W28-L11: Drugs to treat inflammation Flashcards
How do glucocorticoids work?
Inhibit arachadonic acid release and metabolsim
How do CysLT1 receptor antagonists work?
leukotriene (LTC4 and LTD4 ) antagonists
Why aren’t prostaglandins used as drugs?
Generally too unstable and expensive
What are the actions of NSAIDs?
- Anti-inflammatory
- Analgesic
- Anti-pyretic
Adverse effects of NSAIDs?
- Gastro-intestinal
- Bleeding time
- Renal
- Pulmonary
What are the gastro-protective role of PGE2?
Protects mucosa: Increases mucosa secretion and reduce gastric acid secretion
Effective repair of injured area: promotes blood flow and angiogenesis
What do NSAIDs do to renal flow?
Compromise renal blood flow and may increase blood pressure and cause renal failure
What are the pulmonary side effects of NSAIDs?
Bronchoconstriction possibly due to overproduction of leukotrienes
What is special about aspirin?
Acetylates COX which is vascular protective and aspirin triggered lipoxins (resolve resolution)
Why shouldn’t potent NSAIDs be used in the elderly?
they are more susceptible to side effects like ulcers
Why is Celecoxib COX 2 selective?
selectivity due to binding pocket, hydrophobic pocket size
What are the mechanisms of actions of Glucocorticoids?
Transactivation and transrepression
