Migraines

Question 0

Ergotamine

Answer 0

-ergot alkaloids
-used for migraine pain effective at beginning of attack
-high first pass effect
-combined w/ caffeine (helps w/ bioavailability)
MOA - MULTIPLE
-agonist/antagonist at serotonin receptors
-partial/full agonist at dopamine receptors
-constrict cranial vascular bed
ADE
-decreased blood flow
-diarrhea, nausea, vomiting
Contraindications
-peripheral vascular disease or poor circulation, arteriosclerosis, hypertention, angina, history of heart attack/silent ischemia, liver/kidney disease, serious infection
-*needs 24 hour separation from triptans

Question 1

Sumatriptan

Answer 1

“-triptans”
-used for acute migraines
-for nausea, vomiting, photophobia, phonophobia
MOA
-bind to autoreceptors and suppress the release of GCRP via negative feedback of 5-HT (serotonin)
-vasoconstriction of cerebral vessels
-inhibition of vasoactive neurpeptide and nociceptive neurotransmission
ADE
-fatigue, dizziness, paresthesia, warm sensations, tightness (neck chest, throat)
Contraindications
-hepatic/renal function impairment
-Monoamine Oxidase Inhibitor therapy
-hemiplegic migraine (half face paralyzed)
-basilar migraine (loss of vision, double vision, loss of balance)
-hypersensitivity to triptans
-peripheral vascular disease or uncontrolled BP

Question 2

Dihydroergotamine

DHE

Answer 2

-ergot alkaloid
-intractable migraine (favored by clinicians)
-metabolites similar to parent compound
-effects last longer than expected
MOA - MULTIPLE
-agonist/antagonist at serotonin receptors
-partial/full agonist at dopamine receptors
-constrict cranial vascular bed
ADE
-decreased blood flow
Contraindications
-peripheral vascular disease or poor circulation, arteriosclerosis, hypertention, angina, history of heart attack/silent ischemia, liver/kidney disease, serious infection
-needs 24 hour separation from triptans

Question 3

Propranolol

Answer 3

-Beta-blocker
-first line drug for prevention of migraines
-hepatic first pass effect
-lipophilic (dissolves in fat)
MOA
-blocks beta receptors
-decreased HR, decreased contractility, slow conduction
ADE
-bradycardia
-sedation
-vivid dreams
Interactions
-calcium blockers (verapamil)

Question 4

Prochloperazine

Answer 4

-an antidepressant but useful for migraines
-therapeutic for vomitting, nausea, pain
-prochloroperazine prevents more pain than Sumatriptan
MOA
-D2-antagonist in chemoreceptor trigger receptor zone
-inhibits vomiting center (antiemetic)
ADE
-extrapyramidal (uncontrolled muscle movement)
-akathisia (restlessness)
-given in unison with diphenhydramine (benadryl) to prevent akathisia