Relpax Indication:

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

Relpax Mechanism Of Action:

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. Relpax has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

Relpax Drug Interactions:

Citalopram Increased risk of CNS adverse effects
Clarithromycin This macrolide increases the effect and toxicity of eletriptan
Dihydroergotamine Possible severe and prolonged vasoconstriction
Dihydroergotoxine Possible severe and prolonged vasoconstriction
Ergotamine Possible severe and prolonged vasoconstriction
Erythromycin This macrolide increases the effect and toxicity of eletriptan
Escitalopram Increased risk of CNS adverse effects
Fluoxetine Increased risk of CNS adverse effects
Fluvoxamine Increased risk of CNS adverse effects
Itraconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Ketoconazole This potent CYP3A4 inhibitor increases the effect and toxicity of the triptan
Methylergonovine Possible severe and prolonged vasoconstriction
Methysergide Possible severe and prolonged vasoconstriction
Nefazodone Increased risk of CNS adverse effects
Nelfinavir The protease inhibitor increases the effect and toxicity of eletriptan
Paroxetine Increased risk of CNS adverse effects
Ritonavir The protease inhibitor increases the effect and toxicity of eletriptan
Sertraline Increased risk of CNS adverse effects
Venlafaxine Increased risk of CNS adverse effects
Troleandomycin The macrolide increases the effect and toxicity of eletriptan
Ergonovine Possible severe and prolonged vasoconstriction

Relpax Food Interactions:

Exposure to the product (area below curve) and maximum concentrations are increased when product is taken with a high-fat meal.

Relpax Generic Name:

Synonyms:

  • Not Available

Drug Type:

Small Molecule; Approved

Absorption:

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

Toxicity (Overdose):

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

Protein Binding:

Plasma protein binding is moderate and approximately 85%.

Biotransformation:

In vitro studies indicate that eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4. The N-demethylated metabolite of eletriptan is the only known active metabolite.

Half Life:

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

Dosage Forms of Relpax:

Tablet Oral

Chemical IUPAC Name:

3-[[(2R)-1-methylpyrrolidin-2-yl]methyl]-5-(2-phenylsulfonylethyl)-1H-indole

Organisms Affected:

Humans and other mammals

Relpax to general, pharmacology

General, pharmacology..