Unit II Flashcards
Subclasses of tNSAIDs (5)
- salicylates
- pyrazalone derivatives
- acetic/carboxylic acids
- oxicam derivatives
- propionic acid derivatives
3 acetic/carboxylic acid drugs
- indomethacin (Indocin)
- ketorolac (toradol)
- nabumetone (Relafen)
Oxicam drug
meloxicam (Mobic)
3 propionic acid drugs
- ibuprofen (advil, motrin)
- naproxen (Aleve, Naprosyn)
- ketoprofen (orudis)
Characteristics of pyrazalone dereivatives
more potent and longer lasting than aspirin but serious toxicities with chronic use
use of indomethacin
generally limited to arthritic conditions that do not respond to safer agents
Treatment of dysmenorrhea
ibuprofen or naproxen via inhibition of synthesis of endometrial prostaglandin
Inhibitoin of COX-1 PGE->
Lowest risk with ___ highest risk with ___
dyspepsia and gastric ulceration
Low- ibuprofen
high- naproxen
Interfere with COX-1 thromboxane A2 synthesis->
promotion of bleeding
INhibition of COX-1 and COX-2 PGE synthesis->
Highest risk with ___ lowest risk with ____
reversible renal insufficiency: fluid retention
HIgh- ibuprofen
Low- naproxen
Celecoxib (Celebrex) is metabolized by
CYP2C9
Acetylsalicylic acid is hydrolyzed by ____ to _____
esterases
salicylate
Reversible changes following cell injury (4)
- Decreased ATP
- Decreased Na pump (cell swelling)
- increased glycolysis, decreased pH
- D protein synthesis
Irreversible changes following cell injury (3)
- activation of lysosomal enzymes
- DNA, protein degradation
- Increase Ca influx
3 injuries following hypoxia
- 02 therapy - high levels of 02 are needed acutely to keep the patient alive. However, high
levels of 02 radicals are also produced and have toxic effects on cells - especially in the lung. - Acute inflammation - PMNs have enzymes such as myeloperoxidase which produce oxygen
radicals. Many hypoxic tissues are infiltrated with PMNs. - Reperfusion - In hypoxia, xanthine dehydrogenase is proteolytically converted to xanthine
oxidase. Once the hypoxia is corrected, the xanthine oxidase produces activated oxygen species.
2 •OH + 2 GSH->
2 H20 + GSSG
Endogenous pyrogens
IL-1 and TNF
Fibrinogen
Binds red blood cells causing them to form stacks that form sediments
Along with being endogenous pyrogens, what are other roles of TNF and IL-1
- Release leukocytes from the marrow
2. Stimulate E selectin
LTC4, LTD4, LTE4 cause
vascular permeability
growth factor secretion
macrophage
neovascularization
endothelial cell
collagen deposition
fibroblast/myofibroblast
collagen remodeling/retraction
fibroblast
re-epithelialization
epithelial cells/ hepatocytes
Granulation tissue composed of (4
fibroblasts
new capillaries
loose ECM
inflammatory cells (macrophages)
Initial scar
Collagen type III
sacr remodeling
Collagen type I
Prototypic hormone of GCs
cortisol
Prototypic hormone of MCs
aldosterone