relpax

Uses

relpax is a triptan used for the treatment of migraines.

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

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

How relpax works

relpax 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.

relpax 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.

relpax Drug Interaction

Major: duloxetine, duloxetineUnknown: amphetamine / dextroamphetamine, amphetamine / dextroamphetamine, erenumab, erenumab, diphenhydramine, diphenhydramine, pregabalin, pregabalin, rimegepant, rimegepant, topiramate, topiramate, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, cetirizine, cetirizine

relpax Disease Interaction

Major: CAD risk factors, cardiovascular diseaseModerate: liver disease

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 relpax