Adrenocorticoids

Question 1

What are examples of glucocorticoids?

Answer 1

-cortisol (natural)
-cortisone
-corticosterone
-prednisone (synthetic)
-prednisolone
-triamcinolone
-betamethasone
-dexamethasone
-fluticasone
-flunisolide

Question 2

What are examples of Mineralcocorticoids?

Answer 2

-aldosterone (natural)
-deoxycorticosterone
-fludrocortisone (synthetic)

Question 3

What are examples of androgens?

Answer 3

DHEA

Question 4

What is transcortin (CBG)?

Answer 4

corticosteroid-binding globulin, protein that binds cortisol in the blood to keep it inactive and as a supply
note that synthetic glucocorticoids do not do this

Question 5

What are the metabolic effects of corticosteroid binding?

Answer 5

-increase blood glucose
-increase amino acids
-increase triglycerides
to maintain energy supplies to critical organs during stress

Question 6

What effect does cortisol have on the HPA axis?

Answer 6

inhibits further release corticotropin releasing hormone (CRH), from the hypothalamus, and adrenocorticotropic hormone (ACTH), from the anterior pituitary gland

Question 7

What can override the feedback inhibition of cortisol?

Answer 7

severe or chronic stress

Question 8

What are the immune system effects of cortisol?

Answer 8

cortisol has anti-inflammatory effects by blocking mediators of inflammation and inflammatory cytokines

Question 9

Describe Cushing’s syndrome/disease

Answer 9

hyper-secretion of glucocorticoids

Question 10

What are the treatment options for Cushings?

Answer 10

-surgery, radiation, chemotherapy (bc typically tumor related)
-cortisol inhibiting drugs

Question 11

What is the main cause of endogenous Cushings?

Answer 11

pituitary ACTH- producing adenoma (responsible for 70% of cases)

Question 12

Describe Addison’s Disease

Answer 12

hypocortisolism, adrenal insufficiency

Question 13

What is the cause of PRIMARY adrenal insufficiency?

Answer 13

lack of glucocorticoids and mineralocorticoids due to autoimmune reactions that destroy the adrenal cortex, infection, or surgical removal of adrenal glands

Question 14

What is the cause of SECONDARY adrenal insufficiency?

Answer 14

lack of ACTH due to hypothalamic or pituitary disorders or abrupt ceasing of long-term glucocorticoid treatment

Question 15

What is the treatment for Addisons?

Answer 15

replacing/substituting glucocorticoids and mineralocorticoids

Question 16

What is the function of 11beta-HSD 1 in the liver?

Answer 16

11-keto is converted to 11-OH on glucocorticoids, 11-OH is necessary for action, drugs such as prednisone and cortisone require this activity to be active because they are prodrugs

Question 17

What is the function of 11beta-HSD 2 in the liver?

Answer 17

11-OH is converted to 11-keto on glucocorticoids (except dexamethasone) to inactivate the drug

Question 18

What is the indication for oral hydrocortisone?

Answer 18

adrenal insufficiency

Question 19

What are common uses of glucocorticoids?

Answer 19

-asthma and COPD
-rheumatoid arthritis
-skin diseases
-allergies
-organ rejection

Question 20

What glucocorticoids are inhaled to treat asthma?

Answer 20

-fluticasone
-beclomethasone
-budesonide
-flunisolide
-triamcinolone

Question 21

What are the precautions of glucocorticoids?

Answer 21

-adjusting doses= high doses may lead to iatrogenic Cushings
-hyperglycemia
-muscle wasting
-fat deposition
-hidden infection

Question 22

What are the contraindications for glucocorticoid treatment?

Answer 22

-hypertension, heart disease
-infection
-diabetes
-osteoporosis
-glaucoma
-peptic ulcer

Question 23

What is the function of glucocorticoids?

Answer 23

-facilitate stress response, both physical and emotional
-promote metabolism (glucose utilization, lipid metabolism, protein utilization)
-inhibit immune function and inflammation

Question 24

What is the function of mineralocorticoids?

Answer 24

control electrolyte balance (sodium retention, potassium excretion, fluid volume)

Question 25

Describe the function of aldosterone (mineralocorticoid)

Answer 25

receptors located in the kidney, regulates Na+ reabsorption and K+ and H+ excretion

Question 26

What factors can impact aldosterone regulation/levels?

Answer 26

-renin-angiotensin system = increase aldosterone -potassium ion loading= increase aldosterone -ACTH= increase aldosterone

Question 27

How does renin effect aldosterone?

Answer 27

renin secretion by juxtaglomerular cells is regulated by baroreceptors specifically senses of decreased extracellular fluid volume (low BP) -> renin converts angiotensin to angiotensin I which is then converted to angiotensin II by ACEs, angiotensin II stimulates aldosterone synthesis

Question 28

What is the indication of Fludrocortisone?

Answer 28

mineralocorticoid agonist, treats hypoaldosterone (Addisons Disease)

Question 29

What are the adverse effects of mineralocorticoid agonists?

Answer 29

hypokalemia and hypertension

Question 30

What drugs are mineralocorticoid antagonist?

Answer 30

spironolactone and eplerenone

Question 31

Describe Spironolactone

Answer 31

-mineralocorticoid receptor blocker -treat symptoms of hyperaldosteronism, hypertension -also androgen receptor blocker so can treat hirsutism in women or acne

Question 32

What are the adverse effects of mineralocorticoid antagonists?

Answer 32

hyperkalemia, cardiac arrhythmia, menstrual abnormalities

Question 33

Describe Metyrapone

Answer 33

-inhibit 11beta-hydroxylase -decreased synthesis of both cortisol and aldosterone -only drug available for pregnant women with Cushings -may also be used for diagnostic test for adrenal function

Question 34

Describe Mifepristone

Answer 34

-high affinity glucocorticoid and progesterone antagonist -used in inoperable ACTH- secreting tumor

Question 35

What drugs are adrenocortical inhibitors?

Answer 35

-mitotane -metyrapone -osilodrostat -aminoglutethimide -ketoconazole -mifepristone

Question 36

What is the main use of adrenocortical inhibitors?

Answer 36

Cushings