Pharm Flashcards
What do NSAIDs stand for?
Non-steroidal Anti-Inflammatory Drugs
What is the mechanism of action for NSAIDs?
Block cyclooxygenase and prevents the formation of prostaglandins and thromboxane from arachidonic acid.
The eicosanoids include…
Prostaglandins, leukotrienes, and thromboxanes.
Pg and LTs are made from arachidonic acids. What is the rate limiting step? What enzyme is responsible for this?
The rate limiting step is the conversion from phospholipids to arachidonic acid. Phospholipase A2 is the enzyme needed. Synthesized upon demand not stored.
What blocks arachidonic acid formation?
Corticosteroids. They increase lipocortin which inhibits phospholipase A2 (PLA2).
What is the role of cyclooxygenase?
Cox enzymes catalyzes the first two steps in conversion of arachidonic acid to PGs or TXs.
These inhibit cyclooxygenase.
NSAIDs.
What does COX 1 do?
- found in most cells of the body, expressed constituitively.
- protects the stomach
- TXA2 synthesis by platelets
What are the functions of COX2?
- Protects the kidney and cardiac circulation.
- source of PGI2.
- released from blood vessel endothelial cells.
- prevents platelet aggregation.
What cells produce COX 2?
Cox2 is induced in monocytes, fibroblasts, etc during inflammation.
What is the role of 5-Lipooxygenase?
Produced by WBCs metabolizes arachidonic acid to HPETEs –> HETEs –> LTs.
Where is 5LP found?
Mainly in neutrophils, eosinophils, monocytes, macrophages, and mast cells.
Name some functions of LTs.
Increase blood vessel permeability, allows plasma fluid to pass into the extravascular space and causes swelling.
These are potent bronchi constrictors that mediate asthma and anaphylaxis.
LTC4 and LTD4.
This is a potent neutrophil attractor.
LTB4.
