Safety and Efficacy of Eletriptan in the Treatment of Acute Migraine

Abstract

Eletriptan is a new selective serotonin agonist approved for the treatment of acute migraine headaches. To review the pharmacologic, pharmacodynamic, pharmacokinetic, safety, and clinical efficacy data for eletriptan, we searched the literature in PubMed/MEDLINE, EMBASE, International Pharmaceutical Abstracts, and Science Direct databases to gather all published reports from January 1996-October 2004. All English-language reports (abstract or full trial reports) about the pharmacology, pharmacokinetics, clinical efficacy, and safety of eletriptan were reviewed. Eletriptan's pharmacokinetic and pharmacodynamic parameters translate into a favorable safety and efficacy profile. The drug is rapidly absorbed when administered orally, has good bioavailability and central nervous system penetration due to its lipophilicity, and has a long half-life, which contributes to its ability to prevent recurrent headaches. Compared with other serotonin agonists, eletriptan has a longer duration of action and greater lipophilicity. Eletriptan is metabolized through the cytochrome P450 3A4 system; therefore, it does have the potential for clinically significant drug interactions. In clinical trials, eletriptan demonstrated efficacy superior to that of placebo and similar or superior efficacy to that of other serotonin agonists, with limited adverse effects. With clinical use, headache and pain-free responses and headache recurrence rates were similar to those of other serotonin agonists, but the agent is superior to ergotamine tartrate-caffeine. Based on pharmaco-economic data, eletriptan is more cost-effective than other agents in its class. Eletriptan is a safe and cost-effective option for the treatment of migraine headaches.

Migraine and Its Treatment from the Medicinal Chemistry Perspective

“…Especially if it is prescribed together with serotonin derivative drugs which are strong CYP3A4 inhibitors, the evaluation of the disease should be done well. Bioavailability is high and reaches up to 50%. , Its synthesis is shown in Figure .…”

Eletriptan in the management of acute migraine: an update on the evidence for efficacy, safety, and consistent response

“…In fact, the co-administration of eletriptan with other medications able to modify CYP3A4 function might increase or decrease eletriptan plasma levels, with increased risk of development of adverse effects or reduced clinical efficacy [Takiya et al 2006]. The co-administration of maximum doses of eletriptan and ketoconazole, a potent CYP3A4 inhibitor, was associated with a 2.7 fold C max increase and a 6-fold increase in the area under the curve (AUC) [Mathew et al 2003a].…”

“…Eletriptan may interact with substrates, inhibitors and inducers of the CYP3A4 enzyme. In fact, the co-administration of eletriptan with other medications able to modify CYP3A4 function might increase or decrease eletriptan plasma levels, with increased risk of development of adverse effects or reduced clinical efficacy [Takiya et al . 2006].…”

Current aspect of the diagnosis and management of migraine

“…Благодаря самой высокой селе-ктивности среди триптанов он лишен побочных эффектов со стороны сердечно-сосудистой системы. Элетриптан эф-фективно предотвращает повторные приступы мигрени [55]. Он оказался эффективен даже у «трудных» пациентов, которые не были удовлетворены результатами терапии НПВП [56] или другими триптанами [57].…”