Antussan: Full Drug Profile
Antussan - General Information
The d-isomer of the codeine analog of levorphanol. Antussan shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (receptors, N-methyl-D-aspartate) 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.
Pharmacology of Antussan
Antussan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Antussan 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.
Additional information about Antussan
- Antussan Indication
For treatment and relief of dry cough.
- Mechanism Of Action
- Antussan 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. Antussan 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.
- Drug Interactions
- Dihydroquinidine barbiturate Quinidine increases the toxicity of dextromethorphan
- Food Interactions
- Take without regard to meals.
- Generic Name
- Dextromethorphan
- Synonyms
- D-Methorphan; D-Methorphan Hydrobromide; Delta-Methorphan; Dextromethorfan [Czech]; Destrometerfano [Dcit]; Demorphan; Demorphan Hydrobromide; Demorphine; Dextromethorphan Bromhydrate; Dextromethorphan Bromide; Dextrometorfano [Inn-Spanish]; Dextrometorphan; Dextromorphan; Dexyromethorphan; L-Methorphan; Levomethorphan; Levomethorphan [Ban:Dcf:Inn]; Levomethorphane [Inn-French]; Levomethorphanum [Inn-Latin]; Levometorfano [Inn-Spanish]
- Drug Category
- Analgesics, Opioid; Antitussive Agents; Excitatory Amino Acid Antagonists
- Drug Type
- Small Molecule; Approved
- Other Brand Names containing Dextromethorphan
- Antussan; 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; Calmylin;
- Absorption
- Rapidly absorbed from the gastrointestinal tract.
- Biotransformation
- 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.
- Half Life
- 3-6 hours
- Dosage Forms of Antussan
- Lozenge Oral
- Chemical Formula
- C18H25NO
- Dextromethorphan on Wikipedia
- https://en.wikipedia.org/wiki/Dextromethorphan
- Organisms Affected
- Humans and other mammals
