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

What effect does aspirin have on plasma urate levels?

<p>Aspirin increases plasma urate levels significantly (A)</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 (D)</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 (B)</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 (B)</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 (A), Increased renal side effects (D)</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 (A)</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 (C), Lower risk of renal side effects (D)</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 (C)</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 (A)</p> Signup and view all the answers

Why were Rofecoxib (Vioxx®) and Valdecoxib withdrawn from the market?

<p>Potential for serious cardiovascular events (C)</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 (A), More frequent renal side effects (C)</p> Signup and view all the answers

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

<p>Severe gastrointestinal bleeding (B)</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 (C)</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. (B)</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. (B)</p> Signup and view all the answers

Which NSAID is known to potentially induce nephrotoxic syndrome?

<p>Fenoprofen (D)</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 (B)</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. (A)</p> Signup and view all the answers

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

<p>Higher incidence of hypertension (A)</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 (D)</p> Signup and view all the answers

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

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

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

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

What effect do salicylates have in relation to blood coagulation?

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

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

<p>7 days before (B)</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 (D)</p> Signup and view all the answers

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

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

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

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

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

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

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

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

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

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

Non-selective COX inhibitors frequently cause renal side effects.

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

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

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

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

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

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

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

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

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

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

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

Methylsalicylic acid is known primarily for its antithrombotic properties.

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

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

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

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

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

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

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

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

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

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

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

Ketorolac has no reported interactions with oral anticoagulants.

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

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

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

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

<p>False (B)</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

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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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