Podcast
Questions and Answers
What is the primary site of elimination for NSAIDs?
What is the primary site of elimination for NSAIDs?
What is the minimum duration of activity for naproxen sodium?
What is the minimum duration of activity for naproxen sodium?
Which of the following increases the chance of severe stomach bleeding when taking NSAIDs?
Which of the following increases the chance of severe stomach bleeding when taking NSAIDs?
What can be taken with NSAIDs to alleviate stomach upset?
What can be taken with NSAIDs to alleviate stomach upset?
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What is a common adverse effect of NSAIDs, especially in children?
What is a common adverse effect of NSAIDs, especially in children?
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Which of the following medications may increase the risk of stomach bleeding when taken with NSAIDs?
Which of the following medications may increase the risk of stomach bleeding when taken with NSAIDs?
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What should be done with enteric coated or sustained release NSAID preparations?
What should be done with enteric coated or sustained release NSAID preparations?
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What is the mechanism of pain relief for NSAIDs?
What is the mechanism of pain relief for NSAIDs?
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What is the effect of ibuprofen on cardiovascular risk?
What is the effect of ibuprofen on cardiovascular risk?
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Which NSAID is considered the preferred, safer option?
Which NSAID is considered the preferred, safer option?
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What is the mechanism of action of salicylates?
What is the mechanism of action of salicylates?
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How does urinary pH affect the elimination of salicylic acid?
How does urinary pH affect the elimination of salicylic acid?
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What is the potential interaction between NSAIDs and bisphosphonates?
What is the potential interaction between NSAIDs and bisphosphonates?
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Why should aspirin be taken at least 30 minutes before or 8 hours after ibuprofen?
Why should aspirin be taken at least 30 minutes before or 8 hours after ibuprofen?
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What is the maximum analgesic dosage for self-medication with aspirin?
What is the maximum analgesic dosage for self-medication with aspirin?
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What is the indication of aspirin for high-risk patients?
What is the indication of aspirin for high-risk patients?
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What is the potential interaction between NSAIDs and digoxin?
What is the potential interaction between NSAIDs and digoxin?
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How does salicylic acid bind to albumin?
How does salicylic acid bind to albumin?
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Why should caution be exercised when using NSAIDs with antihypertensive agents?
Why should caution be exercised when using NSAIDs with antihypertensive agents?
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What is the potential interaction between NSAIDs and anticoagulants?
What is the potential interaction between NSAIDs and anticoagulants?
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What is the effect of salicylates on pain receptors?
What is the effect of salicylates on pain receptors?
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What is the recommended alternative to ibuprofen when taking aspirin?
What is the recommended alternative to ibuprofen when taking aspirin?
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What is the potential consequence of concurrent use of NSAIDs and bisphosphonates?
What is the potential consequence of concurrent use of NSAIDs and bisphosphonates?
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What should be monitored when using NSAIDs with digoxin?
What should be monitored when using NSAIDs with digoxin?
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NSAIDs are contraindicated in patients with glucose-6-phosphate dehydrogenase deficiency.
NSAIDs are contraindicated in patients with glucose-6-phosphate dehydrogenase deficiency.
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The combination of NSAIDs and bisphosphonates increases the risk of gastrointestinal ulcers.
The combination of NSAIDs and bisphosphonates increases the risk of gastrointestinal ulcers.
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Taking NSAIDs with antacids can reduce stomach upset.
Taking NSAIDs with antacids can reduce stomach upset.
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Concurrent use of NSAIDs and alcohol does not increase the risk of gastrointestinal bleeding.
Concurrent use of NSAIDs and alcohol does not increase the risk of gastrointestinal bleeding.
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The risk of severe stomach bleeding when taking NSAIDs is higher for people who have had stomach ulcers or bleeding problems.
The risk of severe stomach bleeding when taking NSAIDs is higher for people who have had stomach ulcers or bleeding problems.
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NSAIDs can be taken with bisphosphonates without any risk of interaction.
NSAIDs can be taken with bisphosphonates without any risk of interaction.
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NSAIDs decrease the efficacy of digoxin.
NSAIDs decrease the efficacy of digoxin.
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The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink 3 or more alcoholic drinks every day.
The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink 3 or more alcoholic drinks every day.
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The concurrent use of NSAIDs and antihypertensive agents can reduce the efficacy of antihypertensive agents.
The concurrent use of NSAIDs and antihypertensive agents can reduce the efficacy of antihypertensive agents.
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NSAIDs can increase the risk of digoxin toxicity.
NSAIDs can increase the risk of digoxin toxicity.
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The concurrent use of NSAIDs and anticoagulants does not increase the risk of bleeding.
The concurrent use of NSAIDs and anticoagulants does not increase the risk of bleeding.
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Caution should be exercised when using NSAIDs with antihypertensive agents due to the potential for decreased blood pressure control.
Caution should be exercised when using NSAIDs with antihypertensive agents due to the potential for decreased blood pressure control.
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NSAIDs can reduce the risk of myocardial infarction and stroke.
NSAIDs can reduce the risk of myocardial infarction and stroke.
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NSAIDs can increase the risk of bleeding when taken with anticoagulants.
NSAIDs can increase the risk of bleeding when taken with anticoagulants.
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Salicylates are not effective in treating mild to moderate pain from musculoskeletal conditions.
Salicylates are not effective in treating mild to moderate pain from musculoskeletal conditions.
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Aspirin is not indicated for the prevention of thromboembolic events in high-risk patients.
Aspirin is not indicated for the prevention of thromboembolic events in high-risk patients.
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Concomitant use of NSAIDs and bisphosphonates increases the risk of gastrointestinal ulceration.
Concomitant use of NSAIDs and bisphosphonates increases the risk of gastrointestinal ulceration.
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Acetaminophen is not a recommended alternative to ibuprofen when taking aspirin.
Acetaminophen is not a recommended alternative to ibuprofen when taking aspirin.
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Monitoring of free phenytoin levels is not necessary when using ibuprofen concomitantly.
Monitoring of free phenytoin levels is not necessary when using ibuprofen concomitantly.
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The renal clearance of digoxin is increased by NSAIDs.
The renal clearance of digoxin is increased by NSAIDs.
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Aspirin should be taken at least 30 minutes before or 2 hours after ibuprofen.
Aspirin should be taken at least 30 minutes before or 2 hours after ibuprofen.
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NSAIDs do not interact with antihypertensive agents.
NSAIDs do not interact with antihypertensive agents.
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The interaction between NSAIDs and anticoagulants is not clinically significant.
The interaction between NSAIDs and anticoagulants is not clinically significant.
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NSAIDs do not increase the risk of gastrointestinal bleeding when used with alcohol.
NSAIDs do not increase the risk of gastrointestinal bleeding when used with alcohol.
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What is the potential interaction between NSAIDs and bisphosphonates?
What is the potential interaction between NSAIDs and bisphosphonates?
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What is the potential consequence of concurrent use of NSAIDs and antihypertensive agents?
What is the potential consequence of concurrent use of NSAIDs and antihypertensive agents?
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What is the effect of NSAIDs on digoxin?
What is the effect of NSAIDs on digoxin?
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What is the potential interaction between NSAIDs and anticoagulants?
What is the potential interaction between NSAIDs and anticoagulants?
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What is the potential consequence of concurrent use of NSAIDs and alcohol?
What is the potential consequence of concurrent use of NSAIDs and alcohol?
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What is the potential interaction between acetaminophen and warfarin?
What is the potential interaction between acetaminophen and warfarin?
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What is the potential interaction between acetaminophen and alcohol?
What is the potential interaction between acetaminophen and alcohol?
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What is the potential interaction between aspirin and valproic acid?
What is the potential interaction between aspirin and valproic acid?
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What is the cardiovascular risk associated with nonselective NSAIDs, and how does it vary?
What is the cardiovascular risk associated with nonselective NSAIDs, and how does it vary?
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Why is naproxen considered the preferred, safer option compared to ibuprofen?
Why is naproxen considered the preferred, safer option compared to ibuprofen?
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What is the effect of salicylates on pain receptors, and how do they reduce pain?
What is the effect of salicylates on pain receptors, and how do they reduce pain?
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What is the potential interaction between NSAIDs and antihypertensive agents, and why is caution necessary?
What is the potential interaction between NSAIDs and antihypertensive agents, and why is caution necessary?
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How do NSAIDs interact with digoxin, and what should be monitored?
How do NSAIDs interact with digoxin, and what should be monitored?
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What is the effect of concurrent use of NSAIDs and anticoagulants, and what is the risk?
What is the effect of concurrent use of NSAIDs and anticoagulants, and what is the risk?
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What is the effect of concurrent use of NSAIDs and bisphosphonates, and what is the risk?
What is the effect of concurrent use of NSAIDs and bisphosphonates, and what is the risk?
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What is the effect of concurrent use of NSAIDs and alcohol, and what is the risk?
What is the effect of concurrent use of NSAIDs and alcohol, and what is the risk?
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What is the primary mechanism of action for NSAIDs in relieving pain?
What is the primary mechanism of action for NSAIDs in relieving pain?
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What is the potential consequence of concurrent use of NSAIDs and bisphosphonates?
What is the potential consequence of concurrent use of NSAIDs and bisphosphonates?
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How do NSAIDs interact with antihypertensive agents?
How do NSAIDs interact with antihypertensive agents?
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What is the effect of NSAIDs on digoxin levels?
What is the effect of NSAIDs on digoxin levels?
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How do NSAIDs interact with anticoagulants?
How do NSAIDs interact with anticoagulants?
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What is the effect of concurrent use of NSAIDs and alcohol on the risk of gastrointestinal bleeding?
What is the effect of concurrent use of NSAIDs and alcohol on the risk of gastrointestinal bleeding?
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What is the potential interaction between NSAIDs and antihypertensive agents?
What is the potential interaction between NSAIDs and antihypertensive agents?
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What is the effect of NSAIDs on the risk of gastrointestinal bleeding?
What is the effect of NSAIDs on the risk of gastrointestinal bleeding?
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Acetaminophen is potentially _______________________ in doses exceeding 4 g/day, especially with chronic use.
Acetaminophen is potentially _______________________ in doses exceeding 4 g/day, especially with chronic use.
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NSAIDs relieve pain through central and peripheral inhibition of _______________________ and subsequent inhibition of prostaglandin synthesis.
NSAIDs relieve pain through central and peripheral inhibition of _______________________ and subsequent inhibition of prostaglandin synthesis.
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The combination of NSAIDs and _______________________ increases the risk of gastrointestinal ulcers.
The combination of NSAIDs and _______________________ increases the risk of gastrointestinal ulcers.
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Concurrent use of NSAIDs and _______________________ can reduce the efficacy of antihypertensive agents.
Concurrent use of NSAIDs and _______________________ can reduce the efficacy of antihypertensive agents.
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NSAIDs can increase the risk of _______________________ when taken with anticoagulants.
NSAIDs can increase the risk of _______________________ when taken with anticoagulants.
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The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink 3 or more _______________________ drinks every day.
The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink 3 or more _______________________ drinks every day.
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NSAIDs may cause severe _______________________ bleeding.
NSAIDs may cause severe _______________________ bleeding.
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The chance of severe stomach bleeding is higher if you are age 60 or _______________________.
The chance of severe stomach bleeding is higher if you are age 60 or _______________________.
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The cardiovascular risk of nonselective ______ is depend on dose and duration.
The cardiovascular risk of nonselective ______ is depend on dose and duration.
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______ is considered the preferred, safer option among NSAIDs.
______ is considered the preferred, safer option among NSAIDs.
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The concurrent use of NSAIDs and ______ increases the risk of gastrointestinal ulcers.
The concurrent use of NSAIDs and ______ increases the risk of gastrointestinal ulcers.
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NSAIDs can ______ the risk of digoxin toxicity.
NSAIDs can ______ the risk of digoxin toxicity.
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Salicylates are absorbed by passive diffusion of the non-ionized drug in the ______ and small intestine.
Salicylates are absorbed by passive diffusion of the non-ionized drug in the ______ and small intestine.
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The concurrent use of NSAIDs and ______ agents can reduce the efficacy of antihypertensive agents.
The concurrent use of NSAIDs and ______ agents can reduce the efficacy of antihypertensive agents.
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The concurrent use of NSAIDs and ______ can reduce the efficacy of antihypertensive agents.
The concurrent use of NSAIDs and ______ can reduce the efficacy of antihypertensive agents.
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NSAIDs can increase the risk of ______ when taken with anticoagulants.
NSAIDs can increase the risk of ______ when taken with anticoagulants.
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NSAIDs can ______ the risk of bleeding when taken with anticoagulants.
NSAIDs can ______ the risk of bleeding when taken with anticoagulants.
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The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink ______ or more alcoholic drinks every day.
The risk of severe stomach bleeding when taking NSAIDs is higher for people who drink ______ or more alcoholic drinks every day.
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The risk of severe stomach bleeding when taking NSAIDs is higher for people who ______ 3 or more alcoholic drinks every day.
The risk of severe stomach bleeding when taking NSAIDs is higher for people who ______ 3 or more alcoholic drinks every day.
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NSAIDs can increase the risk of ______ toxicity when taken with digoxin.
NSAIDs can increase the risk of ______ toxicity when taken with digoxin.
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Concurrent use of NSAIDs and ______ does not increase the risk of gastrointestinal bleeding.
Concurrent use of NSAIDs and ______ does not increase the risk of gastrointestinal bleeding.
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Acetaminophen is recommended to minimize ______ intake when using acetaminophen.
Acetaminophen is recommended to minimize ______ intake when using acetaminophen.
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The concurrent use of NSAIDs and ______ increases the risk of gastrointestinal ulceration.
The concurrent use of NSAIDs and ______ increases the risk of gastrointestinal ulceration.
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The concurrent use of aspirin and ______ increases the risk of hepatotoxicity.
The concurrent use of aspirin and ______ increases the risk of hepatotoxicity.
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Match the following NSAID interactions with their potential consequences:
Match the following NSAID interactions with their potential consequences:
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Match the following NSAID combinations with their effects:
Match the following NSAID combinations with their effects:
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Match the following NSAID interactions with their risks:
Match the following NSAID interactions with their risks:
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Match the following NSAID effects with their consequences:
Match the following NSAID effects with their consequences:
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Match the following NSAID properties with their characteristics:
Match the following NSAID properties with their characteristics:
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Match the following NSAID interactions with their management:
Match the following NSAID interactions with their management:
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Match the following NSAID effects with their indications:
Match the following NSAID effects with their indications:
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Match the following NSAID interactions with their importance:
Match the following NSAID interactions with their importance:
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Match the following statements with the correct effect of NSAIDs on other medications:
Match the following statements with the correct effect of NSAIDs on other medications:
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Match the following statements with the correct interaction between NSAIDs and other substances:
Match the following statements with the correct interaction between NSAIDs and other substances:
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Match the following statements with the correct effect of NSAIDs on gastrointestinal health:
Match the following statements with the correct effect of NSAIDs on gastrointestinal health:
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Match the following statements with the correct effect of NSAIDs on cardiovascular health:
Match the following statements with the correct effect of NSAIDs on cardiovascular health:
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Match the following statements with the correct effect of NSAIDs on other medications:
Match the following statements with the correct effect of NSAIDs on other medications:
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Match the following statements with the correct effect of NSAIDs on gastrointestinal health:
Match the following statements with the correct effect of NSAIDs on gastrointestinal health:
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Match the following statements with the correct interaction between NSAIDs and other substances:
Match the following statements with the correct interaction between NSAIDs and other substances:
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Match the following statements with the correct effect of NSAIDs on cardiovascular health:
Match the following statements with the correct effect of NSAIDs on cardiovascular health:
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Match the following drug interactions with their potential effects:
Match the following drug interactions with their potential effects:
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Match the following drug interactions with their potential effects:
Match the following drug interactions with their potential effects:
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Match the following drug interactions with their management/preventive measures:
Match the following drug interactions with their management/preventive measures:
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Match the following drug interactions with their potential effects:
Match the following drug interactions with their potential effects:
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Match the following drug interactions with their potential effects:
Match the following drug interactions with their potential effects:
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Match the following drug interactions with their management/preventive measures:
Match the following drug interactions with their management/preventive measures:
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Match the following drug interactions with their potential effects:
Match the following drug interactions with their potential effects:
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Match the following drug interactions with their potential effects:
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Study Notes
Acetaminophen
- Potentially hepatotoxic in doses exceeding 4 g/day, especially with chronic use
- Patients with glucose-6-phosphate dehydrogenase deficiency should use caution when taking acetaminophen
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- Relieve pain through central and peripheral inhibition of cyclooxygenase (COX) and subsequent inhibition of prostaglandin synthesis
- Rapidly absorbed from the GI tract with high bioavailability
- Extensively metabolized, mainly by glucuronidation, to inactive compounds in the liver
- Elimination occurs primarily through the kidneys
- Onset of activity for naproxen sodium and standard ibuprofen is about 30 minutes
- Duration of activity for naproxen sodium is up to 12 hours and 6-8 hours for ibuprofen
- Analgesic, antipyretic, and anti-inflammatory activity
- Useful in managing mild moderate pain of non-visceral origin
Adverse Effects of NSAIDs
- Most frequent adverse effects involve the GI tract and include dyspepsia, heartburn, nausea, anorexia, and epigastric pain
- Increased risk of severe stomach bleeding, especially in:
- Those aged 60 or older
- Those with a history of stomach ulcers or bleeding problems
- Those taking blood thinning (anticoagulant) or steroid drugs
- Those taking other drugs containing prescription or nonprescription NSAIDs
- Those who consume 3 or more alcoholic drinks daily
- Those who take more or for a longer time than directed
Cardiovascular Risk of NSAIDs
- Associated with increased risk for myocardial infarction, heart failure, hypertension, and stroke
- Cardiovascular risk depends on dose and duration
- Ibuprofen has been associated with a significant increase in cardiovascular risk, whereas naproxen has not
Salicylates
- Inhibit prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme (COX1 and COX2)
- Reduce the sensitivity of pain receptors to the initiation of pain impulses at sites of inflammation and trauma
- Absorbed by passive diffusion of the non-ionized drug in the stomach and small intestine
- Factors affecting absorption include dosage form, gastric pH, gastric emptying time, dissolution rate, and the presence of antacids or food
Pharmacokinetics of Salicylates
- Protein binding is concentration dependent
- At concentrations lower than 100 mg/mL, approximately 90% of salicylic acid is bound to albumin
- At concentrations greater than 400 mg/mL, approximately 75% is bound
- Salicylic acid is largely eliminated through the kidney
- Urine pH determines the amount of unchanged drug that is eliminated
Therapeutic Uses of Salicylates
- Effective in treating mild moderate pain from musculoskeletal conditions and fever
- Indicated for prevention of thromboembolic events (e.g., myocardial infarction and stroke) in high-risk patients
Clinically Important Drug-Drug Interactions
- Ibuprofen decreases the antiplatelet effect of aspirin
- Ibuprofen displaces phenytoin from protein binding sites
- NSAIDs increase the risk of GI or esophageal ulceration with bisphosphonates
- NSAIDs inhibit the renal clearance of digoxin
Acetaminophen
- Potentially hepatotoxic in doses exceeding 4 g/day, especially with chronic use
- Patients with glucose-6-phosphate dehydrogenase deficiency should use caution when taking acetaminophen
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- Relieve pain through central and peripheral inhibition of cyclooxygenase (COX) and subsequent inhibition of prostaglandin synthesis
- Rapidly absorbed from the GI tract with high bioavailability
- Extensively metabolized, mainly by glucuronidation, to inactive compounds in the liver
- Elimination occurs primarily through the kidneys
- Onset of activity for naproxen sodium and standard ibuprofen is about 30 minutes
- Duration of activity for naproxen sodium is up to 12 hours and 6-8 hours for ibuprofen
- Analgesic, antipyretic, and anti-inflammatory activity
- Useful in managing mild moderate pain of non-visceral origin
Adverse Effects of NSAIDs
- Most frequent adverse effects involve the GI tract and include dyspepsia, heartburn, nausea, anorexia, and epigastric pain
- Increased risk of severe stomach bleeding, especially in:
- Those aged 60 or older
- Those with a history of stomach ulcers or bleeding problems
- Those taking blood thinning (anticoagulant) or steroid drugs
- Those taking other drugs containing prescription or nonprescription NSAIDs
- Those who consume 3 or more alcoholic drinks daily
- Those who take more or for a longer time than directed
Cardiovascular Risk of NSAIDs
- Associated with increased risk for myocardial infarction, heart failure, hypertension, and stroke
- Cardiovascular risk depends on dose and duration
- Ibuprofen has been associated with a significant increase in cardiovascular risk, whereas naproxen has not
Salicylates
- Inhibit prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme (COX1 and COX2)
- Reduce the sensitivity of pain receptors to the initiation of pain impulses at sites of inflammation and trauma
- Absorbed by passive diffusion of the non-ionized drug in the stomach and small intestine
- Factors affecting absorption include dosage form, gastric pH, gastric emptying time, dissolution rate, and the presence of antacids or food
Pharmacokinetics of Salicylates
- Protein binding is concentration dependent
- At concentrations lower than 100 mg/mL, approximately 90% of salicylic acid is bound to albumin
- At concentrations greater than 400 mg/mL, approximately 75% is bound
- Salicylic acid is largely eliminated through the kidney
- Urine pH determines the amount of unchanged drug that is eliminated
Therapeutic Uses of Salicylates
- Effective in treating mild moderate pain from musculoskeletal conditions and fever
- Indicated for prevention of thromboembolic events (e.g., myocardial infarction and stroke) in high-risk patients
Clinically Important Drug-Drug Interactions
- Ibuprofen decreases the antiplatelet effect of aspirin
- Ibuprofen displaces phenytoin from protein binding sites
- NSAIDs increase the risk of GI or esophageal ulceration with bisphosphonates
- NSAIDs inhibit the renal clearance of digoxin
Acetaminophen
- Can be hepatotoxic in doses exceeding 4 g/day, especially with chronic use.
- Patients with glucose-6-phosphate dehydrogenase deficiency should use caution when taking acetaminophen.
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- Relieve pain through central and peripheral inhibition of cyclooxygenase (COX) and subsequent inhibition of prostaglandin synthesis.
- Are rapidly absorbed from the GI tract with high bioavailability.
- Are extensively metabolized, mainly by glucuronidation, to inactive compounds in the liver.
- Are eliminated primarily through the kidneys.
- Have analgesic, antipyretic, and anti-inflammatory activity.
- Are useful in managing mild to moderate pain of non-visceral origin.
NSAIDs Adverse Effects
- Most frequent adverse effects involve the GI tract and include dyspepsia, heartburn, nausea, anorexia, and epigastric pain.
- May be taken with food, milk, or antacids if upset stomach occurs.
- Can cause severe stomach bleeding, especially in:
- Patients aged 60 or older.
- Those with a history of stomach ulcers or bleeding problems.
- Those taking blood thinning or steroid drugs.
- Those taking other drugs containing NSAIDs.
- Those who consume 3 or more alcoholic drinks daily.
NSAIDs Cardiovascular Risk
- Are associated with increased risk of myocardial infarction, heart failure, hypertension, and stroke.
- Cardiovascular risk depends on dose and duration.
- Ibuprofen is associated with a significant increase in cardiovascular risk, while naproxen is considered the preferred, safer option.
Salicylates
- Inhibit prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme.
- Reduce the sensitivity of pain receptors to the initiation of pain impulses at sites of inflammation and trauma.
- Are absorbed by passive diffusion of the non-ionized drug in the stomach and small intestine.
- Are effective in treating mild to moderate pain from musculoskeletal conditions and fever.
Salicylates Pharmacokinetics
- Protein binding is concentration dependent.
- Are largely eliminated through the kidney.
- Urine pH determines the amount of unchanged drug that is eliminated.
Salicylates Clinical Use
- Aspirin is also indicated for prevention of thromboembolic events (e.g., myocardial infarction and stroke) in high-risk patients.
- The maximum analgesic dosage for self-medication with aspirin is 4 g/day.
Clinically Important Drug-Drug Interactions
- Acetaminophen and alcohol: avoid concurrent use if possible; minimize alcohol intake when using acetaminophen.
- Acetaminophen and warfarin: monitor INR for several weeks when acetaminophen is added or discontinued in patients on warfarin.
- Aspirin and valproic acid: avoid concurrent use; use naproxen instead of aspirin.
- Aspirin and NSAIDs: avoid concurrent use if possible; consider use of gastroprotective agents (e.g., PPIs).
Acetaminophen
- Can be hepatotoxic in doses exceeding 4 g/day, especially with chronic use.
- Patients with glucose-6-phosphate dehydrogenase deficiency should use caution when taking acetaminophen.
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- Relieve pain through central and peripheral inhibition of cyclooxygenase (COX) and subsequent inhibition of prostaglandin synthesis.
- Are rapidly absorbed from the GI tract with high bioavailability.
- Are extensively metabolized, mainly by glucuronidation, to inactive compounds in the liver.
- Are eliminated primarily through the kidneys.
- Have analgesic, antipyretic, and anti-inflammatory activity.
- Are useful in managing mild to moderate pain of non-visceral origin.
NSAIDs Adverse Effects
- Most frequent adverse effects involve the GI tract and include dyspepsia, heartburn, nausea, anorexia, and epigastric pain.
- May be taken with food, milk, or antacids if upset stomach occurs.
- Can cause severe stomach bleeding, especially in:
- Patients aged 60 or older.
- Those with a history of stomach ulcers or bleeding problems.
- Those taking blood thinning or steroid drugs.
- Those taking other drugs containing NSAIDs.
- Those who consume 3 or more alcoholic drinks daily.
NSAIDs Cardiovascular Risk
- Are associated with increased risk of myocardial infarction, heart failure, hypertension, and stroke.
- Cardiovascular risk depends on dose and duration.
- Ibuprofen is associated with a significant increase in cardiovascular risk, while naproxen is considered the preferred, safer option.
Salicylates
- Inhibit prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme.
- Reduce the sensitivity of pain receptors to the initiation of pain impulses at sites of inflammation and trauma.
- Are absorbed by passive diffusion of the non-ionized drug in the stomach and small intestine.
- Are effective in treating mild to moderate pain from musculoskeletal conditions and fever.
Salicylates Pharmacokinetics
- Protein binding is concentration dependent.
- Are largely eliminated through the kidney.
- Urine pH determines the amount of unchanged drug that is eliminated.
Salicylates Clinical Use
- Aspirin is also indicated for prevention of thromboembolic events (e.g., myocardial infarction and stroke) in high-risk patients.
- The maximum analgesic dosage for self-medication with aspirin is 4 g/day.
Clinically Important Drug-Drug Interactions
- Acetaminophen and alcohol: avoid concurrent use if possible; minimize alcohol intake when using acetaminophen.
- Acetaminophen and warfarin: monitor INR for several weeks when acetaminophen is added or discontinued in patients on warfarin.
- Aspirin and valproic acid: avoid concurrent use; use naproxen instead of aspirin.
- Aspirin and NSAIDs: avoid concurrent use if possible; consider use of gastroprotective agents (e.g., PPIs).
Acetaminophen
- Can be hepatotoxic in doses exceeding 4 g/day, especially with chronic use.
- Patients with glucose-6-phosphate dehydrogenase deficiency should use caution when taking acetaminophen.
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- Relieve pain through central and peripheral inhibition of cyclooxygenase (COX) and subsequent inhibition of prostaglandin synthesis.
- Are rapidly absorbed from the GI tract with high bioavailability.
- Are extensively metabolized, mainly by glucuronidation, to inactive compounds in the liver.
- Are eliminated primarily through the kidneys.
- Have analgesic, antipyretic, and anti-inflammatory activity.
- Are useful in managing mild to moderate pain of non-visceral origin.
NSAIDs Adverse Effects
- Most frequent adverse effects involve the GI tract and include dyspepsia, heartburn, nausea, anorexia, and epigastric pain.
- May be taken with food, milk, or antacids if upset stomach occurs.
- Can cause severe stomach bleeding, especially in:
- Patients aged 60 or older.
- Those with a history of stomach ulcers or bleeding problems.
- Those taking blood thinning or steroid drugs.
- Those taking other drugs containing NSAIDs.
- Those who consume 3 or more alcoholic drinks daily.
NSAIDs Cardiovascular Risk
- Are associated with increased risk of myocardial infarction, heart failure, hypertension, and stroke.
- Cardiovascular risk depends on dose and duration.
- Ibuprofen is associated with a significant increase in cardiovascular risk, while naproxen is considered the preferred, safer option.
Salicylates
- Inhibit prostaglandin synthesis from arachidonic acid by inhibiting both isoforms of the COX enzyme.
- Reduce the sensitivity of pain receptors to the initiation of pain impulses at sites of inflammation and trauma.
- Are absorbed by passive diffusion of the non-ionized drug in the stomach and small intestine.
- Are effective in treating mild to moderate pain from musculoskeletal conditions and fever.
Salicylates Pharmacokinetics
- Protein binding is concentration dependent.
- Are largely eliminated through the kidney.
- Urine pH determines the amount of unchanged drug that is eliminated.
Salicylates Clinical Use
- Aspirin is also indicated for prevention of thromboembolic events (e.g., myocardial infarction and stroke) in high-risk patients.
- The maximum analgesic dosage for self-medication with aspirin is 4 g/day.
Clinically Important Drug-Drug Interactions
- Acetaminophen and alcohol: avoid concurrent use if possible; minimize alcohol intake when using acetaminophen.
- Acetaminophen and warfarin: monitor INR for several weeks when acetaminophen is added or discontinued in patients on warfarin.
- Aspirin and valproic acid: avoid concurrent use; use naproxen instead of aspirin.
- Aspirin and NSAIDs: avoid concurrent use if possible; consider use of gastroprotective agents (e.g., PPIs).
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Description
This quiz covers the potential hepatotoxicity of acetaminophen and precautions for patients with glucose-6-phosphate dehydrogenase deficiency. It also discusses the mechanism of pain relief of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs).