Axert (almotriptan malate) tabletsCompany: Pharmacia & Upjohn
Approval Status: Approved May 2001
Treatment for: Migraine with or without aura in adults
Areas: Neurology & Nervous System
Axert has been approved by the FDA for the acute treatment of migraine with or without aura in adults. Axert belongs to a class of drugs known as selective serotonin receptor agonists. These drugs target serotonin receptors and act against migraine headaches by inducing the constriction of blood vessels surrounding the brain.
Migraine attacks are characterized by severe unilateral head pain, which lasts between four and 72 hours. Attacks are often are accompanied by nausea, vomiting and sensitivity to light and/or sound. Approximately 28 million Americans suffer from migraine headaches, with women experiencing migraines at least three times more often than men. For many sufferers, these headaches have a significant impact on their quality of life.
Pharmacia plans to market Axert in the United States under a licensing agreement with Almirall Prodesfarma, SA, Spain. The drug is also approved in the European Union.
Results of controlled clinical trials demonstrated that Axert was highly effective and well tolerated. Data showed that Axert (12.5 mg and 6.25 mg) produced significant relief from migraine headache pain at two hours, with efficacy rates ranging from 57% to 65% (12.5 mg) and 55% to 56% (6.25 mg) compared to placebo.
Side effects associated with the use of Axert include (but are not limited to) the following:
- Paresthesia (tingling or numbness)
- Dry mouth
In controlled trials, Axert showed a low percentage of side effects characteristic of triptans. However, this class of compounds has the potential to cause coronary vasospasm, and as a result Axert is not advised for patients with ischemic or vasospastic coronary artery disease.
Mechanism of Action
Axert Tablets contain almotriptan malate, a selective 5-hydroxytryptamine 1B/1D (5-HT 1B/1D) receptor agonist. Almotriptan binds with high affinity to 5-HT 1D, 5-HT 1B and 5-HT 1F receptors. Almotriptan has weak affinity for 5-HT 1A and 5-HT 7 receptors, but has no significant affinity or pharmacological activity at 5-HT 2, 5-HT 3, 5-HT 4, 5-HT 6; alpha or beta adrenergic; adenosine (A1, A2); angiotensin (AT 1, AT 2); dopamine (D1, D2); endothelin (ET A, ET B); or tachykinin (NK 1, NK 2, NK 3) binding sites.
Current theories on the etiology of migraine headache suggest that symptoms are due to local cranial vasodilation and/or to the release of vasoactive and pro-inflammatory peptides from sensory nerve endings in an activated trigeminal system. The therapeutic activity of almotriptan in migraine can most likely be attributed to agonist effects at 5-HT 1B/1D receptors on the extracerebral, intracranial blood vessels that become dilated during a migraine attack, and on nerve terminals in the trigeminal system. Activation of these receptors results in cranial vessel constriction, inhibition of neuropeptide release and reduced transmission in trigeminal pain pathways. (from Axert Prescribing Information)
More information on migraine headaches can be found at the National Headache Foundation.
Axert Drug Information
The Axert drug information shown above is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.