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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"


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


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)


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


Alternative to Triptans

Dihyro- is water-soluble form of ergotamine


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


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)


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


Effect similary to BB

Other antiepiliptics (topirmate) work, too


MAO inhibitors


Good for menstrual migraines

Verapamil & Nimodipine (Ca-channel blockers)

Prevent vasospams


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


Fast-acting Triptan (nasal or SQ)



DOC: Verapamil

Melatonin may help