Triclabendazole - Drug of Choice for Fascioliasis

Triclabendazole is considered an antihelminthic drug of choice by the WHO to treat fascioliasis. Fascioliasis is a food-borne parasitic disease caused by infection with the L3 larvae of Fasciola hepatica. The L3 larvae work its way to the liver where it grows into an adult fluke and causes fibrosis which can lead to chronic illness. There are many factors affecting the growth and development of F. hepatica and its associated morbidity and mortality, for example, immunological factors such as age, sex, and genetic factors, diet, drug administration, animal species, and strain of worms.

Triclabendazole Uses:

  • Fascioliasis:

    • It is indicated for the treatment of fascioliasis in patients 6 years of age or older.

[bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Adult dose" collapse_text="Adult dose" ]

Triclabendazole Dose in the treatment of Fascioliasis:

  • Oral: 10 mg/kg given twice day (every 12 hours) for two doses; the 250 mg tablets are scored and can be divided into two equal halves, each containing 125 mg
  • The dose should be rounded if it cannot be adjusted exactly.

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Dose in Children" collapse_text="Dose in Children" ]

Triclabendazole Dose in the treatment of Fascioliasis:

  • Children ≥ 6 years and Adolescents:

    • Oral: 10 mg/kg/dose divided twice daily (every 12 hours) for two doses.
    • Note: The dose should be rounded up to the nearest half (125 mg) or whole tablet (250 mg).

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Dose in Pregnancy & lactation" collapse_text="Dose in Pregnancy & lactation" ]

Pregnancy Risk Category: N

      • Its use in pregnancies of human beings is not well documented. Negative fetal outcomes have not been observed in animal reproduction studies.

Use during breastfeeding:

    • Breast milk does not contain triclabendazole. It is not recommended to breastfeed if you are being treated with triclabendazole.

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Renal Dose" collapse_text="Renal Dose" ]

Dose in Kidney Disease:

The drug's label does not provide instructions for dosing adjustment or dosage information. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Dose in Liver disease" collapse_text="Dose in Liver disease" ]

Dose in Liver disease:

The drug's label does not provide instructions for dosing adjustment or dosage information. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Side effects" collapse_text="Side effects" ]

Common Side Effects of Triclabendazole:

  • Central nervous system:

    • Headache
  • Dermatologic:

    • Hyperhidrosis
    • Urticaria
  • Gastrointestinal:

    • Abdominal Pain
    • Decreased Appetite
    • Nausea

Less Common Side Effects of Triclabendazole:

  • Dermatologic:

    • Pruritus
  • Gastrointestinal:

    • Diarrhea
    • Vomiting
  • Hepatic:

    • Increased Serum Bilirubin
    • Increased Serum Aspartate Aminotransferase
    • Increased Serum Alkaline Phosphatase
    • Increased Serum Alanine Aminotransferase
    • Increased liver enzymes
  • Neuromuscular & Skeletal:

    • Musculoskeletal Chest Pain

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Contraindications & warnings" collapse_text="Contraindications & warnings" ]

Contraindications to Triclabendazole:

Do not use this product if you have an allergy to triclabendazole or any other ingredient.

Warnings and precautions

    • Hepatic toxicities:

      • It can cause liver damage. If you experience liver problems, such as nausea, vomiting, unusual weakness, tiredness, loss appetite, yellowing eyes, skin or urine color, stop using this medicine immediately and consult your doctor.
    • Prolongation of QTc:

      • The drug can prolong QT interval. Patients with a history or electrolyte abnormalities and patients who have had treatment for QT prolongation are recommended to monitor their heart rate. Monitoring of heart rate and cardiac rhythm is recommended at baseline, periodically and during treatment.

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Monitoring parameters" collapse_text="Monitoring parameters" ]

Monitoring parameters:

The drug is linked with QT-interval prolongation. Monitoring is recommended in patients with a history of heart failure, electrolyte abnormalities, and prior treatment with drugs that prolong QT interval. Monitor heart rate and a cardiac rhythm at baseline, periodically, and during the treatment. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="How to administer?" collapse_text="How to administer?" ]

How to administer Triclabendazole?

To be swallowed whole or to be crushed and mixed with applesauce. The crushed tablet mixed with applesauce is stable for up to 4 hours. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Pharmacology & MOA" collapse_text="Pharmacology & MOA" ]

Mechanism of action of Triclabendazole:

Triclabendazole, which is highly effective against the trematodes in the genus Fasciola, is widely used. It works by disorganizing the tegument formed by helminthic parasites. Triclabendazole, and its active metabolites, are absorbed into the tegument by mature worms. This results in an increase of larval mortality. It causes death to the helminths, by decreasing their motility and disrupting the cell structure, including inhibition of spermatogenesis. Absorption:

  • Absorption is increased with food.

Protein binding:

  • Triclabendazole: 96.7%;
  • Sulfoxide metabolite: 98.4%;
  • Sulfone metabolite: 98.8% in human plasma

Metabolism:

  • It is primarily metabolized by CYP1A2 (~64%) into its active sulfoxide metabolite and to a lesser extent by CYP2C9, CYP2C19, CYP2D6, CYP3A, and FMO.
  • Sulfoxide metabolite is further metabolized primarily by CYP2C9 to the active sulfone metabolite.

Half-life elimination:

  • Triclabendazole: 8 hours;
  • Sulfoxide metabolite: 14 hours;
  • Sulfone metabolite: 11 hours

Time to peak: T 3.0 ± 0.4 hours. [/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="International Brands" collapse_text="International Brands" ]

International Brand Names of Triclabendazole:

  • Egaten
  • Claben
  • Clabenzole
  • Egaten
  • Fasinex
  • Flucide

[/bg_collapse]   [bg_collapse view="button-blue" color="#f7f2f2" icon="arrow" expand_text="Brands in Pakistan" collapse_text="Brands in Pakistan" ]

Triclabendazole Brands Names in Pakistan:

No Brands Available in Pakistan. [/bg_collapse]