Pharmacology of NSAIDs and COX Inhibitors
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Questions and Answers

Which of the following is a selective COX-2 inhibitor?

  • Naproxen
  • Celecoxib (correct)
  • Ibuprofen
  • Aspirin

    • What is the role of acetyl transferase in the synthesis of PAF?

  • Releases AA and lysoPAF from membrane
  • Acetylates lysoPAF to form PAF (correct)
  • Converts PAF to lysoPAF
  • Inhibits the activity of phospholipase A2

    • What is the effect of PAF on platelets?

  • Releases eicosanoids from platelets
  • Has no effect on platelet aggregation
  • Increases platelet aggregation (correct)
  • Inhibits platelet aggregation

    • What is the source of renin in the renin-angiotensin system?

    <p>Kidney</p> Signup and view all the answers

    What is the function of angiotensin-converting enzyme (ACE) in the renin-angiotensin system?

    <p>Converts angiotensin I to angiotensin II</p> Signup and view all the answers

    What is the effect of angiotensin II on blood pressure?

    <p>Increases blood pressure</p> Signup and view all the answers

    Which of the following is NOT a pharmacological action of PAF?

    <p>Inhibits the release of eicosanoids</p> Signup and view all the answers

    What is the effect of PAF on renal flow?

    <p>Decreases renal flow</p> Signup and view all the answers

    What is the function of angiotensin-converting enzyme (ACE) in the renin-angiotensin system?

    <p>To convert angiotensin I to angiotensin II</p> Signup and view all the answers

    Which of the following enzymes can independently catalyze the conversion of angiotensinogen to angiotensin I?

    <p>Cathepsin D</p> Signup and view all the answers

    What is the effect of angiotensin II on blood pressure?

    <p>It increases blood pressure</p> Signup and view all the answers

    What is the primary function of bradykinin?

    <p>To regulate blood pressure by vasodilation</p> Signup and view all the answers

    Which of the following medications blocks the angiotensin II receptor 1 (AT1R1)?

    <p>Losartan</p> Signup and view all the answers

    What is the precursor to angiotensin I in the renin-angiotensin system?

    <p>Angiotensinogen</p> Signup and view all the answers

    What is the effect of angiotensin II on the kidneys?

    <p>It increases sodium reabsorption in kidney tubules</p> Signup and view all the answers

    What is the role of kallikrein in the synthesis of bradykinin?

    <p>It converts prekallikrein to kallikrein</p> Signup and view all the answers

    Which of the following peptides is a potent vasoconstrictor?

    <p>Endothelin</p> Signup and view all the answers

    What is the effect of ETA receptors on blood pressure?

    <p>Prolonged increase in blood pressure</p> Signup and view all the answers

    Which of the following is a nonselective endothelin receptor antagonist?

    <p>Bosentan</p> Signup and view all the answers

    Which of the following kinins is a nonapeptide?

    <p>Bradykinin</p> Signup and view all the answers

    Which of the following receptors mediates vasodilatation?

    <p>B2</p> Signup and view all the answers

    Which of the following cytokines participates in the pathogenesis of rheumatoid arthritis?

    <p>IL-1</p> Signup and view all the answers

    Which of the following vasodilators acts together with ACh?

    <p>VIP</p> Signup and view all the answers

    What is the indication for blockers of ET-1 receptors?

    <p>Pulmonary arterial hypertension</p> Signup and view all the answers

    Study Notes

    COX Inhibitors

    • Nonselective COX inhibitors: aspirin-like, inhibit both COX-1 and COX-2
    • Selective COX-2 inhibitors: coxibs, preferential COX-2 inhibitors
    • Antipyretic and analgesic effects

    Platelet Activating Factor (PAF)

    • Released from membrane phospholipids by phospholipase A2
    • Synthesized by platelets, monocytes, mast cells, eosinophils, renal medullary cells, and endothelium
    • Pharmacological actions:
      • Increases platelet aggregation
      • Potent vasodilator, decreases blood pressure
      • Constricts pulmonary vessels
      • Increases microvascular permeability
      • Releases eicosanoids, generates superoxides
      • Contracts nonvascular smooth muscles, increases respiratory secretions, and forms pulmonary edema
      • Decreases renal flow

    Biogenic Peptides

    Angiotensin

    • Synthesis: angiotensinogen → angiotensin I → angiotensin II
    • Angiotensin II effects:
      • Vasoconstriction
      • Increases peripheral vascular resistance
      • Increases blood pressure
      • Directly stimulates heart
      • Facilitates epinephrine and aldosterone release
      • Increases Na reabsorption in kidney tubules
      • Releases ADH (vasopressin) to restore blood volume
    • Inhibitors: losartan and valsartan (block angiotensin receptors), captopril and enalapril (inhibit ACE)

    Bradykinin

    • Member of the kinin group
    • Actions:
      • Mediates nociception (pain)
      • Regulates blood pressure (vasodilator)
      • Increases capillary permeability
      • Balances electrolytes and fluid
      • Contracts gut slowly and stimulates prostaglandin synthesis
    • Produced by tissue damage, viral infection, allergic reaction, and inflammation
    • Synthesis: prekallikrein → kallikrein → kininogen → bradykinin
    • Receptors:
      • B1: mediates vasoconstriction
      • B2: mediates vasodilation, permeability, smooth muscle contraction, and pain
      • B3: mediates guinea pig tracheal contraction

    Endothelin

    • Potent vasoconstrictor peptides isolated from aortic endothelial cells
    • Receptors:
      • ETA: causes prolonged increases in blood pressure
      • ETB: causes transient drop in blood pressure
    • Endothelin receptor antagonists: bosentan (nonselective), ambriSentan, macitentan (indicated for PAH treatment)

    Vasodilators and Neuropeptides

    • Vasodilators:
      • NPY (with NA)
      • ANP
      • VIP (with ACh)
      • CGRP
      • Kinins (kallikrein, bradykinin)
      • SP
    • Neuropeptides:
      • CCK: involved in pathogenesis of panic reactions

    Cytokines

    • Soluble proteins and glycoproteins that interact with specific cellular receptors
    • Involved in inflammatory and immune response
    • Cytokines act together on: endothelium, leucocytes, mastocytes, fibroblasts, stem cells, and osteoclasts
    • Examples:
      • Interleukins (ILs)
      • IL-1: participates in the pathogenesis of rheumatoid arthritis
      • IL-2: used in renal carcinoma but has ADRs
      • IL-11: stimulates thrombocytopoiesis

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    Description

    This quiz covers the different types of COX inhibitors, including non-selective and selective inhibitors, as well as their effects on the body. Learn about aspirin-like NSAIDs and their role in pain relief and inflammation reduction.

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