NSAIDS

Question 1

What are NSAIDS used for?

Answer 1

Relief of mild-to-moderate pain (analgesic)
Toothache, headache, backache
Postoperative pain (opiate sparing)
Dysmenorrhea (menstrual pain)
Reduction of fever (antipyretic)
Influenza
Reduction of inflammation (anti-inflammatory)
Rheumatoid arthritis
Osteoarthritis
Other forms of musculo-skeletal inflammation
Soft tissue injuries (strains and sprains)
Gout

Question 2

what is the MOA of NSAIDS?

Answer 2

inhibition of prostaglandins and thromboxane synthesis

NSAIDs inhibit the enzyme cyclo-oxygenase
(COX), which is the rate limiting step for the production of all
prostanoids from their parent compound, arachidonic acid

Question 3

what are the unwanted actions of prostaglandin E2?

Answer 3

Increased pain perception

Increased body temperature

Acute inflammatory response

Immune responses

Tumorigenesis

Inhibition of apoptosis

Question 4

how does PGE2 increase body temperature?

Answer 4

PGE2 stimulates hypothalamic neurones initiating a rise in body temperature

Question 5

what are the desirable effects of PGE2?

Answer 5

bronchodilation
gastroprotection
renal salt and water homeostasis
vasoregulation

Question 6

what is the difference between NSAIDS and paracetamol?

Answer 6

it is not

a NSAID because it has no anti-inflammatory activity. Its actions appear to be largely restricted to nervous tissue

Question 7

what is unique about aspirin as an NSAID?

Answer 7

selective for COX1

bind irreversibly to COX enzymes

Question 8

what are the unwanted effects of aspirin?

Answer 8

• Gastric irritation, ulceration, bleeding, and (in extreme cases) perforation
• Reduced creatinine clearance and possible nephritis (nephrotoxicity)
• Prolonged bleeding times, due to reduced platelet aggregation
• Bronchoconstriction in susceptible individuals (which is why Aspirin is contra-indicated in asthmatics)

Question 9

what is the antidote for paracetamol poisoning?

Answer 9

Add compound with –SH groups

Usually intravenous Acetylcysteine