SUMATRIPTAN SUCCINATE

Clinical safety rating: avoid

Other 5-HT1 agonists and MAOIs can have additive effects Contraindicated in ischemic heart disease and uncontrolled hypertension.

How it works

Selective serotonin 5-HT1B/1D receptor agonist; causes vasoconstriction of cranial blood vessels and inhibits release of pro-inflammatory neuropeptides.

What the body does with it

Metabolism	Hepatic via monoamine oxidase (MAO-A); some CYP450 involvement (CYP1A2, CYP3A4 minor).
Excretion	Primarily renal (60% as unchanged drug and metabolites, 40% via feces); approximately 20% unchanged in urine. Minor biliary excretion.
Half-life	Terminal elimination half-life: approximately 2 hours (range 1–4 hours). Clinical context: Short half-life supports use for acute migraine attacks; no accumulation with standard dosing.
Protein binding	14–21% (low binding; primarily to albumin and alpha1-acid glycoprotein).
Volume of Distribution	2.4 L/kg (range 2.0–3.0 L/kg). Indicates extensive extravascular distribution, crossing blood-brain barrier to reach central 5-HT1 receptors.
Bioavailability	Subcutaneous: 96% (complete); Oral: 15% (low due to first-pass metabolism); Intranasal: 15–17% (relative to SC); Rectal (suppository): ~20%.
Onset of Action	Subcutaneous injection: 10–15 minutes; Oral tablet: 30–60 minutes; Intranasal: 15–30 minutes.
Duration of Action	Subcutaneous: up to 2 hours (may extend to 4 hours with headache recurrence); Oral: 2–4 hours; Intranasal: 2–4 hours. Recurrence common within 24 hours.

Classification & Brands

Dosing & administration

50-100 mg orally at onset of migraine; may repeat after 2 hours if needed, max 200 mg/day. 6 mg subcutaneously as a single dose; may repeat after 1 hour if needed, max 12 mg/day. 20 mg intranasally as a single dose; may repeat after 2 hours if needed, max 40 mg/day.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment required for GFR ≥15 mL/min. For GFR <15 mL/min, triptans are generally avoided; hemodialysis does not remove sumatriptan.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh Class C). In mild to moderate impairment, no dose adjustment recommended; use with caution.
Pediatric use	Adolescents aged 12-17: 10 mg intranasally as a single dose; may repeat once after 2 hours if needed, max 20 mg/day. Pediatric use <12 years not established.
Geriatric use	Elderly patients have increased risk of coronary artery disease; contraindicated if CAD or other vascular disease suspected. Start at low end of dosing range; monitor for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other 5-HT1 agonists and MAOIs can have additive effects Contraindicated in ischemic heart disease and uncontrolled hypertension.

FDA category	Contraindicated
Breastfeeding	Excreted in breast milk; M/P ratio 2.1:1. Limited infant exposure; consider avoiding breastfeeding for 12 hours post-dose. Monitor infant for irritability, sleep disturbance.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show increased fetal abnormalities (e.g., omphalocele, cranioschisis) at high doses. Second/third trimesters: No well-controlled studies; potential for uterine hypertonus and reduced placental perfusion; use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Not recommended for use within 24 hours of another 5-HT1 agonist or ergotamine-containing medication due to risk of coronary vasospasm.

Side Effect Profile

Common Effects	Chest pain
Serious Effects

Absolute Contraindications

Ischemic heart disease, history of myocardial infarction, coronary vasospasm (Prinzmetal angina), peripheral vascular disease, cerebrovascular disease, uncontrolled hypertension, hemiplegic or basilar migraine, use within 24 hours of ergotamine derivatives or other 5-HT1 agonists, concomitant MAO-A inhibitor use or within 2 weeks of discontinuation, severe hepatic impairment.

Clinical Precautions

Precautions

Risk of myocardial ischemia, infarction, and arrhythmia; risk of cerebrovascular events; serotonin syndrome (especially with SSRIs/SNRIs); medication overuse headache; coronary artery disease risk assessment before use.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

SUMATRIPTAN SUCCINATE

Clinical safety rating: avoid

Other 5-HT1 agonists and MAOIs can have additive effects Contraindicated in ischemic heart disease and uncontrolled hypertension.

How it works

Selective serotonin 5-HT1B/1D receptor agonist; causes vasoconstriction of cranial blood vessels and inhibits release of pro-inflammatory neuropeptides.

What the body does with it

Metabolism	Hepatic via monoamine oxidase (MAO-A); some CYP450 involvement (CYP1A2, CYP3A4 minor).
Excretion	Primarily renal (60% as unchanged drug and metabolites, 40% via feces); approximately 20% unchanged in urine. Minor biliary excretion.
Half-life	Terminal elimination half-life: approximately 2 hours (range 1–4 hours). Clinical context: Short half-life supports use for acute migraine attacks; no accumulation with standard dosing.
Protein binding	14–21% (low binding; primarily to albumin and alpha1-acid glycoprotein).
Volume of Distribution	2.4 L/kg (range 2.0–3.0 L/kg). Indicates extensive extravascular distribution, crossing blood-brain barrier to reach central 5-HT1 receptors.
Bioavailability	Subcutaneous: 96% (complete); Oral: 15% (low due to first-pass metabolism); Intranasal: 15–17% (relative to SC); Rectal (suppository): ~20%.
Onset of Action	Subcutaneous injection: 10–15 minutes; Oral tablet: 30–60 minutes; Intranasal: 15–30 minutes.
Duration of Action	Subcutaneous: up to 2 hours (may extend to 4 hours with headache recurrence); Oral: 2–4 hours; Intranasal: 2–4 hours. Recurrence common within 24 hours.

Classification & Brands

Dosing & administration

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment required for GFR ≥15 mL/min. For GFR <15 mL/min, triptans are generally avoided; hemodialysis does not remove sumatriptan.
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh Class C). In mild to moderate impairment, no dose adjustment recommended; use with caution.
Pediatric use	Adolescents aged 12-17: 10 mg intranasally as a single dose; may repeat once after 2 hours if needed, max 20 mg/day. Pediatric use <12 years not established.
Geriatric use	Elderly patients have increased risk of coronary artery disease; contraindicated if CAD or other vascular disease suspected. Start at low end of dosing range; monitor for adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other 5-HT1 agonists and MAOIs can have additive effects Contraindicated in ischemic heart disease and uncontrolled hypertension.

FDA category	Contraindicated
Breastfeeding	Excreted in breast milk; M/P ratio 2.1:1. Limited infant exposure; consider avoiding breastfeeding for 12 hours post-dose. Monitor infant for irritability, sleep disturbance.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show increased fetal abnormalities (e.g., omphalocele, cranioschisis) at high doses. Second/third trimesters: No well-controlled studies; potential for uterine hypertonus and reduced placental perfusion; use only if benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Not recommended for use within 24 hours of another 5-HT1 agonist or ergotamine-containing medication due to risk of coronary vasospasm.

Side Effect Profile

Common Effects	Chest pain
Serious Effects