Inflammation and NSAIDs Overview

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Questions and Answers

What is the primary role of COX-1 in the body?

Stimulates the production of pro-inflammatory prostaglandins

Regulates platelet aggregation in response to injury

Maintains homeostatic functions in tissues (correct)

Induced in response to inflammation

How does PGE2 contribute to the inflammatory response?

Promotes platelet aggregation

Induces bronchoconstriction

Decreases vasodilation

Inhibits gastric acid secretion (correct)

What is the effect of TXA2 in the body?

Inhibits the aggregation of platelets

Causes vasodilation and decreased blood pressure

Promotes aggregation of platelets (correct)

Stimulates contraction of the uterus

Which statement correctly describes prostaglandins in relation to pain?

They act as mediators of pain signals Signup and view all the answers

NSAIDs primarily work by which mechanism?

Inhibiting the production of prostaglandins Signup and view all the answers

What triggers the production of COX-2?

Cytokines stimulation Signup and view all the answers

What is the effect of PGI2 (prostacyclin) in the cardiovascular system?

Inhibits platelet aggregation Signup and view all the answers

What is one of the key functions of PGF2α?

Facilitates uterine contraction Signup and view all the answers

What effect does H2 receptor blockade have on gastric acid secretion?

Decreases gastric acid secretion Signup and view all the answers

Which of the following is NOT a therapeutic use of first-generation antihistamines?

Treatment of bronchial asthma Signup and view all the answers

How do mast cell stabilizers function in the treatment of allergic reactions?

They inhibit the release of histamine from mast cells Signup and view all the answers

What is a common side effect of first-generation H1 antihistamines?

Sedation Signup and view all the answers

Which H1 antihistamine is characterized as having minimal CNS side effects and is specific for H1 receptors?

Cetirizine Signup and view all the answers

What is the half-life of the medication mentioned?

1-2 hours Signup and view all the answers

Which of the following is NOT a clinical use of ibuprofen?

Antibiotic Signup and view all the answers

Which adverse effect is considered less frequent with ibuprofen compared to aspirin?

Gastric upset Signup and view all the answers

What is a contraindication for the use of ibuprofen?

Peptic ulcer Signup and view all the answers

What is one of the formulations of ibuprofen available for rapid relief?

A liquid gel for postsurgical dental pain Signup and view all the answers

Which statement about ibuprofen’s interaction with aspirin is correct?

It antagonizes the irreversible platelet inhibition of aspirin. Signup and view all the answers

Which of the following is likely to be a common side effect of ibuprofen?

Dyspepsia Signup and view all the answers

Which condition would make ibuprofen use particularly risky?

Kidney impairment Signup and view all the answers

What is one clinical application of heteroaryl acetic acids like diclofenac?

Inflammatory conditions Signup and view all the answers

Which of the following medications is noted for being used once a day due to its strong derivative?

Oxaprozin Signup and view all the answers

What is the primary antipyretic effect of NSAIDs attributed to?

Induction of COX-2 in the brain Signup and view all the answers

At what dosage is aspirin commonly used for its cardiovascular protective effects?

81 mg Signup and view all the answers

Which statement regarding the effects of aspirin on platelets is correct?

TXA2 inhibition lasts for the entire life of the platelet. Signup and view all the answers

What adverse effect is commonly associated with aspirin due to COX-1 inhibition?

Gastric distress Signup and view all the answers

Which of the following patients should avoid aspirin due to kidney concerns?

Patients with a glomerular filtration rate < 30 Signup and view all the answers

What is Reye syndrome primarily associated with?

Viral infections in children Signup and view all the answers

Which of the following is a characteristic of ibuprofen compared to aspirin?

It is a reversible inhibitor of COX enzymes Signup and view all the answers

What may occur as a result of aspirin toxicity?

Respiratory and metabolic acidosis Signup and view all the answers

Which one of the following is NOT typically caused by aspirin?

Interstitial nephritis Signup and view all the answers

What is a common side effect of low-dose aspirin therapy?

Prolonged bleeding time Signup and view all the answers

Which of the following side effects is associated with diclofenac sodium?

Gastric upset Signup and view all the answers

What is the primary clinical indication for ketorolac?

Short-term acute pain management Signup and view all the answers

Which of the following patient conditions makes diclofenac potassium the preferred choice?

Cardiovascular disease Signup and view all the answers

What is a known side effect of using celecoxib?

Renal toxicity Signup and view all the answers

Which of the following actions is NOT associated with autacoids?

Production in specific endocrine glands Signup and view all the answers

In which condition is indomethacin specifically used to induce closure?

Patent ductus arteriosus in premature infants Signup and view all the answers

What is the mechanism of action primarily associated with sulindac?

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

What is a common side effect of using heteroaryl acetic acids like ketorolac?

Headaches Signup and view all the answers

Which characteristic is TRUE about COX-2 selective NSAIDs like celecoxib?

They do not interfere with platelet function Signup and view all the answers

What should be avoided when prescribing ketorolac?

Using it for more than five days Signup and view all the answers

Study Notes

Inflammation

Inflammation is a complex protective response to injury
It aims to inactivate or remove damaging agents and promote healing

COX-1 & COX-2

COX-1: A constitutive isoform found in tissues
COX-2: Induced by cytokines, part of an inflammatory response

Prostaglandins (PGs)

PGE2: Pro-inflammatory, causing vasodilation, bronchodilation, inhibition of gastric acid, and sensitization of pain receptors.
PGF2a: Causes uterine contraction, bronchoconstriction, and decreased intraocular pressure.
TXA2: Produced by platelets, inducing platelet aggregation and vasoconstriction.
PGI2: Inhibits platelet aggregation and causes potent vasodilation.

NSAIDs (Nonsteroidal Anti-inflammatory Drugs)

MOA: Inhibit cyclooxygenases (COX), decreasing prostaglandin production.
COX-1: Constitutive - responsible for "house-keeping" functions.
COX-2: Induced by inflammatory factors; responsible for mediating pain.
NSAIDs don't cause pain directly, but sensitize pain receptors.
NSAIDs have antipyretic effects (reduce fever).

Aspirin (ASA)

Therapeutic use: Antipyretic, analgesic, anti-inflammatory at high doses.
Low doses inhibit platelet aggregation (cardiovascular benefits).
Low doses can reduce recurrence risk of MI, stroke & colon cancer.
Irreversibly inhibits TXA2, affecting platelet lifetime.
Results in decreased thrombus formation (anticoagulant effect).
Can cause GI distress, nausea, vomiting, microscopic bleeding.
Prolongs bleeding time; requires adjustment in dose for anticoagulant effects.

Propionic acid derivatives (e.g., Ibuprofen)

Anti-inflammatory, analgesic, and antipyretic effects.
Generally less likely to cause GI upset than aspirin.
Less potent anti-inflammatory than other NSAIDs.
Faster acting and better absorbed than aspirin.
Significant fluid retention effects.

Acetic acid derivatives (e.g., Diclofenac)

More potent anti-inflammatory than analgesics and antipyretics.
More potent than indomethacin and naproxen.
Clinical applications: Inflammatory conditions, musculoskeletal pain, dysmenorrhea, and acute gouty arthritis.
Potential for increased cardiovascular events.
Gastrointestinal ulceration and bleeding risk.

Heteroaryl Acetic Acids (e.g., Ketorolac)

Antipyretic, analgesic, and anti-inflammatory properties.
Indicated for short-term pain management.
Primarily used for acute pain.

COX-2 Selective NSAID: Celecoxib

Selective inhibitor of COX-2.
Less likely to cause gastrointestinal issues.
Potential for cardiovascular risks (e.g., thrombotic events).
Contraindicated for patients with severe renal insufficiency.

Steroidal Anti-inflammatory Drugs (SAIDs)

Short-acting glucocorticoids (e.g., hydrocortisone); Intermediate-acting (e.g., prednisone).

Histamine

An autacoid (local hormone).
Involved in allergic and inflammatory reactions.
Storage and release from mast cells through exocytosis.
Histamine triggers various inflammatory effects.
Mast cell degranulation leads to histamine release.

Histamine Antagonists/Blockers

First generation: Sedating (e.g., diphenhydramine); Second generation (e.g., Cetirizine).
H1 blockers: Block H1 receptors (itching, vasodilation, bronchoconstriction).
H2 blockers: Block H2 receptors (gastric acid secretion; e.g., Cimetidine).

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Description

This quiz covers key concepts related to inflammation, COX-1 and COX-2, and the role of prostaglandins and NSAIDs. Understand how these components interact and their significance in the body's healing processes. Test your knowledge on how nonsteroidal anti-inflammatory drugs work to alleviate pain and inflammation.