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Questions and Answers
Which of the following is NOT a consequence of NSAIDs blocking PGE2 and PGI2 synthesis?
Which of the following is NOT a consequence of NSAIDs blocking PGE2 and PGI2 synthesis?
Why are NSAIDs contraindicated for children/adolescents with fever?
Why are NSAIDs contraindicated for children/adolescents with fever?
What is the main function of PGI2 (Prostacyclin) in the body?
What is the main function of PGI2 (Prostacyclin) in the body?
How do NSAIDs affect arachidonic acid metabolism in the airways?
How do NSAIDs affect arachidonic acid metabolism in the airways?
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Which NSAID has anti-platelet/cardio-protective activity at very low doses?
Which NSAID has anti-platelet/cardio-protective activity at very low doses?
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Why are all NSAIDs considered analgesic and antipyretic?
Why are all NSAIDs considered analgesic and antipyretic?
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What is the main mechanism of action of NSAIDs?
What is the main mechanism of action of NSAIDs?
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Which COX isoform is considered the 'bad' isoform and is inducible by toxins and infectious agents?
Which COX isoform is considered the 'bad' isoform and is inducible by toxins and infectious agents?
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What distinguishes prostacyclin (PGI2) from other prostaglandins?
What distinguishes prostacyclin (PGI2) from other prostaglandins?
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What is the effect of NSAIDs on leukotrienes and other eicosanoids?
What is the effect of NSAIDs on leukotrienes and other eicosanoids?
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What is the chemical class to which Aspirin (acetylsalicylic acid) belongs?
What is the chemical class to which Aspirin (acetylsalicylic acid) belongs?
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Which component is NOT included in the synthesis inhibition by NSAIDs according to the passage?
Which component is NOT included in the synthesis inhibition by NSAIDs according to the passage?
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What is the main prostaglandin responsible for gastric protection and nourishment?
What is the main prostaglandin responsible for gastric protection and nourishment?
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Which synthetic prostaglandin is used for gastric protection and is co-prescribed with NSAIDs to prevent peptic ulcers?
Which synthetic prostaglandin is used for gastric protection and is co-prescribed with NSAIDs to prevent peptic ulcers?
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Which drug is administered for uterine bleeding post-labor and is a synthetic form of PGE2?
Which drug is administered for uterine bleeding post-labor and is a synthetic form of PGE2?
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Which medication, injected directly into the penis, is used for erectile dysfunction by inducing penile vasodilation?
Which medication, injected directly into the penis, is used for erectile dysfunction by inducing penile vasodilation?
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Which prostaglandin is mainly responsible for keeping the ductus arteriosus open in newborns?
Which prostaglandin is mainly responsible for keeping the ductus arteriosus open in newborns?
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Which COX inhibitor is still available on the market in the US among the coxibs or selective COX2 inhibitors?
Which COX inhibitor is still available on the market in the US among the coxibs or selective COX2 inhibitors?
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How do NSAIDs primarily provide pain relief?
How do NSAIDs primarily provide pain relief?
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Which enzyme do non-selective NSAIDs block to affect blood clotting and gastrointestinal functions?
Which enzyme do non-selective NSAIDs block to affect blood clotting and gastrointestinal functions?
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What is the specific target of selective NSAIDs to reduce side effects?
What is the specific target of selective NSAIDs to reduce side effects?
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Which of the following is NOT a mediator released by immune cells during the inflammatory response?
Which of the following is NOT a mediator released by immune cells during the inflammatory response?
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What role do prostaglandins E2 and F2 play in pain perception and inflammation?
What role do prostaglandins E2 and F2 play in pain perception and inflammation?
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Study Notes
NSAIDs Mechanism of Action and Effects
- NSAIDs mediate venodilatation by furosemide, inhibit platelets, and lower pulmonary arterial pressure.
- They cause renal problems by blocking the synthesis of beneficial prostaglandins (PGE2 and PGI2) in the kidney.
Effects on Airways and Asthma
- NSAIDs divert arachidonic acid metabolism to leukotriene synthesis, increasing the risk of bronchospasm and asthma-related inflammation.
Analgesic, Antipyretic, and Anti-Inflammatory Effects
- All NSAIDs are analgesic and antipyretic, except for acetaminophen, which is only analgesic and antipyretic at all doses.
- At higher doses, NSAIDs are also anti-inflammatory, except for acetaminophen.
Aspirin and Cardio-Protective Activity
- Aspirin is contraindicated for fever in children/adolescents due to Reye's syndrome.
- At very low doses, aspirin has anti-platelet/cardio-protective activity via thromboxane TXA2 synthesis inhibition in platelets.
Patent Ductus Arteriosus and GI Protection
- All NSAIDs help close patent ductus arteriosus in preterm infants, with ibuprofen and indomethacin being the NSAIDs of choice.
- COX1 synthesizes PGE1 and PGE2, which protect and nourish gastric mucosa and epithelia.
- Misoprostol, a PGE1 synthetic analog, is co-prescribed with an NSAID for gastric protection.
Additional Uses of Prostaglandins
- Synthetic PGE2 (dinoprostone) is used for uterine bleeding post-labor.
- Synthetic PGE1 (alprostadil) is used for erectile dysfunction, inducing penile vasodilation.
COX Inhibition and Eicosanoids
- The MOA of NSAIDs is cyclooxygenase (COX) inhibition, blocking the synthesis of prostaglandins (PGs) and thromboxanes (TXs).
- Two functional COX isoforms in humans: COX1 (constitutive and "good") and COX2 (inducible and "bad").
- All eicosanoids come from arachidonic acid, and NSAIDs block synthesis of all PGs and TXs but not of leukotrienes or other eicosanoids.
Chemistry and Nomenclature
- All PGs and TXs have 20 carbon atoms (eicosanoids) and are carboxylic acids (arachidonic acid derivatives) with one or more double bonds and at least one ring.
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Description
Test your knowledge on the effects of NSAIDs on venodilatation, platelet inhibition, pulmonary arterial pressure, and renal problems. Learn about how NSAIDs impact arachidonic acid metabolism and leukotriene synthesis.