Benzimidazoles Flashcards
Benzimidazoles
Albendazole
Mebendazole
Thiabendazole
Primarily used for helminthes (worms)
Ranging from common pinworms in children to pathogens causing massive cystic lesions in brain
Most intestinal worms can be cured with a single dose
Tissue invasive diseases- prolonged courses
Mebendazole/thiabendazole no longer available in US
Benzimidazoles MOA
Interfere with elongation of the microtubules that are responsible for parasitic cellular structure- leading to disruption of growth and division
Benzimidazoles Spectrum
Nematodes (roundworms): Ascaris lumbricoides (roundworm) Enterobius vermicularis (pinworm) Necator americanus (hookworm) Strongyloides stercoralis (threadworm)
Cestodes (tapeworms)
Echinococcus (liver abscess)
Taenia solium (neurocysticercosis)
Benzimidazoles Adverse Effects
Albendazole very well tolerated (especially as single dose)
Multi dose regimens- primarily GI; hepatotoxicity and neutropenia rare
Thiabendazole most toxic- CNS effects
Generally avoid them in pregnancy (some data- may be safe after first trimester)
Benzimidazoles Important Facts
Appear to be C450 substrates Strong inducers (phenytoin/rifampin) may lower serum levels
Oral absorption of albendazole is limited; not a problem for intestinal nematode infections; interactions would not be a concern
Be careful of interactions with treatment of systemic infections
For some parasitic infections, drug induced killing of the parasite releases antigens that can cause allergic reactions
Corticosteroids sometimes given to mitigate the effect
Benzimidazoles Good For
Single dose- most intestinal nematode infections
Alternative for treatment of Strongyloides
Treatment for tissue invasive Echinococcus or Taenia infection