Inflammation and Prostaglandins Overview
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What is the primary role of COX-1 in the body?

  • Mediating inflammation response
  • Performing house-keeping functions (correct)
  • Producing pro-inflammatory cytokines
  • Inducing vasodilation during injury

    • Which prostaglandin is primarily associated with stimulating uterine contractions?

  • TXA2
  • PGI2
  • PGE2
  • PGF2α (correct)

    • What is the effect of PGE2 on gastric acid secretion?

  • It inhibits gastric acid secretion (correct)
  • It has no effect on gastric acid secretion
  • It stimulates gastric acid secretion
  • It promotes the secretion of bile acids

    • Which statement accurately describes the role of prostaglandins in pain sensation?

    <p>They sensitize nociceptors to stimuli</p> Signup and view all the answers

    What is a primary action of TXA2 in the body?

    <p>Induction of platelet aggregation</p> Signup and view all the answers

    Which COX isoform is primarily induced by cytokines during inflammation?

    <p>COX-2</p> Signup and view all the answers

    How do NSAIDs primarily achieve their pain-relieving effects?

    <p>By inhibiting cyclooxygenases</p> Signup and view all the answers

    What is a key function of PGI2 in the vascular system?

    <p>Inhibits platelet aggregation</p> Signup and view all the answers

    Which histamine receptor is primarily responsible for causing bronchoconstriction?

    <p>H1</p> Signup and view all the answers

    What is the primary action of epinephrine in the treatment of anaphylactic shock?

    <p>Act as a physiologic antagonist of histamine mediators</p> Signup and view all the answers

    Which of the following statements about first-generation H1 antihistamines is correct?

    <p>They penetrate the blood-brain barrier and often cause sedation.</p> Signup and view all the answers

    Which therapeutic effect is associated with mast cell stabilizers like Cromolyn and Nedocromil?

    <p>Decreased release of histamine from mast cells</p> Signup and view all the answers

    What is a common side effect associated with H2 blockers such as cimetidine?

    <p>Headache and potential gynecomastia</p> Signup and view all the answers

    What is the therapeutic dose of aspirin for cardiovascular protection?

    <p>81 mg</p> Signup and view all the answers

    Which adverse effect is most commonly associated with the gastrointestinal system when using aspirin?

    <p>Epigastric distress</p> Signup and view all the answers

    What happens to thromboxane A2 (TXA2) when low doses of aspirin are administered?

    <p>It is permanently inhibited</p> Signup and view all the answers

    In which instance is aspirin contraindicated due to its effects on the kidneys?

    <p>In patients with a glomerular filtration rate &lt; 30</p> Signup and view all the answers

    What is the mechanism by which IL-1 released from macrophages affects thermoregulation?

    <p>It induces COX-2 leading to increased prostaglandin E production</p> Signup and view all the answers

    Which of the following is a significant potential effect of excessive aspirin intake?

    <p>Vasomotor collapse</p> Signup and view all the answers

    What distinguishes ibuprofen from aspirin in terms of its action on COX enzymes?

    <p>Ibuprofen is a reversible inhibitor, while aspirin irreversibly inhibits COX</p> Signup and view all the answers

    Which condition is most closely related to the risk of Reye syndrome in children?

    <p>Viral infection</p> Signup and view all the answers

    What effect does aspirin have on bleeding time?

    <p>Increases bleeding time</p> Signup and view all the answers

    What is the main consequence of the inhibition of PGE2 and PGI2 by aspirin?

    <p>Increase in renal blood pressure</p> Signup and view all the answers

    What condition makes diclofenac potassium the preferred choice over diclofenac sodium?

    <p>Cardiovascular diseases</p> Signup and view all the answers

    What is a common side effect of ketorolac?

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

    What is the primary reason for combining diclofenac with misoprostol?

    <p>Prevent gastrointestinal ulceration</p> Signup and view all the answers

    Which of the following is NOT a clinical use for glucocorticoids?

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

    What is an important characteristic of celecoxib (Celebrex)?

    <p>Does not cause gastric upset</p> Signup and view all the answers

    Indometacin is primarily used to manage which condition in premature infants?

    <p>Patent ductus arteriosus</p> Signup and view all the answers

    What potential side effect is associated with long-term use of glucocorticoids?

    <p>Delayed wound healing</p> Signup and view all the answers

    What is sulindac primarily used to treat?

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

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

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

    What is the effect of histamine in the body?

    <p>Mediating inflammatory reactions</p> Signup and view all the answers

    What is the half-life of Ibuprofen after oral ingestion?

    <p>1-2 hours</p> Signup and view all the answers

    Which of the following is a common adverse effect of Ibuprofen?

    <p>Fluid retention</p> Signup and view all the answers

    In which condition is Ibuprofen contraindicated?

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

    Which clinical use is NOT associated with Ibuprofen?

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

    What can occur with the concomitant administration of Ibuprofen and Aspirin?

    <p>Antagonism of aspirin's cardioprotective effect</p> Signup and view all the answers

    What type of formulation is NOT indicated for Ibuprofen?

    <p>Intramuscular injection</p> Signup and view all the answers

    Which of the following NSAIDs is noted for being stronger and used once a day?

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

    Which adverse effect is less frequent with Ibuprofen compared to Aspirin?

    <p>Gastric upset</p> Signup and view all the answers

    For which condition is Diclofenac considered more potent compared to Indomethacin and Naproxen?

    <p>Anti-inflammatory action</p> Signup and view all the answers

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

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

    Study Notes

    Inflammation

    • Inflammation is a complex protective response to injury from damaging agents.
    • The goal is to inactivate or remove damaging agents and promote healing.

    COX-1

    • A constitutive isoform present in tissues.

    COX-2

    • Induced by cytokines as part of an inflammatory response.
    • Produces prostaglandins involved in various processes:
      • Vasodilation and bronchodilation.
      • Inhibition of gastric acid secretion.
      • Stimulation of gastric mucus secretion.
      • Sensitization of pain receptors to chemical and mechanical stimuli.
      • Promotion of anterior pituitary hormone release.

    Prostaglandins (PGs)

    • Not initiators of pain, rather mediators.
    • Sensitize nociceptors, which are the actual pain signal to the brain.
    • Reducing sensitization inhibits pain signals.

    Thromboxane A2 (TXA2)

    • Produced by platelets and induces platelet aggregation and vasoconstriction.

    Prostacyclin (PGI2)

    • Produced by blood vessel walls and inhibits platelet aggregation and causes vasodilation.

    NSAIDS Mechanism of Action

    • Inhibit cyclooxygenases (COX).
    • Decreased prostaglandin (PG) production.
    • COX-1 is involved in maintaining normal function.
    • COX-2 is induced by factors like TNF-α and IL-1.
    • NSAIDs have antipyretic effects (i.e., reduce fever).

    Aspirin (ASA)

    • Therapeutic uses include antipyretic, analgesic and anti-inflammatory properties.
    • Low dose (81 mg/day) lowers risk of MI, stroke, colon cancer.
    • Inhibits TXA2 production, prolonged effect.
    • Prevents thrombus formation.
    • Adverse effects include GI distress, nausea, vomits, bleeding, prolongation of bleeding time.

    Prostaglandin Derivatives

    • Ibuprofen and other propionic acid derivatives have similar mechanisms to aspirin.
    • Analgesic, anti-inflammatory, and antipyretic actions.
    • Not as likely to cause GI distress as aspirin.

    Heteroaryl Acetic Acids

    • Diclofenac is a more potent anti-inflammatory agent.
    • Used for various inflammatory and musculoskeletal conditions.
    • Potential side effects include gastric distress, fluid retention, ocular disturbances and hematologic effects.
    • Ketorolac is used for short-term pain management.

    Acetic Acid Derivatives

    • Indomethacin is a derivative of acetic acid.
    • Used for chronic musculoskeletal pain, and some other inflammatory conditions.
    • May be useful for ophthalmological procedures.
    • Potential side effects include gastric irritation, renal issues and others.

    COX-2 Selective NSAID: Celecoxib (Celebrex)

    • Selective COX-2 inhibitor.
    • Well absorbed orally and metabolized in the liver.
    • Excreted in feces and urine.
    • Lower incidence of gastric upset and no effect on platelet aggregation.
    • High incidence of cardiovascular thrombotic events, possibly with some others (like rofecoxib).
    • Not recommended for patients with severe renal insufficiency.

    SAIDs (Steroidal Anti-Inflammatory Drugs)

    • These include glucocorticoids, such as hydrocortisone, cortisone, prednisone, and others.

    Histamine and Other Autacoids

    • These molecules are involved in many bodily responses, including inflammation, allergic reactions, and others.
    • Histamine has many receptor types(H1-H4), which lead to various responses.
    • H1 blockers have many uses, including mild to moderate bronchial asthma, allergic rhinitis, atopic diseases of the eye and giant papillary conjunctivitis.

    H2 Blockers

    • Famotidine, cimetidine and others are H2 receptor antagonists, useful for treating gastritis, GERD, gastric and duodenal ulcers.
    • These medications decrease gastric acid production and thus, can benefit patients with conditions that can be linked to gastric discomfort or high stomach acid.

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    Anti-Inflammatory Agents PDF

    Description

    This quiz covers the key aspects of inflammation, including the roles of COX-1, COX-2, and various prostaglandins like TXA2 and PGI2. Understand how these components interact in the body to mediate responses and promote healing. Test your knowledge on the physiological mechanisms behind inflammation and pain sensation.

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