Triclabendazole is an anthelmintic medication used primarily in the treatment of infections caused by liver flukes, particularly Fasciola hepatica and Fasciola gigantica. Liver flukes are parasitic flatworms that can infect humans and other mammals through the ingestion of contaminated water or plants.

Triclabendazole works by disrupting the fluke's metabolism, leading to paralysis and death of the parasite. It's considered highly effective against liver fluke infections and is often the first-line treatment.

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.

Triclabendazole dose in adult

Triclabendazole Dose in the treatment of Fascioliasis:

• You take it by mouth.
• You take 10 milligrams of triclabendazole for every kilogram of your body weight.
• You need to take it every 12 hours, but only for two doses.

For example, if someone weighs 50 kilograms, they would take 500 milligrams of triclabendazole every 12 hours for two doses. If they have tablets of 250 milligrams, they can split them into halves to get the right dose. If the dose can't be exact, it's better to round it up.

Triclabendazole dose in children

Triclabendazole Dose in the treatment of Fascioliasis:

In children aged 6 years and older, as well as adolescents:

• The dose of triclabendazole is given by mouth.
• They should take 10 milligrams of triclabendazole for every kilogram they weigh, every 12 hours, for just two doses.

For example, if a child weighs 30 kilograms, they would take 300 milligrams of triclabendazole every 12 hours for two doses. If the dose can't be measured exactly, it's fine to round it up to the nearest half (125 milligrams) or whole tablet (250 milligrams).

Pregnancy Risk Category: N

• In studies done on animals, no harmful effects were seen when they were given triclabendazole during pregnancy.
• However, there isn't much information available about using triclabendazole in pregnant women from human studies, as of 2008.

Use during breastfeeding:

• It's uncertain whether triclabendazole passes into breast milk.
• The manufacturer advises that if a mother is considering breastfeeding while using triclabendazole, she should weigh the potential risk of the baby being exposed to the medication against the benefits of breastfeeding for the baby and the benefits of treatment for herself.

Triclabendazole Dose in Kidney Disease:

• The manufacturer's instructions do not include any adjustments in dosage for people with kidney problems because there haven't been any studies done on this.

Triclabendazole Dose in Liver disease:

• The manufacturer's instructions do not include any adjustments in dosage for individuals with liver problems because there haven't been any studies conducted on this.

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

Contraindications to Triclabendazole:

• If someone is allergic to triclabendazole, other benzimidazole medications, or any ingredient in the formulation, they should not take this medication.
• Allergic reactions could be severe and may include symptoms like rash, itching, swelling, dizziness, or difficulty breathing.

Warnings and precautions

Hepatic toxicities:

• Some patients who take triclabendazole may experience temporary rises in liver enzymes and total bilirubin levels, indicating potential liver toxicity.
• If any signs or symptoms of liver problems, such as jaundice (yellowing of the skin or eyes), abdominal pain, or unusual tiredness, occur, patients should seek medical attention promptly.

Prolongation of QTc:

• Triclabendazole can cause a temporary lengthening of a heart's electrical cycle known as QTc interval, as seen in animal studies.
• For patients with a history of QTc prolongation or those taking medications that also prolong QTc, it's important to monitor their heart's electrical activity using an electrocardiogram (ECG).
• This helps doctors keep a close watch on their heart health and ensure safe use of triclabendazole alongside other drugs that might also affect the QTc interval.

Monitoring parameters:

Monitoring Heart Health with ECG

• Who Should be Monitored: Patients with a history of known or suspected QT prolongation or those taking medications that also lengthen QT interval (QTc-prolonging drugs).
• What to Do: Regularly monitor the heart's electrical activity using an electrocardiogram (ECG). This helps doctors keep track of any changes in the heart's rhythm and ensure the safe use of triclabendazole alongside other drugs that might affect the QT interval.

How to administer Triclabendazole?

How to Take Triclabendazole Orally

• Administer with Food: Take triclabendazole with food to help with absorption and reduce the risk of stomach upset.
• Tablet Options:
  • Swallow tablets whole.
  • Divide tablets in half and take with water.
  • Crush tablets and mix with applesauce for easier swallowing.
• Stability with Applesauce:
  • If crushed and mixed with applesauce, the tablet remains stable for up to 4 hours, making it convenient for administration.

Mechanism of action of Triclabendazole:

• Triclabendazole is a type of medication that fights against parasites called Fasciola species, which include liver flukes.
• Research done in test tubes (in vitro) shows that triclabendazole and its active forms are absorbed through the outer layer of both young and adult worms.
• This absorption leads to several effects, such as reducing the worm's ability to maintain its normal electrical balance (resting membrane potential), slowing down its movement, and causing damage to its surface and internal structure.
• This damage includes stopping the production of sperm cells (spermatogenesis) and egg cells (vitelline cells).

Absorption and Distribution:

• Increased Absorption with Food: Taking triclabendazole with food can boost its absorption into the body.
• Volume of Distribution (V): Around 1 liter per kilogram of body weight, indicating how widely the drug is distributed throughout the body.
• Protein Binding: Triclabendazole and its metabolites are highly bound to proteins in human plasma, with percentages ranging from around 96.7% to 98.8%.

Metabolism and Elimination:

• Metabolism: Triclabendazole is mainly broken down by the enzyme CYP1A2 (about 64%), forming its active sulfoxide metabolite. Other enzymes like CYP2C9, CYP2C19, CYP2D6, CYP3A, and FMO also play a role in its metabolism. The sulfoxide metabolite is further metabolized primarily by CYP2C9 to the active sulfone metabolite.
• Elimination Half-life: The time it takes for half of the drug to be eliminated from the body is about 8 hours for triclabendazole, 14 hours for its sulfoxide metabolite, and 11 hours for its sulfone metabolite.

Time to Peak:

• Time to Peak Concentration (T): It takes approximately 3.0 hours (with a small variation) for triclabendazole to reach its highest concentration in the body after administration.

International Brand Names of Triclabendazole:

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

Triclabendazole Brands Names in Pakistan:

No Brands Available in Pakistan.