Triclabendazole
Triclabendazole Uses, Dosage, Side Effects, Food Interaction and all others data.
Triclabendazole, manufactured by Novartis pharmaceuticals, is an antihelminthic drug that was approved by the FDA in February 2019 for the treatment of fascioliasis in humans. Fascioliasis is a parasitic infection often caused by the helminth, Fasciola hepatica, which is also known as “the common liver fluke” or “the sheep liver fluke” or by Fasciola gigantica, another helminth. These parasites can infect humans following ingestion of larvae in contaminated water or food.
Triclabendazole was previously used in the treatment of fascioliasis in livestock, but is now approved for human use.This drug is currently the only FDA-approved drug for individuals with fascioliasis, which affects 2.4 million people worldwide.
Triclabendazole and its metabolites are active against both the immature and mature worms of Fasciola hepatica andFasciola gigantica helminths.
| Trade Name | Triclabendazole |
| Availability | Prescription only |
| Generic | Triclabendazole |
| Triclabendazole Other Names | Triclabendazole |
| Related Drugs | Egaten |
| Type | Oral |
| Formula | C14H9Cl3N2OS |
| Weight | Average: 359.65 Monoisotopic: 357.9501172 |
| Protein binding | Protein-binding of triclabendazole, sulfoxide metabolite and sulfone metabolite in human plasma was 96.7%, 98.4% and 98.8% respectively. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Triclabendazole 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.
Triclabendazole is also used to associated treatment for these conditions: Fascioliasis
How Triclabendazole works
Triclabendazole 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.
Triclabendazole 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.
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