Chemical structure of sumatriptan
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Sumatriptan

Sumatriptan (Imitrex®, Imigran®) is a triptan drug originally developed by Glaxo for the treatment of migraine headaches. Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers. Sumatriptan was the first triptan available (in 1993), and is available only by prescription in the United States. more...

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Mode of action

Sumatriptan is a 5-HT (5-HT1D) agonist. The specific receptor subtype it activates is present in the cranial and basilar arteries. Activation of these receptors causes vasoconstriction of those dilated arteries. Sumatriptan is also shown to decrease the activity of the trigeminal nerve.

Pharmacokinetics

Sumatriptan is administered in several forms; tablets, subcutaneous injection, and nasal spray. Oral administration (as succinate) suffers from poor bioavailability, partly due to presystemic metabolism — some of it gets broken down in the stomach and bloodstream before it reaches the target arteries. A new rapid-release tablet formulation has the same bioavailability, but the maximum concentration is achieved on average 10-15 minutes earlier. When injected, sumatriptan is faster acting (usually within a minute), but the effect lasts for a shorter time. Sumatriptan is metabolised primarily by monoamine oxidase A into an indole acetic acid analogue, part of which is further conjugated with glucuronic acid. These metabolites are excreted in the urine and bile.

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Overcoming GI stasis: new fast-dissolving sumatriptan relieves migraine
From OB/GYN News, 4/1/04 by Norra MacReady

RANCHO MIRAGE, CALIF. -- A new rapid-release formulation of sumatriptan has proved superior to placebo at relieving migraines within 2 hours when taken early in the attack, according to the findings of a randomized, double-blind, multicenter trial.

This formulation was developed for improved gastric disintegration and dispersion in order to overcome the gastrointestinal stasis that occurs with many migraine attacks. It has been available in the United States since January, Diane Boswell said at a meeting sponsored by the Diamond Headache Clinic.

In an intention-to-treat analysis, 66% of the patients who took 100 mg of the new formulation while their pain was still mild were pain free within 2 hours, compared with 51% of patients taking a 50-mg dose and 20% of patients taking the placebo. All differences were statistically significant.

This compares favorably with the action of conventional sumatriptan tablets, said Ms. Boswell, of the department of clinical development and medical affairs at Glaxo-SmithKline UK, which sponsored the study.

A total of 432 patients (359 women, 73 men) with a mean age of 41 years were included in the analysis: 142 in the high-dose group, 137 in the low-dose group, and 153 in the placebo group. The subjects, who experienced a mean of three migraines per month, were instructed to take the medication during the mild phase of a single migraine attack. Their mean time to treatment was 30 minutes. Attacks that started with moderate to severe pain were not studied.

The study's primary end point was complete absence of headache pain within 2 hours of taking the medication.

By 2 hours post treatment, 60% and 53% of the patients taking the 100-mg dose and 50-mg dose, respectively, said they were able to function normally at work or their usual activities, compared with 28% of patients in the placebo group.

Nausea and vomiting were the most commonly reported adverse events. The rate of all adverse events among patients taking the 100-mg formulation was 20%, compared with 14% among patients taking 50 mg sumatriptan and 12% among those taking the placebo.

BY NORRA MACREADY

Los Angeles Bureau

COPYRIGHT 2004 International Medical News Group
COPYRIGHT 2004 Gale Group

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