Home > Medication > How Do Triptans Treat Migraines?

How Do Triptans Treat Migraines?

By: Kathryn Senior PhD - Updated: 13 Sep 2012 | comments*Discuss
 
Triptans Migraine Pain Dilated Blood

Triptans are drugs used to treat severe migraines, the ones that do not respond to standard painkillers such as paracetamol, codeine, aspirin or ibuprofen. They do not actually work by killing pain – they treat migraine by constricting dilated blood vessels that are thought to cause the pain. They also stabilise the levels of several peptides and neurotransmitters that become unbalanced during a migraine attack, allowing the blood vessels and nerve endings to recover more quickly.

Triptans and Serotonin

To understand how triptans work, it is important to understand the role of serotonin in migraine. This molecule is a chemical neurotransmitter – it is present in the brain and passes signals between different nerve cells. Also known as 5-hydroxytryptamine, this neurotransmitter fits into 5HT receptors. When this happens, one of the effects is to make the muscles in the wall of blood vessels contract so that the blood vessel lumen becomes smaller. The whole vessel constricts, drawing the wall in so that it doesn’t press into the tissues surrounding it.

One of the main results of a migraine is that blood vessels in the brain become dilated and distended. This makes them press on the surrounding brain tissue, causing pain. Triptans are known as serotonin agonists – they fit perfectly into the 5HT receptors, so fooling the blood vessels that there is plenty of serotonin present. The blood vessels constrict, so easing the pressure and reducing the sensations of pain.

How were Triptans Developed?

Triptans have only been available since the 1990s and represent a major new treatment for migraines. Before triptans, very severe migraine headaches and cluster headaches were treated using ergotamines, a class of drugs derived from the ergot fungus. These were effective in some people but they have very bad side effects and tend to stop working after they have been used for a while.

The lack of suitable drugs to treat severe migraines led to a directed drug discovery programme from the early 1970s. Research from the decade before had shown that ergotamines worked partly by binding to the 5HT receptor, so Glaxo started to test compounds to see if they could find one that was a good match for the receptor, but that didn’t have as many side effects. Sumatriptan was the first drug that fitted the bill – it bound 5HT, caused blood vessel constriction – and it could be taken in tablet form, rather than being given by injection. Modification of this molecule led to several other members of the triptan family.

What Kinds of Triptans Are There?

Sumatriptan, eletriptan, rizatriptan, almotriptan and zolmitriptan are all used to treat migraine. Triptans mimic the molecular shape of serotonin, but they are not identical. The individual drugs all fit the 5HT receptor but they have slightly different three dimensional shapes. Because we are all different, some people respond better to one particular triptan compared to the others – probably because of genetic variations in the shape of their 5HT receptor. What is a perfect fit for one receptor, will not be a good match for another.

Finding whose receptor fits which triptan the best is trial and error. Someone with severe migraines are usually started on the cheapest and most readily available triptan, but may be moved to others if that first therapy is not effective. Most triptans are prescription only drugs but sumatriptan became available as an over the counter medicine in the UK in 2006.

When to Take Triptans

Triptans are designed to reduce blood vessel distension in the brain – so it is important to wait until you have some definite symptoms of a headache before you take them. Taking triptans during the aura stage of a migraine headache means that they don’t work quite as well. They don’t prevent the headache coming on and then it is difficult to take another dose when you need to.

You might also like...
Share Your Story, Join the Discussion or Seek Advice..
Why not be the first to leave a comment for discussion, ask for advice or share your story...

If you'd like to ask a question one of our experts (workload permitting) or a helpful reader hopfully can help you... We also love comments and interesting stories

Title:
(never shown)
Firstname:
(never shown)
Surname:
(never shown)
Email:
(never shown)
Nickname:
(shown)
Comment:
Validate:
Enter word:
Topics
Latest Comments
  • Mumof3
    Re: Headache With Pins and Needles: Is This Serious?
    I have pins and needles beneath my feet, it has been there for three days now- and hasn't gone away.…
    25 March 2017
  • Ms. Haider
    Re: Headaches and Eyesight
    I wear soft contact lenses in the day time and take them out only when I'm ready to sleep. Even then if the contacts are out and I close…
    12 March 2017
  • Stassie
    Re: Migraine Classification
    My daughter has been diagnosed with migraine as she has most of the symptoms, so her neurologist said it was a classic one; He prescribed…
    10 March 2017
  • Alexandra
    Re: Headaches After Head Injuries
    I had hit ny head on a table and got a headache and it was getting worse so i went home, in the car i had passes out and my mom…
    10 March 2017
  • Alleycat
    Re: Headaches During The Night
    I have started walking with a headache about an hour after falling asleep.This happens at night or if I am sleeping during the day.…
    10 March 2017
  • Jad
    Re: Headaches and Iron Deficiency
    For the last year I've been getting shooting pains up and down the left side of my head which was diagnosed as trigeminal…
    8 March 2017
  • Stassie
    Re: Headaches Caused by Tensions and Stress
    Hi, My daughter, 16, has been diagnosed with having tension headaches, (via CAT scan and MRI) when she was 11. Since…
    7 March 2017
  • DUNK
    Re: Scalp Pain: What Causes It?
    I have suffered severe eye, scalp, jaw pain for 5 years. The pain has been so bad I have thought about suicide more than once. The…
    6 March 2017
  • "common-cold antenna
    Re: Scalp Pain: What Causes It?
    I've had this pain on my scalp in approximately the same area for a long time ( about 26yrs ). It happens just before I get a bout…
    26 February 2017
  • Julie
    Re: What is the Headache Impact Test?
    I wake up with severe headaches in the middle of the night. What do i do to stop it
    12 February 2017
Further Reading...
Our Most Popular...
Add to my Yahoo!
Add to Google
Stumble this
Add to Twitter
Add To Facebook
RSS feed
You should seek independent professional advice before acting upon any information on the HeadacheExpert website. Please read our Disclaimer.