18 Questions
What was the major mechanism of action of all NSAIDs demonstrated by Vane and co-workers?
Inhibition of prostaglandin synthesis
Which compound obtained from willow bark led to the discovery of aspirin in 1899?
Salicylic acid
What strategy was proposed by WHO to provide adequate pain relief for cancer patients?
Around-the-clock pain relief
What is the main difference between NSAIDs and opioids in terms of analgesic strength?
Opioids are stronger analgesics compared to NSAIDs
Which enzyme is responsible for the synthesis of leukotrienes in the prostaglandin synthesis pathway?
Lipoxygenase (LOX)
What is the IASP definition of pain based on the provided text?
An unpleasant sensory and emotional experience associated with or resembling tissue damage
Which enzymes are inhibited by NSAIDs to reduce prostaglandin synthesis?
COX-1
According to the WHO Analgesic Ladder Strategy, what is the recommended step for moderate to severe pain?
Combining NSAIDs with opioids from the beginning
How do weaker analgesics differ from opioids in terms of pain management effectiveness?
Opioids are more potent in managing severe pain than weaker analgesics
Which class of analgesics primarily target COX-2 to reduce inflammation and pain?
Selective COX-2 inhibitors
What is a key difference between the mechanism of action of NSAIDs and opioids in pain management?
Opioids act directly on central nervous system receptors, while NSAIDs reduce inflammation by inhibiting COX enzymes
What is the mechanism by which NSAIDs exert their anti-inflammatory effect?
Blocking COX enzymes selectively
Which prostaglandin is primarily responsible for vascular endothelium vasodilation and inhibition of platelet aggregation?
PGI2
Which class of NSAIDs includes aspirin, ibuprofen, and naproxen?
Non-selective COX inhibitors
What is the primary effect of NSAIDs on platelet function?
Inhibiting platelet aggregation
Which event is a common consequence of NSAID-induced deficiency of prostaglandins (PGs)?
Prolongation of bleeding time
Which prostaglandin is primarily responsible for smooth muscle contraction throughout the body and inhibition of gastric acid secretion?
PGE2
What is the main difference between non-selective and selective COX-2 inhibitors in terms of COX enzyme inhibition?
Non-selective inhibitors block both COX enzymes, while selective inhibitors block COX-1 only.
Study Notes
Pain and NSAIDs
- Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, influenced by biological, psychological, and social factors.
History of NSAIDs
- Willow bark was used for centuries as an analgesic.
- Salicylic acid was obtained by hydrolysis of the bitter glycoside extracted from willow bark in 1838.
- Sodium salicylate was developed in 1875, and acetyl salicylate (Aspirin) was introduced in 1899.
- Vane and co-workers demonstrated that aspirin inhibits prostaglandin production in guinea-pig isolated lungs in 1971, earning a Nobel Prize in Medicine in 1982.
Mechanism of Action of NSAIDs
- NSAIDs inhibit prostaglandin synthesis by blocking the action of cyclooxygenase (COX) enzymes.
- There are two isoforms of COX enzyme: COX-1 and COX-2.
- NSAIDs can block both COX enzymes or selectively block COX-2 enzyme.
Classification of NSAIDs
- Classification based on chemical structure:
- Salicylates (Aspirin)
- Arylalkanoic acids (Indomethacin, Sulindac)
- Heteroarylalkanoic acids (Tolmetin, Diclofenac)
- Oxicams (Piroxicam, Tenoxicam)
- Classification based on COX affinity:
- Non-selective COX inhibitors (Aspirin, Ibuprofen, Diclofenac)
- Selective COX-2 inhibitors (Celecoxib, Etoricoxib)
Effects of NSAIDs
- Beneficial actions:
- Analgesia: prevention of nerve ending sensitization
- Antipyresis: reduction of body temperature
- Anti-inflammatory: reduction in signs of inflammation
- Antithrombotic: inhibition of platelet aggregation
- Adverse effects:
- Gastric mucosal damage
- Prolonged bleeding time
- Limitation of renal blood flow
- Delay/prolongation of labor
- Asthma, hypersensitivity, and anaphylactic reactions
Specific NSAIDs
- Aspirin:
- Non-selective and irreversibly inhibits both COX enzymes
- Classic actions: analgesic, antipyretic, and anti-inflammatory
- Inhibits platelet aggregation
- ADR: salicylism (mild intoxication) and acute salicylate poisoning (severe intoxication)
Learn about the ascending pain pathway, NSAIDs introduction, weaker analgesics, WHO Analgesic Ladder Strategy, and the history of NSAIDs from willow bark to sodium salicylate. Explore the use of non-steroidal anti-inflammatory drugs in pain management.
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