migraine Flashcards
Ergotamine tartrate (Ergomar)
ergotamine tartrate/caffeine/l-belladona alkaloids/sodium pentobarbital (30mg) (Ercaf, Wigraine); ergotamine/caffeine (Cafergot suppository)
Ergot Alkaloids and drugs that act at 5-HT1B receptors and 5HT1D (inhib. rel of pro-inflamm. NTs) SLD
-potent vasocontrictors
(ha due to vasodilation)
- caffiene may help absorption
- “dirty” drug: interacts with serotonin, dopamine, and adrenergic receptors
- only use after triptans fail
- GI upset (use with metoclopramide- anti-emetic)
Sumatriptan (Imitrex)
Specific 5-HT1B/1D agonists,*FLDs* first generation (SubQ, nasal spray, oral, transdermal patch)
-use for acute tx mod-sev. migraine if OTC analgesic/NSAIDs fail, relieve N/V, photo/phonophob
vasoconstriction of dilated intracranial arteries, inhibit rel. of vasodilator/proinflamm. mediators from trigeminal nerve endings
- metab. by MAO
- SE: peripheral vasoconstriction, MI
Zolmitriptan (Zomig, Zomig ZMT)
Specific 5-HT1B/1D agonists second generation (*nasal or oral*)
acts at peripheral trigeminal (vasoconstriction, inhib. vasodilator release)
AND acts centrally: inhibits pain transmission in trigeminal nucleus
-access deep within CNS (more lipophilic) @ 5HT rec
Metoclopramide (Reglan)
Dopamine Antagonists – Antiemetics (IV, IM or oral)
- tx N/V and ha
- use when unresponsive to triptans or oral analgesics
- can give in combo with NSAIDs or sumitriptan
Prochlorperazine (Compazine)
Dopamine Antagonists – Antiemetics (IV, IM or oral)
- tx N/V and ha
- use when unresponsive to triptans or oral analgesics
- can give in combo with NSAIDs or sumitriptan
Chlorpromazine (Thorazine)
Dopamine Antagonists – Antiemetics (IV, IM or oral)
- tx N/V and ha
- use when unresponsive to triptans or oral analgesics
- can give in combo with NSAIDs or sumitriptan
ASA
analgesic
Acetaminophen
analgesic
-effective at tx photophobia, phobia, pain
excedrin: combo of acetaminophen, NSAID (ASA) and caffeine
Ibuprofen
analgesic
propranolol
B-blocker
- ppx to prev. migraines
- ones that lack partial agonist activity have best effect
tox: B-blockers may augment vasoconstriction from ergotamine
timolol
B-blocker
-ppx to prev. migraines
atenolol
B-blocker
-ppx to prev. migraines
amitriptylin (Elavil)
antidepressant
- ppx to prev. migraines
- down-reg of central 5-HT2 and adrenergic receptors (essentially like up-regulating 5-HT1)
-SEs: sedation, anticholinergic SEs
Valproate (Depakote)
anticonvulsant
-similar global brain affect btw seizure and ha
- many drug interactions, only use for severe
- dec. neuronal activity: facilitate GABA NT, modulate glutamate, inhib. Na+ and Ca2+ channels
topiramate (Topamax)
anticonvulsant
-similar global brain affect btw seizure and ha
gabapentin
Neurontin
anticonvulsant
-similar global brain affect btw seizure and ha
Botulinum toxin type A (Botox)
migraine tx, inhib. rel. ACh
effect may last up to 3 months
only med good for medication rebound/overuse ha
migraine prevalence
44.5 million US
F>M
genetic factors
$13 billion lost due to dec. work productivity
migraine effects
decrease oral absorption of drugs during migraines
dec. GI motility
*caffeine helps
90% N/V -consider parenteral admin
migraine prodrome
migraine aura
migraine w.out aura (common migraine)
migraine w. aura (classic migraine)
visual disturbance-“fortification” spectrum-light disturbance, looks like a fort
narrowing of visual fields
headache characteristics
dull ache--intense pulsations typ. Unilat N/V photophob/phonophobia lasts 4-72 hrs improve w. resting in dark room worse with physical activity W>M
postdrome
During this phase some patients may feel tired/depressed or refreshed/euphoric
menstrual migraine
onset of menstruation, due to hormone changes
tension type
muscle contraction headaches - Dull persisting, non-pulsating, non-debilitating, bilateral pain (hatband pattern), not aggravated by physical activity, usually an absence of nausea/vomiting, and absence of aura and photophobia/phonophobia
cluster ha tx
abortive:
O2 inhalation
ergotamine tartrate, dihydroergotamine
subcutaneous sumatriptan
ppx: verapamil lithium carbonate ergotamine tartrate prednisone
physio of migraines
dilated/enlarged BVs–>sensory to brain–>pain perception
(Ergot alkaloids/sumatriptan, zolmiltriptan)
drugs act on 5HT receptors to constrict
AND
5HT1D to inhibit release of pro-inflammatory NTs:
CGRP, NKA, SP
vascular theroy
aura: vasoconstric
pain: vasodil
spreading depression
spreading dec. in cortical e- activity
serotonergic abnormalities
IV inj. of 5-HT can abort spontan./drug-ind. migraine
act at level of serotonin type 1 receptors
abortive tx
OTC NSAIDs, excedrin, tylenol, advil
home: triptans–>ergot alkaloids, dihydroergotamine–>butorphanol nasal spray (last resort)
ER: IV NSAID + metoclopramide–>dihydroegotamine + metoclopramide–>metaclopramide + dexamethasone
> 3 attacks per wk
ppx tx
rebound ha
med overuse ha, can’t take >2x week
combination analgesics, opiates, ergotamine and the triptans
botulinum toxin is only relieving for med overuse ha
NSAIDs mechanism
dec. PG formation–>dec. inflammation in trigeminovascular system–>lessens pain sensitization
Dihydroergotamine (D.H.E.45) (IV, IM, SC, nasal) dihydroergotamine mesylate nasal spray (Migranal)
Ergot Alkaloid, acts at 5-HT1 receptor
acute tx of mod-severe migraine
- like Ergotamine, less vasoconstriction
- dirty drug: acts @ catechoamine, serotonin, dopamine receptors
ergotamine contraindications/interactions
Do not use in pts with peripheral vascular disease
Do not use with B- blockers
*potentiate vasoconstriction
Dihydroergotamine tox
GI upset: stim. CRTZ–>N/V
transient bradycardia, leg wkness, vasospasm (less than ergotamine, less vasoconstr, more a-blocking)
sumatriptan tox
CV: MI, arrhythmia, vasospasm if taken with ergot
“triptan symptoms”: chest/throat tighness, diff breathing, panic, parethesia, feeling of heaviness
do not use sumatriptan with..
MAO inhibitor (phenelzine, isocarboxazid) w.in 2 week time span
evaluate ppx therapy
- stay on for 2-3 mos to see if effective
- continue for 3-6 mos then examine for remission
tension ha tx
abortive:
self medicate w. OTC analgesics
relaxation techniques
ppx:
amitriptyline
botulinum toxin inj.
ha tx for kiddos
- Ibuprofen, acetominophen
- don’t use metoclopramide for antiemetic (extrapyramidal SEs), domperidone may be better
- triptans
- B-blockers for ppx
