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, Reye’s
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
Can’t be used as antipyretic or analgesic agent
due to toxicity
Uses: Barter’s 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 Cushing’s Syndrome
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