Hensetron

Hensetron Uses, Dosage, Side Effects, Food Interaction and all others data.

Hensetron is an indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.

Hensetron appears to be well tolerated with the most frequently reported adverse effect being headache. Extrapyramidal side effects are rare upon using tropisetron.

Trade Name Hensetron
Generic Tropisetron
Tropisetron Other Names Tropisetron
Type
Formula C17H20N2O2
Weight Average: 284.3529
Monoisotopic: 284.152477894
Protein binding

71% bound to plasma protein in a non-specific manner.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country Philippines
Last Updated: September 19, 2023 at 7:00 am
Hensetron
Hensetron

Uses

Hensetron is a 5HT-3 receptor antagonist used as an antiemetic in the treatment of chemotherapy-induced nausea and vomiting.

For the prevention of nausea and vomiting induced by cytotoxic therapy and postoperative.

Hensetron is also used to associated treatment for these conditions: Chemotherapy-Induced Nausea and Vomiting (CINV)

How Hensetron works

Hensetron competitively binds to and blocks the action of serotonin at 5HT3 receptors peripherally on vagus nerve terminals located in the gastrointestinal (GI) tract as well as centrally in the chemoreceptor trigger zone (CTZ) of the area postrema of the central nervous system (CNS). This results in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.

Toxicity

LD50: 265 mg/kg (Rat, oral).

Food Interaction

  • Avoid alcohol.

Volume of Distribution

400-600 L.

Elimination Route

The absorption of tropisetron from the gastrointestinal tract is rapid (mean half-life of about 20 minutes) and nearly complete (more than 95%). Due to first-pass metabolism in the liver, the absolute bioavailability of a 5 mg oral dose is 60%. The peak plasma concentration is attained within three hours.

Half Life

5.7 h.

Clearance

1800 ml/min.

Elimination Route

About 8% of tropisetron is excreted in the urine as unchanged drug, 70% as metabolites; 15% is excreted in the feces.

Innovators Monograph

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*** Taking medicines without doctor's advice can cause long-term problems.
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