Eletriptan as an effective and safe drug in acute migraine therapy
In the pharmacotherapy of acute migraine attacks, a pharmacologically diverse group of triptans is particularly used. The choice of the right antimigraine drug should be individualized, based on the intersection of the patient's nature of complaints and the pharmacological profile of the drug. The following text briefly summarizes the basic characteristics and profile of eletriptan.
Characteristics of Eletriptan
Triptans are used as first-line medications in the therapy of moderate to severe migraine attacks, or even in mild attacks that do not respond to analgesics or non-steroidal anti-inflammatory drugs (NSAIDs). Eletriptan is a selective agonist of 5-HT1B/1D/1F receptors with a vasoconstrictive effect mainly on intracranial vessels. Among the triptans, it stands out for its fastest absorption and best penetration into the CNS and is considered a safe drug with minimal risk of serious adverse effects. Within the group of triptans, it is the drug of choice for patients at cardiovascular risk without the presence of ischemic heart disease (IHD). IHD, along with cerebrovascular diseases, peripheral vascular ischemic disease, and pregnancy, are contraindications to its administration.
Eletriptan in Clinical Studies
In numerous clinical trials, eletriptan has shown to be significantly more effective compared to placebo in treating acute migraine attacks at both available doses (40, 80 mg), and even at a lower dose of 20 mg. A meta-analysis of 74 published studies demonstrated that eletriptan at a dose of 40 mg is more effective compared to all other triptans always in at least one of two evaluated parameters (achieving pain-free status within 2 hours, maintaining pain-free status for 24 hours, headache relief within 2 hours, and maintaining headache relief for 24 hours). According to the results of the meta-analysis, patients taking eletriptan have the highest probability of achieving a pain-free state within 2 hours and maintaining it for 24 hours.
Comparison with Other Triptans
The efficacy of eletriptan was directly compared with some other triptans in so-called head-to-head clinical evaluations. Along with subcutaneously administered sumatriptan, rizatriptan, and zolmitriptan, eletriptan showed the most favorable results in treating acute migraine attacks. At doses of 40 and 80 mg, it was found in one analysis to be more effective and act faster than orally administered sumatriptan at a dose of 100 mg.
Compared to placebo, eletriptan also proved to be an effective antimigraine drug in patients who did not respond to previous sumatriptan treatment or did not tolerate it. Another study focused on switching between triptans documented its efficacy in patients not responding to rizatriptan or NSAIDs.
Drug Interactions
Eletriptan is metabolized exclusively by the hepatic cytochrome P450, primarily CYP3A4. Monoamine oxidase MAO-A, which biotransforms, for example, sumatriptan, does not participate in the metabolism of eletriptan. Patients with mild to moderate liver function disorders have increased maximum plasma concentration (Cmax) and systemic exposure (AUC) of eletriptan, but dose adjustment may not be necessary. Patients with severe liver damage should not take this drug. Clinically significant pharmacokinetic interactions with eletriptan have been reported for several potent CYP3A4 inhibitors (e.g., verapamil or fluconazole), so their concurrent administration should be carefully considered.
Concurrent administration of eletriptan with drugs used for migraine prophylaxis (e.g., beta-blockers, tricyclic antidepressants, or SSRIs) has not shown any interactions or adverse events. An exception is ergotamine and its derivatives (methysergide), which should not be administered 24 hours before or after taking eletriptan due to the risk of increased blood pressure.
Summary and Conclusion
Eletriptan is a safe drug that, in the therapy of acute migraine attacks, shows comparable or higher efficacy compared to other triptans. Although it is the triptan with the most complex pharmacodynamic and pharmacokinetic profile, drug interactions do not pose a significant complication for therapy. Since eletriptan is primarily metabolized by CYP3A4, it is essential to consider its prescription carefully along with potent CYP3A4 inhibitors. Adverse pharmacodynamic interactions occur with ergot alkaloid derivatives.
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Source: Capi M., Curto M., Lionetto L. et al. Eletriptan in the management of acute migraine: an update on the evidence for efficacy, safety, and consistent response. Ther Adv Neurol Disord 2016; 9 (5): 414–423, doi: 10.1177/1756285616650619.
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