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Pharmacology > Adrenal Hormones and their Antagonists > Flashcards

Adrenal Hormones and their Antagonists Flashcards

1
Q

What are the 3 types of steroid hormones produced by adrenal cortex?

A

mineralocorticoids (salt)
glucocorticoids (sugar)
androgens (sex0

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2
Q

What is the major form of adrenal adrogens?

A

Dehydroepiandrosterone (DHEA-S)

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3
Q

What is the first FDA-approved medication contianing DHEA & what is its use?

A

DHEA or Prasterone

Vaginal inserts as treatment of vulvovaginal atrophy —> Decline in Estrogen production after menopause

Tx painful sexual itnercourse due to dryness and thinning of vaginal tissue

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4
Q

What are the 2 kinds of endogenous corticosteroids?

A

Mineralococrticoids and Glucocorticoids

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5
Q

What is the site of synthesis of GLucocorticoids & Mineralocorticoids?

A

Mineralocorticoids = Glomerulosa
Glucocorticoids = Fasciculata

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6
Q

Whata re the naturally-occuring/Endogenous hormones of these corticosteroids?

A

Mineralocorticoids = Aldosterone
Glucocorticoids = Cortisol

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7
Q

What are synthetic analogs/Exogenous corticosteroids?

A

Mineralocorticoids = Fludrocortisone
Glucocorticoids = Prednisone, Prednisolone, Betamethasone, Dexamethasone

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8
Q

What ist the precursor of Aldosterone?

A

11-Deoxycorticosterone

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9
Q

What stimulates release of Aldosterone & Cortisol?

A

Aldosterone = Angiotensin II, HIGH levels of serum K+, ACTH

Cortisol = ACTH

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10
Q

What is the MOA of Aldosterone?

A

Binds to mineralocorticoid receptor (nuclear) in DCT & CT of kidneys —> receptor activation, gene transcription, protein synthesis —> INC expression of Na/K ATPase & ENaC

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11
Q

What is the MOA of Cortisol?

A

Binds to glucocorticoid receptors —> receptor activation, gene transcription, protein synthesis —> effects

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12
Q

What are the effects of Aldosterone & Cortisol?

A

Aldosterone = Salt-retention, Excretion of K, H, SEcretion of bicarbonate

Cortisol = Gluconeogenesis, Glycogenesis, Muscle protein catabolism, Lipolysis, Fat redistribution, Anti-inflammatory & immunosuppressive effects: FTLM

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13
Q

What hormone stimulates secretion of Aldosterone?

A

Angiotensin II

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14
Q

What happens to the acid base balance once Aldosterone has excessive excretion of K & H

A

Hypokalemia
Metabolic alkalosis

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15
Q

What is the only synthetic minteralocorticoid? WHat is its clinical use?

A

FludroCORTISONE

Use: Adrenocortical insufficiency assoc w/ mineralocorticoid deficiency

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16
Q

What are the 3 mechanisms of neuroendocrine control?

A

Episodeic secretion & circadian rhythm of ACTH
Stress responsiveness of hypothalamic-pituitary-adrenal axis
Feedback inhibition of ACTH secretion by cortisol

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17
Q

What is the only steroid that participates in the HPA axis?

A

Cortisol

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18
Q

What are the 2 components of stress response

A

Fast response: EPI or Adrenaline
Slow response: HPA Axis (Cortisol)

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19
Q

What can happen if there is chronic exposure to stress?

A

Maladaptive stress response

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20
Q

How does Cortisol suppress inflammatory and immune response?

A
  1. Inhibits migration of leukocytes to the site of the inflammation
  2. Inhibits function of macraphage, production of inflam cytokines
  3. INhibits inflam mediators (Eicosanoid)
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21
Q

Does cortisol have mineracorticoid acitivity?

A

Yes, but minimally since if has 11-B-hydroxysteroid dehydrogenase type 2

22
Q

What is the best way to administer synthetic glucocorticoids?

A

Oral administration (faster, complete)

23
Q

What is the inactive form of Cortisol?

A

Cortisone
That’s why prednisone is converted to Prednisolone (active form)

24
Q

Aside from Fludrocortisone, what is another corticosteroid?

A

Hydrocortisone

Hydrocortisone + Cortisone = shortest half-life (least potent)

25
Q

Is Fludrocortisone also used for anti-inflammatory conditions?

A

NO, its only indications is for mineralocorticoid deficiency

26
Q

What are the non-adrenal uses of Glucocorticoids?

A

Nasal spray for allergic rhinitis
Budesonide inhaler for asthma
Topical glucocorticoids for dermatitis
Ophthalmic solns for eye diseases
Enema and rectal suppositories for inflammaotry bowel dis (Crohn’s & ulcerative colitis)

27
Q

What is the purpose of Prednisone?

A

Anti-inflammatory effect + Immunosuppression
DEC Ca absorption

28
Q

In what conditions is Prednisone used?

A

RA, SLE, Graves opthalmopathy, Subacute thyroiditis, Nephrotic syndrome, Leukemia and Lymphoma

Tx for translant rejection

Tx for hyeprcalcemia

29
Q

What is the purpose of Dexamethasone?

A

Antiemetic
DEC permeability of BBB to Na —> reduce cerebral edema
Surfacntant production for FLM

30
Q

What are the 2 important glucocorticoids used for non-adrenal conditions?

A

Prednisone
Dexamethasone

31
Q

What are the 3 main adrenal uses of glucocorticoids?

A

Chrousos syndrome
Hormone replacement
Congenital adrenal hyperplasia

32
Q

What condition has a decreased senstiivity to glucocorticoids & INC ACTH resulting to excess production of mineraolcorticoid & Androgen effects?

A

Chrousous syndrome

33
Q

What is the treatment for Chrousos syndrome?

A

Dexamethasone —> suppresses ACTH

34
Q

What hormone replacement is given in Congenital adrehnal hyperplasia, chronic adrenal insufficiency, maintenance after adrenalactomy?

A

Hormone replcement of
Hydrocortisone +/- Fludrocortisone

35
Q

What hormone replacement therapy is given in acute adrenal insufficiency during and immediately after adrenalectomy?

A

High dose IV hydrocortisone

36
Q

What enzyme is deficient in congenital adrenal hyperpllasia?

A

21-a-hydroxylase

37
Q

What is the tx for congenital adrenal hyperplasia?

A

Hydrocortisone

38
Q

What is the glucocorticoid of choice in pregnancy bcos it readily crosses the placenta?

A

Dexamtheosone

39
Q

What are the uses of dexamethasone in preggos?

A
  • at risk of preterm labor (<34 wks)
  • CAH
  • Respiratory distress syndrome
  • genital abnormalities
40
Q

How should dexamethasone be administred to mothers at risk of preterm labor?

A

Short-course of Dexamethasone to accelerate fetal lung maturation

41
Q

What do we do if parents are both carriers of CAH?

A

If fetus is female, they are more at risk of developing genital abnormalities as early as 1st trim. Mothers should start on Dexamethasone as soon as pregnancy is confirmed.

42
Q

What condition results from chronic exposure to excess glucocorticoids?

A

Cushing syndrome

43
Q

What test is done to detect Cushing syndrome?

A

Dexamethasone suppression test

44
Q

What is the difference between Cushing & Pseudo-Cushing syndrome?

A

Pseudo-Cushing = caused by alcohol or psychiatric disorders

45
Q

How do you localize tumor that causes Cushing syndrome?

A

tumor is @ APG —> suppress stimulation of Cortisol secretion

tumor @ adrenal gland —> suppress pitutary secretion of ACTH

tumor is ectopic & ACTH source is external —> Total ACTH will be high & not respond to the suppression effect of DXM

46
Q

What can happen if Corticosteroids are administered >2 wks?

A

Iatrogenic Cushing syndrome
Adrenal suppression

47
Q

What are the clin manifesations of Cushing syndrome?

A

IMPORTANT:
Blindness, weight gain, at risk for DM, short stature, HTN, HTN, HF, Psychosisis, Osteoporosis, Peptic ulcer (H. Pylori)

48
Q

What are certain req before administreing Corticosteroids?

A

Px should be on high-protein & K enriched diets
Receive adequate doses of Vit D
Consider co-morbidities
Obtain CXR & tuberculin test

49
Q

What are the 2 major grps of Adrenocortical antagonists?

A

Synthesis inhibitors
Receptor antagonists

50
Q

What are the diff Adrencocortical antagonists, synthesis inibitors?

A

Aminoglutethimide
Ketoconazole
Abiraterone
Trilostane
Etomidate
Metyrapone
Mitotane

51
Q

What are the diffrent Adrencocortical antagonists, receptor antagonists?

A

Mifepristone
Spironolactone
Eplerenone

Pharmacology (19 decks)

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