A family of tryptamine-based drugs used as abortive medication in the treatment of migraines and cluster headaches.
Effective at treating individual headaches, they do not provide preventive treatment and are not considered a cure for migraine or cluster headaches.
Act as agonists for serotonin 5-HT1B and 5-HT1D receptors at blood vessels and nerve endings in the brain.
The have largely replaced ergotamines to relieve migraine and cluster headaches
They are used for the treatment of severe migraine attacks or those that do not respond to other over-the-counter drugs.
They may not be efficacious for atypical or unusually severe migraine attacks, transformed migraine, or status migrainosus.
Triptans reduce symptoms or abort the attack within 30 to 90 minutes in 70–80% of patients.
Skin testing with triptans can determine effectiveness in migraine: no skin sensitivity suggests efficacy, and If it causes pain , rapid administration of the drug increases benefit.
Triptans are effective for the treatment of cluster headache.
Sumatriptan may be able to prevent altitude sickness.
All marketed triptans are available in oral form and some in form of sublingual tablets.
Sumatriptan and zolmitriptan are also available as nasal sprays.
For sumatriptan, suppositories, a subcutaneous injection, and a transdermal patch is available.
All triptans are contraindicated in patients with cardiovascular diseases, Raynaud’s disease, and peripheral artery disease.
Most triptans are also contraindicated during pregnancy and breastfeeding and for patients younger than 18, but sumatriptan and zolmitriptan
The nasal sprays sumatriptan and zolmitriptan approved for individuals over 12 years of age.
The most common adverse effect is recurrence of migraine.
Coronary spasm in patients with established heart disease, and cardiac events after taking triptans may rarely occur.
Combination of triptans with other serotonergic drugs such as ergot alkaloids, monoamine oxidase inhibitors, selective serotonin reuptake inhibitors (SSRIs), serotonin–norepinephrine reuptake inhibitors (SNRIs) or St John’s wort has been alleged to induce symptoms of a serotonin syndrome.
Combination with ergot alkaloids is contraindicated because of the danger of coronary spasms.
Concomitant use of a selective serotonin reuptake inhibitor or selective norepinephrine reuptake inhibitor for depression with a triptan for migraine did not demonstrate an increased risk of the serotonin syndrome.
Pharmacokinetic interactions by CYP liver enzymes are for most triptans mild to absent.
Their action is attributed to their agonist effects on serotonin 5‑HT1B and 5‑HT1D receptors in blood vessels, causing constriction, and nerve endings in the brain.
Inhibits pro-inflammatory neuropeptide release, including CGRP and substance P.
Triptans are selective agents for 5-HT1B and 5-HT1D.
Triptans have low or even no affinity for other types of 5-HT receptors.
5-HT receptors are classified into seven different families named 5-HT1 to 5-HT7.
Head pain initiated by then activation of trigeminovascular afferent nerves which upon activation releases neuropeptides such as CGRP, substance P and neurokinin A.
Neuropeptides promote neurogenic inflammatory response and transmission and generation of head pain centrally.
5-HT1D has been found responsible for inhibition of neurogenic inflammation.
All triptans, have agonistic effects on the 5-HT1D receptor.
Triptans have at least three modes of action:
vasoconstriction of pain producing intra cranial extracerebral vessels by a direct effect on vascular smooth muscle.
cause vasoconstriction in the human middle meningeal arteries.
inhibition of vasoactive neuropeptide release by trigeminal terminals innervating intracranial vessels and the dura mater.
The trigeminocervical complex has 5-HT1D receptors that bind dihydroergotamine and triptans.
Bioavailability of triptans is between 14% and 70%.
Biological half-life of triptans is between 2 and 26 hours.
There is a good ability for triptans to cross the blood-brain barrier and the rather long half life of some triptans may result in lower frequencies of migraine recurrence.
Newer triptans haven longer half-life in plasma and higher oral bioavailability, but have a higher potential for central nervous side effects.