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Aspirin - 1o MOA
Reversible competitive (-) of COX-1/COX-2 --> (-) PGE syn
Another name for Acetylsalicylic acid?
Aspirin trade name:
Trade name: Azulfidine
Sulfasalazine - MOA:
- "Sulfa..." = hypersensitivity rxn
- (-) COX & LOX
- (-) IL-1 & TNF-a
What is the main benefit of using Sulfasalazine instead of other NSAIDs?
No GI toxicity
- Dose Affect
- Low: Anti-platelet
- Med: Analgesi/Antipyretic
- High: Anti-Inflammatory
Why do you NOT give Aspirin to kids?
Clinical manifestation of Reye Syndrome:
- 1) Respiratory infection
- 2) 4 days later - nausea, vomitting, chg in mental status
- **Liver damage & cerebral edema**
Toxic Dose of Aspirin S/S:
- Uncompensated respiratory/metabolic acidosis
- Decrease RR
What are the Salicylates?
- Aspirin (acetylsalicylic acid)
- Sulfasalazine (Azulfidine)
What are the non-Salicylates?
- Propionic acid derivatives
- Acetic acid derivatives
Propionic acid derivatives:
- (-) COX-1/2
- @ low levels can (-) LOX
- 1o use as analgesic --> can decrease amt of morphine needed
- Weak anti-inflammatory
- High renal toxicity
- GI ulcers
- Alleviated by combined use with Misopristol
- (-) COX-1/2, Phospholipases, Neutrophil migration --> (-) A.A. pathway
- Decrease T/B cell proliferation
- Closure of PDA
- Ankylosing Spondyliti
- use with Probenecid --> Probenecid increases Indomethacin's t1/2
- 3rd Trimester b/c it will prematurely close PDA
- (-) Leukocyte migration
- Decrease production of radicals
- Pts with gastric ulcers
- **Most GI TOXIC**
Celecoxib - MOA:
- Selectively (-) COX-2
- weak anti-platelet
- **BLACK BOX in MI pts**
Acetaminophen - MOA:
- (-) COX-1/2 in CNSAntipyrogenic & Analgesic
- Acetaminophen -p450-> NAPQI -Glutathione-> Excretion
- Toxic dose or w/EtOH:
- Acetaminophen -p450-> NAPQI -glutathione-> increased cyp2EI = liver cell death b/c of increased -SH groups
How do glucocorticoids work?
- MOA - affect gene expression at DNA level
- MOA - Fx as transcription factors --> (-) phospholipases --> (-) COX path --> (-) PGE syn.
Glucocorticoid - Uses:
- Stimulate surfactant syn
What is the Dexamethasone Suppression Test?
Diagnostic test for differential diagnosis of "Non-iatrogenic Cushing's Syndrome"
How does the Dexamethasone Suppression Test work?
- Dexamethasone dosages & affects:
- NORMAL = low dose --> decreases cortisol levels
- Cushing's Dz = high dose --> resets (-) feedback loop decreasing cortisol levels
- Cushing's Syndrome = low/high dose --> NO Chg