Selective 5-HT1B/1D serotonin receptor agonist
ATC code: N02CC01 (Sumatriptan)
A selective 5-HT1B/1D agonist. Constricts dilated cranial vessels via 5-HT1B and blocks release of inflammatory neuropeptides (CGRP, substance P) from trigeminal nerve endings via 5-HT1D. The first triptan on the market (1991), the «gold standard» benchmark for other triptans. Onset 30 minutes (tablets), 10–15 minutes (subcutaneous), 15 minutes (nasal spray). Half-life 2 hours.
First line
First-line for moderate-to-severe migraine attacks per AHS 2024 and EFNS 2022. The Cochrane meta-analysis showed pain-free response at 2 hours with sumatriptan 100 mg in 38% versus 17% on placebo. Subcutaneous 6 mg gives 70% pain-free response – highest efficacy among triptans. Take at the first sign of pain, not during aura. In pregnant migraineurs, sumatriptan has the largest data set among triptans and is preferred when needed.
Sources
First line
Acute migraine in nursing mothers. Per AHS 2024 and SEMNIM 2023, the triptan of choice. Dose 50-100 mg orally at onset, repeat at 2 h if incomplete. Max 200 mg/day.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Sumatriptan is a triptan (a serotonin 5-HT1B/1D receptor agonist). It is prescribed for migraine and cluster headache ( NG150 2021, AHS 2021, and AEMPS Ficha Técnica). For tension-type headache, stress-related headache, hangover, or premenstrual headache, sumatriptan is not indicated and may worsen the picture: regular use for non-migraine headache provokes medication-overuse headache. The drug is contraindicated in ischemic heart disease, prior stroke, and uncontrolled hypertension; coronary vasospasm has been reported in susceptible patients on triptans. If sumatriptan was prescribed for any severe headache outside a migraine or cluster headache indication, consider seeking a second opinion.
6 pairs found. Sorted from critical to minor.
Mechanism
Both are 5-HT1B/1D vasoconstrictors. Additive coronary and peripheral vasospasm. – at least 24-hour washout.
Symptoms
Myocardial ischaemia, stroke within hours.
Management
Combination contraindicated. At least 24 hours between doses.
Mechanism
Both drugs are 5-HT1B/1D vasoconstrictors. Additive effect on coronary and peripheral arteries. requires at least 24-hour separation.
Symptoms
Myocardial ischaemia, stroke, digital ischaemia within hours.
Management
Combination contraindicated. At least 24 hours between ergotamine and any triptan.
Mechanism
Sumatriptan is a 5-HT1B/1D agonist, partly metabolised by MAO-A. Phenelzine irreversibly inhibits MAO – sumatriptan accumulates and excess serotonin triggers fatal serotonin syndrome.
Symptoms
Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.
Management
Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.
Mechanism
Tranylcypromine irreversibly inhibits MAO-A. Sumatriptan accumulates – fatal serotonin syndrome.
Symptoms
Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.
Management
Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.
Mechanism
Selegiline at high doses loses MAO-B selectivity and inhibits MAO-A. Serotonin syndrome risk with triptans.
Symptoms
Agitation, tachycardia, hypertension.
Management
Avoid combination, especially with selegiline above 10 mg/day. Alternative – paracetamol for migraine attack.
Mechanism
Theoretical serotonin syndrome risk with SSRI + triptan. revised the recommendation in 2018 (previously CONTRA) – clinical cases at standard doses are few. Still, monitoring is needed at first use.
Symptoms
Rarely – agitation, tremor, myoclonus. Mainly with high triptan doses or SNRI combination.
Management
Acceptable at standard doses. Inform patient of possible symptoms.
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FDA category C. The largest triptan pregnancy data set (over 5000 pregnancies in Swedish and Norwegian registries) – no described teratogenicity. When a triptan is needed in pregnant patients with severe migraine, sumatriptan is the preferred choice.
Fully compatible. Hale L2. RID 3.5%. Best-studied triptan during breastfeeding. After 100 mg sumatriptan, feeding may be delayed 4-8 h for extra safety, although no clinically significant infant effects have been reported.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Sumatriptan is evaluated for the following indications with varying evidence strength: Migraine during breastfeeding (evidence tier A), Acute migraine attack (evidence tier A), Memory and concentration enhancement (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Sumatriptan (≥ 1 in 100): Chest, neck, or jaw tightness or pressure, Drowsiness, Dizziness, Nausea, Warmth or flushing, Injection-site reactions (subcutaneous). See the Safety section for uncommon and serious reactions.
FDA category C. FDA category C. The largest triptan pregnancy data set (over 5000 pregnancies in Swedish and Norwegian registries) – no described teratogenicity. When a triptan is needed in pregnant patients with severe migraine, sumatriptan is the preferred choice.
Fully compatible. Hale L2. RID 3.5%. Best-studied triptan during breastfeeding. After 100 mg sumatriptan, feeding may be delayed 4-8 h for extra safety, although no clinically significant infant effects have been reported.
Sumatriptan is contraindicated in: Sumatriptan hypersensitivity; Coronary artery disease, prior MI; Uncontrolled hypertension; History of cerebrovascular events (stroke, TIA); Peripheral arterial disease. Full list in the Safety section.