RELPAX

Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches.

For the acute treatment of migraine with or without aura in adults.

Eletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist.

In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses.

While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed.

Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.

5-hydroxytryptamine receptor 1B Agonist 5-hydroxytryptamine receptor 1D Agonist 5-hydroxytryptamine receptor 1F Agonist.

Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.

In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4.

N-demethylated metabolite of eletriptan is the only known active metabolite.

Hover over products below to view reaction partners Eletriptan N-Desmethyleletriptan Eletriptan N-oxide.

The terminal elimination half-life of eletriptan is approximately 4 hours.

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Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.

Eletriptan hydrobromide tablets are 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.

Recent use (i.e., within 24 hours) of another 5-hydroxytryptamine1 (5-HT1) agonist, ergotamine-containing medication, or ergot-type medication such as dihydroergotamine (DHE) or methysergide.

Hypersensitivity to eletriptan hydrobromide tablets (angioedema and anaphylaxis seen) .

Recent use (i.e., within at least 72 hours) of the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, or nelfinavir.

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 eletriptan hydrobromide tablets, 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.

Eletriptan hydrobromide tablets containing 20 mg or 40 mg eletriptan (base) as the hydrobromide salt.

Tablets 20 mg are orange colored, round, biconvex, film-coated tablets debossed with ‘EL’ on one side and ‘20’ on the other side.

They are supplied as follows

Carton of 6 (1 X 6) Unit-dose Tablets NDC 59651-104-69 Eletriptan Hydrobromide Tablets 40 mg are orange colored, round, biconvex, film-coated tablets debossed with ‘EL’ on one side and ‘40’ on the other side.

Carton of 6 (1 X 6) Unit-dose Tablets NDC 72189-517-06 Carton of 12 (2 X 6) Unit-dose Tablets NDC 59651-105-93.

Store at 20° to 25°C (68° to 77°F) .