Trade Names:Relpax- Tablets 24.2 mg- Tablets 48.5 mg
Selective agonist for vascular serotonin (5-HT 1 ) receptor subtype, causing vasoconstriction of cranial arteries.
Eletriptan is well absorbed, reaching a peak plasma level in approximately 1.5 h. The mean absolute bioavailability is approximately 50%.
Eletriptan is approximately 85% protein bound. The Vd is 138 L after IV injection.
The N-demethylated metabolite is active.
The terminal elimination t ½ is approximately 4 h. The mean renal Cl is 3.9 L/h after oral administration. Non-renal Cl accounts for about 90% of total Cl.
Mild to moderate impairment results in an increase in both AUC (34%) and t ½ , while the peak plasma level increased 18%.Elderly
Increased t ½ from about 4.4 to 5.7 h in elderly (65 to 93 yr of age).Age
Increased t ½ from about 4.4 to 5.7 h in younger subjects (18 to 45 yr of age).
Acute treatment of migraine with or without aura.
Ischemic heart disease (eg, angina pectoris); symptoms or findings consistent with ischemic heart disease; coronary artery vasospasm (including Prinzmetal variant angina); significant underlying CV disease; cerebrovascular syndromes (including strokes of any type or transient ischemic attacks); peripheral vascular disease (including ischemic bowel disease); uncontrolled hypertension; hemiplegic or basilar migraine; severe hepatic function impairment; hypersensitivity to any component of the product; within 24 h of treatment with another 5-HT 1 agonist or an ergotamine-containing or ergot-type medication (eg, methysergide).
PO 20 to 40 mg single dose. If required, a second dose may be taken at least 2 h after the initial dose (max, 80 mg/day).
If headache recurs after initial relief, a second tablet may be administered, provided there is an interval of at least 2 h between doses. If first dose is ineffective, do not administer a second dose unless prescribed by health care provider.
Store at controlled room temperature (59° to 86°F).
Risk of vasospastic reactions may be increased. Concomitant use within 24 h of eletriptan is not recommended.Other 5-HT 1 agonists
Concomitant use of other 5-HT 1 agonists within 24 h of eletriptan is not recommended.Potent CYP-450 3A4 inhibitors (eg, clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, troleandomycin)
Eletriptan should not be used within 72 h of drugs that are potent CYP3A4 inhibitors.
None well documented.
Palpitation (at least 1%); coronary artery vasospasm; transient myocardial ischemia; MI; ventricular tachycardia; ventricular fibrillation.
Dizziness, somnolence (7%); headache (4%); hypertonia, hypesthesia, paresthesia, vertigo (at least 1%).
Sweating (at least 1%).
Nausea (8%); dry mouth (4%); dyspepsia, dysphagia (eg, throat tightness, difficulty swallowing) (2%).
Pharyngitis (at least 1%).
Asthenia (10%); pain, tightness, or pressure of chest (4%); stomach pain, cramps, or pressure, abdominal pain or discomfort (2%); back pain, chills (at least 1%).
MonitorSymptoms of migraine attack
Assess pain location, intensity, duration, and associated symptoms of migraine attack and response to treatment.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
There is an increased t ½ (from about 4.4 to 5.7 h) in the elderly (65 to 93 yr of age).
It is recommended that eletriptan not be given to patients in whom unrecognized coronary artery disease (CAD) is predicted based on the presence of risk factors (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, women with surgical or physiological menopause, men older than 40 yr of age). Serious adverse cardiac events, including MI, life-threatening disturbances of cardiac rhythm, and death have been reported within a few hours of administration of a 5-HT 1 agonist.
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists.
Elevation in BP, including hypertensive crisis, have been reported with administration of 5-HT 1 agonists.
Hypertension or other more serious CV symptoms may occur.
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