Cyproheptadine hydrochloride sesquihydrate

Chemical properties

White or slightly yellow, crystalline powder.

The Uses of Cyproheptadine hydrochloride sesquihydrate

Structural studies of an antihistimine

The Uses of Cyproheptadine hydrochloride sesquihydrate

Cyproheptadine hydrochloride sesquihydrate has been used in:

• testing anti-inflammatory activity in serotonin receptor (5-HT) induced inflammation
• the inhibition of 5-HT in in vivo and in vitro bioassays in crabs
• the inhibition of 5-HT in embryo physiological experiments

inhibition of calcitonin gene related peptide (CGRP)

The Uses of Cyproheptadine hydrochloride sesquihydrate

H1-antihistamine, antipruritic

The Uses of Cyproheptadine hydrochloride sesquihydrate

Cyproheptadine is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties. Cyproheptadine is a 5-HT2/5-HT1C serotonin receptor antagonist; H 1 histamine receptor antagonist; antipruritic.

Definition

ChEBI: The sesquihydrate of cyproheptadine hydrochloride. Note that the drug named cyproheptadine hydrochloride generally refers to cyproheptadine hydrochloride sesquihydrate. A sedating antihistamine with antimuscarinic and calcium-channel blocking actions, it i used for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.

brand name

Periactin (Merck).

General Description

Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine. It induced preventive effect against the development of pergolide-induced valvulopathy in a rat model.

Biochem/physiol Actions

Cyproheptadine hydrochloride sesquihydrate is a serotonin receptor (5-HT2/5-HT1C) antagonist, H1 histamine receptor antagonist and an antipruritic. The inhibition of 5-HT by cyproheptadine improves cognitive function in schizophrenia disorder. Cyproheptadine is effective for treating functional gastrointestinal disorders (FGIDs). Food and Drug Administration (FDA) approved cyproheptadine, has antidepressant and antiplatelet functionality. It may be effective in treating thromboembolic disorders. Cyproheptadine inhibits lysine methyltransferase 7/9 (Set7/9) leading to a decrease in estrogen receptor (ERα) expression and growth arrest in breast cancer cells.

Veterinary Drugs and Treatments

Cyproheptadine may be useful in cats as an appetite stimulant. It potentially may be of benefit in the treatment of feline asthma or pruritus in cats, but clinical experience is marginal for this indication.
Cyproheptadine is an antihistamine but its efficacy is questionable for this indication in dogs. The drug may be useful as adjunctive therapy for Cushing’s syndrome probably as result of its antiserotonin activity, however one study demonstrated efficacy in less than 10% of dogs treated for pituitary dependent hyperadrenocorticism.
Cyproheptadine may be useful as adjunctive treatment in dogs or cats with serotonin syndrome.
In horses, cyproheptadine has been used for treating photic head shaking and pars intermedia dysfunction (Equine Cushing’s Disease).