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Flashcards in Steroids Deck (21):
1

What are the two goals of steroid administration

Replacement therapy for primary adrenal insufficiency- glucocorticoid and mineralcorticoids must be replaced

Suppres inflammation and immune responses

2

What are the two classes of glucocorticoids

11-hydroxy-glucocorticoids (intrinsic activity)

11-keto-glucocorticoids ( inactive)

3

What enzyme activates 11-keto glucocorticoids

11B-HSD 1

* prednisone to prednisolone
* cortisone to cortisol

4

The DOA of glucocorticoids depends on what four variables

Protein binding

affinity of the drug for 11-HSD 2 (in kidney)

lipophilicity of drug

affinity of drug for glucocorticoid receptor

5

What syndrome is associated with glucocorticoid administration

Iatrogenic Cushing's syndrome

6

What are the S/S of Iatrogenic Cushing's syndrome

Infection
Hyperglycemia
Osteoporosis
Muscle weakness
Periperal wasting with central obesity
Fat redistribution-Moon face/buffalo hump
Peptic ulcers
Acute psychosis/depression

7

Acute withdrawal of glucocorticoid tx can result in

adrenal insufficiency-Addison's disease

8

What is the typical Stress dose replacement

hydrocortisone 100 mg before, during, and after surgery

9

Cautious administration of glucocorticoids should be used in which patients

Heart disease/HTN/HF
DM
Infectious disease processes

10

Name the short acting synthetic steroids and their relative potencies with respect to glucocorticoid and mineralcorticoid activity

Gluco/Mineral
Hydrocortisone (cortisol) 1.0/1.0
* Cortisone 0.8/0.8
Prednisone 4.0/0.3
Prednisolone 4.0/0.3
* Methylprednisolone 5.0/0.25

11

Name the intermediate-acting synthetic steroids and it's relative potencies with respect to gluc/minercorticoid activity

Gluco/Mineral
Triamcinolone 5.0/0

12

Name the long- acting synthetic steroids and their relative potencies with respect to glucocorticoid and mineralcorticoid activity

Gluco/Mineral
Dexamethasone 30.0/0
Betamethasone 40/0

13

Name the inhaled glucocorticoids

Fluticasone
Beclomethasone
Flunisolide
Triamcinolone

14

What are the clinical uses and SE associated with glucocorticoid receptor agonists

clinical uses: inflammation, autoimmune disease, and prevention of transfusion rxn

SE- Iatrogenic Cushing's syndrome

15

What are the clinical uses and SE associated with the inhaled steroids

Clinical uses- asthma, allergic rhinitis

SE- oropharyngeal candidiasis

16

Can aldosterone be given as a tx for hypoaldosteronism

No, because it has a high hepatic first-pass metabolism of 75%

17

What is the main drug for replacing mineracorticoids and it's SE

Fludrocortisone

SE- HTN, hypokalemia, and cardiac failure

18

What are the three different classes of adrenal steroid INHIBITORS

Inhibitors of Adrenocorticol hormone synthesis

Glucocorticoid receptor antagonists

mineralocorticoid receptor antagonists

19

Name the inhibitors of adrenocortical hormone synthesis and the pathway it effects

Mitotane effects salt, sugar, and sex s/s/s

Aminoglutethimide effects s/s/s

Ketoconazole decreases male sex hormones but increases all other pathways

Metyrapone 11B-hydroxylase inhibitor which effects cortisol synthesis

Trilostane effects both cortisol and aldosterone synthesis

SE: Hypercholesterolemia, gynecosmastia, N/D, pruitus, CNS depression

20

Name the glucocorticoid receptor antagonists and the pathways effected

Mifepristone (RU-486) effects progesterone receptors (induces abortion) and glucocorticoid receptors ( treats life-threatening steroid levels)

*SE- HYPOTHYROIDISM (inhibits T4 to T3 conversion)

21

Name the mineralcorticoid receptor antagonists and the pathways effected

Sprironolactone competes with aldosterone to lower bp and tx HTN

Eplerenone binds only to mineralcorticoid receptors to tx HTN and HF

*SE include gynecomastia, hyperkalemia, metabolic acidosis

*Don't use in patient's with Renal failure