Tolerability and safety of eletriptan in the treatment of migraine: a comprehensive review.
OBJECTIVE
To provide a comprehensive review of the tolerability and safety of eletriptan. Background.-Eletriptan is a potent and selective 5-HT1B/1D agonist that has demonstrated significant efficacy in the acute treatment of migraine in doses of 20 mg, 40 mg, and 80 mg.


METHODS
This review reports the tolerability and safety of eletriptan across a broad spectrum of preclinical studies and clinical trials that collectively included treatment of more than 11 000 subjects and more than 74 000 migraine attacks.


RESULTS
In clinical trials, eletriptan was well tolerated and safe across its dosing range of 20 mg to 80 mg. The adverse event profile of eletriptan 20 mg was similar to placebo, while the most commonly used dose, eletriptan 40 mg, has an adverse event profile that is only marginally higher than placebo. Eletriptan was safe and well tolerated regardless of age or gender, and for both short- and long-term treatment. Eletriptan is metabolized primarily by the CYP3A4 enzyme. Coadministration of potent CYP3A4 inhibitors was not associated with clinically meaningful change in eletriptan tolerability or safety in the population included in these clinical trials. The margin of cardiovascular safety for eletriptan was also confirmed by a well-controlled clinical study in which intravenous eletriptan in excess of an 80-mg dose was rapidly infused in patients undergoing coronary angiography; nonetheless, it is recommended that eletriptan not be coadministered with a limited list of 7 potent CYP3A4 inhibitors; in addition, the triptan class in general (including eletriptan) is contraindicated in patients with symptoms or findings consistent with ischemic heart disease or other significant underlying cardiovascular disease.


CONCLUSIONS
This comprehensive review found that eletriptan is safe and well tolerated, and that relatively large changes in dose and plasma concentration result in minimal changes in tolerability.
D000208:Acute Disease; D000328:Adult; D000368:Aged; D002986:Clinical Trials as Topic; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005260:Female; D006801:Humans; D007211:Indoles / Q000009:adverse effects* / Q000627:therapeutic use*; D008297:Male; D015201:Meta-Analysis as Topic; D008881:Migraine Disorders / Q000188:drug therapy*; D011759:Pyrrolidines / Q000009:adverse effects* / Q000627:therapeutic use*; D017366:Serotonin Receptor Agonists / Q000009:adverse effects* / Q000627:therapeutic use*; D014363:Tryptamines
D007211:Indoles; D011759:Pyrrolidines; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; C115647:eletriptan