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Sumatriptan

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Sumatriptan, Sumatriptan Succinate, Imitrex, Treximet

  • See Also
  1. Triptan
  2. Migraine Abortive Treatment
  3. Triptan Overdose
  • 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
  • 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
  • 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
  • Precautions
  1. Screen for cardiovascular disease before use!
  2. Limit to no more than twice weekly
  • 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
  • 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
  • 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
  • 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]
  • 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
  • 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]
  1. See Triptan Overdose
  • Resources
  1. Sumatriptan Tablet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=121e36fb-471b-4318-bc47-b087ad68c6f7
  2. Sumatriptan Nasal Spray (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cc11b09d-e6cc-4cf8-1495-5ac64d5aae5f
  3. Sumatriptan Injection Solution (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=9b1bb8c9-be3a-47c3-b3bc-9c983cde7d23
  4. Treximet (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=42ddf376-8dc0-4236-be2a-0c6ae92ece04
  5. Triptans (StatPearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK554507/
  6. Where do Triptans act in the treatment of Migraine? (PMC)
    1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1850935/
  • References
  1. Hamilton (2020) Tarascon Pocket Pharmacopoeia
  2. Jamieson (2002) Am J Med 112:138 [PubMed]
  3. Ahn (2005) Pain 115(1-2):1-4 +PMID: 15836963 [PubMed]