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:
DrugBank: Interactions for Almotriptan
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.
Chemical IUPAC Name: N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]-ethanamine
Chemical Formula: C17H25N3O2S
Half Life: 3-4 hours
Drug Type: Approved Drug
# Accession No: APRD00169
CAS Registry Number: 181183-52-8
