Antihelmintics Flashcards
Mebendazole
Benzimidazole
Inhibits polymerization of helminth beta-tubulin, interfering with microtubule-dependent functions (like glucose uptake)
Pin, whip, round, and hook worms
GI disturbances
Tiabendazole
Benzimidazole
Inhibits polymerization of helminth beta-tubulin, interfering with microtubule-dependent functions (like glucose uptake)
Pin, whip, round, and hook worms
GI disturbances
Albendazole
Benzimidazole
Inhibits polymerization of helminth beta-tubulin, interfering with microtubule-dependent functions (like glucose uptake)
Pin, whip, round, and hook worms
GI disturbances
Nitazoxanide
Also antiviral
Treatment of giardiasis and cryptosporidiosis
Inhibit pyruvate:ferredoxin oxidoreductase enzyme-dependent electron transfer, important for anaerobic energy metabolism
Praziquantel
Treatment of flukes and onchocerciasis
Binds to consensus protein kinase C-binding sites in a beta-subunit of schistosome (fluke) voltage-gated calcium channels, inducing Ca2+ influx causing a rapid and prolonged contraction of the musculature, resulting in paralysis and death.
Dizziness
Abdominal distress
Piperazine
Roundworm and threadworm treatment
GABA receptor agonist, causing nerve ending hyperpolarization, inducing paralysis
Urticaria
Seizures
Pyrvinium
Pin worms only
Inhibition of mitochondrial complex 1 and interference of glucose uptake
GI disturbances
Diethylcarbamazine
Derivative of piperazine
Used for elephantiasis
Unknown MOA – Altering helminth surface membrane, interfering with arachidonate metabolism
Allergic side effects related to dying filariae
Niclosamide
Used in tapeworm – no activity for roundworms, pinworms, or hookworms
Diminishes potential of the inner mitochondrial membrane and inhibits/uncouples oxidative phosphorylation
Pruritis
Levamisole
Roundworm treatment
Blocks neuromuscular junctions through stimulation, paralyzing worm
Agranulocytosis
Not used in North America
Ivermectin
First choice for treatment of many filarial infections and onchocerciasis. Some roundworm activity, but no hookworms.
Opens glutamate-gated chloride channels and increasing Cl-, binding to GABA receptors or novel allosteric sites on acetylcholine nicotinic receptor cause increased transmission and paralysis
Skin rash/itching
Post-treatment encephalopathy