Eletriptanum

Eletriptanum Uses, Dosage, Side Effects, Food Interaction and all others data.

Eletriptanum is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches.

Eletriptanum is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses. While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed. Eletriptanum has also been shown to inhibit trigeminal nerve activity in the rat.

Trade Name Eletriptanum
Availability Prescription only
Generic Eletriptan
Eletriptan Other Names Eletriptán, Eletriptan, élétriptan, Eletriptanum
Related Drugs Ubrelvy, Botox, diclofenac, celecoxib, metoclopramide, sumatriptan, Imitrex, Reglan
Type
Formula C22H26N2O2S
Weight Average: 382.519
Monoisotopic: 382.171498776
Protein binding

Plasma protein binding is moderate and approximately 85%.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Eletriptanum
Eletriptanum

Uses

Eletriptanum is a triptan used for the treatment of migraines.

For the acute treatment of migraine with or without aura in adults.

Eletriptanum is also used to associated treatment for these conditions: Acute Migraine, Migraine with acute onset aura

How Eletriptanum works

Eletriptanum binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. In contrast, eletriptan displays insignificant pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. While the full mechanism of action of 5-HT receptor agonists in relieving migrains is not fully elucidated, it is proposed that the activation of 5-HT1 receptors located on intracranial blood vessels leads to vasoconstriction that correlates with the relief of migraine headaches. It is also proposed that the activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system leads to the inhibition of release of pro-inflammatory neuropeptides.

Toxicity

Based on the pharmacology of the 5-HT1B/1D agonists, hypertension or other more serious cardiovascular symptoms could occur on overdose.

Food Interaction

  • Take with or without food. High-fat meals increase exposure, but not to a clinically relevant extent.

Eletriptanum Cholesterol interaction

[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.

Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).

Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.

In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.

As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.

Periodic cardiovascular evaluations should be performed during intermittent, long-term use.

Volume of Distribution

  • 138 L

Elimination Route

Well absorbed after oral administration with a mean absolute bioavailability of approximately 50%.

Half Life

The terminal elimination half-life of eletriptan is approximately 4 hours.

Clearance

  • Renal cl=3.9 L/h

Innovators Monograph

You find simplified version here Eletriptanum

*** Taking medicines without doctor's advice can cause long-term problems.
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