Pharm 3 Nsaids

Front 1

NSAIDS

Front 3

what does cyclooxygenase produce, and from what?

Back 3

arachadonic acid --> PGH2 (which can be converted to other prostaglandins)

Front 4

what does arachadonic acid come from?

Back 4

clel membrane phospholipids

Front 5

what do prostaglandins made by COX do in the stomach (2)?

Back 5

1) decrease cAMP and decrease K/H ATPase in parietal cells; 2) stimulate secretion of mucous HCO3- from epithelial cells

Front 6

what therapy relates to thromboxane A2 and how does it work?

Back 6

aspirin blocks thromboxane A2 and prevents platelet aggregation

Front 7

will nonspecific COX inhibitors be effective in treating asthma, and why?

Back 7

no, because PGF and PGD constrict / PGEs relax bronchial/tracheal muscles

Front 8

what do PGs do to the CV system?

Back 8

increase cardiac output, vasodilate (hypotensive)), PGD2 vasoconstricts

Front 9

what type of pain are salicylates (aspirin, salicylic acid, methyl salicylate) good for?

Back 9

integument, not visceral

Front 10

what are salicylates contraindicated in (4)?

Back 10

1) hemophilia; 2) vit K deficiency; 3) hepatic damage; 4) hypoprothrombinemia (congenital or acquired disorder where factor II (prothrombin) is deficient - this can result from vitamin K deficiency

Front 11

what are the metabolic effects of salicylate?

Back 11

hyperglycemia, glycosuria, increase O2 consumption, CO2 production, and metabolic rate, reduce serum triglycerides, increase fat burning, decrease lipogenesis

Front 12

what are endocrine effects of salicylates (2)?

Back 12

increae glucocorticoid secretion, decrease thyroid function

Front 13

what are the effects of salicylates on pregnancy?

Back 13

decrease birth weight, increase perinatal mortality, anema, and postpartum hemorrhage

Front 14

what cancer is aspirin helpful with?

Back 14

colorectal

Front 15

what are additional contraindications of aspirin?

Back 15

1) viral infections like flu, chickenpox (Reye's syndrome); 2) peptic ulcers

Front 16

what effects do very low (1mg/kg), low (10mg/kg); and high (100mg/kg) doses of aspirin have?

Back 16

very low - antiplatelet; low - analgesic/antipyretic; high - anti-inflammatory

Front 17

what are three AEs of aspirin?

Back 17

tinnitus, vertigo, deafness

Front 18

what happens in aspirin overdose (2) and what results from each?

Back 18

1) hyperventilation --> respiratory alkalosis; 2) salicylate --> fever, dehydration, and metabolic acidosis

Front 19

how does aspirin overdose culminate?

Back 19

shock, coma, organ system failure, death

Front 20

what is the treatment for aspirin overdose?

Back 20

1) induce vomiting/lavage; 2) give fluids and electrolytes to support renal function; 3) administer sodium bicarbonate to counter metabolic acidosis and increase urinary clearance

Front 21

why is acetaminophen not an NSAID?

Back 21

no antiinflammatory activity

Front 22

what does it do, and when is it used?

Back 22

functions only centrally - antipyretic / analgesic (no alteration on bleeding time, uric acid, acid/base)

Front 23

what can acetaminophen OD cause?

Back 23

fatal hepatic necrosis

Front 24

what NSAID is useful for gout, and what class is it a part of?

Back 24

indomethacin - an acetic acid

Front 25

what is another acetic acid with limited toxicity and selectivity for COX2?

Back 25

etodolac

Front 26

what are fenamates and why are they not used much?

Back 26

no advantage in anti-inflammatory activity, but cause diarrhea - mefanamic acid, meclofenamic acid

Front 27

what NSAID was said to have little difference in therapeutic efficacy compared to aspirin, but is better tolerated?

Back 27

tolmetin

Front 28

what drug is an effective analgesic, but a poor anti-inflammatory, that can be administered many ways (IM, IV, oral, and also topically for conjunctivitis) and is limited to short term use?

Back 28

ketorolac

Front 29

what NSAID is approved for long term treatment of RA, osteoarthritis, and ankylosing spondylitis?

Back 29

diclofenac

Front 30

what class of drugs are all anti-inflammatory, analgesic, and antipyretic, and are better tolerated than aspirin and indomethacin?

Back 30

propionic acids (ibuprofen, naproxen, fenoprofen, ketoprofin, flurbiprofen)

Front 31

in what case is ibuprofen used, and what is it effective for?

Back 31

in patients with history of GI intolerance to other NSAIDs - effective analgesic and anti-inflammatory

Front 32

what what type of toxicity does naproxen have, similar frequency to indomethacin?

Back 32

GI, CNS (but naproxen better tolerated, generally)

Front 33

what drug is an effective antiinflammatory agent, but poorly inhibits COX in seminal vesicles, where COX1 is the only type?

Back 33

nimesulide

Front 34

what problem occurs with vioxx?

Back 34

HA, stroke

Front 35

what additional program (besides HA, stroke, DVT) occurs with bextra?

Back 35

severe skin reactions

Front 36

what NSAID suppresed breast tumors in human breast cancer cells, and why?

Back 36

piroxicam, since human cancer cells expres high levels of COX-2

Front 37

what drugs reduce the size/number of colorectal polyps in animal models?

Back 37

aspirin, COX-2 inhibitors

Front 38

what is the MOA of aspirin?

Back 38

suicide inhibitor of COX-1 (thromboxane A2)

Front 39

what drug closes the ductus arteriosus in premature neonates?

Back 39

indomethacin

Front 40

what drug is a first generation selective COX 2 inhibitor that is used for RA and osteoarthritis?

Back 40

celecoxib (celebrex)

Front 41

what things was it said ibuprofen is useful for (3)?

Back 41

1) RA; 2) dysmenorrhea; 3) gout; 4) ankylosing spnodylitis

Front 42

what toxicity does it have, and how well tolerated is it?

Back 42

gastrix toxicity, but is tolerated as well as any nonselective COX inhibitor

Front 43

what is achieved at lower doses with ibuprofen - inflammatory or analgesic effects?

Back 43

analgesic effects achieved at lower doses

Front 44

what is an early COX inhibitor used for rheumatoid and osteoarthritis?

Back 44

indomethacin

Front 45

what is a second generation COX inhibitor that is used for osteo and rheumatoid arthritis, migraine, and fever, with gastric complications and pediatric use?

Back 45

naproxen