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.
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.
White or slightly yellow, crystalline powder.
Structural studies of an antihistimine
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)
H1-antihistamine, antipruritic
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.
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.
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.
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).
