Drug information of eletriptan

eletriptan

Drug group:

Eletriptan is a second generation triptan drug for the treatment of migraine headaches.

Mechanism of effect

Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors.

Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache.

The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

Pharmacodynamic

Eletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses.

While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat.

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

Drug indications

Migraine

Dosage

Migraine Headache

Adult

20-40 mg PO at onset of symptoms; repeat dose after 2 hr if necessary

Not to exceed 80 mg/day

Pediatric

<18 years old: Not recommended

Drug contraindications

Angioedema , basilar migraine

Alerts

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

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

Points of recommendation

Avoid driving and doing other tasks or actions that call for you to be alert until you see how eletriptan affects you.

Use care if you have risks for heart disease (high blood pressure, high cholesterol, overweight, high blood sugar or diabetes, cigarette smoking, man older than 40 years of age, other family members with early heart disease, woman after change of life). Talk with your doctor.

Taking more of eletriptan (a higher dose, more often) than your doctor told you to take may cause your headaches to become worse.

Have your blood pressure checked often. Talk with your doctor.

If you are 65 or older, use eletriptan with care. You could have more side effects.

Take with or without food.

Take with liquids as early as you can after the attack has started.

If your headache comes back after the first dose, 1 more dose may be taken 2 hours after the first one.

Pregnancy level

C


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