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Cyproheptadine
Systematic (IUPAC) name
4-(5 H-dibenzo [a,d]cyclohepten-5-ylidene)- 1 -methylpiperidine hydrochloride
Identifiers
CAS number 129-03-3
ATC code R06AX02
PubChem 2913
DrugBank APRD00033
ChemSpider 2810
Chemical data
Formula C 21H21N 
Mol. mass 287.398 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 96 to 99%
Metabolism Hepatic and renal
Half life 1 to 4 hours
Excretion Fecal and renal
Therapeutic considerations
Pregnancy cat. B(US)
Legal status P (UK)
Routes Oral only
 Yes check.svgY(what is this?)  (verify)

Cyproheptadine (pronounced /ˌsaɪprɵˈhɛptədiːn/; usually as cyproheptadine hydrochloride, trade name Periactin) is an antihistaminic/anticholinergic and antiserotonergic agent. It acts as a 5-HT2 receptor antagonist and also blocks 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 or stimulants),[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 preventative 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 (excess sweating).[17]

Cyproheptadine can stimulate one's appetite.

Adverse effects

While not specifically used as a sedative, cyproheptadine causes drowsiness,[18] as is common with first-generation antihistamines.

Research has shown a supression of growth hormone with doses of 8-12 mg per day taken for 5 days.[19]

Other common side effects include:[20]

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

Research

Cyproheptadine has been shown to improve quality of sleep in sleep-deprived rats...[21]

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

Periactin 4 mg tablets (AU)

Cyproheptadine is used in cats as an appetite stimulant and as an adjunct in the treatment of asthma.[22][23] Possible adverse effects include excitement and aggressive behavior.[22]

The elimination half-life of cyproheptadine in cats is 12 hours.[23]

References

  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. PMID 6271323.  
  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. 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. PMID 4274414. PMC 1412931. 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. 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. 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. ^ Lexi-Comp (August 2008). "Cyproheptadine". The Merck Manual Professional. http://www.merck.com/mmpe/lexicomp/cyproheptadine.html.   Retrieved on October 26, 2008.
  19. ^ 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.  
  20. ^ Cyproheptadine - Drugs.com
  21. ^ 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.  
  22. ^ 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.
  23. ^ 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.







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