Summary: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.

Top Publications

  1. Wenzel R. A comment on acetaminophen, aspirin, and caffeine versus sumatriptan succinate in the early treatment of migraine: results from the ASSET trial. Headache. 2006;46:341; author reply 341-3 pubmed
  2. Ishkanian G, Blumenthal H, Webster C, Richardson M, Ames M. Efficacy of sumatriptan tablets in migraineurs self-described or physician-diagnosed as having sinus headache: a randomized, double-blind, placebo-controlled study. Clin Ther. 2007;29:99-109 pubmed
    ..The purpose of this study was to assess the efficacy and tolerability of sumatriptan succinate 50-mg tablets in patients with migraine presenting with "sinus" headache...
  3. Vera Portocarrero L, Ossipov M, King T, Porreca F. Reversal of inflammatory and noninflammatory visceral pain by central or peripheral actions of sumatriptan. Gastroenterology. 2008;135:1369-78 pubmed publisher
    b>Sumatriptan is used specifically to relieve headache pain. The possible efficacy of sumatriptan was investigated in 2 models of visceral pain. Pancreatic inflammation was induced by intravenous injection of dibutyltin dichloride...
  4. Denuelle M, Boulloche N, Payoux P, Fabre N, Trotter Y, Geraud G. A PET study of photophobia during spontaneous migraine attacks. Neurology. 2011;76:213-8 pubmed publisher
    ..Nevertheless, 2 facts appear to have a link with photophobia: visual cortex hyperexcitability on the one hand and interactions between visual pathway and trigeminal nociception on the other...
  5. Pierce M, Marbury T, O NEILL C, Siegel S, Du W, Sebree T. Zelrix: a novel transdermal formulation of sumatriptan. Headache. 2009;49:817-25 pubmed publisher
    ..Conshohocken, PA, USA), the novel formulation of sumatriptan (formerly known as NP101)...
  6. Tfelt Hansen P. Does sumatriptan cross the blood-brain barrier in animals and man?. J Headache Pain. 2010;11:5-12 pubmed publisher
    b>Sumatriptan, a relatively hydrophilic triptan, based on several animal studies has been regarded to be unable to cross the blood-brain barrier (BBB)...
  7. Harriott A, Scheff N, Gold M. The complex actions of sumatriptan on rat dural afferents. Cephalalgia. 2012;32:738-49 pubmed publisher
    ..rat dural afferents were studied with whole cell and perforated patch techniques in the absence and presence of sumatriptan and/or IM (prostaglandin E2, bradykinin, and histamine)...
  8. Sakai Y, Dobson C, Diksic M, Aube M, Hamel E. Sumatriptan normalizes the migraine attack-related increase in brain serotonin synthesis. Neurology. 2008;70:431-9 pubmed publisher
    ..5-HT synthetic rate during different phases of their migraine attack and after acute antimigraine therapy with sumatriptan, and to compare them with normal controls...
  9. Sheftell F, Bigal M, Tepper S, Rapoport A. Sumatriptan: a decade of use and experience in the treatment of migraine. Expert Rev Neurother. 2004;4:199-209 pubmed
    ..b>Sumatriptan (Imitrex) has been available for the longest time within the class, is most flexible in form and has been given ..

More Information


  1. Ghelardini C, Galeotti N, Grazioli I, Uslenghi C. Indomethacin, alone and combined with prochlorperazine and caffeine, but not sumatriptan, abolishes peripheral and central sensitization in in vivo models of migraine. J Pain. 2004;5:413-9 pubmed
    ..of this study was to investigate whether the 3 active principles of IndoProCaf, alone and combined, compared to sumatriptan, were able to abolish the peripheral sensitization induced by kainic acid and the central sensitization induced ..
  2. Nikai T, Basbaum A, Ahn A. Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008;139:533-40 pubmed publisher
    b>Sumatriptan and the other triptan drugs target the serotonin receptor subtypes1B, 1D, and 1F (5-HT(1B/D/F)), and are prescribed widely in the treatment of migraine...
  3. Cleves C, Tepper S. Sumatriptan/naproxen sodium combination for the treatment of migraine. Expert Rev Neurother. 2008;8:1289-97 pubmed publisher
    b>Sumatriptan 85 mg with naproxen sodium 500 mg, a combination tablet for the acute treatment of migraine, is approved in the USA...
  4. Martin V, Ballard J, Diamond M, Mannix L, Derosier F, Lener S, et al. Relief of menstrual symptoms and migraine with a single-tablet formulation of sumatriptan and naproxen sodium. J Womens Health (Larchmt). 2014;23:389-96 pubmed publisher
    ..randomized controlled trials of 621 adult menstrual migraineurs with dysmenorrhea who treated migraine with sumatriptan-naproxen or placebo...
  5. Mathew N, Landy S, Stark S, Tietjen G, Derosier F, White J, et al. Fixed-dose sumatriptan and naproxen in poor responders to triptans with a short half-life. Headache. 2009;49:971-82 pubmed publisher
    To evaluate efficacy and tolerability of a single, fixed-dose tablet of sumatriptan 85 mg/naproxen sodium 500 mg (sumatriptan/naproxen sodium) vs placebo in migraineurs who had discontinued treatment with a short-acting triptan because ..
  6. Asghar M, Hansen A, Amin F, van der Geest R, Koning P, Larsson H, et al. Evidence for a vascular factor in migraine. Ann Neurol. 2011;69:635-45 pubmed publisher
    ..Data were obtained at baseline, during migraine attack, and after treatment with the migraine abortive drug sumatriptan (a 5-hydroxytryptamine agonist). We found dilatation of both MMA and MCA during migraine attack (p = 0.001)...
  7. Sheshala R, Khan N, Darwis Y. Formulation and optimization of orally disintegrating tablets of sumatriptan succinate. Chem Pharm Bull (Tokyo). 2011;59:920-8 pubmed
    The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug...
  8. Pascual J, Muñoz P. Correlation between lipophilicity and triptan outcomes. Headache. 2005;45:3-6 pubmed
    ..4 = -2.1 almotriptan < -1.5 sumatriptan < -1.0 zolmitriptan < -0.7 rizatriptan < -0.2 naratriptan < 0.5 eletriptan)...
  9. Kostic M, Gutierrez F, Rieg T, Moore T, Gendron R. A prospective, randomized trial of intravenous prochlorperazine versus subcutaneous sumatriptan in acute migraine therapy in the emergency department. Ann Emerg Med. 2010;56:1-6 pubmed publisher
    Intravenous (IV) prochlorperazine with diphenhydramine is superior to subcutaneous sumatriptan in the treatment of migraine patients presenting to the emergency department (ED)...
  10. Anghileri E, Toso V, Perini F. Acute myocardial infarction after sumatriptan administration for cluster headache. Neurol Sci. 2006;26:456-9 pubmed
    The pain of cluster headache attacks is severe, excruciating and selectively responsive to subcutaneous sumatriptan. Serious cardiovascular events attributed to sumatriptan are extremely rare and have most often been reported in patients ..
  11. Juhasz G, Zsombok T, Jakab B, Nemeth J, Szolcsanyi J, Bagdy G. Sumatriptan causes parallel decrease in plasma calcitonin gene-related peptide (CGRP) concentration and migraine headache during nitroglycerin induced migraine attack. Cephalalgia. 2005;25:179-83 pubmed
    b>Sumatriptan-induced changes in plasma calcitonin gene-related peptide (CGRP) concentration and headache intensity were investigated in 19 female migraineurs during nitroglycerin-induced migraine attack...
  12. Diamond S, Freitag F, Feoktistov A, Nissan G. Sumatriptan 6 mg subcutaneous as an effective migraine treatment in patients with cutaneous allodynia who historically fail to respond to oral triptans. J Headache Pain. 2007;8:13-8 pubmed
    The objective of the study was to assess the efficacy of 6 mg subcutaneous (s.c.) sumatriptan to treat migraine and the relationship between response of migraine and cutaneous allodynia in a population of migraine patients who ..
  13. Femenía Font A, Balaguer Fernández C, Merino V, López Castellano A. Combination strategies for enhancing transdermal absorption of sumatriptan through skin. Int J Pharm. 2006;323:125-30 pubmed
    The aim of the present work was to characterize in vitro sumatriptan transdermal absorption through human skin and to investigate the effect of chemical enhancers and iontophoresis applied both individually and in combination...
  14. Sakamoto Y, Sekino Y, Yamada E, Higurashi T, Ohkubo H, Sakai E, et al. Effect of sumatriptan on gastric emptying: a crossover study using the BreathID system. World J Gastroenterol. 2012;18:3415-9 pubmed publisher
    To determine the effect of oral sumatriptan on gastric emptying using a continuous ¹³C breath test (BreathID system). Ten healthy male volunteers participated in this randomized, 2-way crossover study...
  15. Barbanti P, Fabbrini G, Berardelli A. Acute pathological laughter induced by sumatriptan. Cephalalgia. 2008;28:92-3 pubmed
  16. Zinck T, Illum R, Jansen Olesen I. Increased expression of endothelial and neuronal nitric oxide synthase in dura and pia mater after air stress. Cephalalgia. 2006;26:14-25 pubmed
    ..and eNOS and nNOS in pia mater seen after stress could not be antagonized by treatment with the migraine drug sumatriptan. These findings point towards the involvement of increased NO concentrations in dura and pia mater in response ..
  17. Dash S, Bogdanova O, Xavier A, Farkas J, Pullicino P. Cerebral vasospasm from sumatriptan. Neurology. 2004;63:2128 pubmed
  18. Erbilen E, Ozhan H, Akdemir R, Yazici M. A case of myocardial infarction with sumatriptan use. Pediatr Cardiol. 2005;26:464-6 pubmed
    b>Sumatriptan is widely used in the treatment of acute attacks of cluster headache. It is a serotonin-1 (5HT-1) agonist...
  19. Asghar M, Hansen A, Kapijimpanga T, van der Geest R, van der Koning P, Larsson H, et al. Dilation by CGRP of middle meningeal artery and reversal by sumatriptan in normal volunteers. Neurology. 2010;75:1520-6 pubmed publisher
    ..CGRP-induced vasodilation contributes to immediate head pain and whether the migraine-specific abortive drug sumatriptan, a 5-hydroxytryptamine 1B/1D agonist, inhibits CGRP-induced immediate vasodilation and headache...
  20. Mandema J, Cox E, Alderman J. Therapeutic benefit of eletriptan compared to sumatriptan for the acute relief of migraine pain--results of a model-based meta-analysis that accounts for encapsulation. Cephalalgia. 2005;25:715-25 pubmed
    A novel model-based meta-analysis was used to quantify the dose-response relationship of sumatriptan and eletriptan for the proportion of patients that achieve migraine pain relief up to 4 h after treatment...
  21. Mehrotra S, Vanmolkot K, Frants R, van den Maagdenberg A, Ferrari M, Maassenvandenbrink A. The phe-124-Cys and A-161T variants of the human 5-HT1B receptor gene are not major determinants of the clinical response to sumatriptan. Headache. 2007;47:711-6 pubmed
    The 5-HT(1B/1D) receptor agonist sumatriptan is highly effective in the treatment of migraine. However, some patients do not respond to sumatriptan or experience recurrence of the headache after initial relief...
  22. Bakhshayesh B, Seyed Saadat S, Rezania K, Hatamian H, Hossieninezhad M. A randomized open-label study of sodium valproate vs sumatriptan and metoclopramide for prolonged migraine headache. Am J Emerg Med. 2013;31:540-4 pubmed publisher
    The objective of this study is to compare the efficacy and tolerability of intravenous valproic acid (iVPA) with intramuscular metoclopramide + subcutaneous (SQ) sumatriptan for prolonged acute migraine.
  23. Bates E, Nikai T, Brennan K, Fu Y, Charles A, Basbaum A, et al. Sumatriptan alleviates nitroglycerin-induced mechanical and thermal allodynia in mice. Cephalalgia. 2010;30:170-8 pubmed publisher
    ..Moreover, sumatriptan, a drug with relative specificity for migraine, alleviated the NTG-induced allodynia...
  24. Ahn A, Basbaum A. Where do triptans act in the treatment of migraine?. Pain. 2005;115:1-4 pubmed
  25. Brandes J, Kudrow D, Stark S, O Carroll C, Adelman J, O Donnell F, et al. Sumatriptan-naproxen for acute treatment of migraine: a randomized trial. JAMA. 2007;297:1443-54 pubmed
    ..To evaluate the efficacy and safety of a fixed-dose tablet containing sumatriptan succinate and naproxen sodium relative to efficacy and safety of each monotherapy and placebo for the acute ..
  26. Erlichson K, Waight J. Therapeutic applications for subcutaneous triptans in the acute treatment of migraine. Curr Med Res Opin. 2012;28:1231-8 pubmed publisher
    ..This clinical review of subcutaneous sumatriptan discusses its characteristics, efficacy, and tolerability and considers its place in clinical practice...
  27. Sternieri E, Pinetti D, Coccia C, Leone S, Bertolini A, Ferrari A. Pharmacokinetics of sumatriptan in non-respondent and in adverse drug reaction reporting migraine patients. J Headache Pain. 2005;6:319-21 pubmed
    b>Sumatriptan is a selective agonist of 5HT1 (1B/1D) receptors, which has proved to be effective and safe for the acute treatment of migraine attacks...
  28. Siegel S, O NEILL C, Dube L, Kaldeway P, Morris R, Jackson D, et al. A unique iontophoretic patch for optimal transdermal delivery of sumatriptan. Pharm Res. 2007;24:1919-26 pubmed
    ..The purpose of this study was to assess the pharmacokinetic and safety profile of a novel iontophoretic sumatriptan delivery system, NP101, which uses an electrical current to propel sumatriptan across intact skin and into ..
  29. Ghelardini C, Galeotti N, Vivoli E, Grazioli I, Uslenghi C. The central analgesia induced by antimigraine drugs is independent from Gi proteins: superiority of a fixed combination of indomethacin, prochlorperazine and caffeine, compared to sumatriptan, in an in vivo model. J Headache Pain. 2009;10:435-40 pubmed publisher
    ..Gi proteins activity is abolished by pertussis toxin (PTX), compared to its single active ingredients and to sumatriptan. The mice model of abdominal constriction test induced by an i.p. injection of a 0...
  30. Kamel A, Colizza K, Gunduz M, Harriman S, Obach R. In vitro-in vivo correlation for intrinsic clearance for CP-409,092 and sumatriptan: a case study to predict the in vivo clearance for compounds metabolized by monoamine oxidase. Xenobiotica. 2012;42:355-62 pubmed publisher
    Oxidative deamination of the GABA(A) partial agonist CP-409,092 and sumatriptan represents a major metabolic pathway and seems to play an important role for the clearance of these two compounds...
  31. Jakubowski M, Levy D, Goor Aryeh I, Collins B, Bajwa Z, Burstein R. Terminating migraine with allodynia and ongoing central sensitization using parenteral administration of COX1/COX2 inhibitors. Headache. 2005;45:850-61 pubmed
    ..Patients exhibiting migraine with allodynia were divided in two groups (n=14, each): group 1 received delayed sumatriptan injection (6 mg) 4 hours after onset of attack--which failed to render them pain free-and ketorolac infusion (..
  32. Barbanti P, Carpay J, Kwong W, Ahmad F, Boswell D. Effects of a fast disintegrating/rapid release oral formulation of sumatriptan on functional ability in patients with migraine. Curr Med Res Opin. 2004;20:2021-9 pubmed
    A new oral form of sumatriptan has been developed to facilitate tablet disintegration and drug dispersion and to mitigate the effects of gastric stasis that can accompany migraine...
  33. Vrbata P, Berka P, Stranska D, Dolezal P, Musilová M, Cižinská L. Electrospun drug loaded membranes for sublingual administration of sumatriptan and naproxen. Int J Pharm. 2013;457:168-76 pubmed publisher
    ..b>Sumatriptan succinate, naproxen, and its salt as well as combinations of these were incorporated into nanofibrous membranes ..
  34. Evans M, Cheng X, Jeffry J, Disney K, Premkumar L. Sumatriptan inhibits TRPV1 channels in trigeminal neurons. Headache. 2012;52:773-84 pubmed publisher
    To understand a possible role for transient potential receptor vanilloid 1 (TRPV1) ion channels in sumatriptan relief of pain mediated by trigeminal nociceptors. TRPV1 channels are expressed in small nociceptive sensory neurons...
  35. Silberstein S, Mannix L, Goldstein J, Couch J, Byrd S, Ames M, et al. Multimechanistic (sumatriptan-naproxen) early intervention for the acute treatment of migraine. Neurology. 2008;71:114-21 pubmed publisher
    ..To investigate the efficacy and tolerability of a fixed-dose, single-tablet formulation of sumatriptan 85 mg, formulated with RT Technology, and naproxen sodium 500 mg (sumatriptan/naproxen) as early intervention ..
  36. Sandrini G, Cerbo R, Del Bene E, Ferrari A, Genco S, Grazioli I, et al. Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, double-dummy, randomised, parallel grou. Int J Clin Pract. 2007;61:1256-69 pubmed
    ..a fixed combination of indomethacin, prochlorperazine and caffeine (Indoprocaf) was compared with encapsulated sumatriptan in the acute treatment of two migraine attacks...
  37. Friedman B, Hochberg M, Esses D, Bijur P, Corbo J, Paternoster J, et al. A clinical trial of trimethobenzamide/diphenhydramine versus sumatriptan for acute migraines. Headache. 2006;46:934-41 pubmed
    ..Consequently, even though several antiemetic medications as well as SQ sumatriptan have demonstrated efficacy and tolerability for the ED treatment of migraine, there remains a need for more ..
  38. Lipton R, Dodick D, Adelman J, Kaniecki R, Lener S, White J, et al. Consistency of response to sumatriptan/naproxen sodium in a placebo-controlled, crossover study. Cephalalgia. 2009;29:826-36 pubmed publisher
    ..randomized, placebo-controlled, crossover studies were conducted to evaluate consistency of response to sumatriptan/naproxen sodium 85/500 mg (S/NS) over four attacks in adults with migraine...
  39. Wendt J, Cady R, Singer R, Peters K, Webster C, Kori S, et al. A randomized, double-blind, placebo-controlled trial of the efficacy and tolerability of a 4-mg dose of subcutaneous sumatriptan for the treatment of acute migraine attacks in adults. Clin Ther. 2006;28:517-26 pubmed
    The aim of this study was to evaluate the efficacy and tolerability of a single 4-mg dose of sumatriptan SC for the acute treatment of adult patients experiencing a migraine attack with moderate to severe pain...
  40. Goldstein J, Silberstein S, Saper J, Elkind A, Smith T, Gallagher R, et al. Acetaminophen, aspirin, and caffeine versus sumatriptan succinate in the early treatment of migraine: results from the ASSET trial. Headache. 2005;45:973-82 pubmed
    ..acetaminophen 500 mg, aspirin 500 mg, and caffeine 130 mg) with a prescription migraine product (50 mg sumatriptan) in a randomized, controlled clinical trial in which subjects treated at the first sign of a migraine attack...
  41. Dodick D, Lipton R, Goadsby P, Tfelt Hansen P, Ferrari M, Diener H, et al. Predictors of migraine headache recurrence: a pooled analysis from the eletriptan database. Headache. 2008;48:184-93 pubmed publisher
  42. Lappin G, Shishikura Y, Jochemsen R, Weaver R, Gesson C, Brian Houston J, et al. Comparative pharmacokinetics between a microdose and therapeutic dose for clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen), and phenobarbital in human volunteers. Eur J Pharm Sci. 2011;43:141-50 pubmed publisher
    ..a microdose (100 ?g) to predict the human pharmacokinetics (PK) following a therapeutic dose of clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen) and phenobarbital, both within the study and by reference to the ..
  43. Friedman B, Corbo J, Lipton R, Bijur P, Esses D, Solorzano C, et al. A trial of metoclopramide vs sumatriptan for the emergency department treatment of migraines. Neurology. 2005;64:463-8 pubmed
    To compare the efficacy of 20 mg of IV metoclopramide, given up to four times over 2 hours as needed for persistent headache, with 6 mg of subcutaneous sumatriptan for the emergency department treatment of migraine headaches.
  44. Kwong W, Taylor F, Adelman J. The effect of early intervention with sumatriptan tablets on migraine-associated productivity loss. J Occup Environ Med. 2005;47:1167-73 pubmed
    ..This analysis examined productivity loss as a result of migraine after treatment with sumatriptan tablets and patients' usual non-triptan therapy when pain was mild (early intervention) versus when pain was ..
  45. Landy S, Savani N, Shackelford S, Loftus J, Jones M. Efficacy and tolerability of sumatriptan tablets administered during the mild-pain phase of menstrually associated migraine. Int J Clin Pract. 2004;58:913-9 pubmed
    ..double-blind, parallel-group, placebo-controlled clinical trials were conducted to assess the efficacy of sumatriptan tablets, 50mg and 100mg, for treatment during the mild-pain phase of a menstrually associated migraine among ..
  46. Gregor N, Schlesiger C, Akova Oztürk E, Kraemer C, Husstedt I, Evers S. Treatment of cluster headache attacks with less than 6 mg subcutaneous sumatriptan. Headache. 2005;45:1069-72 pubmed
    Subcutaneous (SQ) sumatriptan 6 mg is effective in the treatment of acute cluster headache attacks. However, patients sometimes benefit from a dose less than 6 mg...
  47. Winner P, Landy S, Richardson M, Ames M. Early intervention in migraine with sumatriptan tablets 50 mg versus 100 mg: a pooled analysis of data from six clinical trials. Clin Ther. 2005;27:1785-94 pubmed
    In clinical trials evaluating sumatriptan in the treatment of moderate or severe migraine pain, the 50- and 100-mg doses have been comparably effective and well tolerated...
  48. Obaidi M, Offman E, Messina J, Carothers J, Djupesland P, Mahmoud R. Improved pharmacokinetics of sumatriptan with Breath Powered™ nasal delivery of sumatriptan powder. Headache. 2013;53:1323-33 pubmed publisher
    The purpose of this study was to directly compare the pharmacokinetic (PK) profile of 22-mg sumatriptan powder delivered intranasally with a novel Breath Powered™ device (11?mg in each nostril) vs a 20-mg sumatriptan liquid nasal spray,..
  49. Scholpp J, Schellenberg R, Moeckesch B, Banik N. Early treatment of a migraine attack while pain is still mild increases the efficacy of sumatriptan. Cephalalgia. 2004;24:925-33 pubmed
    To investigate the hypothesis that early treatment of a migraine attack with sumatriptan, while pain is still mild, results in higher pain free rates in comparison to delayed treatment, when pain is at least moderate, we performed a ..
  50. Friedman B, Solorzano C, Esses D, Xia S, Hochberg M, Dua N, et al. Treating headache recurrence after emergency department discharge: a randomized controlled trial of naproxen versus sumatriptan. Ann Emerg Med. 2010;56:7-17 pubmed publisher
    ..The aim of this study is to compare the efficacy of oral sumatriptan with naproxen for treatment of post-ED recurrent primary headache...
  51. Mannix L, Martin V, Cady R, Diamond M, Lener S, White J, et al. Combination treatment for menstrual migraine and dysmenorrhea using sumatriptan-naproxen: two randomized controlled trials. Obstet Gynecol. 2009;114:106-13 pubmed publisher
    To evaluate the efficacy and tolerability of sumatriptan-naproxen during the mild pain phase of a single menstrual migraine attack associated with dysmenorrhea.
  52. Smith T, Goldstein J, Singer R, Pugach N, Silberstein S, Pierce M. Twelve-month tolerability and efficacy study of NP101, the sumatriptan iontophoretic transdermal system. Headache. 2012;52:612-24 pubmed publisher
    To assess the long-term tolerability and efficacy of NP101, a novel transdermal sumatriptan patch being developed for the acute treatment of migraine...
  53. Jennings E, Ryan R, Christie M. Effects of sumatriptan on rat medullary dorsal horn neurons. Pain. 2004;111:30-7 pubmed
    This study examined the cellular actions of the anti-migraine drug sumatriptan, on neurons in the substantia gelatinosa of the spinal trigeminal nucleus pars caudalis...