Migraine Drugs Flashcards
Neurogenic inflammation cascade
Nerve endings release inflammatory substances, some of which activate cyclooxygenase (leading to creation of prostaglandins). These prostaglandins contribute to inflammation and excite nociceptors. Pain transmitted to central nervous system.
Why aren’t opioids used to treat headaches?
Can actually make headache worse:
Increase N/V
Contribute to mast cell degranulation (increased inflammation)
Prevents normal clearance of glutamate, exacerbating CSD.
NSAIDS
Unlikely to cause headache, safe in the presence of vascular disease, non-sedating, no nausea, high doses required.
What is the role of dopamine in migraine?
Dopamine is responsible for the prodromal symptoms of migraine (yawning, cold hands + feet, urination, chocolate craving).
D2 agonist in migraineurs?
Causes migraine
D2 antagonists in migraineurs?
Sedative, antiemetic properties, used to treat migraine
Chlorpromazine, prochlorperazine, droperidol, metoclopramide, domperidone
(Don’t need to know these names)
Advantages of D2 antagonists in migraine treatment?
Disadvantages?
When used IV very effective, reduce nausea/vomiting.
Problems: Prolonged QT, orthostatic hypothension, extrapyramidal effects
Ergot
Potent vasoconstrictor found in rye
Ergotamine
Synthetic ergot, used to treat migraines. Structurally similar to serotonin, NE, and DA. Potent vasoconstrictor – avoid in coronary disease
When to avoid ergotamine?
In patients with coronary disease.
Dihydroergotamine
Injection, intrapulmonary. IV use requires antiemetics.
Long half-life and duration of action.
Useful for medication overuse headaches, but be careful in vascular disease.
Effect of 5-HT IV on migraine
Relieves, but has completely intolerable side-effects
Important serotonin receptors in migraine?
5HT1B (blood vessel constriction), 5HT1D (Nerves), 5HT1F
How do triptans work?
They activate 5HT1B, 5HT1D, 5HT1F (some) autoreceptors, which decrease painful NTs (decrease neurogenic inflammation). Reduce all aspects of migraine disability, no sedation, intrinsic anti-emetics.
Best acting triptan?
Sumatriptan (also has IV form)