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Cyproheptadine


Cyproheptadine
Systematic (IUPAC) name
4-(5 H-dibenzo [a,d]cyclohepten-5-ylidene)- 1 -methylpiperidine hydrochloride
Identifiers
CAS number	129-03-3
ATC code	R06AX02
PubChem	2913
DrugBank	APRD00033
Chemical data
Formula	C₂₁H₂₁N
Mol. mass	287.398 g/mol
Pharmacokinetic data
Bioavailability	?
Protein binding	96 to 99%
Metabolism	Hepatic and renal
Half life	1 to 4 hours
Excretion	Fecal and renal
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status	P(UK)
Routes	Oral only

Cyproheptadine (usually as cyproheptadine hydrochloride, trade name Periactin) is an antihistaminic and antiserotonergic agent. It acts as a 5-HT₂ receptor antagonist and also blocks calcium channels.

Additional recommended knowledge

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Uses

Cyproheptadine is used in the treatment of allergies (specifically Hay fever) and is also used to stimulate appetite in underweight people (e.g. anorexia nervosa).

Cyproheptadine may also be used to combat SSRI-induced sexual dysfunction, but is used cautiously in this manner because it may reverse the effects of the SSRI.

Cyproheptadine is also used for the treatment of Cushing's Syndrome, the treatment of serotonin reactions secondary to meperidine, and may be used, though rarely, as a prophylactic drug for migraine headaches.

Useful in the treatment of Serotonin Syndrome. Antagonise the action of histamine at H1 receptors, reducing histamine-related vasodilation and increased capillary permeability.

They also have anticholinergic activity, some have alpha-blocking activity and some have antiserotonin activity, eg cyproheptadine.

Useful alternative to benzodiazepine hypnotics in the treatment of insomnia. Cyproheptadine may be superior to benzodiazepines in the treatment of insomnia because cyproheptadine enhances sleep quality and quantity whereas benzodiazepines tend to decrease sleep quality.^[1]

Side effects

While not specifically used as a sedative, cyproheptadine causes sedation, likely due to its anti-histamine effects.

Digestive System: epigastric distress (dysphagia), loss of appetite, nausea, vomiting, (it is noted that these side effects are much more common in people with neuromuscular disorders)

References

This article needs additional citations for verification.
Please help improve this article by adding reliable references. Unsourced material may be challenged and removed. (December 2007)

^ Tokunaga S; Takeda Y, Shinomiya K, Hirase M, Kamei C. (Feb 2007). "Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats." (pdf). J Pharmacol Sci. 103 (2): 201-6. PMID 17287588.

v • d • e Antihistamines (primarily R06)
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Substituted alkylamines	Brompheniramine • Chlorphenamine • Dexbrompheniramine • Dexchlorpheniramine • Dimetindene • Pheniramine • Talastine
Substituted ethylenediamines	Chloropyramine • Histapyrrodine • Mepyramine • Methapyrilene • Tripelennamine (Pyribenzamine)
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Piperazine derivatives	Buclizine • Cetirizine • Chlorcyclizine • Cinnarizine • Cyclizine • Hydroxyzine • Levocetirizine • Meclizine • Niaprazine • Oxatomide
Others for systemic use	Antazoline • Azatadine • Bamipine • Cyproheptadine • Deptropine • Dimebon • Ebastine • Epinastine • Ketotifen • Mebhydrolin • Mizolastine • Phenindamine • Pimethixene • Pyrrobutamine • Rupatadine • Triprolidine • selective (Acrivastine • Astemizole • Azelastine • Desloratadine • Fexofenadine • Loratadine • Terfenadine)
For topical use	Bamipine • Chloropyramine • Chlorphenoxamine • Clemastine • Dimetindene • Diphenhydramine • Isothipendyl • Mepyramine • Promethazine • Thenalidine
Antiallergic agents excluding corticosteroids	Antazoline • Azelastine
Other antiallergics	Emedastine • Epinastine • Ketotifen • Olopatadine

Category: Antihistamines

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Cyproheptadine". A list of authors is available in Wikipedia.