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Migraine Pharmacology by Mind Map: Migraine Pharmacology
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Migraine Pharmacology

5HT1 receptor agonists (Triptans)

There's a bunch - They all end in "-triptan"

MOA

5HT1D/5HT1B receptor agonists, 1) constrict large cranial blood vessels, 2) decrease inflammation around sensory nerves, 3) inhibit trigeminal neuronal discharge

PK/admin

Triptans mostly differ from each other in kinetics, Most are short-acting, Naratriptan and Frovatriptan, long-acting: last long enough to out-last the headache!, Have longer time til onset

All available orally, Sumatriptan & Zolmitriptan, Also available in nasal spray and SQ injection (d/t big 1st pass effect)

SE

NV (w/ oral)

Tightness and pressure in chest, D/t cross over w/ 5HT-2 receptors in heart, CI in pts w/ coronary artery Dz and angina

Overuse (>2x/wk) -> rebound headache

DDI, Possible serotonin syndrome in pts on SSRIs

Ergotamine & Dihydroergotamine

Use

Alternative to Triptans

Dihyro- is water-soluble form of ergotamine

MOA

Binds all subtypes of 5HT1 & 2 receptors, as well as adrenergic and dopaminergic receptors, Causes LOTS of SE

Agonist at 5HT1B & 1D receptors on cerebral blood vessels, Responsible for anit-migraine effects, constriction of dilated arteries

PK/admin

Slowly absorbed, Caffeine increases rate & extent of absorption, Cafergot = combo prep w/ caffeine

Rapidly metabolized by liver, may be stored in tissues, Metabolites excreted in bile

Oral and nasal spray forms (DHE only)

SE

NV (really bad)

M weakness & pain, Numbness & tingling in fingers and toes

Chest pain, tachy- or bradycardia, B/c it's so non-specific

Allergic rxns

Dependence, Rebound headaches

DDI, Cafergot + CYP3A4 inhibitor (macrolide, protease inhibitior) may cause fatal ischemia

Migraine prophylaxis

Need prophylaxis if > a few migraines/month

DOC: Propronolol or timolol (beta-blockers)

reduce frequency and severity of attacks

Not all BB will work

Valproate

Effect similary to BB

Other antiepiliptics (topirmate) work, too

Amitriptyline

MAO inhibitors

SSRI

Good for menstrual migraines

Verapamil & Nimodipine (Ca-channel blockers)

Prevent vasospams

Montelukast

MOA, Leukotriene analog?, Decreases inflammation -> decreased frequency

CoNZ Q10

OTC remedy (doesn't really work)

Petasites hybrids (butterbur) root

Actually works!

Tx of Cluster Headaches

Acute

Fast-acting Triptan (nasal or SQ)

O2

Prevention

DOC: Verapamil

Melatonin may help