Podcast
Questions and Answers
What is a potential consequence of chronic analgesic abuse on renal function?
What is a potential consequence of chronic analgesic abuse on renal function?
How does aspirin in low doses affect uric acid levels?
How does aspirin in low doses affect uric acid levels?
What metabolic effects are associated with high doses of aspirin?
What metabolic effects are associated with high doses of aspirin?
What are the effects of aspirin on diuretics and β-blockers?
What are the effects of aspirin on diuretics and β-blockers?
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What recommendation is made regarding the use of NSAIDs after 20 weeks of pregnancy?
What recommendation is made regarding the use of NSAIDs after 20 weeks of pregnancy?
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What effect does aspirin have on plasma urate levels?
What effect does aspirin have on plasma urate levels?
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What is a result of prolonged aspirin use related to uterine contractions during labor?
What is a result of prolonged aspirin use related to uterine contractions during labor?
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What is the role of aldosterone concerning renal effects due to analgesics?
What is the role of aldosterone concerning renal effects due to analgesics?
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What primary risk is associated with selective COX-2 inhibitors as opposed to non-selective COX inhibitors?
What primary risk is associated with selective COX-2 inhibitors as opposed to non-selective COX inhibitors?
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Which of the following is a common side effect of non-selective COX inhibitors?
Which of the following is a common side effect of non-selective COX inhibitors?
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What is the mechanism by which non-selective COX inhibitors exert their effects?
What is the mechanism by which non-selective COX inhibitors exert their effects?
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Selective COX-2 inhibitors are characterized by which of the following pharmacological effects compared to non-selective COX inhibitors?
Selective COX-2 inhibitors are characterized by which of the following pharmacological effects compared to non-selective COX inhibitors?
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Which statement accurately reflects the risk profile of COX-2 inhibitors?
Which statement accurately reflects the risk profile of COX-2 inhibitors?
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What is a common outcome of the excessive aggregation of platelets when using selective COX-2 inhibitors?
What is a common outcome of the excessive aggregation of platelets when using selective COX-2 inhibitors?
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Why were Rofecoxib (Vioxx®) and Valdecoxib withdrawn from the market?
Why were Rofecoxib (Vioxx®) and Valdecoxib withdrawn from the market?
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In comparing selective and non-selective COX inhibitors, which side effect is more pronounced in non-selective COX inhibitors?
In comparing selective and non-selective COX inhibitors, which side effect is more pronounced in non-selective COX inhibitors?
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What is a notable side effect of ketorolac when used as an analgesic?
What is a notable side effect of ketorolac when used as an analgesic?
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Which of the following NSAIDs is considered a good alternative to aspirin in treating flu fevers in children?
Which of the following NSAIDs is considered a good alternative to aspirin in treating flu fevers in children?
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Which of the following statements is true regarding sulindac?
Which of the following statements is true regarding sulindac?
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What is a characteristic feature of selective COX-2 inhibitors compared to traditional NSAIDs?
What is a characteristic feature of selective COX-2 inhibitors compared to traditional NSAIDs?
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Which NSAID is known to potentially induce nephrotoxic syndrome?
Which NSAID is known to potentially induce nephrotoxic syndrome?
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What is the primary clinical use of indomethacin?
What is the primary clinical use of indomethacin?
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How does meloxicam compare to other NSAIDs in terms of COX enzyme selectivity?
How does meloxicam compare to other NSAIDs in terms of COX enzyme selectivity?
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What risk is associated with long-term use of ibuprofen in women?
What risk is associated with long-term use of ibuprofen in women?
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Which of the following is a potential adverse effect of salicylates related to the gastrointestinal tract?
Which of the following is a potential adverse effect of salicylates related to the gastrointestinal tract?
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What is the primary risk associated with administering aspirin to children?
What is the primary risk associated with administering aspirin to children?
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Which of the following conditions is NOT a contraindication for the use of aspirin?
Which of the following conditions is NOT a contraindication for the use of aspirin?
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What effect do salicylates have in relation to blood coagulation?
What effect do salicylates have in relation to blood coagulation?
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How does diclofenac differ from other NSAIDs in terms of gastrointestinal effects?
How does diclofenac differ from other NSAIDs in terms of gastrointestinal effects?
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What is a potential consequence of aspirin use in patients with hyperuricemic conditions?
What is a potential consequence of aspirin use in patients with hyperuricemic conditions?
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When should aspirin be stopped prior to surgery to minimize risks?
When should aspirin be stopped prior to surgery to minimize risks?
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What is the primary mechanism of action for salicylic acid in the treatment of warts?
What is the primary mechanism of action for salicylic acid in the treatment of warts?
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Selectivity for COX-2 increases the risk of peptic ulceration and renal failure.
Selectivity for COX-2 increases the risk of peptic ulceration and renal failure.
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Selective COX-2 inhibitors decrease the risk of thrombotic complications.
Selective COX-2 inhibitors decrease the risk of thrombotic complications.
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Rofecoxib and valdecoxib were removed from the market due to their analgesic effectiveness.
Rofecoxib and valdecoxib were removed from the market due to their analgesic effectiveness.
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Both selective and non-selective COX inhibitors have equal analgesic effects.
Both selective and non-selective COX inhibitors have equal analgesic effects.
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TXA2 is formed by COX-2 while PGI2 is formed by COX-1.
TXA2 is formed by COX-2 while PGI2 is formed by COX-1.
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Selective COX-2 inhibitors are linked to fewer hypersensitivity reactions compared to non-selective COX inhibitors.
Selective COX-2 inhibitors are linked to fewer hypersensitivity reactions compared to non-selective COX inhibitors.
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Non-selective COX inhibitors frequently cause renal side effects.
Non-selective COX inhibitors frequently cause renal side effects.
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Selective COX-2 inhibitors increase the risk of cardiovascular accidents.
Selective COX-2 inhibitors increase the risk of cardiovascular accidents.
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Chronic abuse of analgesics can lead to renal failure due to ischemia from decreased renal PGE2 synthesis.
Chronic abuse of analgesics can lead to renal failure due to ischemia from decreased renal PGE2 synthesis.
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High doses of aspirin are known to improve oxidative phosphorylation efficiency in the body.
High doses of aspirin are known to improve oxidative phosphorylation efficiency in the body.
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Aspirin administration in small doses increases uric acid excretion, making it safe for patients with gout.
Aspirin administration in small doses increases uric acid excretion, making it safe for patients with gout.
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The use of NSAIDs is discouraged after 20 weeks of pregnancy due to their effects on uterine contractions.
The use of NSAIDs is discouraged after 20 weeks of pregnancy due to their effects on uterine contractions.
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Aspirin at low doses has a significant effect on plasma urate levels, reducing the risk of hyperuricemia.
Aspirin at low doses has a significant effect on plasma urate levels, reducing the risk of hyperuricemia.
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Salt and water retention due to decreased renal blood flow can antagonize the effects of diuretics.
Salt and water retention due to decreased renal blood flow can antagonize the effects of diuretics.
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Aspirin and other analgesics can enhance the antihypertensive effects of beta-blockers.
Aspirin and other analgesics can enhance the antihypertensive effects of beta-blockers.
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Chronic analgesic nephropathy is a recognized condition resulting from prolonged use of analgesics.
Chronic analgesic nephropathy is a recognized condition resulting from prolonged use of analgesics.
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Salicylic acid is an effective keratolytic agent used primarily for the treatment of warts.
Salicylic acid is an effective keratolytic agent used primarily for the treatment of warts.
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Methylsalicylic acid is known primarily for its antithrombotic properties.
Methylsalicylic acid is known primarily for its antithrombotic properties.
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Adults may experience severe hepatic injury from salicylate use, but it is more common in children due to Reye's syndrome.
Adults may experience severe hepatic injury from salicylate use, but it is more common in children due to Reye's syndrome.
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Chronic renal diseases are not adversely affected by the use of aspirin.
Chronic renal diseases are not adversely affected by the use of aspirin.
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Aspirin should be discontinued at least 7 days before surgery to reduce the risk of bleeding.
Aspirin should be discontinued at least 7 days before surgery to reduce the risk of bleeding.
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Diclofenac is less nephrotoxic than other NSAIDs but is more gastric irritant.
Diclofenac is less nephrotoxic than other NSAIDs but is more gastric irritant.
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Salicylates can increase the tendency to bleed due to displacement of other drugs from plasma proteins.
Salicylates can increase the tendency to bleed due to displacement of other drugs from plasma proteins.
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Using small-to-moderate doses of aspirin can enhance uric acid excretion in patients with gout.
Using small-to-moderate doses of aspirin can enhance uric acid excretion in patients with gout.
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Sulindac is a potent analgesic with minimal effect on platelet aggregation.
Sulindac is a potent analgesic with minimal effect on platelet aggregation.
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Ibuprofen has been shown to have a higher incidence of nephrotoxic syndrome compared to fenoprofen.
Ibuprofen has been shown to have a higher incidence of nephrotoxic syndrome compared to fenoprofen.
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Indomethacin is considered less toxic compared to other NSAIDs and is often approved for use in children.
Indomethacin is considered less toxic compared to other NSAIDs and is often approved for use in children.
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Celecoxib selectively inhibits COX-1 enzyme more effectively than COX-2 enzyme.
Celecoxib selectively inhibits COX-1 enzyme more effectively than COX-2 enzyme.
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Ketorolac has no reported interactions with oral anticoagulants.
Ketorolac has no reported interactions with oral anticoagulants.
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Long-term use of piroxicam is associated with a reduced risk of gastrointestinal bleeding compared to other NSAIDs.
Long-term use of piroxicam is associated with a reduced risk of gastrointestinal bleeding compared to other NSAIDs.
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Long-term use of ibuprofen is linked to an increased incidence of hypertension in men.
Long-term use of ibuprofen is linked to an increased incidence of hypertension in men.
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Meloxicam is considered non-selective when it comes to COX enzyme inhibition.
Meloxicam is considered non-selective when it comes to COX enzyme inhibition.
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What renal condition can result from chronic analgesic abuse?
What renal condition can result from chronic analgesic abuse?
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How does aspirin use affect plasma levels of uric acid?
How does aspirin use affect plasma levels of uric acid?
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What cardiovascular effects can high doses of aspirin induce?
What cardiovascular effects can high doses of aspirin induce?
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What is the consequence of using NSAIDs after 20 weeks of pregnancy?
What is the consequence of using NSAIDs after 20 weeks of pregnancy?
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What role does aldosterone play in renal effects due to analgesic use?
What role does aldosterone play in renal effects due to analgesic use?
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What recommendation is made regarding the use of aspirin in gout patients?
What recommendation is made regarding the use of aspirin in gout patients?
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Why is chronic renal ischemia a concern for patients abusing analgesics?
Why is chronic renal ischemia a concern for patients abusing analgesics?
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What is the primary risk of using selective COX-2 inhibitors?
What is the primary risk of using selective COX-2 inhibitors?
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What adverse effect is associated with long-term use of salicylates in the gastrointestinal tract?
What adverse effect is associated with long-term use of salicylates in the gastrointestinal tract?
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What major risk is associated with the use of aspirin in children?
What major risk is associated with the use of aspirin in children?
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What adverse effect is specifically increased by selective COX-2 inhibitors compared to non-selective COX inhibitors?
What adverse effect is specifically increased by selective COX-2 inhibitors compared to non-selective COX inhibitors?
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In what way can aspirin potentially impact renal function?
In what way can aspirin potentially impact renal function?
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What condition could be exacerbated by the use of small-to-moderate doses of aspirin?
What condition could be exacerbated by the use of small-to-moderate doses of aspirin?
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Why do selective COX-2 inhibitors lead to increased platelet aggregation?
Why do selective COX-2 inhibitors lead to increased platelet aggregation?
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Which COX enzymes are inhibited by non-selective COX inhibitors?
Which COX enzymes are inhibited by non-selective COX inhibitors?
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How does the use of aspirin affect the bleeding tendency?
How does the use of aspirin affect the bleeding tendency?
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What is the primary use of methylsalicylic acid in a clinical context?
What is the primary use of methylsalicylic acid in a clinical context?
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How frequently do selective COX-2 inhibitors cause hypersensitivity reactions compared to non-selective inhibitors?
How frequently do selective COX-2 inhibitors cause hypersensitivity reactions compared to non-selective inhibitors?
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What important precaution should be taken when administering aspirin before surgery?
What important precaution should be taken when administering aspirin before surgery?
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What was one reason for the withdrawal of Rofecoxib and Valdecoxib from the market?
What was one reason for the withdrawal of Rofecoxib and Valdecoxib from the market?
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Explain the impact of selective COX-2 inhibitors on renal side effects.
Explain the impact of selective COX-2 inhibitors on renal side effects.
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Why should diclofenac be used cautiously in patients with renal issues?
Why should diclofenac be used cautiously in patients with renal issues?
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What is the major pharmacological distinction between the analgesic effects of selective and non-selective COX inhibitors?
What is the major pharmacological distinction between the analgesic effects of selective and non-selective COX inhibitors?
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In terms of gastric side effects, how do selective COX-2 inhibitors compare to non-selective inhibitors?
In terms of gastric side effects, how do selective COX-2 inhibitors compare to non-selective inhibitors?
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What distinguishes sulindac as a prodrug in its pharmacological profile?
What distinguishes sulindac as a prodrug in its pharmacological profile?
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What are the main risks associated with the use of ketorolac as an analgesic?
What are the main risks associated with the use of ketorolac as an analgesic?
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How does ibuprofen serve as an alternative treatment for children with flu fevers?
How does ibuprofen serve as an alternative treatment for children with flu fevers?
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Describe the mechanism by which indomethacin facilitates the closure of patent ductus arteriosus in premature infants.
Describe the mechanism by which indomethacin facilitates the closure of patent ductus arteriosus in premature infants.
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In what way does piroxicam's pharmacokinetic profile differ from other NSAIDs?
In what way does piroxicam's pharmacokinetic profile differ from other NSAIDs?
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What unique advantages do selective COX-2 inhibitors offer in treating inflammation and pain?
What unique advantages do selective COX-2 inhibitors offer in treating inflammation and pain?
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What implications does the long-term use of ibuprofen have for women's cardiovascular health?
What implications does the long-term use of ibuprofen have for women's cardiovascular health?
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How does the selectivity of meloxicam towards COX-2 compare to COX-1, and why is this significant?
How does the selectivity of meloxicam towards COX-2 compare to COX-1, and why is this significant?
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Chronic abuse of analgesics can lead to chronic renal ______ due to ischemia.
Chronic abuse of analgesics can lead to chronic renal ______ due to ischemia.
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High doses of aspirin cause coupling of oxidative phosphorylation and can lead to ______ and hyperpyrexia.
High doses of aspirin cause coupling of oxidative phosphorylation and can lead to ______ and hyperpyrexia.
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The use of NSAIDs after 20 weeks of pregnancy is not ______ due to their effects on uterine contractions.
The use of NSAIDs after 20 weeks of pregnancy is not ______ due to their effects on uterine contractions.
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Low doses of aspirin are not thought to have a significant effect on plasma ______ levels.
Low doses of aspirin are not thought to have a significant effect on plasma ______ levels.
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Salt and water retention occurs due to decreased renal ______ flow.
Salt and water retention occurs due to decreased renal ______ flow.
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Small-to-moderate doses of aspirin can decrease uric acid ______ and thus may be contraindicated in gout.
Small-to-moderate doses of aspirin can decrease uric acid ______ and thus may be contraindicated in gout.
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Aspirin can ______ the diuretic effect of diuretics due to decreased renal function.
Aspirin can ______ the diuretic effect of diuretics due to decreased renal function.
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Prolongation of pregnancy and delay of labor occurs due to inhibition of PGs necessary for uterine ______.
Prolongation of pregnancy and delay of labor occurs due to inhibition of PGs necessary for uterine ______.
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Sulindac is known as a ______ and has a long half-life.
Sulindac is known as a ______ and has a long half-life.
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Ketorolac is a potent analgesic but it can cause severe ______ bleeding.
Ketorolac is a potent analgesic but it can cause severe ______ bleeding.
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Fenoprofen has been reported to induce ______ syndrome.
Fenoprofen has been reported to induce ______ syndrome.
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Long-term use of ibuprofen is associated with an increased incidence of ______ in women.
Long-term use of ibuprofen is associated with an increased incidence of ______ in women.
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Indomethacin is a very potent ______ inhibitor.
Indomethacin is a very potent ______ inhibitor.
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Piroxicam has a long half-life, approximately ______ hours.
Piroxicam has a long half-life, approximately ______ hours.
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Celecoxib is approximately 30 times more potent at inhibiting COX-2 than COX-______.
Celecoxib is approximately 30 times more potent at inhibiting COX-2 than COX-______.
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Selective COX-2 inhibitors are newer forms of NSAIDs that directly target the ______ enzyme responsible for pain.
Selective COX-2 inhibitors are newer forms of NSAIDs that directly target the ______ enzyme responsible for pain.
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Salicylic acid is used for the treatment of ______.
Salicylic acid is used for the treatment of ______.
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A dose of 150 mg/day of Diclofenac can impair renal blood flow and ______.
A dose of 150 mg/day of Diclofenac can impair renal blood flow and ______.
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Reye's syndrome is a severe hepatic injury that can occur in ______.
Reye's syndrome is a severe hepatic injury that can occur in ______.
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Aspirin must be stopped at least 7 days before ______.
Aspirin must be stopped at least 7 days before ______.
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Methylsalicylic acid is used as a counter-irritant for local ______ pain.
Methylsalicylic acid is used as a counter-irritant for local ______ pain.
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Chronic renal diseases may be aggravated by the use of ______.
Chronic renal diseases may be aggravated by the use of ______.
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Salicylates can increase the bleeding tendency due to displacement of other drugs from ______ proteins.
Salicylates can increase the bleeding tendency due to displacement of other drugs from ______ proteins.
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The use of NSAIDs is discouraged after 20 weeks of ______.
The use of NSAIDs is discouraged after 20 weeks of ______.
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Selective COX-2 inhibitors may also increase the risk of cardiovascular ______.
Selective COX-2 inhibitors may also increase the risk of cardiovascular ______.
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Rofecoxib and valdecoxib were withdrawn from the market due to potential adverse ______.
Rofecoxib and valdecoxib were withdrawn from the market due to potential adverse ______.
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The mechanism of selective COX-2 inhibitors focuses on inhibiting the COX-2 ______ enzyme.
The mechanism of selective COX-2 inhibitors focuses on inhibiting the COX-2 ______ enzyme.
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Non-selective COX inhibitors frequently cause ______ side effects.
Non-selective COX inhibitors frequently cause ______ side effects.
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TXA2 is formed by COX-1, whereas PGI2 is formed by COX-______.
TXA2 is formed by COX-1, whereas PGI2 is formed by COX-______.
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Both selective and non-selective COX inhibitors have equal ______ and antipyretic effects.
Both selective and non-selective COX inhibitors have equal ______ and antipyretic effects.
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High doses of selective COX-2 inhibitors can potentially lead to increased ______ complications.
High doses of selective COX-2 inhibitors can potentially lead to increased ______ complications.
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Hypersensitivity reactions are reported to be ______ frequent with selective COX-2 inhibitors.
Hypersensitivity reactions are reported to be ______ frequent with selective COX-2 inhibitors.
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Match the following COX inhibitors with their side effect profiles:
Match the following COX inhibitors with their side effect profiles:
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Match the following COX enzymes with their effects:
Match the following COX enzymes with their effects:
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Match the following reasons for withdrawal of COX inhibitors with the respective drugs:
Match the following reasons for withdrawal of COX inhibitors with the respective drugs:
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Match the following side effects with their corresponding COX inhibitor types:
Match the following side effects with their corresponding COX inhibitor types:
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Match the following classes of COX inhibitors with their pharmacological effects:
Match the following classes of COX inhibitors with their pharmacological effects:
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Match the following side effects with the frequency seen in different COX inhibitors:
Match the following side effects with the frequency seen in different COX inhibitors:
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Match the following health conditions with their associated COX inhibitors:
Match the following health conditions with their associated COX inhibitors:
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Match the following terms with their correct definitions regarding COX inhibitors:
Match the following terms with their correct definitions regarding COX inhibitors:
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Match the following adverse effects with their corresponding causes:
Match the following adverse effects with their corresponding causes:
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Match the following NSAIDs with their notable properties:
Match the following NSAIDs with their notable properties:
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Match the following contraindications with their related conditions:
Match the following contraindications with their related conditions:
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Match the following NSAID mechanisms with their clinical usage:
Match the following NSAID mechanisms with their clinical usage:
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Match the following patient conditions with their precautions when using NSAIDs:
Match the following patient conditions with their precautions when using NSAIDs:
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Match the following NSAID effects with their respective systems:
Match the following NSAID effects with their respective systems:
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Match the following drugs with their effects on renal function:
Match the following drugs with their effects on renal function:
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Match the following NSAID-related terms with their descriptions:
Match the following NSAID-related terms with their descriptions:
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Match the following NSAIDs with their primary characteristics:
Match the following NSAIDs with their primary characteristics:
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Match each NSAID with its specific risk or effect:
Match each NSAID with its specific risk or effect:
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Match the following characteristics with the appropriate selective COX-2 inhibitors:
Match the following characteristics with the appropriate selective COX-2 inhibitors:
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Match each NSAID with its usage details:
Match each NSAID with its usage details:
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Match the following NSAIDs to their common side effects:
Match the following NSAIDs to their common side effects:
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Match the following long-term effects of NSAIDs with the corresponding drugs:
Match the following long-term effects of NSAIDs with the corresponding drugs:
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Match the following NSAIDs with their specific use and response:
Match the following NSAIDs with their specific use and response:
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Match the following statements with the appropriate NSAIDs:
Match the following statements with the appropriate NSAIDs:
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Match the following renal effects of analgesics with their corresponding descriptions:
Match the following renal effects of analgesics with their corresponding descriptions:
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Match the effects of high doses of aspirin with their outcomes:
Match the effects of high doses of aspirin with their outcomes:
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Match the therapeutic uses of salicylates with their indications:
Match the therapeutic uses of salicylates with their indications:
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Match the pharmacological actions related to aspirin with their effects:
Match the pharmacological actions related to aspirin with their effects:
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Match the conditions related to pregnant women’s use of NSAIDs with their recommendations:
Match the conditions related to pregnant women’s use of NSAIDs with their recommendations:
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Match these side effects of aspirin with their associated metabolic effects:
Match these side effects of aspirin with their associated metabolic effects:
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Match the following terms with their correct definitions related to analgesics:
Match the following terms with their correct definitions related to analgesics:
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Match the statements regarding aspirin with their implications:
Match the statements regarding aspirin with their implications:
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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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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.