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36 Cards in this Set
- Front
- Back
Drugs used in prophylaxis of migraines (5)
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Beta-blockers
TCAs Valproate Ca Channel blockers Methysergide |
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Drugs used in acute (abortive) treatment of migraines (6)
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Sumatriptan
Ergotamine Dihydroergotamine NSAIDs (acetaminophen) Metoclopramide "combination" analgesics |
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1st line agents for migraine prophylaxis
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Beta-blockers
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How long does it take for Beta-blockers to have an effect?
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May take a month
Effects increase w/ time |
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% of people that get benefit from beta-blockers
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60 - 80%
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2nd line agents for migraine prophylaxis
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TCAs
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3rd line agent for migraine prophylaxis
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Methysergide
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Efficacy of Calcium channel blockers vs. beta blockers
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Relatively comparable
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What is the receptor action of methysergide itself?
What are its effects? |
Non-specific 5-HT antagonist
(especially 5-HT2) VSM contraction Platelet aggregation CNS neuron depolarization |
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What are the anti-migraine effects of methysergide due to?
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Its metabolite, methylergonovine
(has serotonergic and alpha-1 agonist properties) |
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Rare side effect of methysergide
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Retroperitoneal fibrosis
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What time limitations are there on administering methysergide?
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Should NOT be used for more than 6 months
1-2 month holidays every 6 months |
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What conditions is methysergide contraindicated in (3)?
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PVD, HTN, angina
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What meds should methysergide NOT be used with?
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Beta-blockers
(additive vasoconstriction?) |
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What type of drug is methysergide?
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Semi-synthetic ergot derivative
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What types of headaches do sumatriptans work for?
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Cluster & migraine headaches
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Why does headache recurrence commonly occur w/ sumatriptans?
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Short half-life (~2 hrs.)
No accumulation of metabolites |
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Why is caffeine used w/ ergotamine
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Caffeine boosts ergotamine's oral bioavailability
(normally, it is very low) |
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How is dihydroergotamine different than ergotamine?
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Same clinical effects
BUT, fewer/milder side effects NOT known to produce dependence |
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When is metoclopramide used for migraines?
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When N&V are a prominent symptom
Remember, this is an anti-emetic |
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How do 2nd generation triptans differ from 1st gens?
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Last longer
Cross BBB better |
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3 examples of "combination" analgesic
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Sedative + analgesic + caffeine
Sedative + NSAID + codeine Sedative + analgesic + sympathomimetic amine |
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When is sedative + analgesic + sympathomimetic amine contraindicated?
(this is a "combination" analgesic) |
HTN, HD, glaucoma, Renal disease
When MAO-Is are being used |
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What are sumatriptans structurally related to?
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Serotonin
Activate serotonin receptors on vessels & nerve endings |
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Breakdown of elimination of sumatriptans
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80% hepatic, 20% renal
|
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What is the major side effect of sumatriptans?
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Coronary vasospasm
Note: 1st dose should be administered in front of physician |
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What drugs do sumatriptans interact with? How?
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SSRIs and MAO-Is --> serotonin syndrome
Ergots --> additive vasospasm |
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What is the receptor action of ergotamine? What are the effects?
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Serotinergic, dopaminergic, alpha-adrenergic
(uterine contraction, vasoconstriction, N&V) Ergot receptors --> stasis, thrombosis, gangrene |
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What is ergotamine structurally related to?
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LSD
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What situations is ergotamine contraindicated in?
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PVD, HTN, ischemic HD, renal or hepatic disease, pregnancy
Contraindications due to the ergot effects (thrombosis, stasis, etc.) |
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What can boost the efficacy of NSAIDs and acetaminophen?
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Codeine
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When are tiptans contraindicated? Why?
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In CAD
They cause coronary vasospasm |
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What is the most commonly used drug for abortion of a migraine?
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Sumatriptan
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In a mild migraine, how should you treat (2)?
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ID and avoid triggering factors
Mild analgesics (anti-emetics if necessary) |
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In a moderate migraine, how should you treat (2)?
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Triptan [preferred over ergots](IF CAD not present)
"Combination" analgesic (IF CAD is present) |
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In a severe migraine, how should you treat (3)?
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Triptan or ergot
Anti-emetics Try prophylaxis for 6 months and reassess |