Triptans

Since 1993, as an alternative to the usual pain killers and ergotamines, the substance

  • sumatriptan

is available as the first so-called selective serotonin inhibitor. Until today, a whole range of other drugs in this substance class are available:

  • naratriptan
  • zolmitriptan
  • eletriptan
  • almotriptan
  • rizatriptan
  • frovatriptan

Since triptans not only target the migraine pain itself but also the accompanying symptoms such as nausea, vomiting, photo- and phonophobia, no further medication is required to treat nausea and vomiting.

Triptans work by blocking the release of nerve messengers (neuropeptides and neurotransmitters), which can cause a local, neurogenic inflammation of the blood vessels and the brain. Additionally, triptans can normalise an increased neural activity during a migraine attack in different brain centres and can make dilated connecting passages between arteries and veins (anastomoses) narrower again, which normalises the brain’s oxygen supply.

While ergotamines act everywhere in the body, triptans essentially selectively target areas (5-HT1B and 1D-receptors) located in the precise areas implicated in the disease activity of migraine.

Up-to-date medical treatment is essential

In patients, where other therapies cannot reduce the burden of migraine and in which there are no contraindications for using triptans, the use of this therapy is justified and indeed imperative. Whoever withholds triptans from patients can, in legal terms, render oneself liable to prosecution due to failure to render assistance. If there are no contraindications, a doctor will consider triptans in the following situations:

  • long attack duration
  • severe, long-lasting pain intensity
  • severe, long-lasting nausea and vomiting
  • frequent inability to work
  • signficant impairment of social activities
  • significant side effects of other medications

Important rules for triptans

  • Triptans may only be used after a thorough medical pre-assessment including blood pressure measurement, ECG recording and individual counselling. This is also and especially true for the first use in an emergency situation in cases of severe migraine attacks.
  • They may not be used, if a medication-induced permanent headache is present, or contraindications such as having had a heart attack, stroke or other vascular disorders, high blood pressure, liver or kidney disorders exist.
  • Only take triptans, when the headache phase starts, but then as early as possible. During the aura phase the substance should not be taken. The reason is that it cannot alter aura symptoms directly. Also they cannot effectively improve migraine symptoms when taken too early before the headache phase. Additionally, one assumes that aura symptoms are caused by a constriction of blood vessels. Symptoms could be worsened by taking vasoconstrictive substances such as triptans during this phase.
  • Under no circumstance, triptans may be used in combination with ergotamines. Since both ergotamines and triptans can result in blood vessel constriction, an overlap of both ingredients can result in a dangerous additive vasoconstrictive effect. Since ergotamines are an out-of-date substance in migraine therapy anyway, this problem should only rarely occur. Many patients however take various pills unselectively, sometimes recommended to them by friends, during the confusion of a migraine attack. It is important to pay attention to detail and to not listen to allegedly good advice.
  • Because triptans only have a limited duration of action, in around 30 percent of patients new migraine symptoms occur after the duration of action has passed. This so-called returning headache can be treated with a new dose successfully. Important: this does not mean that the migraine attack is postponed or prolonged! As a rule of thumb, the dose can be repeated once per day. If you have to revert to your medication more than twice in one day, you should work out a new therapy concept with your doctor, resulting in a greater effectiveness. Then, selecting a longer-lasting triptan such as almotriptan, naratriptan or frovatriptan is recommended. Also the combination with a long-acting so called COX-2-inhibitor can reduce the likelihood of an occurrence of a returning headache.
  • Irrespective of the dose, you should in any case make sure not to use the substance on more than 10 days per month, to avoid the development of a medication-overuse headache.
  • Patients with a high attack frequency are often unsure whether they should take the triptan already at the start of an attack. They then come into conflict with at the one hand taking the medication early in the attack, on the other hand avoiding going over the limit of treatment on 10 days per month. For this reason a check list, the so-called “triptan threshold” was developed (see download box top right) to determine the best time to take the medication.
  • Triptans should only be used until an age of 65 years. Meanwhile, there are also studies of using triptans in adolescents aged between 12 and 18. These did not show an increased risk in this age group. In children below the age of 12, triptans should however not be used.
  • Typical side effects of triptans are a slight general feeling of weakness and a non-directional dizziness, paresthesias, feelings of warmth or cold and slight nausea. Very rarely, also a feeling of tightness around the chest or neck can occur. Generally, side effects are mild and disappear by themselves.

Use of triptans in migraine attack therapy

The treatment success of using triptans can be optimised by considering the following:

  • Triptans can also be effective in advanced migraine attacks, but the earlier they are taken, the more complete and sustained the treatment effect will be. They should however only be taken after a possible aura has subsided, at the start of the headache phase.
  • If a triptan is not effective in a migraine attack, repeating the intake of the triptan during the same attack is usually also not effective if the start dose was also the highest recommended individual single dose (e.g. sumatriptan 100mg p.o. or sumatriptan 6mg s.c.). If the patient however starts with a lower dose, e.g. sumatriptan 50mg p.o. or eletriptan 20mg p.o., out of experience repeating the intake after 2 hours can well lead to pain relief. In subsequent attacks, it is recommended however to primarily choose a higher start dose.
  • If a triptan is ineffective also with repeated intake, it does not mean that triptans are generally ineffective in this patient. In these cases, a triptan from a group with greater efficacy (see above) should be chosen. Ultimately, a conclusion about the individual effectiveness of triptans can be drawn when using sumatriptan s.c.
  • Triptans are very safe, so long as the contraindications – here especially any type of vascular disorders – are considered.
  • Due to limited data, for safety reasons triptans should not be used during pregnancy. When breastfeeding, a 24 hour breast-feeding pause after intake of a triptan is required.
  • During the occurrence of a returning headache, the next triptan dose is generally as effective as the previous one. The intake should however not be more frequent than twice per 24 hours and maximally on 3 consecutive days. If patients report regular returning headaches, initially a long-acting triptan such as naratriptan or frovatriptan should be tried. Alternatively the combination of triptans with a long-acting non-steroidal anti-inflammatory drugs such as, for example, naproxen has proved effective.
  • The combination of a triptan with an antiemetic is possible to aid absorption, however frequently not necessary.
  • Overall, acute headache medication and therefore also triptans should not be used on more than 10 days per month, to counteract an increase of migraine attacks and ultimately the development of a medication-overuse headache. For patients with frequent attacks, this may also mean enduring the occasional migraine attack without any treatment. Experience has shown however, that the pain free period after an untreated attack is often much longer than after a (successfully) treated attack.
  • Triptans were initially approved for patients aged 18 years and above. Controlled studies have shown however that especially sumatriptan 10mg nasal spray and ascotop nasal spray are reliably effective and well tolerated, so that these application forms can now officially be used in patients aged 12 years and above.
Use of triptans in the attack therapy of migraine
active ingredient application name use for
Sumatriptan 6 mg for injection -s.c.-needle in autoinjector Imigran Inject Nausea,
works very quickly
-needle-free injection Sumavel DosePro
Sumatriptan nasal spray 20 mg Nasal spray Imigran nausea,
works very quickly
Sumatriptan nasal spray 10 mg Nasal spray Imigran Nausea,
tolerability desired
Sumatriptan Suppositories 25 mg Suppository Imigran nausea,
tolerability desired
Sumatriptan 100 mg Tablet Imigran

Sumatriptan

Very severe attacks
Sumatriptan 50 mg Tablet Imigran
Sumatriptan
Very severe attacks
Zolmitriptan 2,5 mg Tablet Ascotop Severe attacks
Zolmitriptan 2,5 mg Orodispersible tablet severe attacks
Zolmitriptan 5 mg Orodispersible tablet Very severe attacks,
works very quickly
Naramig 2,5 mg Tablet Naramig
over-the-counter: Formigran
Long attacks,
tolerability desired
Rizatriptan 10 mg Tablet Maxalt Works very fast,
very severe attacks
Rizatriptan 10 mg Orodispersible tablet Works very fast,
very severe attacks
Almotriptan 12,5 mg Tablet Almogran
over-the-counter: Dolortriptan
Works very quickly,
long attacks
Eletriptan 40 mg Tablet Relpax Works very quickly,
very severe attacks
Eletriptan 20 mg tablet Works very quickly,
long attacks
Frovatriptan 2,5 mg Tablet Frovatriptan Long attacks,
tolerability desired