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Questions and Answers
What is the primary mechanism of action for NSAIDs?
What is the primary mechanism of action for NSAIDs?
Which of the following effects is NOT associated with NSAIDs?
Which of the following effects is NOT associated with NSAIDs?
What is a specific clinical significance of Aspirin among NSAIDs?
What is a specific clinical significance of Aspirin among NSAIDs?
COX-1 primarily plays a role in which of the following functions?
COX-1 primarily plays a role in which of the following functions?
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The anti-inflammatory effect of NSAIDs is primarily due to their action on which component?
The anti-inflammatory effect of NSAIDs is primarily due to their action on which component?
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What is a primary therapeutic effect of increasing daily dosages of Aspirin?
What is a primary therapeutic effect of increasing daily dosages of Aspirin?
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Which side effect is most commonly associated with COX-1 inhibitors?
Which side effect is most commonly associated with COX-1 inhibitors?
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Which medication can be given to mitigate the gastrointestinal side effects of NSAIDs?
Which medication can be given to mitigate the gastrointestinal side effects of NSAIDs?
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What is a significant advantage of COX-2 selective inhibitors over COX-1 inhibitors?
What is a significant advantage of COX-2 selective inhibitors over COX-1 inhibitors?
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What is a potential cardiovascular risk associated with COX-2 inhibitors?
What is a potential cardiovascular risk associated with COX-2 inhibitors?
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Which effect is NOT associated with COX-1 function?
Which effect is NOT associated with COX-1 function?
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Which of the following is an effect of non-selective NSAIDs?
Which of the following is an effect of non-selective NSAIDs?
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What adverse effect can occur due to the inhibition of PGI2 by COX-2 inhibitors?
What adverse effect can occur due to the inhibition of PGI2 by COX-2 inhibitors?
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Which of the following statements about COX-2 selective inhibitors is true?
Which of the following statements about COX-2 selective inhibitors is true?
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Study Notes
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
- NSAIDs are cyclo-oxygenase inhibitors, preventing the synthesis of prostaglandins.
- These drugs have several effects including:
- Analgesic effect: relieving pain
- Antipyretic action: lowering elevated body temperature to normal
- Anti-inflammatory role: reducing inflammation or swelling
- Antiplatelet action: decreasing platelet aggregation and inhibiting thrombus formation in some NSAIDs
Prostaglandin Synthesis
- Prostaglandins are synthesized from arachidonic acid through two main pathways:
- The COX-1 pathway is responsible for the constitutive production of prostaglandins involved in normal bodily functions like protecting the stomach lining, regulating kidney function, and platelet aggregation.
- The COX-2 pathway is responsible for the inducible production of prostaglandins during inflammation, pain, and fever.
Role of Cyclooxygenases (COX)
- COX-1 is involved in housekeeping functions such as protecting the gastrointestinal tract and kidneys as well as in blood clotting and platelet aggregation.
- COX-2 is associated with inflammation. It is involved in the inflammatory response, pain, and fever.
Classifications of COX Inhibitors
- COX-2 selective NSAIDs: Examples include celecoxib. These drugs tend to have a lower risk of gastrointestinal side effects compared to nonselective NSAIDs but may pose increased cardiovascular risks.
- Semi-selective NSAIDs: A mix of COX-1 and COX-2 selectivity; examples include meloxicam, diclofenac. The effects on the GI tract are moderate compared with the nonselective NSAIDs.
- Nonselective NSAIDs: Examples include ibuprofen, naproxen, and aspirin. They have significant effects on gastrointestinal function and are associated with an increased risk of these side effects. Aspirin's cardiovascular effects make it favourable for low dose use as a preventative measure for stroke and heart attacks.
Effect of NSAIDs
- NSAIDs inhibit the production of prostaglandins involved in pain, fever, inflammation, and blood clotting.
Advantages of NSAIDs
- Anti-inflammatory effects: reducing inflammation
- Inhibition of inflammatory mediators: reducing the effect of chemicals involved in inflammation
- Antiplatelet effect (only in some NSAIDs): decreasing platelet aggregation
Acetaminophen
- Acts centrally on COX-3, resulting in analgesic and antipyretic effects.
- Causes hepatotoxicity at high doses due to accumulation of NAPQI, requiring acetylcysteine treatment.
Side Effects of NSAIDs
- Gastrointestinal (GI) tract effects: ulcers, bleeding
- Renal effects: fluid retention, increase blood pressure
- Cardiovascular effects: possible increased risk of cardiovascular events in some NSAIDs, particularly COX-2 inhibitors.
- Pregnancy and children: contraindicated in certain situations; potential for adverse effects in fetal development and hepatotoxicity
Keeping in Mind
- NSAIDs are contraindicated during pregnancy except low dose aspirin
- Bleeding tendency, premature closure of ductus arteriosus, slowing labour progress
- Aspirin and viral infections in children increase risk of Reyes Syndrome.
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Description
This quiz covers the essential aspects of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), including their mechanism of action, effects, and the role of cyclooxygenases in prostaglandin synthesis. Test your knowledge on analgesic effects, anti-inflammatory functions, and the differences between COX-1 and COX-2 pathways.
