Steroids

Question 1

What are the two goals of steroid administration

Answer 1

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

Suppres inflammation and immune responses

Question 2

What are the two classes of glucocorticoids

Answer 2

11-hydroxy-glucocorticoids (intrinsic activity)

11-keto-glucocorticoids ( inactive)

Question 3

What enzyme activates 11-keto glucocorticoids

Answer 3

11B-HSD 1

• prednisone to prednisolone
• cortisone to cortisol

Question 4

The DOA of glucocorticoids depends on what four variables

Answer 4

Protein binding

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

lipophilicity of drug

affinity of drug for glucocorticoid receptor

Question 5

What syndrome is associated with glucocorticoid administration

Answer 5

Iatrogenic Cushing’s syndrome

Question 6

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

Answer 6

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

Question 7

Acute withdrawal of glucocorticoid tx can result in

Answer 7

adrenal insufficiency-Addison’s disease

Question 8

What is the typical Stress dose replacement

Answer 8

hydrocortisone 100 mg before, during, and after surgery

Question 9

Cautious administration of glucocorticoids should be used in which patients

Answer 9

Heart disease/HTN/HF
DM
Infectious disease processes

Question 10

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

Answer 10

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

Question 11

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

Answer 11

Gluco/Mineral

Triamcinolone 5.0/0

Question 12

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

Answer 12

Gluco/Mineral
Dexamethasone 30.0/0
Betamethasone 40/0

Question 13

Name the inhaled glucocorticoids

Answer 13

Fluticasone
Beclomethasone
Flunisolide
Triamcinolone

Question 14

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

Answer 14

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

SE- Iatrogenic Cushing’s syndrome

Question 15

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

Answer 15

Clinical uses- asthma, allergic rhinitis

SE- oropharyngeal candidiasis

Question 16

Can aldosterone be given as a tx for hypoaldosteronism

Answer 16

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

Question 17

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

Answer 17

Fludrocortisone

SE- HTN, hypokalemia, and cardiac failure

Question 18

What are the three different classes of adrenal steroid INHIBITORS

Answer 18

Inhibitors of Adrenocorticol hormone synthesis

Glucocorticoid receptor antagonists

mineralocorticoid receptor antagonists

Question 19

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

Answer 19

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

Question 20

Name the glucocorticoid receptor antagonists and the pathways effected

Answer 20

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

*SE- HYPOTHYROIDISM (inhibits T4 to T3 conversion)

Question 21

Name the mineralcorticoid receptor antagonists and the pathways effected

Answer 21

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