Drugs to Treat Inflammation

Question 1

How is aspirin protective against cardiovascular disease?

Answer 1

Because it tips the balance towards prostacyclin production because prostacyclin producing endothelians can make more COX while thromboxane producing platelets can’t

Question 2

How do NSAIDs cause bronchoconstriction in 10% of asthmatics?

Answer 2

Inhibition of the production of prostanoids means more arachonic acid is shuttled into leukotriene production which leads to bronchoconstriction

Question 2

Which of the typical effects of NSAIDs does paracetamol lack?

Answer 2

Anti-inflammatory

Question 4

In what physiological state are prostaglandins produced at the greatest level?

Answer 4

During inflammation

Question 4

How do NSAIDs increase bleeding time?

Answer 4

They downregulate thromboxane A2 production which has pro-coagulative effects

Question 5

How do NSAIDs adversely effect the kidney?

Answer 5

Blocking the tonic vasodilation provided by prostacyclin

Question 6

What is the mechanism of the analgesic effect of NSAIDs?

Answer 6

Prostaglandins sensitise nociceptors therefore inhibiting their production reduces pain

Question 8

COX enzymes catalyse the production of what?

Answer 8

Prostaglandins

Prostacyclin

Thromboxane

Question 9

How does aspirin inhibit COX?

Answer 9

Acetylates it

Question 10

What is the effect of lipoxins?

Answer 10

Resolution of inflammation

Question 11

What is unique of the effect of aspirin on COX?

Answer 11

The inhibition of COX is irreversible

Question 11

When does hepatotoxicity occur with paracetamol use?

Answer 11

When the liver capacity to detoxify the paracetamol is exceeded - usually at dose 20x normal

Question 12

How are lipoxins made due to aspirin?

Answer 12

Aspirin Acetylated COX2 produces them

Question 13

What are the general effects of NSAIDs?

Answer 13

Anti-inflammatory

Anti-pyretic

Analgesia

Anti-aggregative

Question 14

What effect does stimulating canabinoid receptors have on tissue?

Answer 14

Anti-inflammatory as well as

Appetite stimulation

Analgesia

Sedation

Psychoactivity

Question 15

What are the 3 mechanisms of action of glucocorticoids at a cellular level?

Answer 15

Direct Transactivation

Direct Transrepression

Tethered transrepression

Question 16

What is mechanism for GIT damage caused by NSAIDs?

Answer 16

Reduce PGE2 > withdraws its protective effects

• increase mucus production
• Increase blood flow
• Decrease H+ secretion
• Promotes angiogenesis

Question 17

Which COX enzyme is more widely expressed?

Answer 17

COX-1

Question 19

How do NSAIDs cause an increase in blood pressure?

Answer 19

Decreases the natriuresis effect of PGE2

Question 20

Why can’t aspirin be used for gout?

Answer 20

Because it shares a renal transporter with uric acid therefore they compete for secretion

Question 21

What are the limitations to using prostaglandins as treatment?

Answer 21

Generally they are unstable and expensive

Question 22

What types of drugs are given the name NSAID?

Answer 22

Non-selective inhibitors of COX-1 and COX-2

Question 23

Why is aspirin contradicted in children?

Answer 23

It is hepatotoxic in a number of children

Question 24

Which NSAID is preferred for fever?

Answer 24

Paracetamol

Question 25

How is tumour necrosis factor alpha being targeted in therapies?

Answer 25

Block it to block its inflammatory effects

eg in rheumatoid arthritis