Pain Relievers, NSAIDS, and Gout
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Questions and Answers

Which NSAID has anti-platelet effects?

  • Ibuprofen
  • Aspirin (correct)
  • Diclofenac
  • Celecoxib

    • What is a common side effect associated with NSAIDs affecting the gastrointestinal system?

  • Acute renal failure
  • Renal impairment
  • Worsening hypertension
  • Gastric ulcers and bleeding (correct)

    • Which NSAID is associated with an increased risk of heart attack and stroke?

  • Celecoxib (correct)
  • Meloxicam
  • Sulindac
  • Ketorolac

    • Which NSAID is least likely to lead to chronic renal failure?

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

    What is the mechanism of action of acetaminophen?

    <p>Inhibits COX-1 &amp; COX-2</p> Signup and view all the answers

    Which NSAID is known for having fewer gastrointestinal side effects compared to aspirin?

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

    What is a common side effect associated with NSAIDs like piroxicam and celecoxib?

    <p>Gastric ulcers and bleeding</p> Signup and view all the answers

    Which NSAID can be combined with aspirin as it lacks antiplatelet effects?

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

    What is the treatment for acetaminophen overdose?

    <p>N-acetylcysteine (NAC)</p> Signup and view all the answers

    What is the mechanism of action of NSAIDs like indomethacin and sulindac?

    <p>Inhibiting the synthesis of prostaglandins by blocking COX enzymes</p> Signup and view all the answers

    Which NSAID is specifically mentioned to be useful in the treatment of patent ductus arteriosus when administered intravenously?

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

    What is a common side effect associated with NSAIDs like indomethacin and sulindac?

    <p>Increased risk of bleeding</p> Signup and view all the answers

    How do NSAIDs like indomethacin and sulindac affect renal function?

    <p>They decrease the renal excretion of aminoglycosides or digitalis</p> Signup and view all the answers

    Which NSAID is known for its high incidence of adverse effects, including gastrointestinal, hematopoietic, and hypersensitivity reactions?

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

    Along with vertigo, what is an initial sign of salicylate toxicity in adults?

    <p>Hearing loss</p> Signup and view all the answers

    What is the common sign of toxicity in children due to salicylate overdose?

    <p>Respiratory alkalosis</p> Signup and view all the answers

    How is salicylate toxicity typically managed in case of emergency?

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

    What is the mechanism of action of NSAIDs?

    <p>Inhibition of COX enzymes</p> Signup and view all the answers

    Which statement about NSAIDs and renal function impairment is true?

    <p>NSAIDs may cause decreased blood flow to the kidney</p> Signup and view all the answers

    What is the mechanism of action of aspirin as an NSAID?

    <p>Inhibition of COX-1 in the bloodstream</p> Signup and view all the answers

    Which of the following is an indication for low-dose aspirin (<300 mg/day)?

    <p>Antiplatelet activity</p> Signup and view all the answers

    How does NSAID use contribute to renal function impairment?

    <p>Worsening hypertension</p> Signup and view all the answers

    What is a potential side effect of prolonged NSAID use related to the kidneys?

    <p>Renal ischemia</p> Signup and view all the answers

    What is a characteristic symptom of salicylate toxicity?

    <p>Increased respiratory depth</p> Signup and view all the answers

    What is the primary mechanism of action of NSAIDs?

    <p>Blocking the cyclooxygenase (COX) enzyme</p> Signup and view all the answers

    Which of the following is a common indication for using NSAIDs?

    <p>Relieving mild to moderate pain and inflammation</p> Signup and view all the answers

    How do NSAIDs affect renal function?

    <p>They may impair renal function by reducing prostaglandin synthesis</p> Signup and view all the answers

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

    <p>Gastrointestinal ulcers</p> Signup and view all the answers

    What is a potential consequence of salicylate toxicity?

    <p>Ringing in the ears (tinnitus)</p> Signup and view all the answers

    What is the mechanism of action of NSAIDs like naproxen in the context of gout treatment?

    <p>Inhibition of prostaglandin synthesis by blocking COX enzymes</p> Signup and view all the answers

    Which of the following conditions is an indication for the use of NSAIDs like naproxen in rheumatoid arthritis?

    <p>Inflammation and pain in joints</p> Signup and view all the answers

    How do NSAIDs like naproxen affect renal function?

    <p>They inhibit prostaglandin synthesis leading to decreased renal blood flow</p> Signup and view all the answers

    What is a potential side effect associated with NSAIDs like naproxen?

    <p>Gastrointestinal symptoms</p> Signup and view all the answers

    Which statement is true regarding salicylate toxicity?

    <p>It can cause tinnitus and respiratory alkalosis</p> Signup and view all the answers

    Which NSAID is known for its less risk of gastrointestinal ulcers and bleeding compared to other NSAIDs like aspirin and naproxen?

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

    What is the main adverse effect associated with celecoxib (Celebrex) use?

    <p>Increased risk of heart attack and stroke</p> Signup and view all the answers

    In the context of gout pharmacotherapy, which medication works by reducing the production of uric acid as an alternative or addition to xanthine oxidase inhibitors?

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

    What is a common adverse effect associated with acetaminophen (paracetamol) use in terms of renal function?

    <p>Deterioration of chronic renal failure</p> Signup and view all the answers

    Which medication used in gout pharmacotherapy works by binding and stabilizing tubulin subunits, leading to the inhibition of urate crystal phagocytosis and neutrophil activation?

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

    Which NSAID is useful as an analgesic in rheumatoid arthritis and gout?

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

    Which NSAID is known for its COX-2 selectivity?

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

    Which NSAID is indicated for short-term management of moderate to severe pain, such as postoperative pain relief, and is 40 times as potent an anti-inflammatory as ibuprofen?

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

    What is the primary reason for the selective inhibition of COX-2 over COX-1 by certain NSAIDs?

    <p>Larger side pocket in COX-2</p> Signup and view all the answers

    Which of the following eicosanoids is not mentioned in the text as being part of the arachidonic acid metabolites group?

    <p>Nitric oxide</p> Signup and view all the answers

    What is the structural basis for the selective inhibition of COX-2 by specific inhibitors?

    <p>Larger side pocket in COX-2</p> Signup and view all the answers

    What is one of the biochemical mediators of inflammation NOT mentioned as an arachidonic acid metabolite?

    <p>Nitric oxide</p> Signup and view all the answers

    What is the primary mechanism of action of Xanthine Oxidase Inhibitors (XOI) in gout pharmacotherapy?

    <p>Reduction of uric acid production</p> Signup and view all the answers

    Which medication acts by inhibiting microtubule polymerization to inhibit urate crystal phagocytosis, neutrophil activation, migration, and degranulation in the context of gout pharmacotherapy?

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

    Which medication catalyzes the breakdown of uric acid to allantoin and is used for refractory chronic gout?

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

    How does Probenecid primarily function in the treatment of chronic gout?

    <p>Inhibition of uric acid reabsorption in proximal tubules</p> Signup and view all the answers

    What is the primary function of Prostaglandins (PGs) mentioned in the text?

    <p>Inducing angiogenesis and stimulating cell growth</p> Signup and view all the answers

    Which enzyme is responsible for converting arachidonic acid into prostaglandin hormones?

    <p>Cyclooxygenases (COXs)</p> Signup and view all the answers

    What is the main role of Leukotrienes (LTs) in the body based on the text?

    <p>Serving as inflammatory mediators during allergy attacks</p> Signup and view all the answers

    Which form of Cyclooxygenases (COXs) is more involved in maintaining normal homeostasis in the body?

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

    What symptoms are typically associated with the release of Leukotrienes (LTs) as mentioned in the text?

    <p>Sneezing, coughing, and difficulty breathing</p> Signup and view all the answers

    Which eicosanoid acts as a potent vasodilator and inhibits platelet aggregation?

    <p>Prostacyclin (PGI2)</p> Signup and view all the answers

    What is the primary function of leukotrienes in the body?

    <p>Recruiting neutrophils and increasing vascular permeability</p> Signup and view all the answers

    Which eicosanoid arises from COX action and stimulates platelet aggregation?

    <p>Thromboxane A2 (TXA2)</p> Signup and view all the answers

    What is unique about lipoxins compared to other eicosanoids?

    <p>They are formed via sequential interactions between 5-LOX and 12-LOX</p> Signup and view all the answers

    Which eicosanoid is known for its anti-inflammatory effects?

    <p>Prostaglandin E2</p> Signup and view all the answers

    How does acetaminophen (Paracetamol) affect renal function?

    <p>Has no impact on renal function</p> Signup and view all the answers

    In gout pharmacotherapy, which medication works by reducing the production of uric acid as an alternative or addition to xanthine oxidase inhibitors?

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

    What is the primary function of leukotrienes in the body based on the text?

    <p>Mediate inflammation</p> Signup and view all the answers

    Which medication used in gout pharmacotherapy inhibits microtubule polymerization to inhibit urate crystal phagocytosis and neutrophil activation?

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

    What is the structural basis for the selective inhibition of COX-2 by specific inhibitors?

    <p>Targeting COX-2 active site more selectively</p> Signup and view all the answers

    Which enzyme catalyzes the final step in the biosynthesis of thromboxane A2 (TXA2)?

    <p>Thromboxane synthase</p> Signup and view all the answers

    Study Notes

    Here are the study notes:

    Salicylates and Respiratory Center

    • Salicylates directly stimulate the respiratory center in the medulla, leading to hyperventilation (increased rate and depth) and respiratory alkalosis
    • Respiratory alkalosis is compensated in the kidney by loss of HCO3-, Na+, and K+ plasma pH is lowered to normal with a loss of fixed anion
    • In children, respiratory alkalosis is followed by a decrease in plasma pH, low plasma HCO3- with near normal pCO2

    Salicylate Toxicity

    • Salicylate toxicity (overdose or poisoning with > 5g/d of aspirin or salicylate) in adults is characterized by tinnitus, hearing loss, and vertigo as initial signs of toxicity
    • In children, common signs of toxicity include acidosis, hyperventilation, and lethargy
    • Rescue: i.v. NaHCO3, alkalization of urine with bicarbonate to reduce salicylate reabsorption, promote excretion, correction of acid-base disturbances, replacement of electrolytes and fluids, cooling, forced diuresis, and hemodialysis

    NSAIDS (Non-Selective Reversible COX Inhibitors)

    • Common agents: Ibuprofen, Naproxen, Ketorolac, Meloxicam, Piroxicam, Sulindac
    • Activity profile: Analgesic, antipyretic, anti-inflammatory, and anti-platelet effects (aspirin)
    • Side effects: GI (gastric, intestinal ulcers, bleeding), renal (acute renal failure, analgesic nephropathy), CV (worsen hypertension, increased risk of heart attack and stroke, except aspirin/naproxen)

    Selective COX-2 Inhibitors

    • Common agents: Celeboxib (Celebrex)
    • Indications: Pain, inflammation, effective in rheumatoid arthritis and osteoarthritis
    • Side effects: CV (increased risk of heart attack and stroke), less risk of GI ulcers/bleeding, lacks anti-platelet effects, can be combined with aspirin, renal (deterioration of chronic renal failure, increase in blood pressure)

    Acetaminophen (Paracetamol)

    • Mechanism of action: Inhibits COX-1 and COX-2, crosses the blood-brain-barrier
    • Indications: Analgesic, antipyretic, poor anti-inflammatory activity in the periphery
    • Side effects: Hepatotoxicity due to acetaminophen overdose, treatment is N-acetylcysteine (NAC) to replenish glutathione stores in the liver

    COX-2 Inhibitors

    • Mechanism of action: Inhibits COX-2, reducing production of prostaglandins
    • Indications: Pain, inflammation, effective in rheumatoid arthritis and osteoarthritis
    • Side effects: CV (increased risk of heart attack and stroke), less risk of GI ulcers/bleeding, lacks anti-platelet effects, can be combined with aspirin, renal (deterioration of chronic renal failure, increase in blood pressure)

    Pharmacotherapy for Gout

    • Indications: Acute gouty arthritis, urate lowering therapy for chronic gout
    • Mechanism of action: Binds and stabilizes tubulin subunits, inhibiting microtubule polymerization, inhibiting urate crystal phagocytosis, neutrophil activation, migration, and degranulation
    • Adverse effects: Severe diarrhea, GI symptoms, rhabdomyolysis, polyneuropathy
    • Contraindications: Uric acid stones, GI symptoms, infusion reactions

    Rheumatoid Arthritis

    • Definition: Long-term, progressive, and disabling autoimmune disease causing inflammation, swelling, and pain in and around the joints and organs
    • Treatment: NSAIDs, disease-modifying anti-rheumatic agents (DMARDs), including chemotherapeutics like methotrexate and biologics### Eicosanoid Metabolism Overview
    • Eicosanoids are essential signaling molecules derived from polyunsaturated fatty acids, particularly arachidonic acid, which is abundant in cell membrane phospholipids.
    • They play crucial roles in regulating various physiological processes such as inflammation, immune response, blood clotting, and smooth muscle contraction.

    Arachidonic Acid Pathways

    • Arachidonic acid serves as a precursor for all four classes of eicosanoids: prostanoids, lipoxygenase products, cyclooxygenase products, and hydroxyeicosatetraenoic acids.
    • The pathways involve two main enzymatic reactions: cyclooxygenase (COX) mediating the production of prostaglandin H2 (PGH2), and lipoxygenase (LOX) responsible for the generation of hydroperoxyeicosatetraenoic acids (HPETE).
    • Both PGH2 and HPETE serve as substrates for subsequent transformations into different classes of eicosanoids.

    Prostaglandins

    • Prostaglandins are one class of eicosanoids with various biological actions depending on the specific prostaglandin type.
    • Prostaglandin E2 (PGE2) has anti-inflammatory effects while prostaglandin F2α (PGF2α) participates in inflammation and uterine contractions.
    • Prostacyclin (PGI2) acts as a potent vasodilator and inhibits platelet aggregation.

    Leukotrienes

    • Leukotrienes are another group of eicosanoids synthesized through LOX activity, specifically 5-lipoxygenase (5-LOX).
    • They are involved in allergies, asthma, and other inflammatory conditions due to their ability to recruit neutrophils and increase vascular permeability.
    • Cysteinyl leukotrienes, including LTC4, LTD4, and LTE4, are the primary active forms responsible for these effects.

    Thromboxanes

    • Thromboxanes arise from COX action, mainly COX-1 and COX-2, and are named after their ability to stimulate aggregation of human platelets, causing blood clots to form.
    • Thromboxane A2 (TXA2) is particularly significant because it induces platelet aggregation and contributes to vasoconstriction.

    Lipoxins

    • Lipoxins are unique among eicosanoids since they are formed via sequential interactions between 5-LOX and 12-LOX at sites of tissue damage.
    • Their formation depends upon the availability of free cis linolenic acid and involves both enzymes simultaneously acting on the AA substrate.
    • Lipoxins create a balance between resolution and persistence of inflammation and allow them to modulate the inflammatory process.

    Pharmacotherapy for Gout

    • Colchicine is used to treat acute gouty arthritis, binding and stabilizing tubulin subunits to inhibit microtubule polymerization, urate crystal phagocytosis, neutrophil activation, migration, and degranulation.
    • Xanthine Oxidase Inhibitors (XOI) reduce the production of uric acid, and are used as an alternative or addition to XOI.
    • Probenecid inhibits uric acid reabsorption in proximal tubules to increase renal elimination.
    • Pegloticase is a recombinant uricase that catalyzes the breakdown of uric acid to allantoin.

    Rheumatoid Arthritis

    • Rheumatoid arthritis is a long-term, progressive, and disabling autoimmune disease causing inflammation, swelling, and pain in and around the joints and organs.
    • NSAIDs, such as aspirin, were once the drug of choice, but DMARDs, disease modifying anti-rheumatic agents, are now the preferred treatment.
    • DMARDs include chemotherapeutics such as methotrexate and biologics.

    NSAIDs

    • NSAIDs have analgesic, antipyretic, anti-inflammatory, and anti-platelet effects (aspirin).
    • Common NSAIDs include ibuprofen, diclofenac, indomethacin, naproxen, ketorolac, meloxicam, and piroxicam.
    • Side effects of NSAIDs include GI, renal, and CV effects.

    COX-2 Inhibitors

    • Celecoxib is a selective COX-2 inhibitor, effective in rheumatoid arthritis and osteoarthritis, with a lower risk of GI ulcers/bleeding.
    • COX-2 inhibitors have CV effects, but lack antiplatelet effects, and can be combined with aspirin.
    • Sulfa drugs, such as celecoxib, should not be used with allergies.

    Pharmacotherapy for Gout and Rheumatoid Arthritis

    • Indomethacin is used to treat rheumatoid arthritis, musculoskeletal pain, and to treat patent ductus arteriosus.
    • Sulindac is metabolized to a sulfide which is the active drug, with less GI toxicity.
    • NSAIDs are used to treat pain, inflammation, and to reduce inflammation during an acute gout attack.

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