Guang Di
Guang Di Uses, Dosage, Side Effects, Food Interaction and all others data.
Guang Di 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.
Guang Di appears to be well tolerated with the most frequently reported adverse effect being headache. Extrapyramidal side effects are rare upon using tropisetron.
Trade Name | Guang Di |
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 | China |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Guang Di 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.
Guang Di is also used to associated treatment for these conditions: Chemotherapy-Induced Nausea and Vomiting (CINV)
How Guang Di works
Guang Di 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
You find simplified version here Guang Di