Imitrex and Migraine, By: Samir

IMITREX [Sumatriptan] is indicated in the use acute treatment of migraine.
Migraine: Migraine, the most common cause of headache, afflicts approximately 15% of women and 6% of men. It is a vascular headache, comes in attacks A useful definition of migraine is a benign and recurring syndrome of headache, nausea, vomiting, and/or other symptoms of neurologic dysfunction in varying admixtures. Migraine can often be recognized by its activators (Red wine, menses, hunger, lack of sleep, glare, estrogen, worry, perfumes, let-down periods) and its deactivators (sleep, pregnancy, exhilaration, triptans). Severe headache attacks, regardless of cause, are more likely to be described as throbbing and associated with vomiting and scalp tenderness. Milder headaches tend to be nondescript—tight, band like discomfort often involving the entire head—the profile of tension-type headache.
IMITREX [Sumatriptan] is a specific and selective 5-hydroxytriptamine1-like [5HT 1-like] receptor agonist with little or no effect at a variety of other receptor types. It produces dose related constriction in the cerebral circulation. It does not bind to alpha adrenergic, beta adrenergic, muscarinic, dopaminergic or benzodiazepine receptors
Interest in the role of 5-HT a.k.a. serotonin in migraine has been renewed due to the introduction of the triptan class of anti-migraine drugs. The triptans are designed to stimulate selectively a particular subpopulation of 5-HT receptors. At least 14 specific 5-HT receptors exist in humans. The triptans are potent agonists of 5-HT1B, 5-HT1D, and 5- HT1F receptors and are less potent at 5-HT1A and 5-HT1E receptors. A growing body of data indicates that the anti-migraine efficacy of the triptans relates to their ability to stimulate 5-HT1B receptors, which are located on both blood vessels and nerve terminals. Selective 5-HT1D receptor agonists have, thus far, failed to demonstrate clinical efficacy in migraine. Triptans that are weak 5-HT1F agonists are also effective in migraine; however, only 5-HT1B efficacy is currently thought to be essential for anti migraine efficacy
History: The development of sumatriptan was the first experimentally based approach to identify and develop a novel therapy for migraine. In 1972, Humphrey and colleagues initiated a long term project aimed at identifying novel therapy for migraine. The goal of this project was to develop selective vasoconstrictors of the extracranial circulation. They focused on the identification of 5-HT receptors in the carotid vasculature, on which the theory of action of traditional anti-migraine drugs was based during the 1970s. Sumatriptan, first synthesized in 1984, potently contracted the dog isolated saphenous vein which is believed to contain the novel 5-HT receptor located in the carotid circulation. Sumatriptan was approved by the FDA in 1992. Mechanism of action:
Before the onset of a migraine, the 5-HT/serotonin level in the brain becomes extremely low. Sumatriptan is structurally similar to serotonin, and is a 5-HT agonist, which is one of the receptors to which serotonin binds. 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 increases the 5-HT levels in the brain. Sumatriptan is also shown to decrease the activity of the trigeminal nerve, which probably accounts for sumatriptan's efficacy in treating cluster headaches. The injectable form of the drug has been shown to abort a cluster headache within fifteen minutes in 96% of cases. This type of headache is extremely painful and debilitating. The peak plasma concentration of IMITREX [Sumatriptan] i.e. on subcutaneous injection is approximately 12 mins and its bioavailability is approximately 97%. While on oral administration, the peak plasma concentration is 1 to 2 hours and bioavailability of only 14% to 17%.
Adverse effects and Contraindications:
Rare but serious cardiac effects have been associated with the administration of Sumatriptan, including coronary artery vasospasm, transient myocardial ischemia, atrial and ventricular arrhythmias, and myocardial infarction. Most such events have occurred in patients with risk factors for coronary artery disease. In general, however only minor side effects are seen with sumatriptan in the acute treatment of migraine. After subcutaneous injection of IMITREX [Sumatriptan], a majority of patients report transient mail pain, stinging, or burning sensation at the site of injection. Other side effects are: - Paresthesia - Asthenia and fatigue - Flushing - Feelings of pressure - Tightness - Pain in neck, chest and jaw - Drowsiness - Nausea - Sweating.
IMITREX [Sumatriptan] is contraindicated in patients who have a history of ischemic or vasospastic coronary artery disease, cerebrovascular or peripheral vascular disease, or other significant cardiovascular diseases. This drug is also contraindicated in patients in patients with uncontrolled hypertension and in those patients who are on monoamine oxidase inhibitors. It is not recommended for use in the pediatric age group and should not be used in the pregnant and lactating mothers.
Indication:
IMITREX [Sumatriptan] is effective in the acute treatment of migraine, with or without aura. The treatment should begin as soon as possible after the onset of a migraine attack. Approximately 70% of individuals report significant headache relief from a 6 mg subcutaneous dose of IMITREX [Sumatriptan]. This dose maybe repeated once within a 24-hour period if the headache doesn’t subside after the first dose of sumatriptan. It should not be used concurrently with or within 24 hours of an ergot derivative nor should it be used with another triptan with 24 hours of each other. IMITREX [Sumatriptan] is not useful for prophylaxis of migraine.
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Have you noticed anything particular triggering your headaches?

Help Your Doctor Help You With Your Headache.

Author: David Wilding 
   

 

 

 

Benign (harmless) headaches can sometimes be just as severe as those from a more sinister cause. The first concern of the Doctor is to make sure what is causing your headache. To do this, he relys on the person's descriptions of the symptoms, any pattern that the headaches may follow and any possible triggers.

Every single year, almost 75% of American suffer with headaches. They are often scared that they may have a brain tumor or a stroke.



Benign (harmless) headaches can sometimes be just as severe as those from a more sinister cause. The first concern of the Doctor is to make sure what is causing your headache. To do this, he relys on the person's descriptions of the symptoms, any pattern that the headaches may follow and any possible triggers.



So what sort of things will your Doctor be looking at? If you are planning to visit your Doctor because of headaches, this list will be a useful check point for you. Having the answers to these questions will help both you and your Doctor.



How long have these headaches been going on?



As a general rule, the longer you have been suffering a similar sort of headache – the more likely it is to be harmless (however debilitating or painful). Sufferers with migraine will often have started having them as a child, teen or young adult. Migraine may finish when a woman begins her menopause – but they can also start at that time, too. Tension headaches can start at any time.



Does anyone else in your family suffer with headaches? Migraines can often run in families but cluster headaches don’t.



How frequently do you suffer with these headaches?



Your doctor will want to you to tell him how many times a day, month or year you get headaches. This will help to decide whether the treatment should be:



Prophylactic (preventing the headaches from starting)

Abortive (trying to stop a headache attack that is already happening)



Has the pattern of your headaches changed – or are you getting them more often?



Many people struggle on with headaches for months or even years. What finally brings them to the Doctor is a change in that pattern or the headaches becoming more severe. The Doctor will want to know what is causing your headache and check out the things that might be making it worse.



When you have a headache, where is the pain located?



The location will help your Doctor to diagnose what type your headache is. For instance:



Migraine: anywhere in the head but most common in the temple area.

Tension headaches: Felt on one or both sides. May be in the front. Commonly most intense in the neck, shoulder and back of the head.

Cluster headaches: always on one side – usually around the eye. 



Try and describe the pain for me?

Again, this will help with the diagnosis:



Migraine: commonly throbbing or pulsating

Tension headache: dull, dragging ache – often tight band 

Cluster headaches: Deep and intensely painful as if something sharp and hot is being pushed into the eye



Do you have any other symptoms with the headache?



Migraine: losing appetite, feeling sick, being sick, dislike of light and/ or noise

Tension headaches: stiff or sore neck, grinding teeth at night, clenched jaw

Cluster headaches: watering eye, blocked nose



How long does the headache last?

· 

Migraine: commonly less than 24 hours. Or may be as short as 20 minutes or go on for weeks – although less common. Usually a pain-free period between migraines.

Tension headache: Can last for days, weeks and rarely, years.

Cluster headache: Very severe, but short. Usually 30-90 minutes, repeated 2-6 times during a ‘bout’



Do your headaches always seem to be at a particular time?



Migraine: The sufferer often wakes up with one. May happen more at weekends. Women with menstrual migraine may have them a few days before their period.

Tension headaches: Commonly during stressful times.

Cluster headaches: Often wake the person from a deep sleep at night.



Have you or your family noticed your behavior or mood changing because of the headaches?



Migraine: Person can become withdrawn, easily irritated and want to be on their own.

Tension headaches: Happy to receive care and attention.

Cluster headaches: The person may pace up and down, hold their head or rock during an attack.



Headache sufferers are at a higher risk of depression due to their condition (or sometimes the depression causes the condition).

Signs of depression that the Doctor is looking for are:



Poor sleeping – either too much or too little

Feeling tired all the time

Loss of appetite

Loss of interest in sex



Do you get any warning signs that a headache is going to start?



15% of all migraine sufferers may get a warning in the form of an ‘aura’. This is often seeing dazzling lights or zig-zag lines.

Numbness and/or noticing a distinctive odor are also auras.

If you have an aura that carries on after your headache has finished, make sure you tell the Doctor.







Headaches and migraines can have many triggers. If you know what yours are, that’s fine. If not, it may help to keep a headache diary – which includes what you have eaten and done during that day. This will help the Doctor to find out what is causing your headache and what type it is.



Knowing the answers to these questions will help your doctor determine the typr of headasche you have and the best way to combat the pain.