Drug intelligence / Profile preview

dextromethorphan

Development stage
Approved
Lead developer
Axsome Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Dextromethorphan is a widely used over-the-counter antitussive (cough suppressant) found in more than 120 cold and cough medications, either alone or in combination with other drugs. It is primarily indicated for the temporary relief of cough caused by the common cold, flu, or other conditions. Dextromethorphan acts on the central nervous system to suppress the cough reflex by decreasing activity in specific areas of the brain that trigger coughing. Mechanistically, it is a nonselective serotonin reuptake inhibitor, a sigma‑1 receptor agonist, and at higher doses acts as an NMDA receptor antagonist via its active metabolite dextrorphan. While structurally related to morphine derivatives (morphinan class), it does not have significant opioid activity at therapeutic doses. In 2022, a combination product containing dextromethorphan and bupropion was approved for major depressive disorder.

Brand names
RobitussinBabee CofBenylin DM PediatricBuckleys MixtureCreomulsionCreo-Terpin
Other names
dextromethorphan hydrobromideDXM
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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