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cyproheptadine

 
American Heritage Dictionary:

cy·pro·hep·ta·dine

Home > Library > Literature & Language > Dictionary
(sī'prō-hĕp'tə-dēn') pronunciation
n.
An antihistamine, C21H21N, used to relieve the symptoms of various allergic reactions, such as itching and skin rash.

[CY(CLIC) + PRO(PYL) + HEPTA- + (PIPERI)DINE.]


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Drug Info:

Cyproheptadine

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Home > Library > Health > Drug Info

Brand names: Periactin®

Chemical formula:



Cyproheptadine Hydrochloride Oral tablet

What is this medicine?

CYPROHEPTADINE (si proe HEP ta deen) is a antihistamine. This medicine is used to treat allergy symptoms. It is can help stop runny nose, watery eyes, and itchy rash.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• any chronic disease
• glaucoma
• prostate disease
• ulcers or other stomach problems
• an unusual or allergic reaction to cyproheptadine, other medicines foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take your doses at regular intervals. Do not take your medicine more often than directed.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for children as young as 2 years of age for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
• MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate

This medicine may also interact with the following medications:
• alcohol
• barbiturate medicines for inducing sleep or treating seizures
• medicines for depression, anxiety or psychotic disturbances
• medicines for movement abnormalities
• medicines for sleep
• medicines for stomach problems
• some medicines for cold or allergies

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Tell your doctor if your symptoms do not improve or if they get worse.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your eye doctor if the problem does not go away or is severe.

This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• agitation, nervousness, excitability, not able to sleep
• chest pain
• irregular, fast heartbeat
• pain or difficulty passing urine
• seizures
• unusual bleeding or bruising
• unusually weak or tired
• yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• constipation or diarrhea
• headache
• loss of appetite
• nausea, vomiting
• stomach upset
• weight gain

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

American Heritage Stedman's Medical Dictionary:

cy·pro·hept·a·dine

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Home > Library > Health > Medical Dictionary
(sī'prō-hĕp'tə-dēn)
n.

An antihistamine used to relieve the symptoms of various allergic reactions, such as itching and skin rash.

Saunders Veterinary Dictionary:

cyproheptadine

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Home > Library > Animal Life > Veterinary Dictionary

A histamine and serotonin antagonist used as an antipruritic and antihistaminic. It has also been used in the treatment of pituitary-dependent hyperadrenocorticism.

Wikipedia on Answers.com:

Cyproheptadine

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Home > Library > Miscellaneous > Wikipedia
Cyproheptadine
Systematic (IUPAC) name
4-(5H-dibenzo [a,d]cyclohepten-5-ylidene)-1-methylpiperidine hydrochloride
Clinical data
Trade names Periactin
AHFS/Drugs.com monograph
MedlinePlus a682541
Pregnancy cat. B(US)
Legal status P (UK)
Routes Oral
Pharmacokinetic data
Protein binding 96 to 99%
Metabolism Hepatic and renal
Half-life 8.6 hours[1]
Excretion Fecal and renal
Identifiers
CAS number 129-03-3 YesY 969-33-5 (hydrochloride)
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 (play /ˌsaɪprɵˈhɛptədiːn/), sold under the brand name Periactin, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.

Contents

Indications

Periactin (cyproheptadine) 4 mg tablets
  • Cyproheptadine is used to treat allergic reactions (specifically hay fever).[2]
  • Can also be used as a preventive measure against migraine in children and adolescents.[10][11][12][13][14]

Pharmacology

Cyproheptadine is known to be an antagonist (or inverse agonist depending on the site in question) of the following receptors, listed in order of potency from greatest to least (Ki):

It also has weak but likely negligible affinity for the following sites (Ki):

Additionally, cyproheptadine possesses calcium channel-blocking[30] and local anesthetic properties.[31]

Pharmacokinetics

Cyproheptadine is well-absorbed following oral ingestion, with peak plasma levels occurring after 1-3 hours.[32] Its half-life when taken orally is approximately 8 hours.[1]

Adverse effects

While not specifically used as a sedative, cyproheptadine causes drowsiness,[33] 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.[34]

Other common side effects include:[35]

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

Veterinary use

Cyproheptadine is used in cats as an appetite stimulant and as an adjunct in the treatment of asthma.[36][37] Possible adverse effects include excitement and aggressive behavior.[36]

The elimination half-life of cyproheptadine in cats is 12 hours.[37] Cyproheptadine has been used successful in treatment of Pituitary Pars Intermedia Dysfunction (PPID) in horses. [38]

References

  1. ^ a b Gunja N, Collins M, Graudins A (2004). "A comparison of the pharmacokinetics of oral and sublingual cyproheptadine". Journal of Toxicology. Clinical Toxicology 42 (1): 79–83. PMID 15083941. 
  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. doi:10.1542/peds.100.6.977. 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. ^ Moguilevsky N, Varsalona F, Noyer M, et al. (September 1994). "Stable expression of human H1-histamine-receptor cDNA in Chinese hamster ovary cells. Pharmacological characterisation of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene". European Journal of Biochemistry / FEBS 224 (2): 489–95. doi:10.1111/j.1432-1033.1994.00489.x. PMID 7925364. http://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0014-2956&date=1994&volume=224&issue=2&spage=489. 
  21. ^ a b Peroutka SJ (May 1988). "Antimigraine drug interactions with serotonin receptor subtypes in human brain". Annals of Neurology 23 (5): 500–4. doi:10.1002/ana.410230512. PMID 2898916. 
  22. ^ a b Bonhaus DW, Weinhardt KK, Taylor M, et al. (1997). "RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist". Neuropharmacology 36 (4–5): 621–9. doi:10.1016/S0028-3908(97)00049-X. PMID 9225287. 
  23. ^ Stanton T, Bolden-Watson C, Cusack B, Richelson E (June 1993). "Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics". Biochemical Pharmacology 45 (11): 2352–4. doi:10.1016/0006-2952(93)90211-E. PMID 8100134. 
  24. ^ a b c d e Toll L, Berzetei-Gurske IP, Polgar WE, et al. (March 1998). "Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications". NIDA Research Monograph 178: 440–66. PMID 9686407. 
  25. ^ a b F. S. Dukhovich (15 August 2005). Pharmacological aspects of molecular recognition. Nova Publishers. p. 117. ISBN 978-1-59454-676-1. http://books.google.com/books?id=9hvuXVPepMQC&pg=PA117. Retrieved 27 November 2011. 
  26. ^ Kohen R, Metcalf MA, Khan N, et al. (January 1996). "Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor". Journal of Neurochemistry 66 (1): 47–56. doi:10.1046/j.1471-4159.1996.66010047.x. PMID 8522988. http://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0022-3042&date=1996&volume=66&issue=1&spage=47. 
  27. ^ a b Bard JA, Zgombick J, Adham N, Vaysse P, Branchek TA, Weinshank RL (November 1993). "Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase". The Journal of Biological Chemistry 268 (31): 23422–6. PMID 8226867. http://www.jbc.org/cgi/pmidlookup?view=long&pmid=8226867. 
  28. ^ Hoyer D, Neijt HC (March 1988). "Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding". Molecular Pharmacology 33 (3): 303–9. PMID 3352595. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3352595. 
  29. ^ Runyon SP, Savage JE, Taroua M, Roth BL, Glennon RA, Westkaemper RB (March 2001). "Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene". Bioorganic & Medicinal Chemistry Letters 11 (5): 655–8. doi:10.1016/S0960-894X(01)00023-3. PMID 11266163. http://linkinghub.elsevier.com/retrieve/pii/S0960894X01000233. 
  30. ^ 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. 
  31. ^ Riccioppo Neto F (March 1979). "The local anesthetic effect of cyproheptadine on mammalian nerve fibres". European Journal of Pharmacology 54 (3): 203–7. doi:10.1016/0014-2999(79)90078-5. PMID 428422. 
  32. ^ Lindsay Murray; Frank Daly; David McCoubrie; Mike Cadogan (15 January 2011). Toxicology Handbook. Elsevier Australia. p. 388. ISBN 978-0-7295-3939-5. http://books.google.com/books?id=KDOeIldGWxQC&pg=PT388. Retrieved 27 November 2011. 
  33. ^ Lexi-Comp (August 2008). "Cyproheptadine". The Merck Manual Professional. http://www.merck.com/mmpe/lexicomp/cyproheptadine.html.  Retrieved on October 26, 2008.
  34. ^ 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. 
  35. ^ Cyproheptadine - Drugs.com
  36. ^ 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.
  37. ^ 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.
  38. ^ 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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Copyrights:

American Heritage Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
American Heritage Stedman's Medical Dictionary. The American Heritage® Stedman's Medical Dictionary Copyright © 2002, 2001, 1995 by Houghton Mifflin Company.  Read more
Saunders Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia on Answers.com. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article Cyproheptadine.  Read more

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