CPTP 3.15 - Drugs in Inflammation, Allergy and Pain 2

Question 1

Describe the basic function of corticosteroids?

Answer 1

Bind to specific receptors in the cytoplasm - corticosteroid/receptor complex dimerises and is transported to the nucleus
Complex binds to steroid responsive element on DNA = DNA synthesis/inhibition

Question 2

Name an endogenous glucocorticoid and describe their 5 functions?

Answer 2

Hydrocortisone

1. Increase nutrient availability
2. Increase resistance to stress
3. Anti-inflammatory action
4. Immunosupressive actions
5. Alter the release of other hormones

Question 3

How do glucocorticoids increase nutrient availability?

Answer 3

Increase gluconeogenesis - decrease glucose uptake by cells/decrease glycogen storage
Decreased protein stores in all parts of body (except liver)
Decreased protein synthesis

Question 4

How do glucocorticoids increase resistance to stress?

Answer 4

By increasing glucose stores the body is able to use this energy to fend off stress

Question 5

How do glucocorticoids have anti-inflammatory effects?

Answer 5

1. Up-regulate the expression of ANTI-inflammatory proteins
2. Down regulate the expression of PRO-inflammatory proteins
3. Induce annexin.1 (lipocortin1)
4. Inhibit COX expression

Question 6

How do glucocorticoids up-regulate anti-inflammatory proteins?

Answer 6

Up-regulate 1kB - which inhibits the activation of NFkB (pro-inflammatory) and IL-4 and IL-10 and TGF-B

Question 7

What happens when glucocorticoids induce anexin.1 (lipocortin.1)?

Answer 7

Inhibits leukocyte inflammatory effects

Inhibits phospholipase A (eicosanoid pathway)

Question 8

What vascular effects do glucocorticoids have?

Answer 8

Reduce vasodilation

Decrease fluid exudate

Question 9

What cellular effects go glucocorticoids have?

Answer 9

Acute inflammation = decrease the number and activity of leukocytes
Chronic infection = decrease the activity of mononuclear cells
RAPID decrease of degranulation of mast cells/basophils
Decrease the generation of cytokines by macrophages and the concentration of complement within the blood

Question 10

Name two short acting glucocorticoids?

Answer 10

Hydrocortisone

Fludrocortisone

Question 11

Name two intermediate acting glucocorticoids?

Answer 11

Prednisolone

Methylprednisolone

Question 12

Name one long acting glucocorticoids?

Answer 12

Betamethasone

Question 13

Name a condition in which the patient has adrenocorticle insufficiency?

Answer 13

Addison’s disease - NO corticosteroids produced

Question 14

How is cortisol metabolised?

Answer 14

Phase.1 reduction by 11-Beta-hydroxysteroid dehydrogenase 2 (11B-HSD2) into inactive metabolites which are subsequently metabolised

Question 15

Name five side-effects associated with corticosteroids?

Answer 15

Hypertension
G.I disease
Muscle tissue wastage 
Osteoporosis
Hyperglycaemia

Question 16

Name the main endogenous mineralocorticoid and where does it act?

Answer 16

Aldosterone

Kidney tubules and collecting ducts

Question 17

Name the two functions mineralocorticoids have?

Answer 17

Increased reabsorbtion of Na+ and HCO3- and H2O = Increased blood volume and blood pressure
Decreased reabsorption of K+ - can lead to hypokalaemia and alkalosis

Question 18

Name a condition in which there is XS aldosterone (mineralocorticoid) secretion and state its effects?

Answer 18

Conn’s disease - Na+/H2O retension - Increased BP

Hypertension//alkalosis//hypokalaemia

Question 19

Name a condition in which there is deficient secretion of aldosterone (mineralocorticoid) and state its effects?

Answer 19

Decreased ECF and decreased K+ excretion = Hyperkalaemia/acidosis/dehydration