Overview
Eletriptan hydrobromide tablets contain eletriptan hydrobromide, which is a selective 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptor agonist. Eletriptan hydrobromide is chemically designated as (R)-3-[(1-Methyl-2-pyrrolidinyl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole monohydrobromide, and it has the following chemical structure: [Chemical Structure] The molecular formula is C22H26N2O2S .
Mechanism of Action
12.1 Mechanism of Action Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 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 eletriptan hydrobromide for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/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. 12.
Indications
- Eletriptan hydrobromide tablets are 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 eletriptan hydrobromide tablets, reconsider the diagnosis of migraine before eletriptan hydrobromide tablets are administered to treat any subsequent attacks. Eletriptan hydrobromide tablets are not intended for the prevention of migraine attacks.
Common Doses
- 40 mg
- 20 mg
- 80 mg
Dosage
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 [see CLINICAL STUDIES (14)]. 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.
Contraindications
- 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 [see WARNINGS AND PRECAUTIONS (5.1)]. Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see WARNINGS AND PRECAUTIONS (5.2)].
Side Effects
- The following adverse reactions are described elsewhere in other sections of the prescribing information: Myocardial ischemia and myocardial infarction, and Prinzmetal’s angina [see WARNINGS AND PRECAUTIONS (5.2)] Arrhythmias [see WARNINGS AND PRECAUTIONS (5.3)] Chest, throat, neck, and/or jaw pain/tightness/pressure [see WARNINGS AND PRECAUTIONS (5.4)] Cerebrovascular events [see WARNINGS AND PRECAUTIONS (5.4)] Other vasospasm reactions [see WARNINGS AND PRECAUTIONS (5.5)] Medication overuse headache [see WARNINGS AND PRECAUTIONS (5.6)] Serotonin syndrome [see WARNINGS AND PRECAUTIONS (5.
Interactions
- 7.1 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 eletriptan hydrobromide within 24 hours of each other is contraindicated. Concomitant use of other 5-HT1 agonists within 24 hours of eletriptan hydrobromide treatment is contraindicated [see CONTRAINDICATIONS (4)]. 7.