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Eletriptan
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<h2 id="approval-and-availability">Approval and availability</h2> <p>Eletriptan was approved by the US <a href="/facts/Food_and_Drug_Administration/rCEnh9WB">Food and Drug Administration</a> (FDA) in December 2002, for the acute treatment of migraine with or without <a href="/facts/Aura_(symptom)/lJmQPY0J">aura</a> in adults.<a class="footnote-ref" id="fnref:3" href="#fn:3"><sup>3</sup></a> It is available only by <a href="/facts/Medical_prescription/4jt1T3mY">prescription</a> in the United States, Canada and Australia. It is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. It is available in 20 mg and 40 mg strengths. But unfortunately for unknown reasons this product is hardly available in Germany if at all. </p><p>Eletriptan was covered by <a href="https://patents.google.com/patent/US5545644">U.S. Patent no. 5545644</a><a class="footnote-ref" id="fnref:4" href="#fn:4"><sup>4</sup></a><a class="footnote-ref" id="fnref:5" href="#fn:5"><sup>5</sup></a> and <a href="https://patents.google.com/patent/US6110940">U.S. Patent no. 6110940</a>;<a class="footnote-ref" id="fnref:6" href="#fn:6"><sup>6</sup></a><a class="footnote-ref" id="fnref:7" href="#fn:7"><sup>7</sup></a> both now expired. </p> <h2 id="mechanism-of-action">Mechanism of action</h2> <p class="note">Further information: <a href="/facts/Serotonin_receptor_agonist/zqbpWcFg">Serotonin receptor agonist</a> and <a href="/facts/Triptan/uKlcQDWr">Triptan § Mechanism_of_action</a></p> <p>Eletriptan is believed to reduce swelling of the blood vessels surrounding the brain. This swelling is associated with the head pain of a migraine attack. Eletriptan blocks the release of substances from nerve endings that cause more pain and other symptoms like nausea, and sensitivity to light and sound. It is thought that these actions contribute to relief of symptoms by eletriptan. </p><p>Eletriptan is a <a href="/facts/Serotonin_receptor_agonist/zqbpWcFg">serotonin receptor agonist</a>, specifically an <a href="/facts/Agonist/nz8U5NNp">agonist</a> of certain <a href="/facts/5-HT1_receptor/c2tVGHCw">5-HT1 family receptors</a>. Eletriptan binds with high affinity to the <a href="/facts/5-HT1B/zM2xads8">5-HT[1B</a>, <a href="/facts/5-HT1D/zzGzggdV">1D</a>, <a href="/facts/5-HT1F/7rRWhUwl">1F]</a> receptors. It has a modest affinity to the <a href="/facts/5-HT1A/aMCB3tvc">5-HT[1A</a>, <a href="/facts/5-HT1E/rBSqpDuD">1E</a>, <a href="/facts/5-HT2B_receptor/Sy104fUR">2B</a>, <a href="/facts/5-HT7/rcpLc6FL">7]</a> receptors, and little to no affinity at the <a href="/facts/5-HT2A/YfTglQKQ">5-HT[2A</a>, <a href="/facts/5-HT2C_receptor/RuyLstWf">2C</a>, <a href="/facts/5-HT3/7Qa2T8v3">3</a>, <a href="/facts/5-HT4/aFSHbN6U">4</a>, <a href="/facts/5-HT5A/Iclxf8po">5A</a>, <a href="/facts/5-HT6/2QQJ7upp">6]</a> receptors. </p><p>Eletriptan has no significant affinity or pharmacological activity at <a href="/facts/Adrenergic_receptor/uoAeJbcN">adrenergic</a> <a href="/facts/Alpha-1_adrenergic_receptor/JbPCT974">α1</a>, <a href="/facts/Alpha-2_adrenergic_receptor/QmUrvvYn">α2</a>, or <a href="/facts/Beta-adrenergic_receptor/uoAeJbcN">β</a>; <a href="/facts/Dopamine_receptor/fgsjJwkL">dopaminergic</a> <a href="/facts/D1_receptor/fkWRTblS">D1</a> or <a href="/facts/D2_receptor/SmmP3QyU">D2</a>; <a href="/facts/Muscarinic_acetylcholine_receptor/caIdoqrW">muscarinic</a>; or <a href="/facts/Opioid_receptor/eDIAqgV3">opioid receptors</a>. Eletriptan could be efficiently co-administered with nitric oxide synthase (NOS's) inhibitors for the treatment of NOS-dependent diseases (US patent US 2007/0254940). </p><p>Two theories have been proposed to explain the efficacy of 5-HT1 receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. </p> <h2 id="side-effects">Side effects</h2> <p>Common side effects include <a href="/facts/Hypertension/wlAvBfcf">hypertension</a>, <a href="/facts/Tachycardia/ycmyzP7q">tachycardia</a>, headache, dizziness, drowsiness and symptoms similar to <a href="/facts/Angina_pectoris/rT1brdwS">angina pectoris</a>. Severe allergic reactions are rare.<a class="footnote-ref" id="fnref:8" href="#fn:8"><sup>8</sup></a> </p> <h2 id="contraindications">Contraindications</h2> <p>Eletriptan is contraindicated in patients with various diseases of the heart and circulatory system, such as angina pectoris, severe hypertension, and <a href="/facts/Heart_failure/7fckX3Jm">heart failure</a>, as well as in patients that have had a stroke or heart attack. This is due to the unusual side effect of coronary vasoconstriction due to serotonin 5HT1B antagonism, which can precipitate a <a href="/facts/Heart_attack/xoGw0qcG">heart attack</a> in those already at risk. It is also contraindicated in severe <a href="/facts/Renal/HBspPrv9">renal</a> or <a href="/facts/Hepatic/Rtp4Fk2b">hepatic</a> impairment due to its extensive liver metabolism through <a href="/facts/CYP3A4/MqD09gEj">CYP3A4</a>.<a class="footnote-ref" id="fnref:9" href="#fn:9"><sup>9</sup></a> </p> <h2 id="interactions">Interactions</h2> <p>Strong inhibitors of the liver enzyme CYP3A4, such as <a href="/facts/Erythromycin/dPt7avsU">erythromycin</a> and <a href="/facts/Ketoconazole/UQcvnER5">ketoconazole</a>, significantly increase blood plasma concentration of eletriptan and should be separated by at least 72 hours. <a href="/facts/Ergot_alkaloid/7Uw5WeoP">Ergot alkaloids</a>, such as <a href="/facts/Dihydroergotamine/Y3ELJ85t">dihydroergotamine</a>, add to the drug's hypertensive effect and should be separated by at least 24 hours.<a class="footnote-ref" id="fnref:10" href="#fn:10"><sup>10</sup></a> </p> <h2 id="additional-chemical-names">Additional chemical names</h2> <ul><li><a href="/facts/Merck_Index/3X9mzhzx">Merck Index</a>: 3-[[(2<i>R</i>)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole</li> <li>5-[2-(benzenesulfonyl)ethyl]-3-(1-methylpyrrolidin-2(<i>R</i>)-ylmethyl)-1H-indole</li> <li>(<i>R</i>)-5-[2-(phenylsulfonyl)ethyl]-3-[(1-methyl-2-pyrrolidinyl)methyl]-1H-indole</li></ul> <h2 id="society-and-culture">Society and culture</h2> <h3>Brand names</h3> <p>It is sold in the United States, Canada, Australia, and the United Kingdom under the brand name Relpax,<a class="footnote-ref" id="fnref:11" href="#fn:11"><sup>11</sup></a><a class="footnote-ref" id="fnref:12" href="#fn:12"><sup>12</sup></a><a class="footnote-ref" id="fnref:13" href="#fn:13"><sup>13</sup></a> and in several other countries under the brand name Relert. </p><p>In the US, Relpax is marketed by <a href="/facts/Viatris/bvI5oTMP">Viatris</a> after Upjohn was spun off from Pfizer.<a class="footnote-ref" id="fnref:14" href="#fn:14"><sup>14</sup></a><a class="footnote-ref" id="fnref:15" href="#fn:15"><sup>15</sup></a><a class="footnote-ref" id="fnref:16" href="#fn:16"><sup>16</sup></a> </p> <h2 id="references">References</h2> <ol> <li id="fn:1"><p>Bhambri R, Mardekian J, Liu LZ, Schweizer E, Ramos E (2015). "A review of the pharmacoeconomics of eletriptan for the acute treatment of migraine". International Journal of General Medicine. 8: 27–36. doi:10.2147/IJGM.S73673. PMC 4296958. PMID 25624770. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4296958" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4296958</a> <a href="#fnref:1" class="footnote-back-ref">↩</a></p></li> <li id="fn:2"><p>Capi M, Curto M, Lionetto L, de Andrés F, Gentile G, Negro A, et al. (September 2016). "Eletriptan in the management of acute migraine: an update on the evidence for efficacy, safety, and consistent response". Therapeutic Advances in Neurological Disorders. 9 (5): 414–23. doi:10.1177/1756285616650619. PMC 4994780. PMID 27582896. <a href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4994780" target="_blank">https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4994780</a> <a href="#fnref:2" class="footnote-back-ref">↩</a></p></li> <li id="fn:3"><p>"Drug Approval Package: Relpax (Eletriptan) NDA #021016". U.S. Food and Drug Administration (FDA). 4 April 2002. Retrieved 11 November 2020. <a href="https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm" target="_blank">https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm</a> <a href="#fnref:3" class="footnote-back-ref">↩</a></p></li> <li id="fn:4"><p>"Drug Approval Package: Relpax (Eletriptan) NDA #021016". U.S. Food and Drug Administration (FDA). 4 April 2002. Retrieved 11 November 2020. <a href="https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm" target="_blank">https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm</a> <a href="#fnref:4" class="footnote-back-ref">↩</a></p></li> <li id="fn:5"><p>U.S. Patent no. 5545644, John E. Macor & Martin J. Wythes, Indole Derivatives, 13 August 1996. <a href="https://patents.google.com/patent/US5545644" target="_blank">https://patents.google.com/patent/US5545644</a> <a href="#fnref:5" class="footnote-back-ref">↩</a></p></li> <li id="fn:6"><p>"Drug Approval Package: Relpax (Eletriptan) NDA #021016". U.S. Food and Drug Administration (FDA). 4 April 2002. Retrieved 11 November 2020. <a href="https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm" target="_blank">https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21016_Relpax.cfm</a> <a href="#fnref:6" class="footnote-back-ref">↩</a></p></li> <li id="fn:7"><p>U.S. Patent no. 6110940, Valerie Denise Harding, et al., Salts of an anti-migraine indole derivative, 29 August 2000. <a href="https://patents.google.com/patent/US6110940" target="_blank">https://patents.google.com/patent/US6110940</a> <a href="#fnref:7" class="footnote-back-ref">↩</a></p></li> <li id="fn:8"><p>Jasek W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 6984–8. ISBN 978-3-85200-181-4. <a href="978-3-85200-181-4" target="_blank">978-3-85200-181-4</a> <a href="#fnref:8" class="footnote-back-ref">↩</a></p></li> <li id="fn:9"><p>Jasek W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 6984–8. ISBN 978-3-85200-181-4. <a href="978-3-85200-181-4" target="_blank">978-3-85200-181-4</a> <a href="#fnref:9" class="footnote-back-ref">↩</a></p></li> <li id="fn:10"><p>Jasek W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 6984–8. ISBN 978-3-85200-181-4. <a href="978-3-85200-181-4" target="_blank">978-3-85200-181-4</a> <a href="#fnref:10" class="footnote-back-ref">↩</a></p></li> <li id="fn:11"><p>"Relpax- eletriptan hydrobromide tablet, film coated". DailyMed. 10 December 2019. Retrieved 11 November 2020. <a href="https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=986dc112-b97b-44a3-bfaf-074f906f8bb2" target="_blank">https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=986dc112-b97b-44a3-bfaf-074f906f8bb2</a> <a href="#fnref:11" class="footnote-back-ref">↩</a></p></li> <li id="fn:12"><p>"Relpax Product information". Health Canada. 25 April 2012. Retrieved 11 November 2020. <a href="https://health-products.canada.ca/dpd-bdpp/info.do?lang=en&code=74152" target="_blank">https://health-products.canada.ca/dpd-bdpp/info.do?lang=en&code=74152</a> <a href="#fnref:12" class="footnote-back-ref">↩</a></p></li> <li id="fn:13"><p>"Relpax 20mg Film-Coated Tablets. - Summary of Product Characteristics (SmPC)". (emc). 3 July 2020. Retrieved 11 November 2020. <a href="https://www.medicines.org.uk/emc/product/1568/smpc" target="_blank">https://www.medicines.org.uk/emc/product/1568/smpc</a> <a href="#fnref:13" class="footnote-back-ref">↩</a></p></li> <li id="fn:14"><p>"Pfizer Completes Transaction to Combine Its Upjohn Business with Mylan". Pfizer. 16 November 2020. Retrieved 17 June 2024 – via Business Wire. <a href="https://www.businesswire.com/news/home/20201116005378/en/" target="_blank">https://www.businesswire.com/news/home/20201116005378/en/</a> <a href="#fnref:14" class="footnote-back-ref">↩</a></p></li> <li id="fn:15"><p>"Relpax". Pfizer. Retrieved 17 June 2024. <a href="https://www.pfizer.com/products/product-detail/relpax" target="_blank">https://www.pfizer.com/products/product-detail/relpax</a> <a href="#fnref:15" class="footnote-back-ref">↩</a></p></li> <li id="fn:16"><p>"Brands". Viatris. 16 November 2020. Retrieved 17 June 2024. <a href="https://www.viatris.com/en/products/brands" target="_blank">https://www.viatris.com/en/products/brands</a> <a href="#fnref:16" class="footnote-back-ref">↩</a></p></li> </ol>