pharmacology

Question 1

-triptan MOA

Answer 1

agonists at 5-HT 1D/1B presynaptic autoreceptors causing vasoconstriction of painful intracranial vessels, inhibiting vasoactive neuropeptides (CGRP), and inhibiting nociceptive neurotransmission

Question 2

-triptan use

Answer 2

migraine symptoms (nausea, vomiting, photophobia, phonophobia)

Question 3

-triptan selection

Answer 3

fast vs. slow onset of activity / duration
formulation (oral, injection, nasal)
formulary tier and availability (sumatriptan = generic)

Question 4

-triptan pharmacokinetics

Answer 4

oral, nasal, subcutaneous (sumatriptan)

rapid onset of action

Question 5

-triptan AE’s

Answer 5

fatigue, dizziness, paresthesia, warm sensations, tightness (neck, chest, throat)

Question 6

-triptan contraindications

Answer 6

hepatic / renal dysfunction
MAO inhibitor therapy
hemiplegic or basilar (loss of vision, double vision, loss of balance) migraines
peripheral vascular disease / HTN

Question 7

ergot alkaloid basics

Answer 7

produced by Claviceps pururea (fungus) that also produces histamine, ACh, etc.
DHE, ergotamine, methysergide (prophylactic)

Question 8

ergot alkaloid MOA

Answer 8

agonist / antagonist at alpha1-adrenergic and 5HT 1A / 1D receptors
partial or full agonists at dopamine receptors (AE)
cause vasoconstriction of cranial vascular bed

Question 9

ergotamine uses

Answer 9

migraine pain, effective at beginning of attack

Question 10

DHE uses

Answer 10

intractable migraine

Question 11

ergotamine ADME

Answer 11

oral and suppository
high first pass effect
combined with caffeine to help bioavailabilty
excreted by liver

Question 12

DHE ADME

Answer 12

SC, IV, IN, oral
metabolized by liver, excreted in feces
metabolites are similar to parent compound -> effects last longer than expected

Question 13

ergot alkaloid AE

Answer 13

decreased blood flow to brain, heart, and extremities

ergotamine: diarrhea, nausea, vomiting

Question 14

ergot alkaloid contraindications

Answer 14

obstructive vascular disease / poor circulation
collagen disease
HTN, arteriosclerosis
history of MI, angina
liver / kidney disease
serious infection
separate dose from triptans by 24 hours

Question 15

beta-blockers use

Answer 15

first line drug for migraine prevention

Question 16

beta receptors

Answer 16

1 - stimulates heart
2 - vasodilation, bronchodilation
3 - relaxes bladder

Question 17

propranolol ADME

Answer 17

oral
hepatic first pass effect, metabolized by liver
lipophilic

Question 18

beta-blocker AE’s

Answer 18

bradycardia, sedation, vivid dreams

Question 19

beta-blocker drug interactions

Answer 19

with calcium blockers (i.e. verapamil) -> causes severe hypotension, bradycardia, heart failure, cardiac conductance abnormalities

Question 20

indications for migraine prevention medication

Answer 20

> 2 per month, lasting longer than 24 hours each
disrupt life for 3 or more days
abortive therapy fails or is overused (>2/week)
symptom meds fail or are contraindicated
production or risk of permanent neurologic injury

Question 21

prochlorperazine MOA

Answer 21

antiemetic, antipsychotic

D2-antagonist in chemoreceptor trigger receptor zone

Question 22

prochlorperazine use

Answer 22

migraine associated vomiting, nausea, pain

Question 23

prochlorperazine ADME

Answer 23

oral, rectal, IV

reduces pain more than sumatriptan

Question 24

prochlorperazine AE’s

Answer 24

extrapyramidal (acute dystonic effects - involuntary muscle contractions)
akathisia (restlessness) - but less if given with diphenhydramine

Question 25

botulinum toxin A

Answer 25

MOA: enzymatic removal of amino acids in fusion proteins critical to release of ACh
use: prevention of migraine

Question 26

medication overuse headache (MOH)

Answer 26

prevalent in 50% of patients in headache centers

treat with education and detoxification