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Brand Name: Axert
Active Ingredient: almotriptan malate
Indication: Treatment of acute migraine headache in adults
Company Name: Pharmacia & Upjohn
Availability: NDA filed with FDA on December 17, 1999

Axert: Introduction

During a migraine headache attack, changes in brain activity induce inflammation of blood vessels and nerves in the head. Attacks may be triggered by alcohol, certain foods, too much or too little sleep, menstruation, emotional stress, or environmental factors. The “triptan” family of drugs, which bind to serotonin receptors in the brain, is currently the most effective class of agents for treating migraine headache. Sumatriptan (Imitrex, manufactured by Glaxo Wellcome) was the first serotonin agonist to be approved for treating migraine, but the search continues for even more effective agents with fewer side effects.

Axert (almotriptan malate) is one such drug, marketed by Pharmacia & Upjohn and developed by Almirall Prodesfarma, S.A., Spain, where the drug is currently available. Pharmacia & Upjohn filed an New Drug Application for Axert with the FDA on December 17, 1999, for the treatment of acute migraines in adults, and the FDA is currently evaluating data on the drug’s safety and effectiveness. Data presented at the annual meeting of the American Academy of Neurology (AAN) in May 2000 indicate that Axert is as effective as sumatriptan, but with fewer adverse side effects.

Axert: Clinical Study Results

In one reported at the AAN meeting, 1,173 adult patients took a single dose of either Axert 12.5 mg (591 patients) or Imitrex 50 mg (582 patients) at the onset of a migraine attack. Both treatments relieved pain within two hours after taking the drug (58% for Axert vs. 57% for Imitrex). Similar pain relief was also observed between the treatment groups at 30 minutes and one hour.

Fifteen percent of patients treated with Axert experienced side effects compared with 19% of Imitrex patients. A significant difference was reported in the number of patients reporting chest pain: 0.3% of the group treated with Axert and 2.2% of the Imitrex group. The most frequently reported side effects, each of which was reported by less than 3.5% of patients in either group, were nausea, dizziness, and sleepiness. Patients receiving Axert reported that they were less bothered by side effects than those receiving Imitrex.

In another study reported at the meeting — a six-month trial to study long-term safety — 582 adult patients took Axert to relieve the pain from a total of 10,605 migraine attacks. Two hours after administration, patients experienced pain relief in 76% of the attacks. Patients reported being pain-free at two hours in 49% of attacks. In 1,718 migraine relapses that occurred within 24 hours, taking a second dose of Axert relieved pain in 86% and abolished pain in 59% at two hours.

Axert: What You Should Know

The most frequent side effects associated with Axert are nausea, dizziness, and drowsiness. Patients who are also taking propranolol may do so in conjunction with Axert without any interaction.

New drug trials suggest that Pfizer’s drug Relpax (eletriptan) may be one of the most effective drugs for the treatment of migraine headaches. Researchers at Memorial University in St. John’s Newfoundland, conducted a randomized trial in 774 patients using 40 mg and 80 mg doses of eletriptan compared to 50 and 100 mg doses of the drug sumatriptan. It was found that 67 percent of the eletriptan 80 mg patients and 64 percent of the eletriptan 40 mg patients were pain-free two hours after dosing, compared to 53 percent of the patients who received sumatriptan 100 mg and 50 percent of those who received 50 mg. Two hours after dosing, 65 percent of patients in the eletriptan 80 mg group were able to resume at least some normal activities, compared to just 51 percent of patients in the 100 mg sumatriptan group. Results of the trials were presented by Dr. William Pryse-Phillips, neurologist and director of the migraine clinic at Memorial University, at the 9th Congress of the International Headache Society meeting in Barcelona, Spain.

If you are a woman between ages 20 and 44 years and suffer from migraine headaches you may have an increased risk for ischemic stroke. In this type of stroke the brain cells do not get enough oxygen, usually because either the vessel itself has narrowed-which may be a temporary condition-or the blood vessel is blocked by a clot or plaque. The lower level of oxygen causes cells to die. Symptoms, including migraines, vary according to the part of the brain affected.

A family history of migraines also increases your risk for both ischemic and hemorrhagic strokes even if you do not have them yourself. Hemorrhagic stroke occurs when a vessel breaks, allowing blood to bleed into the brain. This deprives cells upstream of an oxygen supply and they die. If enough blood escapes and puts pressure on other vessels, circulation and oxygen will be cut off to other areas of the brain

High blood pressure, use of birth control pills, and/or smoking increase this risk significantly because they cause blood vessels to constrict and limit blood flow to the brain. Changes in frequency or type of migraines were not found to be a predictor of stroke in study participants who use birth control pills. However, if taking birth control pills you should tell the physician prescribing them about your migraines or any other type of headache you experience.

Up to 40 percent of strokes occurring in women with migraines may develop directly from this type of headache.

Synthesizing the results of three previous studies, researchers from the Headache Care Center in Springfield, Missouri, concluded that one 2.5 mg dose of zolmitriptan (Zomig) may provide long-term relief from migraines.

The findings, which were presented at the Diamond Headache Clinic’s Headache Update `99, analyze the compiled data of three different studies. Each study compared groups of participants that took either zolmitriptan (Zomig) or a placebo, though no one knew which pill they were taking.

The studies show that migraines most often occur between six and seven in the morning when people are getting ready for work and school. Taking the medication between 6 and 9 a.m. provided headache relief for an average of 23 hours for those who responded to the medication. Participants who responded to the placebo had an average relief time lasting only eight hours.

Approximately 60 percent of those taking a single dose (2.5 mg) of zolmitriptan had a positive response within two hours of taking the drug, whereas only 22 to 39 percent of the people taking the placebo responded positively in that amount of time.

The researchers concluded that zolmitriptan (Zomig) does provide long-acting, reliable relief for migraine, despite the time of day the headache occurs.

The manufacturer suggests that the medication is appropriate to treat acute migraines in adults, either with or without an aura. It’s not recommended if you have hypertension, ischemic heart disease, or another significant type of heart condition.

Side effects include feelings of pain, pressure, and heaviness or tightness in various parts of the body, including the chest. Adverse effects that appeared during clinical trials ranged from mild to moderate, with the most prevalent being asthenia (weakness), dizziness, and nausea.

The discovery of a feedback system that’s active during a migraine headache has researchers at the University of Iowa questioning some of the traditional theories about migraine headaches.

The team found that inflammatory agents released during a migraine seem to signal certain nerve cells (neurons) in your brain to increase production of a neuropeptide, calcitonin gene-related peptide, or CGRP. One result of CGRP’s presence is to stimulate your brain tissue to release more inflammatory agents. The new inflammatory agents send more signals to the neurons to release more CGRP, the cycle continues, and so does your migraine.

At present, the most effective migraine medication on the market is sumatriptan, which provides relief for 50 to 75 percent of the people who use it. Even though scientists know it works, they don’t understand why or how.

While studying the drug, the Iowa researchers discovered that sumatriptan keeps calcium levels high in the neurons. In most cases, a high-calcium level also means a high level of neuropeptides in the affected neurons. However, when the participants took sumatriptan, CGRP didn’t increase, which may be one reason why this drug works so well against migraines. If the CGRP doesn’t increase, then the inflammatory agent-CGRP cycle described earlier is broken.

Interestingly, the same signal (calcium release) can give two different reactions depending on the strength and duration of the signal. A short, fast burst of calcium causes an increase in the CGRP, which continues the cycle and your headache. However, if the calcium increase is a slow, steady rise, it actually lessens the amount of CGRP that is released. Researchers believe it is this second type of calcium increase that sumatriptan brings about.

As a follow-up to this study, researchers will look for the exact mechanism for the initial release of CGRP, with the hope that blocking this action would divert the migraine.

Those who suffer cluster headaches may have non-painful warnings that the headaches are going to occur anywhere from several days to several weeks before their onset, according to a study done by researchers at the Universidad Nacional de Rosario in Argentina.

Four patients in the study described various symptoms that preceded the onset of cluster headaches. The first patient’s symptoms were described as “eye discomfort,” a heightened state of anxiety, and a feeling of having “something inside my head.”

The second patient complained of eye discomfort that was aggravated by reading or noise. The third patient reported feeling numbness in the left temple about a week before the onset of the headaches. And the last patient described discomfort on the right side of the head.

Cluster headaches are similar to migraines and occur as often as two or three times a day over a period of weeks. They come on suddenly, and sufferers experience throbbing pain behind the nostril and one eye. The attacks rarely last longer than two hours, and it may be weeks or months in between attacks.

This study is important, said researchers, because it demonstrates that “changes occur in the nervous system that anticipate the autonomic (self-controlling) and painful manifestations.” Also, recognizing that warning symptoms can occur before the severe pain strikes is the first step in developing preventive treatment and a better understanding” of the cause of cluster headaches.

When brain images are taken of people who experience primary headaches, they’re normal. This has led scientists to believe that headaches come from dysfunction rather than an abnormality in the structure of the brain. However, researchers from the National Hospital for Neurology and Neurosurgery in London are suggesting that this conclusion may have been made in error.

Headaches not directly due to injury or disease are called primary headaches. Included in this category are tension, migraine, and cluster headaches. Magnetic resonance imaging (MRI) or computed tomography (CT) scans have consistently shown no structural abnormality in these people—until now.

With a new type of imaging called voxel-based morphometry, British researchers have conducted a study that shows that people with cluster headaches have an abnormality in the part of the brain called the hypothalamus. The hypothalamus lies deep in the brain and is responsible for maintaining a constant internal environment, including temperature and wakefulness, and carrying out certain behavior patterns—sexual behavior, physical expression of emotions, and pain and pleasure. It affects the nervous system directly and through hormones.

Researchers compared the brain images of 25 people with cluster headaches to the brain images of 29 people in the control group. Fourteen of the headache sufferers had a headache during the test.

The tests showed that all the people with cluster headaches had a greater density of grey matter in their hypothalamus. Researchers then compared the two groups using positron emission tomography (PET). The PET scans showed both structural and functional abnormalities in this same area of the hypothalamus.

Now that an exact area of the brain has been identified with cluster headaches, researchers are hoping to develop more effective treatments for these and other types of primary headaches.

However, they can’t say that the extra grey matter actually causes the headache, just that all the participants with cluster headaches had this hypothalamic density. Perhaps the increased density is the result of the headaches, not the cause. Further testing will be needed to explore the exact association between primary headaches and hypothalamic abnormality.