MIGRAINE HEADACHE MEDICATIONS

All dosing is for ADULTS unless otherwise specified. P = drugs with pediatric dosing recommendations.
PRICING INFO


References:
CGRP INHIBITOR STUDIES



Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Almotriptan

Axert®
Axert® - tablet
  • 6.25 mg
  • 12.5 mg

Comes in dose pack of 6 or 12 tablets
Migraine headache
  • Adolescents 12 - 17 years
    • Initial: 6.25 - 12.5 mg
    • May repeat in 2 hours if needed
    • Do not exceed 25 mg in 24 hours
  • Adults
    • Initial: 6.25 - 12.5 mg
    • In adults, the 12.5 mg dose tends to be more effective
    • May repeat in 2 hours if needed
    • Do not exceed 25 mg in 24 hours

With strong CYP3A4 inhibitors
  • Initial: 6.25 mg
  • Maximum: 12.5 mg in 24 hours
  • Avoid concomitant CYP3A4 strong inhibitors in patients with kidney or liver disease
  • See CYP3A4 for a list of inhibitors
Axert®
YES/$$$$
(12 tablets)
Other
  • May take without regard to food

Pharmacokinetics
  • Time to max level: 1 - 3 hours
  • Half-life: 3 - 4 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
  • Acute migraine headache with or without aura in adults and adolescents
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 12.5 mg dose

Adolescents 12 - 17 years
  • Somnolence - 5%, P - 2%
  • Nausea - 3%, P - 0%
  • Dizziness - 3%, P - 2%
  • Headache - 2%, P - 1%
  • Paresthesia - 1%, P - <1%

Adults
  • Nausea - 2%, P - 1%
  • Dry mouth - 1%, P - 0.5%
  • Paresthesia - 1%, P - 0.5%
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • CYP3A4 strong inhibitors - almotriptan is a CYP3A4 sensitive substrate. When taken with a strong CYP3A4 inhibitor, starting dose should be 6.25 mg and daily dose should not exceed 12.5 mg. Avoid concomitant CYP3A4 strong inhibitors in patients with kidney or liver disease.
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Sulfonamide sensitivity - almotriptan contains a sulfonyl group. Patients with sulfonamide allergy may also have an allergic reaction to almotriptan.
  • Ophthalmic effects - in rat studies, almotriptan was found to bind to melanin in the retina. In another study, almotriptan was associated with corneal opacities in dogs. In both studies, very high doses of almotriptan were used. The significance of these effects in humans is unknown.
  • Liver disease - starting dose should be 6.25 mg. Do not exceed 12.5 mg in 24 hours.
  • Kidney disease
    • CrCl < 30 ml/min: starting dose should be 6.25 mg. Do not exceed 12.5 mg in 24 hours.
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Eletriptan

Relpax®
Relpax® - tablet
  • 20 mg
  • 40 mg
  • 40 mg dose comes in package of 6 or 12 tablets
  • 20 mg dose comes in package of 6 tablets
Migraine headache
  • Initial: 20 - 40 mg
  • May repeat in 2 hours if needed
  • More patients responded to the 40 mg dose in trials
  • Do not exceed 80 mg in 24 hours
Relpax®
YES/$$
(6 tablets)
Other
  • May take without regard to food

Pharmacokinetics
  • Time to max level: 1.5 hours
  • Half-life: 4 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
  • Acute migraine headache with or without aura in adults
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 40 mg dose. Only side effects that occurred at an incidence greater than placebo are listed

  • Dizziness - 6%, P - 3%
  • Somnolence - 6%, P - 4%
  • Weakness - 5%, P - 3%
  • Paresthesia - 3%, P - 2%
  • Dry mouth - 3%, P - 2%
  • Upset stomach - 2%, P - 1%
  • Difficulty swallowing - 2%, P - 0.2%
  • Chest tightness - 2%, P - 1%
  • Abdominal pain - 2%, P - 1%
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • CYP3A4 strong inhibitors - DO NOT COMBINE. Eletriptan is a CYP3A4 sensitive substrate. Concomitant administration can lead to increased exposure to eletriptan. Eletriptan should not be taken within 72 hours of a CYP3A4 strong inhibitor.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Kidney disease - no dose adjustment necessary
  • Liver disease
    • Mild-to-moderate (Child-Pugh A/B) - no dose adjustment necessary
    • Severe (Child-Pugh C) - has not been studied. Not recommended.
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Frovatriptan

Frova®
Frova® - tablet
  • 2.5 mg

Comes in dose pack of 9 tablets
Migraine headache
  • Initial: 2.5 mg
  • May repeat in 2 hours if needed
  • Do not exceed 7.5 mg in 24 hours
Frova®
YES/$$$$
(9 tablets)
Other
  • May take without regard to food

Pharmacokinetics
  • Time to max level: 2 - 4 hours
  • Half-life: 26 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications

  • Acute migraine headache with or without aura in adults
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 2.5 mg dose. Only side effects that occurred at an incidence greater than placebo are listed.

  • Dizziness - 4%, P - 3%
  • Headache - 4%, P - 2%
  • Flushing - 4%, P - 2%
  • Fatigue - 3%, P - 2%
  • Skeletal pain - 3%, P - 2%
  • Dry mouth - 2%, P - 1%
  • Hot or cold sensation - 2%, P - 1%
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Kidney disease - no dose adjustment necessary
  • Liver disease
    • Mild-to-moderate (Child-Pugh A/B) - no dose adjustment necessary
    • Severe (Child-Pugh C) - has not been studied. Use caution.
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Naratriptan

Amerge®
Amerge® - tablet
  • 1 mg
  • 2.5 mg

Comes in dose pack of 9 tablets
Migraine headache
  • Initial: 1 - 2.5 mg
  • May repeat in 4 hours if needed
  • Do not exceed 5 mg in 24 hours
Amerge®
YES/$
(9 tablets)
Other
  • May take without regard to food

Pharmacokinetics
  • Time to max level: 2 - 3 hours
  • Half-life: 6 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications

  • Acute migraine headache with or without aura in adults
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 2.5 mg dose. Only side effects that occurred at an incidence greater than placebo are listed.

  • Nausea - 5%, P - 4%
  • Paresthesia - 2%, P - <1%
  • Dizziness - 2%, P - 1%
  • Drowsiness - 2%, P - <1%
  • Malaise/Fatigue - 2%, P - 1%
  • Throat/neck symptoms - 2%, P - 1%
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Kidney disease
    • CrCl 30 - 90 ml/min - starting dose is 1 mg; do not exceed 2.5 mg over 24 hours
    • CrCl < 15 ml/min - DO NOT USE
  • Liver disease
    • Mild-to-moderate (Child-Pugh A/B) - starting dose is 1 mg; do not exceed 2.5 mg over 24 hours
    • Severe (Child-Pugh C) - DO NOT USE
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Rizatriptan

Maxalt®
Maxalt-MLT®
Maxalt® - tablet
  • 5 mg
  • 10 mg
  • Comes in carton of 18 tablets

Maxalt-MLT®
orally disintegrating tablet

  • 5 mg
  • 10 mg
  • Comes in carton of 18 tablets
Migraine headache
  • Pediatric (6 - 17 years)
    • < 40 kg (88 lbs): 5 mg
    • ≥ 40 kg (88 lbs): 10 mg
    • The efficacy and safety of more than one dose in 24 hours has not been established
  • Adults
    • Initial: 5 - 10 mg
    • May repeat in 2 hours if needed
    • Do not exceed 30 mg in 24 hours

When taken with propranolol
  • Pediatric (6 - 17 years)
    • < 40 kg (88 lbs): DO NOT COMBINE
    • ≥ 40 kg (88 lbs): Do not exceed a single 5 mg dose in 24 hours
  • Adults
    • Initial: 5 mg
    • Do not exceed 15 mg in 24 hours
Maxalt®
YES/$
(9 tablets)

Maxalt-MLT®
YES/$
(9 tablets)
Other
  • May take without regard to food
Maxalt-MLT
  • Administration with liquid is not necessary
  • Dissolves on tongue and is swallowed with saliva
  • Do not remove from blister pack until just prior to dosing

Pharmacokinetics
Maxalt
  • Time to max level: 1 - 1.5 hours
  • Half-life: 2 - 3 hours

Maxalt-MLT
  • Time to max level: 1.7 - 2.2 hours
  • Half-life: 2 - 3 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
  • Acute migraine headache with or without aura in adults and pediatric patients 6 - 17 years old
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 10 mg dose. Only side effects that occurred at an incidence greater than placebo are listed.

Adults
  • Dizziness - 9%, P - 5%
  • Somnolence - 8%, P - 4%
  • Fatigue - 7%, P - 2%
  • Nausea - 6%, P - 4%
  • Paresthesia - 4%, P - <2%
  • Chest pain - 3%, P - 1%
  • Pain, location unspecified - 3%, P - <2%
  • Dry mouth - 3%, P - 1%
  • Neck/throat/jaw pain - 2%, P - 1%
  • Regional pain - 2%, P - 0%
  • Headache - 2%, P - <1%
  • MAO-A inhibitors and nonselective MAO inhibitors - DO NOT COMBINE or start rizatriptan within 2 weeks of discontinuing an MAO inhibitor. Rizatriptan is metabolized by MAO-A. Selective MAO-A and nonselective MAO inhibitors may increase blood levels. Selective MAO-B inhibitors would not be expected to affect rizatriptan levels.
  • Propranolol - propranolol increases rizatriptan levels. See Dosage for dosing recommendations.
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Phenylketonuria - Maxalt-MLT contains phenylalanine. The 5 and 10 mg orally disintegrating tablets contain 1.1 and 2.1 mg phenylalanine, respectively.
  • Kidney disease
    • CrCl ≥ 10 ml/min: no dose adjustment necessary
  • Liver disease
    • Mild (Child-Pugh A) - no dose adjustment necessary
    • Moderate-severe (Child-Pugh B/C) - clearance is decreased. Use caution.
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Sumatriptan

Imitrex®
Zembrace®
Onzetra®
Imitrex® - tablet
  • 25 mg
  • 50 mg
  • 100 mg
  • Comes in packs of 9 tablets

Imitrex® - nasal spray
  • 5 mg
  • 20 mg
  • Comes in box with 6 single-dose spray devices

Imitrex® prefilled syringe and vial
  • 6 mg (6 mg/0.5 ml)

Imitrex® statdose injection
  • 4 mg (4 mg/0.5 ml)
  • 6 mg (6 mg/0.5 ml)
  • Comes in pack with 2 cartridges

Zembrace® injection
  • 3 mg single use autoinjector
  • Comes in pack with 4 injectors

Onzetra® nasal powder
  • Comes in kit with 8 pouches and 2 delivery systems
  • Each pouch contains 2 nosepieces
  • Each nosepiece contains 11 mg sumatriptan

Treximet® - tablet
Sumatriptan : naproxen
  • 85 mg : 500 mg
Migraine headache
    Imitrex tablet
    • Initial: 25 - 100 mg
    • May repeat in 2 hours if needed
    • Do not exceed 200 mg in 24 hours
    • 50 mg dose may be more effective than 25 mg dose
    • If tablet is given after injection, may give up to 100 mg/day of tablet doses
    Imitrex nasal spray
    • Initial: 5, 10, or 20 mg
    • May repeat one time in 2 hours if needed
    • Do not exceed 40 mg in 24 hours
    • If a 10 mg dose is desired, administer a 5 mg dose in each nostril
    • 20 mg dose may be more effective than lower doses
    Imitrex injection
    • Initial: 6 mg subcutaneously
    • May repeat in 1 hour if needed
    • Do not exceed 12 mg in 24 hours
    • If side effects are dose limiting, lower doses (1 - 5 mg) may be used.
    Zembrace injection
    • Initial: 3 mg subcutaneously
    • May repeat in 1 hour if needed
    • Do not exceed 12 mg in 24 hours
    Onzetra nasal powder
    • Initial: 22 mg (2 nosepieces) via delivery device
    • A second dose (22 mg) may be given 2 hours later
    • Do not exceed 44 mg in 24 hours
    Treximet
    • Initial: 1 tablet (85/500)
    • May repeat one time in 2 hours if needed
    • Do not exceed 2 tablets in 24 hours

Cluster headache
    Imitrex injections
    • Initial: 6 mg subcutaneously
    • May repeat in 1 hour if needed
    • Do not exceed 12 mg in 24 hours
Imitrex tablet
YES/$
(9 tablets)

Imitrex nasal spray
YES/$$$-$$$$
(6 sprays)

Imitrex syringe
YES/$$
(2 syringes)

Imitrex vial
YES/$
(1 vial)

Imitrex statdose
YES/$$-$$$
(2 cartridges)

Zembrace
NO/$$$$
(4 injections)

Onzetra
NO/$$$$
(8 pouches)

Treximet
YES/$$$$
9 tablets)

Other
  • May take without regard to food
Imitrex, Zembrace injections
  • Injection is typically given in the side of the thigh or the upper arm
  • Store at room temperature. Protect from light.
Imitrex nasal spray
  • Blow nose before administering
  • Store at room temperature. Protect from light.
Onzetra nasal powder
  • Powder capsule is placed into delivery device
  • Device is placed in nose and mouth. Patient blows through mouthpiece and powder is delivered into nose.
  • Store at room temperature

Pharmacokinetics
Imitrex tablet
  • Time to max level: 2 - 2.5 hours
  • Half-life: 2.5 hours
Imitrex, Zembrace injections
  • Time to max level: 12 minutes
  • Half-life: ∼ 2 hours
Imitrex nasal spray
  • Time to max level: ?
  • Half-life: ∼ 2 hours
Onzetra nasal powder
  • Time to max level: 45 minutes
  • Half-life: 3 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
Imitrex tablet and nasal spray / Zembrace / Onzetra
  • Acute migraine headache with or without aura in adults
Imitrex injections
  • Acute migraine headache with or without aura in adults
  • Cluster headache
Tablet
    NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 50 mg dose. Only side effects that occurred at an incidence greater than placebo are listed.
    • Paresthesia - 5%, P - 2%
    • Chest pain - 2%, P - 1%
    • Neck/throat/jaw pain - 2%, P - <1%
    • Fatigue - 2%, P - <1%

Injection
    NOTE: Side effects listed are from the Imitrex PI (6 mg dose). Only side effects that occurred at an incidence ≥ 3% more than placebo are listed.
    • Injection site reaction - 59%, P - 24%
    • Tingling - 14%, P - 3%
    • Dizziness - 12%, P - 4%
    • Warm/hot sensation - 11%, P - 4%
    • Burning sensation - 7%, P - <1%
    • Heavy feeling - 7%, P - 1%
    • Pressure sensation - 7%, P - 2%
    • Flushing - 7%, P - 2%
    • Weakness - 5%, P - <1%
    • Neck pain stiffness - 5%, P - <1%
    • Feeling of tightness - 5%, P - <1%
    • Numbness - 5%, P - 2%
    • Chest discomfort - 5%, P - 1%
    • Chest tightness - 3%, P - <1%
    • Throat discomfort - 3%, P - <1%

Nasal spray
    NOTE: Side effects listed are for the 20 mg dose. Only side effects that occurred at an incidence ≥ 1% more than placebo are listed.
    • Bad/unusual taste - 24.5%, P - 1.7%
    • Nausea/vomiting - 13.5%, P - 11.3%
    • Nasal discomfort - 3.8%, P - 2.4%
    • Throat discomfort - 2.4%, P - 0.9%
    • Burning sensation - 1.4%, P - 0.1%

Onzetra nasal powder
    • Abnormal taste - 20%, P - 3%
    • Nasal discomfort - 11%, P - 1%
    • Rhinorrhea - 5%, P - 2%
    • Rhinitis - 2%, P - 0%
  • MAO-A inhibitors and nonselective MAO inhibitors - DO NOT COMBINE or start sumatriptan within 2 weeks of discontinuing an MAO inhibitor. Sumatriptan is metabolized by MAO-A. Selective MAO-A and nonselective MAO inhibitors may increase blood levels.
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Local irritation (nasal spray) - in trials, symptoms such as burning, numbness, paresthesia, discharge, and pain or soreness were reported in about 5% of patients. Symptoms typically resolved after 2 hours. The long-term effects of imitrex nasal spray on the nose and throat have not been evaluated.
  • Seizures - in rare cases, patients have experienced seizures after taking sumatriptan. Use caution in susceptible patients.
  • Corneal opacities - in dogs, sumatriptan has been shown to cause corneal opacities and other defects. It is unknown if similar effects occur in humans.
  • Kidney disease - has not been studied. Use caution.
  • Liver disease
    • Mild to moderate (Child-Pugh A/B) - maximum single dose is 50 mg
    • Severe (Child-Pugh C) - DO NOT USE
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Zolmitriptan

Zomig®
Zomig-ZMT®
Zomig® - tablet
  • 2.5 mg
  • 5 mg
  • Comes in pack of 6 tablets for 2.5 mg dose and 3 tablets for 5 mg dose

Zomig-ZMT®
orally disintegrating tablet

  • 2.5 mg
  • 5 mg
  • Comes in pack of 6 tablets for 2.5 mg dose and 3 tablets for 5 mg dose

Zomig® - nasal spray
  • 2.5 mg
  • 5 mg
  • Comes in box with 6 single-dose spray devices
Migraine headache
    Zomig / Zomig-ZMT tablet
    • Initial: 2.5 - 5 mg
    • May repeat in 2 hours if needed
    • Do not exceed 10 mg in 24 hours
    • 2.5 mg tablet may be broken in half for a lower dose. Do not half oral disintegrating tablet.
    • In studies, 5 mg dose offered little benefit over 2.5 mg dose
    Zomig nasal spray
    • Initial: 2.5 mg intranasally
    • May repeat in 2 hours if needed
    • Dose of 5 mg may be used in some patients
    • Do not exceed 10 mg in 24 hours
Zomig®
YES/$
(3X5mg tablets)

Zomig-ZMT®
YES/$
(3X5mg tablets)

Zomig nasal spray
NO/$$$$
(6 doses)

Other
Zomig
  • May take without regard to food
  • 2.5 mg tablet is scored so it may be broken in half
Zomig-ZMT
  • Administration with liquid is not necessary
  • Dissolves on tongue and is swallowed with saliva
  • Do not remove from blister pack until just prior to dosing
  • Do not break in half
Nasal spray
  • Blow nose before use
  • Store at room temperature

Pharmacokinetics
Zomig tablet
  • Time to max level: 1.5 hours
  • Half-life: 3 hours
Zomig-ZMT
  • Time to max level: 3 hours
  • Half-life: 3 hours
Zomig nasal spray
  • Time to max level: 3 hours
  • Half-life: 3 hours
Mechanism of action
  • Triptans are serotonergic agonists that have a high affinity for 5-HT1D and 5-HT1B receptors
  • The mechanism by which they alleviate migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
  • Acute migraine headache with or without aura in adults
NOTE: P = % of patients on placebo who reported side effect. Side effects listed are for the 2.5 mg dose. Only side effects that occurred at an incidence ≥ 2% more than placebo are listed.

  • Nausea - 9%, P - 4%
  • Dizziness - 8%, P - 4%
  • Paresthesia - 7%, P - 2%
  • Neck/throat/jaw pain - 7%, P - 3%
  • Somnolence - 6%, P - 3%
  • Chest pain - 3%, P - 1%
  • Other pressure/tightness/heaviness - 2%, P - 0%
  • MAO-A inhibitors and nonselective MAO inhibitors - DO NOT COMBINE or start zolmitriptan within 2 weeks of discontinuing an MAO inhibitor. Zolmitriptan is metabolized by MAO-A. Selective MAO-A and nonselective MAO inhibitors may increase blood levels. Selective MAO-B inhibitors would not be expected to affect zolmitriptan levels.
  • Ergotamines - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Other 5-HT1 agonists - DO NOT COMBINE. Triptans should not be taken within 24 hours of other 5-HT1 agonists including other triptans.
  • Cimetidine - cimetidine has been shown to double the half-life and AUC of zolmitriptan
  • SSRIs/SNRIs - triptans are serotonergic medications, and they may increase the risk of serotonin syndrome (SS) when taken with SSRIs and SNRIs. A study that looked at the risk of SS with this drug combination found it to be very low. [PMID 29482205]
  • Cardiovascular disease - triptans have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Wolff-Parkinson-White syndrome and other accessory pathway conduction disorders - DO NOT USE
  • Prinzmetal's variant angina - DO NOT USE. Triptans may exacerbate vasospastic heart disease.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Chest pain and tightness - triptans may cause a sensation of pain and tightness in the chest, neck, and/or throat. These symptoms are more common with injectable drug forms. In most patients, triptan-induced chest pain is not thought to be caused by ischemia and is generally not serious. [1,4]
  • Cardiac arrhythmias - in a small number of patients, life-threatening arrhythmias have been reported within a few hours of taking triptans
  • Hypertension - triptans may cause a short-term rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - triptans may exacerbate symptoms of Raynaud's syndrome
  • Vision changes - rare cases of vision changes and vision loss have been reported with triptan use
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking triptans. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including triptans (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Anaphylactic reactions - cases of anaphylaxis including angioedema have been reported in patients taking triptans
  • Ophthalmic effects - in rat studies, zolmitriptan at very high doses was found to bind to melanin in the retina. The significance of this in humans is unknown.
  • Phenylketonuria - Zomig-ZMT contains phenylalanine. The 2.5 mg and 5 mg tablets contain 2.81 mg and 5.62 mg of phenylalanine respectively.
  • Kidney disease
    • CrCl ≥ 26 ml/min: no dose adjustment necessary
    • CrCl 5 - 25 ml/min: clearance is reduced by 25%. Use caution.
  • Liver disease
    • Moderate-severe (Child-Pugh B/C) - clearance is decreased. Severe blood pressure elevations may occur. Use doses < 2.5 mg or avoid use.
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side Effects Drug Interactions Contraindications / Precautions
Ergotamine
tartrate

Cafergot®
Migergot®
Cafergot® - tablet
ergotamine : caffeine
  • 1 mg : 100 mg

Migergot® - suppository
ergotamine : caffeine
  • 2 mg : 100 mg
  • Comes in boxes of 12 suppositories
Migraine headache
    Cafergot
    • Initial: 2 tablets with first sign of headache
    • May take 1 additional tablet every 30 minutes if needed
    • Do not exceed 6 tablets
    • Total weekly dose should not exceed 10 tablets
    Migergot
    • Initial: one suppository at start of headache
    • May repeat one time in 1 hour if needed
    • Do not exceed 2 suppositories
    • Total weekly dose should not exceed 5 suppositories
Cafergot®
NO/$$$$
(30 tablets)

Migergot®
NO/$$$$
(12 suppositories)

Other
Cafergot
  • May take without regard to food
Migergot
  • Store in refrigerator

Pharmacokinetics
Cafergot/Migergot
  • Time to max level: ?
  • Half-life: 2 hours [5]
Mechanism of action
  • Ergotamine is a serotonergic agonist that has a high affinity for 5-HT1B/1D receptors. It also binds dopamine and noradrenaline receptors. [5]
  • The mechanism by which ergotamine alleviates migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
Cafergot/Migergot
  • Migraine headache in adults

NOTE: Incidence of side effects with ergotamine is not well-defined

  • Paraesthesia
  • Nausea and vomiting
  • Numbness
  • Weakness
  • Vertigo
  • Edema
  • Itching
  • Anal ulcer (suppository)
  • CYP3A4 inhibitors - DO NOT COMBINE with strong CYP3A4 inhibitors. Ergotamine is a sensitive CYP3A4 substrate. Life-threatening peripheral ischemia has been reported with combined use. Use caution with mild to moderate CYP3A4 inhibitors.
  • Vasoconstrictors - DO NOT COMBINE. May cause elevated blood pressure.
  • Other 5HT1 agonists (ex. triptans) - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Propranolol - propranolol may potentiate the vasoconstrictive properties of ergotamines
  • Nicotine - nicotine may potentiate the vasoconstrictive properties of ergotamines
  • SSRIs/SNRIs - ergotamine is a serotonergic medication, and it may increase the risk of serotonin syndrome when taken with SSRIs and SNRIs
  • Cardiovascular disease - ergotamines have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Prinzmetal's variant angina - DO NOT USE. Ergotamines may exacerbate vasospastic heart disease.
  • Pregnancy and nursing - DO NOT USE. Ergotamines may cause fetal harm, and they possesses oxytocic properties. Ergotamines may inhibit prolactin and suppress lactation.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Fibrosis - there have been case reports of pleural, retroperitoneal, and cardiac valvular fibrosis following long-term use of ergotamines
  • Hypertension - ergotamines may cause a rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - ergotamines may exacerbate symptoms of Raynaud's syndrome
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking ergotamines. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including ergotamines (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Kidney disease - has not been studied. Do not use in severe kidney disease (CrCl < 30 ml/min).
  • Liver disease - has not been studied. Do not use in severe liver disease (Child-Pugh C)
Drug Dosage form Dosage Generic/Price Other / Pharmacokinetics Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Dihydroergotamine
mesylate

D.H.E. 45®
Migranal®
D.H.E. 45® - injection
  • 1 mg (1 mg/ml)
  • Comes in single dose vials and ampules
  • Comes in packs of 10 vials/ampules

Migranal® - nasal spray
  • 4 mg
  • Comes in vial that is attached to spray device
  • Comes in pack of 8 vials
Migraine headache
    D.H.E. 45 injection
    • Initial: 1 mg given intramuscularly or subcutaneously
    • May repeat in 1 hour if needed
    • Do not exceed 3 mg in 24 hours
    • Total weekly dose should not exceed 6 mg
    Migranal nasal spray
    • One spray (0.5mg) in each nostril. Fifteen minutes later, an additional spray should be administered in each nostril (total dose of 2 mg).
    • No benefit of doses greater than 2 mg has been demonstrated
    • The safety of doses greater than 3 mg in 24 hours has not been evaluated

Cluster headache
    D.H.E. 45 injection
    • Initial: 1 mg given intramuscularly or subcutaneously
    • May repeat in 1 hour if needed
    • Do not exceed 3 mg in 24 hours
    • Total weekly dose should not exceed 6 mg
D.H.E. 45®
YES/$$$$
(10 doses)

Migranal®
YES/$$$$
(8 doses)

Other
D.H.E. 45
  • For subcutaneous injection, inject in the middle of the thigh
  • Store below 25°C (77°F), in light-resistant containers
  • Do not refrigerate or freeze
  • Solution should be clear and colorless
Migranal
  • Sprayer must be primed 4 times prior to administration
  • Once sprayer is assembled, drug is good for 8 hours
  • Store below 25°C (77°F). Do not refrigerate or freeze.

Pharmacokinetics
D.H.E. 45 injection
  • Time to max level: ?
  • Half-life: 9 hours
Migranal
  • Time to max level: ?
  • Half-life: 10 hours
Mechanism of action
  • Dihydroergotamine is a serotonergic agonist that has a high affinity for 5-HT1D receptors. It also binds with high affinity to 5-HT1A, 5-HT2A, 5-HT2C, noradrenaline α2A, α2B α1, and dopamine D2L and D3 receptors.
  • The mechanism by which dihydroergotamine alleviates migraine headaches is not completely understood. Proposed theories include the following:
    • Cranial vasoconstriction
    • Inhibition of vasoactive peptide release
    • Blockade of neurotransmitter release in the dorsal horn
    • Facilitation of descending pain inhibitory systems [1]

FDA-approved indications
D.H.E. 45
  • Acute migraine headache with or without aura in adults
  • Cluster headache
Migranal
  • Acute migraine headache with or without aura in adults
D.H.E. 45
    NOTE: Incidence of side effects with D.H.E. 45 is not well-defined
    • Paraesthesia
    • Dizziness
    • Anxiety
    • Shortness of breath
    • Headache
    • Flushing
    • Diarrhea
    • Rash
    • Increased sweating

Migranal
    NOTE: P = % of patients on placebo who reported side effect. Only side effects that occurred at an incidence of ≥ 2% more than placebo are listed
    • Runny nose - 26%, P - 7%
    • Nausea - 10%, P - 4%
    • Altered sense of taste - 8%, P - 1%
    • Application site reaction - 6%, P - 2%
    • Dizziness - 4%, P - 2%
    • Vomiting - 4%, P - 1%
    • Pharyngitis - 3%, P - 1%
    • Diarrhea - 2%, P - <1%
  • CYP3A4 inhibitors - DO NOT COMBINE with strong CYP3A4 inhibitors. Dihydroergotamine is a sensitive CYP3A4 substrate. Life-threatening peripheral ischemia has been reported with combined use. Use caution with mild to moderate CYP3A4 inhibitors.
  • Vasoconstrictors - DO NOT COMBINE. May cause elevated blood pressure.
  • Other 5HT1 agonists (ex. triptans) - DO NOT COMBINE. May cause prolonged vasospastic reactions. Do not use within 24 hours of each other.
  • Propranolol - propranolol may potentiate the vasoconstrictive properties of ergotamines
  • Nicotine - nicotine may potentiate the vasoconstrictive properties of ergotamines
  • SSRIs/SNRIs - dihydroergotamine is a serotonergic medication, and it may increase the risk of serotonin syndrome when taken with SSRIs and SNRIs
  • Cardiovascular disease - ergotamines have the potential to cause coronary, cerebral, and peripheral vasospasm. Because of this, they should not be used in patients with known cardiac ischemia, cerebral ischemia (TIA and stroke), or peripheral ischemia (bowel ischemia, intermittent claudication, etc.). Patients at high-risk for having vascular disease (e.g. diabetics, smokers, obese, etc.) should also use caution.
  • Prinzmetal's variant angina - DO NOT USE. Ergotamines may exacerbate vasospastic heart disease.
  • Pregnancy and nursing - DO NOT USE. Ergotamines may cause fetal harm, and they possesses oxytocic properties. Ergotamines may inhibit prolactin and suppress lactation.
  • Hemiplegic or basilar migraine - DO NOT USE
  • Fibrosis - there have been case reports of pleural, retroperitoneal, and cardiac valvular fibrosis following prolonged daily use of injectable dihydroergotamine mesylate
  • Hypertension - ergotamines may cause a rise in blood pressure. Use caution in patients with uncontrolled hypertension.
  • Raynaud's syndrome - ergotamines may exacerbate symptoms of Raynaud's syndrome
  • Serotonin syndrome - serotonin syndrome has occurred in patients taking ergotamines. The risk may be higher when taken with other serotonergic medications.
  • Medication overuse headache - overuse of headache medications including ergotamines (e.g. ≥ 10 days a month) may cause an increase in headache frequency and worsening headache with drug withdrawal.
  • Kidney disease - has not been studied. Do not use in severe kidney disease (CrCl < 30 ml/min).
  • Liver disease - has not been studied. Do not use in severe liver disease (Child-Pugh C)
Drug Dosage form Dosage / Studies Generic/Price Other Mechanism of Action / FDA-approved indications Side effects Drug Interactions Contraindications / Precautions
Erenumab-aooe

Aimovig™
Aimovig
SureClick Autoinjector

  • 70 mg/ml
  • Comes as single autoinjector or carton with 2 autoinjectors
Prevention of migraine headache
  • Dosing: 70 mg subcutaneous injection once monthly
  • Some patients may benefit from 140 mg once monthly which is given as two consecutive 70 mg doses
  • If a dose is missed, administer as soon as possible and give next dose in 1 month

Studies
Aimovig™
NO/$$$$
(1 dose)

Other
  • Store in refrigerator protected from light
  • At room temperature, Aimovig is good for 7 days
  • Administer in the abdomen, thigh, or upper arm
Mechanism of action
  • Erenumab-aooe is a human monoclonal antibody that binds to the calcitonin gene-related peptide (CGRP) receptor and antagonizes CGRP receptor function
  • Calcitonin gene–related peptide (CGRP) is a chemical mediator involved in eliciting migraine headaches through nociceptive mechanisms in the trigeminovascular system

FDA-approved indications
  • Prevention of migraines in adults
    NOTE: P = % of patients on placebo who reported side effect
    • Injection site reactions - 6%, P - 3%
    • Constipation - 1%, P - 1%
    • Muscle cramps - <1%, P - <1%
  • None known
  • Anti-erenumab-aooe antibodies - in studies, anti-erenumab-aooe antibodies developed in 6.2% (48/778) of patients receiving 70 mg once monthly and 2.6% (13/504) of patients receiving 140 mg once monthly. It's unknown if antibody development is associated with reduced efficacy or increased hypersensitivity.
  • Kidney disease In patients with mild or moderate renal impairment, pharmacokinetics were not affected. Erenumab-aooe has not been studied in severe renal impairment (CrCl < 30 ml/min). Renal impairment is not expected to affect the pharmacokinetics of erenumab-aooe.
  • Liver disease - has not been studied. Hepatic impairment is not expected to affect the pharmacokinetics of erenumab-aooe.