Fiszki Anki: NSAIDs Mechanism of Action, Renal Adverse Effects of NSAIDs, NSAIDs - Propionic Acid Derivatives

Pytanie

What is the initial step in the arachidonic acid cascade?

Odpowiedź

The initial step is the activation of phospholipase A2 (PLA2) triggered by the stimulation of IgE receptors. PLA2 then acts on phospholipids in cell membranes.

Pytanie

Which enzymes metabolize arachidonic acid (ARA) into PGG2 and PGH2?

Odpowiedź

Cyclooxygenase-1 (PTGS1) and cyclooxygenase-2 (PTGS2) metabolize ARA to prostaglandin G2 (PGG2) and prostaglandin H2 (PGH2).

Pytanie

What are the primary prostanoids that mediate inflammation?

Odpowiedź

Prostaglandin PGE2 and prostacyclin PGI2 are the primary prostanoids that mediate inflammation. They increase local blood flow, vascular permeability, and leukocyte infiltration.

Pytanie

What role do PGE2 and PGI2 play in pain perception?

Odpowiedź

PGE2 and PGI2 reduce the threshold to stimulation of nociceptors, causing peripheral sensitization. Reversal of this sensitization is a main component of NSAID analgesic activity.

Pytanie

How do prostanoids contribute to hyperalgesia and allodynia?

Odpowiedź

Prostanoids disinhibit the glycinergic pathways, which increases the excitability of spinal dorsal horn neurons, leading to hyperalgesia and allodynia.

Pytanie

What is the mediator causing fever, and how do NSAIDs counteract it?

Odpowiedź

PGE2 is the mediator causing fever. It activates EP3 receptors on thermosensitive neurons in the hypothalamus. NSAIDs suppress this response by inhibiting COX-2-dependent PGE2 synthesis.

Pytanie

How does aspirin's enzymatic inhibition differ from most other NSAIDs?

Odpowiedź

Aspirin is a non-competitive, irreversible inhibitor of COX enzymes because it acetylates the proteins in the arachidonic acid-binding channel. Most other NSAIDs are competitive, noncompetitive, or mixed reversible inhibitors.

Pytanie

Why are COX-2 selective NSAIDs less prone to inducing gastric ulcers?

Odpowiedź

Selective COX-2 inhibitors are less prone to inducing gastric ulcers than equally efficacious doses of isoform nonselective NSAIDs because they primarily inhibit COX-2, preserving COX-1's cytoprotective functions in the gastric mucosa.

Pytanie

How does aspirin provide cardioprotective effects?

Odpowiedź

Aspirin provides cardioprotective effects due to irreversible acetylation of platelet COX-1, which inhibits platelet function and reduces the risk of serious vascular events.

Pytanie

What is the main mechanism by which NSAIDs provide therapeutic effects?

Odpowiedź

The main therapeutic effect of NSAIDs is based on their ability to inhibit prostaglandin production.