Drug intelligence / Profile preview

ondansetron + bupivacaine

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Perineural, Intravenous, Intrathecal
01

Overview

Ondansetron + bupivacaine is a combination of two pharmaceutical agents used primarily in anesthesia and pain management settings. Ondansetron is a selective serotonin 5-HT3 receptor antagonist, commonly used to prevent nausea and vomiting associated with chemotherapy, radiotherapy, or surgery. Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels on neuronal membranes, inhibiting nerve impulse transmission and providing local or regional anesthesia. When combined, these drugs are investigated for their potential synergistic effects in perioperative care. Some studies suggest that adding ondansetron to bupivacaine may hasten the onset of sensory and motor block and improve postoperative analgesia; however, other research indicates that systemic ondansetron does not significantly alter the intensity or duration of sensory/motor block from spinal anesthesia with bupivacaine[1][3][4]. The combination has been explored via perineural administration (directly around nerves) as well as intravenous routes. The mechanism involves: - Ondansetron blocking serotonin 5-HT3 receptors (antiemetic effect; possible modulation of pain pathways). - Bupivacaine blocking voltage-gated sodium channels (local anesthetic effect). This combination does not have a unique brand name or widespread regulatory approval as a fixed-dose product but may be compounded for specific clinical research protocols.

02

Targets

NaV alpha (Voltage-gated sodium channel alpha subunit family)HTR3A (5-hydroxytryptamine receptor 3A)

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