II. Indications: General

  1. Migraine Abortive Treatment (adults)
    1. Intranasal form has been used off-label for age >8 years
  2. Cluster Headache (subcutaneous form)
  3. Controversial cohorts in whom Triptan use is now thought safe (Cardiovascular Risk Factors)
    1. Controlled Diabetes Mellitus
    2. Controlled Hypertension
    3. Controlled Hyperlipidemia
    4. Postmenopausal women
    5. Men over age 40 years

III. Contraindications

  1. Severe hepatic Impairment
  2. Coronary Artery Disease
  3. Prinzmetal's Angina
  4. Uncontrolled Hypertension
  5. Basilar Artery Migraine
  6. Familial Hemiplegic Migraine
  7. Ischemic Cerebrovascular Accident
  8. Pregnancy
  9. Concurrent Medication use (absolute contraindications)
    1. MAO Inhibitor use
    2. Ergotamine use in prior 24 hours

IV. Mechanism

  1. Serotonergic 5-HT1 receptor Agonists
  2. Inhibits sensory dural nerve fiber neuropeptide release
  3. Intracranial extracerebral artery Vasoconstriction
    1. Mediated by Triptan direct effect on cerebrovascular Smooth Muscle

V. Precautions

  1. Screen for cardiovascular disease before use!
  2. Limit to no more than twice weekly

VI. Medications

  1. Sumatriptan (Imitrex)
    1. Oral 25 mg, 50 mg, 100 mg
      1. Generic dosing may be as low as $3/dose
    2. Intranasal forms
      1. Intranasal Imitrex: 5 mg, 20 mg (box of 6)
      2. Intranasal Tosymra: 10 mg
      3. Intranasal Onzetra Xsail: 11 mg powder
      4. Even generic dosing approaches $100/dose
    3. Subcutaneous Injections
      1. Subcutaneous Imitrex Injection: 6 mg prefilled syringe cartridges (box of 4)
      2. Subcutaneous Zembrace SymTouch 3 mg autoinjector
  2. Treximet (combination with Naproxen)
    1. Contains Sumatriptan 85 mg with Naproxen 500 mg
    2. Released as Sumatriptan becomes generically available
    3. Cheaper to purchase generic Sumatriptan (when available) and Naproxen separately
    4. Contraindicated in eGFR <30 ml/min
  3. Zecurity patch (listed for historical reasons only)
    1. Removed from market 2016 due to serious adverse effects including burns
    2. http://www.fda.gov/Drugs/DrugSafety/ucm504588.htm

VII. Dosing

  1. Limit to use in adults
    1. Intranasal form has been used off-label for age >8 years
  2. Subcutaneous Sumatriptan
    1. Initial: 6 mg SC
      1. May repeat in 1 hour if no effect with first dose
      2. Doses of 1-5 mg may be used if 6 mg is not tolerated
      3. If Headache returns, may switch to oral tablets, giving 25 mg every 2 hours (max 100 mg in 24 hours)
    2. Maximum: 12 mg/day
    3. Do NOT give IM or IV (use only SQ)
  3. Oral Sumatriptan
    1. Dose 25 to 100 mg orally every 2 hours as needed
      1. Start at 50 to 100 mg for first oral dose for best efficacy in young adult without contraindications
    2. Maximum: 200 mg in 24 hours
    3. Adjust for hepatic Impairment
      1. Mild to moderate hepatic Impairment: Limit maximum dose to 50 mg
      2. Severe hepatic Impairment: Avoid oral Sumatriptan
  4. Oral Treximet
    1. Adults
      1. Take 1 tablet (85/500 mg) orally at Migraine onset
      2. May repeat once in 2 hours
      3. Maximum: 2 tabs in 24 hours
      4. Limit to one 10/60 mg in mild to moderate hepatic Impairment (and avoid in severe hepatic Impairment)
    2. Child age >12 years
      1. Give 1 tablet (10/60 mg) orally at Migraine onset
      2. Maximum: 1 tablet (85/500 mg) in 24 hours
  5. Intranasal Sumatriptan
    1. Initial: 5, 10 or 20 mg intranasal
      1. Dose responsive (20 mg most effective)
    2. Repeat after 2 hours as needed
    3. Maximum: 40 mg in 24 hours
    4. Safety of use in over 4 Headaches per month not known
    5. Although FDA approved only for adults, Intranasal form has been used off-label for age >8 years
      1. Weight 20 to 39 kg: 10 mg intranasally at Headache onset, and may repeat once in 2 hours
      2. Weight >40 kg: 20 mg intranasally at Headache onset, and may repeat once in 2 hours

VIII. Adverse Effects

  1. See Triptan Overdose
  2. Injection (e.g. Sumatriptan)
    1. Tingling, Flushing or burning Sensation at injection sites
  3. Intranasal preparations
    1. Dysgeusia (Terrible taste)
  4. Vasospasm
    1. Generally benign in low risk populations
    2. Avoid in Coronary Artery Disease, Cerebrovascular Disease, Peripheral Arterial Disease
    3. Also avoid in hemiplegic Migraine or basilar Migraine
  5. Medication Overuse Headaches
    1. Highest risk with >10 doses per month
    2. Limit to two doses weekly

IX. Safety

  1. Unknown safety in Lactation
  2. Pregnancy Category C (most Triptans, but generally avoided in pregnancy)
    1. See Migraine Medications in Pregnancy
    2. Not recommended for routine use in pregnancy
    3. Avoid Treximet in pregnancy overall (contains Naproxen)
    4. Consult obstetrics before use
    5. May be considered if Migraines are uncontrolled, debilitating
      1. If used, Sumatriptan has the longest safety data
    6. Adverse effects in pregnancy
      1. Avoid in first trimester (fetal malformations and adverse pregnancy outcomes)
      2. Risk of uterine atony and peripartum Hemorrhage (but may be considered in debilitating Headache)
      3. Associated with hyperactivity and emotionality at age 3 in exposed children (AHRQ)
    7. References
      1. Nezvalova-Henriksen (2010) Headache 50(4): 563-75 +PMID: 20132339 [PubMed]

X. Drug Interactions

  1. See absolute contraindications above
    1. Ergotamine
    2. MAO Inhibitors
  2. Lithium
  3. Selective Serotonin Reuptake Inhibitor (SSRI)
    1. Risk of Serotonin Syndrome when combined with SSRI, SNRI or MAO Inhibitors

XI. Efficacy: Sumatriptan

  1. Efficacy dependent on mode of drug delivery
    1. Subcutaneous effective in 80% of patients
    2. Intranasal effective in 70% of patients
    3. Oral effective in 60% of patients
  2. Oral form does not prevent Migraine recurrence
    1. Rapoport (1995) Neurology 45:1505-9 [PubMed]

XII. Management: Overdose or Toxicity

XIV. References

Images: Related links to external sites (from Bing)

Related Studies

Cost: Medications

sumatriptan (on 10/19/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
SUMATRIPTAN 20 MG NASAL SPRAY Generic $19.13 each
SUMATRIPTAN 4 MG/0.5 ML INJECT Generic $132.25 per ml
SUMATRIPTAN 5 MG NASAL SPRAY Generic $36.07 each
SUMATRIPTAN 6 MG/0.5 ML AUTOINJ Generic $65.60 per ml
SUMATRIPTAN 6 MG/0.5 ML CART Generic $113.31 per ml
SUMATRIPTAN 6 MG/0.5 ML INJECT Generic $65.02 per ml
SUMATRIPTAN 6 MG/0.5 ML VIAL Generic $16.71 per ml
SUMATRIPTAN SUCC 100 MG TABLET Generic $0.50 each
SUMATRIPTAN SUCC 25 MG TABLET Generic $0.60 each
SUMATRIPTAN SUCC 50 MG TABLET Generic $0.43 each
SUMATRIPTAN-NAPROXEN 85-500 MG Generic $26.51 each
imitrex (on 1/1/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
IMITREX 100 MG TABLET Generic $0.50 each
IMITREX 20 MG NASAL SPRAY Generic $19.13 each
IMITREX 5 MG NASAL SPRAY Generic $36.07 each
IMITREX 50 MG TABLET Generic $0.43 each
IMITREX 6 MG/0.5 ML CARTRIDGES Generic $113.31 per ml

Ontology: Sumatriptan (C0075632)

Definition (NCI) A sulfonamide triptan with vasoconstrictor activity. Sumatriptan selectively binds to and activates serotonin 5-HT1D receptors in the central nervous system (CNS), thereby constricting cerebral blood vessels. This may lead to a relief in pain from vascular headaches. Sumatriptan may also relieve vascular headaches by decreasing the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during a migraine, by reducing extravasation of plasma proteins, and by decreasing the release of other mediators of inflammation from the trigeminal nerve.
Definition (CSP) sulfonamide serotonin agonist and vasoconstrictor that acts selectively at 5HT1 receptors; frequently used in treating migraines.
Definition (MSH) A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D018170
SnomedCT 350311006, 395892000, 322822007
LNC LP28529-3, MTHU013332
English Sumatriptan, 3-(2-(Dimethylamino)ethyl)-N-methyl-1H-indole-5-methanesulfonamide, 1H-Indole-5-methanesulfonamide, 3-(2-(dimethylamino)ethyl)-N-methyl-, sumatriptan, sumatriptan (medication), selective 5-HT receptor agonists sumatriptan, SUMATRIPTAN, Sumatriptan [Chemical/Ingredient], SUMAtriptan, Sumatriptan product, Sumatriptan (substance), Sumatriptan product (product), Sumatriptan product (substance)
Swedish Sumatriptan
Czech sumatriptan
Finnish Sumatriptaani
Russian SAMATRIPTAN, SUMATRIPTAN, САМАТРИПТАН, СУМАТРИПТАН
Japanese コハク酸スマトリプタン, スマトリプタン, イミグラン
Spanish sumatriptán (producto), sumatriptán, producto (producto), sumatriptán, sumatriptán, producto, sumatriptano (sustancia), sumatriptano, Sumatriptán
Polish Sumatryptan
French Sumatriptan
German Sumatriptan
Italian Sumatriptan
Portuguese Sumatriptana

Ontology: Sumatriptan Succinate (C0206599)

Definition (NCI) The succinate salt form of sumatriptan, a member of the triptan class of compounds with anti-migraine property. Sumatriptan succinate selectively binds to and activates serotonin 5-HT1 receptors. This results in constriction of meningeal, dural, cerebral or pial blood vessels via stimulation of the 5-HT1B receptors, thereby reducing the vascular pulsation and may provide relief in migraine headaches. Furthermore, agonistic action of this agent through presynaptic stimulation of 5-HT1D and/or 5-HT1F receptors prevents release of vasoactive and pro-inflammatory neuropeptide (calcitonin gene-related peptide), thereby may also relieve migraine headaches. In addition, central inhibition of pain transmission via the inhibition of trigeminal neurons in the brain stems and upper spinal cord mediated by 5-HT1B, 5-HT1D or 5-HT 1F receptors also aides in the alleviation of migraine pain.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D018170
SnomedCT 322805005, 96215002
English Succinate, Sumatriptan, sumatriptan succinate, sumatriptan succinate (medication), selective 5-HT receptor agonists sumatriptan succinate, sumatriptan (as succinate), SUMATRIPTAN SUCCINATE, Sumatriptan Succinate [Chemical/Ingredient], SUMAtriptan Succinate, Sumatriptan succinate, Sumatriptan succinate (substance), Sumatriptan succinate [dup] (substance), Sumatriptan Succinate
French Succinate de sumatriptan
Spanish succinato de sumatriptano (sustancia), succinato de sumatriptano, succinato de sumatriptán

Ontology: Imitrex (C0721044)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
English Imitrex, imitrex