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Questions and Answers
What is the primary mechanism of action of NSAIDs?
Which of the following NSAIDs is a selective COX-2 inhibitor?
What is a common side effect of long-term NSAID use?
What is the primary reason for avoiding aspirin in children with viral infections?
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What is the antidote for paracetamol overdose?
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What is the primary benefit of selective COX-2 inhibitors?
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What is a characteristic of aspirin that distinguishes it from other NSAIDs?
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What is a potential complication of high-dose or long-term aspirin use?
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What is the primary effect of aspirin on the body's acid-base balance?
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What is a common use of aspirin in high-risk patients?
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Study Notes
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
- NSAIDs are a class of drugs used to reduce inflammation, pain, and fever
- They do not contain steroids and are also known as 'NSAIDs' or 'antipyretic agents'
- NSAIDs work by inhibiting the production of prostaglandins, which are involved in inflammation
- Key NSAIDs include aspirin, ibuprofen, diclofenac, and celecoxib
Mechanism of Action
- NSAIDs target two enzymes: COX-1 and COX-2
- COX-1 is responsible for normal physiological functions like protecting the stomach lining
- COX-2 is induced during inflammation and causes pain, fever, and swelling
- NSAIDs can either be non-selective (inhibit both COX-1 and COX-2) or selective COX-2 inhibitors
Benefits and Risks
- NSAIDs provide analgesic (pain-relieving), antipyretic (fever-reducing), and anti-inflammatory effects
- However, inhibiting COX-1 can also lead to stomach ulcers and bleeding
- Selective COX-2 inhibitors aim to minimize this risk by targeting only the inflammatory pathway
Specific NSAIDs
- Aspirin: Has cardiovascular protective effects but can also cause stomach bleeding and ulcers
- Ibuprofen: Common over-the-counter NSAID used for pain, fever, and inflammation in children
- Diclofenac: Potent NSAID frequently prescribed for musculoskeletal pain and inflammation
- Celecoxib: A selective COX-2 inhibitor with reduced risk of gastrointestinal side effects
Considerations
- NSAIDs should be used cautiously, especially in elderly patients or those with pre-existing conditions
- Monitoring of electrolyte balance and renal function is important with long-term NSAID use
- Potential side effects include hypertension, edema, and increased cardiovascular risk### Acetylsalicylic Acid (Aspirin) Overview
- Aspirin is the only irreversible cyclooxygenase (COX) inhibitor, meaning it permanently blocks the enzyme responsible for prostaglandin production
- This gives aspirin anti-inflammatory, antipyretic (fever-reducing), and anti-platelet (blood thinning) properties
- Aspirin is commonly used to prevent heart attacks and strokes in high-risk patients due to its anti-platelet effects
Aspirin Adverse Effects
- Can cause gastrointestinal ulcers and bleeding due to reduction in protective prostaglandins
- High-dose or long-term use can lead to hyperuricemia (high uric acid levels)
- Should be avoided in children with viral infections due to risk of Reye's syndrome, a rare and serious condition
Aspirin Toxicity
- Aspirin poisoning can lead to respiratory alkalosis initially, as the drug stimulates the respiratory center
- This depletes carbon dioxide in the body, causing a shift towards metabolic acidosis which is a severe, life-threatening condition
- Symptoms include nausea, vomiting, tinnitus, and altered vision
Paracetamol (Acetaminophen) Toxicity
- Paracetamol is a commonly used pain and fever medication, generally considered safe
- However, overdose can cause liver damage, as a toxic metabolite (NAPQI) is produced that depletes glutathione in the liver
- Prompt treatment with the antidote N-acetylcysteine is crucial to prevent irreversible liver injury
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
- Reduce inflammation, pain, and fever without containing steroids
- Work by inhibiting prostaglandin production, which is involved in inflammation
- Key examples include aspirin, ibuprofen, diclofenac, and celecoxib
Mechanism of Action
- Target two enzymes: COX-1 and COX-2
- COX-1 is responsible for normal physiological functions like protecting the stomach lining
- COX-2 is induced during inflammation and causes pain, fever, and swelling
- Can be non-selective (inhibit both COX-1 and COX-2) or selective COX-2 inhibitors
Benefits and Risks
- Provide analgesic, antipyretic, and anti-inflammatory effects
- Inhibiting COX-1 can lead to stomach ulcers and bleeding
- Selective COX-2 inhibitors aim to minimize this risk by targeting only the inflammatory pathway
Specific NSAIDs
- Aspirin: Has cardiovascular protective effects, but can cause stomach bleeding and ulcers
- Ibuprofen: Common over-the-counter NSAID used for pain, fever, and inflammation in children
- Diclofenac: Potent NSAID frequently prescribed for musculoskeletal pain and inflammation
- Celecoxib: A selective COX-2 inhibitor with reduced risk of gastrointestinal side effects
Considerations
- Use cautiously, especially in elderly patients or those with pre-existing conditions
- Monitor electrolyte balance and renal function with long-term NSAID use
- Potential side effects include hypertension, edema, and increased cardiovascular risk
Acetylsalicylic Acid (Aspirin)
- Irreversible cyclooxygenase (COX) inhibitor, permanently blocking the enzyme responsible for prostaglandin production
- Has anti-inflammatory, antipyretic, and anti-platelet properties
- Used to prevent heart attacks and strokes in high-risk patients due to its anti-platelet effects
Aspirin Adverse Effects
- Can cause gastrointestinal ulcers and bleeding due to reduction in protective prostaglandins
- High-dose or long-term use can lead to hyperuricemia
- Should be avoided in children with viral infections due to risk of Reye's syndrome
Aspirin Toxicity
- Can lead to respiratory alkalosis initially, followed by metabolic acidosis, a severe and life-threatening condition
- Symptoms include nausea, vomiting, tinnitus, and altered vision
Paracetamol (Acetaminophen) Toxicity
- Overdose can cause liver damage, as a toxic metabolite (NAPQI) depletes glutathione in the liver
- Prompt treatment with the antidote N-acetylcysteine is crucial to prevent irreversible liver injury
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Description
Understand the mechanism of action of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), including their effects on inflammation, pain, and fever. Learn about the key enzymes targeted by NSAIDs and their classification.
