NSAIDs

Question 1

What are the 5 cardinal signs of inflammation?

Answer 1

• Calor (Heating)
• Rubor (Redness)
• Tumor (Swelling)
• Dolor (Dull, persistent pain)
• Loss of Function

These signs were first described by Aulus Cornelius Celsus.

Question 2

What is the mechanism of action (MOA) of traditional NSAIDs like aspirin?

Answer 2

Inhibition of cyclooxygenase (COX-1/2) and irreversibly blocks prostanoid production

Aspirin irreversibly acetylates COX, forming covalent bonds.

Question 3

What distinguishes COX-1 from COX-2?

Answer 3

• COX-1: Constitutive in most cells; involved in homeostasis
• COX-2: Inducible by IL-1β and TNF-α; involved in inflammation

COX-2 is constitutively expressed in the kidney and female reproductive tract.

Question 4

What are the biological functions of PGI2?

Answer 4

• Vasodilatation
• Inhibition of platelet aggregation
• Renin release
• Natriuresis

PGI2 plays a role in regulating blood pressure and cardiovascular health.

Question 5

What is the historical significance of aspirin?

Answer 5

First acetylated salicylic acid in 1897; became widely available in 1900

Aspirin is one of the most popular drugs, with around 100 billion tablets taken per year.

Question 6

What are the adverse effects of traditional NSAIDs?

Answer 6

• GI tract: Nausea, vomiting, gastric upset, gastric ulceration
• Pseudo-allergic reactions
• Bleeding due to blood thinning
• Kidney issues
• Pregnancy toxicity

Aspirin can cause Reye’s syndrome in children with viral infections.

Question 7

What is the mechanism of action of paracetamol?

Answer 7

CNS-selective COX inhibitor, possibly COX-3

Paracetamol is effective as an antipyretic and analgesic but has weak anti-inflammatory properties.

Question 8

True or False: All NSAIDs are COX-2 inhibitors.

Answer 8

False

Most NSAIDs are non-selective COX-1/2 inhibitors
While COX-2 inhibitors were developed to reduce gastrointestinal side effects, all NSAIDs inhibit COX-2.

Question 9

Fill in the blank: Aspirin is often prescribed at low doses as a _______ for those at risk of cardiovascular diseases.

Answer 9

blood thinner

This use helps to reduce the risk of stroke and heart attacks.

Question 10

What are the advantages of paracetamol?

Answer 10

• Good analgesic
• Potent antipyretic
• Spares the GI tract
• Few side effects
• Safe for pediatric use

Paracetamol has relatively few drug-drug interactions.

Question 11

What are the limitations of COX-2 selective inhibitors (coxibs)?

Answer 11

• Not completely GI tract sparing
• Renal toxicity
• Contraindicated in third trimester of pregnancy
• Impair wound healing

Coxibs may increase the risk of thrombosis due to increased TXA2 levels.