Tropisetron hydrochloride

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

Tropisetron hydrochloride 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.

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

Tropisetron hydrochloride
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Tropisetron hydrochloride
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	Russia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Tropisetron hydrochloride 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.

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

How Tropisetron hydrochloride works

Tropisetron hydrochloride 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.