Cyclooxygenase Enzyme and Inflammation
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Questions and Answers

What is the primary function of COX-1 in the stomach?

  • Producing TXA2 to induce platelet aggregation
  • Producing PGH2 to stimulate inflammation
  • Producing PGE2 to provide a protective effect (correct)
  • Producing PGI2 to prevent platelet aggregation

Which of the following NSAIDs is known to cause irreversible covalent modification?

  • Celecoxib
  • Ibuprofen
  • Flurbiprofen
  • Aspirin (correct)

What is the primary mechanism of action of Paracetamol?

  • Unknown, but it may involve multiple mechanisms (correct)
  • Inhibition of COX-3 in the CNS
  • Decrease in nitric oxide synthesis in the spinal cord
  • Inhibition of COX-1 and COX-2

What is the main difference between COX-1 and COX-2 in terms of their structure?

<p>COX-1 has a smaller hydrophobic channel (D)</p> Signup and view all the answers

Which of the following is a potential side effect of NSAIDs?

<p>Increased risk of cardiovascular disease (C)</p> Signup and view all the answers

What is the main difference between COX-1 and COX-2 in terms of their expression?

<p>COX-1 is constitutive, while COX-2 is inducible (C)</p> Signup and view all the answers

What is the primary function of the lipid mediators mentioned in the text?

<p>To resolve inflammation (C)</p> Signup and view all the answers

What is the target of NSAIDs according to the text?

<p>Cyclooxygenase (C)</p> Signup and view all the answers

COX-1 is primarily found in the CNS and produces PGI2 to prevent platelet aggregation.

<p>False (B)</p> Signup and view all the answers

All NSAIDs are selective for COX-2.

<p>False (B)</p> Signup and view all the answers

Paracetamol is an NSAID.

<p>False (B)</p> Signup and view all the answers

COX-2 is constitutively expressed and found in endothelial cells.

<p>False (B)</p> Signup and view all the answers

GI bleeding is a possible side effect of NSAIDs.

<p>True (A)</p> Signup and view all the answers

Rofecoxib is a non-selective NSAID.

<p>False (B)</p> Signup and view all the answers

Cyclooxygenase is a pro-resolution lipid mediator.

<p>False (B)</p> Signup and view all the answers

NSAIDs are selective inhibitors of COX-2.

<p>False (B)</p> Signup and view all the answers

Study Notes

Cyclooxygenase Enzyme

  • Produces PGG2 and PGH2
  • Has two subtypes: COX-1 and COX-2

COX-1 Subtype

  • Constitutive and widespread
  • Produces PGE2 in the stomach, which is protective
  • Found in platelets, where it produces TXA2 for aggregation
  • Has a small hydrophobic channel, which can be inhibited by small molecules

COX-2 Subtype

  • Inducible, with synthesis increased by cytokines
  • Produces high levels of PGs in areas of inflammation
  • Found in endothelial cells, where it produces PGI2 to prevent aggregation, and in the CNS
  • Has a larger channel, which can be inhibited by drugs with bulky side groups that cannot enter COX-1

NSAIDS (Non-steroidal Anti-inflammatory Drugs)

  • Non-selective (COX-1 and COX-2) inhibitors:
    • Aspirin (irreversible covalent modification)
    • Ibuprofen (reversible)
    • Ketorolac
    • Flurbiprofen
  • COX-2 selective (generally reversible) inhibitors:
    • Celecoxib
    • Rofecoxib
  • Side effects: GI bleeding, possible increased cardiovascular risk

Paracetamol

  • Not an anti-inflammatory drug
  • Several proposed mechanisms of action, including:
    • COX-3 in CNS
    • Decrease nitrox oxide synthesis in spinal cord
    • Metabolite NAPQI inhibiting neurotransmission
  • Antipyretic analgesic, extremely safe and well-tolerated
  • Given for a wide range of conditions
  • Liver toxicity a concern

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Description

Learn about the cyclooxygenase enzyme, its subtypes COX-1 and COX-2, and their roles in inflammation and platelet aggregation. Understand how they produce prostaglandins and thromboxane, and how they can be inhibited by small molecules. This quiz covers the basics of cyclooxygenase as a drug target.

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