Axert: Full Drug Profile

Axert - General Information

Axert is a triptan drug for the treatment of migraine headaches. Axert is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and stopping the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Axert does not prevent migraine attacks.

Pharmacology of Axert

Axert is a selective 5-hydroxytryptamine receptor subtype agonist indicated for the acute treatment of migraine attacks with or without aura in adults. Axert is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine. Axert is an agonist for a vascular 5-hydroxytryptamine receptor subtype (probably a member of the 5-HT_1D family) having only a weak affinity for 5-HT_1A, 5-HT_5A, 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 Axert 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 Axert in humans.

Axert for patients

Axert Interactions

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 C_max of approximately 6%. No dose adjustment is necessary.

Other 5-HT_1B/1D Agonists

Concomitant use of other 5-HT_1B/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.

Axert Contraindications

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 uncontrolled hypertension.

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 its ingredients.

Additional information about Axert

Axert Indication

For the treatment of acute migraine headache in adults

Mechanism Of Action

Axert binds with high affinity to human 5-HT_1B and 5-HT_1D receptors leading to cranial blood vessel constriction.

Drug Interactions

Citalopram Increased risk of CNS adverse effects

Food Interactions

Take without regard to meals.

Generic Name

Almotriptan

Drug Category

Anti-migraine Agents; Anti-inflammatory Agents; Vasoconstrictor Agents; Selective Serotonin Agonists

Drug Type

Small Molecule; Approved

Other Brand Names containing Almotriptan

Axert; Almogran;

Protein Binding

35%

Half Life

3-4 hours

Dosage Forms of Axert

Tablet Oral

Chemical IUPAC Name

N,N-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indol-3-yl]ethanamine

Chemical Formula

C17H25N3O2S

Almotriptan on Wikipedia

https://en.wikipedia.org/wiki/Almotriptan

Organisms Affected

Humans and other mammals