NSAIDs Flashcards
Prostacyclins action
Vasodilation and inhibit platelet aggregation
Thromboxane action
Vasoconstriction and promotes platelet aggregation
Prostaglandins action
Vasodilation and increased vascular permeability
Lipoxins action
Inhibit neutrophil adhesion and chemotaxis
Leukotriene B4 and 5-HPETE action
Chemotaxis
Leukotrienes action
Vasoconstriction
Bronchospasm
Increased Vascular Permeability
Zileuton:
Inhibits 5-lipoxygenase
Zafirlukast and Montelukast:
Inhibit CysLT1 receptors for Leukotrienes
Aspirin Dose:
Anti-platelet: 81 mg/day or 325 mg every other day
Anti-pyresis/Analgesia: 325-650 mg every 4-6 hrs
Anti-Inflammatory: 3.2-6 grams/day in divided doses
Cox-2 Selective NSAID:
Celecoxib
Indomethacin:
- Anti-inflammatory
- Close patent ductus arteriosus
Ibuprofen:
- Anti-pyresis and Analgesic
- Lower incidence of GI distress but not ulcers
- 2400 mg/day max dose
Naproxen:
-Same as ibuprofen just longer half life
Ketorlac:
- Pure COX-1 inhibitor
- MAJOR RISK FOR GASTRIC INJURY
COX-1 Mainly Produces:
Thromboxane
COX-2 Mainly Produces:
Prostacyclin
Celecoxib:
- Pure COX-2 inhibitor
- Used for chronic OA
Acetaminophen:
- Weak COX-1 and COX-2
- Strong COX-3
- Anti-pyretic
- Not good analgesic
- No anti-inflammatory effects
- Preferred Anti-pyresis and analgesic in kids
Acetaminophen Dose:
- NO MORE THAN 4 Grams a Day
- Fever and Analgesic 325-650 mg/day
Anti-cancer drugs used as immunosuppressants:
- Methotrexate
- Cyclophosphamide
- Azathioprine
Methotrexate:
- Inhibits dihydrofolate reductase
- Decreasing THF and therefore purine/DNA
- DECREASES LYMPHOCYTE PROLIFERATION
- Promotes adenosine release -> suppresses inflammation
- Inhibits AICAR transformylase -> increase level of adenine intracellularly
Azathioprine:
- Prodrug converted to 6-MP
- Interrupts DNA and RNA
- SUPPRESSION of T and B cell Proliferation
Cyclosporine:
- Reduces T-cell responsiveness
- Inhibit cytokine formation
- IMMUNE SUPPRESSION MAJOR SE
Mycophenolate:
- Inhibits inosine monophosphate dehydrogenase needed for guanosine synthesis
- Anti T and B cell proliferation only