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Exam #3 - Drugs for Treatment of Migraines
N/A
29
Pharmacology
Graduate
10/24/2009

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Term
Phases of Migraine Headaches
Definition
premonitory features, aura, headache, and resolution
Term
Premonitory Features
Definition
pt my experience mood & appetite changes hours to days before migraine attack; neurologic symptoms (photophobia, phonophobia), psychological symptoms (anxiety, depression, euphoria, irritability, drowsiness, hyperactivity, restlessnes); autonomic symptoms (polyuria, diarrhea, constipation); & constitutional symptoms (stiff neck, yawning, thirst, food cravings, anorexia)
Term
Common Migraine
Definition
migraine without aura
Term
Classic Migraine
Definition
migraine WITH aura
Term
Aura
Definition
phase of a migraine attack that refers to focal neurological symptoms that occur in 31% of pts with migraines; usually lasts less than 1 hr & usually ends 1 hr before headache phase starts
Term
Headache Phase
Definition
phase of migraine that starts about 1 hr after the end of aura; progresses from a dull ache to intense unilateral pulsations taht worsen over time; about 90% of pts will have GI symtpoms like nausea and vomiting; may also experience photophobia, phonophobia, or osmophobia during this phase; pain begins in frontotemporal region & may extend to neck & back of skull; may last 4 to 72 hrs if left untreated
Term
Alleviating headache phase of Migraine Attacks
Definition
rest in a dark room; DO NOT do any physical activity
Term
Resolution Phase
Definition
during this phase, pts may feel tired/depressed or refreshed/euphoric
Term
Cause of Migraine Headaches
Definition
thought to result from inappropriate dilation of intracranial extracerebral blood vessels; inappropriate activation of trigeminal complex which causes dilation of intracranial blood vessels through the inappropriate release of CGRP (calcitonin gene-related product), NKA (neurokinin A), & SP (substance P)
Term
Prophylactic Therapy of Migraines
Definition
type of treatment used when frequent attacks requiring acute medication more than twice a week
Term
Treatment of Mild-Moderate Acute Therapy Symptoms
Definition
1st line: analgesics, NSAIDS (acetaminophen, APAP/aspirin/caffeine, aspirin, ibuprofen, naproxen); 2nd line: combination analgesics (midrin, aspirin/butalbital/caffeine); 3rd line: triptans; 4th line: opioid combination analgesics, butorphanol nasal spray
Term
Treatment of Severe Symptomatic Acute Attacks
Definition
1st line: DHE or ergotamine tartrate (bypass NSAIDs, analgesics, combos); 2nd line: triptans; 3rd line: opioid combination analgesics
Term
Rebound Headache
Definition
medication overuse headache that occurs when using drugs for abortive treatment of migraines; characterized by increased frequency of headaches and an increase in drug consumption; most commonly occurs when taking: combo analgesics, opiates, ergotamine tartrate, & triptans; use these meds only about 2 times per week to avoid problem
Term
NSAIDs
Definition
used as abortive treatment of migraines; analgesics; MoA: ability to block prostaglandin synthesis which prevents inflammation in trigeminovascular system & lessens pain sensitization; Use with caution in pts with peptic ulcer disease, renal disease, or hypersensitivies to aspirin
Term
isometheptene + dichoralphenazone + APAP (Midrin)
Definition
combo analgesic that is as effective as oral ergotamine tartrate with fewer side effects; first drug in combo is a synthetic sympathomimetic with alpha & beta-adrenergic activity causing mild vasoconstrictor activity; 2nd drug in product is included for its sedative effect; C/I's: glaucoma, renal disease, HPN, heart & liver disease, concurrent use with MAOI's
Term
Opiates (butorphanol)
Definition
last resort medications for treatment to abort migraines; reserved for severe infrequent HAs where conventional therapies are not effective or are contraindicated
Term
ergotamine tartrate
Definition
oral, sublingual, and suppository drug used in acute treatment of moderate to severe migraines; MoA: "dirty drug" that interacts with serotonin, DA, and adrenergic receptors; effectiveness is mediated by activation of 5-HT1b receptors & vasoconstriction of dilated intracranial arteries, resulting in decreased pulsations, also may reduce neurogenic inflammation; Max oral/sublingual dose: 6 mg/attack or 10 mg/wk; may be combined with caffeine to potentiate vasoconstriction & improve intestinal absorption; may be combined with Belladonna alkaloids to reduce nausea & vomiting
Term
Toxicity, ADRs, C/I's for ergotamine tartrate
Definition
drug is a powerful vasoconstrictor; C/I: pts with peripheral vascular disease, beta-blockers may potentiate vasoconstriction caused by drug; GI upset (nausea, vomiting, anorexia): activates central DA receptors in CRTZ, may require adjunctive therapy with metoclopramide (Reglan); erythromycin can interfere with liver metabolism of ergotamine & cause ergot toxicity; more C/I's: cardiovascular disease, sepsis, liver & kidney disease, pregnancy/breast feeding
Term
Dihydroergotamine (D.H.E. 45)
Definition
drug effective in acute treatment of moderate to severe migraines; incompletely absorbed in GI tract, administered parenterally; MoA: direct vasoconstriction of dilated intracranial arteries leading to decreased pulsations & reduced neurogenic inflammation by decreasing release of vasodilator/proinflammatory neuropeptide transmitters; causes less vasoconstriction than ergotamine
Term
sumatriptan (Imitrex)
Definition
derivative of serotonin used in acute treatment of moderate to severe migraines; SC, PO, or nasal spray forms; metabolized by MAO-A; MoA: constriction of inflamed/dilated intracranial arteries & by inhibiting release of vasodilator/proinflammatory mediators, relieves nausea, vomiting, photophobia, & phonophobia associated with migraine attacks; SEs: cardiovascular (MIs...C/I in pts with pre-existing coronary artery disease), injection site rxn, triptan symptoms (chest & throat tightness, difficulty in breathing, panic/anxiety, paresthesias, feeling of heaviness), C/I with use of a MAOI
Term
second generation triptans (zolmitriptan [Zomig], etc.)
Definition
triptans with greater bioavailability; act at peripheral components of trigeminovascular system; have greater lipid solubility, and act centrally to inhibit pain transmission in trigeminal nucleus
Term
prochlorperazine (Compazine)
Definition
DA antagonist useful for treatment of acute migraine unresponsive to sumatriptan, DHE, or oral analgesics; relieve headache pain & have anti-emetic activity
Term
methysergide (Sansert)
Definition
effective agent for prophylactic management of migraine & cluster headaches; prescribed only when other prophylactic therapies (propanolol) fail; no longer available in US; MoA: 5-HT2 receptor antagonist and 5-HT1 receptor agonist; NOT effective for acute treatment of migraines; protective effect takes 1-2 days to develop; SE's: FIBROSIS & FIBROTIC COMPLICATIONS - to avoid, d/c drug for about 4 weeks every 6 months, CV: angina, CNS: LSD-like effects; C/I's: pts with cardiovascular disease & fibrotic disease
Term
propanolol (Inderal) & timolol
Definition
first drugs of choice for migraine prophylaxis; beta-blockers that lack partial agonist activity (ISA) are most effective; SEs: fatigue, cold extremities, dizziness, CNS side effects, impotence
Term
amitriptyline (Elavil)
Definition
tricyclic antidepressant that can be used to prophylactically treat migraines; MoA: unknown but thought to involve down regulation of central 5-HT2 and adrenergic receptors; SEs: anticholinergic effects (dry mouth, blurred vision, urinary retention, cardiac arrhythmias); C/I in pts with glaucoma, BPH, & heart disease
Term
calcium channel blockers (verapamil)
Definition
unapproved use to treat migraines prophylactically; questionable effectiveness, takes up to 8 wks for any possible advantages; MoA: unknown but thought to alter vascular smooth muscle reactivity; SEs: constipatoin, orthostatic hypotension; C/I's: bradycardias, concomitant use of beta-blockers
Term
valproic acid:valproate sodium 1:1 (Depakote)
Definition
antiepileptic drug found to be effective in migraine prophylaxis; MoA: facilitating GABA neurotransmission, modulating glutamate, & inhibiting Na & Ca channel activity; SE's: N/V, weakness, somnolence, weight gain, tremor, hair loss, hepatic toxicity
Term
topiramate (Topamax)
Definition
anticonvulsants used to prophylactically treate migraines; Adverse Effects: paresthesia, fatigue, anorexia, weight loss, diarrhea, memory problems, & nausea
Term
gabapentin (Neurontin)
Definition
anticonvulsants used to treat migraines prophylacticaly; Adverse Effects: somnolence, asthenia (weakness), dizziness
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