Cyproheptadine

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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.^[1]

[edit] Uses

Cyproheptadine is used in the treatment of allergies (specifically hay fever)^[2] and is also used to stimulate appetite in underweight people (e.g. anorexia nervosa).

Cyproheptadine is used in serotonin syndrome, a complex of symptoms associated with selective serotonin reuptake inhibitors, especially when taken in excess dose and in the disease carcinoid in which serotonin is overproduced by tumor cells.^[3][4]

Cyproheptadine can also be used as a preventative measure against migraine in children and adolescents.^{[5][6][7][8][9]}

[edit] Side effects

While not specifically used as a sedative, cyproheptadine causes sedation, likely due to its anti-histamine effects.^{[citation needed]}

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)^{[citation needed]}

Cyproheptadine can also cause over-sleeping (10 Hours) in children and adolescents.^{[citation needed]}

[edit] Research

Cyproheptadine has been shown to improve quality of sleep in sleep-deprived rats.^[10]

[edit] References