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pharmachologic effect

The tablets of the drug are an anti-migraine agent. buy augmentin online A specific and selective agonist of 5-HT1-serotonin receptors, localized mainly in the blood vessels of the brain, and does not affect other subtypes of 5-HT-serotonin receptors (5-HT2-7). It causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues with blood (dilation of the vessels of the meninges and / or their edema is the main mechanism for the development of migraine in humans), without significantly affecting the cerebral blood flow.

It inhibits the activity of the terminal receptors of afferent trigeminal fibers in the dura mater (as a result, the release of sensory neuropeptides decreases). Eliminates nausea and photophobia associated with a migraine attack. In 50-70% of cases, it quickly eliminates an attack when taken orally at a dose of 25-100 mg. Within 24 hours in 1/3 of cases, relapse may develop, requiring repeated use.

The onset of action is 30 minutes after ingestion at a dose of 100 mg and 10-15 minutes after intranasal administration of 20 mg.

Pharmacological properties

Sumatriptan has two mechanisms of action when used:

 

  • excitation of serotonin 5-HT1 receptors of the muscles of the vessels of the carotid arteries, smooth muscle narrows under the action of the substance;
  • the drug blocks the production of sensory neuropeptides.

 

With the expansion of blood vessels, the brain receives a lot of blood, which leads to the formation of migraine. It does not have an analgesic effect, therefore, the use to eliminate other forms of headaches is not relevant.

Pharmacokinetics

After oral administration, it is rapidly absorbed. 70% of the maximum plasma concentration is reached after 45 minutes. Cmax in plasma is 54 ng / ml. Bioavailability - 14% (due to presystemic metabolism and incomplete absorption). Plasma protein binding is 14-21%.

It is metabolized by oxidation with the participation of monoamine oxidase (mainly isoenzyme A) with the formation of metabolites, the main of which are the indolacetic analog of sumatriptan, which does not have pharmacological activity against 5-HT1-serotonin receptors, and its glucuronide. It is excreted by the kidneys, mainly in the form of metabolites..

Driving a car while taking pills

The instructions for use with sumatriptan indicate that drowsiness may develop with course treatment. http://en.m.wikipedia.org/wiki/Sumatriptan The presence of migraine in itself affects the ability to drive a vehicle. Doctors recommend giving up driving during periods of acute bouts of pain and treatment with sumatriptan.

If a person is engaged in activities associated with increased risks and depending on concentration of attention, it is better to stop work during treatment with the drug for a while. Possible slowdown of psychomotor reactions when taking medication.