How NSAIDs Work

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Questions and Answers

What is one of the effects of prostaglandin E2 in the stomach?

Increasing the production of protective mucus (correct)

Increasing the secretion of acid

Decreasing the production of protective mucus

Reducing uterine contractions

What is the main difference between irreversible and reversible COX inhibitors?

Their mechanism of action

Their effectiveness in treating pain

Their ability to inhibit COX-1 and COX-2

Their duration of action (correct)

How does aspirin work as an antiplatelet medication?

By irreversibly inhibiting COX-1 (correct)

By increasing thromboxane A2 production

By reversibly inhibiting COX-1

By inhibiting COX-2

What is the effect of aspirin on bleeding time?

It increases bleeding time Signup and view all the answers

What is the anti-inflammatory effect of salicylate?

Inhibiting COX-2 Signup and view all the answers

What is the dose-dependent effect of aspirin?

Antiplatelet effect at low doses Signup and view all the answers

What is the difference between non-selective COX inhibitors and selective COX-2 inhibitors?

Their ability to inhibit COX-1 Signup and view all the answers

What is the effect of non-selective COX inhibitors on aspirin's antiplatelet effect?

It decreases the antiplatelet effect Signup and view all the answers

What is the indication for indomethacin in neonates and premature infants?

Closure of patent ductus arteriosus Signup and view all the answers

What is the main difference between celecoxib and other NSAIDs?

Its lack of antiplatelet effect Signup and view all the answers

What is the mechanism of action of NSAIDs?

Inhibition of COX enzymes Signup and view all the answers

Which COX inhibitor is selective for COX-2?

Celecoxib Signup and view all the answers

What is the primary difference between reversible and irreversible COX inhibitors?

Reversibility Signup and view all the answers

What is the indication for aspirin that is not shared with other NSAIDs?

Antiplatelet Signup and view all the answers

What is the side effect of NSAIDs that is most severe in the aspirin coop?

Gastritis Signup and view all the answers

What is the condition associated with Samter’s triad?

Asthma Signup and view all the answers

What is the medication that is used to close patent ductus arteriosus?

Indomethacin Signup and view all the answers

What is the side effect of aspirin that is represented by a young man wearing headphones?

Ototoxicity Signup and view all the answers

What is the medication that is represented by a bulletproof vest?

Ibuprofen Signup and view all the answers

What is the indication for NSAIDs that is not shared with aspirin?

Gout Signup and view all the answers

What is the primary function of NSAIDs in the body?

To decrease the production of prostaglandins Signup and view all the answers

What is the source of arachidonic acid in the body?

Membrane phospholipids broken down by phospholipase A2 Signup and view all the answers

What is the difference between COX-1 and COX-2 enzymes?

COX-1 is constitutive, while COX-2 is inducible Signup and view all the answers

What is the effect of prostaglandins on nociceptors?

They decrease the threshold for activation Signup and view all the answers

What is the role of cyclooxygenase in the body?

It converts arachidonic acid into prostaglandins Signup and view all the answers

What is the outcome of increased prostaglandin production in the body?

Increased vasodilation and pain Signup and view all the answers

What is the advantage of combining aspirin with a selective COX-2 inhibitor?

It does not decrease the antiplatelet effect of aspirin. Signup and view all the answers

What is the effect of COX-1 inhibition in the stomach?

It decreases the concentration of cytoprotective prostaglandins. Signup and view all the answers

Why do NSAIDs inhibit COX-2 in the kidneys?

To decrease the level of prostaglandins that dilate the renal artery. Signup and view all the answers

What is the effect of low doses of aspirin taken right before bedtime?

It lowers blood pressure. Signup and view all the answers

What is the-term for the combination of asthma, nasal polyps, and NSAID hypersensitivity?

Samter's triad Signup and view all the answers

Why should aspirin not be given to children with viral infections to reduce fever?

It can lead to Reye's syndrome. Signup and view all the answers

What is the effect of high doses of salicylate on the body?

It inhibits oxidative phosphorylation. Signup and view all the answers

What is the treatment for aspirin overdose?

Administration of activated charcoal and alkalization of urine. Signup and view all the answers

What is the term for the condition characterized by liver damage and progressive encephalopathy?

Reye's syndrome Signup and view all the answers

What is the term for the NSAID-induced condition characterized by chronic nephritis or renal papillary necrosis?

Analgesic nephropathy Signup and view all the answers

What is the primary function of phospholipase A2 in the context of inflammation?

To take membrane phospholipids and produce arachidonic acid Signup and view all the answers

What is the effect of prostaglandin E2 on nociceptors?

It increases their sensitivity to stimuli Signup and view all the answers

Which of the following is NOT a characteristic of COX-1?

It is triggered by immune cells and vascular endothelial cells Signup and view all the answers

What is the effect of NSAIDs on prostaglandins?

They decrease the production of prostaglandins Signup and view all the answers

What is the source of arachidonic acid in the body?

It is produced from membrane phospholipids Signup and view all the answers

What is the effect of cyclooxygenase on arachidonic acid?

It converts arachidonic acid into prostaglandins Signup and view all the answers

What is the primary effect of aspirin on platelet function?

Decrease in thromboxane A2 production Signup and view all the answers

Which of the following NSAIDs is available in parenteral form?

Ketorolac, ibuprofen, and indomethacin Signup and view all the answers

What is the primary indication for celecoxib?

Treatment of pain and inflammation Signup and view all the answers

What is the effect of aspirin on bleeding time?

Increase in bleeding time Signup and view all the answers

Which of the following is a characteristic of irreversible COX inhibitors?

Irreversible inhibition of COX-1 and COX-2 Signup and view all the answers

What is the primary mechanism of action of NSAIDs?

Inhibition of COX-1 and COX-2 Signup and view all the answers

Which of the following NSAIDs is used to treat severe acute pain?

Ketorolac Signup and view all the answers

What is the effect of low doses of aspirin on platelet function?

Decrease in platelet aggregation Signup and view all the answers

What is the primary difference between aspirin and non-aspirin NSAIDs?

Aspirin is irreversible, while non-aspirin NSAIDs are reversible Signup and view all the answers

Which of the following is a characteristic of selective COX-2 inhibitors?

Lack of antiplatelet effect Signup and view all the answers

What is the primary mechanism of action of NSAIDs in treating pain, inflammation, and fever?

Inhibition of COX enzymes Signup and view all the answers

Which of the following medications is NOT used to treat gout?

Aspirin Signup and view all the answers

What is the primary difference between the effects of aspirin and reversible COX inhibitors on the stomach?

Aspirin causes more severe bleeding Signup and view all the answers

Which of the following medications is used to treat pain, inflammation, and fever, but not gout?

Aspirin Signup and view all the answers

What is the primary effect of COX-2 inhibition in the kidneys?

Increased blood pressure Signup and view all the answers

Which of the following is a common side effect of NSAIDs that is most severe with aspirin?

Gastritis Signup and view all the answers

What is the primary indication for ketorolac?

Post-surgical pain relief Signup and view all the answers

Which of the following is NOT a side effect of aspirin overdose?

Gastritis Signup and view all the answers

What is the primary difference between the effects of COX-1 and COX-2 inhibition?

COX-1 inhibition affects the stomach Signup and view all the answers

Which of the following medications is used to treat a specific condition in neonates and premature infants?

Indomethacin Signup and view all the answers

What is the reason why selective COX-2 inhibitors cause the least gastrointestinal side effects?

They don't affect COX-1 in the stomach Signup and view all the answers

What is the mechanism by which low doses of aspirin taken right before bedtime can lower blood pressure?

The mechanism is still being studied Signup and view all the answers

What is the result of chronic abuse of NSAIDs in individuals with underlying heart, liver, or kidney disease?

It can lead to analgesic nephropathy Signup and view all the answers

What is the reason why people with nasal polyps and asthma are more likely to experience NSAID hypersensitivity?

They are more likely to have Samter's triad Signup and view all the answers

What is the effect of high doses of salicylate on the body's energy production?

It inhibits oxidative phosphorylation Signup and view all the answers

What is the treatment for aspirin overdose that helps facilitate salicylate excretion?

Alkalization of urine by sodium bicarbonate Signup and view all the answers

What is the difference between the effects of aspirin and other NSAIDs on the renin-angiotensin-aldosterone system?

Aspirin increases blood pressure, while other NSAIDs decrease it Signup and view all the answers

What is the outcome of increased lactic acid production in the body due to salicylate overdose?

It leads to metabolic acidosis Signup and view all the answers

What is the reason why aspirin should not be given to children with viral infections to reduce fever?

It can lead to Reye's syndrome Signup and view all the answers

What is the effect of salicylate on the blood-brain barrier at high doses?

It shifts towards its non-ionized form, salicylic acid, and crosses the blood-brain barrier Signup and view all the answers

Which of the following effects of prostaglandin E2 is NOT mentioned in the text?

Increasing the production of acid in the stomach Signup and view all the answers

What is the primary mechanism of action of acetaminophen?

Reversibly inhibiting COX in the central nervous system Signup and view all the answers

What is the main reason why acetaminophen is preferred over aspirin in certain individuals?

It does not affect COX in platelets and the stomach Signup and view all the answers

What is the toxic metabolite produced by the metabolism of acetaminophen?

N-acetyl-p-benzoquinone imine Signup and view all the answers

What is the primary treatment for acetaminophen toxicity?

Administration of N-acetylcysteine Signup and view all the answers

What is the condition that can occur in children after a viral infection and is associated with the use of aspirin?

Reye's syndrome Signup and view all the answers

What is the main difference between the effects of acetaminophen and NSAIDs?

Acetaminophen does not inhibit COX peripherally Signup and view all the answers

What is the role of glutathione in the metabolism of acetaminophen?

It inactivates the toxic metabolite produced by acetaminophen Signup and view all the answers

What is the primary indication for acetaminophen in children?

Fever and mild to moderate pain Signup and view all the answers

What is the common characteristic of individuals who are more susceptible to acetaminophen toxicity?

They have a lower glutathione level Signup and view all the answers

What is the primary effect of prostaglandin E2 on the body?

It increases the sensitivity of nociceptors to pain Signup and view all the answers

What is the role of cyclooxygenase in the production of prostaglandins?

It converts arachidonic acid to prostaglandin E2 Signup and view all the answers

What is the primary effect of acetaminophen on prostaglandin production?

It decreases the production of prostaglandin E2 Signup and view all the answers

What is the mechanism by which COX-2 is induced during inflammation?

It is induced by immune cells and vascular endothelial cells Signup and view all the answers

What is the primary effect of prostaglandin E2 on blood vessels?

It causes vasodilation Signup and view all the answers

What is the primary source of arachidonic acid in the body?

It is produced by phospholipase A2 Signup and view all the answers

Study Notes

Prostaglandins and Inflammation

Prostaglandin E2 causes uterine contractions, decreases acid secretion, and increases protective mucus production in the stomach.
Prostaglandins are involved in inflammation, pain, and fever.

NSAIDs and COX Enzymes

NSAIDs work by inhibiting cyclooxygenase (COX) enzymes.
COX enzymes have two isoforms: COX-1 and COX-2.
COX-1 is a constitutive enzyme, always active, while COX-2 is inducible and triggered by immune cells and vascular endothelial cells during inflammation.

Aspirin (Irreversible COX Inhibitor)

Works by irreversibly inhibiting both COX-1 and COX-2.
Taken orally, with most absorption in the ileum.
Irreversibly inhibits COX-1 in platelets, decreasing thromboxane A2 production, making it useful as an antiplatelet medication.
Effects persist until new platelets are produced that can synthesize COX-1 enzymes.
Increases bleeding time without affecting PT or PTT.
Metabolized in the liver to salicylate, which has anti-inflammatory properties.
Used to treat headaches, musculoskeletal pain, osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis.
Effects are dose-dependent: low doses (under 300 mg/day) work as an antiplatelet medication, medium doses (300-2400 mg/day) work as an antipyretic and analgesic, and high doses (over 2400 mg/day) work as an anti-inflammatory medication.

Non-Selective COX Inhibitors (Reversible)

Include ibuprofen, naproxen, ketorolac, indomethacin, sulindac, and meloxicam.
Reversibly inhibit both COX-1 and COX-2.
Can be taken orally or parenterally (ketorolac, ibuprofen, and indomethacin).
Have antiplatelet effects, but are transient due to reversible inhibition.
Inhibit COX-2, reducing inflammation, pain, and fever.
Used to treat pain, inflammation, and fever, as well as gout, patent ductus arteriosus, and acute pain after surgery.

Selective COX-2 Inhibitors

Include celecoxib.
Reversibly inhibit COX-2, reducing inflammation, pain, and fever.
Lack antiplatelet effects.
Used to treat pain, inflammation, and fever.

Side Effects and Precautions

NSAIDs can cause gastrointestinal problems (gastritis, ulcers, bleeding) by blocking COX-1.
NSAIDs can cause kidney damage and hypertension by inhibiting COX-2.
Hypersensitivity reactions can occur, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, and anaphylaxis.
Cross-hypersensitivity can occur between NSAIDs.
Individuals with nasal polyps and asthma are more likely to experience NSAID hypersensitivity (Samter's triad).
Aspirin overdose can be fatal, causing tinnitus, deafness, headache, vomiting, respiratory alkalosis, and metabolic acidosis.
Treatment of aspirin overdose includes activated charcoal, urinary alkalization, ventilatory support, and management of acid-base imbalance.### Prostaglandin E2 and NSAIDs
Prostaglandin E2 causes uterine contractions, decreases acid secretion, and increases protective mucus production in the stomach
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) inhibit cyclooxygenase, decreasing prostaglandin production, and are used to treat inflammation, pain, and fever

Classification of NSAIDs

Irreversible COX inhibitors: aspirin (acetylsalicylic acid)
Reversible COX inhibitors:
- Non-selective COX inhibitors: ibuprofen, naproxen, ketorolac, indomethacin, sulindac, meloxicam
- Selective COX-2 inhibitors: celecoxib

Aspirin (Acetylsalicylic Acid)

Irreversibly inhibits COX-1 and COX-2
Taken orally, absorbed in the ileum
Decreases thromboxane A2 production in platelets, making it an antiplatelet medication
Effect persists until new platelets are produced
Metabolized into salicylate in the liver, which has anti-inflammatory properties
Used to treat headaches, musculoskeletal pain, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis
Dose-dependent effects:
- Low doses (<300 mg/day): antiplatelet medication
- Medium doses (300-2400 mg/day): antipyretic and analgesic
- High doses (>2400 mg/day): anti-inflammatory medication

Non-Selective COX Inhibitors

Reversibly inhibit COX-1 and COX-2
Include ibuprofen, naproxen, ketorolac, indomethacin, sulindac, meloxicam
Available in oral and parenteral forms (except sulindac and meloxicam)
Antiplatelet effect is transient and competes with aspirin's effect
Used to treat pain, inflammation, and fever, including gout, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis
Indomethacin also used to close patent ductus arteriosus in neonates and premature infants
Ketorolac used to treat severe acute pain, usually after surgery

Selective COX-2 Inhibitors

Celecoxib
Reversibly inhibits COX-2, reducing inflammation, pain, and fever
Lacks antiplatelet effect
Used to treat pain, inflammation, and fever, including osteoarthritis, rheumatoid arthritis, ankylosing spondylitis

Side Effects of NSAIDs

Gastritis and gastric ulcers (most severe with aspirin)
Kidney damage and hypertension
Cross-hypersensitivity between NSAIDs

Acetaminophen

Reversibly inhibits COX in the central nervous system
Used to treat fever and mild to moderate pain
Not an NSAID due to lack of peripheral COX inhibition
Indications: fever, myalgia, headache
Preferred in individuals with bleeding disorders, peptic ulcers, or allergies to aspirin
First-line therapy for children with fever or pain (due to risk of Reye's syndrome with aspirin)
Metabolized by hepatocytes in the liver
Can cause liver toxicity due to NAPQI production
Treatment: administration of N-acetylcysteine (NAC)

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Description

Learn how Non-steroidal anti-inflammatory drugs (NSAIDs) reduce inflammation, relieve pain, and lower fever by decreasing the production of prostaglandins. Understand the body's response to harmful stimuli and how NSAIDs interact with it.