Triptans - Acute Medicines

Triptans (Selective 5-HT1 Agonists)

The class of Acute Medicines known as ‘Triptans’ is a selective 5-HT1 agonists for the treatment of migraines. They work by acting on serotonin receptors in the brain (5-HT1B and 5-HT1D receptors), thereby blocking transmission of pain pathways. They only reduce migraine pain but not other types of pain and are therefore migraine-specific. They also help other symptoms of a migraine attack such as nausea and vomiting, and sensitivity to light and sound.

According to Migraine Canada, there are currently 7 Triptans available in Canada. They are sumatriptan, zolmitriptan, rizatriptan, naratriptan, almotriptan, eletriptan and frovatriptan. The oldest, and most widely studied triptan is sumatriptan. 2

All Triptans are contradicted in patients with a history of heart disease or vascular diseases (such as heart attack, angina, stroke, peripheral vascular insufficiency) 2 , however one Triptan is not necessarily better than another, in terms of efficacy. Like other types of medicines, a successful response varies among patients.

Side effects of triptans are generally minimal but may include drowsiness, dizziness, fatigue (may also be due to migraine attack), numbness or tingling, tightness in the neck, jaw or chest (chest tightness is not usually due to heart attack but if it persists or is severe consult with physician or go to Emergency)

Sumatriptan (Imitrex or generic version)

Sumatriptan (Imitrex, or generic versions) is the oldest and first triptan to be developed. According to WebMD it helps to relieve headache pain and other migraine symptoms (including nausea and vomiting, sensitivity to light/sound). 1 The subcutaneous injection is very effective, stopping an attack within about 10-15 minutes but has more side effects than oral or nasal forms.

Experts agree that it is most effective if taken at the start of the pain. This selective serotonin agonist was discovered in 1980 and truly changed the acute treatment of migraine management. 2

Sumatriptan is an effective acute treatment for migraines. It comes in a few formats:

  • Oral Tablets or DF tablets (dissolve in stomach)
  • Injections (to be administered subcutaneously)
  • Nasal spray

Zolmitriptan (Zomig)

Zolmitriptan is another triptan used to abort (stop) a migraine in process. 3 It is marketed in Canada under the Brand name of Zomig as well as generic versions.

It comes in a variety of forms, such as:

  • Oral Tablets
  • Rapid Melt tablets (dissolve in the mouth) – but do not act faster than oral tablets
  • Nasal spray

Rizatriptan (Maxalt, or generic)

Rizatriptan (trade name Maxalt or generic) is a 5-HT1 receptor agonist of the triptan class of drugs developed by Merck Frosst Canada, for the acute treatment of migraine headaches. 4

This medication comes in the following formats:

  • Oral Tablets
  • Wafer (dissolves on the tongue) – but does not act faster than oral tablets 5

Naratriptan (Amerge)

Naratriptan in Canada is marketed by GlaxoSmithKline under the brand name of Amerge. Naratriptan belongs to a class of medications known as triptan agonists. 6 7

This medications comes in the following formats:

  • Oral Tablets

Almotriptan (Axert or Generics)

Almotriptan is a triptan drug for the acute treatment of migraine headaches. 8 9

This medication is not used to prevent migraines from happening, but like all triptans, it is designed to abort (stop) a migraine in process.

This medications comes in the following formats:

  • Oral Tablets

Eletriptan (Relpax)

Eletriptan is a second generation triptan drug developed by Pfizer Inc for the acute treatment of migraine headaches. 21 22 It is sold in Canada under the name Relpax 10 11

This medications comes in the following formats:

  • Oral Tablets

Frovatriptan (Frova)

Frovatriptan (marketed as Frova) is an abortive medication used for the treatment of Migraine attacks in adults. It belongs to the class of medicine known as 5-HT1 agonists. It has the longest duration of action of the triptan class. 12

This medication comes in the following formats:

  • Oral Tablets

In the above available triptans, the Nasal Spray method of administration may be a consideration if nausea or vomiting is an issue. See nasal sprays section.

Message About Triptans From Migraine Canada

There now are 7 different triptans available in Canada, and some have more that one formulation: injections, tablets to swallow, tablets that dissolve in the mouth, and nasal sprays. 13

If you are taking one but are not getting an excellent response, it is worthwhile trying another. You likely will not want to try all of them but if you don’t hit a home run, it is worthwhile trying at least 3 or 4, especially if your migraine attacks are severe enough to put you in bed or interfere significantly with your work. 14

* please note that some brand names of the above drugs are no longer offered - a generic version may be available

Triptans: Treat Early or Late - Dr. Stephen Silberstein & Dr. William Young

Dr. Stephen Silberstein is a professor of Neurology and Director of the Jefferson Headache Centre at Thomas Jefferson University in Philadelphia, PA. Dr. William Young is an Assistant Professor of Neurology at the Jefferson Headache Centre in Philadelphia, PA. Theses “Headache Experts” wrote a book called Migraine and Other Headaches.

In their book they discuss whether patients should treat early or late. They suggest that “it is clear that early treatment gets rid of migraine more quickly and more completely than if treatment is delayed. Early treatment also reduces the number of pills needed to treat each attack but be careful --it may increase the risk of using too frequently (which may result in medication overuse headache) and chronic headaches in people with frequent migraine.” 15

Concerns about Triptans - Dr. Elizabeth Leroux (Migraine Canada)

Very often, triptans are perceived as dangerous and their price is quite high compared to anti-inflammatories. This contributes to their image of being powerful and therefore dangerous. By stimulating the serotonin receptors, they cause a slight vasocontriction of the arteries. For this reason, they can't be prescribed for people with poorly controlled high blood pressure, heart disease, or those who have had a stoke. Again, because of their action on serotonin receptors, triptans have been the object of a warning from the Food and Drug Administration (FDA) recommending they not be prescribed to people taking anti-depressants, since they also stimulate the serotonin system. The stimulatory effect of the 2 drugs combined could result in serotonin syndrome, a potentially dangerous reaction. But the American Headache Society has reviewed all cases of serotonin syndrome in relation to triptans and has determined that the risk of developing this syndrome because of triptans is negligible. And let's not forget that these drugs have been taken safely by millions of people for more than twenty years. 16

REFERENCES

  1. Web MD - Sumatriptan
  2. Migraine Canada - Triptans
  3. MedicineNet.com - Zolmitriptan
  4. Wikipedia - Rizatriptan
  5. Medscape - Rizatriptan
  6. Rexall.ca - Naratriptan
  7. Wikipedia - Naratriptan
  8. MedicineNet - Almotriptan
  9. DrugBank.ca/drugs - Almotriptan
  10. DrugBank - Eletriptan
  11. MedicineNet - Eletriptan
  12. WebMD - Frovatriptan
  13. Migraine Canada - Triptans avalable
  14. Migraines.org - Triptans
  15. Silberstein, S & Young, W - Migraine and Other Headaches, pg 95 - 2004 - When to treat Migraines with triptans
  16. Concerns about Triptans: Dr. Elizabeth Leroux, Migraines: More than a Headache, Dundurn Press 2016, pg. 134

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