NSAIDs, sedative-hypnotics, alcohols, anti-seizure, anes, anti-parkinsons Flashcards
nonselective irreversible cox1 and 2 inhibitor, reduces plt production of TXA2, stimulator of plt aggregation; duration of use for arterial thrombosis; associated with ___ in children; prevents uric acid _______so (must/ must not) be used in gout
ASA; 8-10 days(plt lifespan); Reye syndrome; excretion; must not
ASA dose effective for reducing platelet aggregation; follows ____ order elimination
<300mg/day; first order
ASA dose effective as anti-inflamm; follows ____ order elimination
2400-4000mg/d; zero order
ASA intermediate dose for
antipyretic and analgesic
ASA toxic dose
150mg/kg (21 ASA 500mg tabs)
ASA lethal dose
30g (60 500mg tabs)
nonselective reversible cox1 and 2 inhibitor, inhibits prostaglandin synthesis; long-term use reduces risk of ___
ibuprofen, diclofenac, mefanamic acid, meloxicam, piroxicam; colon CA
prevents NSAID-induced gastritis
misoprostol
COX 2>COX1
meloxicam, peroxicam
only IV NSAID, used for post-surgical analgesia; purely analgesic, no anti-inflamm; use for ___ hrs only
Ketorolac; 72
nonselective reversible COX inhibitor used for gout and closure of PDA; special SE
indomethacin; hematologic (aplastic anemia, thrombocytopenia)
selective Cox-2 inhibitor; available IV form; risk for MI and stroke
celecoxib; parecoxib; rofecoxib and valdecoxib
selective Cox-3 inhibitor, weak effect on cox1 and 2; MC SE especially with _____ use; antidote
Paracetamol; hepatotoxicity; alcohol; NAC
similar drug of paracetamol which can cause renal papillary necrosis and interstitial nephritis
phenacetin
in Paracetamol toxicity, ____ accumulates due to oxidation by ______; region of liver preferentially involved
NAPQ1 (N-acetyl-p-benzoquinoneimime); CYP2E1; centrilobular region (zone III)
paracetamol toxic dose; lethal dose
150mg/kg; 15g
MOA of MTX; first choice DMARD for tx of ____; rescue agent
inhibits AICAR transformylase and thymidylate synthetase with secondary effects on PMN chemotaxis; RA; leucovorin (folinic acid)
binds to TNF-a; used for Crohn’s disease, TV reactivation, lymphoma; synergistic effect w/ MTX
infliximab, etanercept
forms 6-thioguianine (purine anti-metabolite) which suppresses inosinic acid synthesis, b and t-cell function, Ig production and IL-2 secretion; similar MOA with ____ (chemotx); don’t give with ____
azathioprine; mercaptopurine; allopurinol
DMARD also anti-malarial; SE; safe for pregnant?
chloroquine; ocular toxicity (retinal reposits); safe
forms phosphoramide mustard which cross-links DNA to prevent replication, supresses t-cell and b-cell; metabolite ____ causes_____; rescue agent
cyclophosphamide; acrolein; hemorrhagic cystits; mesna
inhibits IL-1 and IL-2 receptor production, secondarily inhibits macrophage t-cell interaction and t-cell responsiveness; SE
cyclosporine; gingival hyperplasia
inhibits inosine monophosphate dehydrogenase (impt in guanine synthesis), inhibits T-cell proliferation; SE
mycophenolate mofetil; reversible myelosuppression
DMARD which inhibits release of inflamm cytokines; SE
sulfasalazine; hemolytic anemia, methemoglobinemia; reversible infertility in men
microtubule assembly inhibitor, decreases macrophage migration and phagocytosis; used in gout and familial mediterranean fever; SE
colchicine; agranulocytosis, necrosis, ARF
first line for acute gouty attack; MOA
NSAIDS (indomethacin); inhibi`ts urate crsytal phagocytosis
competes with uric acid for reabsorption in the proximal tubules thereby increasing uric acid excretion; similar drug; SE; potentiates other weak acids e.g. (____)
probenecid; sulfinpyrazone; nephrotic syndrome (probenecid), aplastic anemia; penicillin, MTX
these drugs (3) may precipitate acute gout during early phase of drug action; so coadminister with ___ or ___
probenecid, allopurinol, febuxostat; colchicine or indomethacin
irreversible xanthine oxidase inhibitor, lowers production of uric acid; SE; inhibits metab of ___ and ___
allopurinol; peripheral neuritis, aplastic anemia, cataracts (idiosyncratic); mercaptopurine and azathioprine
first line for chronic gout, tumor lysis syndrome
allopurinol
reversible inhibitor of xanthine oxidase
febuxostat
GABA receptor effect of benzodiazepine; barbiturates; which is safer?
inc frequency, duration; benzodiazepine
short acting benzodiazepine; similar drugs; useful for
midazolam, brotizolam, trazolam, etizolam, oxazepam; anes induction
intermediate acting benzodiazepine; similar drugs
lorazepam, alprazolam, clonazepam, estazolam, nitrazepam, temazepam, lormazepam
causes both anterograde and retrograde amnesia hence banned in Phils
lorazepam
site of anterograde amnesia; retrograde
hippocampus; thalamus
abnormal sleep pattern from use of benzodiazepines
decreased REM sleep
long-acting benzodiazepine; similar drugs; used as a date rape drug
diazepam; chlorazepate, chlordiazepoxide, flurazepam, quazepam; flunitrazepam
benzodiazepine with longest half life
chlordiazepoxide
date rape drugs
alcohol, flunitrazepam (aka Rohypnol), gamma-hydroxybutyrate
toxic dose of benzodiazepine, antidote
1000x, flumazenil
ultrashort-acting barbiturate; similar drugs; used for (2)
thiopental, methohexital, thiamylal; anes induction, inc ICP
short/intermediate-acting barbiturates
pento, seco, amo, buta, aprobarbital, talbutal
long-acting barbiturate; useful in ____ syndrome
phenobarbital, mephobarbital, primidone; Gilbert’s syndrome (unconjugated hyperbilirubinemia)
remarkable SE of barbiturates; enzyme deficient
acute intermittent porphyria; hmb synthase
most catastrophic sx of sedative-hypnotic withdrawal
rebound suicide
newer hypnotic acting like a benzodiazepine used for insomnia; effects reversed with
zolpidem, zaleplon, eszopiclone; flumazenil
order of dependence among sedative-hypnotics
barbiturates>benzodiazepines>zolpidem
anxiolytic which partially antagonizes 5-HT1a receptors and possibly D2 receptos used for generalized anxiety d/o
buspirone
this system is responsible for ethanol metab at blood levels higher than 100mg/dl
microsomal ethanol oxidizing system (MEOS)