Drug intelligence / Profile preview

tramadol + ondansetron

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

Overview

Tramadol + ondansetron is a combination of two small molecule drugs, tramadol and ondansetron, sometimes co-administered in clinical settings. Tramadol is an analgesic with dual mechanisms of action as a μ-opioid receptor agonist and inhibitor of serotonin and norepinephrine reuptake, used for moderate to moderately severe pain. Ondansetron is a selective 5-HT3 (serotonin) receptor antagonist primarily used as an antiemetic to prevent nausea and vomiting. When administered together, there is evidence that ondansetron can reduce the analgesic efficacy of tramadol by antagonizing spinal 5-HT3 receptors involved in pain modulation. Additionally, this combination increases the risk for serotonin syndrome and cardiac arrhythmias such as QT prolongation; thus, their concurrent use should be approached with caution or avoided unless specifically indicated[1][4][5].

02

Targets

SERT (Sodium-dependent serotonin transporter)HTR3A (5-hydroxytryptamine receptor 3A)NET (Norepinephrine Transporter)MOR (Mu opioid receptor)

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