Inflammation and NSAIDs Overview
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Questions and Answers

What is the primary role of COX-1 in the body?

  • Stimulates the production of pro-inflammatory prostaglandins
  • Regulates platelet aggregation in response to injury
  • Maintains homeostatic functions in tissues (correct)
  • Induced in response to inflammation

How does PGE2 contribute to the inflammatory response?

  • Promotes platelet aggregation
  • Induces bronchoconstriction
  • Decreases vasodilation
  • Inhibits gastric acid secretion (correct)

What is the effect of TXA2 in the body?

  • Inhibits the aggregation of platelets
  • Causes vasodilation and decreased blood pressure
  • Promotes aggregation of platelets (correct)
  • Stimulates contraction of the uterus

Which statement correctly describes prostaglandins in relation to pain?

<p>They act as mediators of pain signals (D)</p> Signup and view all the answers

NSAIDs primarily work by which mechanism?

<p>Inhibiting the production of prostaglandins (B)</p> Signup and view all the answers

What triggers the production of COX-2?

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

What is the effect of PGI2 (prostacyclin) in the cardiovascular system?

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

What is one of the key functions of PGF2α?

<p>Facilitates uterine contraction (C)</p> Signup and view all the answers

What effect does H2 receptor blockade have on gastric acid secretion?

<p>Decreases gastric acid secretion (A)</p> Signup and view all the answers

Which of the following is NOT a therapeutic use of first-generation antihistamines?

<p>Treatment of bronchial asthma (D)</p> Signup and view all the answers

How do mast cell stabilizers function in the treatment of allergic reactions?

<p>They inhibit the release of histamine from mast cells (C)</p> Signup and view all the answers

What is a common side effect of first-generation H1 antihistamines?

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

Which H1 antihistamine is characterized as having minimal CNS side effects and is specific for H1 receptors?

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

What is the half-life of the medication mentioned?

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

Which of the following is NOT a clinical use of ibuprofen?

<p>Antibiotic (D)</p> Signup and view all the answers

Which adverse effect is considered less frequent with ibuprofen compared to aspirin?

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

What is a contraindication for the use of ibuprofen?

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

What is one of the formulations of ibuprofen available for rapid relief?

<p>A liquid gel for postsurgical dental pain (D)</p> Signup and view all the answers

Which statement about ibuprofen’s interaction with aspirin is correct?

<p>It antagonizes the irreversible platelet inhibition of aspirin. (D)</p> Signup and view all the answers

Which of the following is likely to be a common side effect of ibuprofen?

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

Which condition would make ibuprofen use particularly risky?

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

What is one clinical application of heteroaryl acetic acids like diclofenac?

<p>Inflammatory conditions (D)</p> Signup and view all the answers

Which of the following medications is noted for being used once a day due to its strong derivative?

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

What is the primary antipyretic effect of NSAIDs attributed to?

<p>Induction of COX-2 in the brain (A)</p> Signup and view all the answers

At what dosage is aspirin commonly used for its cardiovascular protective effects?

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

Which statement regarding the effects of aspirin on platelets is correct?

<p>TXA2 inhibition lasts for the entire life of the platelet. (B)</p> Signup and view all the answers

What adverse effect is commonly associated with aspirin due to COX-1 inhibition?

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

Which of the following patients should avoid aspirin due to kidney concerns?

<p>Patients with a glomerular filtration rate &lt; 30 (C)</p> Signup and view all the answers

What is Reye syndrome primarily associated with?

<p>Viral infections in children (C)</p> Signup and view all the answers

Which of the following is a characteristic of ibuprofen compared to aspirin?

<p>It is a reversible inhibitor of COX enzymes (C)</p> Signup and view all the answers

What may occur as a result of aspirin toxicity?

<p>Respiratory and metabolic acidosis (D)</p> Signup and view all the answers

Which one of the following is NOT typically caused by aspirin?

<p>Interstitial nephritis (D)</p> Signup and view all the answers

What is a common side effect of low-dose aspirin therapy?

<p>Prolonged bleeding time (B)</p> Signup and view all the answers

Which of the following side effects is associated with diclofenac sodium?

<p>Gastric upset (A), Salt and water retention (D)</p> Signup and view all the answers

What is the primary clinical indication for ketorolac?

<p>Short-term acute pain management (A)</p> Signup and view all the answers

Which of the following patient conditions makes diclofenac potassium the preferred choice?

<p>Cardiovascular disease (D)</p> Signup and view all the answers

What is a known side effect of using celecoxib?

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

Which of the following actions is NOT associated with autacoids?

<p>Production in specific endocrine glands (C)</p> Signup and view all the answers

In which condition is indomethacin specifically used to induce closure?

<p>Patent ductus arteriosus in premature infants (A)</p> Signup and view all the answers

What is the mechanism of action primarily associated with sulindac?

<p>Inhibition of prostaglandin synthesis through COX-1 and COX-2 (B)</p> Signup and view all the answers

What is a common side effect of using heteroaryl acetic acids like ketorolac?

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

Which characteristic is TRUE about COX-2 selective NSAIDs like celecoxib?

<p>They do not interfere with platelet function (A)</p> Signup and view all the answers

What should be avoided when prescribing ketorolac?

<p>Using it for more than five days (D)</p> Signup and view all the answers

Flashcards

Inflammation

A protective response to injury, aiming to remove damaging agents and promote healing.

COX-1

A constitutive enzyme involved in various bodily functions, not just inflammation.

COX-2

An enzyme induced by inflammation, producing inflammatory mediators.

Prostaglandins (PGs)

Molecules that mediate various bodily functions, including pain and inflammation.

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PGE2

A pro-inflammatory prostaglandin causing vasodilation, bronchodilation, and pain sensitization.

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NSAIDs MOA

NSAIDs reduce prostaglandin production by inhibiting cyclooxygenases (COX).

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Nociceptors

Sensory nerve endings that transmit pain signals to the brain.

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Pain sensitization

Increased sensitivity to painful stimuli, mediated by inflammatory molecules like prostaglandins.

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What is the main mechanism of action for NSAIDs?

NSAIDs reduce inflammation and pain by inhibiting the production of prostaglandins. They achieve this by blocking the enzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2).

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Why can aspirin cause stomach upset?

Aspirin irreversibly inhibits COX-1, an enzyme that protects the stomach lining. This can lead to irritation and bleeding in the stomach.

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What is the cardioprotective effect of low-dose aspirin?

Aspirin inhibits the production of thromboxane A2 (TXA2), a platelet-activating agent, thus reducing platelet aggregation and the risk of blood clots.

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Why are NSAIDs contraindicated in patients with kidney disease?

NSAIDs can reduce the production of prostaglandins that maintain renal blood flow. This can lead to vasoconstriction and kidney damage.

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How does ibuprofen differ from aspirin in terms of COX inhibition?

Ibuprofen is a reversible COX inhibitor, meaning its effect is temporary, while aspirin irreversibly inhibits COX enzymes.

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What is Reye Syndrome?

A serious complication of aspirin use in children, particularly after viral infections, characterized by liver dysfunction and brain swelling.

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What are some signs of mild aspirin toxicity?

Mild aspirin toxicity can manifest as nausea, vomiting, hyperventilation, headache, dizziness, and tinnitus.

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What is the role of interleukin-1 (IL-1) in fever?

IL-1, released by macrophages, triggers the production of prostaglandins in the brain, leading to changes in the body's thermostat and fever.

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What are the therapeutic uses of aspirin?

Aspirin has antipyretic, analgesic, and anti-inflammatory effects. It also reduces the risk of heart attacks, strokes, and colon cancer at low doses.

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What is a key difference between ibuprofen and aspirin?

Ibuprofen is a more potent anti-inflammatory drug than aspirin, despite both inhibiting COX enzymes.

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Ibuprofen

A nonsteroidal anti-inflammatory drug (NSAID) used for pain relief, fever reduction, and inflammation. It is rapidly absorbed, has a short half-life, and is highly bound to plasma proteins.

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Ibuprofen's Clinical Uses

Ibuprofen is used to treat various conditions such as pain, fever, inflammation, acute gouty arthritis, and a heart condition called patent ductus arteriosus.

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Ibuprofen's Adverse Effects

Common side effects include upset stomach, fluid retention, and allergic reactions. Rare but serious effects can include blood cell disorders.

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Ibuprofen's Contraindications

Ibuprofen should not be taken by individuals with peptic ulcers, allergies to aspirin, kidney or liver problems, during pregnancy, or by those with hemophilia.

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Ibuprofen's Interaction with Aspirin

Ibuprofen reduces the effectiveness of aspirin in preventing heart disease, because it blocks aspirin's effect on platelets.

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Diclofenac

A nonsteroidal anti-inflammatory drug (NSAID) in the heteroaryl acetic acid group. It is more potent than indomethacin and naproxen, and has stronger anti-inflammatory effects than analgesic or antipyretic effects.

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Diclofenac's Applications

Diclofenac is used to treat various inflammatory conditions, and is often prescribed for pain management.

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General NSAID Characteristics

Most nonsteroidal anti-inflammatory drugs (NSAIDs) are reversible inhibitors of cyclooxygenase (COX), an enzyme involved in inflammation. They are often used for conditions like rheumatoid arthritis and ankylosing spondylitis because they tend to have fewer gastrointestinal side effects than aspirin.

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NSAIDs' Common Side Effects

Dyspepsia (indigestion), gastric bleeding, headache, tinnitus (ringing in the ears), and dizziness are some of the common side effects associated with NSAIDs.

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NSAID Effectiveness & Mechanism

NSAIDs work by inhibiting the production of prostaglandins, which are molecules that mediate inflammation and pain. This mechanism leads to a decrease in pain, fever, and inflammation.

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Diclofenac Sodium

A NSAID common for musculoskeletal pain, but prone to retaining salt and water, potentially increasing blood pressure.

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Diclofenac Potassium

A preferred NSAID choice for patients with cardiovascular diseases, as it's less likely to retain salt and water compared to its sodium counterpart.

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Ketorolac (Toradol/Acular)

A NSAID with strong analgesic effects, but more potent for pain relief than reducing inflammation. Primarily used for short-term acute pain management.

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Indomethacin

A potent NSAID used for chronic musculoskeletal pain, preterm infant heart duct closure, and various inflammatory conditions.

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Sulindac (Clinoril)

A NSAID chemically related to indomethacin, often used for osteoarthritis, rheumatoid arthritis, and gout. It's a prodrug processed by the liver.

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Celecoxib (Celebrex)

A selective COX-2 inhibitor, primarily for osteoarthritis, not a general analgesic. Does not affect platelet function.

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SAIDs (Steroidal Anti-inflammatories)

Powerful drugs with broad anti-inflammatory effects, used for various conditions, including arthritis, asthma, and allergic reactions.

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Autacoids

Local hormones, like histamine and prostaglandins, produced by tissues themselves and acting locally.

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Histamine

An important autacoid involved in allergic reactions, gastric acid secretion, and neurotransmission.

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Histamine Storage

Histamine is stored in mast cells bound to acidic proteins and heparin, released upon triggering an inflammatory response.

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Histamine Release - Tissue Injury

Any physical (mechanical) or chemical damage to tissue, skin, or mucous membranes triggers the immediate release of histamine from mast cells. This happens because the injury causes degranulation and histamine release from mast cells.

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Histamine Release - Allergic Reactions

Exposure to an antigen by a previously sensitized individual can trigger an immediate allergic reaction. Sensitization occurs when IgE antibodies attach to the surface of mast cells. Upon re-exposure to the antigen, these IgE antibodies trigger mast cell degranulation and histamine release.

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H1 Receptor Function

The H1 receptor is involved in various physiological processes, including: modulation of the circadian cycle, itching, systemic vasodilation, bronchoconstriction, and ileum contraction.

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Epinephrine in Anaphylaxis

Epinephrine (adrenaline) is the first-line treatment for anaphylactic shock. It acts as a physiologic antagonist to many of the mediators of anaphylaxis, including histamine. Its effectiveness arises from its ability to cause smooth muscle relaxation counteracting the bronchoconstriction caused by histamine.

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Mast Cell Stabilizers

These drugs, like Cromolyn and Nedocromil, reduce the degranulation of mast cells triggered by antigens. They are used in the treatment of asthma and allergies by preventing the release of histamine and other inflammatory mediators.

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Study Notes

Inflammation

  • Inflammation is a complex protective response to injury
  • It aims to inactivate or remove damaging agents and promote healing

COX-1 & COX-2

  • COX-1: A constitutive isoform found in tissues
  • COX-2: Induced by cytokines, part of an inflammatory response

Prostaglandins (PGs)

  • PGE2: Pro-inflammatory, causing vasodilation, bronchodilation, inhibition of gastric acid, and sensitization of pain receptors.
  • PGF2a: Causes uterine contraction, bronchoconstriction, and decreased intraocular pressure.
  • TXA2: Produced by platelets, inducing platelet aggregation and vasoconstriction.
  • PGI2: Inhibits platelet aggregation and causes potent vasodilation.

NSAIDs (Nonsteroidal Anti-inflammatory Drugs)

  • MOA: Inhibit cyclooxygenases (COX), decreasing prostaglandin production.
  • COX-1: Constitutive - responsible for "house-keeping" functions.
  • COX-2: Induced by inflammatory factors; responsible for mediating pain.
  • NSAIDs don't cause pain directly, but sensitize pain receptors.
  • NSAIDs have antipyretic effects (reduce fever).

Aspirin (ASA)

  • Therapeutic use: Antipyretic, analgesic, anti-inflammatory at high doses.
  • Low doses inhibit platelet aggregation (cardiovascular benefits).
  • Low doses can reduce recurrence risk of MI, stroke & colon cancer.
  • Irreversibly inhibits TXA2, affecting platelet lifetime.
  • Results in decreased thrombus formation (anticoagulant effect).
  • Can cause GI distress, nausea, vomiting, microscopic bleeding.
  • Prolongs bleeding time; requires adjustment in dose for anticoagulant effects.

Propionic acid derivatives (e.g., Ibuprofen)

  • Anti-inflammatory, analgesic, and antipyretic effects.
  • Generally less likely to cause GI upset than aspirin.
  • Less potent anti-inflammatory than other NSAIDs.
  • Faster acting and better absorbed than aspirin.
  • Significant fluid retention effects.

Acetic acid derivatives (e.g., Diclofenac)

  • More potent anti-inflammatory than analgesics and antipyretics.
  • More potent than indomethacin and naproxen.
  • Clinical applications: Inflammatory conditions, musculoskeletal pain, dysmenorrhea, and acute gouty arthritis.
  • Potential for increased cardiovascular events.
  • Gastrointestinal ulceration and bleeding risk.

Heteroaryl Acetic Acids (e.g., Ketorolac)

  • Antipyretic, analgesic, and anti-inflammatory properties.
  • Indicated for short-term pain management.
  • Primarily used for acute pain.

COX-2 Selective NSAID: Celecoxib

  • Selective inhibitor of COX-2.
  • Less likely to cause gastrointestinal issues.
  • Potential for cardiovascular risks (e.g., thrombotic events).
  • Contraindicated for patients with severe renal insufficiency.

Steroidal Anti-inflammatory Drugs (SAIDs)

  • Short-acting glucocorticoids (e.g., hydrocortisone); Intermediate-acting (e.g., prednisone).

Histamine

  • An autacoid (local hormone).
  • Involved in allergic and inflammatory reactions.
  • Storage and release from mast cells through exocytosis.
  • Histamine triggers various inflammatory effects.
  • Mast cell degranulation leads to histamine release.

Histamine Antagonists/Blockers

  • First generation: Sedating (e.g., diphenhydramine); Second generation (e.g., Cetirizine).
  • H1 blockers: Block H1 receptors (itching, vasodilation, bronchoconstriction).
  • H2 blockers: Block H2 receptors (gastric acid secretion; e.g., Cimetidine).

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Description

This quiz covers key concepts related to inflammation, COX-1 and COX-2, and the role of prostaglandins and NSAIDs. Understand how these components interact and their significance in the body's healing processes. Test your knowledge on how nonsteroidal anti-inflammatory drugs work to alleviate pain and inflammation.

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