Adrenocorticosteroids 2.1

Question 1

Glucocorticoid Agonists (6)

Answer 1

1) Prednisone
2) Hydrocortisone
3) Dexamethasone
4) Beclomethasone
5) Triamcinolone
6) Methylprednisolone

Question 2

Mineralocorticoid Agonists (2)

Answer 2

1) Aldosterone

2) Fludocortisone

Question 3

Glucocorticoid Antagonist

Answer 3

Mifepristone

Question 4

Mineralocorticoid Antagonist

Answer 4

Sprionolactone

Question 5

Glucocorticoids peak release time at?

Answer 5

6 am

Question 6

Hyrodrocortisone also known as?

Answer 6

Cortisol

Question 7

MOA of Glucocorticoid agonist?

Answer 7

Binds a cytoplastmic receptor forming a complex that enters the nucleus and alters gene regulation (GRE) producing a specific tissue response

Question 8

Metabolic effects of Cortisol (3)

Answer 8

1) Gluconeogenesis and glycogen synthesis which leads to increase serum glucose levels (leading to stimulation of insulin release & inhibiting uptake by muscle cells)
2) Stimulates lipolysis ( leading to fat deposition and redistribution… Cushings)
3) Stimulates protein catabolism

Net result: maintain adequate glucose supply to brain.

Question 9

Catabolic effects of Cortisol (3)

Answer 9

1) In addition to protein catabolism, cortisol also has effects in lymphoid and connective tissue, muscle, peripheral fat and skin (wasting occurs at high concentrations)
2) Osteoporosis
3) Children -> growth retardation

Question 10

Immunosuppressive effects of Cortisol on Leukocytes (3)

Answer 10

1) Increased neutrophils (increased influx into blood & decrease migration from blood vessels)
2) Decreased lymphocytes (T & B cells), monocytes, eosinophils and basophils (movement from vascular bed to lymphoid tissue)
3) Vasoconstriction due possibly to suppression of mast cell degranulation (decrease histamine release and capillary permeability)

Question 11

Anti-inflammatory effects of Cortisol (3)

Answer 11

1) Inhibition of phospholipase A2 (through induction and activation of annexin I) which blocks arachidonic acid release
2) Cyclooxygenase-2 synthesis is reduced (through inhibition of NF-kB)
3) Induction of MAPK phosphatase I (inhibits proinflammatory signaling pathways)

Question 12

“Other” effects of Cortisol (7)

Answer 12

1) CNS - behavioral changes (insomnia -> depression)
2) Increased intracranial pressure
3) Supression of release of ACTH, GH, TSH, LH
4) Peptic ulcers
5) Increase platelets & RBC’s
6) Renal function
7) Development of Fetal Lungs

Question 13

Prednisone is a prodrug which is rapidly converted to what?

Answer 13

Prednisolone

Question 14

What is important to know regarding the PK of Beclomethasone?

Answer 14

Short 1/2 life & penetrates airway mucosa (low systemic toxicity)

Question 15

Synthetic Glucocorticoids which are aerosols

Answer 15

1) Beclomethasone

2) Triamcinolone

Question 16

Mineralocorticoid Effects

Answer 16

1) Promote Na reabsorption from Renal Tubule

2) Promote K and H excretion