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Title: Triptan  
Author: World Heritage Encyclopedia
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Subject: Serotonin receptor agonist, Sumatriptan, Frovatriptan, Methysergide, Dihydroergotamine
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Triptans are a family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches. They were first introduced in the 1990s. While effective at treating individual headaches, they do not provide preventative treatment and are not considered a cure.

Triptans include sumatriptan (Imitrex, Imigran, Cinie, Illument, Migriptan), rizatriptan (Maxalt), naratriptan (Amerge, Naramig), zolmitriptan (Zomig), eletriptan (Relpax), almotriptan (Axert, Almogran), frovatriptan (Frova, Migard, Frovamig), avitriptan (BMS-180,048), and donitriptan (F-11356).

sumatriptan rizatriptan naratriptan eletriptan
almotriptan frovatriptan avitriptan zolmitriptan


  • Medical uses 1
  • Mechanism of action 2
  • Discovery and development 3
  • Availability 4
  • Effectiveness 5
    • Migraine 5.1
    • Altitude sickness 5.2
  • Adverse effects 6
  • See also 7
  • References 8

Medical uses

Summary of triptan warnings
Do not use if these are present: Consult pharmacist; use with caution if these are present:
A history of any of these:
  1. Heart attack[1]
  2. Stroke[1]
  3. Transient ischemic attack[1]
  4. Familial hemiplegic migraine[1]

Currently living with any of these:

  1. Coronary artery disease[1]
  2. Peripheral vascular disease[1]
  3. uncontrolled high blood pressure[1]
  1. Men older than 40[1]
  2. Women older than 55[1]
  3. taking certain antidepressants - ask doctor for specifics[1]
  4. family history of early Cardiovascular disease[1]
  5. family history of stroke[1]
  6. diabetes[1]
  7. high cholesterol[1]
  8. menopause[1]
  9. obesity[1]
  10. pregnancy[1]
  11. Smoking[1]

Triptans are used in the treatment of migraines and cluster headaches.

Mechanism of action

Their action is attributed to their agonist[2] effects on serotonin 5-HT1B and 5-HT1D receptors in cranial blood vessels (causing their constriction) and subsequent inhibition of pro-inflammatory neuropeptide release. Evidence is accumulating that these drugs are effective because they act on serotonin receptors in nerve endings as well as the blood vessels. This leads to a decrease in the release of several peptides, including CGRP and substance P.

Discovery and development


These drugs have been available only by prescription (US, Canada and UK), but sumatriptan became available over-the-counter in the UK in June, 2006.[3] The brand name of the OTC product in the UK is Imigran Recovery. The patent on Imitrex STATDose expired in December 2006, and injectable sumatriptan became available in generic formula in August 2008. Sumavel Dosepro is a needle free delivery of injectable sumatriptan that was approved in the US by the FDA in July 2009.[4] Sumatriptan became available as a generic in the US in late 2009. Sumatriptan used to be sold over-the-counter in Romania, under the Imigran brand; however, as of August 2014 prescription is required. Sumatriptan is also available as a nasal spray, and Phase III clinical trials with a iontophoretic patch (Zelrix) are under way as of April 2010.



Sumatriptan and related selective serotonin receptor agonists are excellent for severe migraine attacks or those that do not respond to NSAIDs [5] or other over-the-counter drugs.[6] Triptans are a mid-line treatment suitable for many migraineurs with typical attacks. They may not work for atypical or unusually severe migraine attacks, transformed migraine, or status (continuous) migrainosus.

Triptans are highly effective, reducing the symptoms or aborting the attack within 30 to 90 minutes in 70-80% of patients.

Assessment of efficacy may be contaminated by how the triptan is encapsulated in order to mask active treatment.[7]

A test measuring a person's skin sensitivity during a migraine may indicate whether the individual will respond to treatment with triptans.[8] Triptans are most effective in those with no skin sensitivity; with skin sensitivity, it is best to take triptans within twenty minutes of the headache's onset.

Altitude sickness

A single randomized controlled trial found that sumatriptan may be able to prevent altitude sickness.[9]

Adverse effects

Triptans have few side effects if used in correct dosage and frequency. The most common adverse effect is recurrence of migraine. A systematic review found that "rizatriptan 10 mg was the only triptan with a recurrence rate greater than that of placebo".[10]

There is a theoretical risk of coronary spasm in patients with established heart disease, and cardiac events after taking triptans may rarely occur.[11]

There is the potential for life-threatening serotonin syndrome (a syndrome of changes in mental status, autonomic instability, neuromuscular abnormalities, and gastrointestinal symptoms) in patients taking triptans and selective serotonin reuptake inhibitors (SSRIs) or selective serotonin/norepinephrine reuptake inhibitors (SNRIs) at the same time.[12]

At least two types of triptans (sumatriptan and rizatriptan) have been listed under the unacceptable medication by the Canadian Blood Services, as a potential risk to the recipient; hence, donors are required not to have taken the medication for the last 72 hours.

See also


  1. ^ a b c d e f g h i j k l m n o p q r  
  2. ^ Tepper, S. J.; Rapoport, A. M.; Sheftell, F. D. (2002). "Mechanisms of action of the 5-HT1B/1D receptor agonists". Archives of neurology 59 (7): 1084–1088.  
  3. ^ "Pharmacies to sell migraine drug". BBC NEWS. 2006-05-19. Retrieved 2006-09-05. 
  4. ^ Zogenix, inc. Press release
  5. ^ Brandes JL, Kudrow D, Stark SR, et al. (2007). "Sumatriptan-naproxen for acute treatment of migraine: a randomized trial". JAMA 297 (13): 1443–54.  
  6. ^ Lipton RB, Baggish JS, Stewart WF, Codispoti JR, Fu M (2000). "Efficacy and safety of acetaminophen in the treatment of migraine: results of a randomized, double-blind, placebo-controlled, population-based study". Arch. Intern. Med. 160 (22): 3486–92.  
  7. ^ Fuseau E, Petricoul O, Sabin A, et al. (2001). "Effect of encapsulation on absorption of sumatriptan tablets: data from healthy volunteers and patients during a migraine". Clinical therapeutics 23 (2): 242–51.  
  8. ^ Burstein, R., Collins, B., Jakubowski, M. (2004) Defeating migraine pain with triptans: A race against the development of cutaneous allodynia. Annals of Neurology, (55) 1. pg. 19-26.
  9. ^ Jafarian S, Gorouhi F, Salimi S, Lotfi J (2007). "Sumatriptan for prevention of acute mountain sickness: randomized clinical trial". Ann. Neurol. 62 (3): 273–7.  
  10. ^ Pascual J, Mateos V, Roig C, Sanchez-Del-Rio M, Jiménez D (2007). "Marketed oral triptans in the acute treatment of migraine: a systematic review on efficacy and tolerability". Headache 47 (8): 1152–68.  
  11. ^ Dahlöf CG, Mathew N (1998). "Cardiovascular safety of 5HT1B/1D agonists--is there a cause for concern?". Cephalalgia : an international journal of headache 18 (8): 539–45.  
  12. ^ US Food and Drug Administration (2006-07-19). "Information for Healthcare Professionals".  
  • Tepper S. J., Rapoport A. M. (1999). "The triptans - A summary". CNS Drugs 12 (5): 403–417.  
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