Ballicules.com

Eletriptan

RELPAX

What it is5-HT1B/1D agonist; acute migraine.

Why this oneIt is the high-efficacy oral triptan whose selection is most often limited by CYP3A4 interactions.

What limits itStrong CYP3A4 inhibitors are contraindicated. Coronary vasospasm precludes use in ischemic or vasospastic disease.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Acute migraine (with or without aura)Adults20 or 40 mg PRN40 mg PRN40 mg single dose; 80 mg/24h

Renal Undefined

Hepatic Severe: not recommended (not evaluated); mild-moderate not specifically addressed

Second dose no sooner than 2 h after first; max 80 mg per 24 h

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Insufficient human data; animal developmental toxicity at clinically relevant doses.

Lactation Excreted in human milk; minimize infant exposure by avoiding breastfeeding for 24 h after treatment.

NO BOXED WARNINGS

Principal riskCoronary vasospasm; CYP3A4-dependent

Cost, est. cash$10–$300/month

Generic entry2017

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger1 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityAgent-specific vascular, serotonergic or hepatic risks; acute overdose is usually limited outside ergot or cardiovascular agents.

Mechanism of action: Eletriptan ballicule

Eletriptan ballicule: receptor binding, kinetics and half-life diagram

Open Eletriptan in the interactive console ↗