Corticosteroids Flashcards

1
Q

What are the 2 main actions of Corticosteroids?

A
  1. Anti-Inflammatory

2. Immune Suppression

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2
Q

What are the 2 main actions of Corticosteroids?

A
  1. Anti-Inflammatory

2. Immune Suppression

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3
Q

What are the 4 ways that Corticosteroids carry out their effects?

A
  • Decrease prostaglandins/leukotrienes
  • Decrease immune cells and cytokines
  • Decrease neutrophil/macrophage transmigration
  • Decrease cell adhesion molecules
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4
Q

What are general uses of Corticosteroids?

A

Inflammation

Immune and Allergic Disorders

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5
Q

What is the treatment for Adrenal Insufficiency and Congenital Adrenal Hyperplasia?

A

Hydrocortisone + Fludrocortisone

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6
Q

Corticosteroids bind to transcription factors and cause what to occur?

A
  • HSP90 dissociates

= > Altered gene expression

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7
Q

Cortisol (glucocorticoid) and Aldosterone (mineralcorticoid) have what in common?

A

SAME affinity for the MR (mineralcorticoid receptor)

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8
Q

Aldosterone, Cortisol, Testosterone and Estradiol are all created from what precursor?

A

Cholesterol

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9
Q

17-hydroxyprogesterone creates what 3 endogenous corticosteroids?

A

Cortisol
Testosterone
Estradiol

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10
Q

Cortisol vs Cortisone - which is the active form?

A

Cortisol

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11
Q

What enzyme takes Cortisol to Cortisone and what is the end result/

A

11-beta HSD2

=> INACTIVATION

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12
Q

What enzyme takes Cortisone to Cortisol and what is the end result?

A

11-beta HSD1

=> ACTIVATION

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13
Q

What are the 3 active forms of Cortisol?

A

Cortisol
Corticosterone
Prednisolone

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14
Q

What are some adverse effects of Corticosteroids?

A
Infections
Osteoporosis
Hyperglycemia
Hypertension
Skin thinning
HPA insufficiency
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15
Q

Should you give Glucocorticoids chronically?

A

NO

– give shortest dose for shortest time possible

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16
Q

What are the corticosteroid effects on carbohydrate metabolism?

A
  • Increased gluconeogenesis
  • Increased glycogen synthesis
  • DECREASED GLUCOSE UPTAKE
    = Hyperglycemia
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17
Q

What are the corticosteroid effects on lipid metabolism?

A
  • Increased lipogenesis
  • Increased lipolysis
    = Change in fat distribution
18
Q

What are the corticosteroid effects on protein metabolism?

A
  • Decreased protein synthesis

= Myopathy and muscle wasting

19
Q

What are 2 known inhibitors of 11-beta HSD2?

A

Glycyrrhizin

Carbenoxolone

20
Q

What are 2 known inhibitors of 11 - beta HSD2?

A

Glycyrrhizin

Carbenoxolone

21
Q

What do inhibitors of 11-beta HSD2 cause to occur?

A
  • INCREASED Cortisol
  • Increased (+) of the MR 2
  • Increased Na+ and H20 retention with K+ loss
    = INCREASED BP
22
Q

What do Glycyrrhizin and Carbenoxolone cause to occur?

A
  • (-) 11-beta HSD2
  • INCREASED CORTISOL
  • Increased (+) of MR2 receptor
  • Increased Na+ and H20 retention with K+ loss
    = INCREASD BP
23
Q

What are the short-medium acting glucocorticoids and how long do they act?

A

Cortisol
Cortisone
= < 12 hours

24
Q

What are the short-medium acting glucocorticoids and how long do they act?

A

Cortisol
Cortisone
= < 12 hours

25
What are the 4 intermediate acting glucocorticoids?
Prednisone Prednisolone Methylprednisolone Triamcinolone
26
What are the 4 intermediate acting glucocorticoids?
Prednisone Prednisolone Methylprednisolone Triamcinolone
27
What are the 2 long acting glucocorticoids and how long do they act?
Betamethasone Dexamethasone = > 36 hours
28
What are the 2 long acting glucocorticoids and how long do they act?
Betamethasone Dexamethasone = > 36 hours
29
Moving from short acting to long acting glucocorticoids, which have the highest anti-inflammatory activity?
Long acting
30
Mitodane treats?
Adrenal gland cancer
31
Prednisolone is a ____ and it (+) what receptor?
Corticosteroid | (+) GR
32
What is a Glucocorticoid Receptor ANTAGONIST?
Mifepristone
33
What is Mifepristone?
Glucocorticoid Receptor ANTAGONIST
34
What is a synthetic Mineralcorticoid used to act at the kidney and affect salt/water balance?
Fludrocortisone
35
What are the effects of using Fludrocortisone?
(Mineralcorticoid) | = Na+ and H20 retention with K+ and H+ excretion
36
Metyrapone can diagnose? It can treat?
Diagnose Adrenal Insufficiency | Treats Cushing Syndrome
37
What are 2 Mineralcorticoid Receptor ANTAGONISTS?
Spironolactone | Eplerenone
38
What are 3 adverse effects of using the Mineralcorticoid Receptor ANTAGONISTS and what are they?
Spironolactone Eplerenone => Gynecomastia, Hyperkalemia, increased creatinine
39
What is a glucocorticoid synthesis inhibitor?
Ketaconazole
40
What drug can (-) steroid hormone synthesis and what are 2 adverse effects it has?
Ketaconazole | - hepatic dysfunction and drug interactions