nce of triclabendazole in human milk, the effects on the breastfed infant, or theeffects on milk production. Published animal data indicate that triclabendazole is detected in goat milk whenadministered as a single dose to one lactating animal. When a drug is present in animal milk, it is likely that thedrug will be present in human milk. The developmental and health benefits of breastfeeding should beconsidered along with the mother’s clinical need for EGATEN and any potential adverse effects on thebreastfed infant from EGATEN or from the underlying maternal condition.
8.4 Pediatric Use
Safety and effectiveness of EGATEN has been established in pediatric patients aged 6 years and older.
Safety and effectiveness of EGATEN in pediatric patients below the age of 6 years have not been established.
8.5 Geriatric Use
Clinical studies of EGATEN did not include sufficient numbers of patients aged 65 and over to determinewhether the elderly respond differently from younger patients. In general, dose selection for an elderly patientshould be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and ofconcomitant disease or other drug therapy.
8.6 Renal Impairment
EGATEN has not been studied in patients with renal impairment.
8.7 Hepatic Impairment
EGATEN has not been studied in patients with hepatic impairment.
10 OVERDOSAGE
The reported symptom of overdosage following ingestion of approximately 54 mg/kg of EGATEN
(approximately 2.7 times the recommended dose) was nausea. The patient recovered following osmotic diuresis.
11 DESCRIPTION
EGATEN (triclabendazole) tablet is an orally administered anthelmintic for immediate release. Triclabendazoleis designated chemically as benzimidazole derivative, 6-chloro-5-(2, 3-dichlorophenoxy)-2-(methylthio)-1Hbenzimidazole(triclabendazole). The molecular formula for triclabendazole is C14H9Cl3N2OS and the molecular
weight is 359.65 g/mol. The chemical structure of triclabendazole is shown below:
Triclabendazole is a white or almost white, crystalline powder.
EGATEN tablets are pale red, speckled, capsule shaped, biconvex tablets, with imprint “EG EG” on one sideand functionally scored on both sides. Each tablet contains 250 mg of triclabendazole.
Inactive Ingredients: colloidal silicon dioxide, iron oxide red, lactose monohydrate, maize starch, magnesiumstearate, methylhydroxyethylcellulose.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Triclabendazole is an anthelmintic against Fasciola species [see Microbiology (12.4)].
12.2 Pharmacodynamics
Triclabendazole exposure-response relationships and the time course of pharmacodynamics response areunknown.
12.3 Pharmacokinetics
After oral administration of a single dose of 10 mg/kg triclabendazole with a 560-kcal meal to patients withfascioliasis, mean peak plasma concentrations (Cmax) for triclabendazole, the sulfoxide and sulfone metaboliteswere 1.16, 38.6, and 2.29 mol/L, respectively. The area under the curve (AUC) for triclabendazole, the
sulfoxide and sulfone metabolites were 5.72, 386, and 30.5 mol∙h/L, respectively.
Absorption
Following oral administration of a single dose of triclabendazole at 10 mg/kg with a 560-kcal meal to patientswith fascioliasis, the median Tmax for the parent compound and the sulfoxide metabolite was 3 to 4 hours.
Effect o |
