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How effective are triptans (serotonin 1b/1d agonists) for acute migraine treatment
Oral sumatriptan, almotriptan, eletriptan, rizatriptan, and zolmitriptan relieve the pain in about 65% to 70% with better efficacy than frovatriptan and naratriptan.
Sumatriptan subcutaneous (SC) 6 mg provides headache relief in 70% by 2 hours and 80% by 4 hours.
Sumatriptan 20 mg nasal spray (NS) and zolimitriptan 5 mg NS are second fastest.
Sumatriptan SC, NS, and iontophoretic transdermal patch are preferred for those with prominent nausea/vomiting or who do not respond to oral triptans.
All acute medications are more effective when taken when the pain is mild.
| Drug (Brand Name) | Formulation | Strengths (mg) |
|---|---|---|
| Almotriptan (Axert) | Tablets | 12.5 |
| Eletriptan (Relpax) | Tablets | 40 |
| Frovatriptan (Frova) | Tablets | 2.5 |
| Naratriptan (Amerge) | Tablets | 1, 2.5 |
| Rizatriptan (Maxalt) | Tablets | 5, 10 |
| Orally disintegrating preparation ∗ (Maxalt MLT) | 5, 10 | |
| Sumatriptan (Imitrex) | Subcutaneous injection | 6 |
| Tablets | 25, 50, 100 | |
| Nasal spray | 5, 20 | |
| Sumatriptan patch (Zecuity) | Iontophoretic transdermal patch worn for 4 hours | 6.5 |
| Sumatriptan/naproxen (Treximet) | Tablet | 85/500 |
| Zolmitriptan (Zomig) | Tablets | 2.5, 5 |
| Orally disintegrating preparation ∗ (Zomig ZMT) | 2.5, 5 | |
| Nasal spray | 5 |
Modified with permission from Evans RW: Headaches. In: ACP Medicine, BC Decker, 2009.
What are contraindications to triptans? What about the risk of serotonin syndrome (SS)?
According to the package insert (PI), contraindications to use include those with ischemic heart disease, Prinzmetal’s angina, Wolff–Parkinson–White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders, cerebrovascular syndromes (including strokes and transient ischemic attacks), peripheral vascular disease (including ischemic bowel disease), uncontrolled hypertension, hemiplegic or basilar migraine, and use within 24 hours of ergotamine derivatives.
The PI also warns that SS may occur with 5-HT 1 agonists, particularly when used concomitantly with other serotonergic drugs.
The American Headache Society’s position paper concludes, “The currently available evidence does not support limiting the use of triptans with selective serotonin reuptake inhibitors or selective serotonin/norepinephrine reuptake inhibitors, or the use of triptan monotherapy, due to concerns for serotonin syndrome.”
Sources
- Zimmer C: Soul made flesh. The discovery of the brain—and how it changed the world . New York. Free Press, pp 189-199, 2004.
- Pearce JMS: Historical aspects of migraine. J Neurol Neurosurg Psychiatry 49:1097-1103, 1986.
