Triclabendazole

Indications

Triclabendazole is used for: Fascioliasis

Adult Dose

Fascioliasis Indicated for treatment of fascioliasis 10 mg/kg PO x2 doses administered 12 hr apart Tablets are scored and divisible into two equal halves of 125 mg If dosage cannot be adjusted exactly, round dose upwards

Child Dose

Fascioliasis Indicated for treatment of fascioliasis in patients ?6 years <6 years: Safety and efficacy not established >6 years 10 mg/kg PO x2 doses administered 12 hr apart Tablets are scored and divisible into two equal halves of 125 mg If dosage cannot be adjusted exactly, round dose upwards

Renal Dose

Administration

Contra Indications

Hypersensitivity to triclabendazole and/or to other benzimidazole derivatives or to any of the excipients

Precautions

Transient QT prolongation noted; monitor ECG in patients with a history of QT prolongation or when used in patients who receive drugs that prolong the QT interval

Pregnancy-Lactation

Pregnancy There are no available data on use in pregnant women to inform a drug- associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes Lactation There are no data on presence in human milk, effects on the breastfed infant, or effects on milk production Published animal data indicate that triclabendazole is detected in goat milk when administered as a single dose to one lactating animal When a drug is present in animal milk, it is likely that the drug will be present in human milk Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

Interactions

In vitro data suggest coadministration of triclabendazole and CYP2C19 substrates may increase plasma concentrations of CYP2C19 substrates; potential elevated concentrations of CYP2C19 substrates is expected to be transient based on the short elimination half-life and short treatment duration of triclabendazole

Adverse Effects

Side effects of Triclabendazole : >10% 10 mg/kg total Abdominal pain (56%) Hyperhidrosis (23%) 20 mg/kg total in 2 divided doses Abdominal pain (93%) Hyperhidrosis (25%) Nausea (18%) Decreased appetite (18%) Headache (14%) Urticaria (11%) 1-10% (10 mg/kg total) Vertigo (9%) Nausea (8%) Urticaria (7%) Vomiting (6%) Headache (6%) Dyspnea (5%) Pruritus (4%) Asthenia (4%) Musculoskeletal chest pain (4%) Cough (4%) Decreased appetite (3%) Chest pain (3%) Pyrexia (2%) Jaundice (2%) Chest discomfort (2%)

Mechanism of Action

Mechanism of action is not fully elucidated Studies in vitro and/or in infected animals suggest that triclabendazole and its active metabolites (sulfoxide and sulfone) are absorbed by the tegument of the immature and mature worms of Fasciola hepatica and Fasciola gigantica, leading to a decrease of the resting membrane potential, inhibition of tubulin function as well as protein and enzyme synthesis