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Medication Safety Issues
Sound-alike/look-alike issues:
SUMAtriptan may be confused with saxagliptin, sitaGLIPtin, somatropin, zolmitriptan
International issues:
Imitrex® may be confused with Nitrex® which is a brand name for isosorbide mononitrate in Italy
Pronunciation
(soo ma TRIP tan)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Oral, SubQ: Acute treatment of migraine with or without aura
SubQ: Acute treatment of cluster headache episodes
Pregnancy Risk Factor
C
Pregnancy Considerations
There are no adequate and well-controlled studies using sumatriptan in pregnant women. Use only if potential benefit to the mother outweighs the potential risk to the fetus. A pregnancy registry has been established to monitor outcomes of women exposed to sumatriptan during pregnancy (800-336-2176). Preliminary data from the registry do not suggest a greater risk of birth defects than the general population and so far a specific pattern of malformations has not been identified. However, sample sizes are small and studies are ongoing. In some (but not all) animal studies, administration was associated with embryolethality, fetal malformations and pup mortality.
Lactation
Enters breast milk/use caution (AAP rates “compatible”)
Breast-Feeding Considerations
The amount of sumatriptan an infant would be exposed to following breast-feeding is considered to be small (although the mean milk-to-plasma ratio is ~4.9, weight adjusted doses estimates suggest breast-fed infants receive 3.5% of a maternal dose). Expressing and discarding the milk for 8-12 hours after a single dose is suggested to reduce the amount present even further. The half-life of sumatriptan in breast milk is 2.22 hours.
Contraindications
Hypersensitivity to sumatriptan or any component of the formulation; patients with ischemic heart disease or signs or symptoms of ischemic heart disease (including Prinzmetal's angina, angina pectoris, myocardial infarction, silent myocardial ischemia); cerebrovascular syndromes (including strokes, transient ischemic attacks); peripheral vascular syndromes (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 inhibitor, specifically MAO type A inhibitors; management of hemiplegic or basilar migraine; prophylactic treatment of migraine; severe hepatic impairment; not for I.V. administration
Warnings/Precautions
Concerns related to adverse effects:
• Cardiac events: Coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death have been reported with 5-HT1 agonist administration. Patients who experience sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing should be evaluated for coronary artery disease or Prinzmetal's angina before receiving additional doses.
• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke have been reported with 5-HT1 agonist administration.
• Elevated blood pressure: Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension.
• Vasospasm-related events: Peripheral vascular ischemia and colonic ischemia have been reported with 5-HT1 agonist.
Disease-related concerns:
• Coronary artery disease: Should not be given to patients who have risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Patients with suspected CAD should have cardiovascular evaluation to rule out CAD before considering use; if cardiovascular evaluation “is satisfactory”, first dose should be given in the healthcare provider's office. Periodic evaluation of cardiovascular status should be done in all patients.
• Hepatic impairment: Use with caution in patients with hepatic impairment. Drug clearance may be reduced leading to increased plasma concentrations; dosage reduction of the oral product is recommended.
• Seizure disorders: Use with caution in patients with history of seizure disorder or in patients with a lowered seizure threshold.
Concurrent drug therapy issues:
• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans) or agents which reduce sumatriptan's metabolism. Concurrent use of serotonin precursors (eg, tryptophan) is not recommended.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children <18 years of age.
Other warnings/precautions:
• Appropriate use: Only indicated for the treatment of migraine or cluster headache.
Adverse Reactions
Injection:
>10%:
Central nervous system: Dizziness (12%), warm/hot sensation (11%)
Local: Pain at injection site (59%)
Neuromuscular & skeletal: Paresthesia (14%)
1% to 10%:
Cardiovascular: Chest pain/tightness/heaviness/pressure (2% to 3%), hyper-/hypotension (1%)
Central nervous system: Burning (7%), feeling of heaviness (7%), flushing (7%), pressure sensation (7%), feeling of tightness (5%), drowsiness (3%), malaise/fatigue (1%), feeling strange (2%), headache (2%), tight feeling in head (2%), cold sensation (1%), anxiety (1%)
Gastrointestinal: Abdominal discomfort (1%), dysphagia (1%)
Neuromuscular & skeletal: Neck, throat, and jaw pain/tightness/pressure (2% to 5%), mouth/tongue discomfort (5%), weakness (5%), myalgia (2%); muscle cramps (1%), numbness (5%)
Ocular: Vision alterations (1%)
Respiratory: Throat discomfort (3%), nasal disorder/discomfort (2%)
Miscellaneous: Diaphoresis (2%)
Nasal spray:
>10%: Gastrointestinal: Bad taste (13% to 24%), nausea (11% to 13%), vomiting (11% to 13%)
1% to 10%:
Central nervous system: Dizziness (1% to 2%)
Respiratory: Nasal disorder/discomfort (2% to 4%), throat discomfort (1% to 2%)
Tablet:
1% to 10%:
Cardiovascular: Chest pain/tightness/heaviness/pressure (1% to 2%), hyper-/hypotension (1%), palpitation (1%), syncope (1%)
Central nervous system: Burning (1%), dizziness (>1%), drowsiness (>1%), malaise/fatigue (2% to 3%), headache (>1%), nonspecified pain (1% to 2%, placebo 1%), vertigo (<1% to 2%), migraine (>1%), sleepiness (>1%)
Gastrointestinal: Diarrhea (1%), nausea (>1%), vomiting (>1%), hyposalivation (>1%)
Genitourinary: Hematuria (1%)
Hematologic: Hemolytic anemia (1%)
Neuromuscular & skeletal: Neck, throat, and jaw pain/tightness/pressure (2% to 3%), paresthesia (3% to 5%), myalgia (1%), numbness (1%)
Otic: Ear hemorrhage (1%), hearing loss (1%), sensitivity to noise (1%), tinnitus (1%)
Respiratory: Allergic rhinitis (1%), dyspnea (1%), nasal inflammation (1%), nose/throat hemorrhage (1%), sinusitis (1%), upper respiratory inflammation (1%)
Miscellaneous: Hypersensitivity reactions (1%), nonspecified pressure/tightness/heaviness (1% to 3%, placebo 2%); warm/cold sensation (2% to 3%, placebo 2%)
Route unspecified: <1%: Postmarketing and uncontrolled studies (limited to important or life-threatening): Abdominal aortic aneurysm, abdominal discomfort, abnormal menstrual cycle, abnormal/elevated liver function tests, accommodation disorders, acute renal failure, agitation, anaphylactoid reaction, anaphylaxis, anemia, angioneurotic edema, arrhythmia, atrial fibrillation, bronchospasm, cerebral ischemia, cerebrovascular accident, convulsions, deafness, death, decreased appetite, dental pain, diarrhea, dyspeptic symptoms, dysphagia, dystonic reaction, ECG changes, fluid disturbances (including retention), flushing, gastrointestinal pain, hallucinations, heart block, hematuria, hemolytic anemia, hiccups, hypersensitivity reactions, intestinal obstruction, intracranial pressure increased, ischemic colitis, joint ache, muscle stiffness, nose/throat hemorrhage, numbness of tongue, optic neuropathy (ischemic), pancytopenia, paresthesia, phlebitis, photosensitivity, Prinzmetal's angina, pruritus, psychomotor disorders, pulmonary embolism, rash, Raynaud syndrome, sensation changes, shock, subarachnoid hemorrhage, swallowing disorders, syncope, thrombocytopenia, thrombophlebitis, thrombosis, transient myocardial ischemia, TSH increased, vasculitis, vision loss, xerostomia
Drug Interactions
Ergot Derivatives: May enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Risk X: Avoid combination
MAO Inhibitors: May decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ. Risk X: Avoid combination
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Sibutramine: May enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Risk X: Avoid combination
Storage
Store at 2°C to 20°C (36°F to 86°F). Protect from light.
Mechanism of Action
Selective agonist for serotonin (5-HT1B and 5-HT1Dreceptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Pharmacodynamics/Kinetics
Onset of action: ~30 minutes
Distribution: Vd: 2.4 L/kg
Protein binding: 14% to 21%
Metabolism: Hepatic, primarily via MAO-A isoenzyme
Bioavailability: SubQ: 97% ± 16% of that following I.V. injection; Oral: 15%
Half-life elimination: Injection, tablet: 2.5 hours; Nasal spray: 2 hours
Time to peak, serum: 5-20 minutes
Excretion:
Injection: Urine (38% as indole acetic acid metabolite, 22% as unchanged drug)
Nasal spray: Urine (42% as indole acetic acid metabolite, 3% as unchanged drug)
Tablet: Urine (60% as indole acetic acid metabolite, 3% as unchanged drug); feces (40%)
Dosage
Adults:
Oral: A single dose of 25 mg, 50 mg, or 100 mg (taken with fluids). If a satisfactory response has not been obtained at 2 hours, a second dose may be administered. Results from clinical trials show that initial doses of 50 mg and 100 mg are more effective than doses of 25 mg, and that 100 mg doses do not provide a greater effect than 50 mg and may have increased incidence of side effects. Although doses of up to 300 mg/day have been studied, the total daily dose should not exceed 200 mg. The safety of treating an average of >4 headaches in a 30-day period have not been established.
Intranasal: A single dose of 5 mg, 10 mg, or 20 mg administered in one nostril. A 10 mg dose may be achieved by administering a single 5 mg dose in each nostril. If headache returns, the dose may be repeated once after 2 hours, not to exceed a total daily dose of 40 mg. The safety of treating an average of >4 headaches in a 30-day period has not been established.
SubQ: Up to 6 mg; if side effects are dose-limiting, lower doses may be used. A second injection may be administered at least 1 hour after the initial dose, but not more than 2 injections in a 24-hour period.
Dosage adjustment in renal impairment: Dosage adjustment not necessary
Dosage adjustment in hepatic impairment: Bioavailability of oral sumatriptan is increased with liver disease. If treatment is needed, do not exceed single doses of 50 mg. The nasal spray has not been studied in patients with hepatic impairment, however, because the spray does not undergo first-pass metabolism, levels would not be expected to alter. Use of all dosage forms is contraindicated with severe hepatic impairment.
Administration: Oral
Should be taken with fluids as soon as symptoms appear.
Administration: I.V.
Do not administer I.V.; may cause coronary vasospasm.
Administration: Other
Administer injection formulation subcutaneously. An autoinjection device (STATdose System®) is available for use with the 4 mg and 6 mg cartridges.
Patient Education
Take at first sign of migraine attack. This drug is to be used to reduce your migraine, not to prevent or reduce the number of attacks. Follow exact instructions for use.
Nasal spray: Administer dose into one nostril. If headache returns or is not fully resolved after the first dose, the dose may be repeated after 2 hours. Do not exceed 40 mg in 24 hours.
Oral: If headache returns or is not fully resolved after first dose, the dose may be repeated after 2 hours. Do not exceed 200 mg in 24 hours. Take whole with fluids.
SubQ: If headache returns or is not fully resolved after first dose, the dose may be repeated after 1 hour. Do not exceed two injections in 24 hours.
All forms: Do not take any form of this drug within 24 hours of any other migraine medication without consulting prescriber. May cause dizziness, fatigue, or drowsiness (use caution when driving or engaging in tasks that require alertness until response to drug is known); or nausea or vomiting (small, frequent meals, frequent mouth care, chewing gum, or sucking on lozenges may help). Report chest tightness or pain; excessive drowsiness; acute abdominal pain; skin rash or burning sensation; muscle weakness, soreness, or numbness; respiratory difficulty; or any other persistent adverse reactions. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
Geriatric Considerations
Use cautiously in the elderly, particularly since many elderly have cardiovascular disease which would put them at risk for cardiovascular adverse effects. Safety and efficacy in the elderly (>65 years) have not been established. Pharmacokinetic disposition is, however, similar to that in young adults.
Anesthesia and Critical Care Concerns/Other Considerations
Clinical Pearls/Comments: Sumatriptan should not be used in patients with a history of vasospastic disease, Prinzmetal's angina, or any critical vascular disease.
Cardiovascular Considerations
Coronary vasospasm has been associated with 5-HT1B/1D agonists. These agents are contraindicated in patients with documented ischemic of vasospastic coronary artery disease. Patients with risk factors for CAD may receive these agents, provided a cardiovascular evaluation yields satisfactory evidence that the patient is free of cardiovascular disease. In patients with risk factors for CAD, administration of the initial dose in a medically staffed/equipped facility (ie, physician's office) is recommended. In addition, ECG monitoring after the initial dose should be considered. Patients who acquire risk factors for CAD, or long-term users of agents from this class of medications, should undergo periodic cardiovascular evaluation.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Bad taste, dysphagia, hyposalivation (tablet), mouth/tongue discomfort (injection).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Dizziness is common; may cause drowsiness
Mental Health: Effects on Psychiatric Treatment
Contraindicated with other serotonin agonists (SSRIs) and MAO inhibitors
Nursing: Physical Assessment/Monitoring
For use only with a clear diagnosis of migraine or cluster headaches. Use caution with CAD or history of seizure disorder. Assess potential for interactions with other pharmacological agents patient may be taking (eg, ergot-containing drugs, MAO inhibitors, SSRIs). See Administration for specifics of SubQ, intranasal, oral formulation use. Assess therapeutic effectiveness (relief of headaches) and adverse response (eg, dizziness, tingling, drowsiness, myalgia, vision alternation, nausea, vomiting; reactions differ according to formulation). Teach patient proper use according to formulation (eg, with SubQ, appropriate injection technique and syringe/needle disposal), possible side effects/appropriate interventions, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. Note: Strength expressed as sumatriptan base
Injection, solution, as succinate: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Imitrex®: 4 mg/0.5 mL (0.5 mL); 6 mg/0.5 mL (0.5 mL)
Solution, intranasal [spray]: 5 mg/0.1 mL (6s); 20 mg/0.1 mL (6s)
Imitrex®: 5 mg/0.1 mL (6s); 20 mg/0.1 mL (6s)
Tablet, as succinate: 25 mg, 50 mg, 100 mg
Imitrex®: 25 mg, 50 mg, 100 mg
Pricing: U.S. (www.drugstore.com)
Kit (Imitrex STATdose Refill)
6 mg/0.5 mL (1): $206.82
Kit (Imitrex STATdose System)
6 mg/0.5 mL (1): $206.81
Kit (SUMAtriptan Succinate Refill)
6 mg/0.5 mL (1): $159.98
Solution (Imitrex)
5 mg/ACT (1): $52.85
6 mg/0.5 mL (2.5): $471.08
20 mg/ACT (6): $248.19
Solution (SUMAtriptan)
5 mg/ACT (1): $39.99
20 mg/ACT (1): $39.99
Tablets (Imitrex)
25 mg (9): $259.67
50 mg (9): $241.28
100 mg (9): $226.78
Tablets (Sumatriptan Succinate)
25 mg (9): $219.99
Tablets (SUMAtriptan Succinate)
50 mg (9): $199.99
Tablets (Sumatriptan Succinate)
100 mg (9): $199.97
References
Akpunonu BE, Mutgi AB, and Federman DJ, “Subcutaneous Sumatriptan for Treatment of Acute Migraine in Patients Admitted to the Emergency Department: A Multicenter Study,” Ann Emerg Med, 1995, 25(4):464-9.
“American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
Blier P and Bergeron R, “The Safety of Concomitant Use of Sumatriptan and Antidepressant Treatments,” J Clin Psychopharmacol, 1995, 15(2):106-9.
Boyd IW and Rohan AP, “Sumatriptan - Induced Chest Pain,” Lancet, 1994, 344(8939):1704-5.
Boyer EW and Shannon M, “The Serotonin Syndrome,” New Engl J Med, 2005, 352:1112-20.
Curtin T, Brooks AP, and Roberts JA, “Cardiorespiratory Distress After Sumatriptan Given by Injection,” BMJ, 1992, 305(6855):713-4.
Diamond S, “The Use of Sumatriptan in Patients on Monoamine Oxidase Inhibitors,” Neurology, 1995, 45(6):1039-40.
Edwards KR, Bennington VT, and Ellis J, “Intracerebral Hemorrhage Associated With Sumatriptan,” Headache, 1995, 35:309.
Ilett KF, Kristensen JH, Wojnar-Horton RE, et al, “Drug Distribution in Human Milk,” Aust Prescriber, 1997, 20(2): 35-40.
Kelly KM, “Cardiac Arrest Following Use of Sumatriptan,” Neurology, 1995, 45(6):1211-3.
La Porta LD, “Recurrent Depression After Sumatriptan Administration for Treatment of Migraine,” J Clin Psychopharmacol, 1995, 15(1):81-2.
Loder E, “Safety of Sumatriptan in Pregnancy. A Review of the Data So Far,” CNS Drugs, 2003; 17(1):1-7.
Luman W and Gray RS, “Adverse Reactions Associated With Sumatriptan,” Lancet, 1993, 341(8852):1091-2.
MacDonald JT, “Treatment of Juvenile Migraine With Subcutaneous Sumatriptan,” Headache, 1994, 34(10):581-2.
Ottervanger JP, et al, “Characteristics of Sumatriptan-Induced Chest Pain,” Pharm World Sci, 1995, 17:3.
Ottervanger JP, et al, “Determinants of Sumatriptan-Induced Chest Pain,” Pharm World Sci, 1995, 17:7.
Ottervanger JP, van Witsen TB, Valkenburg HA, et al, “Adverse Reactions Attributed to Sumatriptan: A Postmarketing Study in General Practice,” Eur J Clin Pharmacol, 1994, 47(4):305-9.
Palmer J, Feldman R, Mancini GB, et al, “Glyceryl Trinitrate Reversal of Post-Sumatriptan Coronary Artery Narrowing,” Lancet, 1995, 345(8961):1366.
Reiff-Eldridge R, Heffner CR, Ephross SA, et al, “Monitoring Pregnancy Outcomes After Prenatal Drug Exposure Through Prospective Pregnancy Registries: A Pharmaceutical Company Commitment,” Am J Obstet Gynecol, 2000, 182(1): 159-63.
Scott AK, “Sumatriptan Clinical Pharmacokinetics,” Clin Pharmacokinet, 1994, 27(5):337-44.
Srinivas NR, Igwenezue KB, Hainsworth JD, et al, “Lack of Pharmacokinetic Interaction Between Butorphanol Tartrate Nasal Spray and Sumatriptan Succinate,” J Clin Pharmacol, 1995, 35(4):432-7.
Srinivas NR, Shyu WC, Upmalis D, et al, “Lack of Pharmacokinetic Interaction Between Butorphanol Tartrate Nasal Spray and Sumatriptan Succinate,” J Clin Pharmacol, 1995, 35(4):432-7.
Stricker BH, “Coronary Vasospasm and Sumatriptan,” BMJ, 1992, 305(6845):118.
Walton-Shirley M, Flowers K, and Whiteside JH, “Unstable Angina Pectoris Associated With Imitrex Therapy,” Cathet Cardiovasc Diagn, 1995, 34(2):188.
Weidmann B, Jansen W, Bojko P, et al, “Sumatriptan-Induced Myocardial Infarction,” Intensivmedizin und Nofallmediczin, 1994, 31:353.
International Brand Names
Lexi-Comp.com
Last full review/revision November 2009
Content last modified November 2009
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