Selective COX-2 Inhibitors Overview
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Questions and Answers

What is a potential consequence of chronic analgesic abuse on renal function?

  • Decreased renal blood flow (correct)
  • Increased production of renal PGE2
  • Enhanced uric acid excretion
  • Increased synthesis of renal PGI2

    • How does aspirin in low doses affect uric acid levels?

  • Decreases uric acid excretion (correct)
  • Has no effect on uric acid levels
  • Only affects uric acid in high doses
  • Increases uric acid excretion

    • What metabolic effects are associated with high doses of aspirin?

  • No significant metabolic changes observed
  • Inhibition of oxidative phosphorylation causing bradycardia
  • Enhanced oxidative phosphorylation leading to hyperpyrexia (correct)
  • Decreased heart rate and normal body temperature

    • What are the effects of aspirin on diuretics and β-blockers?

    <p>Antagonizes the diuretic effect and reduces β-blocker efficacy</p> Signup and view all the answers

    What recommendation is made regarding the use of NSAIDs after 20 weeks of pregnancy?

    <p>Use of NSAIDs is strongly discouraged</p> Signup and view all the answers

    What effect does aspirin have on plasma urate levels?

    <p>Aspirin increases plasma urate levels significantly</p> Signup and view all the answers

    What is a result of prolonged aspirin use related to uterine contractions during labor?

    <p>Prolongation of pregnancy and delay of labor</p> Signup and view all the answers

    What is the role of aldosterone concerning renal effects due to analgesics?

    <p>Increases sodium and water retention</p> Signup and view all the answers

    What primary risk is associated with selective COX-2 inhibitors as opposed to non-selective COX inhibitors?

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

    Which of the following is a common side effect of non-selective COX inhibitors?

    <p>Frequent hypersensitivity reactions</p> Signup and view all the answers

    What is the mechanism by which non-selective COX inhibitors exert their effects?

    <p>They inhibit COX-1 and COX-2 enzymes</p> Signup and view all the answers

    Selective COX-2 inhibitors are characterized by which of the following pharmacological effects compared to non-selective COX inhibitors?

    <p>Higher risk of thrombotic complications</p> Signup and view all the answers

    Which statement accurately reflects the risk profile of COX-2 inhibitors?

    <p>They are associated with a higher risk of myocardial infarction</p> Signup and view all the answers

    What is a common outcome of the excessive aggregation of platelets when using selective COX-2 inhibitors?

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

    Why were Rofecoxib (Vioxx®) and Valdecoxib withdrawn from the market?

    <p>Potential for serious cardiovascular events</p> Signup and view all the answers

    In comparing selective and non-selective COX inhibitors, which side effect is more pronounced in non-selective COX inhibitors?

    <p>Frequent gastric side effects</p> Signup and view all the answers

    What is a notable side effect of ketorolac when used as an analgesic?

    <p>Severe gastrointestinal bleeding</p> Signup and view all the answers

    Which of the following NSAIDs is considered a good alternative to aspirin in treating flu fevers in children?

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

    Which of the following statements is true regarding sulindac?

    <p>It is a prodrug with a long half-life.</p> Signup and view all the answers

    What is a characteristic feature of selective COX-2 inhibitors compared to traditional NSAIDs?

    <p>They target the COX-2 enzyme responsible for inflammation.</p> Signup and view all the answers

    Which NSAID is known to potentially induce nephrotoxic syndrome?

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

    What is the primary clinical use of indomethacin?

    <p>To aid in the closure of patent ductus arteriosus in premature infants</p> Signup and view all the answers

    How does meloxicam compare to other NSAIDs in terms of COX enzyme selectivity?

    <p>It is slightly selective for COX-2.</p> Signup and view all the answers

    What risk is associated with long-term use of ibuprofen in women?

    <p>Higher incidence of hypertension</p> Signup and view all the answers

    Which of the following is a potential adverse effect of salicylates related to the gastrointestinal tract?

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

    What is the primary risk associated with administering aspirin to children?

    <p>Reye’s syndrome</p> Signup and view all the answers

    Which of the following conditions is NOT a contraindication for the use of aspirin?

    <p>Pediatric asthma</p> Signup and view all the answers

    What effect do salicylates have in relation to blood coagulation?

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

    How does diclofenac differ from other NSAIDs in terms of gastrointestinal effects?

    <p>It is less gastric irritant</p> Signup and view all the answers

    What is a potential consequence of aspirin use in patients with hyperuricemic conditions?

    <p>Inhibition of uric acid excretion</p> Signup and view all the answers

    When should aspirin be stopped prior to surgery to minimize risks?

    <p>7 days before</p> Signup and view all the answers

    What is the primary mechanism of action for salicylic acid in the treatment of warts?

    <p>Keratolytic action</p> Signup and view all the answers

    Selectivity for COX-2 increases the risk of peptic ulceration and renal failure.

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

    Selective COX-2 inhibitors decrease the risk of thrombotic complications.

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

    Rofecoxib and valdecoxib were removed from the market due to their analgesic effectiveness.

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

    Both selective and non-selective COX inhibitors have equal analgesic effects.

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

    TXA2 is formed by COX-2 while PGI2 is formed by COX-1.

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

    Selective COX-2 inhibitors are linked to fewer hypersensitivity reactions compared to non-selective COX inhibitors.

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

    Non-selective COX inhibitors frequently cause renal side effects.

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

    Selective COX-2 inhibitors increase the risk of cardiovascular accidents.

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

    Chronic abuse of analgesics can lead to renal failure due to ischemia from decreased renal PGE2 synthesis.

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

    High doses of aspirin are known to improve oxidative phosphorylation efficiency in the body.

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

    Aspirin administration in small doses increases uric acid excretion, making it safe for patients with gout.

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

    The use of NSAIDs is discouraged after 20 weeks of pregnancy due to their effects on uterine contractions.

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

    Aspirin at low doses has a significant effect on plasma urate levels, reducing the risk of hyperuricemia.

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

    Salt and water retention due to decreased renal blood flow can antagonize the effects of diuretics.

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

    Aspirin and other analgesics can enhance the antihypertensive effects of beta-blockers.

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

    Chronic analgesic nephropathy is a recognized condition resulting from prolonged use of analgesics.

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

    Salicylic acid is an effective keratolytic agent used primarily for the treatment of warts.

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

    Methylsalicylic acid is known primarily for its antithrombotic properties.

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

    Adults may experience severe hepatic injury from salicylate use, but it is more common in children due to Reye's syndrome.

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

    Chronic renal diseases are not adversely affected by the use of aspirin.

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

    Aspirin should be discontinued at least 7 days before surgery to reduce the risk of bleeding.

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

    Diclofenac is less nephrotoxic than other NSAIDs but is more gastric irritant.

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

    Salicylates can increase the tendency to bleed due to displacement of other drugs from plasma proteins.

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

    Using small-to-moderate doses of aspirin can enhance uric acid excretion in patients with gout.

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

    Sulindac is a potent analgesic with minimal effect on platelet aggregation.

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

    Ibuprofen has been shown to have a higher incidence of nephrotoxic syndrome compared to fenoprofen.

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

    Indomethacin is considered less toxic compared to other NSAIDs and is often approved for use in children.

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

    Celecoxib selectively inhibits COX-1 enzyme more effectively than COX-2 enzyme.

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

    Ketorolac has no reported interactions with oral anticoagulants.

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

    Long-term use of piroxicam is associated with a reduced risk of gastrointestinal bleeding compared to other NSAIDs.

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

    Long-term use of ibuprofen is linked to an increased incidence of hypertension in men.

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

    Meloxicam is considered non-selective when it comes to COX enzyme inhibition.

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

    What renal condition can result from chronic analgesic abuse?

    <p>Chronic analgesic nephropathy.</p> Signup and view all the answers

    How does aspirin use affect plasma levels of uric acid?

    <p>Aspirin can decrease uric acid excretion.</p> Signup and view all the answers

    What cardiovascular effects can high doses of aspirin induce?

    <p>High doses can cause tachycardia and hyperpyrexia.</p> Signup and view all the answers

    What is the consequence of using NSAIDs after 20 weeks of pregnancy?

    <p>It may prolong pregnancy and delay labor.</p> Signup and view all the answers

    What role does aldosterone play in renal effects due to analgesic use?

    <p>Aldosterone increases sodium and water retention.</p> Signup and view all the answers

    What recommendation is made regarding the use of aspirin in gout patients?

    <p>Aspirin should be avoided in patients with gout.</p> Signup and view all the answers

    Why is chronic renal ischemia a concern for patients abusing analgesics?

    <p>It results from decreased synthesis of renal prostaglandins.</p> Signup and view all the answers

    What is the primary risk of using selective COX-2 inhibitors?

    <p>Increased risk of cardiovascular events.</p> Signup and view all the answers

    What adverse effect is associated with long-term use of salicylates in the gastrointestinal tract?

    <p>Epigastric pain and gastric ulcers.</p> Signup and view all the answers

    What major risk is associated with the use of aspirin in children?

    <p>Reye's syndrome.</p> Signup and view all the answers

    What adverse effect is specifically increased by selective COX-2 inhibitors compared to non-selective COX inhibitors?

    <p>The risk of cardiovascular accidents is increased by selective COX-2 inhibitors.</p> Signup and view all the answers

    In what way can aspirin potentially impact renal function?

    <p>It can cause analgesic nephropathy and reduce renal blood flow.</p> Signup and view all the answers

    What condition could be exacerbated by the use of small-to-moderate doses of aspirin?

    <p>Gout.</p> Signup and view all the answers

    Why do selective COX-2 inhibitors lead to increased platelet aggregation?

    <p>Selective COX-2 inhibitors reduce the production of PGI2 while allowing TXA2 formation, leading to increased platelet aggregation.</p> Signup and view all the answers

    Which COX enzymes are inhibited by non-selective COX inhibitors?

    <p>Non-selective COX inhibitors inhibit both COX-1 and COX-2.</p> Signup and view all the answers

    How does the use of aspirin affect the bleeding tendency?

    <p>It increases the bleeding tendency by inhibiting platelet aggregation.</p> Signup and view all the answers

    What is the primary use of methylsalicylic acid in a clinical context?

    <p>As a counter-irritant for local rheumatic pain.</p> Signup and view all the answers

    How frequently do selective COX-2 inhibitors cause hypersensitivity reactions compared to non-selective inhibitors?

    <p>Hypersensitivity reactions are less frequent with selective COX-2 inhibitors compared to non-selective COX inhibitors.</p> Signup and view all the answers

    What important precaution should be taken when administering aspirin before surgery?

    <p>Aspirin must be stopped at least 7 days prior to surgery.</p> Signup and view all the answers

    What was one reason for the withdrawal of Rofecoxib and Valdecoxib from the market?

    <p>They were withdrawn due to potential adverse cardiovascular effects.</p> Signup and view all the answers

    Explain the impact of selective COX-2 inhibitors on renal side effects.

    <p>Selective COX-2 inhibitors still have a frequent risk of renal side effects, similar to non-selective ones.</p> Signup and view all the answers

    Why should diclofenac be used cautiously in patients with renal issues?

    <p>It can impair renal blood flow and decrease glomerular filtration rate (GFR).</p> Signup and view all the answers

    What is the major pharmacological distinction between the analgesic effects of selective and non-selective COX inhibitors?

    <p>Both have equal analgesic and antipyretic effects.</p> Signup and view all the answers

    In terms of gastric side effects, how do selective COX-2 inhibitors compare to non-selective inhibitors?

    <p>Selective COX-2 inhibitors have less frequent gastric side effects compared to non-selective inhibitors.</p> Signup and view all the answers

    What distinguishes sulindac as a prodrug in its pharmacological profile?

    <p>Sulindac is converted in the body to its active form, providing a long half-life and effective anti-inflammatory properties.</p> Signup and view all the answers

    What are the main risks associated with the use of ketorolac as an analgesic?

    <p>Ketorolac is a potent analgesic but has a significant risk of causing severe gastrointestinal bleeding.</p> Signup and view all the answers

    How does ibuprofen serve as an alternative treatment for children with flu fevers?

    <p>Ibuprofen effectively reduces fever and is generally well-tolerated, making it a safer option compared to aspirin in children.</p> Signup and view all the answers

    Describe the mechanism by which indomethacin facilitates the closure of patent ductus arteriosus in premature infants.

    <p>Indomethacin inhibits prostaglandin synthesis, which prevents the maintenance of the patent ductus arteriosus, promoting its closure.</p> Signup and view all the answers

    In what way does piroxicam's pharmacokinetic profile differ from other NSAIDs?

    <p>Piroxicam has a long half-life of approximately 45 hours, allowing for once-daily dosing compared to many other NSAIDs.</p> Signup and view all the answers

    What unique advantages do selective COX-2 inhibitors offer in treating inflammation and pain?

    <p>Selective COX-2 inhibitors specifically target the COX-2 enzyme associated with inflammation, minimizing gastrointestinal side effects compared to non-selective NSAIDs.</p> Signup and view all the answers

    What implications does the long-term use of ibuprofen have for women's cardiovascular health?

    <p>Long-term ibuprofen use is associated with an increased incidence of hypertension in women, raising cardiovascular risk.</p> Signup and view all the answers

    How does the selectivity of meloxicam towards COX-2 compare to COX-1, and why is this significant?

    <p>Meloxicam is slightly more selective for COX-2 than COX-1, which helps reduce gastrointestinal side effects associated with non-selective inhibition.</p> Signup and view all the answers

    Chronic abuse of analgesics can lead to chronic renal ______ due to ischemia.

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

    High doses of aspirin cause coupling of oxidative phosphorylation and can lead to ______ and hyperpyrexia.

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

    The use of NSAIDs after 20 weeks of pregnancy is not ______ due to their effects on uterine contractions.

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

    Low doses of aspirin are not thought to have a significant effect on plasma ______ levels.

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

    Salt and water retention occurs due to decreased renal ______ flow.

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

    Small-to-moderate doses of aspirin can decrease uric acid ______ and thus may be contraindicated in gout.

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

    Aspirin can ______ the diuretic effect of diuretics due to decreased renal function.

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

    Prolongation of pregnancy and delay of labor occurs due to inhibition of PGs necessary for uterine ______.

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

    Sulindac is known as a ______ and has a long half-life.

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

    Ketorolac is a potent analgesic but it can cause severe ______ bleeding.

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

    Fenoprofen has been reported to induce ______ syndrome.

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

    Long-term use of ibuprofen is associated with an increased incidence of ______ in women.

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

    Indomethacin is a very potent ______ inhibitor.

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

    Piroxicam has a long half-life, approximately ______ hours.

    <p>45</p> Signup and view all the answers

    Celecoxib is approximately 30 times more potent at inhibiting COX-2 than COX-______.

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

    Selective COX-2 inhibitors are newer forms of NSAIDs that directly target the ______ enzyme responsible for pain.

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

    Salicylic acid is used for the treatment of ______.

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

    A dose of 150 mg/day of Diclofenac can impair renal blood flow and ______.

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

    Reye's syndrome is a severe hepatic injury that can occur in ______.

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

    Aspirin must be stopped at least 7 days before ______.

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

    Methylsalicylic acid is used as a counter-irritant for local ______ pain.

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

    Chronic renal diseases may be aggravated by the use of ______.

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

    Salicylates can increase the bleeding tendency due to displacement of other drugs from ______ proteins.

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

    The use of NSAIDs is discouraged after 20 weeks of ______.

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

    Selective COX-2 inhibitors may also increase the risk of cardiovascular ______.

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

    Rofecoxib and valdecoxib were withdrawn from the market due to potential adverse ______.

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

    The mechanism of selective COX-2 inhibitors focuses on inhibiting the COX-2 ______ enzyme.

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

    Non-selective COX inhibitors frequently cause ______ side effects.

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

    TXA2 is formed by COX-1, whereas PGI2 is formed by COX-______.

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

    Both selective and non-selective COX inhibitors have equal ______ and antipyretic effects.

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

    High doses of selective COX-2 inhibitors can potentially lead to increased ______ complications.

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

    Hypersensitivity reactions are reported to be ______ frequent with selective COX-2 inhibitors.

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

    Match the following COX inhibitors with their side effect profiles:

    <p>Non-selective COX inhibitors = Increased thrombotic complications Selective COX-2 inhibitors = Decreased thrombotic complications</p> Signup and view all the answers

    Match the following COX enzymes with their effects:

    <p>COX-1 = Inhibits renal protective prostaglandins COX-2 = Inhibits inflammatory prostaglandins</p> Signup and view all the answers

    Match the following reasons for withdrawal of COX inhibitors with the respective drugs:

    <p>Rofecoxib (Vioxx®) = Potential renal failure Valdecoxib = Potential gastric ulceration</p> Signup and view all the answers

    Match the following side effects with their corresponding COX inhibitor types:

    <p>Frequent hypersensitivity reactions = Non-selective COX inhibitors Less frequent hypersensitivity reactions = Selective COX-2 inhibitors Frequent renal side effects = Selective COX-2 inhibitors</p> Signup and view all the answers

    Match the following classes of COX inhibitors with their pharmacological effects:

    <p>Both COX classes = Equal analgesic and antipyretic effects Selective COX-2 inhibitors = Increased platelet aggregation Non-selective COX inhibitors = Decreased platelet aggregation</p> Signup and view all the answers

    Match the following side effects with the frequency seen in different COX inhibitors:

    <p>Gastric side effects = Frequent in non-selective COX inhibitors Thrombotic complications = Increased in selective COX-2 inhibitors Renal side effects = Frequent in both types Hypersensitivity reactions = Less frequent in selective COX-2 inhibitors</p> Signup and view all the answers

    Match the following health conditions with their associated COX inhibitors:

    <p>Cardiovascular accidents = Selective COX-2 inhibitors Peptic ulceration risk = Non-selective COX inhibitors Renal failure risk = Selective COX-2 inhibitors Gastric complications = Non-selective COX inhibitors</p> Signup and view all the answers

    Match the following terms with their correct definitions regarding COX inhibitors:

    <p>TXA2 = Promotes platelet aggregation PGI2 = Inhibits platelet aggregation COX-1 = Is a constitutive enzyme COX-2 = Inducible enzyme associated with inflammation</p> Signup and view all the answers

    Match the following adverse effects with their corresponding causes:

    <p>GIT ulcers = Chronic use of salicylates Reye's syndrome = Hepatic injury in children Analgesic nephropathy = Prolonged analgesic use Bleeding tendency = Aspirin's effect on plasma proteins</p> Signup and view all the answers

    Match the following NSAIDs with their notable properties:

    <p>Diclofenac = Less gastric irritant but more nephrotoxic Aspirin = Antithrombotic effects Methylsalicylic acid = Counter-irritant for rheumatic pain Salicylic acid = Keratolytic action for warts</p> Signup and view all the answers

    Match the following contraindications with their related conditions:

    <p>Hemophilia = Hemorrhagic disorders Gastritis = GIT disorders Uncontrolled hypertension = Risk of bleeding Chronic renal diseases = Aggravated renal failure</p> Signup and view all the answers

    Match the following NSAID mechanisms with their clinical usage:

    <p>Salicylic acid = Treatment of warts Methylsalicylic acid = Local pain relief Aspirin = Prevention of thrombosis Diclofenac = Pain management in arthritis</p> Signup and view all the answers

    Match the following patient conditions with their precautions when using NSAIDs:

    <p>Peptic ulcer = Avoid aspirin Asthma = Risk of bronchospasm Gout = May inhibit uric acid excretion Pregnancy = Stop aspirin 7 days prior to surgery</p> Signup and view all the answers

    Match the following NSAID effects with their respective systems:

    <p>GIT = Nausea and vomiting Hepatic = Reversible hepatic injury in adults Blood = Increased bleeding tendency Uterus = Prolongation of pregnancy</p> Signup and view all the answers

    Match the following drugs with their effects on renal function:

    <p>Aspirin = Decreased diuretic effect of loop diuretics Diclofenac = Impaired renal blood flow NSAIDs = Increased risk of renal failure Salicylates = Salt and water retention</p> Signup and view all the answers

    Match the following NSAID-related terms with their descriptions:

    <p>Keratolytic = Salicylic acid action Counter-irritant = Methylsalicylic acid use Antipyretic = Not recommended for routine use Antirheumatic = Used in rheumatoid arthritis</p> Signup and view all the answers

    Match the following NSAIDs with their primary characteristics:

    <p>Sulindac = Prodrug with long half-life Ketorolac = Potent analgesic with risk of severe GIT bleeding Ibuprofen = Good alternative to aspirin in children with flu fevers Piroxicam = Higher risk of bleeding and ulceration than other NSAIDs</p> Signup and view all the answers

    Match each NSAID with its specific risk or effect:

    <p>Fenoprofen = Induces nephrotoxic syndrome Indomethacin = Potent COX inhibitor but more toxic Meloxicam = Slightly selective for COX-2 Celecoxib = Approximately 30 times more potent at inhibiting COX-2 than COX-1</p> Signup and view all the answers

    Match the following characteristics with the appropriate selective COX-2 inhibitors:

    <p>Celecoxib = High potency for COX-2 inhibition Etoricoxib = Used for treatment of osteoarthritis Meloxicam = Slight preference for COX-2 enzyme Rofecoxib = Withdrawn from the market due to safety concerns</p> Signup and view all the answers

    Match each NSAID with its usage details:

    <p>Indomethacin = Approved for patent ductus arteriosus closure in infants Ketorolac = Used for short-term management of severe pain Ibuprofen = Long-term use may increase hypertension risk Sulindac = Minimal effect on platelet aggregation</p> Signup and view all the answers

    Match the following NSAIDs to their common side effects:

    <p>Fenoprofen = Nephrotoxicity potential Ketorolac = Gastrointestinal bleeding risk Piroxicam = Increased risk of ulceration Sulindac = Minimal platelet aggregation effect</p> Signup and view all the answers

    Match the following long-term effects of NSAIDs with the corresponding drugs:

    <p>Ibuprofen = Increased incidence of hypertension in women Ketorolac = Risk of severe gastrointestinal complications Indomethacin = Potent analgesic with higher toxicity Piroxicam = Long half-life associated with bleeding risk</p> Signup and view all the answers

    Match the following NSAIDs with their specific use and response:

    <p>Celecoxib = Inhibits COX-2 enzyme to reduce inflammation Ketorolac = Used mainly for acute pain management Meloxicam = Has some selectivity for COX-2 Sulindac = Used for rheumatic pain and osteoarthritis</p> Signup and view all the answers

    Match the following statements with the appropriate NSAIDs:

    <p>Indomethacin = Highly potent but relatively more toxic Fenoprofen = Reported to induce nephrotoxic syndrome Ibuprofen = Alternative to aspirin safe for children Ketorolac = Can cause severe GIT bleeding in long-term use</p> Signup and view all the answers

    Match the following renal effects of analgesics with their corresponding descriptions:

    <p>Analgesic nephropathy = Chronic renal failure from analgesic abuse Salt and water retention = Due to decreased renal blood flow Antagonize diuretic effect = Decreased effectiveness of diuretics Uric acid excretion = Small-to-moderate doses can decrease excretion</p> Signup and view all the answers

    Match the effects of high doses of aspirin with their outcomes:

    <p>Tachycardia = Increased heart rate Hyperpyrexia = Elevated body temperature Prolongation of pregnancy = Delay in labor onset Inhibition of PGs = Prevention of uterine contractions</p> Signup and view all the answers

    Match the therapeutic uses of salicylates with their indications:

    <p>Analgesic = Pain relief in mild-to-moderate pain Antipyretic = Reduction of fever Anti-inflammatory = Relief from inflammatory conditions Cardiovascular prophylaxis = Prevention of thromboembolic events</p> Signup and view all the answers

    Match the pharmacological actions related to aspirin with their effects:

    <p>Inhibition of PGE2 synthesis = Decreased renal blood flow Inhibition of aldosterone synthesis = Salt and water retention Antagonization of beta-blockers = Reduced antihypertensive effect Inhibition of PG I2 production = Increased cardiovascular risks</p> Signup and view all the answers

    Match the conditions related to pregnant women’s use of NSAIDs with their recommendations:

    <p>After 20 weeks = NSAIDs are not recommended Prolonged labor = Due to inhibition of PGs Use in late pregnancy = Caution advised due to risks Uterine contractions = Inhibited by NSAID use</p> Signup and view all the answers

    Match these side effects of aspirin with their associated metabolic effects:

    <p>High-dose effects = Coupling of oxidative phosphorylation Renal ischemia = Chronic use leading to nephropathy Uric acid retention = Can worsen conditions like gout Antiplatelet effect = Reduction in thrombus formation</p> Signup and view all the answers

    Match the following terms with their correct definitions related to analgesics:

    <p>Chronic analgesic nephropathy = Renal damage from long-term analgesic use Analgesic tolerance = Reduced response to pain relief from repeated use NSAIDs contraindication = Risk factors that preclude their use Opioid overdose = Potentially life-threatening condition from excessive use</p> Signup and view all the answers

    Match the statements regarding aspirin with their implications:

    <p>Low-dose aspirin = Minimal effect on uric acid levels High doses of aspirin = Risk of tachycardia and hyperpyrexia Aspirin and diuretics = May reduce the effectiveness of diuretics Salicylate metabolism = Associated with various therapeutic properties</p> Signup and view all the answers

    Study Notes

    Selective COX-2 Inhibitors

    • Selective COX-2 inhibitors reduce the risk of peptic ulceration but do not eliminate the risk of renal failure and other adverse effects associated with NSAIDs.
    • Increased risk of cardiovascular accidents, such as myocardial infarction and stroke, arises from elevated TXA2 levels due to COX-1 activity, while COX-2 inhibition decreases PGI2.
    • Rofecoxib (Vioxx®) and valdecoxib were withdrawn from the market in 2004 and 2005 due to concerns over adverse cardiovascular effects.

    Non-selective COX Inhibitors vs. Selective COX-2 Inhibitors

    • Non-selective COX inhibitors inhibit both COX-1 and COX-2; selective inhibitors primarily target COX-2.
    • Both classes exhibit equal analgesic and antipyretic effects.
    • Gastric side effects are more common with non-selective inhibitors, while selective inhibitors show fewer gastric adverse effects.
    • Non-selective inhibitors generally have decreased thrombotic complications, whereas selective COX-2 inhibitors may increase these risks.

    Renal Effects of NSAIDs

    • Analgesic nephropathy from chronic NSAID use can lead to renal failure due to decreased renal blood flow and reduced PGE2 and PGI2 synthesis.
    • Salt and water retention from decreased renal blood flow can antagonize diuretics and β-blockers' effects.
    • Aspirin at low doses can inhibit uric acid excretion, contraindicating its use in gout patients.

    Metabolic Effects and Pregnancy

    • NSAIDs can cause tachycardia and hyperpyrexia at high doses due to oxidative phosphorylation uncoupling.
    • Use of NSAIDs in pregnancy after 20 weeks is discouraged as they can prolong pregnancy and delay labor by inhibiting necessary prostaglandins.

    Therapeutic Uses of Salicylates

    • Effective as analgesics and antipyretics for mild-to-moderate pain but should not be routinely used to lower fever.
    • Functions as anti-inflammatory and anti-rheumatic agents in conditions such as rheumatoid arthritis and rheumatic fever.
    • Salicylic acid provides keratolytic effects for treating warts; methylsalicylic acid serves as a counter-irritant for local pain.

    Adverse Effects of Salicylates

    • Common gastrointestinal issues include epigastric pain, nausea, vomiting, and risk of gastric ulcers.
    • Hepatic effects include mild reversible injury in adults and severe injury, such as Reye's syndrome, in children.
    • Analgesic nephropathy can develop, along with potential water retention and gout exacerbation.
    • Increased bleeding tendency due to drug displacement from plasma proteins and possible hypersensitivity reactions.

    Precautions and Contraindications

    • Use cautiously in patients with gastrointestinal disorders, bleeding disorders, chronic renal and liver disease, uncontrolled hypertension, and those requiring surgery.
    • Aspirin should be discontinued one week before surgery.

    Other NSAIDs

    • Diclofenac: Widely used; less gastric irritant but can impair renal function at high doses. Combined with PGE analogs to decrease ulceration.
    • Sulindac and Ketorolac: Minimal effects on platelet aggregation; ketorolac is a potent analgesic with risks of GIT bleeding.
    • Ibuprofen, Fenoprofen, Ketoprofen: Safe alternative to aspirin for children; long-term use may lead to hypertension.
    • Indomethacin: Strong COX inhibitor; approved to close patent ductus arteriosus in premature infants.
    • Piroxicam: Long half-life; higher likelihood of bleeding and ulceration compared to other NSAIDs.

    Selective COX-2 Inhibitors

    • Include celecoxib, etoricoxib, and meloxicam, which specifically target COX-2 for pain and inflammation.
    • Celecoxib has a potency 30 times greater at inhibiting COX-2 than COX-1, while meloxicam shows slight selectivity for COX-2.

    Selective COX-2 Inhibitors

    • Selective COX-2 inhibitors reduce the risk of peptic ulceration but do not eliminate the risk of renal failure and other adverse effects associated with NSAIDs.
    • Increased risk of cardiovascular accidents, such as myocardial infarction and stroke, arises from elevated TXA2 levels due to COX-1 activity, while COX-2 inhibition decreases PGI2.
    • Rofecoxib (Vioxx®) and valdecoxib were withdrawn from the market in 2004 and 2005 due to concerns over adverse cardiovascular effects.

    Non-selective COX Inhibitors vs. Selective COX-2 Inhibitors

    • Non-selective COX inhibitors inhibit both COX-1 and COX-2; selective inhibitors primarily target COX-2.
    • Both classes exhibit equal analgesic and antipyretic effects.
    • Gastric side effects are more common with non-selective inhibitors, while selective inhibitors show fewer gastric adverse effects.
    • Non-selective inhibitors generally have decreased thrombotic complications, whereas selective COX-2 inhibitors may increase these risks.

    Renal Effects of NSAIDs

    • Analgesic nephropathy from chronic NSAID use can lead to renal failure due to decreased renal blood flow and reduced PGE2 and PGI2 synthesis.
    • Salt and water retention from decreased renal blood flow can antagonize diuretics and β-blockers' effects.
    • Aspirin at low doses can inhibit uric acid excretion, contraindicating its use in gout patients.

    Metabolic Effects and Pregnancy

    • NSAIDs can cause tachycardia and hyperpyrexia at high doses due to oxidative phosphorylation uncoupling.
    • Use of NSAIDs in pregnancy after 20 weeks is discouraged as they can prolong pregnancy and delay labor by inhibiting necessary prostaglandins.

    Therapeutic Uses of Salicylates

    • Effective as analgesics and antipyretics for mild-to-moderate pain but should not be routinely used to lower fever.
    • Functions as anti-inflammatory and anti-rheumatic agents in conditions such as rheumatoid arthritis and rheumatic fever.
    • Salicylic acid provides keratolytic effects for treating warts; methylsalicylic acid serves as a counter-irritant for local pain.

    Adverse Effects of Salicylates

    • Common gastrointestinal issues include epigastric pain, nausea, vomiting, and risk of gastric ulcers.
    • Hepatic effects include mild reversible injury in adults and severe injury, such as Reye's syndrome, in children.
    • Analgesic nephropathy can develop, along with potential water retention and gout exacerbation.
    • Increased bleeding tendency due to drug displacement from plasma proteins and possible hypersensitivity reactions.

    Precautions and Contraindications

    • Use cautiously in patients with gastrointestinal disorders, bleeding disorders, chronic renal and liver disease, uncontrolled hypertension, and those requiring surgery.
    • Aspirin should be discontinued one week before surgery.

    Other NSAIDs

    • Diclofenac: Widely used; less gastric irritant but can impair renal function at high doses. Combined with PGE analogs to decrease ulceration.
    • Sulindac and Ketorolac: Minimal effects on platelet aggregation; ketorolac is a potent analgesic with risks of GIT bleeding.
    • Ibuprofen, Fenoprofen, Ketoprofen: Safe alternative to aspirin for children; long-term use may lead to hypertension.
    • Indomethacin: Strong COX inhibitor; approved to close patent ductus arteriosus in premature infants.
    • Piroxicam: Long half-life; higher likelihood of bleeding and ulceration compared to other NSAIDs.

    Selective COX-2 Inhibitors

    • Include celecoxib, etoricoxib, and meloxicam, which specifically target COX-2 for pain and inflammation.
    • Celecoxib has a potency 30 times greater at inhibiting COX-2 than COX-1, while meloxicam shows slight selectivity for COX-2.

    Selective COX-2 Inhibitors

    • Selective COX-2 inhibitors reduce the risk of peptic ulceration but do not eliminate the risk of renal failure and other adverse effects associated with NSAIDs.
    • Increased risk of cardiovascular accidents, such as myocardial infarction and stroke, arises from elevated TXA2 levels due to COX-1 activity, while COX-2 inhibition decreases PGI2.
    • Rofecoxib (Vioxx®) and valdecoxib were withdrawn from the market in 2004 and 2005 due to concerns over adverse cardiovascular effects.

    Non-selective COX Inhibitors vs. Selective COX-2 Inhibitors

    • Non-selective COX inhibitors inhibit both COX-1 and COX-2; selective inhibitors primarily target COX-2.
    • Both classes exhibit equal analgesic and antipyretic effects.
    • Gastric side effects are more common with non-selective inhibitors, while selective inhibitors show fewer gastric adverse effects.
    • Non-selective inhibitors generally have decreased thrombotic complications, whereas selective COX-2 inhibitors may increase these risks.

    Renal Effects of NSAIDs

    • Analgesic nephropathy from chronic NSAID use can lead to renal failure due to decreased renal blood flow and reduced PGE2 and PGI2 synthesis.
    • Salt and water retention from decreased renal blood flow can antagonize diuretics and β-blockers' effects.
    • Aspirin at low doses can inhibit uric acid excretion, contraindicating its use in gout patients.

    Metabolic Effects and Pregnancy

    • NSAIDs can cause tachycardia and hyperpyrexia at high doses due to oxidative phosphorylation uncoupling.
    • Use of NSAIDs in pregnancy after 20 weeks is discouraged as they can prolong pregnancy and delay labor by inhibiting necessary prostaglandins.

    Therapeutic Uses of Salicylates

    • Effective as analgesics and antipyretics for mild-to-moderate pain but should not be routinely used to lower fever.
    • Functions as anti-inflammatory and anti-rheumatic agents in conditions such as rheumatoid arthritis and rheumatic fever.
    • Salicylic acid provides keratolytic effects for treating warts; methylsalicylic acid serves as a counter-irritant for local pain.

    Adverse Effects of Salicylates

    • Common gastrointestinal issues include epigastric pain, nausea, vomiting, and risk of gastric ulcers.
    • Hepatic effects include mild reversible injury in adults and severe injury, such as Reye's syndrome, in children.
    • Analgesic nephropathy can develop, along with potential water retention and gout exacerbation.
    • Increased bleeding tendency due to drug displacement from plasma proteins and possible hypersensitivity reactions.

    Precautions and Contraindications

    • Use cautiously in patients with gastrointestinal disorders, bleeding disorders, chronic renal and liver disease, uncontrolled hypertension, and those requiring surgery.
    • Aspirin should be discontinued one week before surgery.

    Other NSAIDs

    • Diclofenac: Widely used; less gastric irritant but can impair renal function at high doses. Combined with PGE analogs to decrease ulceration.
    • Sulindac and Ketorolac: Minimal effects on platelet aggregation; ketorolac is a potent analgesic with risks of GIT bleeding.
    • Ibuprofen, Fenoprofen, Ketoprofen: Safe alternative to aspirin for children; long-term use may lead to hypertension.
    • Indomethacin: Strong COX inhibitor; approved to close patent ductus arteriosus in premature infants.
    • Piroxicam: Long half-life; higher likelihood of bleeding and ulceration compared to other NSAIDs.

    Selective COX-2 Inhibitors

    • Include celecoxib, etoricoxib, and meloxicam, which specifically target COX-2 for pain and inflammation.
    • Celecoxib has a potency 30 times greater at inhibiting COX-2 than COX-1, while meloxicam shows slight selectivity for COX-2.

    Selective COX-2 Inhibitors

    • Selective COX-2 inhibitors reduce the risk of peptic ulceration but do not eliminate the risk of renal failure and other adverse effects associated with NSAIDs.
    • Increased risk of cardiovascular accidents, such as myocardial infarction and stroke, arises from elevated TXA2 levels due to COX-1 activity, while COX-2 inhibition decreases PGI2.
    • Rofecoxib (Vioxx®) and valdecoxib were withdrawn from the market in 2004 and 2005 due to concerns over adverse cardiovascular effects.

    Non-selective COX Inhibitors vs. Selective COX-2 Inhibitors

    • Non-selective COX inhibitors inhibit both COX-1 and COX-2; selective inhibitors primarily target COX-2.
    • Both classes exhibit equal analgesic and antipyretic effects.
    • Gastric side effects are more common with non-selective inhibitors, while selective inhibitors show fewer gastric adverse effects.
    • Non-selective inhibitors generally have decreased thrombotic complications, whereas selective COX-2 inhibitors may increase these risks.

    Renal Effects of NSAIDs

    • Analgesic nephropathy from chronic NSAID use can lead to renal failure due to decreased renal blood flow and reduced PGE2 and PGI2 synthesis.
    • Salt and water retention from decreased renal blood flow can antagonize diuretics and β-blockers' effects.
    • Aspirin at low doses can inhibit uric acid excretion, contraindicating its use in gout patients.

    Metabolic Effects and Pregnancy

    • NSAIDs can cause tachycardia and hyperpyrexia at high doses due to oxidative phosphorylation uncoupling.
    • Use of NSAIDs in pregnancy after 20 weeks is discouraged as they can prolong pregnancy and delay labor by inhibiting necessary prostaglandins.

    Therapeutic Uses of Salicylates

    • Effective as analgesics and antipyretics for mild-to-moderate pain but should not be routinely used to lower fever.
    • Functions as anti-inflammatory and anti-rheumatic agents in conditions such as rheumatoid arthritis and rheumatic fever.
    • Salicylic acid provides keratolytic effects for treating warts; methylsalicylic acid serves as a counter-irritant for local pain.

    Adverse Effects of Salicylates

    • Common gastrointestinal issues include epigastric pain, nausea, vomiting, and risk of gastric ulcers.
    • Hepatic effects include mild reversible injury in adults and severe injury, such as Reye's syndrome, in children.
    • Analgesic nephropathy can develop, along with potential water retention and gout exacerbation.
    • Increased bleeding tendency due to drug displacement from plasma proteins and possible hypersensitivity reactions.

    Precautions and Contraindications

    • Use cautiously in patients with gastrointestinal disorders, bleeding disorders, chronic renal and liver disease, uncontrolled hypertension, and those requiring surgery.
    • Aspirin should be discontinued one week before surgery.

    Other NSAIDs

    • Diclofenac: Widely used; less gastric irritant but can impair renal function at high doses. Combined with PGE analogs to decrease ulceration.
    • Sulindac and Ketorolac: Minimal effects on platelet aggregation; ketorolac is a potent analgesic with risks of GIT bleeding.
    • Ibuprofen, Fenoprofen, Ketoprofen: Safe alternative to aspirin for children; long-term use may lead to hypertension.
    • Indomethacin: Strong COX inhibitor; approved to close patent ductus arteriosus in premature infants.
    • Piroxicam: Long half-life; higher likelihood of bleeding and ulceration compared to other NSAIDs.

    Selective COX-2 Inhibitors

    • Include celecoxib, etoricoxib, and meloxicam, which specifically target COX-2 for pain and inflammation.
    • Celecoxib has a potency 30 times greater at inhibiting COX-2 than COX-1, while meloxicam shows slight selectivity for COX-2.

    Selective COX-2 Inhibitors

    • Selective COX-2 inhibitors reduce the risk of peptic ulceration but do not eliminate the risk of renal failure and other adverse effects associated with NSAIDs.
    • Increased risk of cardiovascular accidents, such as myocardial infarction and stroke, arises from elevated TXA2 levels due to COX-1 activity, while COX-2 inhibition decreases PGI2.
    • Rofecoxib (Vioxx®) and valdecoxib were withdrawn from the market in 2004 and 2005 due to concerns over adverse cardiovascular effects.

    Non-selective COX Inhibitors vs. Selective COX-2 Inhibitors

    • Non-selective COX inhibitors inhibit both COX-1 and COX-2; selective inhibitors primarily target COX-2.
    • Both classes exhibit equal analgesic and antipyretic effects.
    • Gastric side effects are more common with non-selective inhibitors, while selective inhibitors show fewer gastric adverse effects.
    • Non-selective inhibitors generally have decreased thrombotic complications, whereas selective COX-2 inhibitors may increase these risks.

    Renal Effects of NSAIDs

    • Analgesic nephropathy from chronic NSAID use can lead to renal failure due to decreased renal blood flow and reduced PGE2 and PGI2 synthesis.
    • Salt and water retention from decreased renal blood flow can antagonize diuretics and β-blockers' effects.
    • Aspirin at low doses can inhibit uric acid excretion, contraindicating its use in gout patients.

    Metabolic Effects and Pregnancy

    • NSAIDs can cause tachycardia and hyperpyrexia at high doses due to oxidative phosphorylation uncoupling.
    • Use of NSAIDs in pregnancy after 20 weeks is discouraged as they can prolong pregnancy and delay labor by inhibiting necessary prostaglandins.

    Therapeutic Uses of Salicylates

    • Effective as analgesics and antipyretics for mild-to-moderate pain but should not be routinely used to lower fever.
    • Functions as anti-inflammatory and anti-rheumatic agents in conditions such as rheumatoid arthritis and rheumatic fever.
    • Salicylic acid provides keratolytic effects for treating warts; methylsalicylic acid serves as a counter-irritant for local pain.

    Adverse Effects of Salicylates

    • Common gastrointestinal issues include epigastric pain, nausea, vomiting, and risk of gastric ulcers.
    • Hepatic effects include mild reversible injury in adults and severe injury, such as Reye's syndrome, in children.
    • Analgesic nephropathy can develop, along with potential water retention and gout exacerbation.
    • Increased bleeding tendency due to drug displacement from plasma proteins and possible hypersensitivity reactions.

    Precautions and Contraindications

    • Use cautiously in patients with gastrointestinal disorders, bleeding disorders, chronic renal and liver disease, uncontrolled hypertension, and those requiring surgery.
    • Aspirin should be discontinued one week before surgery.

    Other NSAIDs

    • Diclofenac: Widely used; less gastric irritant but can impair renal function at high doses. Combined with PGE analogs to decrease ulceration.
    • Sulindac and Ketorolac: Minimal effects on platelet aggregation; ketorolac is a potent analgesic with risks of GIT bleeding.
    • Ibuprofen, Fenoprofen, Ketoprofen: Safe alternative to aspirin for children; long-term use may lead to hypertension.
    • Indomethacin: Strong COX inhibitor; approved to close patent ductus arteriosus in premature infants.
    • Piroxicam: Long half-life; higher likelihood of bleeding and ulceration compared to other NSAIDs.

    Selective COX-2 Inhibitors

    • Include celecoxib, etoricoxib, and meloxicam, which specifically target COX-2 for pain and inflammation.
    • Celecoxib has a potency 30 times greater at inhibiting COX-2 than COX-1, while meloxicam shows slight selectivity for COX-2.

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    Description

    This quiz covers the key differences between selective COX-2 inhibitors and non-selective COX inhibitors, including their effects on gastrointestinal side effects, renal failure, and cardiovascular risks. It also discusses the history of Rofecoxib and valdecoxib and their market withdrawal. Test your understanding of these important pharmacological concepts.

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