NSAIDS

Question 1

aspirin clinical effects

Answer 1

anti-inflammatory (directly in tissue); analgesic (2ndary to anti-inflammatory); antipyretic (only if temp is inc); anti-platelet (slightly inhibit thromboxane)

Question 2

anti-inflammatory effects of aspirin

Answer 2

non-selective COX inhibition - irreversible actylation (unique), salicylate-induced reversible inhibition (like NSAIDs); interference w/kallikrein/bradykinin system (minor) - interfere w/granulocyte adherence, PMN leukos, macrophages

Question 3

analgesic effects of aspirin

Answer 3

mild/moderate pain; site of pain - peripheral; 2ndary to anti-inflammation; minor 2ndary cns effect at subcortical sites; co-medication in moderate/severe pain

Question 4

antipyretic effects of aspirin

Answer 4

dec high temp, normal temp unaffected; regulation at cns level (cox inhibition, IL-1 formation); vasodilation; profuse sweating

Question 5

anti-platelet effects of aspirin

Answer 5

irreversible acetylation of thromboxane synthetase - low dose effect, specific for aspirin, pre-systemic effect on thrombosis in portal vein, 8-10d effect, effects add up, stop after surgery; inhibit thromboxane synthetase by salicylate - high dose effect, mild

Question 6

aspirin combined effect on coagulation

Answer 6

irreversibly inhibits TXA2 for life of platelet -> inc BT; inhibits COX in endothelial cells, but can synth new COX

Question 7

aspirin adverse effects

Answer 7

analgesic, short-term doses - upset GI, slight inc BT; prolonged tx - erosive gastritis, gastric/duodenal ulcers/complications -> MUST have protection; high dose (unusual) - cns syndrome - salicylism (vomiting, tinnitus, vertigo); low dose - inc urate levels -> gout -> inc dose -> dec gout; impaired renal fxn when combo w/2d nsaid; aspirin-asthma; reye syndrome -> NEVER give to kids w/fever/viral infection

Question 8

aspiring intoxication

Answer 8

respiratory alkalosis, then metabolic acidosis, mixed imbalances of acid-base homeostasis

Question 9

aspirin adverse effects on kidneys

Answer 9

dec renal blood flow; acute interstitial nephritis; analgesic nephropathy

Question 10

aspirin adverse effects on kidney: dec renal blood flow

Answer 10

pt’s w/compromised renal perfusion -> kidney synth PGE2, PGI2 (vasodilators) to balance vasoconstriction; aspirin dec PGs -> dec PGE2 -> inc na/h2o & dec PGI2 -> hyperkalemia, acute renal failure

Question 11

aspirin adverse effects on kidneys: acute interstitial nephritis

Answer 11

type I hypersensitivity -> acute renal failure; almost any drug can cause interstitial nephritis, most common -> antibiotics/nsaids

Question 12

aspirin adverse effects on kidneys: analgesic nephropathy

Answer 12

chronic interstitial nephritis from prolonged analgesics use, esp combos of diff agents; renal papillary necrosis after yrs -> chronic interstitial nephritis -> progressive chronic renal failure

Question 13

aspirin clinical uses: antiplatelet dose level

Answer 13

prevent coronary events, transient ischaemic attacks; reduce colon ca incidence

Question 14

aspirin clinical uses: analgesic dose level

Answer 14

tx mild/moderate pain; fever (not kids); moderate pain when combo w/codein; adjunct tx of severe pain w/strong opioids

Question 15

ibuprofen characteristics

Answer 15

commonly used minor analgesic, otc

Question 16

ibuprofen pk

Answer 16

oral, 99% protein bound

Question 17

ibuprofen pd

Answer 17

nsaid

Question 18

ibuprofen adverse effects

Answer 18

GI (less than aspirin); RARE: rash, pruritius, aseptic meningitis, tinnitus, dizziness, headache, fluid retention, acute renal failure, interstitial nephritis, nephrotic syndrome, hepatitis

Question 19

diclofenac moa

Answer 19

potent COX inhibitor, some selectivity for COX-2

Question 20

diclofenac pk

Answer 20

t1/2~1h; accums in synovial fluid (t1/2~6h); enteric-coate, sustained release available - important for chronic joint pain

Question 21

diclofenac uses

Answer 21

analgesic (in combo w/codeine); antirheumatic

Question 22

diclofenac adverse effects

Answer 22

like other nsaids

Question 23

indomethacin characteristics

Answer 23

the more potent -> more efficacious -> more side effects

Question 24

indomethacin moa

Answer 24

more potent, unselective COX inhibitor; additional anti-inflammatory effects

Question 25

indomethacin pk

Answer 25

t1/2~10h

Question 26

indomethacin adverse effects

Answer 26

severe nsaid-like; abdominal pain, diarrhea, GI bleeding, pancreatitis, hyperkalemia, renal failure, thrombocytopenia, APLASTIC anemia

Question 27

indomethacin uses

Answer 27

ONLY in rheumatic, arthritic complaints

Question 28

piroxicam moa

Answer 28

potent, unselective COX inhibitor; additional anti-inflammatory effects

Question 29

piroxicam pk

Answer 29

t1/2~55h -> once daily dosing, accumulation

Question 30

piroxicam adverse effects

Answer 30

severe nsaid-like; GI (~20%+); pancreatitis; hyperkalemia; renal failure; thrombocytopenia; aplastic anemia

Question 31

piroxicam uses

Answer 31

ONLY for rheumatologists or not at all

Question 32

acetaminophen characteristics

Answer 32

NOT an NSAID; frequently used as minor analgesic

Question 33

acetaminophen pk

Answer 33

oral; t1/2~2h

Question 34

acetaminophen pd

Answer 34

analgesic (like aspirin), antipyretic (like aspirin); NOT anti-inflammatory, NOT anti-platelet

Question 35

acetaminophen adverse effects

Answer 35

mild inc in hepatic enzymes; RARE: hepatic failure, renal failure, dizziness, excitement, disorientation

Question 36

acetaminophen intoxification

Answer 36

fatal hepatic failure, antidote - acetylcysteine

Question 37

risk for NSAID-induced GI bleeding

Answer 37

low: acetaminophen, ibuprofen; intermediate: aspirin, diclofenac; high: piroxicam, indomethacin, ketoprofen

Question 38

COX isoenzymes

Answer 38

COX-1 - constitutive - for homeostasis; COX-2 - induced by growth factors, tumor promoters, cytokines - major source of prostanoids in inflammation, ca