Which medications in the drug class Serotonin 5-HT-Receptor Agonists (Triptans) are used in the treatment of Migraine Headache?

Updated: Oct 21, 2019
  • Author: Jasvinder Chawla, MD, MBA; Chief Editor: Helmi L Lutsep, MD  more...
  • Print
Answer

Serotonin 5-HT-Receptor Agonists (Triptans)

Triptans are used as abortive medications for moderately severe to severe migraine headaches. These drugs are selective serotonin agonists, specifically acting at 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptors on intracranial blood vessels and sensory nerve endings. 

The most common side effects of triptans are as follows: Asthenia, nausea/vomiting, dizziness, somnolence, chest, throat, or jaw tightness/discomfort, worsening of head pain (often transient)

Drug interactions occur with potent CYP450 3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir), which may increase toxicity, and with concurrent administration of ergot-containing drugs, which may increase vasospastic reactions. Zolmitriptan, eletriptan, and naratriptan are primarily metabolized by CYP450 3A4.

Sumatriptan (Imitrex, Sumavel DosePro, Alsuma, Onzetra, Sumavel, Zeculty, Zembrace)

5-HT1B/1D receptor agonist. Sumatriptan has the most options for drug delivery. It is available in intranasal, subcutaneous, and oral formulations. The efficacy of sumatriptan is 82% at 20 minutes when administered by injection, 52-62% at 2 hours when administered intranasally, and 67-79% at 4 hours when administered orally. [132, 133, 134]

Naratriptan (Amerge)

A selective agonist for serotonin 5-HT1B/1D  receptors, naratriptan has higher bioavailability and a longer half-life than sumatriptan, which may contribute to a lower rate of headache recurrences. Naratriptan has a slow onset of action and a duration of action of up to 24 hours, with low headache recurrence rate. It is useful for patients with slow onset, prolonged migraine, such as menstrual migraine.

Pain relief is experienced by 60-68% of patients within 4 hours of treatment and maintained for up to 24 hours in 49-67% of patients. Naratriptan is one of the few triptans that is not contraindicated for use in combination with monoamine oxidase inhibitors (MAOIs).

Zolmitriptan (Zomig, Zomig-ZMT)

A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, zolmitriptan suppresses the inflammation associated with migraine headaches. It has an efficacy of 62% at 2 hours and of 75-78% within 4 hours.

Rizatriptan (Maxalt, Maxalt-MLT)

A selective agonist for serotonin 5-HT1B/1D receptors in cranial arteries, rizatriptan suppresses the inflammation associated with migraine headaches. It has a reported early onset of action (30 min) and an efficacy of 71% at 2 hours. It has the fastest onset of action of the triptans.

Almotriptan (Axert)

A selective 5-HT1B/1D receptor agonist, almotriptan results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. It induces cranial vessel constriction, inhibits neuropeptide release, and reduces pain transmission in trigeminal pathways.

Frovatriptan (Frova)

Frovatriptan is a selective 5-HT1B/1D receptor agonist with a long half-life (26-30 h) and a low headache recurrence rate within 24 hours of taking the drug. It constricts cranial vessels, inhibits neuropeptide release, and reduces pain transmission in trigeminal pathways. Frovatriptan is one of the few triptans that is not contraindicated for use in combination with MAOIs.

Eletriptan (Relpax)

A selective serotonin agonist, eletriptan specifically acts at 5-HT1B/1D/1F receptors on intracranial blood vessels and sensory nerve endings to relieve pain associated with acute migraine.

Eletriptan is primarily metabolized by CYP3A4 and should not be used within at least 72 hours of potent CYP3A4 inhibitors. Eletriptan is one of the few triptans that is not contraindicated for use in combination with MAOIs.

Sumatriptan and naproxen (Treximet)

This is a combination product containing sumatriptan, a selective 5-HT1B/1D receptor agonist, and naproxen sodium, an arylacetic acid NSAID, in a fixed combination of sumatriptan 85 mg and naproxen sodium 500 mg. It is indicated for acute migraine. Sumatriptan mediates vasoconstriction of the basilar artery and vasculature of dura mater, which correlates with migraine relief. Naproxen provides analgesic, anti-inflammatory, and antipyretic properties. It decreases the activity of cyclo-oxygenase (COX), thereby interrupting prostaglandin synthesis.

Sumatriptan intranasal (Imitrex Intranasal, Onzetra Xsail)

Selective 5-HT1B/1D receptor agonist in cranial arteries. Elicits vasoconstrictive and anti-inflammatory effects, It is associated with antidromic neuronal transmission and relief of migraine headache. It is indicated for treatment of acute attack of migraine headache with or without aura. Available as a liquid nasal spray or a dry powder administered using the Xsail breath-powered delivery device.

Sumatriptan transdermal (Zecuity)

Selective 5-HT1B/1D receptor agonist. Indicated for treatment of acute migraine attack with or without aura. Delivered as a transdermal patch along with iontophoresis.


Did this answer your question?
Additional feedback? (Optional)
Thank you for your feedback!