Eletriptan

Oral
Acute migraine attacks

Mild to moderate: Initially, 20 mg. Max: 40 mg/24 hours. Severe: Contraindicated.

Severe: Contraindicated.

Moderately severe, severe, or uncontrolled hypertension; confirmed coronary heart disease, including ischaemic heart disease (e.g. angina pectoris, previous MI, or silent ischaemia); coronary artery vasospasm, objective or subjective symptoms of ischaemic heart disease or Prinzmetal's angina, significant arrhythmias or heart failure, peripheral vascular disease, history of CVA or TIA, Wolff-Parkinson-White syndrome, arrhythmias associated with other cardiac accessory conduction pathway disorders, ischaemic bowel disease. Severe hepatic and renal impairment. Within 24 hours of treatment with another 5-HT₁ receptor agonist, or an ergotamine-containing medication. Within at least 72 hours of treatment with potent CYP3A4 inhibitors.

Patient at risk of coronary artery disease (e.g. patient with hypertension, hypercholesterolaemia, diabetes, obesity; smokers or users of nicotine substitution therapy, men >40 years old, post-menopausal women, strong family history of coronary artery disease, or those in whom unrecognised cardiac disease is likely). Not indicated for the prophylaxis of migraine. Not indicated for the treatment of hemiplegic, ophthalmoplegic, or basilar migraine; cluster headache or atypical headaches (headaches which may be possibly related to a serious condition such as stroke or aneurysm rupture) where cerebrovascular vasoconstriction may be harmful. Mild to moderate renal impairment. Pregnancy and lactation.

Significant: Sensations of tightness, pain, and pressure in the chest, throat, neck, and jaw; elevation in blood pressure, including hypertensive crisis with acute impairment of organ systems; non-coronary vasospastic reactions (e.g. peripheral vascular ischaemia, gastrointestinal vascular ischemia/infarction), Raynaud's syndrome.
Cardiac disorders: Palpitations, tachycardia, arteriospasm coronary.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Abdominal pain or discomfort, nausea, dry mouth, dyspepsia, dysphagia, vomiting. Rarely, ischaemic colitis.
General disorders and administration site conditions: Asthenia, chills, pain.
Musculoskeletal and connective tissue disorders: Back pain, myalgia.
Nervous system disorders: Paraesthesia, somnolence, headache, dizziness, tingling or abnormal sensation, hypertonia, hypoaesthesia, myasthenia. Rarely, syncope, CVA.
Respiratory, thoracic and mediastinal disorders: Pharyngitis, rhinitis, throat tightness.
Skin and subcutaneous tissue disorders: Sweating, rash, pruritus, urticaria.
Vascular disorders: Flushing, feeling of warmth.
Potentially Fatal: Cardiac rhythm disturbance (e.g. ventricular tachycardia, ventricular fibrillation), coronary artery vasospasm (Prinzmetal's angina), cerebral or subarachnoid haemorrhage, stroke; anaphylaxis, anaphylactoid, and hypersensitivity reactions (e.g. angioedema). Rarely, acute MI or myocardial ischaemia.

PO: C

This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.

Establish a clear diagnosis of migraine prior to treatment. Monitor blood pressure, heart rate, ECG with 1st dose in patients with a likelihood of unrecognised coronary disease (e.g. significant hypertension, hypercholesterolaemia, obese, diabetics, smokers, family history of coronary disease); headache severity. Assess for signs and symptoms of serotonin syndrome and hypersensitivity reactions.

Symptoms: Hypertension or other more serious CV symptoms. Management: Supportive treatment.

Increased risk of serotonin syndrome with SSRIs, SNRIs, TCAs, and MAOIs.
Potentially Fatal: May result in additive vasospastic effect when taken within 24 hours of using ergot alkaloids (e.g. ergotamine, dihydroergotamine, methysergide) or other 5-HT₁ receptor agonists. Potent CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir) significantly increase the exposure of eletriptan when used within at least 72 hours of each other.

Increased bioavailability with high-fat meals. Increased incidence of adverse effects with St. John's wort.

Description:
Mechanism of Action: Eletriptan is a selective agonist of serotonin (5-HT_1B/1D/1F receptors). Its exact mechanism of action in the management of migraine has yet to be established, however, current data suggest that it causes constriction of certain intracranial blood vessels, inhibits pro-inflammatory neuropeptide release, and reduces transmission in the trigeminal pain pathway, thereby relieving migraine.
Onset: Headache relief: 30 minutes.
Pharmacokinetics:
Absorption: Rapidly and well absorbed from the gastrointestinal tract. Bioavailability: Approx 50%; increased with a high-fat meal. Time to peak plasma concentration: Approx 1.5-2 hours.
Distribution: Enters breast milk. Plasma protein binding: Approx 85%.
Metabolism: Metabolised in the liver mainly by the CYP3A4 isoenzyme to the active, N-demethylated metabolite.
Excretion: Mainly via metabolism (approx 90%); urine (approx 10%). Elimination half-life: Approx 4 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 77993, Eletriptan. https://pubchem.ncbi.nlm.nih.gov/compound/Eletriptan. Accessed Feb. 27, 2023.

Store below 30°C. Protect from moisture.

Antimigraine Preparations

N02CC06 - eletriptan ; Belongs to the class of selective serotonin (5HT1) agonists preparations. Used to relieve migraine.

Anon. Eletriptan Hydrobromide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/12/2022.

Anon. Eletriptan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/12/2022.

Buckingham R (ed). Eletriptan Hydrobromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/12/2022.

Eletriptan Hydrobromide Tablet, Film Coated (Ajanta Pharma USA Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/12/2022.

Joint Formulary Committee. Eletriptan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/12/2022.

Relpax 20 mg Film Coated Tablets (Upjohn UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 12/12/2022.