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The Discovery and Development of the Triptans, a Major Therapeutic Breakthrough

As the first highly effective and well-tolerated drug for the acute treatment of migraine, it was hailed as a medical breakthrough. Many clinicians still describe, in both private and public forums, their first experience of witnessing at first hand the “miraculous” and rapid disappearance of their patient's symptoms after subcutaneous injection of sumatriptan during a severe migraine attack. To this day, no triptan can provide greater relief than that provided by parenterally administered sumatriptan.

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 When It Comes To Migraines, the Drugs Are Almost As Bad As the Pain

But even the most preferred and well-studied migraine treatments aren't always perfect. Triptans, which are a class of abortive drugs, and have received the most scientific evaluation, work by binding to serotonin receptors in the brain.

Articles of Interest

Which Triptan Medication Is Best for Migraine Relief?

Seven triptans are available in the U.S. with a prescription. Three of the most common are sumatriptan, zolmitriptan, and rizatriptan. One triptan isn’t necessarily better than the other.

An Overview of Generic Triptans for Migraine

Triptans are recommended as first-line therapy for the treatment of acute migraine attacks in combination with an NSAID or paracetamol (acetaminophen), or as monotherapy, if preferred.

Comparison of New Pharmacologic Agents With Triptans for Treatment of Migraine

New drug discovery programs shifted the focus to the development of 2 classes of drugs: ditans, a group of antimigraine drugs targeting 5-hydroxytryptamine1F (5-HT1F) receptors, and gepants, a group of calcitonin gene-related peptide (CGRP) receptor antagonists.

Facts About Triptans

Unlike other acute medications, triptans are considered selective serotonin receptor agonists, meaning that triptans work by stimulating serotonin, a neurotransmitter found in the brain, to reduce inflammation and constrict blood vessels, thereby stopping the headache or migraine.

Medication Overuse Headache

Some people might find that they can treat their attacks with acute medication such as paracetamol, ibuprofen, or triptans. But if these medications are taken too often, they can actually cause medication overuse headache.

Oral and Intranasal Triptans for Migraine

Learn about how triptans work and who they can help, as well as dosing, side effects, and contraindications.

Triptans and CGRP blockade – impact on the cranial vasculature

Thirty years after discovery of agonists for serotonin 5-HT1B and 5-HT1D receptors (triptans) and less than fifteen after the proof of concept of the gepant class of CGRP receptor antagonists, we are still a long way from understanding their precise site and mode of action in migraine.

Triptans play a larger role in medication overuse headache

The study suggests, Drs. Silberstein and Welch write, that “the pharmacological and clinical presentation of triptan-induced MOH is different from other acute headache drugs such as ergots and analgesics.” Therefore, a clinician might suspect triptan-induced MOH when a patient with migraine experiences a frequency in migraine attacks.

Triptans: Targeting the Serotonin Receptor

The approval of sumatriptan in 1992 was a breakthrough in migraine treatment.1 It took decades of research about the role of serotonin and serotonin receptors in migraine. Some of these ideas turned out to be incorrect. Yet they led to important discoveries along the way.

Weekly Dose: triptans, drugs that relieve migraine but only if taken at the right time

Triptans activate subtypes of the serotonin receptor, which is believed to produce vasoconstriction and oppose the cascade of events that leads to migraine headache.

Resources

Sumatriptan

Oral sumatriptan has demonstrated effectiveness in treating a single acute migraine attack. The absorption of sumatriptan is rapid after oral and subcutaneous administration.

StatPearls

Triptans are a class of medications used in the treatment of migraine headaches. Triptans act as antimigraine agents by selectively binding to the serotonin receptors 5-HT1B and 5-HT1D. Triptan binding to the vascular 5-HT1B receptors leads to vasoconstriction of the cranial arteries, which painfully dilate during a migraine attack.