Flashcards in EXAM #4: NSAIDs AND GOUT Deck (39):
What types of chronic conditions does inflammation underlie?
What are the four cardinal signs of inflammation?
What are the non-AA and cytokine proinflammatory mediators?
What are the arachnadonic acid proinflammatory mediators?
What cytokine is highly proinflammatory?
What is the primary MOA / target of the NSAIDs?
Inhibition of prostglandin production by inhibiting COX-1 and COX-2
Is acetaminophen an NSAID?
What is the general function of COX-1 and 2?
Conversion of arachnadonic acid to prostaglandins (PGE2 and PGI2)
What is the specific function of COX-1?
- Maintains homeostasis
- Constitutively expressed
What is the important function associated with COX-1 and side effects of NSAIDs?
Synthesis of PG that protect the stomach lining
What is the specific function of COX-2?
- Production of inflammatory molecules
Where in the AA pathway do corticosteroids block?
What is the MOA of aspirin?
Hydrolyzed to salicylic acid, which is a reversible COX inhibitor
Why is there a high potential for drug-drugs interactions with aspirin?
Binds to plasma proteins
What are the dose-dependent effects of ASA at a LOW dose?
What are the dose-dependent effects of ASA at a HIGH dose?
Describe the mechanism of the anti-pyretic effects seen with ASA?
- Blocks PG in the CNS to RESET temp. in thalamus
- Dilation of BV
- Decrease in temperature
How does ASA prolong bleeding time?
COX-1 inhibition prevents thromboxane formation
What are the major side effects associated with ASA?
1) GI Tract upset
2) GI irritation due to a loss of GI protective PGs
3) Platelet inhibition
List the non-selective COX inhibitors.
What is Indomethacin commonly used to treat?
2) Ankylosing spondylitis
What is the major advantage of COX-2 selective inhibitors?
Less side effects
What is the feared complication of COX-2 inhibitors?
Cardiovascular thrombotic events
List the COX-2 selective inhibitors.
What is the MOA of Acetaminophen?
What is the major toxicity associated with Acetaminophen?
What is the therapeutic dose of Acetaminophen?
What dose of Acetaminophen produces liver necrosis?
What dose of Acetaminophen produces liver failure?
What is the MOA of Capsaicin?
- Binds vanilloid receptor
- Releases substance P
- Prolonged use depletes stores of Substance P in the PNS and spinal cord
*This depletion of Substance P is analgesic*
What do you need to remember about prescribing NSAIDs?
No one best NSAID for everyone
What is Gout associated with?
What is the goal of gout therapy?
Control pain and inflammation
What is the primary drug to treat an acute gout attack?
What is the MOA of Colchicine?
Anti-inflammatory effects mediated by inhibiting leukocyte migration and phagocytosis
What are the xanthine oxidase inhibitors?
How is allopurinol used clinically?
To prevent flares i.e. given between gout attacks
What is the MOA of Probenecid and Sulfinpyrazone?
Inhibit tubular absorption of uric acid and increase renal clearance of uric acid