Cyproheptadine

Structural formula
General
Non-proprietary name	Cyproheptadine
other names	4- (5 H -dibenzo [ a, d ] cyclohepten-5-ylidene) -1-methylpiperidine ( IUPAC )
Molecular formula	C 21 H 21 N
External identifiers / databases
EC number	204-928-9
ECHA InfoCard	100,004,482
PubChem	2913
DrugBank	DB00434
Wikidata	Q417884
Drug information
ATC code	R06 AX02
Drug class	Antiallergic
Mechanism of action	Antihistamine
properties
Molar mass	287.40 g · mol -1
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Cyproheptadine ( trade name : Peritol ^® ) is a drug that is used , among other things, to treat cold urticaria .

It was patented by Sharp and Dohme in 1961.

Clinical information

Application areas (indications)

The use of cyproheptadine is hardly of any importance. The effectiveness of the drug for various claimed fields of application is poorly documented. The only area of application for cyproheptadine that is legally approved in Germany is the treatment of cold urticaria when conventional antihistamines are not sufficiently effective. In the USA, cyproheptadine preparations are also approved as antiallergic agents for the treatment of seasonal allergic or vasomotor rhinitis , allergic conjunctivitis and allergic skin conditions, for ameliorating allergic reactions to blood or plasma and for treating dermographism . In veterinary medicine, cyproheptadine is used to stimulate appetite, but the active ingredient is not approved for animals.

Outside the approval, cyproheptadine is recommended for the treatment of serotonin syndrome , a clinical picture that is usually triggered by overdosing or interactions between serotoninergic drugs. However, the effectiveness of cyproheptadine in the treatment of post-traumatic stress disorders has not been proven. In the preventive treatment ( prophylaxis ) of migraines , cyproheptadine is the drug of the third choice. There is hardly any evidence of its effectiveness for this area of application either.

Pharmacological properties

Cyproheptadine is a tricyclic compound that has an antagonistic effect on histamine H ₁ receptors and on serotonin receptors and also has a weak anticholinergic effect. Experimentally, cyproheptadine also inhibits acid sphingomyelinase .

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ Lee EE, Maibach HI: Treatment of urticaria. An evidence-based evaluation of antihistamines . In: American Journal of Clinical Dermatology . 2, No. 1, 2001, pp. 27-32. PMID 11702618 .
↑ Cyproheptadine Official FDA information, side effects and uses. . Retrieved September 12, 2010.
^ Brown ™, Skop BP, Mareth TR: Pathophysiology and management of the serotonin syndrome . In: Ann Pharmacother . 30, No. 5, May 1996, pp. 527-533. PMID 8740336 .
↑ Bryant RA, Friednman M: Medication and non-medication treatments of post-traumatic stress disorder . In: Curr Opin Psychiatry . 14, 2001, pp. 119-123.
↑ Silberstein SD: Practice parameter: evidence-based guidelines for migraine headache (an evidence-based review): report of the Quality Standards Subcommittee of the American Academy of Neurology . In: Neurology . 55, No. 6, September 2000, pp. 754-62. PMID 10993991 .
↑ Kornhuber J, Tripal P, Reichel M, Terfloth L, Bleich S et al .: Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. . In: J. Med. Chem. . 51, 2008, pp. 219-237.

literature

Römpp Lexicon Chemistry. 10 ed. Thieme, Stuttgart a. New York 1996-1999. P. 858.
C.-J. Estler (Ed.): Pharmacology and Toxicology . 4th edition. Schattauer, Stuttgart 1995. pp. 98-99.

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[pmid11702618-2] Lee EE, Maibach HI: Treatment of urticaria. An evidence-based evaluation of antihistamines . In: American Journal of Clinical Dermatology . 2, No. 1, 2001, pp. 27-32. PMID 11702618 .

[3] Cyproheptadine Official FDA information, side effects and uses. . Retrieved September 12, 2010.

[pmid8740336-4] Brown ™, Skop BP, Mareth TR: Pathophysiology and management of the serotonin syndrome . In: Ann Pharmacother . 30, No. 5, May 1996, pp. 527-533. PMID 8740336 .

[5] Bryant RA, Friednman M: Medication and non-medication treatments of post-traumatic stress disorder . In: Curr Opin Psychiatry . 14, 2001, pp. 119-123.

[pmid10993991-6] Silberstein SD: Practice parameter: evidence-based guidelines for migraine headache (an evidence-based review): report of the Quality Standards Subcommittee of the American Academy of Neurology . In: Neurology . 55, No. 6, September 2000, pp. 754-62. PMID 10993991 .

[Kornhuber_et_al._(2008)-7] Kornhuber J, Tripal P, Reichel M, Terfloth L, Bleich S et al .: Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. . In: J. Med. Chem. . 51, 2008, pp. 219-237.