Cyproheptadine

Cyproheptadine
Cyproheptadine
Systematic (IUPAC) name
4-(5H-dibenzo [a,d]cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride
Clinical data
AHFS/Drugs.com monograph
MedlinePlus a682541
Pregnancy cat. B(US)
Legal status P (UK)
Routes Oral only
Pharmacokinetic data
Protein binding 96 to 99%
Metabolism Hepatic and renal
Half-life 1 to 4 hours
Excretion Fecal and renal
Identifiers
CAS number 129-03-3 YesY
ATC code R06AX02
PubChem CID 2913
IUPHAR ligand 277
DrugBank APRD00033
ChemSpider 2810 YesY
UNII 2YHB6175DO YesY
KEGG D07765 YesY
ChEBI CHEBI:4046 YesY
ChEMBL CHEMBL516 YesY
Chemical data
Formula C21H21N 
Mol. mass 287.398 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Cyproheptadine (trade name Periactin) pronounced /ˌsaɪprɵˈhɛptədiːn/; usually as cyproheptadine hydrochloride is an antihistaminic/anticholinergic and antiserotonergic agent. It also acts as a 5-HT2 receptor antagonist as well as blocking calcium channels.[1]

Contents

Uses

Cyproheptadine is used to treat allergic reactions (specifically hay fever).[2]

Cyproheptadine has shown effectiveness in the treatment of nightmares including nightmares related to post traumatic stress disorder.[3][4]

Cyproheptadine has been used in the management of moderate to severe cases of serotonin syndrome (a complex of symptoms associated with the use of serotonergic drugs, such as selective serotonin reuptake inhibitors and monoamine oxidase inhibitors),[5][6][7] and in the disease carcinoid in which serotonin is overproduced by tumor cells.[8][9]

Cyproheptadine can also be used as a preventive measure against migraine in children and adolescents.[10][11][12][13][14]

Cyproheptadine can relieve SSRI-induced sexual dysfunction[15][16] and drug-induced hyperhydrosis (excessive sweating).[17]

Cyproheptadine is also used in the treatment of cyclical vomiting syndrome[18] and to stimulate the appetite.[19]

Adverse effects

While not specifically used as a sedative, cyproheptadine causes drowsiness,[20] as is common with first-generation antihistamines.

Research has shown a suppression of growth hormone with doses of 8–12 mg per day taken for 5 days.[21]

Other common side effects include:[22]

  • Dizziness
  • Blurred vision
  • Constipation
  • Dry mouth, throat, or nose
  • Excitability
  • Nausea
  • Nervousness
  • Restlessness or akathisia

Research

Cyproheptadine has been shown to improve quality of sleep in sleep-deprived rats.[23]

Cyproheptadine interacts with several other medications such as MAOIs (monoamine oxidase inhibitors) and potassium salts and can cause adverse reactions. Anti-cholinergic medications such as Cyproheptadine, when used in conjunction with oral potassium salts, can cause slowing of GI transit and increases the local exposure to high potassium concentrations. High potassium concentrations may lead to GI tract ulceration or stenosis.

Veterinary use

Cyproheptadine is used in cats as an appetite stimulant and as an adjunct in the treatment of asthma.[24][25] Possible adverse effects include excitement and aggressive behavior.[24]

The elimination half-life of cyproheptadine in cats is 12 hours.[25]. Cyproheptadine has been used successful in treatment of Pituitary Pars Intermedia Dysfunction (PPID) in horses. [26]

References

Periactin (cyproheptadine) 4 mg tablets (AU)
  1. ^ Lowe DA, Matthews EK, Richardson BP (November 1981). "The calcium antagonistic effects of cyproheptadine on contraction, membrane electrical events and calcium influx in the guinea-pig taenia coli". British Journal of Pharmacology 74 (3): 651–63. PMC 2071752. PMID 6271323. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2071752. 
  2. ^ MedlinePlus Drug Information: Cyproheptadine
  3. ^ Rijnders, R. J.P.; Laman, DM; Van Diujn, H (2000). "Cyproheptadine for Posttraumatic Nightmares". American Journal of Psychiatry 157 (9): 1524-a. doi:10.1176/appi.ajp.157.9.1524-a. PMID 10964879. http://ajp.psychiatryonline.org/cgi/content/full/157/9/1524-a. 
  4. ^ Gupta, S; Popli, A; Bathurst, E; Hennig, L; Droney, T; Keller, P (May 1998). "Efficacy of cyproheptadine for nightmares associated with posttraumatic stress disorder.". Comprehensive psychiatry 39 (3): 160–4. doi:10.1016/S0010-440X(98)90076-1. ISSN 0010-440X. PMID 9606583. 
  5. ^ Mills KC (October 1995). "Serotonin syndrome". American Family Physician 52 (5): 1475–82. PMID 7572570. 
  6. ^ Gillman PK (1999). "The serotonin syndrome and its treatment". Journal of Psychopharmacology (Oxford, England) 13 (1): 100–9. doi:10.1177/026988119901300111. PMID 10221364. 
  7. ^ Hall M, Buckley N (2003). "Serotonin syndrome". Australian Prescriber 26 (3): 62–3. http://www.australianprescriber.com/magazine/26/3/62/3. 
  8. ^ Berry EM, Maunder C, Wilson M (January 1974). "Carcinoid myopathy and treatment with cyproheptadine (Periactin)". Gut 15 (1): 34–8. doi:10.1136/gut.15.1.34. PMC 1412931. PMID 4274414. http://gut.bmj.com/cgi/pmidlookup?view=long&pmid=4274414. 
  9. ^ Moertel, Charles G.; Kvols, LK; Rubin, J (1991). "A study of cyproheptadine in the treatment of metastatic carcinoid tumor and the malignant carcinoid syndrome". Cancer 67 (1): 33–6. doi:10.1002/1097-0142(19910101)67:1<33::AID-CNCR2820670107>3.0.CO;2-E. PMID 1985720. http://www3.interscience.wiley.com/journal/112674381/abstract. 
  10. ^ Wendy G Mitchell et al. (2006). "Childhood Migraine Variants". http://www.emedicine.com/neuro/TOPIC494.HTM. 
  11. ^ UVA Neurogram: Treatment of Pediatric Migraine
  12. ^ Netdoctor: Periactin
  13. ^ Migraines in Children and Adolescents
  14. ^ Klimek A (1979). "Cyproheptadine (Peritol) in the treatment of migraine and related headache". Ther Hung 27 (2): 93–4. PMID 494146. 
  15. ^ Keller Ashton A, Hamer R, Rosen RC (1997). "Serotonin reuptake inhibitor-induced sexual dysfunction and its treatment: a large-scale retrospective study of 596 psychiatric outpatients". Journal of Sex & Marital Therapy 23 (3): 165–75. doi:10.1080/00926239708403922. PMID 9292832. 
  16. ^ McCormick S, Olin J, Brotman AW (September 1990). "Reversal of fluoxetine-induced anorgasmia by cyproheptadine in two patients". Journal of Clinical Psychiatry 51 (9): 383–4. PMID 2211550. 
  17. ^ Ashton AK, Weinstein WL (May 2002). "Cyproheptadine for drug-induced sweating". American Journal of Psychiatry 159 (5): 874–5. doi:10.1176/appi.ajp.159.5.874-a. PMID 11986151. http://ajp.psychiatryonline.org/cgi/pmidlookup?view=long&pmid=11986151. 
  18. ^ Andersen JM, Sugerman KS, Lockhart JR, Weinberg WA (December 1997). "Effective Prophylactic Therapy for Cyclic Vomiting Syndrome in Children Using Amitriptyline or Cyproheptadine". PEDIATRICS 100 (6): 977–981. PMID 9374568. http://pediatrics.aappublications.org/cgi/content/abstract/100/6/977. 
  19. ^ Long-term trial of cyproheptadine as an appetite stimulant in cystic fibrosis | Wiley Online Library
  20. ^ Lexi-Comp (August 2008). "Cyproheptadine". The Merck Manual Professional. http://www.merck.com/mmpe/lexicomp/cyproheptadine.html.  Retrieved on October 26, 2008.
  21. ^ Rosskamp RH, Haverkamp F, von Kalckreuth G (May 1990). "The effect of cyproheptadine on plasma growth hormone (GH) and on somatostatin response to GH-releasing hormone in man". Horm. Metab. Res. 22 (5): 295–7. doi:10.1055/s-2007-1004905. PMID 1971804. 
  22. ^ Cyproheptadine - Drugs.com
  23. ^ Tokunaga S; Takeda Y, Shinomiya K, Hirase M, Kamei C. (February 2007). "Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats." (pdf). J Pharmacol Sci. 103 (2): 201–6. doi:10.1254/jphs.FP0061173. PMID 17287588. http://www.jstage.jst.go.jp/article/jphs/103/2/201/_pdf. 
  24. ^ a b Dowling PM (February 8, 2005). "Drugs Affecting Appetite". In Kahn CM, Line S, Aiello SE (eds.). The Merck Veterinary Manual (9th ed.). John Wiley & Sons. ISBN 0-911910-50-6. http://www.merckvetmanual.com/mvm/index.jsp?cfile=htm/bc/190302.htm.  Retrieved on October 26, 2008.
  25. ^ a b Dowling PM (February 8, 2005). "Systemic Therapy of Airway Disease: Cyproheptadine". In Kahn CM, Line S, Aiello SE (eds.). The Merck Veterinary Manual (9th ed.). John Wiley & Sons. ISBN 0-911910-50-6. http://www.merckvetmanual.com/mvm/index.jsp?cfile=htm/bc/190907.htm.  Retrieved on October 26, 2008.
  26. ^ Merck Vet Manual. "Hirsutism Associated with Adenomas of the Pars Intermedia". http://www.merckvetmanual.com/mvm/index.jsp?cfile=htm/bc/40504.htm. Retrieved April 24, 2011. 
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Look at other dictionaries:

  • cyproheptadine — cy·pro·hep·ta·dine .sī prō hep tə .dēn n a drug C21H21N that acts antagonistically to histamine and serotonin and is used esp. in the treatment of asthma * * * n. a potent antihistamine used to treat allergies and itching skin conditions; it also …   Medical dictionary

  • cyproheptadine — n. a potent antihistamine used to treat allergies, such as hay fever and urticaria; it also inhibits the effects of serotonin and is used to prevent migraine attacks. Cyproheptadine is administered by mouth; drowsiness is a common side effect.… …   The new mediacal dictionary

  • cyproheptadine — A drug that is used to treat asthma, allergies, and colds, and to relieve itching caused by certain skin disorders. It has also been used to stimulate appetite and weight gain, and is being studied in the treatment of weight loss caused by cancer …   English dictionary of cancer terms

  • cyproheptadine — noun an antihistamine (trade name Periactin) used to treat some allergic reactions • Syn: ↑Periactin • Usage Domain: ↑trade name (for: ↑Periactin) • Hypernyms: ↑antihistamine * * * …   Useful english dictionary

  • cyproheptadine — noun Etymology: cyclic + propyl + hepta + piperidine Date: 1971 a histamine and serotonin antagonist C21H21N used especially in the form of its hydrochloride to treat allergy symptoms and hives …   New Collegiate Dictionary

  • cyproheptadine — /suy proh hep teuh deen /, n. Pharm. a phenothiazine analogue, C21H21N, with antihistaminic action, used in the symptomatic treatment of hay fever and itching. [1970 75; CY(CLO ) + PRO(PYL) + HEPTA + (PIPERI)DINE] * * * …   Universalium

  • cyproheptadine — noun An antihistaminic, anticholinergic and antiserotonergic agent …   Wiktionary

  • cyproheptadine — cy·pro·hep·ta·dine …   English syllables

  • cyproheptadine hydrochloride — A potent antagonist of histamine and serotonin, with H1 antihistaminic and antipruritic actions. * * * cy·pro·hep·ta·dine hy·dro·chlo·ride (si″pro hepґtə dēn) [USP] an antihistamine (H1 receptor antagonist) with sedative,… …   Medical dictionary

  • Benzocycloheptenes — Cyproheptadine …   Wikipedia

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