Analgesic, Antipyretic, Anti-Inflammatory Drugs

Front 1

2 major pathways that arachidonic acid enters?

Back 1

lipoxygenase
cyclo-oxygenase

Front 2

lipoxygenase produces?

Back 2

leukotrienes (LTB4, LTC4/B4/E4)

Front 3

cyclo-oxygenase produces?

Back 3

prostaglandins
thromboxane
prostacyclin

Front 4

COX1?

Back 4

housekeeping enzyme, present in most cells

Front 5

COX2?

Back 5

only in setting of inflammation

Front 6

NSAIDs major differences from narcotic analgesics?

Back 6

1.lower maximal effect
2.no addiction
3.free of CNS effects

Front 7

mechanism of NSAIDs?

Back 7

inhibition of PG biosynthesis by COX1 and COX2

Front 8

therapeutic uses of NSAIDs?

Back 8

analgesic
antipyretic
anti-inflammatory
primary dysmenorrhea
patent ductus arteriosus
colon cancer

Front 9

side effects of NSAIDs?

Back 9

GI ulceration and intolerance;
blockade of platelet aggregation;
inhibition of uterine motility;
inhibition of PG-mediated renal effects;
hypersensitivity reaction

Front 10

characteristics of hypersensivity reactions to NSAIDs?

Back 10

asthmatic attacks;
urticaria;
angioedema;
cross reactivity to all aspirin-like drugs

Front 11

warning on package insert of NSAIDs?

Back 11

GI toxicity such as bleeding, ulcer, and perforation

Front 12

misoprostol?

Back 12

synthetic PGE1 analog given with NSAIDs to protect GI mucosa;
side effect is diarrhea

Front 13

given with NSAIDs to protect GI mucosa?

Back 13

misoprostol

Front 14

advantage in terms of side effects of selective COX2 inhibitors?

Back 14

no gastric ulceration and intolerance; no inhibition of platelet function

Front 15

aspirin mechanism of action and importance?

Back 15

irreversible acetylation of cyclooxygenase;
platelet effects persist for lifetime of platelet (8-10 days) - surgical considerations

Front 16

early, reversible warning of aspirin toxicity?

Back 16

tinnitus or deafness

Front 17

aspirin intoxication?

Back 17

disturbance of acid-base balance (resp alkalosis followed by metabolic acidosis);
salicylism: headache, dizziness, tinnitus, mental confusion, drowsiness, sweating

Front 18

contraindications for aspirin?

Back 18

ulcer
asthma
gout
influenza (Reye's syndrome)

Front 19

diflunisal?

Back 19

antiinflammatory potency >aspirin;
not given for analgesic or antipyretic;
less auditory side effects

Front 20

mesalamine?

Back 20

salicylate;
used for local effect in IBD

Front 21

acetaminophen?

Back 21

analgesic and antipyretic, weak anti-inflammatory

Front 22

adverse effect of acetaminophen?

Back 22

fatal hepatic necrosis

Front 23

antidote to acetaminophen toxicity?

Back 23

mucomyst (N-acetylcysteine)

Front 24

mucomyst (N-acetylcysteine)?

Back 24

antidote to acetaminophen toxicity

Front 25

justification for giving N-acetylcysteine for acetaminophen toxicity?

Back 25

gives body more cysteine to make more glutathione to process toxic intermediates to a safer metabolite that can be excreted

Front 26

what condition increases risk of acetaminophen toxicity and why?

Back 26

chronic alcoholism;
induction of p450 enzyme that processes acetaminophen to a toxic intermediate

Front 27

therapeutic uses of indomethacin?

Back 27

acute gout and ankylosing spondylitis;
patent ductus arteriosus in premature infants

Front 28

adverse effects of indomethacin?

Back 28

GI: nausea, vomiting, anorexia, abdominal pain;
CNS: severe frontal headache (15-25%), may be associated with dizziness, confusion, depression

Front 29

sulindac?

Back 29

prodrug NSAID;
less ulcerogenic potential, GI irritation, and blood loss are less severe than aspirin

Front 30

therapeutic uses of tolmetin?

Back 30

JRA
not gout

Front 31

diclofenac mechanism?

Back 31

reduce synthesis of both PG and leukotrienes

Front 32

toxic effects of diclofenac?

Back 32

GI
hepatotoxicity

Front 33

1st injectable NSAID?

Back 33

ketorolac

Front 34

ketorolac indications?

Back 34

short-term (<5 days) managment of moderately severe acute pain that requires analgesia at the opioid level, usually in a postoperative setting

Front 35

naproxen advantage over aspirin?

Back 35

less GI irritation but 20x more potent than aspirin

Front 36

ketoprofen mechanism of action?

Back 36

inhibits both cyclooxygenases and lipoxygenase

Front 37

oxaprozin?

Back 37

long half life (40-60 hrs) resulting in increased patient compliance

Front 38

piroxicam mechanism?

Back 38

potent reversible inhibitor of cyclooxygenase

Front 39

piroxican half life and consequence?

Back 39

extended half-life (50-60 hrs) with steady state concentration reached at 7-12 days

Front 40

meloxicam mechanism?

Back 40

preferentially inhibit COX2 over COX1

Front 41

only nonacid NSAID?

Back 41

nabumetone

Front 42

nabumetone?

Back 42

nonacid NSAID;
ketone prodrug;
preferentially inhibits COX2 (at low dose)

Front 43

only COX2 selective inhibitor still on market?

Back 43

celecoxib

Front 44

celecoxib?

Back 44

COX2 selective inhibitor resulting in fewer ulcers and no effect on platelet aggregation or prothrombin time

Front 45

why was rofecoxib (vioxx) removed from the market?

Back 45

cardiovascular event

Front 46

indications for disease modifying antirheumatic drugs?

Back 46

patients who are refractory to therapeutic regimens of NSAIDs

Front 47

associated with fatal infusion reactions?

Back 47

rituximab

Front 48

abatacept mechanism and administration method?

Back 48

inhibit T cell activation;
IV injection

Front 49

rituximab mechanism and administration method?

Back 49

chimeric monoclonal antibody specific to the antigen CD20 B lymphocytes

Front 50

etanercept mechanism and administration method?

Back 50

bind to TNF and block interaction with cell surface TNF receptors;
SC

Front 51

adalimumab mechanism, administration method, and half life?

Back 51

bind to TNF-α and block interaction with p55 and p75 cell surface TNF receptors;
SC;
half life = 10-20 days

Front 52

infliximab mechanism and administration method?

Back 52

binds to soluble and membrane-bound TNF-α and inhibits binding of TNF-α with its receptors;
IV

Front 53

Other disease modifying antirheumatic drugs?

Back 53

methotrexate and other immunosuppressive drugs;
antimalarial drugs (chloroquine, hydroxychloroquine);
sulfaxalazine;
penicillamine;
gold