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QuickView for Cyproheptadine (compound)

Summary
General Info

PubChem

PubChem Compound 11954233

PubChem Compound 11954233

Name:	Cyproheptadine
PubChem Compound ID:	11954233
Description:	A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
Molecular formula:	C₄₂H₅₀Cl₂N₂O₃
Molecular weight:	701.763 g/mol
Synonyms:	Cyproheptadine hydrochloride; D02234; Periactin; Periactin (TN); Cyproheptadine hydrochloride (JP15/USP); 41354-29-4

DrugBank

Identification

Name:	Cyproheptadine
Name (isomeric):	DB00434
Drug Type:	small molecule
Description:	A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.
Brand:	Peritol, Eiproheptadine, Cyproheptadine Hcl, Periactin, Periactinol, Periactine, Cyproheptadiene, Cypoheptadine, Dibenzosuberonone/Cyproheptadine, Dronactin
Category:	Serotonin Antagonists, Antihistamine derivatives, Gastrointestinal Agents, Histamine H1 Antagonists, Antipruritics, Anti-Allergic Agents
CAS number:	129-03-3

Pharmacology

Indication:	For treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, cold urticaria, dermatographism, and as therapy for anaphylactic reactions adjunctive to epinephrine.
Pharmacology:	Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cy... show more » Cyproheptadine is a piperidine antihistamine. Unlike other antihistamines, this drug also antagonizes serotonin receptors. This action makes Cyproheptadine useful in conditions such as vascular headache and anorexia. Cyproheptadine does not prevent the release of histamine but rather competes with free histamine for binding at HA-receptor sites. Cyproheptadine competitively antagonizes the effects of histamine on HA-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. Most antihistamines possess significant anticholinergic properties, but Cyproheptadine exerts only weak anticholinergic actions. Blockade of central muscarinic receptors appears to account for Cyproheptadine's antiemetic effects, although the exact mechanism is unknown. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Cyproheptadine also has been used to counter vascular headaches, which many believe are caused by changes in serotonin activity, however it is unclear how Cyproheptadine exerts a beneficial effect on this condition. show less «
Mechanism of Action:	Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. An... show more » Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. show less «
Absorption:	Well absorbed after oral administration.
Protein binding:	96 to 99%
Biotransformation:	Hepatic (cytochrome P-450 system) and some renal.
Route of elimination:	After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered radioactivity was excreted in the urine.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid alcohol.

Take with food.

Drug interaction:

Triprolidine	Triprolidine and Cyproheptadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Donepezil	Possible antagonism of action
Trospium	Trospium and Cyproheptadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Metyrapone	This combination renders test invalid
Fluoxetine	Possible antagonism of action

Targets

Histamine H1 receptor

5-hydroxytryptamine 2A receptor

5-hydroxytryptamine 2C receptor

Muscarinic acetylcholine receptor M1

Muscarinic acetylcholine receptor M2

Muscarinic acetylcholine receptor M3