You are in: eMedicine Specialties > Emergency Medicine > NEUROLOGY Headache, MigraineArticle Last Updated: Jan 3, 2008AUTHOR AND EDITOR INFORMATIONAuthor: Michelle Blanda, MD, Chair, Department of Emergency Medicine, Summa Health System; Professor of Emergency Medicine, Northeastern Ohio Universities College of Medicine Michelle Blanda is a member of the following medical societies: American College of Emergency Physicians and Society for Academic Emergency Medicine Coauthor(s): Jeff T Wright, MD, Instructor, Department of Emergency Medicine, Summa Health System; Corporation President and Consulting Staff, Summa Emergency Associates, Inc Editors: Edward A Michelson, MD, Program Director, Associate Professor, Department of Emergency Medicine, University Hospital Health Systems in Cleveland; Francisco Talavera, PharmD, PhD, Senior Pharmacy Editor, eMedicine; J Stephen Huff, MD, Associate Professor of Emergency Medicine and Neurology, Department of Emergency Medicine, University of Virginia Health Sciences Center; John D Halamka, MD, MS, Associate Professor of Medicine, Harvard Medical School, Beth Israel Deaconess Medical Center; Chief Information Officer, CareGroup Healthcare System and Harvard Medical School; Attending Physician, Division of Emergency Medicine, Beth Israel Deaconess Medical Center; Pamela L Dyne, MD, Associate Professor, Program Director, Department of Medicine, Division of Emergency Medicine, University of California at Los Angeles School of Medicine Author and Editor Disclosure Synonyms and related keywords: migraine variant, classic migraine, cluster headache, aura, dizziness, tinnitus, scotomas, photophobia, visual scintillations, bright zigzag lines, migraine with aura, migraine without aura, dopamine receptor hypersensitivity, visual aura, fortification spectra, geometric visual patterns, hemianopsia, blind spots, hallucinations, hemicrania,throbbingheadache, pulsatile headache, lightheadedness, phonophobia, Valsalva maneuvers, hemiplegic migraine, aphasia, third nerve palsy, ophthalmoplegic migraine, ocular muscle paralysis, ptosis, alcohol consumption, fatigue, emotional stress, birth control pills,vasodilators INTRODUCTIONBackgroundMigraine headaches are recurrent headaches that may be unilateral or bilateral. Migraine headaches may occur with or without a prodrome. The aura of a migraine may consist of neurologic symptoms, such as dizziness, tinnitus, scotomas, photophobia, or visual scintillations (eg, bright zigzag lines). The International Headache Society (IHS) redefined and classified headaches to formulate the current categorization, which has been maintained in the second edition. The headache previously described as classic migraine is now known as migraine with aura, and that described as common migraine is now termed migraine without aura. Migraines without aura are the most common, accounting for more than 80% of all migraines. In April 2000, the US Headache Consortium, a multispecialty group that includes the American College of Emergency Physicians, released evidence-based guidelines for the diagnosis, treatment, and prevention of migraine headaches. Guidelines are also available from the American Academy of Neurology, the National Headache Foundation, and the Canadian Association of Emergency Physicians. PathophysiologyThe pathophysiology of migraine headaches is not clearly understood. Growing evidence supports the role of neurogenic peptides, such as serotonin and dopamine, in the brain. These vasoactive neuropeptides stimulate an inflammatory cascade with the release of endothelial cells, mast cells, and platelets. This inflammation causes vasodilation and a perivascular reaction. The serotonin receptor (5-HT) is believed to be the most important receptor in the headache pathway. Some of the symptoms associated with migraine headaches, such as nausea (80%), vomiting (50%), yawning, irritability, hypotension, and hyperactivity, can be associated with dopamine receptor activation. Dopamine receptor hypersensitivity has been shown experimentally with dopamine agonists such as apomorphine, bromocriptine, and pergolide. Dopamine antagonists, such as metoclopramide (Reglan), haloperidol (Haldol), and prochlorperazine (Compazine), have been shown clinically to treat migraine headaches effectively. FrequencyUnited StatesAn estimated 10-20% of the US population suffers from migraine headaches. Frequency of headaches varies greatly by individual. An estimated 6% of men and 15-17% of women in the United States have migraine. Migraine is the second most common type of headache syndrome in the United States. Tension headaches are the most common. SexMigraines most commonly are found in women, with a 3:1 female-to-male ratio. In childhood, however, migraines are more common in boys than in girls. AgeThe first attack often is in childhood, and incidence increases in adolescence. More than 80% of patients who develop migraines will have a first attack by age 30. Migraines continue through the patient's 30s and 40s. They may begin or occur at any age but are rare after age 50. With increased age, attacks usually decrease in severity and frequency. Age older than 55 years is a strong predictor for intracranial pathology. CLINICALHistoryModerately severe to severe headache with or without a prodrome
Physical
CausesExact etiology is unknown.
DIFFERENTIALSHeadache, Cluster Headache, Tension Meningitis Sinusitis Stroke, Hemorrhagic Stroke, Ischemic Subarachnoid Hemorrhage Temporal Arteritis
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| Drug Name | Acetaminophen and codeine (Tylenol #3) |
|---|---|
| Description | Drug combination indicated for treatment of mild to moderately severe headache. Note: Some patients may respond to maximal acetaminophen alone, without codeine. |
| Adult Dose | 30-60 mg/dose based on codeine content PO q4-6h or 1-2 tab q4h; not to exceed 12 tab/d (4 g acetaminophen/d) |
| Pediatric Dose | 0.5-1 mg/kg/dose based on codeine content PO q4-6h; 10-15 mg/kg/dose based on acetaminophen content; not to exceed 2.6 g/d of acetaminophen |
| Contraindications | Documented hypersensitivity |
| Interactions | CNS depressants or tricyclic antidepressants increase toxicity |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Caution in patients dependent on opiates because this substitution may result in acute opiate-withdrawal symptoms; caution in severe renal or hepatic dysfunction |
| Drug Name | Acetaminophen (Tylenol, Aspirin Free Anacin, Panadol) |
|---|---|
| Description | DOC for treatment of pain in patients with documented hypersensitivity to aspirin or NSAIDs, in those with upper GI disease, or in those taking oral anticoagulants. |
| Adult Dose | 325-650 mg PO q4-6h or 1000 mg tid/qid; not to exceed 4 g/d |
| Pediatric Dose | <12 years: 10-15 mg/kg/dose PO q4-6h prn; not to exceed 2.6 g/d >12 years: 325-650 mg PO q4h; not to exceed 5 doses in 24 h |
| Contraindications | Documented hypersensitivity; G-6-PD deficiency |
| Interactions | Rifampin can reduce analgesic effects; barbiturates, carbamazepine, hydantoins, and isoniazid may increase hepatotoxicity |
| Pregnancy | B - Fetal risk not confirmed in studies in humans but has been shown in some studies in animals |
| Precautions | Hepatotoxicity possible in chronic alcoholism following various dose levels; severe or recurrent pain or high or continued fever may indicate serious illness; acetaminophen contained in many OTC products, and combined use with these products may result in cumulative acetaminophen doses exceeding recommended maximum dose |
| Drug Name | Aspirin (Anacin, Ascriptin, Bayer Aspirin) |
|---|---|
| Description | May alleviate migraine attacks by inhibiting prostaglandin synthesis. Mild migraines usually respond well to this medication. |
| Adult Dose | 325-650 mg PO q4-6h prn; not to exceed 4 g/d |
| Pediatric Dose | 10-15 mg/kg/dose PO q4-6h; not to exceed 60-80 mg/kg/d |
| Contraindications | Documented hypersensitivity; liver damage; hypoprothrombinemia; vitamin K deficiency; bleeding disorders; asthma Because of association with Reye syndrome, do not use in children (<16 y) with flu |
| Interactions | Antacids and urinary alkalinizers may decrease effects; corticosteroids decrease salicylate serum levels; anticoagulants may cause additive hypoprothrombinemic effects and increased bleeding time; may antagonize uricosuric effects of probenecid and increase toxicity of phenytoin and valproic acid; doses >2 g/d may potentiate glucose-lowering effect of sulfonylurea drugs |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | May cause transient decrease in renal function and aggravate chronic kidney disease; avoid use in patients with severe anemia, in those with history of blood coagulation defects, or in those taking anticoagulants |
These agents may alleviate migraine pain by inhibiting prostaglandin synthesis, reducing serotonin release, and blocking platelet aggregation. Although the effects of NSAIDs in the treatment of migraine pain tend to be patient specific, ibuprofen usually is the DOC for the initial therapy. Other options include naproxen, ketoprofen, and ketorolac.
| Drug Name | Naproxen (Anaprox, Naprelan, Naprosyn) |
|---|---|
| Description | Used for relief of mild to moderately severe headaches. Inhibits inflammatory reactions and pain by decreasing activity of enzyme cyclooxygenase, thus inhibiting prostaglandin synthesis. |
| Adult Dose | 500 mg PO followed by 250 mg q6-8h; not to exceed 1.25 g/d |
| Pediatric Dose | <2 years: Not established >2 years: 2.5 mg/kg/dose PO; not to exceed 10 mg/kg/d |
| Contraindications | Documented hypersensitivity; peptic ulcer disease; recent GI bleeding or perforation; renal insufficiency |
| Interactions | Aspirin increases risk of inducing serious NSAID-related adverse effects; probenecid may increase concentrations and, possibly, toxicity; may decrease effects of hydralazine, captopril, and beta-blockers; may decrease diuretic effects of furosemide and thiazides; may increase PT in patients taking anticoagulants (monitor PT closely and instruct patients to watch for signs of bleeding); may increase risk of methotrexate toxicity; may increase phenytoin levels |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | Acute renal insufficiency, interstitial nephritis, hyperkalemia, hyponatremia, and renal papillary necrosis may occur; patients with preexisting renal disease or compromised renal perfusion risk acute renal failure; leukopenia occurs rarely, is transient, and usually returns to normal during therapy; persistent leukopenia, granulocytopenia, or thrombocytopenia warrants further evaluation and may require discontinuation of drug |
| Drug Name | Ketoprofen (Oruvail, Orudis, Actron) |
|---|---|
| Description | Used for relief of mild to moderately severe headaches and inflammation. Administer small dosages initially to patients with small body size, elderly patients, and patients with renal or liver disease. Doses >75 mg does not increase therapeutic effects. Administer high doses with caution, and closely observe the patient for response. |
| Adult Dose | 25-50 mg PO q6-8h prn; not to exceed 300 mg/d |
| Pediatric Dose | <3 months: Not established 3 months to 12 years: 0.1-1 mg/kg PO q6-8h >12 years: Administer as in adults |
| Contraindications | Documented hypersensitivity |
| Interactions | Aspirin increases risk of inducing serious NSAID-related adverse effects; probenecid may increase concentrations and, possibly, toxicity; may decrease effects of hydralazine, captopril, and beta-blockers; may decrease diuretic effects of furosemide and thiazides; may increase PT in patients taking anticoagulants (monitor PT closely and instruct patients to watch for signs of bleeding); may increase risk of methotrexate toxicity; may increase phenytoin levels |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | Caution in congestive heart failure, hypertension, and decreased renal and hepatic function; caution in coagulation abnormalities or during anticoagulant therapy |
| Drug Name | Ketorolac (Toradol) |
|---|---|
| Description | Inhibits prostaglandin synthesis by decreasing activity of enzyme cyclooxygenase, which results in decreased formation of prostaglandin precursors. PO form available, but no advantage vs other less expensive PO NSAIDs. |
| Adult Dose | 30 mg IV single dose (most common route used in ED) >65 years, renal impairment, or body weight <50 kg: 15 mg IV single dose 30-60 mg IM initially, followed by 15-30 mg q6h prn; not to exceed 5 d of treatment; consider only 1-2 d of treatment in elderly patients because of increased risk of GI bleeding |
| Pediatric Dose | Not established; recommended dose 0.4-1 mg/kg once |
| Contraindications | Documented hypersensitivity; peptic ulcer disease; recent GI bleeding or perforation; renal insufficiency; high risk of bleeding Do not administer into CNS |
| Interactions | Aspirin increases risk of inducing serious NSAID-related adverse effects; probenecid may increase concentrations and, possibly, toxicity; may decrease effects of hydralazine, captopril, and beta-blockers; may decrease diuretic effects of furosemide and thiazides; may increase PT in patients taking anticoagulants (monitor PT closely and instruct patients to watch for signs of bleeding); may increase risk of methotrexate toxicity; may increase phenytoin levels |
| Pregnancy | B - Fetal risk not confirmed in studies in humans but has been shown in some studies in animals D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | Acute renal insufficiency, hyperkalemia, hyponatremia, interstitial nephritis, and renal papillary necrosis may occur; increases risk of acute renal failure in patients with preexisting renal disease or compromised renal perfusion; low WBC counts (rare) usually return to normal during ongoing therapy; discontinue therapy if persistent leukopenia, granulocytopenia, or thrombocytopenia occurs |
These agents are used to treat migraine and the emesis associated with acute attacks.
| Drug Name | Prochlorperazine (Compazine) |
|---|---|
| Description | Antidopaminergic drug that blocks postsynaptic mesolimbic dopamine receptors, has an anticholinergic effect, and can depress reticular activating system, possible mechanism for relieving nausea and vomiting. |
| Adult Dose | 5-10 mg PO/IM tid/qid; not to exceed 40 mg/d 2.5-10 mg IV q3-4h prn (most common route given in ED); not to exceed 10 mg/dose or 40 mg/d 25 mg PR bid |
| Pediatric Dose | 2.5 mg PO/PR q8h or 5 mg q12h prn; not to exceed 15 mg/d IV not recommended for children 0.1-0.15 mg/kg/dose IM; change to PO as soon as possible |
| Contraindications | Documented hypersensitivity; bone marrow suppression; narrow-angle glaucoma; severe liver or cardiac disease |
| Interactions | Coadministration with other CNS depressants or anticonvulsants may cause additive effects; with epinephrine may cause hypotension |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Drug-induced Parkinson syndrome or pseudoparkinsonism occurs quite frequently; akathisia most common extrapyramidal reaction in elderly; lowers seizure threshold; caution with history of seizures |
| Drug Name | Promethazine (Phenergan) |
|---|---|
| Description | Phenothiazine derivative that possesses antihistaminic, sedative, antimotion sickness, antiemetic, and anticholinergic effects. |
| Adult Dose | 12.5 mg PO/PR tid and 25 mg hs 25 mg IV/IM, repeat prn in 2 h; switch to PO as soon as possible |
| Pediatric Dose | <2 years: Contraindicated >2 years: 0.25-1 mg/kg PO/IV/IM/PR q4-6h prn |
| Contraindications | Documented hypersensitivity; children younger than 2 y (incidences of death due to respiratory depression) |
| Interactions | May have additive effects with other CNS depressants or anticonvulsants; with epinephrine may cause hypotension |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Caution in cardiovascular disease, impaired liver function, seizures, sleep apnea, and asthma |
| Drug Name | Metoclopramide (Reglan) |
|---|---|
| Description | Indicated for migraine-associated nausea. Works by blocking dopamine receptors in the chemoreceptor trigger zone of the CNS. Can be used as an alternative to prochlorperazine. Studies have shown that prochlorperazine is better. |
| Adult Dose | 5-10 mg PO or 5-20 mg IV/IM tid |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; pheochromocytoma or GI hemorrhage, obstruction or perforation; history of seizure disorders |
| Interactions | Anticholinergic agents may antagonize effects of metoclopramide; opiate analgesics may increase metoclopramide toxicity in CNS |
| Pregnancy | B - Fetal risk not confirmed in studies in humans but has been shown in some studies in animals |
| Precautions | Caution in history of mental illness and Parkinson disease |
| Drug Name | Droperidol (Inapsine) |
|---|---|
| Description | Neuroleptic agent that may reduce emesis by blocking dopamine stimulation of chemoreceptor trigger zone. |
| Adult Dose | 2.5-10 mg IV/IM q3-4h prn (2.5 mg for headache) |
| Pediatric Dose | <2 years: Not established 2-12 years: 0.088-0.165 mg/kg IV/IM prn >12 years: Administer as in adults |
| Contraindications | Documented hypersensitivity; prolonged QT interval |
| Interactions | May increase toxicity of CNS depressants |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Hypovolemic patients may experience hypotension; droperidol may decrease pulmonary arterial pressure; tardive dyskinesia in patients receiving droperidol is 40%; elderly persons may experience high rate of extrapyramidal reactions; life-threatening arrhythmias may occur in patients receiving this medication (for droperidol, the black box warning: potentially fatal QT prolongation; many institutions recommend an ECG or rhythm strip to look for QT prolongation before administering) |
These are direct vasoconstrictors of smooth muscle in cranial blood vessels. Their activity depends on the CNS vascular tone at the time of administration.
| Drug Name | Ergotamine tartrate (Cafergot, Cafatine, Cafetrate) |
|---|---|
| Description | Has alpha-adrenergic antagonist and serotonin antagonist effects. Causes constriction of peripheral and cranial blood vessels. |
| Adult Dose | 2 tab PO at onset of attack, 1 tab q30min prn; not to exceed 6 tab per attack or 10 tab/wk 1 tab SL at first sign of attack and 1 tab q30min; not to exceed 3 tab/d or 5 tab/wk 1 supp PR at first sign of attack with second dose after 1 h prn; not to exceed 2 supp/attack or 5 supp/wk |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; hepatic or renal disease; peptic ulcer disease; sepsis; peripheral vascular disease |
| Interactions | Increases effects of heparin; increases toxicity of nitroglycerin, propranolol, erythromycin, and clarithromycin |
| Pregnancy | X - Contraindicated; benefit does not outweigh risk |
| Precautions | Avoid using prolonged regimens because of danger of causing gangrene or dependency |
| Drug Name | Dihydroergotamine (D.H.E. 45, Migranal Nasal Spray) |
|---|---|
| Description | More effective when given early in migraine attack. Has alpha-adrenergic antagonist and serotonin antagonist effects. |
| Adult Dose | 1 mg IM at first sign of headache, repeat q1h; not to exceed 3 mg total dose 2 mg IV maximum dose for faster effects; most commonly given at 0.5-1 mg IV with antiemetic; not to exceed 6 mg/wk Intranasal: 1 spray into each nostril and repeat prn within 15 min; not to exceed 6 sprays/d or 8 sprays/wk |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; sumatriptan or zolmitriptan within last 24 h; MAOIs in last 2 wk |
| Interactions | Increases effects of heparin; increases toxicity of nitroglycerin, propranolol, erythromycin, and clarithromycin |
| Pregnancy | X - Contraindicated; benefit does not outweigh risk |
| Precautions | Caution in angina, hypertension, impaired renal or hepatic function, or peripheral vascular disease |
The stimulation of 5-HT1 receptors produce a direct vasoconstrictive effect.
| Drug Name | Sumatriptan (Imitrex) |
|---|---|
| Description | Selective agonist for serotonin 5-HT1 receptors in cranial arteries. Suppresses inflammation associated with migraine headaches. |
| Adult Dose | 25 mg PO; if satisfactory response not observed in 2 h, additional dose of up to 100 mg may be administered; additional doses at intervals of 2 h prn; not to exceed 300 mg/d 6 mg SC; if satisfactory response not observed in 1 h, an additional 6 mg SC may be administered; not to exceed 2 injections/d Intranasal: Single dose of 5, 10, or 20 mg may be administered in 1 nostril; give 10-mg dose by administering single 5-mg dose in each nostril; if satisfactory response not observed in 2 h, additional dose may be administered; not to exceed 40 mg/d |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; ischemic heart disease; uncontrolled hypertension; coadministration or within 2 wk of MAOIs |
| Interactions | Toxicity may increase when used within 24 h of ergotamines or other 5-HT agonists; coadministration with SSRIs may cause weakness, hyperreflexia, or incoordination; CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, erythromycin) may increase plasma concentration and subsequent toxicity |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Flushing and chest pain are common; hypertensive crisis, coronary artery vasospasm, cardiac arrest, peripheral ischemia, and bloody diarrhea may occur rarely Patients with known or suspected coronary artery disease may have increased risk of myocardial ischemia, infarction, or other cardiac or cerebrovascular events (5-HT1 agonists may cause coronary vasospasm) |
| Drug Name | Zolmitriptan (Zomig, Zomig-ZMT) |
|---|---|
| Description | Selective agonist for serotonin 5-HT1 receptors in cranial arteries. Suppresses inflammation associated with migraine headaches. |
| Adult Dose | 2.5 mg or 5 mg PO; repeat dose after 2 h prn; not to exceed 10 mg/d |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; ischemic heart disease; uncontrolled hypertension; another serotonin agonist or ergotamine within last 24 h; MAOI within last 2 wk |
| Interactions | Toxicity may increase when used within 24 h of ergotamines or other 5-HT agonists; coadministration with SSRIs may cause weakness, hyperreflexia, or incoordination; CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, erythromycin) may increase plasma concentration and subsequent toxicity |
| Pregnancy | X - Contraindicated; benefit does not outweigh risk |
| Precautions | Flushing and chest pain are common; hypertensive crisis, coronary artery vasospasm, cardiac arrest, peripheral ischemia, bloody diarrhea, and death may occur Decrease dose of almotriptan and do not exceed 12.5 mg/d in renal or hepatic impairment |
| Drug Name | Frovatriptan (Frova) |
|---|---|
| Description | Used to treat acute migraine. Selective 5-HT1B/1D receptor agonist with long half-life of 24 h and low headache recurrence rate within 24-hour period of taking the drug. Results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. Has unique characteristics and benefits in the acute treatment of migraine. |
| Adult Dose | 2.5 mg PO once at onset of migraine attack |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; hemiplegic or basilar migraine; ischemic heart disease; uncontrolled hypertension |
| Interactions | Toxicity may increase when used within 24 h of ergotamines or other 5-HT agonists; coadministration with SSRIs may cause weakness, hyperreflexia, or incoordination |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Hypertensive crisis, coronary artery vasospasm, cardiac arrest, peripheral ischemia, bloody diarrhea, and death may occur |
| Drug Name | Eletriptan (Relpax) |
|---|---|
| Description | Selective serotonin agonist. Specifically acts at 5-hydroxytryptamine 1B/1D/1F (5-HT1B/1D/1F) receptors on intracranial blood vessels and sensory nerve endings to relieve pain associated with acute migraine. |
| Adult Dose | 20-40 mg/dose PO at onset of migraine; if initial dose ineffective, may repeat dose once after 2 h; not to exceed 80 mg/d |
| Pediatric Dose | <18 years: Not established |
| Contraindications | Documented hypersensitivity; severe hepatic impairment; age >65 y; administration within 72 h of potent CYP450 3A4 inhibitors |
| Interactions | Potent CYP450 3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir) may increase toxicity; concurrent administration with ergot-containing drugs may increase vasospastic reactions |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Patients with known or suspected coronary artery disease may have increased risk of myocardial ischemia, infarction, or other cardiac or cerebrovascular events (5-HT1 agonists may cause coronary vasospasm) |
| Drug Name | Almotriptan (Axert) |
|---|---|
| Description | Used to treat acute migraine. Selective 5-HT1B/1D receptor agonist. Results in cranial vessel constriction, inhibition of neuropeptide release, and reduced pain transmission in trigeminal pathways. |
| Adult Dose | 6.25-12.5 mg PO at onset of migraine; may repeat once, not to exceed 25 mg/d |
| Pediatric Dose | <18 years: Not recommended >18 years: Administer as in adults |
| Contraindications | Documented hypersensitivity; hemiplegic or basilar migraine; ischemic heart disease; uncontrolled hypertension |
| Interactions | Toxicity may increase when used within 24 h of ergotamines or other 5-HT agonists; coadministration with SSRIs may cause weakness, hyperreflexia, or incoordination; CYP450-3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, erythromycin) may increase plasma concentration and subsequent toxicity |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Decrease dose and do not exceed 12.5 mg/d in renal or hepatic impairment |
| Drug Name | Rizatriptan (Maxalt, Maxalt-MLT) |
|---|---|
| Description | Selective agonist for serotonin 5-HT1 receptors in cranial arteries and suppresses the inflammation associated with migraine headaches. |
| Adult Dose | 5-10 mg PO q2h prn for headache; not to exceed 30 mg/d |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity |
| Interactions | Toxicity increases when administered concomitantly with ergot-containing drugs, selective serotonin reuptake inhibitors, and MAOIs |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Hypertensive crisis, coronary artery vasospasm, cardiac arrest, peripheral ischemia, bloody diarrhea, and death may occur when administering this medication |
These agents are useful in aborting migraine attacks.
| Drug Name | Isometheptene dichloralphenazone acetaminophen (Midrin) |
|---|---|
| Description | Has sympathomimetic properties. Dilates cranial and cerebral arterioles, causing reduction in stimuli that lead to vascular headaches. |
| Adult Dose | 2 cap PO at once followed by 1 cap q1h until satisfactory response obtained; not to exceed 5 cap/12 h |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; glaucoma; hypertension; organic heart disease; severe renal disease; hepatic disease; MAOI within last 2 wk |
| Interactions | Concurrent MAOIs may result in severe headache, hypertension, and hyperpyrexia, which, in turn, may result in hypertensive crisis |
| Pregnancy | C - Fetal risk revealed in studies in animals but not established or not studied in humans; may use if benefits outweigh risk to fetus |
| Precautions | Caution in hypertension, peripheral vascular disease, and recent cardiovascular injuries |
These agents are used in combination with aspirin and acetaminophen for pain relief and to induce sleep. Caffeine is also used to increase GI absorption. However, butalbital and narcotics are associated with rebound headaches. Increasing the use of combination preparations may fail to provide pain relief and worsen headache symptoms.
| Drug Name | Acetaminophen/butalbital/caffeine (Fioricet) |
|---|---|
| Description | Drug combination used to relieve tension headaches. Barbiturate component has generalized depressant effect on CNS. |
| Adult Dose | 1-2 tab or cap PO q4h; not to exceed 6 tab or cap/d |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity |
| Interactions | Effects decreased by phenothiazines, quinidine, tricyclic antidepressants, theophylline, haloperidol, chloramphenicol, ethosuximide, corticosteroids, warfarin, doxycycline, and beta-blockers; effects increased by CNS depressants, methylphenidate, valproic acid, propoxyphene, and benzodiazepines |
| Pregnancy | D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | Risk of rebound headache and overuse; caution in patients with history of substance abuse |
| Drug Name | Aspirin/butalbital/caffeine (Fiorinal) |
|---|---|
| Description | Drug combination used to relieve tension headaches. Barbiturate component has generalized depressant effect on CNS. |
| Adult Dose | 1-2 tab or cap PO q4h; not to exceed 6 tab or cap/d |
| Pediatric Dose | Not established |
| Contraindications | Documented hypersensitivity; children or adolescents experiencing flulike symptoms or chickenpox |
| Interactions | Effects decreased by phenothiazines, quinidine, tricyclic antidepressants, theophylline, haloperidol, chloramphenicol, ethosuximide, corticosteroids, warfarin, doxycycline, and beta-blockers; effects increased by CNS depressants, methylphenidate, valproic acid, propoxyphene, and benzodiazepines |
| Pregnancy | D - Fetal risk shown in humans; use only if benefits outweigh risk to fetus |
| Precautions | Risk of rebound headache and overuse; caution in patients with history of substance abuse |
Article Last Updated: Jan 3, 2008