Eletriptan

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Relpax; Belgium: Relert; Bulgaria: Relpax; Czech Republic: Relpax; Denmark: Relpax; Estonia: Relpax; Finland: Relert; France: Relpax; Germany: Relpax; Greece: Relpax; Hungary: Relpax; Ireland: Relpax; Italy: Relpax; Latvia: Relpax; Lithuania: Relpax; Netherlands: Relpax; Poland: Relpax; Portugal: Relert; Romania: Relpax; Slovakia: Relpax; Slovenia: Relpax; Spain: Relpax; Sweden: Relpax; UK: Relpax.

North America

Canada: Relpax; USA: Relpax.

Latin America

Mexico: Relpax.

Asia

Japan: Relpax.

Drug combinations

Chemistry

Eletriptan Hydrobromide: C~22~H~26~N~2~O~2~S HBr. Mw: 463.43. R-3-[(1-Methyl-2-pyrrolidinyl)methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole monohydrobromide. CAS-177834-92-3 (1997).

Pharmacologic Category

Antimigraine Agents; Selective Serotonin Agonists; Serotonin 5-HT~1B~, 5-HT~1D~ Receptor Agonist. (ATC-Code: N02CC06).

Mechanism of action

A selective agonist of serotonin 5-HT~1B~, 5-HT~1D~ receptors. It is suggested that eletriptan may ameliorate migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and/or reduced transmission in the trigeminal pain pathway.

Therapeutic use

Used for acute treatment of attacks of migraine with or without aura in adults.

Pregnancy and lactiation implications

There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if potential benefit to the mother outweighs possible risk to the fetus. Teratogenic effects observed in animal studies. Eletriptan is distributed into human milk. Caution if used in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to eletriptan or any ingredient in the formulation. Ischemic heart disease (e.g. angina pectoris, MI, silent ischemia). Coronary vasospasm (e.g. prinzmetal variant angina). Other serious underlying cardiovascular disease (e.g. uncontrolled hypertension). Cerebrovascular syndromes (e.g. stroke syndrome, transient ischemic attacks). Peripheral vascular ischemia (e.g. ischemic bowel disease). Basilar or hemiplegic migraine. Treatment within the previous 24 hours with another 5-HT~1~ receptor agonist or with an ergot alkaloid (e.g. ergotamine, dihydroergotamine, methysergide). Use within 72 hours of potent inhibitors of the CYP3A4 isoenzyme (e.g. ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir). Severe hepatic impairment. Known hypersensitivity to eletriptan or any ingredient in the formulation.

Warnings and precautions

Only indicated for treatment of acute migraine. Risk of coronary vasospasm, myocardial ischemia and/or infarction, life-threatening cardiac rhythm disturbances, and death associated with use of 5-HT~1~ receptor agonists. Use of eletriptan not recommended in known or suspected ischemic or vasospastic heart disease or in likelihood of unrecognized coronary artery disease. Cerebral or subarachnoid hemorrhage, stroke, and other adverse cerebrovascular effects, some of which resulted in death, have occurred in patients treated with 5-HT~1~ receptor agonists. Patients with history of migraine may be at increased risk for certain cerebrovascular events (e.g. stroke, hemorrhage, transient ischemic attack). Peripheral vascular ischemia and colonic ischemia with abdominal pain and bloody diarrhea reported in patients treated with 5-HT~1~ receptor agonists. Substantial increases in blood pressure, including hypertensive crises, reported rarely following administration of 5-HT~1~ receptor agonists in patients with or without history of hypertension. Potentially life-threatening serotonin syndrome reported during concurrent therapy with 5-HT~1~ receptor agonists and SSRIs or SNRIs. Concurrent use of serotonin precursors (e.g. tryptophan) not recommended. Possible accumulation of eletriptan and/or its metabolites in melanin-rich tissues (such as the eye) over time, resulting in potential toxicity in these tissues with extended use. Not recommended for use in patients under 18 years of age. Increases in blood pressure may be more pronounced in geriatric patients. Use with caution in hepatic impairment. Use in severe hepatic impairment contraindicated.

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