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Triptan

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Triptan, Serotonin 5-HT1 Receptor Agonist, Selective 5-HT Receptor Agonist

  • See Also
  1. Migraine Abortive Treatment
  2. Triptan Overdose
  3. Sumatriptan
  4. Rizatriptan
  5. Zolmitriptan
  6. Naratriptan
  7. Eletriptan
  8. Frovatriptan
  9. Almotriptan
  • Indications
  • General
  1. Migraine Abortive Treatment
  2. Cluster Headache
  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. Coronary Artery Disease
  2. Prinzmetal's Angina
  3. Uncontrolled Hypertension
  4. Basilar Artery Migraine
  5. Familial Hemiplegic Migraine
  6. Ischemic Cerebrovascular Accident
  7. Pregnancy
  8. 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
  1. Screen for cardiovascular disease before use!
  2. Limit to no more than twice weekly
  1. Subcutaneous Sumatriptan
    1. Initial: 6 mg SC
    2. Repeat in 12 hours prn
    3. Maximum: 12 mg/day
    4. Even generic dosing approaches $100/dose
  2. Oral Sumatriptan
    1. Dose 25 to 100 mg orally every 2 hours prn
      1. Start at max single dose, 100 mg orally for best efficacy in young adult without contraindications
    2. Maximum: 300 mg/day
    3. Generic dosing may be as low as $3/dose
  3. Intranasal Sumatriptan
    1. Initial: 5, 10 or 20 mg intranasal
      1. Dose responsive (20 mg more effective)
    2. Repeat after 2 hours prn
    3. Maximum: 40 mg/day
    4. Safety of use in over 4 Headaches per month not known
  4. 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
  5. Other Sumatriptan formulations
    1. Zecurity patch
      1. Removed from market 2016 due to serious adverse effects including burns
      2. http://www.fda.gov/Drugs/DrugSafety/ucm504588.htm
  1. Initial: 5 to 10 mg orally (MLT form is lingual)
    1. Start at max single dose, 10 mg orally for best efficacy in young adult without contraindications
  2. Repeat dose in 2 hours
  3. Maximum: 30 mg in 24 hours
  1. Initial: 1 to 2.5 mg orally
  2. Repeat in 4 hours
  3. Maximum: 5 mg in 24 hours
  4. Generic options available, but more expensive than Sumatriptan, Rizatriptan
  5. Consider for longer lasting Migraines (but have delayed onset)
  1. Oral
    1. Initial: 1.25 to 2.5 mg orally
    2. Repeat dose every 2 hours
    3. Maximum: 10 mg in 24 hours
  2. Intranasal
    1. Dose: 5 mg spray (single dose unit)
    2. Onset: 15 minutes (faster than oral preparations)
  1. Initial: 20 to 40 mg orally
  2. May repeat dose in 2 hours
  3. Maximum: 40 mg/dose or 80 mg/day
  1. Initial: 6.25 to 12.5 mg orally; may repeat in 2 hours
  2. Maximum: 2 doses in 24 hours
  1. Initial dosing: 2.5 mg orally; may repeat in 2 hours
  2. Maximum dose: 7.5 mg per day
  3. Consider for longer lasting Migraines (but have delayed onset)
  • Adverse Effects
  1. See Triptan Overdose
  2. 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
  3. Medication Overuse Headaches
    1. Highest risk with >10 doses per month
    2. Limit to two doses weekly
  4. Injection (e.g. Sumatriptan)
    1. Tingling, Flushing or burning Sensation at injection sites
  5. Intranasal preparations
    1. Dysgeusia (Terrible taste)
  • 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. Consult obstetrics before use
    4. May be considered if Migraines are uncontrolled, debilitating
      1. If used, Sumatriptan has the longest safety data
    5. 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)
    6. 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
  4. Propranolol with Rizatriptan
    1. Requires reducing Rizatriptan dose
  1. Most effective oral agents (compared with Imitrex 100 mg PO)
    1. Rizatriptan (Maxalt) 10 mg orally
    2. Eletriptan (Relpax) 80 mg orally
    3. Almotriptan (Axert) 12.5 mg orally (least side effects)
  2. References
    1. Ferrari (2001) Lancet 358:1668-75 [PubMed]
  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. Triptans (StatPearls)
    1. https://www.ncbi.nlm.nih.gov/books/NBK554507/
  2. Where do Triptans act in the treatment of Migraine? (PMC)
    1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1850935/
  • References
  1. Jamieson (2002) Am J Med 112:138 [PubMed]
  2. Ahn (2005) Pain 115(1-2):1-4 +PMID: 15836963 [PubMed]