Sumatriptan
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Sumatriptan (succinate)
Imitrex (oral, injectable, nasal), Tosymra (nasal spray), Onzetra Xsail (nasal powder), Zembrace SymTouch (low-dose autoinjector), Sumavel DosePro (needle-free SC)
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Summary
Common uses
Acute migraine with or without aura (FDA)0, Cluster headache (FDA; subcutaneous and nasal formulations specifically)0
Pharmacy
Starting dose
Oral: 50-100 mg at migraine onset, may repeat in 2 hours if needed. SC: 6 mg, may repeat in 1 hour. Nasal: 5-20 mg per nostril, may repeat in 2 hours
Preparations
Oral tablets 25, 50, 100 mg; SC injection 4, 6 mg autoinjector; needle-free SC 6 mg (Sumavel); nasal spray 5, 20 mg; nasal powder 22 mg (Onzetra Xsail); low-dose autoinjector 3 mg (Zembrace SymTouch)
US FDA Max
200 mg/day (oral); 12 mg/day (SC); 40 mg/day (nasal spray); 44 mg/day (Onzetra)
Pharmacology
Routes
Oral, subcutaneous, intranasal
Onset
10 minutes (SC); 15-30 minutes (nasal); 30-60 minutes (oral)
Duration
2-4 hours; headache recurrence rate ~20-30% within 24 hours
Half-life
2 hours[1]
Bioavailability
~14% (oral; substantial first-pass); ~97% (subcutaneous); ~17% (nasal)[1]
Pregnancy
Limited human data; pregnancy registry data have been broadly reassuring relative to baseline malformation rates.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Selective 5-HT1B and 5-HT1D receptor agonist. The 5-HT1B effect on cranial blood vessels produces vasoconstriction that reverses the neurogenic vasodilation of migraine; the 5-HT1D effect inhibits CGRP and other vasoactive neuropeptide release at trigeminal nerve terminals, blunting the neuroinflammatory cascade that drives migraine pain.0 Contraindicated in coronary artery disease, vasospastic angina (Prinzmetal), uncontrolled hypertension, history of ischemic stroke, and hemiplegic or basilar migraine. Serotonin syndrome risk with SSRIs and SNRIs has FDA labeling but the clinical incidence is debated. Should not be combined with ergot derivatives within 24 hours. Medicine-overuse headache is the major chronic-use complication, with the threshold of ≥10 days of triptan use per month[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Imitrex (sumatriptan succinate), GSK, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020132s029,020626s025,020080s055lbl.pdf