Sumatriptan

Sumatriptan, a member of the triptan class of medications, is a widely used treatment for migraine and cluster headaches. Recognized for its vasoconstrictive properties, Sumatriptan functions by selectively binding to and activating serotonin 5-HT1D receptors located in the central nervous system (CNS). This action leads to the constriction of cerebral blood vessels, often resulting in headache relief.

Sumatriptan

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Mechanism of Action

The primary mechanism of Sumatriptan's efficacy lies in its interaction with the 5-HT1D receptors in the CNS, which results in cerebral vasoconstriction. As the dilation of blood vessels is believed to be related to migraine and cluster headaches, Sumatriptan's ability to induce vasoconstriction may lead to relief from these conditions.

Additionally, Sumatriptan may influence the pathophysiology of migraines by decreasing the release of vasoactive neuropeptides from the trigeminal nerve's perivascular axons within the dura mater. It also potentially reduces the extravasation of plasma proteins, thereby reducing inflammation. Furthermore, it may suppress the release of other inflammation mediators from the trigeminal nerve.

Clinical Use

Sumatriptan is indicated for acute treatment of migraine attacks with or without aura, as well as the treatment of cluster headaches. It is not designed for prophylactic therapy to prevent future attacks or to reduce the frequency of attacks. It should only be used where a clear diagnosis of migraine or cluster headache has been established.

Adverse Effects

The most commonly reported side effects of Sumatriptan are tingling, warmth, flushing, and feelings of discomfort or pressure, which are generally transient. More serious side effects such as chest pain and tightness may occur and require medical attention. Sumatriptan should be used with caution in individuals with underlying heart conditions due to its vasoconstrictive action.

Pharmacokinetics

Orally administered Sumatriptan is well absorbed in the digestive tract but has low bioavailability due to first-pass metabolism in the liver. It is primarily excreted in urine, with a minor amount excreted in feces. The half-life of Sumatriptan is approximately 2.5 hours.

Sumatriptan Resources
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See Also

• Migraine
• Cluster headache
• Serotonin
• 5-HT1D receptor