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Eletriptan: profile and news
Health calendar: 2/1/06 Jan 31, 2006 Health calendar: 2/1/06 Jan 31, 2006 Eletriptan 40 mg Efficacious in Patients with Migraine at Risk of ... Oct 17, 2005 Headache Recurrence and Efficacy of Eletriptan in Caucasian and ... Oct 17, 2005 New Be Stronger Than Your Migraine Campaign to Help Sufferers ... Jun 29, 2005 Neurogen Corporation Announces Dr. Stephen Uden Appointed ... Jun 22, 2005 Neurogen Corporation Announces Dr. Stephen Uden Appointed ... Jun 22, 2005 E-prescribing System Had No Effect on Formulary Compliance or ... Jun 6, 2005 Health calendar: 4/5/05 Apr 4, 2005 Health calendar: 4/5/05 Apr 4, 2005 Triptan Nonresponder Studies: Implications for Clinical Practice Mar 7, 2005 Triptan Nonresponder Studies: Implications for Clinical Practice Mar 7, 2005 Other information Indication For the treatment of acute migraine headache in adults Pharmacology Almotriptan is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Almotriptan is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Almotriptan is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT1D family) having only a weak affinity for 5-HT1A, 5-HT5A, and 5-HT7 receptors and no significant affinity or pharmacological activity at 5-HT2, 5-HT3 or 5-HT4 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic, dopamine1,; dopamine2; muscarinic, or benzodiazepine receptors. This action in humans correlates with the relief of migraine headache. In addition to causing vasoconstriction, experimental data from animal studies show that Almotriptan also activates 5-HT1 receptors on peripheral terminals of the trigeminal nerve innervating cranial blood vessels, which may also contribute to the antimigrainous effect of Almotriptan in humans. Mechanism Of Action Almotriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to cranial blood vessel constriction. Drug Category Anti-migraine Agents; Anti-inflammatory Agents; Vasoconstrictor Agents; Selective Serotonin Agonists; ATC:N02CC05 Brand Names/Synonyms Almotriptan; Axert; Eletriptan Dosage Forms TABLET Absorption Not Available Interactions -->Interactions for Almotriptan: Ergot-Containing Drugs These drugs have been reported to cause prolonged vasospastic reactions. Because there is a theoretical basis that these effects may be additive, use of ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide) and AXERT® within 24 hours of each other should be avoided. Monoamine Oxidase Inhibitors Coadministration of moclobemide resulted in a 27% decrease in almotriptan clearance and an increase in Cmax of approximately 6%. No dose adjustment is necessary. Other 5-HT1B/1D Agonists Concomitant use of other 5-HT1B/1D agonists within 24 hours of treatment with AXERT® is contraindicated. Propanolol The pharmacokinetics of almotriptan were not affected by coadministration of propranolol. Selective Serotonin Reuptake Inhibitors (SSRIs) SSRIs (e.g., fluoxetine, fluvoxamine, paroxetine, sertraline) have been rarely reported to cause weakness, hyperreflexia, and incoordination when coadministered with 5-HT1 agonists. If concomitant treatment with AXERT® and an SSRI is clinically warranted, appropriate observation of the patient is advised. Verapamil Coadministration of almotriptan and verapamil resulted in a 24% increase in plasma concentrations of almotriptan. No dose adjustment is necessary. Ketoconazole and Other Potent CYP3A4 Inhibitors Coadministration of almotriptan and the potent CYP3A4 inhibitor ketoconazole (400 mg q.d. for 3 days) resulted in an approximately 60% increase in the area under the plasma concentration-time curve and maximal plasma concentrations of almotriptan. Although the interaction between almotriptan and other potent CYP3A4 inhibitors (e.g., itraconazole, ritonavir, and erythromycin) has not been studied, increased exposures to almotriptan may be expected when almotriptan is used concomitantly with these medications. Drug/Laboratory Test Interactions AXERT® is not known to interfere with commonly employed clinical laboratory tests.
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