Migraine Pharmacology

WVSOM Neuro: Schriefer 3/14/11

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Migraine Pharmacology by Mind Map: Migraine Pharmacology

1. 5HT1 receptor agonists (Triptans)

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

1.2. MOA

1.2.1. 5HT1D/5HT1B receptor agonists

1.2.1.1. 1) constrict large cranial blood vessels

1.2.1.2. 2) decrease inflammation around sensory nerves

1.2.1.3. 3) inhibit trigeminal neuronal discharge

1.3. PK/admin

1.3.1. Triptans mostly differ from each other in kinetics

1.3.1.1. Most are short-acting

1.3.1.2. Naratriptan and Frovatriptan

1.3.1.2.1. long-acting: last long enough to out-last the headache!

1.3.1.2.2. Have longer time til onset

1.3.2. All available orally

1.3.2.1. Sumatriptan & Zolmitriptan

1.3.2.1.1. Also available in nasal spray and SQ injection (d/t big 1st pass effect)

1.4. SE

1.4.1. NV (w/ oral)

1.4.2. Tightness and pressure in chest

1.4.2.1. D/t cross over w/ 5HT-2 receptors in heart

1.4.2.2. CI in pts w/ coronary artery Dz and angina

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

1.4.4. DDI

1.4.4.1. Possible serotonin syndrome in pts on SSRIs

2. Ergotamine & Dihydroergotamine

2.1. Use

2.1.1. Alternative to Triptans

2.1.2. Dihyro- is water-soluble form of ergotamine

2.2. MOA

2.2.1. Binds all subtypes of 5HT1 & 2 receptors, as well as adrenergic and dopaminergic receptors

2.2.1.1. Causes LOTS of SE

2.2.2. Agonist at 5HT1B & 1D receptors on cerebral blood vessels

2.2.2.1. Responsible for anit-migraine effects

2.2.2.2. constriction of dilated arteries

2.3. PK/admin

2.3.1. Slowly absorbed

2.3.1.1. Caffeine increases rate & extent of absorption

2.3.1.1.1. Cafergot = combo prep w/ caffeine

2.3.2. Rapidly metabolized by liver

2.3.2.1. may be stored in tissues

2.3.2.2. Metabolites excreted in bile

2.3.3. Oral and nasal spray forms (DHE only)

2.4. SE

2.4.1. NV (really bad)

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

2.4.3. Chest pain, tachy- or bradycardia

2.4.3.1. B/c it's so non-specific

2.4.4. Allergic rxns

2.4.5. Dependence

2.4.5.1. Rebound headaches

2.4.6. DDI

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

3. Migraine prophylaxis

3.1. Need prophylaxis if > a few migraines/month

3.2. DOC: Propronolol or timolol (beta-blockers)

3.2.1. reduce frequency and severity of attacks

3.2.2. Not all BB will work

3.3. Valproate

3.3.1. Effect similary to BB

3.3.2. Other antiepiliptics (topirmate) work, too

3.4. Amitriptyline

3.5. MAO inhibitors

3.6. SSRI

3.6.1. Good for menstrual migraines

3.7. Verapamil & Nimodipine (Ca-channel blockers)

3.7.1. Prevent vasospams

3.8. Montelukast

3.8.1. MOA

3.8.1.1. Leukotriene analog?

3.8.1.2. Decreases inflammation -> decreased frequency

3.9. CoNZ Q10

3.9.1. OTC remedy (doesn't really work)

3.10. Petasites hybrids (butterbur) root

3.10.1. Actually works!

4. Tx of Cluster Headaches

4.1. Acute

4.1.1. Fast-acting Triptan (nasal or SQ)

4.1.2. O2

4.2. Prevention

4.2.1. DOC: Verapamil

4.2.2. Melatonin may help