NSAIDS and Paracetamol

Question 1

What are the 3 key fore drugs we need to know that come under NSAID category?

1 - aspirin, atorvastatin, naproxen
2 - aspirin, paracetamol, naproxen
3 - aspirin, ibuprofen, naproxen
4 - paracetamol, ibuprofen, aspirin

Answer 1

3 - aspirin, ibuprofen, naproxen

Question 2

Which pathway are NSAIDs ultimately trying to inhibit?

Answer 2

• cyclooxygenase pathway

Question 3

Do NSAIDs mainly work centrally or peripherally?

Answer 3

• peripherally reducing prostaglandins

Question 4

COX-I and COX-II has a number of adverse effects. What are the 3 key adverse effects of inhibiting COX-I and II?

Answer 4

1 - peptic ulcers
2 - renal failure
3 - fluid retention and heart failure

Question 5

Prostaglandins can cause problems if there is too much as we seen in inflammatory conditions. What 2 positive effects to prostaglandin, specifically E2 and I2 have on the stomach?

Answer 5

1 - increased gastric acid secretion
2 - increased mucus production
- TOO MUCH NSAIDS WILL STOP BOTH OF THE ABOVE AND CAUSE PEPTIC ULCERS

Question 6

How do NSAIDs lead to renal problems?

Answer 6

• prostaglandins are vasodilators and increase afferent blood flow to kidneys
• NSAIDs inhibit prostaglandins and reduce blood flow causing acute kidney disease

Question 7

Selective COX-2 inhibitors all have what letters at the end of their names?

1 - mab
2 - purinol
3 - olone
4 - coxib

Answer 7

4 - coxib

- core drug is etoricoxib (binds and inhibits COX-II)

Question 8

Selective COX-2 inhibitors all have coxib at the end of their names. What is the core COX-2 inhibitor that we need to know?

1 - naproxen
2 - etoricoxib
3 - rituximab
4 - prednisolone

Answer 8

2 - etoricoxib

Question 9

What are the 3 main effects of NSAIDs?

Answer 9

1 - analgesic
2 - anti-inflammatory
3 - antipyretic

Question 10

What are the 3 key adverse events of selective COX-2 inhibitors?

1 - fertility issues, CVD, increased INR (prothrombin time)
2 - peptic ulcers, CVD, increased INR (prothrombin time)
3 - fertility issues, CKD, increased INR (prothrombin time)
4 - fertility issues, CVD, DVT

INR = international normalised ratio (a measure of blood thickness, high is thin)

Answer 10

1 - fertility issues, CVD, increased INR (prothrombin time)

Question 11

Does paracetamol perform the same 3 functions as NSAIDs?

Answer 11

• no
• only analgesic and antipyretic
• NOT ANTI-INFLAMMATORY

Question 12

Paracetamol is metabolised in the liver and generally is excreted by the kidneys. However, there is a small portion of paracetamol that is metabolised by the enzyme cytochrome P450. This metabolism then leads to a very toxic compound called what?

1 - glucuronidation
2 - N-acetyl-p-benzoquinone imine (NAPQI)
3 - sulfation
4 - CYP450

Answer 12

2 - N-acetyl-p-benzoquinone imine (NAPQI)

Question 13

Paracetamol is metabolised in the liver and generally is excreted by the kidneys. However, there is a small portion of paracetamol that is metabolised by the enzyme cytochrome P450. This metabolism then leads to a very toxic compound called N-acetyl-p-benzoquinone imine or NAPQI. At normal levels of paracetamol there is an enzyme in the liver that is able to neutralise NAPQI. What is this enzyme called?

1 - glutathione
2 - phenyotoin
3 - sulfation
4 - CYP450

Answer 13

1 - glutathione

Question 14

Paracetamol is metabolised in the liver and generally is excreted by the kidneys. However, there is a small portion of paracetamol that is metabolised by the enzyme cytochrome P450. This metabolism then leads to a very toxic compound called N-acetyl-p-benzoquinone imine or NAPQI. At normal levels of paracetamol there is an enzyme in the liver that is able to neutralise NAPQI, called glutathione. What can happen if a patient takes too much paracetamol and how can this become toxic?

Answer 14

• lots of paracetamol needs metabolising, meaning more NAPQI will be produced
• hepatocytes are unable to produce sufficient glutathione to neutralise NAPQI
• NAPQI then damages the liver and can cause liver failure

Question 15

Overdose of paracetamol leads to excessive levels of NAPQI in the liver, which is very toxic and can cause liver failure. What can patients be give to treat this?

1 - metformin
2 - atorvastatin
3 - antibiotic
4 - N-acetylcysteine (IV)

Answer 15

4 - N-acetylcysteine (IV)

- precursor of glutathione, so will neutralise NAPQI

Question 16

What are the 4 core drugs corticosteroids?

Answer 16

1 - Methylprednisolone
2 - Prednisolone
3 - Hydrocortisone
4 - Beclometasone

Question 17

Mechanism of action of corticosteroids?

Answer 17

• same effect that glucocorticoids have
• down-regulate pro-inflammatory genes
• able to inhibit phospholipase A2 and inhibit arachidonic acid, so also COX-I and II

Question 18

Immune cells are able to utilise an enzyme called phospholipase A2 and get it to act on membrane phospholipids in order to create a 20 carbon poly-unsaturated fatty acid called what?

1 - cyclooxygenase
2 - arachidonic acid
3 - C reactive protein
4 - lactate dehydrogenase

Answer 18

2 - arachidonic acid

Question 19

Immune cells are able to utilise an enzyme called phospholipase A2 and get it to act on membrane phospholipids in order to create a 20 carbon poly-unsaturated fatty acid called arachidonic acid (AA). The AA provides a substrate for cyclooxygenase. What 2 things can this then go on to create?

Answer 19

• COX-I

- COX-II

Question 20

Immune cells are able to utilise an enzyme called phospholipase A2 and get it to act on membrane phospholipids in order to create a 20 carbon poly-unsaturated fatty acid called arachidonic acid (AA). The AA provides a substrate for cyclooxygenase. creating COX-I and II. COX-II and I can the produce 3 things, what are they?

1 - prostaglandins, TNF-a, prostacyclin
2 - prostaglandins, prostacyclin, thromboxane
3 - prostaglandins, IL-6, prostacyclin
4 - prostaglandins, thromboxane, IL-1

Answer 20

2 - prostaglandins, prostacyclin, thromboxane

prostacyclin = member of prostaglandins family, inhibits platelet activation and vasodilator

Question 21

What do the terms inducible and constitutive refer to?

Answer 21

• inducible = molecule needs to be activates (COX-II)

- constitutive = molecule is always switched on (COX-I)

Question 22

What is the core category cyclooxgenase-2 inhibitor drug we need to know?

1 - Naproxen
2 - Etoricoxib
3 - Azathioprine
4 - Ciclosporin

Answer 22

2 - Etoricoxib

Question 23

Etoricoxib is the core category cyclooxgenase-2 inhibitor drug that we need to know. What is the mechanism of action of this drug?

Answer 23

• binds and inhibits the COX-2 enzyme