Fasinash Sheep Bolus

Uses

Fasinash Sheep Bolus is an anthelmintic drug used to treat fascioliasis.

This drug is indicated for the treatment of fascioliasis in patients aged 6 years old and above.

Fasinash Sheep Bolus is also used to associated treatment for these conditions: Fascioliasis

How Fasinash Sheep Bolus works

Fasinash Sheep Bolus is an anthelmintic agent against Fasciola species.

The mechanism of action against Fasciola species is not fully understood at this time. In vitro studies and animal studies suggest that triclabendazole and its active metabolites (sulfoxide and sulfone) are absorbed by the outer body covering of the immature and mature worms, causing a reduction in the resting membrane potential, the inhibition of tubulin function as well as protein and enzyme synthesis necessary for survival. These metabolic disturbances lead to an inhibition of motility, disruption of the worm outer surface, in addition to the inhibition of spermatogenesis and egg/embryonic cells.

A note on resistance

In vitro studies, in vivo studies, as well as case reports suggest a possibility for the development of resistance to triclabendazole. The mechanism of resistance may be multifactorial and include changes in drug uptake/efflux mechanisms, target molecules, and changes in drug metabolism. The clinical significance of triclabendazole resistance in humans is not yet elucidated.

Toxicity

Oral LD50 (rat): >8 gm/kg; Oral LD50 (mouse): >8 gm/kg

A note on the use in pregnancy

There are no available data on triclabendazole use in pregnant women to calculate a drug associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Reproductive studies in animals (rat and rabbits) have not demonstrated an increased risk of increased fetal abnormalities with exposure to triclabendazole during the organogenesis period at doses which were about 0.3 to 1.6 times the maximum recommended human dose (MRHD) of 20 mg/kg.

Carcinogenesis/Mutagenesis

No genotoxic risk was noted for triclabendazole tested in 6 genotoxicity in vitro and in vivo assays.

Impairment of Fertility

No drug-related effects on reproductive performance, mating ratios or indices of fertility have been observed in a 2-generation reproductive and developmental toxicity study in rats.

A note on use in breastfeeding

There are no human findings on the presence of triclabendazole in milk, the effects on a nursing infant, or the effects on maternal milk production. The results of animal studies indicate that triclabendazole is found in goat milk when given as a single dose to a lactating female goat. When a drug is found to be present in animal milk, the likelihood that it will be found in human milk is high. Excercise caution if this drug is administered during nursing.

Food Interaction

• Take with food. Taking triclabendazole with food increases the bioavailability of triclabendazole and its sulfoxide metabolite.

Fasinash Sheep Bolus Drug Interaction

Major: dolasetronModerate: fluticasone / salmeterol, umeclidinium / vilanterolUnknown: amphotericin b lipid complex, isotretinoin, aspirin, tocilizumab, corticotropin, alteplase, loxapine, epinephrine, theophylline, ketotifen ophthalmic, amoxicillin, aluminum hydroxide, testosterone, RHO Immunoglobulin , mesalamine, benazepril, diclofenac topical

Volume of Distribution

The apparent volume of distribution (Vd) of the sulfoxide metabolite in fed patients is about 1 L/kg.

Elimination Route

After a single oral dose of 10 mg/kg triclabendazole with a 560-kcal meal to patients diagnosed with fascioliasis, mean peak plasma concentrations (Cmax) for triclabendazole, the sulfoxide, and sulfone metabolites were 1.16, 38.6, and 2.29 μmol/L, respectively. The area under the curve (AUC) for triclabendazole, the sulfoxide and sulfone metabolites were 5.72, 386, and 30.5 μmol∙h/L, respectively.

After the oral administration of a single dose of triclabendazole at 10 mg/kg with a 560 calorie meal to patients with fascioliasis, the median Tmax for the parent compound as well as the active sulfoxide metabolite was 3 to 4 hours.

Effect of Food Cmax and AUC of triclabendazole and sulfoxide metabolite increased about 2-3 times when triclabendazole was administered as a single dose at 10 mg/kg with a meal containing approximately 560 calories. Additionally, the sulfoxide metabolite Tmax increased from 2 hours in fasting subjects to 4 hours in fed subjects .

Half Life

The plasma elimination half-life (t1/2) of triclabendazole, the sulfoxide and sulfone metabolites in human is about 8, 14, and 11 hours, respectively.

Elimination Route

No data regarding excretion is available in humans. In animals, triclabendazole is primarily excreted by the biliary tract in the feces (90%), together with the sulfoxide and sulfone metabolite. Less than 10% of an oral dose is found excreted in the urine.

Innovators Monograph

You find simplified version here Fasinash Sheep Bolus