Dosing and uses of Relpax (eletriptan)
Adult dosage forms and strengths
tablet
- 20mg
- 40mg
Migraine Headache
20-40 mg PO at onset of symptoms; repeat dose after 2 hr if necessary
Not to exceed 80 mg/day
Renal Impairment
Monitor for increase in blood pressure; dose adjustment not necessary
Hepatic Impairment
Mild to moderate impairment: Dose adjustment not necessary
Severe impairment: Do not administer
Pediatric dosage forms and strengths
<18 years old: Not recommended
Geriatric dosage forms and strengths
Migraine headache: See adult dosing
Relpax (eletriptan) adverse (side) effects
1-10%
Asthenia (5-10%)
Dizziness (5-10%)
Headache (5-10%)
Somnolence (5-10%)
Nausea (5-10%)
Chest pain/tightness (1-4%)
Palpitation (>1%)
Flushing (>1%)
Chills (>1%)
Hypertonia (>1%)
Hypoesthesia (>1%)
Pain (>1%)
Paresthesia (>1%)
Vertigo (>1%)
Weakness (>1%)
Abdominal pain/discomfort (>1%)
Dysphagia (>1%)
Dyspepsia (>1%)
Xerostomia (>1%)
Back pain (>1%)
Pharyngitis (>1%)
Diaphoresis (>1%)
Postmarking Reports
Cardiac ischemia
Seizures
Vomiting
Warnings
Contraindications
Hypersensitivity, including angioedema and anaphylaxis
History of CAD or coronary artery vasospasm
Wolff-Parkinson-White syndrome or other cardiac accessory conduction pathway disorders
History of stroke or TIA, or history of hemiplegic or basilar migraine because such patients are at a higher risk of stroke
Peripheral vascular disease
Ischemic bowel disease
Uncontrolled hypertension
Severe hepatic impairment
Do not use within 24 hr of another 5-HT1 agonist or ergot derivative
Within at least 72 hr of treatment with the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, or nelfinavir
Cautions
Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache)
Myocardial ischemia/infarction or Prinzmetal’s angina reported (see Contraindications)
Life-threatening cardiac rhythm disturbances including VT and VFIB leading to reported within a few hr following the administration of 5-HT1 agonists
Cerebral hemorrhage, subarachnoid hemorrhage, and stroke have occurred in patients treated with 5-HT1 agonists, and some have resulted in fatalities
Sensations of tightness, pain, and pressure in the chest, throat, neck, and jaw commonly occur after treatment and are usually non-cardiac in origin; however, perform a cardiac evaluation in patients at high cardiac risk
Significant increase in blood pressure including hypertensive crisis with acute impairment of organ systems reported
Anaphylaxis/anaphylactoid and hypersensitivity reactions, including angioedema reported (see Contraindications)
Pregnancy and lactation
Pregnancy category: C
Lactation: Enters breast milk; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Relpax (eletriptan)
Mechanism of action
Selective 5-HT1 receptor agonist in cranial arteries. Causes vasoconstriction and reduces inflammation associated with antidronic neuronal transmission associated with relief of migraine
Pharmacokinetics
Half-Life elimination: 4 hr
Peak Plasma Time: 1.5-2 hr
Bioavailability: 50%
Protein bound: 85%
Vd: 138 L
Metabolism: hepatic CYP3A4
Metabolites: N-demethylated eletriptan (10-20%)
Renal Clearance: 3.9 L/hr
Excretion: 90% Non-renaL
