at neuromuscular junction by stimulating nicotinic receptors resulting in paralysis via depolarization
  • Ascaris lumbricoides
  • Necator americanus 
  • Enterobius vermicularis
Agents That Increase Susceptibility of Microfilariae to Phagocytosis
Diethylcarbamazine
  • Sensitizes microfilarie to phagocytosis which immobilizes them via an unknown mechanism
  • Wucheria bancrofti
  • Brugia malayi
  • Loa loa
  • Onchocerca volvulus
  • Toxocariasis
Hyperpolarizing Agents Via Chloride Channel Opening
Ivermectin
  • Binds to glutamate-gated chloride ion (Cl-) channels in microfilaria increasing Cl- permeability resulting in paralysis via hyperpolarization
  • Intensifies GABA transmission
  • Impairs intrauterine development of Onchocera volvulus microfilariae
    • may also inhibit its release from pregnant worms
  • Onchocerca volvulus
  • Strongyloides stercolais
  • Ascaris lumbricoides
  • Trichuris trichiura
  • Enterobius vermicularis
  • Filariasis
Paralyzing Agents Via Increasing Calcium Ion Permeability
Praziquantel
  • Causes ↑ Ca2+ permeability in the parasite leading muscle contraction and ultimately paralysis by sustained contraction
  • Schistosomiasis
  • Clonorchiasis
  • Paragonimiasis
  • Taenia solium
  • Other trematodes and cestodes
Oxidative Phosphorylation Inhibitors
Niclosamide
  • Impairs ATP production by uncoupling of oxidative phosphorylation in the electron transport chain
  • Tapeworm infections
  • Fasciolopsis buski
Miscellaneous
Piperazine
  • Selectively binds to GABA receptors resulting in paralysis via hyperpolarization
  • Parasite is expelled from intestinal lumen of host via peristalsis of host
  • Ascariasis
Oxamniquine
  • Inhibits nucleic acid metabolism
  • Paralyzes via unknown mechanism
  • Schistosoma mansoni
 


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