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Questions and Answers
What is a significant effect of NSAIDs on body temperature regulation?
What is a significant effect of NSAIDs on body temperature regulation?
- They inhibit prostaglandin production in the hypothalamus. (correct)
- They lower the body temperature set point.
- They have no effect on body temperature.
- They increase the production of thermoregulatory hormones.
What is a common side effect associated with the long-term use of aspirin as an NSAID?
What is a common side effect associated with the long-term use of aspirin as an NSAID?
- Decreased platelet aggregation.
- Gastric bleeding due to its irreversible action on COX enzymes. (correct)
- Increased blood flow to the kidneys.
- Reversible inhibition of prostaglandin synthesis.
Which statement best describes the mechanism of action of NSAIDs?
Which statement best describes the mechanism of action of NSAIDs?
- They enhance the production of arachidonic acid.
- They inhibit COX1 and COX2, reducing prostaglandin synthesis. (correct)
- They increase the activity of inflammatory mediators.
- They promote vasodilation by increasing prostanoid levels.
Which of the following is NOT a therapeutic effect of NSAIDs?
Which of the following is NOT a therapeutic effect of NSAIDs?
What role does COX-2 specifically play in the inflammatory response?
What role does COX-2 specifically play in the inflammatory response?
What is a significant side effect of long-term glucocorticoid treatment?
What is a significant side effect of long-term glucocorticoid treatment?
Which drug is primarily classified as an anti-rheumatoid agent?
Which drug is primarily classified as an anti-rheumatoid agent?
What action do glucocorticoids have on glucose metabolism?
What action do glucocorticoids have on glucose metabolism?
How does paracetamol differ in its anti-inflammatory properties compared to NSAIDs?
How does paracetamol differ in its anti-inflammatory properties compared to NSAIDs?
What is a characteristic of selective COX inhibitors compared to non-selective ones?
What is a characteristic of selective COX inhibitors compared to non-selective ones?
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Study Notes
Classes of Anti-Inflammatory Drugs
- Non-Steroidal Anti-Inflammatory Drugs (NSAIDs): Include ibuprofen, diclofenac, and aspirin, providing relief for chronic joint conditions, headaches, and acute injuries.
- Disease-Modifying Anti-Rheumatic Drugs (DMARDs): Target rheumatoid arthritis with slow-acting agents like sulfasalazine and methotrexate.
- Steroids (Glucocorticoids): Synthesized from cholesterol, examples are cortisone and prednisone; act on inflammation broadly.
Mechanism of Action
-
NSAIDs Mechanism:
- Inhibit COX-1 and COX-2 enzymes, reducing prostaglandin synthesis, leading to decreased inflammation, pain, and fever.
- COX-1 maintains tissue homeostasis; COX-2 is induced in response to inflammation.
- Side effects include gastric irritation, renal impacts, and prolonged bleeding from platelet function inhibition.
- Aspirin irreversibly inhibits COX, beneficial for chronic conditions but risks gastric bleeding.
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Antipyretic Effects:
- Reset body temperature set-point through inhibition of prostaglandin production in the hypothalamus.
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Analgesic Effects:
- Reduce peripheral prostaglandins that sensitize nociceptors and inhibit spinal cord pain fiber sensitization.
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Paracetamol:
- Exhibits weak anti-inflammatory properties, primarily analgesic and antipyretic, with minimal gastric irritation.
- Functions through weak inhibition of COX-3 and conversion to AM404.
Anti-Rheumatoid Drugs
- Purpose: Slow-acting to alleviate symptoms and reduce inflammation in rheumatoid arthritis.
- Examples: Include methotrexate, gold compounds, and others.
Steroids (Glucocorticoids)
- Effects on Metabolism: Reduce glucose uptake, increase gluconeogenesis, leading to potential hyperglycemia and changes in fat distribution (moon face).
- Anti-Inflammatory Action: Inhibit both early and late inflammation phases via gene regulation after binding to intracellular receptors.
- Side Effects: Long-term/high-dose use can lead to immune suppression, slow wound healing, and metabolic disturbances.
Efficacy vs. Side Effects
- On-Target Effects: Excess stimulation or inhibition can produce adverse effects.
- Off-Target Effects: Non-selective drugs may generate unwanted outcomes at high doses.
COX Inhibitors
- Selective vs. Non-Selective: Important to weigh the benefits and downsides of different COX inhibitors and steroids concerning their selectivity and associated risks.
Drug Development Principles
- Biochemical Principles: Understanding the underlying principles aids in designing effective COX inhibitors.
- Drug Delivery: Considerations for novel drug design focus on efficient delivery for inflammation treatment.
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