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Eletriptan Hydrobromide

Pronunciation: EL-e-TRIP-tan HYE-droe-BROE-mide
Class: Serotonin 5-HT 1 receptor agonist

Trade Names

Relpax
- Tablets, oral 20 mg
- Tablets, oral 40 mg

Pharmacology

Selective agonist for vascular serotonin (5-HT 1 ) receptor subtype, causing vasoconstriction of cranial arteries.

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Pharmacokinetics

Absorption

Well absorbed orally; T max is approximately 1.5 h. The mean absolute bioavailability is approximately 50%. AUC and C max are increased by approximately 20% to 30%, respectively, when administered with a high-fat meal.

Distribution

Eletriptan is approximately 85% protein bound. The Vd is 138 L (IV).

Metabolism

Primarily metabolized by CYP3A4. The N-demethylated metabolite is active.

Elimination

The terminal elimination half-life of eletriptan and the metabolite is approximately 4 and 13 h, respectively. The mean renal Cl is 3.9 L/h after oral administration. Nonrenal Cl accounts for approximately 90% of total Cl.

Special Populations

Renal Function Impairment

No significant change in Cl was observed with mild, moderate, or severe renal impairment, although BP elevations were observed.

Hepatic Function Impairment

Mild to moderate impairment results in an increase in both AUC (34%) and half-life, while the C max increased 18%.

Elderly

Increased half-life from approximately 4.4 to 5.7 h in elderly patients (65 to 93 y of age).

Gender

The pharmacokinetics are unaffected by gender.

Race

Japanese men had a 35% reduction in eletriptan exposure.

Menstrual cycle

Pharmacokinetics remained consistent throughout the phases of the menstrual cycle.

Indications and Usage

Acute treatment of migraine with or without aura.

Contraindications

Cerebrovascular syndromes (including strokes of any type or transient ischemic attacks); coronary artery vasospasm (including Prinzmetal variant angina); hemiplegic or basilar migraine; hypersensitivity to any component of the product; ischemic heart disease (eg, angina pectoris, history of MI, documented silent ischemia); peripheral vascular disease (including ischemic bowel disease); severe hepatic impairment; significant underlying CV disease; symptoms or findings consistent with ischemic heart disease; uncontrolled hypertension; use within 24 h of treatment with another 5-HT 1 agonist or an ergotamine-containing or ergot-type medication (eg, dihydroergotamine, methysergide).

Dosage and Administration

Adults

PO 20 to 40 mg single 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.

Storage/Stability

Store between 59° and 86°F.

Drug Interactions

Ergot derivatives (eg, dihydroergotamine)

Risk of vasospastic reactions may be increased. Concomitant use within 24 h of eletriptan is not recommended.

Linezolid, SNRIs (eg, duloxetine, venlafaxine), SSRIs (eg, citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)

The risk of serotonin syndrome (eg, agitation, altered consciousness, ataxia, myoclonus, overactive, reflexes, shivering) may be increased. If concomitant treatment is clinically warranted, appropriate observation of the patient is advised.

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)

Eletriptan should not be used within 72 h of drugs that are potent CYP3A4 inhibitors.

Propranolol

Eletriptan concentrations may be increased. However, no increases in BP were observed. No eletriptan dosage adjustment appears to be needed for patients taking propranolol.

Adverse Reactions

Cardiovascular

Palpitation (at least 1%); coronary artery vasospasm, MI, transient myocardial ischemia, ventricular fibrillation, ventricular tachycardia.

CNS

Asthenia (10%); dizziness, somnolence (7%); headache, paresthesia (4%); hypertonia, hypesthesia, vertigo (at least 1%); seizures (postmarketing).

Dermatologic

Sweating (at least 1%).

GI

Nausea (8%); dry mouth (4%); abdominal pain or discomfort, dyspepsia, dysphagia (eg, throat tightness, difficulty swallowing), stomach pain, cramps, or pressure (2%).

Musculoskeletal

Back pain (at least 1%).

Respiratory

Pharyngitis (at least 1%).

Miscellaneous

Pain, tightness, or pressure of chest (4%); chills, pain (at least 1%).

Precautions

Monitor

Assess pain location, intensity, duration, and associated symptoms of migraine attack and response to treatment. Monitor for an increase in BP, especially in renal impairment and elderly patients. Perform a CV evaluation prior to first use and obtain an ECG on the first use during the initial interval following administration in patients with risk factors for cardiac ischemia. Perform periodic CV evaluations in patients who have or acquire risk factors predictive of coronary artery disease (CAD) and are intermittent long-term users of eletriptan.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

BP was increased to a greater extent in the elderly.

Hepatic Function

Contraindicated in patients with severe hepatic impairment.

Blood pressure elevation

Significant BP elevations, including hypertensive crisis, have been reported with administration of 5-HT 1 agonists.

Cerebrovascular events

Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists, and some have resulted in fatalities.

Chest, jaw, or neck tightness

Sensations of tightness, pain, pressure, and heaviness in the precordium, throat, and jaw have been reported after treatment. These symptoms have not been associated with arrhythmias or ischemic ECG changes.

CV/Cardiac events

It is recommended that eletriptan not be given to patients in whom unrecognized 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 y). 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.

Melanin binding

Because eletriptan binds to melanin, it may accumulate in melanin-rich tissues (eg, eye), possibly causing toxicity after extended use.

Serotonin syndrome

Life-threatening serotonin syndrome may occur, particularly when combined with serotonin reuptake inhibitors.

Vasospasm-related events

Both peripheral vascular ischemia and colonic ischemia with abdominal pain and bloody diarrhea have been reported with 5-HT 1 agonists.

Overdosage

Symptoms

Hypertension or other more serious CV symptoms may occur.

Patient Information

  • Advise patient to read the patient information leaflet before starting therapy and again with each refill.
  • Explain that drug is to be used only during migraine and does not prevent or reduce the number of attacks. Emphasize that drug is used only to treat an actual migraine attack and should not be used to prevent migraine headaches or treat headaches caused by other conditions.
  • Advise patient that drug is to be taken as soon as symptoms of migraine appear. A second dose may be taken if symptoms return, but no sooner than 2 h following the first dose. For a given attack, if there is no response to the first tablet, do not take a second tablet without first consulting with health care provider. Do not take more than 2 tablets in any 24-h period.
  • Advise patient that safety of treating more than 3 headaches in a 30-day period has not been established and to inform health care provider if headaches are occurring more frequently.
  • Advise patient to immediately notify health care provider if any of the following occur after taking a dose of eletriptan: severe chest pain or chest pain that does not go away; sudden and/or severe stomach pain; shortness of breath; wheezing; swelling of the eyelids, face, or lips.
  • Advise patient that if tightness, pain, pressure, or heaviness in chest, throat, neck, or jaw occurs when using eletriptan, to discuss these symptoms with health care provider before using again.
  • Advise patient to notify health care provider if feelings of tingling, heat, flushing, tiredness, dizziness, heaviness, or pressure after treatment occur.
  • Advise patient that drug may cause fatigue or dizziness and to use caution while driving or performing other activities requiring mental alertness.
  • Advise patient to avoid unnecessary exposure to sunlight or tanning lamps and to use sunscreen and wear protective clothing to avoid photosensitivity reactions.
  • Instruct patient to continue to take migraine prophylactic medications daily as directed.
  • Advise patient not currently taking a migraine prophylactic drug to discuss the use of such drugs with health care provider.

Copyright © 2009 Wolters Kluwer Health.

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