PharmExam4- composition/MOA Flashcards
active metabolite Nortriptiline
amtriptiline
most potent, selective inhibitor of NE reuptake
imipramine
most selective for inhibition of serotonin reuptake
clomipramine
unique: NO action on transporters; EXTREMELY strong affinity for histamine
trimipramine
D2 receptor antagonist; mixed antidepressant and neuroleptic
amoxapine
unique- binds NE but HIGHER affinity for dopa
buproprion
antagonist at 5HT2/3 and H1
mirtazepine
block sero and NE?
SNRIs
block 5HT2a and 5HT1a at high doses
trazadone
blocks 5HT2
nefazodone
serotonin reuptake blockade, potent inhibitor of P450
SSRIs
substitute for sodium
lithium
blocks turnover and release of dopa and NE but INCREASED SEROTONIN
lithium
depletes phosphatidylinositol-4,5 biphosphate (PIP2)
lithium
reversibly inhibits nerve conduction .. binds and inhibits opening of sodium channels on INTRACELLULAR side
local anesth.
prototype, competitive antagonist at nicotinic receptor
curarine
prevents depolarization by Ach (hypotension from histamine release)
d-Tubocurarine
laudanosine metabolite, histamine release
atracurium
NO laudanosine, no histamine release, more potent
CISatracurium
non depolarizing steroid that blocks muscarinic receptors (part of triple cocktail lethal injxn)
pancuronium
non depolarizing steroid that has slight antimusc effects, for ppl w/ CV probs
rocuronium
nicotinic agonist- fasiculations followed by desensitized
succinylcholine
alpha 2 agonist, spasmolytic
tizanidine
blocks ryanodine receptor in Ca release channels
dantrolene
blocks Ach in NMJ
botox
NET & SERT inhibitor, NMDA antagonist
methadone
quick onset, short DOA, faster than morphine but slower than heroine, many options?
fentanyl (i.e. transmucosal for cancer pain)
anticholinergic so NO BRADY or CONSTIPATION
meperidine
prodrug that undergoes demethylation to become activated
codeine
weak inhibitor of NET and SERT reuptake and u agonist
tramadol
kappa agonist, mu antagonist
nalbuphine
MU partial agonist, kappa antagonist
buprenorphine
at higher doses also zero order kinetics
aspirin
reduces prostaglandin formation, does NOT affect leukotrienes
aspirin
TNF alpha and NO synthesis inhibitor
flubiprofen
inhibits cyclooxygenase AND lipoxygenase activity
ketoprofen
extremely potent- ONLY to reach a narcotic analgesic level
ketoprofen
not good at inhibiting inflammation, mostly parenteral, almost as good as morphine
ketorolac
only NON ACID NSAID, ketone prodrug
nabumetone
pyrroleacetic acid
tolmetin
binds to 5HT1B and 1D- agonists; cause vasoconstriction
triptans
5HT1B and D agonists; antidote is nitroprusside
ergot alkaloids
NONpurine xanthine oxidase inhibitor
febuxostat
inhibits organic anion transporter so that you can’t reabsorb uric acid
probenecid
inhibits nociceptor transmission in dorsal horn
tizanidine