Steroids Flashcards

1
Q

Are steroids stored or synthesized as needed?

A

They are synthesized as needed. The rate of secretion equals the rate of synthesis

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2
Q

Where is aldosterone synthesized?

A

Zona glomerulosa

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3
Q

What are the steps in aldosterone synthesis

A

Cholesterol –> Pregnenolone –> Deoxycorticosterone –> Aldosterone

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4
Q

Where is cortisol synthesized?

A

Zona fasciculata and reticularis

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5
Q

What are the steps in cortisol synthesis?

A

Cholesterol –> Pregnenolone –> Deoxycortisol –> Cortisol

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6
Q

Where is androstenedione synthesized?

A

Zona fasciculata and reticularis

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7
Q

What are the steps in androstenedione synthesis?

A

Cholesterol –> Pregnenolone –> Androstenedione

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8
Q

What hormone regulates the synthesis of cortisol?

A

ACTH

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9
Q

What controls the synthesis of aldosterone? (2 items)

A

Angiotensin II and plasma potassium

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10
Q

How are steroids inactivated in the liver? (3 items)

A
  1. Reduction of A ring
  2. Sulfate conjugation
  3. Glucuronide conjugation
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11
Q

What is the mechanism of adrenocorticosteroid hormones? (5 steps)

A
  1. Binds to cytosolic steroid receptor
  2. Translocated to nucleus
  3. Stimulates transcription of mRNA
  4. Stimulates mRNA directed protein synthesis
  5. Proteins mediate glucocorticoid effects
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12
Q

What effect do glucocorticoids have on gluconeogenesis from liver?

A

Increases

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13
Q

What effect do glucocorticoids have on amino acids in the body?

A

Increased mobilization from skeletal muscle, skin etc.

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14
Q

What effect do glucocorticoids have on plasma glucose levels?

A

Increase

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15
Q

What effect do glucocorticoids have on urinary nitrogen excretion?

A

Increase

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16
Q

What effect do glucocorticoids have on peripheral glucose utilization?

A

Reduces

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17
Q

What are the 6 major effects of glucocorticoids on carbohydrate and protein metabolism?

A
  1. Enhanced liver gluconeogenesis
  2. Stimulation of amino acid mobilization
  3. Increased plasma glucose levels
  4. Increased liver glycogen
  5. Increased urinary nitrogen excretion
  6. Reduced peripheral glucose utilization
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18
Q

What are the 2 major effects of glucocorticoids on lipid metabolism?

A
  1. Redistribution of body fat (moon face, buffalo hump)

2. Stimulation of release of fatty acids from adipose tissue

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19
Q

What enzyme is responsible for the specificity of the glucocorticoid receptor?

A

11B hydroxysteroid dehydrogenase

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20
Q

What substance inhibits 11B hydroxysteroid dehydrogenase?

A

Licorice – glycyrrhizic acid

21
Q

How are the relative affinities of Cortisol and Aldosterone for the mineralocorticoid receptor?

A

The are about the same

22
Q

What kind of affinity does Cortisone have for the mineralocorticoid receptor?

A

none

23
Q

What effects does activation of the mineralocorticoid receptor have on electrolyte and mineral levels? (3 items)

A
  1. Increase in Na reabsorption
  2. Increase in K+ and H+ excretion
  3. Increase in blood pressure
24
Q

What effects do glucocorticoids have on CNS? (2 items)

A
  1. Sleepiness

2. Lability of mood

25
Q

How do glucocorticoids suppress the immune system? (3 items)

A
  1. They affect cell traffic or accumulation. They reduce access of cells to target tissue. They cause redistribution of cells out of the vascular space.
  2. They prevent neutrophil adherence to endothelium
  3. They inhibit action of chemotactic factors.
26
Q

How do glucocorticoids affect macrophage function? (3 items)

A
  1. Inhibit antigen processing
  2. Inhibit binding to Fc receptors
  3. Inhibit synthesis and release of IL-1
27
Q

How do glucocorticoids affect T-lymphocyte function? (4 items)

A
  1. They interfere with macrophage antigen processing
  2. Interfere with action of lymphokines
  3. Absence of IL-1 prevents activation
  4. Reduces IL-2 synthesis
28
Q

How do glucocorticoids exert their anti-inflammatory effects? (4 items)

A
  1. Inhibits signs and symptoms of inflammation by inhibiting immune system
  2. Inhibits arachidonic acid release so synthesis of PGs and Leukotrienes is reduced
  3. Inhibits induction of cyclooxygenase-2 by cytokines
  4. Decreases capillary permeability
29
Q

Why are glucocorticoids used in adrenal insufficiency?

A

steroid replacement therapy

30
Q

When are glucocorticoids used in rheumatoid arthritis?

A

Only in progressive disease and in combination with salicylates, gold salts, and physical therapy.

31
Q

How are steroids administered in osteoarthritis?

A

intra-articular injection

32
Q

What types of allergic diseases are steroids effective for? (5 items)

A
  1. Hay fever
  2. Serum sickness
  3. Drug reaction
  4. Anaphylaxis
  5. Bronchial asthma
33
Q

What are 6 examples of steroid drugs?

A
  1. Cortisol
  2. Dexamethasone (Decadron)
  3. Prednisolone
  4. Fludrocortisone (Florinef)
  5. Aldosterone
34
Q

What is the most potently anti-inflammatory steroid?

A

Dexamethasone

35
Q

What are the first and second most potent steroids for sodium retention?

A
  1. Aldosterone

2. Fludrocortisone

36
Q

What is the major contraindication for steroid use?

A

existing infection - particularly TB

37
Q

What toxic effects are experienced with rapid withdrawal of steroids?

A
  1. Adrenal insufficiency

2. Salt wasting and cardiovascular collapse

38
Q

What adverse effects occur with prolonged steroid therapy?

A
  1. Suppression of pituitary and adrenal function

2. Cushings syndrome

39
Q

What are the symptoms of Cushing’s syndrom? (6 effects)

A
  1. Moon face and buffalo hump
  2. Poor wound healing
  3. Thin skin
  4. Hypertension
  5. Thin extremities
  6. Striae
40
Q

What is Metyrapone?

A

It is a steroid synthesis inhibitor

41
Q

How does Metyrapone work?

A

It blocks 11-beta hydroxylation so synthesis is stopped at 11-desoxycortisol
This causes ACTH levels to rise and stimulate excretion of 17-hydroxycorticoids and 11-desoxycortisol

42
Q

What is the name of a competitive antagonist of the progesterone and glucocorticoid receptor?

A

Mifepristone

43
Q

What is the clinical use of Mifepristone? (2 uses)

A
  1. Termination of pregnancy

2. Treatment of Cushing disease

44
Q

How do Spironolactone and Eplerenone work?

A

They are competitive antagonists of the mineralocorticoid receptor.

45
Q

What are Spironolactone and Eplerenone used for?

A

Diuresis

  1. Treatment of hypertension
  2. Cardiac hypertophy and heart failure
46
Q

What drug is a progesterone receptor agonist, mineralocorticoid antagonist, and androgen receptor antagonist?

A

Drospirenone

47
Q

What is the progesterone receptor antagonism of Drospirenone used for?

A
  1. Used with estrogen to suppress ovulation

2. Used with estrogen as hormone replacement therapy in post-menopausal women

48
Q

What is the advantage of the mineralocorticoid antagonism of Drospirenone used for?

A
  1. Diuresis

2. Antagonizes the salt retaining effects of estrogen