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Questions and Answers
What is the essential characteristic of the acidic moiety in NSAIDs?
What is the essential characteristic of the acidic moiety in NSAIDs?
What property do NSAIDs differ in based on the lipophilic character of their aryl groups?
What property do NSAIDs differ in based on the lipophilic character of their aryl groups?
What range typically describes the pKa values of NSAIDs?
What range typically describes the pKa values of NSAIDs?
What is the major role of the acidic group in NSAIDs?
What is the major role of the acidic group in NSAIDs?
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Which process leads to the inactivation of many NSAIDs?
Which process leads to the inactivation of many NSAIDs?
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What is a major pathway of clearance for many NSAIDs?
What is a major pathway of clearance for many NSAIDs?
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What is the mechanism of action for acetylsalicylic acid as an inhibitor of COX?
What is the mechanism of action for acetylsalicylic acid as an inhibitor of COX?
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What is the consequence of inhibiting the synthesis of thromboxane A by acetylsalicylic acid?
What is the consequence of inhibiting the synthesis of thromboxane A by acetylsalicylic acid?
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Why are platelets unable to synthesize additional COX upon inhibition by acetylsalicylic acid?
Why are platelets unable to synthesize additional COX upon inhibition by acetylsalicylic acid?
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Study Notes
NSAIDs Characteristics
- The essential characteristic of the acidic moiety in NSAIDs is the presence of a carboxylic acid or an enolic acid.
Lipophilic Character and pKa Values
- NSAIDs differ in their lipophilicity based on the aryl groups, which affects their ability to penetrate tissues and cells.
- The pKa values of NSAIDs typically range from 3 to 5, indicating their acidic nature.
Acidic Group Role
- The major role of the acidic group in NSAIDs is to provide a binding site for the enzyme cyclooxygenase (COX), allowing for inhibition.
Inactivation and Clearance
- Many NSAIDs are inactivated through glucuronidation, a process that leads to their elimination.
- A major pathway of clearance for many NSAIDs is through the kidneys, where they are excreted in the urine.
Acetylsalicylic Acid Mechanism
- The mechanism of action for acetylsalicylic acid as an inhibitor of COX is through the irreversible acetylation of the enzyme, which leads to its inhibition.
Thromboxane A Synthesis
- The consequence of inhibiting the synthesis of thromboxane A by acetylsalicylic acid is the prevention of platelet aggregation.
Platelet COX Synthesis
- Platelets are unable to synthesize additional COX upon inhibition by acetylsalicylic acid because they lack a nucleus and are unable to transcribe new COX enzyme.
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Description
Test your knowledge of NSAIDs chemical and pharmacologic properties with this quiz. Explore the structural and functional characteristics of NSAIDs, including their acidic nature and COX inhibitory activity.
