Brands, Medical Use, Clinical Data
- Analgesics, Opioid
- Antitussive Agents
- Excitatory Amino Acid Antagonists
Brands / Synonyms
Antussan; Atuss DS Suspension; Balminil DM; Balminil DM Children; Benylin Adult Formula Cough Suppressant; Benylin DM; Benylin DM 12 Hour; Benylin DM for Children; Benylin DM for Children 12 Hour; Benylin Pediatric Cough Suppressant; Bromhist; Calmylin #1; Canfodion; Chlorphen MAL DEX HBR Pseudoeph; Cosylan; Cough-X; Creo-Terpin; D-Methorphan; D-Methorphan Hydrobromide; Delsym; Delsym Cough Formula; Delta-Methorphan; Demorphan; Demorphan Hydrobromide; Demorphine; Destrometerfano [Dcit]; Dextromethorfan; Dextromethorfan [Czech]; Dextromethorphan Bromhydrate; Dextromethorphan Bromide; Dextromethorphan [Ban:Inn]; Dextrometorfano [Inn-Spanish]; Dextrometorphan; Dextromorphan; Dexyromethorphan; Diabe-Tuss DM Syrup; Dormetan; Dormethan; Guaifenesin-DM NR Liquid; Hihustan M.; Hold DM; Koffex DM; L-Methorphan; Levomethorphan; Levomethorphan [Ban:Dcf:Inn]; Levomethorphane [Inn-French]; Levomethorphanum [Inn-Latin]; Levometorfano [Inn-Spanish]; Medicon; Methorate Hydrobromide; Methorphan; Metrorat; Myphetane DX; Novahistex DM; Novahistine DM; Pertussin CS Children's Strength; Pertussin DM Extra Strength; Promethazine and Dextromethorphan; Promethazine DM; Racemethorphan [as D-Form]; Robitussin Maximum Strength Cough Suppressant; Robitussin Pediatric; Robitussin Pediatric Cough Suppressant; Romilar; Sucrets 4 Hour Cough Suppressant; Triaminic DM Long Lasting for Children; Trocal; Tusilan; Tussade; Vicks 44 Cough Relief
For treatment and relief of dry cough.
Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Dextromethorphan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist and acts as a non-competitive channel blocker. It is one of the widely used antitussives, and is also used to study the involvement of glutamate receptors in neurotoxicity.
Mechanism of Action
Dextromethorphan is an opioid-like drug that binds to and acts as antagonist to the NMDA glutamatergic receptor, it is an agonist to the opioid sigma 1 and sigma 2 receptors, it is also an alpha3/beta4 nicotinic receptor antagonist and targets the serotonin reuptake pump. Dextromethorphan is rapidly absorbed from the gastrointestinal tract, where it enters the bloodstream and crosses the blood-brain barrier. The first-pass through the hepatic portal vein results in some of the drug being metabolized into an active metabolite of dextromethorphan, dextrorphan, the 3-hydroxy derivative of dextromethorphan.
Rapidly absorbed from the gastrointestinal tract.
Biotrnasformation / Drug Metabolism
Hepatic. Rapidly and extensively metabolized to dextrorphan (active metabolite). One well known metabolic catalyst involved is a specific cytochrome P450 enzyme known as 2D6, or CYP2D6.