Adrenocorticoids Flashcards

1
Q

What are examples of glucocorticoids?

A

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

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2
Q

What are examples of Mineralcocorticoids?

A

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

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3
Q

What are examples of androgens?

A

DHEA

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4
Q

What is transcortin (CBG)?

A

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

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5
Q

What are the metabolic effects of corticosteroid binding?

A

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

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6
Q

What effect does cortisol have on the HPA axis?

A

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

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7
Q

What can override the feedback inhibition of cortisol?

A

severe or chronic stress

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8
Q

What are the immune system effects of cortisol?

A

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

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9
Q

Describe Cushing’s syndrome/disease

A

hyper-secretion of glucocorticoids

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10
Q

What are the treatment options for Cushings?

A

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

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11
Q

What is the main cause of endogenous Cushings?

A

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

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12
Q

Describe Addison’s Disease

A

hypocortisolism, adrenal insufficiency

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13
Q

What is the cause of PRIMARY adrenal insufficiency?

A

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

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14
Q

What is the cause of SECONDARY adrenal insufficiency?

A

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

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15
Q

What is the treatment for Addisons?

A

replacing/substituting glucocorticoids and mineralocorticoids

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16
Q

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

A

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

17
Q

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

A

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

18
Q

What is the indication for oral hydrocortisone?

A

adrenal insufficiency

19
Q

What are common uses of glucocorticoids?

A

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

20
Q

What glucocorticoids are inhaled to treat asthma?

A

-fluticasone
-beclomethasone
-budesonide
-flunisolide
-triamcinolone

21
Q

What are the precautions of glucocorticoids?

A

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

22
Q

What are the contraindications for glucocorticoid treatment?

A

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

23
Q

What is the function of glucocorticoids?

A

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

24
Q

What is the function of mineralocorticoids?

A

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

25
Q

Describe the function of aldosterone (mineralocorticoid)

A

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

26
Q

What factors can impact aldosterone regulation/levels?

A

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

27
Q

How does renin effect aldosterone?

A

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

28
Q

What is the indication of Fludrocortisone?

A

mineralocorticoid agonist, treats hypoaldosterone (Addisons Disease)

29
Q

What are the adverse effects of mineralocorticoid agonists?

A

hypokalemia and hypertension

30
Q

What drugs are mineralocorticoid antagonist?

A

spironolactone and eplerenone

31
Q

Describe Spironolactone

A

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

32
Q

What are the adverse effects of mineralocorticoid antagonists?

A

hyperkalemia, cardiac arrhythmia, menstrual abnormalities

33
Q

Describe Metyrapone

A

-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

34
Q

Describe Mifepristone

A

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

35
Q

What drugs are adrenocortical inhibitors?

A

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

36
Q

What is the main use of adrenocortical inhibitors?

A

Cushings