DrugindexOnline^{2nd edition}

Pronouncation: (ell-eh-TRIP-tan HIGH-droe-BROE-mide)
Class: Serotonin 5-HT ₁ receptor agonist

Trade Names:
Relpax
- Tablets 24.2 mg
- Tablets 48.5 mg

Mechanism of Action

Pharmacology

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

Pharmacokinetics

Absorption

Eletriptan is well absorbed, reaching a peak plasma level in approximately 1.5 h. The mean absolute bioavailability is approximately 50%.

Distribution

Eletriptan is approximately 85% protein bound. The Vd is 138 L after IV injection.

Metabolism

The N-demethylated metabolite is active.

Elimination

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.

Special Populations

Hepatic Function Impairment

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).

Indications and Usage

Acute treatment of migraine with or without aura.

Contraindications

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).

Dosage and Administration

Adults

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.

Storage/Stability

Store at controlled room temperature (59° to 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.

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.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

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

CNS

Dizziness, somnolence (7%); headache (4%); hypertonia, hypesthesia, paresthesia, vertigo (at least 1%).

Dermatologic

Sweating (at least 1%).

GI

Nausea (8%); dry mouth (4%); dyspepsia, dysphagia (eg, throat tightness, difficulty swallowing) (2%).

Respiratory

Pharyngitis (at least 1%).

Miscellaneous

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%).

Precautions

Monitor Symptoms of migraine attack Assess pain location, intensity, duration, and associated symptoms of migraine attack and response to treatment.

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

There is an increased t _½ (from about 4.4 to 5.7 h) in the elderly (65 to 93 yr of age).

CV/Cardiac events

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.

Cerebrovascular events

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

Hypertensive crisis

Elevation in BP, including hypertensive crisis, have been reported with administration of 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 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 frovatriptan: severe chest pain or chest pain that does not go away; sudden and/or severe stomach pain; shortness of breath; wheezing; swelling of eyelids, face, or lips.
• Advise patient that if tightness, pain, pressure or heaviness in chest, throat, neck, or jaw occurs when using sumatriptan, 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.