3. Headache Tx Flashcards
migraine abortive agent for kids?
acetaminophen and ibuprofen
wt binds B2 kinin receptor?
native bradykinin and kallidin
Triptans:
AE?
Contraindicaitons?
Headache reccurence
Ergot alkaloid w/i 24 hrs, vascular disease, ischmic heart disease, SSRIs
2 Tricyclic antidepressants for headache? side effect?
amitriptyline and nortriptyline
weight gain and tiredness due to antimuscarinic properties
use for ergot alkaloids? MOA? sublingual ergot? nasal spray and injection ergot? 2 Side effects? 4 contraindications?
moderate to severe migraine abortive agent
5-HT1 agonist
ergotamine - sublingual
dihydroergotamine - nasal/injection
AE: nausea/V & vasoconstriciton
CI: prego, vascular disease, ischemic heart disease, Triptans
wt cleaves low molecular weight kininogen?
tissue kallikrein cleaves it to kallidin.
then aminopeptidase cleaves to bradykinin
Ketorolac use? route? hw long to use?
moderate to severe headaches
IV or oral
max of 5 days
most potent vasodilating peptide in trigemnial system?
CGRP (calcitonin gene related peptide)
wt cleaves kinins into active kinin metabolites?
carboxypeptidase N and M (kinase I)
botox use for headaches? hw to administer? MOA?
prophylaxis for migraine
multiple injections in head/neck
Inhibit release of acetylcholine
is B1 or B2 kinin receptor inducable?
B1
4 anticonvulsants used to tx headache? wc is tetragenic?
Valproic acid (tetragenic)
Topiramate
Gabapentin
Levetricatem
anti-migraine effects of triptans at:
vascular level?
neurogenic level?
Central level?
vasoconstriction of cranial blood vessels
reduced trigeminal sensory activation
inhibit neurotransmitter release from trigeminal in brainstem and cervical spine
2 Beta blockers prophylactic for headache?
MOA?
Propanolol Atenolol
MOA not clear - hyperfunctioning sympathetic suspected cause of migraine
2 drugs to tx IIH?
Acetazolamide and Topiramate
longest acting triptan?
frovatriptan
wt binds B1 kinin receptor?
bradykinin and kinin active metabolites
MOA of triptans? use?
5-HT1B/1D agonist. abort migraine pain and induce vasoconstriction
Serotonin effect on: Platelets CV GI CNS
Platelets - promotes platelet aggregation
CV - casoconstriction
GI - inc motility
CNS - regulate sensory perception and nociception
2 enzymes that metabolize serotonin?
urinary metabolite?
MAO then aldehyde dehydrogenase
5-Hydroxyindoeacetic acid (5-HIAA)
3 things released upon stimulaiton of B kinin receptors?
PGs
NO
EDHF
compare AEs of triptans and ergot alkaloids? why?
triptans have less AEs
bc more selective for 5-HT1
wt cleaves high molecular weight kininogen?
plasma kallikrein
enzyme that hydrolyzes bradykinin to inactive products?
Angiotensin I-Converting Enzyme (ACE/Kinase II)
kinin effect on:
inflammation
respiration
CV
inflammation - inc permeability –> promote
respiration - bronchospasms
CV - low BP and vasodilate
role of coagulation pathway in kinin?
factor XIIa converts plasma prekallikrein to plasma kallikrein
3 effects of binding B kinin receptor?
Vasodilation
Na excretion
Pain (acute)
headache abortive drug contraindicated in pregnancy?
ergot alkaloid
fastest onset triptan?
ROA?
metabolism?
Rizatriptan
sublingual
MAO metabolism
prototype triptan? routes of administration?
sumatriptan
SC, oral or nasal spray
migraine abortive agent for pregos?
ibuprofen and acetaminophen except 3rd trimester
4 stages of migraine? times of each?
- prodome - GI effects (1-2 days)
- Aura (20-60 min prior to attack
- Attack (4-72 hrs)
- Postdrome
MOA of ergot alkaloids and triptans?
bind 5-HT1B/D receptor
