Anti-Inflammatory agents

Question 1

What is an NSAID?

Answer 1

Non-Steroidal Anti-Inflammatory Drug

Question 2

How are membrane phospholipids converted into leukotrienes?

Answer 2

Membrane phospholipids get converted into arachidonic acid by phospholipase A2
Arachidonic acid is then broken down into leukotrienes by Lipoxygenase

Question 3

How are membrane phospholipids converted into prostaglandins?

Answer 3

Membrane phospholipids get converted into arachidonic acid by phospholipase A2
Arachidonic acid is then broken down into different prostaglandin classes by Cyclo-oxygenase (COX) enzyme

Question 4

Which enzyme is targeted by corticosteroids?

Answer 4

Phospholipase A2 preventing the formation of arachidonic acid

Question 5

What are some examples of glucocorticosteroids?

Answer 5

Hydrocortisone
Betamethasone
Prednisolone

Question 6

Which enzyme is targeted by NSAIDs?

Answer 6

The Cyclo-oxygenase enzyme (COX)

Question 7

What are some examples of NSAIDs?

Answer 7

Aspirin, Ibuprofen, Naproxen and celecoxib

Question 8

Where are steroid hormones produced?

Answer 8

In the adrenal gland that sit on the kidneys

Question 9

What are the 2 types of corticosteroid receptors?

Answer 9

Glucocorticoid receptors
Mineralocorticoid receptors

Question 10

How do steroid drugs affect the cell?

Answer 10

Drugs pass through the plasma membrane
Here, they bind to glucocorticoid receptors
These allow passage into the nucleus where they bind to GRE (Glucocorticoid Response Elements) on DNA

Question 11

What are the main therapeutic effects of glucocorticoid drugs?

Answer 11

Pain relief
Anti-allergy
Immunosupression
Anti-inflammatory
Decreased blood vessel permeability

Question 12

What side effects can glucocorticoid drugs have on muscles?

Answer 12

Increased risk of myopathies causing muscle weakness

Question 13

What side effects can glucocorticoid drugs have on bone?

Answer 13

Can cause osteoporosis
Can cause aseptic necrosis of the femur

Question 14

What side effects can glucocorticoid drugs have on the skin?

Answer 14

Causes skin thinning

Question 15

What side effects can glucocorticoid drugs have on metabolism?

Answer 15

Hyperglycaemia
Weight gain
Fluid retention
Cushingoid appearance - fat build up on the sides of the face

Question 16

What side effects can glucocorticoid drugs have on the CNS and adrenal system?

Answer 16

HPA insufficiency
Neuropsychiatric disorders

Question 17

What side effects can glucocorticoid drugs have on the eyes?

Answer 17

Cataracts
Glaucoma

Question 18

What side effects can glucocorticoid drugs have on the cardiovascular system?

Answer 18

Hypertension

Question 19

What side effects can glucocorticoid drugs have on the gastrointestinal system?

Answer 19

Increased stomach acid production

Question 20

What do inhaled steroids increase the risk of thrush?

Answer 20

Steroids can be deposited in the oropharynx causing local immunosuppression, allowing the growth of Candida albicans

Question 21

What is CRH?

Answer 21

Corticotrophin Releasing Hormone

Question 22

What causes the release of CRH and where is it released from?

Answer 22

The hypothalamus, stimulated by stress or the Circadian rhythm

Question 23

What does CRH do?

Answer 23

It stimulates the anterior pituitary gland to release ACTH

Question 24

What is ACTH?

Answer 24

AdrenoCorticoTrophic Hormone

Question 25

What does ACTH do?

Answer 25

It stimulates the release of glucocorticoids from the adrenal glands

Question 26

What is the HPA axis?

Answer 26

Stress/circadian rhythm Stimulates hypothalamus Releases CRH Stimulates anterior pituitary gland Releases ACTH Stimulates adrenal glands Releases glucocorticoid steroids Stimulates hypothalamus to reduce CRH production Regulates steroid hormone levels

Question 27

How do glucocorticoid drugs cause HPA insufficiency?

Answer 27

Addition of glucocorticoid steroids into the blood stream stimulates the hypothalamus to reduce CRH levels After prolonged use (3 weeks) the adrenal glands no longer produce glucocorticoids on their own, leading to adrenal insufficiency

Question 28

What would happen if steroids were stopped instantly, instead of slowly decreased?

Answer 28

The adrenal glands would no longer produce endogenous glucocorticoids, so the person would fall into a coma

Question 29

What are the 2 types of COX enzyme?

Answer 29

COX-1 and COX-2

Question 30

What is the function of COX-1?

Answer 30

COX-1 is always present in low levels , within the body and involved in platelet regulation, kidney function and regulation of stomach acid

Question 31

What is the function of COX-2?

Answer 31

COX-2 is an inducible enzyme that, when activated, causes inflammation, leading to pain, heat and swelling

Question 32

What are some common side effects of NSAIDs?

Answer 32

Adverse GI effects (Abdominal bleeding) Reduced renal function in predisposed patients) Hypertension

Question 33

What is misoprostol and why is it combined with NSAIDs?

Answer 33

Misoprostol is a synthetic prostaglandin medication When bound to an NSAID, it can prevent gastric bleeding and discomfort by regulating the stomach lining which can be prevented by the NSAID alone

Question 34

What is a DMARD?

Answer 34

Disease Modifying Anti-Rheumatic Drug

Question 35

What are some examples of DMARDs?

Answer 35

Methotrexate Sulfasalazine

Question 36

What are the advantages of DMARDs over NSAIDs?

Answer 36

They can be used for longer periods of time

Question 37

What are some examples of immunosuppressant drugs?

Answer 37

Ciclosporin Azathioprine Tacrolimus Mycophenolate mofetil

Question 38

What are some examples of biological immunosuppressant?

Answer 38

Infliximab Rituximab

Question 39

What are the 2 types of antihistamines and what are some examples of each?

Answer 39

1st generation (Sedating) - Promethazine, Cyclizine, Chlorphenamine 2nd generation (Non-sedating) - Fexofenadine, loratadine