Adrenocorticoids

Question 1

3 Classes of Adrenocortical Hormones

Answer 1

Glucocorticoids - Cortisol

Mineralocorticoids - Aldosterone

Adrenal Androgens - Androstenedione

Question 1

Locations of Adrenocortical Hormones

Answer 1

Cortisol - Zona fasciculata

Aldosterone - Zona glomerulosa

Androstenedione - Zona reticularis

Question 2

Glucocorticoid Receptor

Answer 2

Intracellular receptor

Binds cortisol

Bound to HSPs

Activates mediates gene transcription

Question 3

Glucocorticoid Functions

Answer 3

Promote normal intermediary metabolism

Increase resistance to stress

Promote anti-inflammatory action

Affect other systems

Question 4

Cortisol

Answer 4

Principle glucocorticoid

Question 5

Corticosteroids - General Information

Answer 5

Used to primarily to treat:
- Inflammation
- Allergic responses
- Hematologic disorders

Administration routes vary:
- Oral
- Injectable
- Topical

Question 6

Short to Medium-Acting Glucocorticoids

Answer 6

Hydrocortisone (Cortisol)

Cortisone (Cortisone Acetate)

Prednisone

Prednisolone (Orapred, Pediapred)

Methylprednisolone (Medrol)

Question 7

Intermediate-Acting Glucocorticoids

Answer 7

Triamcinolone (Kenalog, Nasacort, Aristospan)

Question 8

Long-Acting Glucocorticoids

Answer 8

Betamethasone (Celestone)

Dexamethasone (Decadron)

Fluocinolone (Iluvien)
- Intravitreal implant
- Indicated for diabetic macular edema

Question 9

Corticosteroids and Fetal Lung Maturation

Answer 9

Fetal lung maturation regulated by cortisol

Maternal IM betamethasone in anticipation of preterm delivery within next 7 days

ACOG recommends two 12-mg dose of betamethasone given IM 24 hours apart OR four 6-mg doses of dexamethasone administered IM every 12 hours

Reduces death rate and neurodevelopmental impairment

The benefit of corticosteroid administration is greatest at 2-7 days after the initial dose (should not be administer unless there is “substantial clinical concern” for imminent preterm birth)

Question 10

Nasal Corticosteroids

Answer 10

Triamcinolone (Nasacort)

Budesonide (Rhinocort)

Fluticasone (Flonase)

Mometasone (Nasonex)

Beclomethasone (Beconase)

Question 11

Uses of Nasal Corticosteroids

Answer 11

To relieve nasal congestion, hay fever or allergic symptoms

Question 12

Therapeutic Uses and Disease States

Answer 12

Replacement therapy of primary adrenocortical insufficiency (Addison’s disease)

Diagnosis of Cushing’s Syndrome

Replacement therapy for congenital adrenal hyperplasia (CAH)
- Results from enzyme defect in 1+ adrenal steroid hormones

Relief of inflammatory symptoms
- Persistent asthma, infections, IBD, RA, eczema, etc

Treatment of allergies
- Allergic rhinitis especially

Acceleration of fetal lung maturation
- Impending premature births

Question 13

Addison’s Disease

Answer 13

Adrenocortical insufficiency

Diagnosed by the lack of response to ACTH

Treatment with steroids (hydrocortisone) corrects deficiency
- Without treatment, it is fatal

Addisonian crisis
- Can occur due to sudden withdrawal of corticosteroids
- Slowly taper down long-term corticosteroid use

Question 14

Cushing’s Syndrome

Answer 14

Caused by hypersecretion of glucocorticoids (hypercortisolism) that results from excessive ACTH release
- Anterior pituitary dysfunction or adrenal tumor

Corticosteroids are diagnostic for this condition

Diagnosed by cortisol levels and dexamethasone suppression test
- Dexamethasone suppresses cortisol release in the absence of Cushing’s

Question 15

Adverse Effects of Corticosteroid

Answer 15

Decreased growth in children

Osteoporosis (negative calcium balance)

Increased appetite

Glaucoma

Increased risk of infection (impaired wound healing)

Emotional disturbances (Euphoria depression)

Centripetal distribution of body fat

Increased risk of diabetes

Hypokalemia

Hypertension

Peripheral edema

Question 16

General Considerations for Corticosteroid Therapy

Answer 16

Usually not curative alone

Avoid chronic therapy if possible

Evaluate for presence of other disease states (diabetes, peptic ulcer, osteoporosis, CV functions, psychological disturbances)

Supplement diet appropriately (high protein, calorie management, high K+ / low Na+, vitamin D, and calcium for osteoporosis)

Question 17

Mineralocorticoids

Answer 17

Help control fluid status and concentration of electrolytes (especially K+ and Na+)

Synthesis stimulated by Angiotensin I / II, increased K+, decreased Na+

Question 18

Mineralocorticoid Drugs

Answer 18

Aldosterone
Fludrocortisone (Florinef Acetate)

Question 19

Aldosterone

Answer 19

Synthesized in zona glomerulosa

Promotes sodium/water retention in kidney collecting ducts

Question 20

Fludrocortisone (Florinef Acetate)

Answer 20

Most common mineralocorticoid used therapeutically

Has both glucocorticoid and mineralocorticoid activity (low doses select for mineralocorticoid)

Question 21

Adrenocortical Antagonists

Answer 21

Ketoconazole (Nizoral)

Spironolactone (Aldactone)

Eplerenone (Inspra)

Mifepristone (Mifeprex)

Question 22

Ketoconazole (Nizoral)

Answer 22

Inhibits all gonadal and adrenal steroid hormone synthesis

Used to treat Cushing’s

At low doses - antifungal

Question 23

Spironolactone (Aldactone)

Answer 23

Aldosterone and androgen antagonist

Treats hirsutism

Question 24

Eplerenone (Inspra)

Answer 24

Aldosterone antagonist

Treats high BP

Question 25

Mifepristone (Mifeprex)

Answer 25

Glucocorticoid and progesterone receptor antagonist

Sometimes used in Cushing’s management

Also used in combination with misoprostol for medical pregnancy termination