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Antimigraine drug
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Antimigraine drug
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks.
Examples of specific antimigraine drug classes include triptans (first line option), ergot alkaloids, ditans and gepants. Migraines can also be treated with unspecific analgesics such as nonsteroidal anti-inflammatory drugs (NSAIDs) or acetaminophen. Opioids are not recommended for treatment of migraines.
The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. Due to their safety, efficacy and selectivity, triptans are considered first line agents for abortion of migraines. These medications are selective 5-HT1B/1D receptor agonists with some activity at 5-HT1F. They produce an antimigraine effect by vasoconstriction of the vessels in the brain, as well as inhibiting trigeminal CGRP release and pain transmission. They are normally well tolerated but the vasoconstrictor effects can lead to problematic side effects such as nausea, dizziness and chest discomfort, and therefore require caution in patients with cardiovascular disease. There is also an increased risk of gastrointestinal adverse events. Triptans use is limited to less than ten times per month in order to reduce medication overuse headache (MOH).
Ergot alkaloids include ergotamine and dihydroergotamine. This medication class targets the CGRP receptor pathway due to their likeness to serotonin, dopamine and noradrenaline. They show activity at serotonin 5-HT1-2, dopamine D2-like and alpha1/alpha2-adrenoreceptors. Their lack of selectivity leads to more adverse effects, making them second line compared to triptans. However, they have been shown to prevent recurrence better than triptans. Adverse effects include nausea, vomiting, paresthesia, and ergotism. Their use is limited to less than ten times per month in order to reduce medication overuse headache (MOH). The oral dosage administrative form is considered less effective than nasal or parenteral forms and has been discontinued in Canada. Ergotamine is contraindicated during pregnancy.
Ditans (eg. lasmiditan) are a new group of anti migraine drugs which were developed due some of the concerns with the 1st line triptans (eg. adverse effects, concern with use in cardiovascular disease, use of less than 10x per month to reduce MOH). Ditans are 5-HT1F receptors agonists. Lasmiditan has been suggested to have less pain relief when compared to the triptans at the 2 hour mark post taking the medication. Lasmiditan was shown to have higher adverse events (dizziness, fatigue and nausea) than the triptans or another novel medication class, CGRP antagonists. However, they could be an option for patients with cardiovascular risks due to their lack of vasoconstriction . Due to risk of dizziness, those who take lasmiditan should avoid driving 8 hours after taking. Another ditan that was ultimately not marketed is alniditan.
Gepants (eg. rimegepant, ubrogepant, and atogepant) are also a new group of anti migraine drugs, along with ditans. They are calcitonin gene-related peptide (CGRP) receptor antagonists. Gepants have been suggested to have less pain relief at 2 hours compared to triptans. Similar to ditans, they offer another therapy option that does not include vasoconstriction, thus may be suitable for those with cardiovascular risk factors. They are well tolerated with fewer adverse effects compared to triptans .
NSAIDS are a nonspecific medication used for abortion of migraines due to their analgesic properties. They can be used for mild to moderate migraines, but are less effective against severe migraines. Similar to the triptans and ergots alkaloids, their use should be limited to less than 10x per month to reduce MOH. Acetaminophen is an analgesic that can also be used, but NSAIDS should be tried first due to their anti-inflammatory properties. However, acetaminophen would be considered first line in pregnant patients. Combination therapy of an NSAID with a triptan can be used when either medication is insufficient alone for migraine relief or recurrence . Long term NSAID use has risks including nephrotoxicity and cardiotoxicity, and long term acetaminophen use is associated with hepatoxicity. If warranted, an antiemetic can be used in combination with an NSAID.
Opioids are not recommended for treatment of acute migraines due to their significant side effect profile, including twice the risk of medication overuse headache when compared to NSAIDS, acetaminophen or triptans. In addition, their strength of efficacy has shown to be low or insufficient for pain relief of migraines. Importantly, there is also risk of addiction and opioid use disorder.
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Antimigraine drug
Antimigraine drugs are medications intended to reduce the effects or intensity of migraine headache. They include drugs for the treatment of acute migraine symptoms as well as drugs for the prevention of migraine attacks.
Examples of specific antimigraine drug classes include triptans (first line option), ergot alkaloids, ditans and gepants. Migraines can also be treated with unspecific analgesics such as nonsteroidal anti-inflammatory drugs (NSAIDs) or acetaminophen. Opioids are not recommended for treatment of migraines.
The triptan drug class includes 1st generation sumatriptan (which has poor bioavailability), and second generation zolmitriptan. Due to their safety, efficacy and selectivity, triptans are considered first line agents for abortion of migraines. These medications are selective 5-HT1B/1D receptor agonists with some activity at 5-HT1F. They produce an antimigraine effect by vasoconstriction of the vessels in the brain, as well as inhibiting trigeminal CGRP release and pain transmission. They are normally well tolerated but the vasoconstrictor effects can lead to problematic side effects such as nausea, dizziness and chest discomfort, and therefore require caution in patients with cardiovascular disease. There is also an increased risk of gastrointestinal adverse events. Triptans use is limited to less than ten times per month in order to reduce medication overuse headache (MOH).
Ergot alkaloids include ergotamine and dihydroergotamine. This medication class targets the CGRP receptor pathway due to their likeness to serotonin, dopamine and noradrenaline. They show activity at serotonin 5-HT1-2, dopamine D2-like and alpha1/alpha2-adrenoreceptors. Their lack of selectivity leads to more adverse effects, making them second line compared to triptans. However, they have been shown to prevent recurrence better than triptans. Adverse effects include nausea, vomiting, paresthesia, and ergotism. Their use is limited to less than ten times per month in order to reduce medication overuse headache (MOH). The oral dosage administrative form is considered less effective than nasal or parenteral forms and has been discontinued in Canada. Ergotamine is contraindicated during pregnancy.
Ditans (eg. lasmiditan) are a new group of anti migraine drugs which were developed due some of the concerns with the 1st line triptans (eg. adverse effects, concern with use in cardiovascular disease, use of less than 10x per month to reduce MOH). Ditans are 5-HT1F receptors agonists. Lasmiditan has been suggested to have less pain relief when compared to the triptans at the 2 hour mark post taking the medication. Lasmiditan was shown to have higher adverse events (dizziness, fatigue and nausea) than the triptans or another novel medication class, CGRP antagonists. However, they could be an option for patients with cardiovascular risks due to their lack of vasoconstriction . Due to risk of dizziness, those who take lasmiditan should avoid driving 8 hours after taking. Another ditan that was ultimately not marketed is alniditan.
Gepants (eg. rimegepant, ubrogepant, and atogepant) are also a new group of anti migraine drugs, along with ditans. They are calcitonin gene-related peptide (CGRP) receptor antagonists. Gepants have been suggested to have less pain relief at 2 hours compared to triptans. Similar to ditans, they offer another therapy option that does not include vasoconstriction, thus may be suitable for those with cardiovascular risk factors. They are well tolerated with fewer adverse effects compared to triptans .
NSAIDS are a nonspecific medication used for abortion of migraines due to their analgesic properties. They can be used for mild to moderate migraines, but are less effective against severe migraines. Similar to the triptans and ergots alkaloids, their use should be limited to less than 10x per month to reduce MOH. Acetaminophen is an analgesic that can also be used, but NSAIDS should be tried first due to their anti-inflammatory properties. However, acetaminophen would be considered first line in pregnant patients. Combination therapy of an NSAID with a triptan can be used when either medication is insufficient alone for migraine relief or recurrence . Long term NSAID use has risks including nephrotoxicity and cardiotoxicity, and long term acetaminophen use is associated with hepatoxicity. If warranted, an antiemetic can be used in combination with an NSAID.
Opioids are not recommended for treatment of acute migraines due to their significant side effect profile, including twice the risk of medication overuse headache when compared to NSAIDS, acetaminophen or triptans. In addition, their strength of efficacy has shown to be low or insufficient for pain relief of migraines. Importantly, there is also risk of addiction and opioid use disorder.
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