Trade Names:Imitrex- Injection 4 mg per 0.5 mL (as succinate)- Injection 6 mg per 0.5 mL (as succinate)- Spray, nasal 5 mg- Spray, nasal 20 mg- Tablets 25 mg (as succinate)- Tablets 50 mg (as succinate)- Tablets 100 mg (as succinate)Apo-Sumatriptan (Canada)CO Sumatriptan (Canada)Gen-Sumatriptan (Canada)Imitrex DF (Canada)Novo-Sumatriptan (Canada)Novo-Sumatriptan DF (Canada)PMS-Sumatriptan (Canada)ratio-Sumatriptan (Canada)Sandoz Sumatriptan (Canada)
Selective agonist for vascular serotonin (5-HT) receptor subtype, causing vasoconstriction of cranial arteries.
Sumatriptan T max for subcutaneous, oral, and intranasal administration is 0.17, 1.5, and 1.5 h, respectively. C max for subcutaneous, oral, and intranasal administration is 72, 54, and 13 mg/L, respectively. AUC for subcutaneous, oral, and intranasal administration is 90, 158, and 48 mcg/L•h, respectively. Bioavailability for subcutaneous, oral, and intranasal administration is 96%, 14%, and 15.8%, respectively.
Sumatriptan protein binding is 14% to 21%.
Sumatriptan t ½ for subcutaneous, oral, and intranasal administration is 2, 2, and 1.8 h, respectively.
Bioavailability following oral administration may be markedly increased in patients with liver disease.Race
No apparent difference in pharmacokinetics based on race.
Acute treatment of migraine attacks with or without aura; treatment of acute cluster headaches (injection only).
IV use (causes coronary vasospasm); patients with history, signs, or symptoms of ischemic heart disease (eg, angina, including Prinzmetal variant; MI; silent myocardial ischemia); cerebrovascular or peripheral vascular syndromes; uncontrolled hypertension; concurrent use or use within 24 h of ergotamine-containing preparations; management of hemiplegic or basilar migraine; severe hepatic function impairment; hypersensitivity to any component of the product.
PO Recommended dose is up to 100 mg taken with fluids. Doses of 100 mg have not been proven to provide a greater effect than 50 mg. If headache returns, a single additional dose may be taken after 2 h up to a max of 200 mg per day. If headache returns following an initial dose with the injection, additional doses of single tablets (up to 100 mg per day) may be given with an interval of at least 2 h between tablet doses. Subcutaneous Administer as soon as symptoms appear. Max single adult dose is 6 mg. Max dose per 24 h is two 6 mg injections separated by at least 1 h. Available in auto-injection prefilled syringe devices that deliver 4 or 6 mg for easy use; however, lower doses should be used in patients who have adverse reactions at the usual dose.
Intranasal Administer a single dose of 5, 10, or 20 mg in one nostril. A 10 mg dose can be achieved by the administration of a single 5 mg dose in each nostril. If headache returns, the dose may be repeated once after 2 h. Do not exceed a total daily dose of 40 mg.Hepatic Function Impairment
Max single dose is 50 mg.
Store tablets and nasal spray at ambient room temperature (47° to 86°F) or in refrigerator (36° to 46°F). Store injectable at 36° to 86°F. Protect from light. Protect nasal spray and injection from light.
Increased risk of vasospastic reactions; therefore, coadministration of two 5-HT 1 agonists within 24 h of each other is contraindicated.Ergot-containing drugs
May cause additive prolonged vasospastic reactions. Avoid use within 24 h of each other.MAOIs
Sumatriptan concentrations may be elevated, increasing the risk of serious adverse reactions (eg, coronary artery vasospasm). Therefore, when possible, avoid coadministration.Selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
Weakness, hyperreflexia, and incoordination have been reported rarely.Sibutramine
Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness, may occur.
None well documented.
Flushing (7%); decreased or increased BP, palpitation, syncope (at least 1%); atrial fibrillation, cardiomyopathy, colonic ischemia, Prinzmetal variant angina, pulmonary embolism, shock, thrombophlebitis (postmarketing).
Dizziness/vertigo (12%); paresthesia (5%); drowsiness/sedation, malaise or fatigue (3%); headache (2%); anxiety (1%); cerebrovascular accident, dysphasia, panic disorder, subarachnoid hemorrhage, vasculitis (postmarketing).
Sweating (2%); exacerbation of sunburn (postmarketing).
Unusual taste (25% intranasal); discomfort in nasal cavity or sinuses (4%); throat discomfort (3%); visual alterations (1%); allergic rhinitis, ear, nose, and throat hemorrhage, external otitis, hearing loss, nasal inflammation, sensitivity to noise, sinusitis, tinnitus, upper respiratory inflammation (at least 1%); deafness, ischemic optic neuropathy, loss of vision, retinal artery occlusion, retinal vein thrombosis (postmarketing).
Mouth or tongue discomfort (5%); nausea, vomiting (4% [14% intranasal]); jaw discomfort (2%); abdominal discomfort, dysphagia (1%); diarrhea, gastric symptoms (at least 1%); ischemic colitis with rectal bleeding, xerostomia (postmarketing).
Acute renal failure (postmarketing).
Hemolytic anemia, pancytopenia, thrombocytopenia (postmarketing).
Elevated LFTs (postmarketing).
Allergic vasculitis, anaphylaxis/anaphylactoid reactions, erythema, pruritus, rash, shortness of breath, urticaria (postmarketing).
Injection-site reaction (59%); contusion, induration, lipoatrophy (subcutaneous), pain, redness, stinging, subcutaneous bleeding, swelling (postmarketing).
Neck pain or stiffness, weakness (5%); myalgia (2%); muscle cramps (1%).
Bronchospasm (1%); dyspnea (at least 1%).
Tingling (14%); warm/hot sensation (11%); burning sensation (8%); feeling of heaviness or pressure (7%); feeling of tightness, numbness (5%); cold sensation, tightness in chest (3%); feeling strange, head tightness, pain, pressure in chest (2%).
Exclude potentially serious neurologic conditions before treating headaches in patients not previously diagnosed with migraine or cluster headache.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
Use is not recommended because elderly patients are more likely to have decreased hepatic function, they are at higher risk of coronary artery disease, and blood pressure increases may be more pronounced.
Life-threatening and fatal hypersensitivity reactions (eg, anaphylaxis or anaphylactoid) have been reported.
Use with caution in patients with diseases that may alter absorption, metabolism, or excretion of drugs (eg, hepatic or renal function impairment); use with caution in patients with a history of epilepsy or conditions associated with lowered seizure thresholds.
Serious coronary events, some resulting in death, can occur after sumatriptan use. Administer first dose in health care provider's office to patients at possible risk of unrecognized coronary disease. If symptoms consistent with angina occur, conduct ECG evaluation for ischemic changes. May cause coronary vasospasm in patients with history of coronary heart disease. Rare reports of MI, major arrhythmias, angina symptoms, and death.
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported.
Elevation in BP, including hypertensive crisis, have been reported.
Because sumatriptan binds to melanin, it may accumulate in melanin-rich tissues (eg, eye), possibly causing toxicity after extended use.
Peripheral vascular ischemia and colonic ischemia with abdominal pain and bloody diarrhea have been reported. Also, transient and permanent blindness and partial vision loss have been reported.
Life-threatening serotonin syndrome may occur, particularly when combined with serotonin reuptake inhibitors.
Ataxia, cyanosis, erythema of extremities, inactivity, injection-site reactions (eg, desquamation, hair loss, scab formation), mydriasis, paralysis, reduced respiratory rate, seizures, tremor.
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