sumatriptan (Rx)

>10%

Injection site reaction (≤86%)

Paresthesia (5-14%)

Dizziness (12%)

Warm/hot sensation (11%)

1-10%

Chest discomfort/pressure/tightness (2-5%)

Jaw or neck tightness (1-5%)

Diaphoresis (2%)

Burning sensation (7%)

Cold sensation (1%)

Dysphagia

Sore throat (3%)

Malaise (1%)

Abdominal distress (1%)

Frequency Not Defined

Agitation

Cardiac arrhythmia: V-fib/V-tach (rare)

Dysuria

Eye irritation

Flushing

MI and coronary artery vasospasm in patients with CAD risk factors (extremely rare)

Nasal discomfort

Palpitations

Tingling

Weakness

Contraindications

Current/history of ischemic cardiac, cerebrovascular, or peripheral vascular syndromes (angina, MI, stroke, TIA, ischemic bowel disease)

History of stroke, transient ischemic attack, or hemiplegic or basilar migraine

History of coronary artery disease or coronary artery vasospasm

Wolff-Parkinson-White syndrome or other cardiac accessory conduction pathway disorders

Uncontrolled hypertension

DO NOT use IV

Within 2 weeks of MAO-A inhibitors

Within 24 hours of another 5-HT1 receptor agonist or ergot-type medications

Severe hepatic impairment

History of hypersensitivity to drug or components

Uncontrolled hypertension

Cautions

Use when clear diagnosis of migraine established

Equally effective at any stage of migraine, although early use recommended

Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache); detoxification may be necessary

Binds to melanin, may cause toxicity to melanin-rich tissues on prolonged use

Very rare reports of transient and permanent blindness and significant partial vision loss

Serotonin syndrome may occur, particularly during combined use with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine); discontinue therapy if it occurs

Cerebral/subarachnoid hemorrhage and stroke reported with 5-HT1 agonist administration; discontinue if it occurs

Significant elevation of blood pressure, including hypertensive crisis, reported

Not for administration to patients with risk factors for coronary artery disease

Use caution in patients with history of seizure disorder or lowered seizure threshold

May cause depression including dizziness, weakness, or drowsiness (infrequent); caution when operating heavy machinery

Coronary artery vasospasm, transient ischemia, ventricular tachycardia/fibrillation, myocardial infarction, cardiac arrest and death reported with use 5HT1 agonists; perform cardiac evaluation in patients with multiple cardiovascular risk factors; evaluate for coronary artery disease in patients at high risk; discontinue therapy if arrhythmia occurs

Use oral formulations with caution in patients with mild-to-moderate hepatic impairment if treatment necessary and advisable; presystemic clearance, when administered orally, is reduced in hepatic impairment and cause an increase in plasma concentrations; dose reduction recommended; when adminsitered parenterally (SC, intranasal), does not undergo first pass metabolism and may not cause increase in plasma concentrations

Hypersensitivity reactions, including angioedema and anaphylaxis, reported; needle shield of prefilled syringe contains dry natural rubber (a latex derivative) that has potential to cause allergic reactions in latex-sensitive individuals

Pregnancy

Data from a prospective pregnancy exposure registry and epidemiological studies of pregnant women have not detected increased frequency of birth defects or consistent pattern of birth defects among women exposed to sumatriptan compared with general population; in developmental toxicity studies in rats and rabbits, oral administration of sumatriptan to pregnant animals was associated with embryolethality, fetal abnormalities, and pup mortality; when administered by intravenous route to pregnant rabbits, sumatriptan was embryolethal

However, possible disease-associated maternal and/or embryo/fetal risk reported; several studies have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy

Lactation

Sumatriptan is excreted in human milk following subcutaneous administration; there are no data on effects of sumatriptan on breastfed infant or effects of sumatriptan on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for injection and any potential adverse effects on breastfed infant from sumatriptan or from underlying maternal condition

Infant exposure to sumatriptan can be minimized by avoiding breastfeeding for 12 hr after therapy

Mechanism of Action

Selective 5-HT1B and 5-HT1D receptor agonist in cranial arteries; elicits vasoconstrictive and anti-inflammatory effects; associated with antidromic neuronal transmission and relief of migraine headache

Absorption

Bioavailability: 15% (PO); 97% (SC)

Onset: 10 min (SC); 30 min (PO)

Duration: 9-24 hr (SC)

Peak plasma time: 0.5-3 hr (PO); 5-20 minutes (SC)

Peak plasma concentration: 18-51 ng/mL (PO); 55-108 ng/mL (SC, 6 mg dose)

Distribution

Protein bound: 14-21%

Vd: 2.4 L/kg

Metabolism

Metabolized via hepatic MAO-A isoenzyme

Elimination

Half-life: 2-2.5 hr (PO); 115 min (IV)

Renal clearance: 264 mL/min

Total body clearance: 1176-1200 mL/min

Excretion: Urine (60%); feces (40%)