Eletriptan

RELPAX is indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use: • Use only if a clear diagnosis of migraine has been established. If a patient has no response to the first migraine attack treated with RELPAX, reconsider the diagnosis of migraine before RELPAX is administered to treat any subsequent attacks. • RELPAX is not intended for the prevention of migraine attacks. • Safety and effectiveness of RELPAX have not been established for cluster headache. RELPAX is a serotonin (5-HT 1B/1D ) receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. Limitations of Use: • Use only after a clear diagnosis of migraine has been established. • Not indicated for the prophylactic therapy of migraine. • Not indicated for the treatment of cluster headache

Eletriptan binds with high affinity to 5-HT 1B, 5-HT 1D and 5-HT 1F receptors, has modest affinity for 5-HT 1A, 5-HT 1E, 5-HT 2B and 5-HT 7 receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of RELPAX for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

The maximum recommended single dose is 40 mg. In controlled clinical trials, single doses of 20 mg and 40 mg were effective for the acute treatment of migraine in adults. A greater proportion of patients had a response following a 40 mg dose than following a 20 mg dose. If the migraine has not resolved by 2 hours after taking RELPAX, or returns after transient improvement, a second dose may be administered at least 2 hours after the first dose. The maximum daily dose should not exceed 80 mg. The safety of treating an average of more than 3 migraine attacks in a 30-day period has not been established. • Single dose: 20 mg or 40 mg. • Maximum single dose: 40 mg. • May repeat dose after 2 hours if needed, not to exceed 80 mg in any 24-hour period

RELPAX is contraindicated in patients with: • Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal's angina. • Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders. • History of stroke, transient ischemic attack (TIA), or history or current evidence of hemiplegic or basilar migraine because these patients are at a higher risk of stroke. • Peripheral vascular disease. • Ischemic bowel disease. • Uncontrolled hypertension.

RELPAX should only be used where a clear diagnosis of migraine has been established. • Myocardial ischemia/infarction or Prinzmetal's angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors. • Arrhythmias: Discontinue RELPAX if occurs. • Chest/throat/neck/jaw pain, tightness, pressure, or heaviness: Generally not myocardial ischemia, evaluate high risk patients for CAD. • Cerebral hemorrhage, subarachnoid hemorrhage, or stroke: Discontinue RELPAX if occurs. • Gastrointestinal ischemia or infarction events, or peripheral vasospastic reactions: Discontinue RELPAX if occurs. • Medication overuse headache: Detoxification may be necessary. • Serotonin syndrome: Discontinue RELPAX if occurs

The following adverse reactions are described elsewhere in other sections of the prescribing information: • Myocardial ischemia and myocardial infarction, and Prinzmetal's angina • Arrhythmias • Chest, throat, neck, and/or jaw pain/tightness/pressure • Cerebrovascular events • Other vasospasm reactions • Medication overuse headache • Serotonin syndrome • Increase in blood pressure • Hypersensitivity reactions Most common adverse reactions (≥ 5% and > placebo) were asthenia, nausea, dizziness, and somnolence. These reactions appear to be dose-related.

Ergot-Containing Drugs Including Other 5-HT 1B/1D Agonists Ergot-containing drugs have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine [DHE] or methysergide) and RELPAX within 24 hours of each other is contraindicated. Concomitant use of other 5-HT 1 agonists within 24 hours of RELPAX treatment is contraindicated.

Store at 20°C to 25°C (68°F to 77°F), excursions permitted between 15°C to 30°C (59°F to 86°F).