Cyproheptadine hydrochloride sesquihydrate Chemical Properties

Melting point:

165 °C (dec.)(lit.)

storage temp. 

Inert atmosphere,Room Temperature

solubility 

ethanol: soluble

form 

solid

color 

white to slightly yellow

λmax

285nm(0.05mol/L H2SO4)(lit.)

Merck 

14,2773

CAS DataBase Reference

41354-29-4(CAS DataBase Reference)

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-36/37/38

Safety Statements 

26-36

RIDADR 

UN 2811 6.1/PG 3

WGK Germany 

3

RTECS 

TM7050000

HazardClass 

6.1

PackingGroup 

III

HS Code 

29333990

Toxicity

LD50 orally in mice: 74.2 mg/kg (Loux)

MSDS

• Language:English Provider:SigmaAldrich

Cyproheptadine hydrochloride sesquihydrate Usage And Synthesis

Antihistamines

Cyproheptadine hydrochloride is a kind of pipecolic antihistamines,it can compete with histamine released from the organization for H1 receptor on effector cells , thereby it can prevent the onset of an allergic reaction, and release histamine-induced spasm and congestion effects, this product has a strong H1 receptor antagonism, its anti-histamine effect is stronger than chlorpheniramine, promethazine . There are mild to moderate anti-serotonin effects and anticholinergic effects. In addition, there is a stimulate appetite effect, and weight gains after a certain time.
Clinically cyproheptadine hydrochloride is mainly used for acute and chronic urticaria (especially it has a good effect on cold urticaria ), papular urticaria, angioedema, atopic eczema, contact dermatitis, food allergy, drug allergy, allergic rhinitis, hay fever, allergic conjunctivitis, allergic to insect stings and migraine. It has some therapeutic effect on bronchial asthma . It is acceptable for the adjuvant treatment of Cushing's syndrome, acromegaly. In addition,as an appetite enhancer,it is used for neuropathic fear of food. There are reports about acanthosis nigricans treatment, prevention of necrotizing pyoderma.
【Dosage 】oral often release dosage : (1) allergic diseases: adult, once 2~4mg, one day 2 or 3 times. (2) Cushing's syndrome, applicable to the treatment of cases of bilateral adrenal hyperplasia,it can inhibit the hypothalamic release of corticotropin releasing hormone (CRH) and inhibit the secretion of pituitary adrenocorticotropic hormone (ACTH), thereby lowering plasma ACTH and cortisol levels; adults start one day 8mg,which can be gradually increased to one day24mg; the usual dose is one day 12~24mg, divided doses,it needs long-term use; in the case of cortical function inadequate after total resection or subtotal bilateral adrenal, on one hand ,supple corticosteroids, on the other hand,take cyproheptadine,which can reduce the chance of occurrence of pituitary tumors.
The above information is edited by the chemicalbook of Tian Ye.

Uses

Anticoagulant, anti-allergic drugs. It can be used for urticaria, eczema, and allergic contact dermatitis, skin itching and other allergic reactions. It can also be used for Cushing's diseases and acromegaly.

Chemical Properties

White or slightly yellow, crystalline powder.

Uses

H1-antihistamine, antipruritic

Uses

Structural studies of an antihistimine

Uses

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)

Uses

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).

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