Hypersensitivity to eletriptan. Known or suspected ischaemic heart disease (e.g. angina pectoris, MI, silent ischaemia), coronary artery vasospasm (e.g. Prinzmetal variant angina), severe or uncontrolled HTN, Wolff-Parkinson-White syndrome or arrhythmias, heart failure, previous CVA or TIA, peripheral vascular disease, ischaemic bowel disease, basilar or hemiplegic migraine. Severe hepatic and renal impairment. Concomitant admin w/ 5-HT1 receptor agonists or ergot alkaloids.
Special Precautions
Patient at risk of coronary artery disease (e.g. HTN, DM, hypercholesterolaemia, smoker or user of nicotine therapy, post-menopausal women, men >40 yr, strong family history of coronary artery disease, obesity). Mild to moderate renal impairment. Pregnancy and lactation.
This drug may cause dizziness, somnolence, or weakness, if affected, do not drive or operate machinery.
Monitoring Parameters
Determine a clear diagnosis of migraine before treatment. Monitor CV status prior initiation of treatment and periodically thereafter; hepatic and renal function. Perform periodic CV evaluation for patients w/ risk factors for coronary artery disease who are receiving intermittent long-term therapy.
Overdosage
Symptoms: HTN and other CV symptoms. Management: Supportive treatment.
Drug Interactions
Increased peak plasma concentration w/ potent CYP3A4 enzyme inhibitors (e.g. ketoconazole, clarithromycin, ritonavir). Potential risk of serotonin syndrome w/ SSRIs or serotonin norepinephrine reuptake inhibitors (SNRIs). Potentially Fatal: May cause additive vasospastic effect when used concomitantly w/ ergot alkaloids (e.g. ergotamine, dihydroergotmaine, methysergide) or other 5-HT1 receptor agonists.
Food Interaction
Increased bioavailability w/ high-fat meal.
Action
Description: Eletriptan is a selective agonist of serotonin (5-HT1B/1D/1F) receptors. It causes constriction of intracranial blood vessels and reduction of sterile inflammation associated w/ antidronic neuronal transmission, thereby relieving migraine. Pharmacokinetics: Absorption: Well absorbed. Bioavailability: Approx 50%. Time to peak plasma concentration: 1.5-2 hr. Distribution: Enters breast milk (small amount). Volume of distribution: 138 L. Plasma protein binding: Approx 85%. Metabolism: Metabolised in the liver by CYP3A4 enzyme to the active, N-demethylated metabolite. Excretion: Elimination half-life: Approx 4 hr.
Chemical Structure
Eletriptan Source: National Center for Biotechnology Information. PubChem Database. Eletriptan, CID=77993, https://pubchem.ncbi.nlm.nih.gov/compound/Eletriptan (accessed on Jan. 22, 2020)
N02CC06 - eletriptan ; Belongs to the class of selective serotonin (5HT1) agonists preparations. Used to relieve migraine.
References
Anon. Eletriptan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/03/2017.Buckingham R (ed). Eletriptan Hydrobromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2017.Joint Formulary Committee. Eletriptan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2017.McEvoy GK, Snow EK, Miller J et al (eds). Eletriptan Hydrobromide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 08/03/2017.Relpax Tablet, Film Coated (Roerig). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 08/03/2017.
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