Drug intelligence / Profile preview

Alprazolam + Tropisetron

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of alprazolam and tropisetron is used in clinical settings, particularly for managing chemotherapy-induced nausea and vomiting (CINV). Alprazolam, a benzodiazepine, acts as a positive allosteric modulator of GABA~A~ receptors, producing dose-dependent CNS depression and a calming effect. It is used for anxiety disorders, panic disorder, and off-label for CINV. Tropisetron, a 5HT-3 receptor antagonist, selectively blocks serotonin at 5HT3 receptors to suppress chemotherapy and radiotherapy-induced nausea and vomiting. It is generally well-tolerated, with headache being the most common side effect. Studies indicate that the addition of alprazolam to 5HT-3 receptor antagonists like tropisetron can significantly improve antiemetic efficacy in cancer patients receiving chemotherapy. The combination carries an increased risk of CNS depression due to potential synergistic effects on the central nervous system.

02

Targets

GABRR (GABA-A receptor subunit rho)HTR3A (5-hydroxytryptamine receptor 3A)

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