Brands, Medical Use, Clinical Data
- Anti-migraine Agents
- Anti-inflammatory Agents
- Vasoconstrictor Agents
- Selective Serotonin Agonists
Brands / Synonyms
For the treatment of acute migraine headache in adults
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.
Biotrnasformation / Drug Metabolism
AXERT® (almotriptan malate) Tablets should not be given to patients with ischemic heart
disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or to patients who have
symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm, including Prinzmetal's
variant angina, or other significant underlying cardiovascular disease.
Because AXERT® may increase blood pressure, it should not be given to patients with
AXERT® should not be administered within 24 hours of treatment with another 5-HT1 agonist, or an
ergotamine-containing or ergot-type medication like dihydroergotamine or methysergide.
AXERT® should not be given to patients with hemiplegic or basilar migraine.
AXERT® is contraindicated in patients who are hypersensitive to almotriptan or any of
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
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.
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.