triclabendazole (Egaten)

Indications

• treatment of liver flukes, fascioliasis & paragonimiasis

Dosage

• 2 doses of 10 mg/kg given 12 hours with food

Tabs: 250 mg

Pharmacokinetics

• volume of distribution: 1 L/kg
• protein binding 96-98%
• 1/2life is 8 hours & 11-14 hours for sulfone & sulfoxide metabolites
• metabolized by CYP1A2 (approximately 64%) into its active sulfoxide metabolite & to a lesser extent by CYP2C9, CYP2C19, CYP2D6, CYP3A, & FMO
• the sulfoxide metabolite is further metabolized primarily by CYP2C9 to the active sulfone metabolite & to a lesser extent by CYP1A1, CYP1A2, CYP1B1, CYP2C19, CYP2D6 & CYP3A4
• in animals, the drug is largely excreted via the biliary tract in the feces (90%), together with the sulfoxide & sulfone metabolite
  • < 10% of an oral dose is excreted in the urine

Adverse effects

• headache, abdominal pain, musculoskeletal chest pain
• urticaria, pruritus, hyperhidrosis
• nausea, vomiting, diarrhea, decreased appetite

Notes

• treatment in hospital may be required

More general terms

• antihelmintic

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=50248
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=67609548