4. NSAIDS MoA: reversible, competitive inhibition of COX
Irreversible inactivation by Aspirin Most block COX-1 and -2
Celecoxib is COX-2 inhibitor Inhibit synthesis of PGs but NOT
leukotrienes Indomethacin is extremely potent Reduce elevated
temperature due to PGE1 & PGE2 Analgesic and antipyretic
effects do not undergo tolerance Toxicity: Acute renal failure
& Nephrotic syndrome
5. Agents Effect NSAID Block Effect PGE2, PGI2, PGD2 Enhance
early stages of inflammation Anti-inflammatory PGE2, PGI2 Pain
receptors in peripherals Peripheral analgesic effect PGE1, PGE2
Increase body temp set Antipyretic point
6. SALICYCLATES RS: moderate/high doses stimulate; toxic dose
depresses US: high doses cause inhibition of uric acid
reabsorption, decrease GFR hypovolemia acute renal failure; chronic
doses can cause renal lesions Hematopoietic: low/moderate =
decreased platelet aggregation (decrease TXA2, increase PGI2); high
dose = sideropenia (iron deficiency) Uses: general analgesic,
Ulcerative colitis and Crohns disease (mesalamine &
olsalazine), Thromboemolic disease prophylaxis Toxicity: 1%
hypersensitivity, 15% adverse effects (heartburn, nausea, fecal
blood loss, gastric bleeding, tinnitus, deafness, vertigo),
toxicity in pregnancy, Reyes syndrome in children, Analgesic
nephropathy
7. Non-Salicyclate NSAIDS All effects similar to salicyclates
Greatest analgesic agent efficacy: Ketorolac Greatest
anti-inflammatory: Indomethacin, Piroxicam, Diclofenac MoA: COX-1
inhibition: indomethacin, piroxicam COX-2 inhibition: celecoxib,
meloxicam COX-1 and 2 inhibitors: ibuprofen, naproxen,
diclofenac
8. Non-Salicyclate NSAIDS Propionic Acid Derivatives MoA:
reversible competitive inhibition of COX Acetic Acid Derivates MoA:
reversible competitive inhibition of COX and decrease in oxygen
radicals Diclofenac: ankylosing spondylitis, eye inflammation,
chronic tx of Rheumatoid Arthritis Ketorolac: analgesic agent, 60%
excreted by kidneys renal damage Oxicams MoA: piroxicam is potent
reversible COX-1 inhibition; meloxicam for COX-2 Piroxicam has 100%
oral bio and ~50 hr half life
9. Indomethacin Powerful COX-1 inhibitor Also inhibits: PLA2
PMN cell migration T-Cell and B-Cell proliferation Everything else
is same as other NSAIDS Cant be used as antipyretic or analgesic
agent due to toxicity Uses: Barters syndrome, PDA, nephrogenic
diabetes insipidus
10. Analgesic-Antipyretic Drugs Acetaminophen 95%
biotransformed in liver Small amount toxic metabolite formed NAPQI
hepatotoxicity Potent COX inhibitor in CNS; weak in inflamed
tissues
11. Anti-Inflammatory Steroids Glucocorticoids MoA: Alters #,
distribution, function of peripheral macrophages; decreases
leukocytes, macros, cyto, etc Inhibition of PG and LT synthesis
Decrease postcapillary permeability Inhibits effects of complement
system Strong inhibitors of cellular immunity Weak inhibitors of
humoral immunity Diagnostic use: Dexamethasone suppression test
used for differential diagnosis of Cushings Syndrome
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