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Migraine Medication List
Triptans |
almotriptan (Axert ®)
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INDICATION: Acute treatment of migraine with or without aura Mechanism of Action Selective agonist for serotonin (5-HT1B, 5-HT1D, 5-HT1F receptors) in cranial arteries; causes vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine 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 ®)
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INDICATION: Acute treatment of migraine, with or without aura. NOTE: Oral eletriptan is effective in the treatment of acute migraine attacks, and may be faster-acting than oral sumatriptan. It will compete with oral rizatriptan and oral zolmitriptan (which also have a relatively rapid onset) as a substitute for oral sumatriptan in moderate-to-severe migraine headache. Mechanism of Action Selective agonist for serotonin (5-HT1B, 5-HT1D, 5-HT1F receptors) in cranial arteries; causes vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine 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 ®)
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INDICATION: Acute treatment of migraine, with or without aura. Mechanism of Action Selective agonist for serotonin (5-HT1B and 5-HT1D receptor) in cranial arteries to cause vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine. 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 ®)
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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 ®)
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INDICATIONS: Acute treatment of migraine with or without aura Mechanism of Action Selective agonist for serotonin (5-HT1D receptor) in cranial arteries to cause vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine 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 ®)
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INDICATIONS: Oral, SubQ: Acute treatment of migraine with or without aura SubQ: Acute treatment of cluster headache episodes Mechanism of Action Selective agonist for serotonin (5-HT1D receptor) in cranial arteries to cause vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine 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 ®)
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MOA: Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in
cranial arteries to cause vasoconstriction and reduce sterile
inflammation associated with antidromic neuronal transmission
correlating with relief of migraine INDICATIONS: Acute treatment of migraine with or without aura 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)
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INDICATIONS: Abort or prevent vascular headaches, such as migraine, migraine variants, or so-called "histaminic cephalalgia" Mechanism of Action Has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha-adrenergic receptors depending upon their site; is a highly active uterine stimulant; it causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers 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 ®)
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INDICATIONS: Treatment of migraine headache with or without aura; injection also indicated for treatment of cluster headaches Mechanism of Action Ergot alkaloid alpha-adrenergic blocker directly stimulates vascular smooth muscle to vasoconstrict peripheral and cerebral vessels; also has effects on serotonin receptors 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):
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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. |
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Pharmacokinetic properties
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