Version May 2024
Dosage guidance:
Safety: Triptans should not be used within 24 hours of the use of an ergotamine preparation or a different triptan (Ref).
Cluster headache, acute: Note: As monotherapy or in combination with 100% oxygen. Some experts recommend initial treatment with only 100% oxygen if available (Ref). Limit use to <10 days per month to avoid medication-overuse headache (Ref).
SUBQ (preferred route): Initial: 6 mg once; a lower dose of 3 mg may be effective in select patients (Gregor 2005). If initial dose was effective but headache recurs, may repeat a dose (usually same as first dose) after ≥1 hour; some experts recommend waiting ≥2 hours before repeating a dose (Ref). Maximum dose: 6 mg per dose; 12 mg in 24 hours.
Intranasal (alternative route) (off-label): Solution: Initial: 20 mg once in single nostril contralateral to side of headache (Ref). If initial dose was effective but headache recurs, may repeat the dose after ≥2 hours. Maximum dose: 40 mg in 24 hours.
Note: When treating acute cluster headache, following initiation of medication(s) for prevention of cluster headaches, patients with ≥2 headaches per day may temporarily receive >2 doses of sumatriptan per day (either SubQ or intranasal at usual dose and interval) until prophylaxis becomes effective, according to some experts (Ref).
Cyclic vomiting syndrome (migraine associated), abortive therapy (off-label use): Note: To be administered during the prodrome or shortly after vomiting begins (eg, within 30 to 45 minutes); may be used alone for relatively mild or infrequent episodes. If symptoms are frequent or severe, may be used in conjunction with ongoing prophylactic therapy (Ref).
Intranasal: 20 mg; may repeat after 2 hours in patients with no or partial response (maximum: 6 doses/week) (Ref).
SUBQ: 6 mg; may repeat after 1 hour in patients with no or partial response (maximum: 6 doses/week) (Ref).
Migraine, moderate to severe, acute treatment:
Note: Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment. Some experts recommend a large initial dose, as it may be more effective than multiple smaller doses. When attack is complicated by vomiting or severe nausea, a nonoral preparation may be more effective. Limit use to <10 days per month to avoid medication-overuse headache (Ref).
Oral: 50 to 100 mg as a single dose (Ref). If symptoms persist or return, may repeat dose (usually same as first dose) after ≥2 hours. Maximum dose: 100 mg/dose; 200 mg per 24 hours.
Intranasal:
Solution: Usual: 20 mg as a single dose in 1 nostril; if symptoms persist or return, may repeat dose after ≥2 hours. Maximum dose: 40 mg per 24 hours.
Powder, breath-activated: 22 mg as a single dose; using product-specific device, give as one 11 mg capsule insufflated in each nostril. If symptoms persist or return, may repeat dose after ≥2 hours. Maximum dose: 44 mg per 24 hours. Refer to product-specific administration instructions.
Spray: 10 mg as a single dose in 1 nostril. If symptoms persist or return, may repeat dose after ≥1 hour. Maximum dose: 30 mg per 24 hours. May also administer at least 1 hour following a dose of another sumatriptan product (use following another 5-HT1 agonist is contraindicated).
SUBQ: Usual: 6 mg once. If symptoms persist or return, may repeat dose (usually same as first dose) after ≥1 hour. If 6 mg was not tolerated, subsequent doses of 1 to 5 mg may provide sufficient relief with better tolerability. Maximum dose: 6 mg/dose; 12 mg per 24 hours.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Note: No data exist regarding the pharmacokinetic disposition of sumatriptan in kidney impairment (Ref). The following recommendations are extrapolated from pharmacokinetic studies in patients with normal kidney function.
Oral, intranasal, SUBQ:
Altered kidney function: No dosage adjustment necessary for any degree of kidney impairment [renal clearance accounts for only 20% of total clearance (Ref)] (Ref).
Augmented renal clearance (measured urinary CrCl ≥130 mL/minute/1.73 m 2 ): Augmented renal clearance (ARC) is a condition that occurs in certain critically ill patients without organ dysfunction and with normal serum creatinine concentrations. Young patients (<55 years of age) admitted post trauma or major surgery are at highest risk for ARC, as well as those with sepsis, burns, or hematologic malignancies. An 8- to 24-hour measured urinary CrCl is necessary to identify these patients (Ref).
No dosage adjustment necessary (Ref).
Hemodialysis, intermittent (thrice weekly): Unlikely to be significantly dialyzed (large Vd): No supplemental dose or dosage adjustment necessary (Ref).
Peritoneal dialysis: Unlikely to be significantly dialyzed (large Vd): No dosage adjustment necessary (Ref).
CRRT: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): No dosage adjustment necessary (Ref).
Mild to moderate hepatic impairment:
Oral: Bioavailability of oral sumatriptan is increased with liver disease. If treatment is needed, do not exceed single doses of 50 mg.
Intranasal: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, dosage adjustment not expected due to extensive non-hepatic metabolism to inactive agents.
SUBQ: No dosage adjustment necessary.
Severe hepatic impairment: Oral, intranasal, and subcutaneous (Imitrex and Zembrace injection) formulations are contraindicated in severe hepatic impairment.
Refer to adult dosing.
(For additional information see "Sumatriptan: Pediatric drug information")
Migraine: Limited data available: Note: Results of clinical studies are mixed with regards to efficacy, particularly with oral and SUBQ sumatriptan doses.
Intranasal:
Children 5 to 12 years: Intranasal: 5 mg, 10 mg, or 20 mg administered in one nostril as a single dose as soon as possible after the onset of migraine; dose should be selected on an individual basis. A double-blind, placebo-controlled study of 129 patients (mean age: 12.4 years; range: 8 to 17 years) used a weight-based dosing regimen: Body weight: 20 to 39 kg: 10 mg/dose; body weight ≥40 kg: 20 mg/dose; however, relatively few children <12 years of age were included in the study (Ref). A small, randomized, double-blind, placebo-controlled study of 14 children (age range: 6 to 9 years; median: 8.2 years) used intranasal doses of 20 mg/dose (Ref). A small, retrospective review of 10 children (age range: 5 to 12 years; mean: 9.9 years) used intranasal doses of 5 mg (n=2) or 20 mg (n=8) (Ref).
Children ≥12 years and Adolescents: Intranasal: 10 mg or 20 mg administered in one nostril as a single dose as soon as possible after the onset of migraine; a lower dose of 5 mg as a single dose may also be effective; dose should be selected on an individual basis (Ref).
Oral:
Note: According to the manufacturer, efficacy of oral sumatriptan monotherapy was not established in five controlled trials in adolescent patients; frequency of adverse events was dose-related and age-dependent (ie, younger patients reported more adverse events). Guidelines do not recommend oral sumatriptan alone due to very low confidence in efficacy; however, the combination product of sumatriptan and naproxen is recommended in patients ≥12 years of age (Ref).
Children ≥10 years and Adolescents: Oral: 25 mg or 50 mg as a single dose administered within 30 minutes of headache onset. There was no statistically significant improvement in pain relief at 2 hours; however, some improvement was noted (Ref).
SUBQ:
Children ≥6 years and Adolescents: SUBQ: 3 to 6 mg as a single dose. An open-label prospective trial of 17 children 6 to 16 years with juvenile migraine used SUBQ doses of 6 mg in 15 patients weighing 30 to 70 kg, and 3 mg/dose in two children weighing 22 kg and 30 kg (Ref). Another open-label prospective trial in 50 consecutive children (ages 6 to 18 years) with severe migraine used SUBQ doses of 0.06 mg/kg/dose. Relief was reported as good/excellent in 84% of the patients; 16% reported fair to poor relief; additional studies are needed (Ref).
Cyclic vomiting syndrome (CVS), abortive therapy: Limited data available:
Note: Based on efficacy data in adolescents and extrapolation from migraine efficacy in children, sumatriptan could be considered for treatment in children <12 years of age with refractory CVS using migraine treatment doses. Dosing for individuals ≥12 years of age is below; for dosing in younger children, refer to Migraine dosing (Ref).
Intranasal: Nasal solution: Children ≥12 years and Adolescents: Intranasal: 20 mg administered as a single dose in 1 nostril; doses should be administered as soon as possible after the onset of prodromal symptoms. If there is no response or partial response to the first dose, may consider repeating after 1 to 2 hours. (Ref).
SUBQ: Adolescents: SUBQ: 3 to 6 mg as a single dose; doses should be administered as soon as possible after the onset of prodromal symptoms. If there is no response or partial response to the first dose, some experts recommend repeating after 1 to 2 hours (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, dosage adjustment not expected due to extensive metabolism to inactive agents.
The following is based on adult data (Ref):
Mild to moderate hepatic impairment:
Intranasal: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, because the intranasally administered drug does not undergo first-pass metabolism, serum concentrations would not be expected to be altered.
Oral: Bioavailability of oral sumatriptan is increased with liver disease. In adults, the maximum dose should not exceed 50 mg.
SUBQ: No dosage adjustment necessary; has been studied and pharmacokinetics were not altered in patients with hepatic impairment compared to healthy patients.
Severe hepatic impairment: Oral, nasal, and SUBQ (Imitrex and Zembrace injection) formulations are contraindicated with severe hepatic impairment.
Prolonged QT interval on ECG and subsequent ventricular arrhythmias, including torsades de pointes (TdP) and ventricular fibrillation leading to death, have been reported with sumatriptan, most commonly in the presence of additional risk factors (Ref). In contrast, postmarketing studies have found no association between triptan use and ventricular arrhythmias (Ref).
Onset: Rapid; occurred within 1 hour of administration (Ref)
Risk factors:
Drug-induced QTc prolongation/TdP (in general):
• Females (Ref)
• Age >65 years (Ref)
• Structural heart disease (eg, history of myocardial infarction or heart failure with reduced ejection fraction) (Ref)
• History of drug-induced TdP (Ref)
• Genetic defects of cardiac ion channels (Ref)
• Congenital long QT syndrome (Ref)
• History of drug-induced TdP (Ref)
• Baseline QT interval prolongation (eg, >500 msec) or lengthening of the QTc by ≥60 msec (Ref)
• Electrolyte disturbances (eg, hypocalcemia, hypokalemia, hypomagnesemia) (Ref)
• Bradycardia (Ref)
• Hepatic impairment (Ref)
• Kidney impairment (Ref)
• Loop diuretic use (Ref)
• Sepsis (Ref)
• Concurrent administration of multiple medications (≥2) that prolong the QT interval or increase drug interactions that increase serum drug concentrations of QT prolonging medications (Ref)
Coronary artery vasospasm, transient ischemia, acute myocardial infarction (MI), Takotsubo cardiomyopathy, cardiac arrest, and death have been reported with 5-HT1 agonist administration, including sumatriptan in adult and pediatric patients (Ref). Increased blood pressure, including hypertensive crisis, has been reported on rare occasions in patients with and without a history of hypertension. In contrast, postmarketing studies have found no association between triptan use and MI or non-MI ischemic heart disease (Ref). The American Headache Society's consensus statement on the cardiovascular safety profile of triptans noted the safety of this drug class in patients with migraines without known or clinically suspected coronary artery disease (Ref).
Mechanism: Dose-related; related to the pharmacologic action (ie, vasoconstriction). Binds to 5-HT1B receptors in coronary arteries and has been shown to narrow human coronary arteries in vivo by 10% to 20% during angiography (Ref). At therapeutic doses, triptans, which are 5-HT1B/1D agonists, have minimal potential to cause significant constriction of nondiseased arteries (Ref). For chest symptoms, nonischemic mechanisms are hypothesized, including direct effect on the pulmonary vasculature, alterations in skeletal muscle energy metabolism and heightened sensory sensitivity during a migraine attack (Ref).
Onset: Rapid; symptoms of acute myocardial infarction developed between 10 to 180 minutes (median 15 minutes) in patients taking sumatriptan subcutaneously and from 30 to 60 minutes (median 60 minutes) following oral administration (Ref). Onset of chest symptoms was generally 5 to 30 minutes (Ref).
Risk factors:
• Risk factors for coronary artery disease (CAD) (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) (Ref)
Hemorrhagic stroke (including subarachnoid hemorrhage) and ischemic stroke have been reported in adult and pediatric patients (Ref). A study of FDA adverse event reports indicated that there may be a significant, although rare, risk of severe ischemic cerebrovascular events in patients on triptans (Ref). In contrast, several cohort studies have not found an association between triptan use and stroke or transient ischemic attacks (Ref). Since migraine is an independent risk factor for stroke (Ref), it is challenging to define the role of triptans in precipitating stroke.
Mechanism: Dose-related; related to the pharmacologic action (ie, vasoconstriction) (Ref).
Onset: Rapid; generally occurs within 24 hours (Ref) and may present as quickly as 4 minutes after SubQ injection (Ref).
Risk factors:
• Migraine (independent risk factor for stroke) (Ref)
• Smoking (Ref)
• Use of estrogen-based oral contraceptives (Ref)
• Young females (Ref)
CNS depression, such as dizziness, asthenia, or drowsiness, which may impair physical or mental abilities, have been reported (Ref). Other CNS effects, including abnormal dreams, agitation, ataxia, confusion, tremor, and vertigo, may occur (Ref). Analysis of double-blind, placebo-controlled trials suggest that CNS adverse reactions, such as drowsiness and asthenia, may be related to unmasking of CNS symptoms associated with resolution of the migraine attack rather than representing drug-related adverse reactions (Ref). There are also reports of akathisia, acute dystonia, and pathological laughter associated with use (Ref).
Mechanism: Dose-related; related to pharmacologic action. Despite the hydrophilicity of sumatriptan, it has been shown to cross the blood-brain barrier and penetrate the CNS causing pharmacological effects (Ref).
Onset: Rapid; akathisia has been reported to occur within 5 to 10 minutes of SubQ administration (Ref). Dystonia has been reported to occur within 15 to 60 minutes of oral administration (Ref).
Risk factors:
• Dose (Ref)
• Lipophilicity (almotriptan 12.5 mg, naratriptan 2.5 mg, and sumatriptan 50 mg with the lowest incidence and eletriptan 40 and 80 mg, rizatriptan 10 mg, and zolmitriptan 2.5 and 5 mg with the highest incidence) (Ref); however, other studies have not shown a correlation (Ref)
Transient and permanent blindness and significant partial vision loss have been reported with use in adult and pediatric patients. Since visual disorders may be part of a migraine attack, a causal relationship between these events and the use of 5-HT1 agonists has not been clearly established. Other ocular effects include accommodation disorders, conjunctivitis, disorders of sclera, external ocular muscle disorders, eye edema and swelling, eye hemorrhage, eye itching, eye pain, keratitis, mydriasis, and visual disturbances. Other reported ocular effects include ischemic optic neuropathy (Ref), oculomotor nerve paralysis resulting in double vision and ptosis (Ref), recurrent paresis of the superior division of the oculomotor nerve (Ref), and bilateral angle-closure glaucoma (Ref).
Mechanism: Dose-related; ischemic ocular effects may be related to the pharmacologic action (ie, vasoconstriction) (Ref). Acute intraocular pressure elevation: Unknown; however, serotonin may play a role (Ref).
Onset: Bilateral angle-closure glaucoma: Rapid; occurred within 1 week of 1 dose (Ref).
Peripheral ischemia, reversible cerebral vasoconstriction syndrome (RCVS), ischemic colitis, splenic infarction, and Raynaud's disease have been reported with 5-HT1 agonists (Ref). In a review of drug-induced Raynaud syndrome, triptans were not identified as a cause (Ref).
Mechanism: RCVS: Unknown; may be caused by transient dysregulation of cerebral vascular autonomic regulation mechanism resulting in multifocal vasoconstriction (Ref).
Onset: Varied; median onset of 2 days in case reports of ischemic colitis (Ref) to onset of 6 months in a case report of cerebral vasospasm (Ref). In one review, serious vascular adverse events occurred after the first administration in 5 patients, after 2 to 4 administrations in 5 patients and after months or years in 15 patients (Ref).
Risk factors:
• Concurrent use of drugs, such as dihydroergotamine, methysergide, and selective serotonin reuptake inhibitors (Ref).
Serotonin syndrome may occur, particularly when used concomitantly with other serotonergic drugs. Serotonin syndrome occurs primarily through activation of 5-HT2A receptors, although 5-HT1A receptors may also play a role. Triptans are serotonin agonists with weak affinity for the 5-HT1A subtype and no activity at 5-HT2 (Ref). Since triptans have no activity at the 5-HT2 receptors, they theoretically should not cause serotonin syndrome (Ref); however, animal models have suggested that repeated exposure to triptans, including overdose, may induce serotonin syndrome via upregulation of serotonin synthesis (Ref). Onset typically occurs minutes to hours after initiation, dose increase, or addition of a serotonergic drug (Ref). Risk factors may include concomitant use of other serotonergic drugs, including selective serotonin reuptake inhibitors or selective norepinephrine reuptake inhibitors antidepressants; however, literature is conflicting (Ref). Concomitant use of opioids may also increase risk (Ref).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
Injection:
>10%:
Local: Injection-site reaction (30% to 59%; including bleeding at injection site, bruising at injection site, burning sensation at injection site, erythema at injection site, pain at injection site, swelling at injection site, warm sensation at injection site)
Nervous system: Dizziness (≤12%) (table 1), feeling hot (≤11%), tingling sensation (14%), vertigo (≤12%) (table 2)
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|---|---|
|
12% |
4% |
6 mg |
SUBQ |
Migraine |
547 |
370 |
Defined as dizziness/vertigo |
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|---|---|
|
12% |
4% |
6 mg |
SUBQ |
Migraine |
547 |
370 |
Defined as dizziness/vertigo |
1% to 10%:
Cardiovascular: Chest discomfort (5%), chest pressure (2%), chest tightness (3%), flushing (7%)
Dermatologic: Diaphoresis (2%)
Gastrointestinal: Nausea and vomiting (4%)
Local: Local discomfort (jaw or throat: 2% to 3%)
Nervous system: Asthenia (5%) (table 3), burning sensation (7%), drowsiness (≤3%) (table 4), feeling of heaviness (7%), headache (2%), numbness (5%), paresthesia (5%), sedated state (≤3%), sensation of pressure (7%), sensation of tightness (5%), strange feeling (2%), tight feeling in the head (2%)
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|
|
5% |
<1% |
6 mg |
SUBQ |
Migraine |
547 |
370 |
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|---|---|
|
3% |
2% |
6 mg |
SUBQ |
Migraine |
547 |
370 |
Defined as drowsiness/sedation |
Neuromuscular & skeletal: Myalgia (2%), neck pain (≤5%), neck stiffness (≤5%)
Respiratory: Bronchospasm (1%), nasal discomfort (nasal cavity: ≤2%), sinus discomfort (≤2%)
Nasal:
>10%:
Gastrointestinal: Dysgeusia (≤25%), nausea (≤14%), vomiting (≤14%)
Nervous system: Unusual taste (≤25%)
Respiratory: Nasal discomfort (≤11%)
1% to 10%:
Local: Local irritation (≤5%), localized burning (1%), localized numbness (≤5%)
Nervous system: Dizziness (≤2%) (table 5), paresthesia (≤5%), vertigo (≤2%) (table 6)
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|---|---|
|
2% |
0.9% |
10 mg |
Nasal spray |
Migraine |
1,007 |
704 |
Defined as dizziness/vertigo |
|
1% |
0.9% |
5 mg |
Nasal spray |
Migraine |
496 |
704 |
Defined as dizziness/vertigo |
|
1% |
0.9% |
20 mg |
Nasal spray |
Migraine |
1,212 |
704 |
Defined as dizziness/vertigo |
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
Comments |
|---|---|---|---|---|---|---|---|
|
2% |
0.9% |
10 mg |
Nasal spray |
Migraine |
1,007 |
704 |
Defined as dizziness/vertigo |
|
1% |
0.9% |
5 mg |
Nasal spray |
Migraine |
496 |
704 |
Defined as dizziness/vertigo |
|
1% |
0.9% |
20 mg |
Nasal spray |
Migraine |
1,212 |
704 |
Defined as dizziness/vertigo |
Respiratory: Nasal cavity pain (≤5%), rhinitis (2%), rhinorrhea (≤5%), sinus discomfort (≤4%), sore nose (≤5%)
Tablet:
1% to 10%:
Cardiovascular: Chest pain (≤2%), chest pressure (≤2%), chest tightness (≤2%), hot and cold flashes (3%)
Gastrointestinal: Sore throat (≤3%)
Local: Local pain (2%)
Nervous system: Fatigue (≤3%), feeling of heaviness (≤3%), heaviness of chest (≤2%), malaise (≤3%), pain (≤8%), paresthesia (3% to 5%), sensation of pressure (≤8%), sensation of tightness (≤3%), vertigo (2%) (table 7)
|
Drug ( Sumatriptan ) |
Placebo |
Dose |
Dosage Form |
Indication |
Number of Patients ( Sumatriptan ) |
Number of Patients (Placebo) |
|---|---|---|---|---|---|---|
|
2% |
<1% |
100 mg |
Tablet |
Migraine |
437 |
309 |
|
<1% |
<1% |
50 mg |
Tablet |
Migraine |
771 |
309 |
|
<1% |
<1% |
25 mg |
Tablet |
Migraine |
417 |
309 |
Neuromuscular & skeletal: Jaw pain (≤3%), jaw pressure (≤3%), jaw tightness (≤3%), neck pain (≤3%)
Respiratory: Pharyngeal edema (≤3%)
Postmarketing (any route):
Cardiovascular: Acute myocardial infarction (Chalaupka 2009), cardiomyopathy (takotsubo) (Mohan 2019), coronary artery vasospasm (Stricker 1992), hypertensive crisis, increased blood pressure, myocarditis (eosinophilic) (Al Ali 2006), palpitations, peripheral ischemia, prolonged QT interval on ECG (Stillman 2013), Raynaud disease, torsades de pointes (Stillman 2013), ventricular fibrillation (Laine 1999)
Dermatologic: Urticaria (Pradalier 1996)
Gastrointestinal: Ischemic colitis (Nguyen 2014)
Hematologic & oncologic: Splenic infarction (Arora 2006)
Hypersensitivity: Anaphylaxis (Lee 2020), angioedema (Dachs 1995), nonimmune anaphylaxis
Nervous system: Akathisia (López-Alemany 1997), cerebellar infarction (Jayamaha 1995), dystonia (Singhal 2002), heaviness in neck (includes jaw or throat), hemorrhagic stroke (Combremont 2001), ischemic stroke (Gazioglu 2012), reversible cerebral vasoconstriction syndrome (Kato 2016), seizure (Kumlien 2010), subarachnoid hemorrhage (Pfadenhauer 2006), tremor
Neuromuscular & skeletal: Neck pressure, neck tightness
Ophthalmic: Angle-closure glaucoma (Hsu 2017), blindness, oculomotor nerve paralysis (Novistkaya 2017), optic neuropathy (Chiari 1994), vision loss (partial) (Novistkaya 2017)
Respiratory: Epistaxis
Hypersensitivity (eg, angioedema, anaphylaxis) to sumatriptan or any component of the formulation; ischemic heart disease or signs or symptoms of ischemic heart disease (coronary artery vasospasm, Prinzmetal angina, angina pectoris, MI, silent myocardial ischemia); history of cerebrovascular syndromes (including strokes, transient ischemic attacks), history of hemiplegic or basilar migraine; peripheral vascular disease (including ischemic bowel disease); uncontrolled hypertension; use within 24 hours of ergotamine derivatives; use within 24 hours of another 5-HT1 agonist; concurrent administration or within 2 weeks of discontinuing an MAO type A inhibitors; Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders; severe hepatic impairment.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in the US labeling): Valvular heart disease; significant underlying cardiovascular disease (eg, atherosclerotic disease, congenital heart disease); ophthalmoplegic migraine.
Disease-related concerns:
• Hepatic impairment: Use oral formulations of sumatriptan with caution (and with dosage limitations) in patients with mild to moderate hepatic impairment where treatment is necessary and advisable. Presystemic clearance of orally administered sumatriptan is reduced in hepatic impairment, leading to increased plasma concentrations; dosage reduction of the oral product is recommended. Non-oral routes of administration (intranasal, subcutaneous) do not undergo similar hepatic first-pass metabolism and are not expected to result in significantly altered pharmacokinetics in patients with hepatic impairment. Use of the oral, intranasal, Imitrex, and Zembrace injectable is contraindicated in severe hepatic impairment.
• Seizure disorders: Use with caution in patients with history of seizure disorder or in patients with a lowered seizure threshold; seizures have been reported after sumatriptan administration in patients with or without a history of seizures.
Special populations:
• Older adult: Use with caution; perform a cardiovascular evaluation prior to initiation of therapy in older adult patients with cardiovascular risk factors (eg, diabetes, hypertension, smoking, obesity, strong family history of coronary artery disease) and periodically during intermittent long-term use.
Dosage form specific issues:
• Latex: The packaging (needle cover of prefilled syringe) may contain dry natural rubber, which is a derivative of latex.
Other warnings/precautions:
• Appropriate use: Only indicated for the acute treatment of migraine or cluster headache (depending on product); not indicated for migraine or cluster headache prophylaxis, or for the treatment of hemiplegic or basilar migraine. Acute migraine agents (eg, 5-HT1 agonists, opioids, ergotamine, or a combination of the agents) used for 10 or more days per month may lead to worsening of headaches (medication overuse headache); withdrawal treatment may be necessary in the setting of overuse. If a patient does not respond to the first dose, the diagnosis of migraine or cluster headache should be reconsidered; rule out underlying neurologic disease in patients with atypical headache and in patients with no prior history of migraine or cluster headache.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Exhaler Powder, Nasal, as succinate [strength expressed as base]:
Onzetra Xsail: 11 mg per nosepiece (2 ea)
Solution, Nasal:
Imitrex: 5 mg/actuation (1 ea [DSC]); 20 mg/actuation (1 ea [DSC])
Tosymra: 10 mg/actuation (1 ea)
Generic: 5 mg/actuation (1 ea); 20 mg/actuation (1 ea)
Solution, Subcutaneous, as succinate [strength expressed as base]:
Generic: 6 mg/0.5 mL (0.5 mL)
Solution, Subcutaneous, as succinate [strength expressed as base, preservative free]:
Imitrex: 6 mg/0.5 mL (0.5 mL)
Generic: 6 mg/0.5 mL (0.5 mL)
Solution Auto-injector, Subcutaneous, as succinate [strength expressed as base]:
Zembrace SymTouch: 3 mg/0.5 mL (0.5 mL)
Generic: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Solution Auto-injector, Subcutaneous, as succinate [strength expressed as base, preservative free]:
Imitrex STATdose System: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Zembrace SymTouch: 3 mg/0.5 mL (0.5 mL)
Generic: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Solution Cartridge, Subcutaneous, as succinate [strength expressed as base]:
Generic: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Solution Cartridge, Subcutaneous, as succinate [strength expressed as base, preservative free]:
Imitrex STATdose Refill: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Generic: 4 mg/0.5 mL (0.5 mL [DSC]); 6 mg/0.5 mL (0.5 mL [DSC])
Solution Prefilled Syringe, Subcutaneous, as succinate [strength expressed as base, preservative free]:
Generic: 6 mg/0.5 mL (0.5 mL [DSC])
Tablet, Oral, as succinate [strength expressed as base]:
Imitrex: 25 mg, 50 mg, 100 mg
Generic: 25 mg, 50 mg, 100 mg
May be product dependent
Exhaler Powder (Onzetra Xsail Nasal)
11MG/NOSEPC (per each): $70.50
Solution (SUMAtriptan Nasal)
5 mg/ACT (per each): $59.04 - $81.33
20 mg/ACT (per each): $42.80 - $81.33
Solution (SUMAtriptan Succinate Subcutaneous)
6 mg/0.5 mL (per 0.5 mL): $13.20 - $85.00
Solution (Tosymra Nasal)
10 mg/ACT (per each): $117.00
Solution Auto-injector (Imitrex STATdose System Subcutaneous)
4 mg/0.5 mL (per 0.5 mL): $289.51
6 mg/0.5 mL (per 0.5 mL): $289.51
Solution Auto-injector (SUMAtriptan Succinate Subcutaneous)
4 mg/0.5 mL (per 0.5 mL): $107.36 - $187.03
6 mg/0.5 mL (per 0.5 mL): $92.20 - $112.51
Solution Auto-injector (Zembrace SymTouch Subcutaneous)
3 mg/0.5 mL (per 0.5 mL): $207.37
Solution Cartridge (Imitrex STATdose Refill Subcutaneous)
4 mg/0.5 mL (per 0.5 mL): $274.20
6 mg/0.5 mL (per 0.5 mL): $274.20
Tablets (Imitrex Oral)
25 mg (per each): $41.68
50 mg (per each): $90.86
100 mg (per each): $90.86
Tablets (SUMAtriptan Succinate Oral)
25 mg (per each): $23.72 - $28.25
50 mg (per each): $25.14
100 mg (per each): $25.14
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Nasal:
Imitrex: 5 mg/actuation (1 ea); 20 mg/actuation (1 ea)
Solution, Subcutaneous, as succinate [strength expressed as base]:
Generic: 6 mg/0.5 mL (0.5 mL)
Solution Auto-injector, Subcutaneous, as succinate [strength expressed as base]:
Imitrex: 6 mg/0.5 mL (0.5 mL)
Tablet, Oral, as succinate [strength expressed as base]:
Imitrex DF: 50 mg, 100 mg
Generic: 25 mg, 50 mg, 100 mg
Administer as soon as symptoms appear.
Intranasal:
Powder: For intranasal administration with the Xsail device only. Remove the clear device cap from the reusable delivery device; remove one 11 mg disposable nosepiece from the foil pouch and click into the device body. Prior to administration, pierce the capsule inside the nosepiece by pressing and releasing the white piercing button one time on the device body. Insert the nosepiece into one nostril so there is a tight seal; rotate the device to place the mouthpiece in the mouth. Blowing forcefully through the mouthpiece for 2 to 3 seconds will deliver the powder into the nasal cavity; vibration may occur. Do not press white button while blowing into mouthpiece. Once administered into the first nostril, remove and discard nosepiece; repeat same process using a second 11 mg nosepiece into the other nostril to administer the remainder of the 22 mg dose.
Solution: Each nasal spray unit is preloaded with 1 dose; do not test the spray unit before use; remove unit from plastic pack when ready to use; while sitting down, gently blow nose to clear nasal passages; keep head upright and close one nostril gently with index finger; hold container with other hand, with thumb supporting bottom and index and middle fingers on either side of nozzle; insert nozzle into nostril about 1/2 inch; close mouth; take a breath through nose while releasing spray into nostril by pressing firmly on blue plunger; remove nozzle from nostril; keep head level for 10 to 20 seconds and gently breathe in through nose and out through mouth; do not breathe deeply.
Spray: Each nasal spray unit is preloaded with 1 dose; do not test the spray unit before use; remove unit from plastic pack when ready to use; while sitting down, gently blow nose to clear nasal passages; keep head upright and close one nostril gently with index finger; hold container with other hand, with thumb supporting bottom and index and middle fingers on either side of nozzle; insert half of the spray nozzle into nostril and angle outward; tilt head back slightly and breath slowly through nose while releasing spray into nostril by pressing firmly on plunger; remove nozzle from nostril; keep head level for 10 to 20 seconds and gently breathe in through nose and out through mouth; do not breathe deeply.
SUBQ: Not for IM or IV use. Needle penetrates 1/4 inch of skin; use in areas of the body with adequate skin and subcutaneous thickness (lateral thigh or upper arm). In patients receiving doses other than 4 or 6 mg, use the 6 mg single-dose vial instead of the autoinjector device.
Administer as soon as symptoms appear.
Intranasal:
Solution: Each nasal spray unit is preloaded with 1 dose; do not test the spray unit before use; remove unit from plastic pack when ready to use; while sitting down, gently blow nose to clear nasal passages; keep head upright and close one nostril gently with index finger; hold container with other hand, with thumb supporting bottom and index and middle fingers on either side of nozzle; insert nozzle into nostril about 1/2 inch; close mouth; take a breath through nose while releasing spray into nostril by pressing firmly on blue plunger; remove nozzle from nostril; keep head level for 10 to 20 seconds and gently breathe in through nose and out through mouth; do not breathe deeply.
Oral: Administer with water or other fluids; swallow tablet whole; do not split tablet.
SUBQ: Administer SUBQ only; do not administer IM; do not administer IV (may cause coronary vasospasm). Needle penetrates 1/4 inch of skin; use in areas of the body with adequate skin and SUBQ thickness (lateral thigh or upper arm). Do not use the auto-injector device for doses that are not 4 to 6 mg; vials should be used.
Cluster headache, acute: SUBQ (excluding Zembrace): Acute treatment of cluster headache episodes in adults as monotherapy or in combination with 100% oxygen.
Migraine, moderate to severe, acute treatment: Intranasal, Oral, SUBQ: Acute treatment of migraine with or without aura in adults
Cyclic vomiting syndrome (migraine associated), abortive therapy
SUMAtriptan may be confused with SAXagliptin, SITagliptin, somatropin, ZOLMitriptan
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Bromocriptine: May enhance the adverse/toxic effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Management: Consider alternatives to this combination when possible. If combined, monitor for increased bromocriptine and triptan toxicities. Risk D: Consider therapy modification
Droxidopa: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Monoamine Oxidase Inhibitors: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Monoamine Oxidase Inhibitors may increase the serum concentration of Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Serotonergic Agents (High Risk): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of other Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
In a study using full-term, healthy human placentas, limited amounts of sumatriptan were found to cross the placenta (Schenker 1995).
Pregnancy outcome data for sumatriptan are available from a pregnancy registry sponsored by GlaxoSmithKline. As of September 2012, data were available for 617 pregnancies (626 infants/fetuses; 528 with first trimester exposure) exposed to sumatriptan (including 7 pregnancies also exposed to naratriptan). Following sumatriptan exposure, the risk of major birth defects following first trimester exposure was 4.2% and no consistent pattern of birth defects was observed. The pregnancy registry was closed to enrollment in January 2012 (Ephross 2014). Data from the pregnancy registry were compared to data obtained from an insurance claims database. Between 1996 and 2012, the database recorded 3,496 pregnancies with first trimester exposure to sumatriptan. The risk of major birth defects was the same as that observed in the pregnancy registry (4%) (Yusuf 2018).
An analysis of data collected between 1995 and 2008 using the Swedish Medical Birth Register reported pregnancy outcomes following 5-HT1B/1D agonist (triptan) exposure. An increased risk of major congenital malformations was not observed following sumatriptan exposure (2,229 exposed during the first trimester) (Källén 2011). An increased risk of major congenital malformations was also not observed using data collected from a Norwegian pregnancy registry study. This study included 415 women who used sumatriptan during the first trimester of pregnancy between 2004 and 2007 (Nezvalová-Henriksen 2013). A meta-analysis of six studies, most evaluating sumatriptan (including Källén 2011 and Nezvalová-Henriksen 2013), did not find triptan exposure in pregnancy to increase the risk for major congenital malformations, low birth weight, or birth <37 weeks' gestation (Dudman 2022).
Triptans relieve migraine pain by selectively binding to serotonin receptors, resulting in vasoconstriction of cranial arteries. Although the effects on uterine blood flow have not been evaluated, 1 case report suggests excessive use of a triptan may cause placental hypoperfusion (ACOG 2022; Viard 2021).
Treatment for migraine headaches in pregnant patients should be individualized (AHS [Ailani 2021]). Triptans are not the preferred initial treatment for acute migraine headache in pregnant patients (ACOG 2022). If a triptan is needed when first-line therapy is ineffective, sumatriptan may be considered under close supervision. Triptans should be avoided in pregnant patients with cardiac disease or hypertension (ACOG 2022; CHS [Worthington 2013]; EHF [Steiner 2019]).
Acute treatment of cluster headache in pregnant patients is similar to nonpregnant adults; however, if effective, use of sumatriptan nasal spray may be preferred over SUBQ to limit systemic exposure (AHS [Robbins 2016]; Bjørk 2021; Schindler 2022).
Sumatriptan is present in breast milk.
Data related to the presence of sumatriptan in breast milk are available from 2 studies.
• Sumatriptan 6 mg SUBQ was administered as a single dose to 5 women (mean duration of lactation 22.2 weeks) and milk concentrations were measured over 8 hours. The mean maximum concentration of sumatriptan in breast milk was 87.2 mcg/L (range: 61.9 to 112.5 mcg/L). The median half-life in breast milk was 2.2 hours and the maximum milk concentrations occurred between 1.7 and 3.5 hours after the maternal dose. Using the cumulative excretion of sumatriptan, authors of the study calculated the relative infant dose (RID) of sumatriptan to be 3.5% of the weight-adjusted maternal dose (Wojnar-Horton 1996).
• A study of 19 lactating women (6 weeks to 30 months postpartum) treated for migraine headaches included 7 patients taking sumatriptan SUBQ (n=1), nasal spray (n=1), or tablet (n=4), and 1 woman who used both the nasal spray and tablet. During the study, infants were fed previously expressed breast milk. Breast milk was sampled prior to and at intervals up to 24 hours after the dose. Using the average breast milk concentration observed, authors of the study calculated the estimated exposure to the breastfed infant to be 1.7 mcg/kg/day, providing a RID of 1.8% based on a maternal dose of sumatriptan 6 mg SUBQ. Following maternal use of the sumatriptan 20 mg nasal spray (n=2), the estimated exposure to the breastfed infant was calculated to be 1.2 to 1.5 mcg/kg/day (RID 0.4%). Following administration of a sumatriptan 50 mg tablet (n=4), the estimated exposure to the breastfed infant varied between 1.6 to 7.6 mcg/kg/day (RID 0.2% to 1.4%); the estimated exposure to the breastfeeding infant following sumatriptan 100 mg tablet (n=1) was 6.3 mcg/kg/day (RID 0.4%). When calculations were based on maximum breast milk concentrations, the RID for sumatriptan was 0.8% to 3.8%. A large interindividual variability among breast milk concentrations was found with all the triptans in the study, even when considering dose and dosage form (Amundsen 2021).
• In general, breastfeeding is considered acceptable when the RID is <10% (Anderson 2016; Ito 2000).
Treatment for migraine headaches in lactating patients should be individualized (AHS [Ailani 2021]). According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Withholding breastfeeding for 8 to 12 hours after the maternal dose will minimize infant exposure via breast milk. In addition, the poor oral bioavailability of sumatriptan will limit absorption. The decision to withhold breastfeeding following a dose of sumatriptan should be part of a shared decision-making process (ACOG 2022).
Headache severity, mental alertness, BP; signs/symptoms of serotonin syndrome such as mental status changes (eg, agitation, hallucinations, delirium, coma), autonomic instability (eg, tachycardia, labile BP, diaphoresis), neuromuscular changes (eg, tremor, rigidity, myoclonus), GI symptoms (eg, nausea, vomiting, diarrhea), and/or seizures; signs/symptoms suggestive of angina; perform a cardiovascular evaluation prior to initiation of therapy in 5-HT1 agonist-naive patients who have multiple cardiovascular risk factors (eg, increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD); monitor ECG with first dose in patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation and consider periodic cardiovascular evaluation in such patients during intermittent long-term use; in patients with sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing, evaluate for coronary artery disease or Prinzmetal angina prior to additional doses (if dosing resumed and symptoms recur, monitor with ECG).
Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) on intracranial blood vessels and sensory nerves of the trigeminal system; causes vasoconstriction and reduces neurogenic inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Onset of action: Oral: ~30 minutes; Intranasal: ~15 to 30 minutes; SUBQ: ~10 minutes; Peak effect: Oral: 2 to 4 hours.
Distribution: Vd (central): SUBQ: 50 L; Vd (apparent): Oral, Intranasal: 2.7 L/kg.
Protein binding: 14% to 21%.
Metabolism: Hepatic to an indole acetic acid metabolite (inactive) which then undergoes ester glucuronide conjugation; may be metabolized by monoamine oxidase (MAO); extensive first-pass metabolism following oral administration.
Bioavailability: Intranasal: Solution 17% (compared to SUBQ), Powder 19% (compared to SUBQ), Spray 58% to 87% (compared to SUBQ); Oral: 15%; SUBQ: 97% ± 16%.
Half-life elimination: Distribution: 15 minutes; Terminal: 2 hours; range: 1 to 4 hours.
Time to peak, serum: Oral: 2 to 2.5 hours; Intranasal: Powder: ~45 minutes; Spray: Median 10 minutes (range: 5 to 23 minutes); SUBQ: 12 minutes (range: 4 to 20 minutes).
Excretion:
Intranasal: Urine (42% of total dose as indole acetic acid metabolite; 3% of total dose as unchanged drug).
Oral: Urine (~60% of total dose, mostly as indole acetic acid metabolite; 3% of total dose as unchanged drug); feces (~40%).
SUBQ: Urine (38% of total dose as indole acetic acid metabolite; 22% of total dose as unchanged drug).
Hepatic function impairment: Bioavailability following oral administration may be markedly increased in patients with hepatic disease.
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