Almotriptan (Axert—Pharmacia Corporation) For Migraine
By William T. Elliott, MD, FACP, and James Chan, PharmD, PhD
The FDA has approved Pharmacia’s almotriptan malate for the treatment of migraine with or without aura in adults. The drug is touted as being as effective as other triptans, but with a favorable side effect profile, especially cardiovascular side effects. Almotriptan will be marketed by Pharmacia under the trade name "Axert."
Indications
Almotriptan is indicated for the acute treatment of migraine with or without aura in adults.
Dosage
The recommended dose of almotriptan is 6.25 mg or 12.5 mg initially. If the headache returns, the dose may be repeated after 2 hours. No more than 2 doses should be taken within a 24-hour period. The safety of using almotriptan for more than 4 headaches in a 30-day period has not been established. Patients with impaired renal or hepatic function should take an initial dose of 6.25 mg.1
Almotriptan is supplied as 6.25 mg and 12.5 mg tablets.
Potential Advantages
The incidence of chest pain associated with almotriptan in preclinical studies was lower than that reported for sumatriptan in premarketing studies.2 Single doses from 12.5 mg to 50 mg did not have a significant effect on the electrocardiography of healthy volunteers while doses of 25 mg and 50 mg had a small dose-related increase in systolic and diastolic blood pressure up to 4 hours postdose (2.78 and 4.17 mg Hg and 3.77 and 6.11 mg Hg, respectively).3 Animal studies also suggest a more favorable cardiovascular safety profile than sumatriptan.4 In a comparative assessment of almotriptan and sumatriptan, patients reported they were more satisfied with the side effects profile of almotriptan.5 Subjects were asked "how bothered" they were by any side effects of the study medication. No differences were reported in terms of pain relief, functional status, or health-related quality of life. Almotriptan, as with naratriptan, does not appear to interact with propranolol as some patients may be taking the latter for migraine prophylaxis.6
Potential Disadvantages
As with other 5-HT 1B/1D agonists, almotriptan is contraindicated in patients with documented ischemic heart disease or symptoms consistent with ischemic heart disease.1 Cerebrovascular (eg, stroke), vasospastic-related events (eg, colonic ischemia), and increases in blood pressure have been reported with 5-HT1 agonists.
Almotriptan is metabolized by monamine oxidase and, to a lesser degree, cytochrome P450 3A4 and 2D6. Inhibitors of MAO and CYP 3A4 are expected to reduce the elimination of almotriptan. Coadministration with SSRIs has been reported, albeit rarely, to cause weakness, hyperflexia, and incoordination.1
Comments
Almotriptan is a 5-HT 1B/1D receptor agonist similar to other triptans such as sumatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan. These drugs are thought to act on the receptors in meningeal arteries and trigeminovascular nerve endings.7 The newer agents have better oral bioavailability compared to sumatriptan. Their efficacy and recurrence rates appear to be similar with the possible exception of a lower efficacy with naratriptan and a lower recurrence rate and a faster onset with rizatriptan.8 Almotriptan is priced the same for either strength, about $11 per tablet.
Clinical Implications
Almotriptan provides another alternative for the oral management of migraine. While differences among the triptans appear small, there may be a greater interpatient difference in response and tolerance.7 Premarketing clinical studies suggest that almotriptan may have a low incidence of chest symptoms compared to what has been reported with sumatriptan. Chest symptoms have been reported as a frequent occurrence with sumatriptan, but are rarely significant.9 There are no comparative studies among the triptans specifically assessing differences in chest pain. Some difference may be attributed to variations in subject inclusion and a wider definition of chest pain. Until there are data to clearly differentiate among the triptans, they are all contraindicated in patients with suspected or documented ischemic heart disease.
References
1. Axert Product Information. Pharmacia Corporation. May 2001.
2. Dodick DW. Headache. 2001;41(5):449-455.
3. Boyce M, et al. J Cardiovasc Pharmacol. 2001;37(3):280-289.
4. Gras J, et al. Eur J Pharmacol. 2000;410(1):53-59.
5. Colman SS, et al. Clin Ther. 2001;23(1):127-145.
6. Fleishaker JC, et al. Clin Pharmacol Ther. 2000;67(5):498-503.
7. Deleu D, Hanssens Y. J Clin Pharmacol. 2000;40(7):687-700.
8. Tfelt-Hansen P, et al. Drugs. 2000;60(6):1259-1287.
9. Visser WH, et al. Cephalalgia. 1996;16(8):554-559.
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