Triptans are a family of antimigraine drugs used to abort migraines and cluster headaches. While effective at treating individual headaches, they do not provide preventive treatment and are not curative. They are not effective for the treatment of tension–type headache, except in persons who also experience migraines. Triptans do not relieve other kinds of pain. They are taken orally and by other routes. The drugs of this class act as agonists for serotonin 5-HT1B and 5-HT1D receptors at blood vessels and nerve endings in the brain. Some also activate the 5-HT1F receptor. Structurally, triptans are substituted tryptamines or closely related to tryptamines, for instance the psychedelic drug dimethyltryptamine (DMT). The first clinically available triptan was sumatriptan, which has been marketed since 1991. Subsequently, a variety of other triptans have also been marketed, including zolmitriptan, naratriptan, rizatriptan, almotriptan, eletriptan, and frovatriptan. Triptans have largely replaced ergoline drugs like ergotamine and dihydroergotamine, an older class of medications used to relieve migraine and cluster headaches.
Medical uses
Migraine Triptans are used for the treatment of severe migraine attacks or those that do not respond to NSAIDs or other over-the-counter drugs. Triptans are a mid-line treatment suitable for many migraineurs with typical attacks. They may not work for atypical or unusually severe migraine attacks, transformed migraine, or status migrainosus (continuous migraine). Triptans are highly effective, reducing the symptoms or aborting the attack within 30 to 90 minutes in 70–80% of patients. A 2024 systematic review and network meta analysis compared the effectiveness of medications for acute migraine attacks in adults. It found that triptans were the most effective class of drugs followed by non-steroidal anti-inflammatories. A test measuring a person's skin sensitivity during a migraine may indicate whether the individual will respond to treatment with triptans. Triptans are most effective in those with no skin sensitivity; with skin sensitivity, it is best to take triptans within twenty minutes of the headache's onset. Oral rizatriptan and nasal zolmitriptan are the most used triptans for migraines in children.
Correct timing of intake Triptans should be taken as soon as possible after the onset of pain. In case of migraine with aura they are to be taken after the aura and with the onset of pain. If taken too early, they may not have the full effect on symptom reduction, and in case of an aura, they can worsen the aura. It is assumed that blood vessels are constricted during the aura phase and dilated during the pain phase, so a constrictive medication like a triptan is not recommended during the aura.
Cluster headache Triptans are effective for the treatment of cluster headache. This has been demonstrated for subcutaneous sumatriptan and intranasal zolmitriptan, the former of which is more effective according to a 2013 Cochrane review. Tablets were not considered appropriate in this review.
Altitude sickness A single randomized controlled trial found that sumatriptan may be able to prevent altitude sickness.
Available forms All marketed triptans are available in oral form; some in form of sublingual tablets. Sumatriptan and zolmitriptan are also available as nasal sprays. For sumatriptan, a number of other application forms are marketed: suppositories, a subcutaneous injection, an iontophoretic transdermal patch, which uses low voltage controlled by a pre-programmed microchip to deliver a single dose of sumatriptan through the skin within 30 minutes; a drug-device combination containing sumatriptan powder that is "breath powered" allowing the user to blow sumatriptan powder in to their nostrils; as well as a needle-free injection system that works with air pressure.
Contraindications All triptans are contraindicated in patients with cardiovascular diseases (coronary spasms, symptomatic coronary artery disease, after a heart attack or stroke, uncontrolled hypertension, Raynaud's disease, peripheral artery disease). Most triptans are also contraindicated during pregnancy and breastfeeding and for patients younger than 18; but sumatriptan and zolmitriptan nasal sprays are also approved for youths over 12. In spite of expert opinion and evidence to the contrary, the FDA and some other drug governance bodies have stated that monoamine oxidase inhibitors are contraindicated for sumatriptan, zolmitriptan and rizatriptan, and combination with ergot alkaloids such as ergotamine for all substances. At least two triptans (sumatriptan and rizatriptan) have been listed under the unacceptable medication by the Canadian Blood Services as a potential risk to the recipient; hence, donors are required not to have taken the medication for the last 72 hours.
Adverse effects Triptans have few side effects if used in correct dosage and frequency. The most common adverse effect is recurrence of migraine. A systematic review found that "rizatriptan 10 mg was the only triptan with a recurrence rate [the reappearance of moderate to severe pain within 24 hours after the response at 2 hours] greater than that of placebo". There is a theoretical risk of coronary spasm in patients with established heart disease, and cardiac events after taking triptans may rarely occur.
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