Apo-Eletriptan

Apo-Eletriptan Uses, Dosage, Side Effects, Food Interaction and all others data.

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

Apo-Eletriptan 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. Apo-Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.

Apo-Eletriptan
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Apo-Eletriptan
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	Canada, United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Apo-Eletriptan is a triptan used for the treatment of migraines.

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

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

How Apo-Eletriptan works

Apo-Eletriptan 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.

Apo-Eletriptan 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.