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Migraine Medication List

almotriptan (Axert ®) eletriptan (Relpax ®)
frovatriptan (Frova ®) naratriptan (Amerge ®)
rizatriptan (Maxalt ®) sumatriptan (Imitrex ®)
zolmitriptan (Zomig ®) Pharmacokinetic Properties

Other agents

Cafergot ® (ergotamine/caffeine) dihydroergotamine (DHE 45 ®)
Midrin ® (isometheptine/ dichlorphenazone/ apap):  

Triptans

almotriptan  (Axert ®)  top of page icon

Mechanism of Action
Almotriptan binds with high affinity to 5-HT1D, 5-HT1B, and 5-HT1F receptors. Almotriptan has weak affinity for 5-HT1A and 5-HT7 receptors, but has no significant affinity or pharmacological activity at 5-HT2, 5-HT3, 5-HT4, 5-HT6; alpha or beta adrenergic; adenosine (A1, A2); angiotensin (AT1, AT2); dopamine (D1, D2); endothelin (ETA, ETB); or tachykinin (NK1, NK2, NK3) binding sites.

DOSING (ADULTS):
Oral: Adults: Migraine: Initial: 6.25-12.5 mg in a single dose; if the headache returns, repeat the dose after 2 hours; no more than 2 doses in 24-hour period
Note: If the first dose is ineffective, diagnosis needs to be re-evaluated. Safety of treating more than 4 migraines/month has not been established.

Dosage adjustment in renal impairment: Initial: 6.25 mg in a single dose; maximum daily dose: </= 12.5 mg

Dosage adjustment in hepatic impairment: Initial: 6.25 mg in a single dose; maximum daily dose: </= 12.5 mg

SUPPLIED:
Tablet, as malate: 6.25 mg, 12.5 mg

eletriptan (Relpax ®)  top of page icon

Mechanism of Action
Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. Eletriptan has no significant affinity or pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors.

Two theories have been proposed to explain the efficacy of 5-HT receptor agonists in migraine. One theory suggests that activation of 5-HT1 receptors located on intracranial blood vessels, including those on the arteriovenous anastomoses, leads to vasoconstriction, which is correlated with the relief of migraine headache. The other hypothesis suggests that activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release

INDICATIONS AND USAGE
RELPAX is indicated for the acute treatment of migraine with or without aura in adults.

RELPAX is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see package insert for CONTRAINDICATIONS). Safety and effectiveness of RELPAX Tablets have not been established for cluster headache, which is present in an older, predominantly male population


DOSING (ADULTS):
Oral: Acute migraine: 20-40 mg; if the headache improves but returns, dose may be repeated after 2 hours have elapsed since first dose; maximum 80 mg/day.
Note: If the first dose is ineffective, diagnosis needs to be re-evaluated. Safety of treating >3 headaches/month has not been established.

Dosage adjustment in renal impairment: No dosing adjustment needed; monitor for increased blood pressure

Dosage adjustment in hepatic impairment:
Mild to moderate impairment: No adjustment necessary
Severe impairment: Use is contraindicated

SUPPLIED:
Tablet, as hydrobromide [film coated]: 20 mg, 40 mg

frovatriptan  (Frova ®)  top of page icon

Mechanism of Action
Frovatriptan is a 5-HT receptor agonist that binds with high affinity for 5-HT1B and 5-HT1D receptors. Frovatriptan has no significant effects on GABAA mediated channel activity and has no significant affinity for benzodiazepine binding sites.

Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. In anesthetized dogs and cats, intravenous administration of frovatriptan produced selective constriction of the carotid vascular bed and had no effect on blood pressure (both species) or coronary resistance (in dogs).

INDICATIONS AND USAGE
FROVA is indicated for the acute treatment of migraine attacks with or without aura in adults.

FROVA is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see package insert for CONTRAINDICATIONS). The safety and effectiveness of FROVA have not been established for cluster headache, which is present in an older, predominately male, population

DOSING (ADULTS):
Oral: Migraine: 2.5 mg; if headache recurs, a second dose may be given if first dose provided some relief and at least 2 hours have elapsed since the first dose (maximum daily dose: 7.5 mg)
Dosage adjustment in renal impairment: No adjustment necessary

Dosage adjustment in hepatic impairment: No adjustment necessary in mild to moderate hepatic impairment; use with caution in severe impairment

SUPPLIED:
Tablet, as base: 2.5 mg

naratriptan  (Amerge ®)  top of page icon

INDICATIONS:
Treatment of acute migraine headache with or without aura

DOSING (ADULTS): Oral: 1-2.5 mg at the onset of headache; it is recommended to use the lowest possible dose to minimize adverse effects. If headache returns or does not fully resolve, the dose may be repeated after 4 hours; do not exceed 5 mg in 24 hours.

Elderly: Not recommended for use in the elderly

Dosing in renal impairment:
Clcr: 18-39 mL/minute: Initial: 1 mg; do not exceed 2.5 mg in 24 hours
Clcr: <15 mL/minute: Do not use

Dosing in hepatic impairment: Contraindicated in patients with severe liver failure; maximum dose: 2.5 mg in 24 hours for patients with mild or moderate liver failure; recommended starting dose: 1 mg

SUPPLIED:
Tablet: 1 mg, 2.5 mg

rizatriptan  (Maxalt ®)  top of page icon

DOSING (ADULTS):
Note: In patients with risk factors for coronary artery disease, following adequate evaluation to establish the absence of coronary artery disease, the initial dose should be administered in a setting where response may be evaluated (physician's office or similarly staffed setting). ECG monitoring may be considered.
Oral: 5-10 mg, repeat after 2 hours if significant relief is not attained; maximum: 30 mg in a 24-hour period (use 5 mg dose in patients receiving propranolol with a maximum of 15 mg in 24 hours)

Note: For orally-disintegrating tablets (Maxalt-MLT™): Patient should be instructed to place tablet on tongue and allow to dissolve. Dissolved tablet will be swallowed with saliva.

SUPPLIED:
Tablet, as benzoate (Maxalt®): 5 mg, 10 mg
Tablet, orally-disintegrating, as benzoate (Maxalt-MLT®): 5 mg, 10 mg.

sumatriptan (Imitrex ®)  top of page icon

Mechanism of Action
Sumatriptan is a selective agonist for a vascular 5-hydroxytryptamine1 receptor subtype (probably a member of the 5-HT1D family) with no significant affinity (as measured using standard radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic; dopamine1; dopamine2; muscarinic; or benzodiazepine receptors.

The vascular 5-HT1 receptor subtype to which sumatriptan binds selectively, and through which it presumably exerts its antimigrainous effect, is present on cranial arteries in both dog and primate, on the human basilar artery, and in the vasculature of the isolated dura mater of humans. In these tissues, sumatriptan activates this receptor to cause vasoconstriction, an action in humans correlating with the relief of migraine and cluster headache. In the anesthetized dog, sumatriptan selectively reduces the carotid arterial blood flow with little or no effect on arterial blood pressure or total peripheral resistance. In the cat, sumatriptan selectively constricts the carotid arteriovenous anastomoses while having little effect on blood flow or resistance in cerebral or extracerebral tissues.

INDICATIONS AND USAGE
IMITREX Injection is indicated for 1) the acute treatment of migraine attacks with or without aura and 2) the acute treatment of cluster headache episodes.

IMITREX Injection is not for use in the management of hemiplegic or basilar migraine (see package insert for CONTRAINDICATIONS)

DOSING (ADULTS):
Oral: A single dose of 25 mg, 50 mg, or 100 mg (taken with fluids). If a satisfactory response has not been obtained at 2 hours, a second dose may be administered. Results from clinical trials show that initial doses of 50 mg and 100 mg are more effective than doses of 25 mg, and that 100 mg doses do not provide a greater effect than 50 mg and may have increased incidence of side effects. Although doses of up to 300 mg/day have been studied, the total daily dose should not exceed 200 mg. The safety of treating an average of >4 headaches in a 30-day period have not been established.

Intranasal: A single dose of 5 mg, 10 mg, or 20 mg administered in one nostril. A 10 mg dose may be achieved by administering a single 5 mg dose in each nostril. If headache returns, the dose may be repeated once after 2 hours, not to exceed a total daily dose of 40 mg. The safety of treating an average of >4 headaches in a 30-day period has not been established.

SubQ: 6 mg; a second injection may be administered at least 1 hour after the initial dose, but not more than 2 injections in a 24-hour period. If side effects are dose-limiting, lower doses may be used.

Dosage adjustment in renal impairment: Dosage adjustment not necessary

Dosage adjustment in hepatic impairment: Bioavailability of oral sumatriptan is increased with liver disease. If treatment is needed, do not exceed single doses of 50 mg. The nasal spray has not been studied in patients with hepatic impairment, however, because the spray does not undergo first-pass metabolism, levels would not be expected to alter. Use of all dosage forms is contraindicated with severe hepatic impairment.

Administration
Oral: Should be taken with fluids as soon as symptoms appear.
Injection solution: For SubQ administration; do not administer I.V.; may cause coronary vasospasm.

SUPPLIED:
Note: Expressed as sumatriptan base
Injection, solution, as succinate: 12 mg/mL (0.5 mL)
Intranasal spray: 5 mg (100 uL unit dose spray device); 20 mg (100 uL unit dose spray device)
Tablet, as succinate: 25 mg, 50 mg, 100 mg

zolmitriptan  (Zomig ®) top of page icon

Mechanism of Action
Zolmitriptan binds with high affinity to human recombinant 5-HT1D and 5-HT1B receptors. Zolmitriptan exhibits modest affinity for 5-HT1A receptors, but has no significant affinity (as measured by radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3, 5-HT4, alpha1-, alpha2- or beta1-adrenergic; H1, H2, histaminic; muscarinic; dopamine1, or dopamine2 receptors. The N-desmethyl metabolite also has high affinity for 5-HT1B/1D and modest affinity for 5-HT1A receptors.

Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

INDICATIONS AND USAGE:
ZOMIG is indicated for the acute treatment of migraine with or without aura in adults.

ZOMIG is not intended for the prophylactic therapy of migraine or for use in the management of hemiplegic or basilar migraine (see package insert for CONTRAINDICATIONS). Safety and effectiveness of ZOMIG have not been established for cluster headache, which is present in an older, predominantly male population.

DOSING (ADULTS):
Migraine:
Tablet: Initial: </= 2.5 mg at the onset of migraine headache; may break 2.5 mg tablet in half.

Orally-disintegrating tablet: Initial: 2.5 mg at the onset of migraine headache.

Nasal spray: Initial: 1 spray (5 mg) at the onset of migraine headache.

Note: Use the lowest possible dose to minimize adverse events. If the headache returns, the dose may be repeated after 2 hours; do not exceed 10 mg within a 24-hour period. Controlled trials have not established the effectiveness of a second dose if the initial one was ineffective

Elderly: No dosage adjustment needed but elderly patients are more likely to have underlying cardiovascular disease and should have careful evaluation of cardiovascular system before prescribing.

Dosage adjustment in renal impairment: No dosage adjustment recommended. There is a 25% reduction in zolmitriptan's clearance in patients with severe renal impairment (Clcr 5-25 mL/minute)

Dosage adjustment in hepatic impairment: Administer with caution in patients with liver disease, generally using doses <2.5 mg. Patients with moderate-to-severe hepatic impairment may have decreased clearance of zolmitriptan, and significant elevation in blood pressure was observed in some patients.

Administration
Administer as soon as migraine headache starts.
Tablet: May be broken

Orally-disintegrating tablet: Must be taken whole; do not break, crush or chew; place on tongue and allow to dissolve; administration with liquid is not required

Nasal spray: Blow nose gently prior to use. After removing protective cap, instill device into nostril. Block opposite nostril; breathe in gently through nose while pressing plunger of spray device. One dose (5 mg) is equal to 1 spray in 1 nostril.

SUPPLIED:
Solution, nasal spray [single dose] (Zomig®): 5 mg/0.1 mL (0.1 mL).
Tablet (Zomig®): 2.5 mg, 5 mg.
Tablet, orally-disintegrating (Zomig-ZMT™): 2.5 mg, 5 mg.

Other

Cafergot ® (ergotamine/caffeine)  top of page icon

CLINICAL PHARMACOLOGY
Ergotamine is an alpha adrenergic blocking agent with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The compound also has the properties of serotonin antagonism. In comparison to hydrogenated ergotamine, the adrenergic blocking actions are less pronounced and vasoconstrictive actions are greater.

Caffeine, also a cranial vasoconstrictor, is added to further enhance the vasoconstrictive effect without the necessity of increasing ergotamine dosage.

Many migraine patients experience excessive nausea and vomiting during attacks, making it impossible for them to retain any oral medication. In such cases, therefore, the only practical means of medication is through the rectal route where medication may reach the cranial vessels directly, evading the splanchnic vasculature and the liver.

INDICATIONS AND USAGE
CAFERGOT® (ergotamine tartrate and caffeine)
Indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants or so-called “histaminic cephalalgia”.

DOSING (ADULTS):
Oral: Two tablets at onset of attack; then 1 tablet every 30 minutes as needed; maximum: 6 tablets per attack; do not exceed 10 tablets/week.

Rectal: One suppository rectally at first sign of an attack; follow with second dose after 1 hour, if needed; maximum: 2 per attack; do not exceed 5/week.

SUPPLIED:
Suppository, rectal (Cafergot®): Ergotamine tartrate 2 mg and caffeine 100 mg (12s)
Tablet (Cafergot®, Wigraine®): Ergotamine tartrate 1 mg and caffeine 100 mg

dihydroergotamine  (DHE 45 ®) top of page icon

Mechanism of Action
Dihydroergotamine binds with high affinity to 5-HT1Dalpha and 5-HT1Dbeta receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline alpha2A, alpha2B and alpha1 receptors, and dopamine D2L and D3 receptors.

The therapeutic activity of dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. Two current theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine. One theory suggests that activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache. The alternative hypothesis suggests that activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.

In addition, dihydroergotamine possesses oxytocic properties.

INDICATIONS AND USAGE
Dihydroergotamine mesylate injection is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes.

DOSING (ADULTS):
I.M., SubQ: 1 mg at first sign of headache; repeat hourly to a maximum dose of 3 mg total; maximum dose: 6 mg/week

I.V.: 1 mg at first sign of headache; repeat hourly up to a maximum dose of 2 mg total; maximum dose: 6 mg/week

Intranasal: 1 spray (0.5 mg) of nasal spray should be administered into each nostril; if needed, repeat after 15 minutes, up to a total of 4 sprays. Note: Do not exceed 3 mg (6 sprays) in a 24-hour period and no more than 8 sprays in a week.

Elderly: Patients >65 years of age were not included in controlled clinical studies

Dosing adjustment in renal impairment: Contraindicated in severe renal impairment

Dosing adjustment in hepatic impairment: Dosage reductions are probably necessary but specific guidelines are not available; contraindicated in severe hepatic dysfunction

SUPPLIED:
Injection, solution, as mesylate (D.H.E. 45®): 1 mg/mL (1 mL) [contains ethanol 94%]
Solution, intranasal spray, as mesylate (Migranal®): 4 mg/mL [0.5 mg/spray] (1 mL) [contains caffeine 10 mg/mL]

Midrin ® (isometheptine/ dichlorphenazone/ apap):  top of page icon

INDICATIONS
For relief of tension and vascular headaches*.

*Based on a review of this drug (isometheptene mucate) by the National Academy of Sciences-National Research Council and/or other information, FDA has classified the other indication as "possibly" effective in the treatment of migraine headache. Final classification of the less-than-effective indication requires further investigation.

CLINICAL PHARMACOLOGY
Isometheptene Mucate, a sympathomimetic amine, acts by constricting dilated cranial and cerebral arterioles, thus reducing the stimuli that lead to vascular headaches. Dichloralphenazone, a mild sedative, reduces the patient's emotional reaction to the pain of both vascular and tension headaches. Acetaminophen raises the threshold to painful stimuli, thus exerting an analgesic effect against all types of headaches.


DOSAGE AND ADMINISTRATION
FOR RELIEF OF MIGRAINE HEADACHE: The usual adult dosage is two capsules at once, followed by one capsule every hour until relieved, up to 5 capsules within a twelve hour period.

FOR RELIEF OF TENSION HEADACHE: The usual adult dosage is one or two capsules every four hours up to 8 capsules a day.

SUPPLIED:
Each red capsule contains Isometheptene Mucate USP, 65 mg, Dichloralphenazone USP, 100 mg, and Acetaminophen USP, 325 mg.

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.

Pharmacokinetic properties
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triptan kinetics
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