Pharm: L17: Glucocorticoids

Question 1

Glucocorticoids:

1. What does it do to Carbs, protein and Fat
2. Antagonizes what?
3. Redistribution of Body Fat?

Answer 1

1. Increase blood levels of Glucose FFA and AAs
2. Insulin
3. Extremities –> Central

Question 2

Glucocorticoids:

1. Cardiovascular

Answer 2

1. INCREASE Vascular Responsiveness to Sympathetic Stimulation and some Na+ and H2O RETENTION (normal ranges: Cortisol 200:1 Aldosterone)

Question 3

Glucocorticoids:

1. Endocrine Effects

Answer 3

1. Negative feedback on CRH –> Decreased ACTH

Decreases GH, TSH, LH (decreased sex steroids –> inhibits reproduction)

Inhibits Vit D action (decreased Ca2+ deposition into bone)

INCREASED PTH –> Increased Ca2+ loss from bone.

Increased EPI production in Adrenal Medulla

Question 4

Glucocorticoids:

1. Immunosuppressive
2. Blocks ALL STEPS in INFLAMMATION
3. Suppression of WOUND HEALING

Answer 4

1. decreased WBCs and leukocyte function
2. Heat, erythema, swelling, tenderness, decreased PLA2, COX2, CYTOKINES, IgE response
3. Early: edema, fibrin deposition, neutrophil migration and phagocytosis

Late: Collagen synthesis and deposition

Question 5

Glucocorticoids:

1. CNS

Answer 5

1. Mood elevation, insomnia, restlessness, anxiety, depression, psychosis.

GI: Peptic ulcer development

Question 6

Glucocorticoid

1. Hydrocortisone (Cortisol)
2. Cortisone

Answer 6

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Question 7

Mineralocorticoid

1. Fludrocortisone
   a. Use?
   b. Effects?

Answer 7

1. a. Tx for Adrenocortical Insufficiency when More Mineralocorticoid effects are needed.
   b. Like ALDOSTERONE. Has Glucocorticoid effects but SIGNIFICANT Mineralocorticoid Properties

Question 8

Anti-Inflammatory

1. Hydrocortisone…-ones…

Answer 8

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Question 9

What do Mineralocorticoids do?

Answer 9

1. Aldosterone is most important. Angiotensin II and/or K+ main stimuli for Aldosterone.

ACTH (minor stimulus for aldosterone)

Physiological: Increases Na+ and H2O retention and Increases Excretion of K+ and H+

Question 10

Glucocorticoid Excess: What disease and causes?

Answer 10

1. Cushing’s Disease or Syndrome (ACTH Excess (tumor) and Cortisol Excess (tumor and Exogenous Glucocorticoids)

Question 11

Adrenocortical Insufficiency

Answer 11

Lack of Corticosteroids (Addison’s Disease, Adrenal and Pituitary Malfunction)

Question 12

1. Hydrocortisone (minor anti-inflammation)
   a. AKA?
   b. Properties?
   c. Replacement Therapy for what?
2. Cortisone
   a. Properties?
   b. Has to be converted to what and where in order to be active?
   c. Replacement therapy for what?

Answer 12

1. a. CORTISOL
   b. Mineralocorticoid and Glucocorticoid
   c. for Adrenal insufficiency
2. a. Significant mineralocorticoid as well as glucocorticoid properties
   b. to HYDROCORTISONE in the Liver in order to be Active
   c. for Adrenal Insufficiency

Question 13

1. Prednisone and Prednisolone
   a. Properties
   b. What does prednisone have to be converted to?

c. Which is the MOST COMMONLY PRESCRIBED ORAL GLUCOCORTICOID?

Answer 13

1. a. Glucocorticoid effects and mineralocorticoid (but more gluco)
   b. Prednisolone in the LIVER to become ACTIVE

c. PREDNISONE!!

Question 14

Triamcinolone and Methylprednisolone

a. activity?
b. Most newer drugs are like what?

Answer 14

1. Virtually NO mineralocorticoid activity but HIGH Glucocorticoid activity
   b. these.

Question 15

What 2 drugs are SHORT ACTING?

Answer 15

Hydrocortisone and Cortisone

Question 16

What 2 are LONG ACTING?

Answer 16

BetaMETHAsone and DexaMETHAsone

Question 17

Therapeutic Uses for Corticosteroids

Answer 17

RA; Asthma (first step in Asthma Tx used in Conjunction w/a B2-Agonist: Increase Sensitivity)

Intranasal for RHINITIS

Lupus, Allergic RxNs, Shock, Organ Transplants

Question 18

Adverse Effects w/Corticosteroids

1. Infections
2. Hyperglycemia
3. CNS
4. Osteoporosis

Answer 18

1. can mask symptoms; More susceptible to Serious Infections
2. Can UNMASK Diabetes in some patients
3. Restlessness, Insomnia, Psychosis, Increased Appetite (Even w/ACUTE Txs)
4. MOST DAMAGING and THERAPEUTICALLY LIMITING EFFECT (30-50% of Chronic Patients!!), Vertebral and Rib Fractures most Common (Tx: Ca2+, Vit D, and Bisphosphonates)

Question 19

Adverse Effects

1. Iatrogenic Adrenal Insufficiency

Answer 19

1. 1-2 wks of HIGH DOSE therapy –> HPA Depression
   * ABRUPT Drug cessation –> ACUTE ADRENAL INSUFFICIENCY (want GRADUAL withdrawal)

*Stress can cause ADRENAL CRISIS in CHRONIC PATIENTS

Question 20

Adverse Effects

Miscellaneous (Cushingoid) Side effects?

Answer 20

1. Acne; Truncal Obesity; Buffalo Hump; Moon Face; DYSMENORRHEA, Skin Atrophy and Thinning

Question 21

CIs?

Answer 21

None in Adrenal Insufficiency

Question 22

Optometry specific

Answer 22

Optic adverse effects: Hypertension/Glaucoma, Secondary Ocular Infection, Posterior Subcapsular Cataracts

*Use: Dry Eye; Uveitis; Contact Dermatitis; Scleritis; Chalazion; Reduces Inflammation