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Antussan

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
Quinidine Quinidine increases the toxicity of dextromethorphan
Quinidine barbiturate Quinidine increases the toxicity of dextromethorphan
Fluoxetine Combination associated with possible serotoninergic syndrome
Isocarboxazid Possible severe adverse reaction
Memantine Increased risk of CNS adverse effects
Moclobemide Increased CNS toxicity
Paroxetine Combination associated with possible serotoninergic syndrome
Phenelzine Possible severe adverse reaction
Rasagiline Possible severe adverse reaction
Selegiline Combination associated with possible serotoninergic syndrome
Sibutramine Combination associated with possible serotoninergic syndrome
Terbinafine Terbinafine increases dextromethorphan levels
Tranylcypromine Possible severe adverse reaction
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.
Toxicity (Overdose): Not Available
Protein Binding: Not Available
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
Tablet Oral
Liquid Oral
Strip Oral
Suspension Oral
Capsule Oral
Syrup Oral
Chemical IUPAC Name: Not Available
Chemical Formula: C18H25NO
Dextromethorphan on Wikipedia: http://en.wikipedia.org/wiki/Dextromethorphan
Organisms Affected: Humans and other mammals