Drugs for Migraine Flashcards
for migraines with mild to moderate symptoms, what are the first and second line options?
first line: simple analgesics (acetaminophen, acetaminophen-aspirin-caffeine)
second line (if inadequate response): NSAID-triptan combination (naproxen-sumatriptan)
for migraines with moderate to severe symptoms, what are the first (2) and second (3) line options?
first line: selective serotonin 1B/D receptor agonists (“-triptans”) or NSAID-triptan combination (naproxen-sumatriptan)
second line: CGRP antagonists (“-gepants”) or serotonin receptor 1F agonists (“-ditans”) or ergots (dihydroergotamine, ergotamine)
what is the general mechanism of acetaminophen (analgesic) and NSAIDs such as aspirin, naproxen, ibuprofen, and diclofenac in treating migraines?
inhibit prostaglandin synthesis —> prevent neuro-mediated inflammation in the trigeminovascular system
what are the adverse effects and contraindications (3) of acetaminophen (analgesic) and NSAIDs such as aspirin, naproxen, ibuprofen, and diclofenac?
GI adverse effects: dyspepsia, N/V, diarrhea
Renal adverse effects: hemodynamically-mediated AKI, acid-base disorders, acute interstitial nephritis
contraindications: previous ulcer disease, renal disease, aspirin hypersensitivity
what are 3 actions by which selective serotonin 5-HT(1B/D) receptor agonists (“-triptans”) treat migraines?
ex: sumatriptan, rizatriptan, zolmitriptan, eletriptan, almotriptan, naratriptan, frovatriptan
- normalization of dilated intracranial arteries via enhanced vasoconstriction
- inhibition of vasoactive CGRP (calcium gene-related peptide) release from perivascular trigeminal neurons
- inhibition of transmission through second-order neurons ascending to the thalamus
what is the clinical use of “-triptan” medications? what kind of drugs are these?
ex: sumatriptan, rizatriptan, zolmitriptan, eletriptan, almotriptan, naratriptan, frovatriptan
selective serotonin 5-HT(1B/D) receptor agonists
specifically treat migraines (first line for moderate-severe attacks)
basically vasoconstrict over-dilated intracranial arteries and inhibit transmission of neurons ascending to the thalamus (sensation)
what are the adverse effects and contraindications (3) of selective serotonin 5-HT(1B/D) receptor agonists (“-triptans”)?
ex: sumatriptan, rizatriptan, zolmitriptan, eletriptan, almotriptan, naratriptan, frovatriptan
treat mod-severe migraines
adverse: paresthesia, dizziness, somnolence, flushing, chest/neck tightness/pressure
contraindications: ischemic heart disease, uncontrolled HTN, cerebrovascular disease (agonists at coronary artery serotonin receptors!)
also should be avoided in patients receiving SSRI/SNRI antidepressants - risk of serotonin syndrome
what are 3 ways by which calcitonin gene-related peptide (CGRP) receptor antagonists (“-gepants”) treat migraines?
ex: ubrogepant, rimegepant, zavegepant, atogepant
- inhibition of exaggerated trigeminal pain signaling
- inhibition of trigeminal-mediated vasodilation
- inhibition of neurogenic inflammation in the trigeminovascular system
what kind of drugs are “-gepants,” and what is their clinical use?
ex: ubrogepant, rimegepant, zavegepant, atogepant
calcitonin gene-related peptide (CGRP) receptor antagonists
specifically treat migraines (second line for moderate-severe attacks, if “-triptans” fail)
basically inhibit overactivity of trigeminal nerve pain signaling/ vasodilation
what is the potential for drug-drug interactions with calcitonin gene-related peptide (CGRP) receptor antagonists (“-gepants”)?
ex: ubrogepant, rimegepant, zavegepant, atogepant
treat mod-severe migraines (2nd line)
potential interactions when administered alongside CYP3A modulators
safety in children has not been established
what are the 2 mechanisms by which serotonin 5HT(1F) receptor agonists (“-ditans”) such as lasmiditan treat migraines?
- inhibit exaggerated trigeminal pain signaling
- inhibit neurogenic inflammation in the trigeminovascular system
what kind of drugs are “-ditans” such as lasmiditan, and what are their clinical use?
serotonin 5HT(1F) receptor agonists
specifically treat migraines (2nd line for mod-severe attacks if inadequate response to “-triptans”)
basically block overactivity of trigeminal nerve pain signaling
lasmiditan should be avoided in patients receiving which type of antidepressant? why?
serotonin 5HT(1F) receptor agonists (“-ditans”) used to treat migraines
avoid in patients receiving SSRI or SNRI antidepressants due to risk of serotonin syndrome
what are 3 mechanisms by which ergots treat migraines?
ex: dihydroergotamine (DHE), ergotamine
nonselective serotonin 5-HT(1) receptor agonists
- normalization of dilated intracranial arteries via enhanced vasoconstriction
- inhibition of exaggerated trigeminal pain signaling
- inhibition of neurogenic inflammation in the trigeminovascular system
what kind of drug is dihydroergotamine (DHE), and what is it used to treat?
nonselective serotonin 5-HT(1) receptor agonist
treats mod-severe migraine attacks (2nd line, if inadequate response to “-triptans”)
limited use due to tolerability - N/V, chest tightness, diarrhea, paresthesia, muscle pain
