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4420 Test 3 Adrenocorticoids, Franklin
Review of Adrenocorticoids for test 3. By Dr. Franklin
18
Pharmacology
Professional
03/29/2012

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Cards

Term
How may adrenocorticoids & adrenocortical antagonists be classified?
Definition
  • Glucocorticoids - Effects on intermediary metabolism
    • Major human one is cortisol
  • Mineralcorticoids - Effects on salt retention
    • Major one is aldosterone
  • Androgenic or estrogenic activity
    • Major human one is dehydroepiandrosterone sulfated form (DHEAS)
Term
How do glucocoricoids dramatically reduce inflammation?
Definition
  1. Affecting concentration, distribution and function of leukocytes.
  2. Suppressive effects on infllammatory cytokines and chemokines.
  3. Suppressive effects on other lipid and glucolipid mediators of inflammation.
Term
How do glucocorticoids induce their immunosuppressive (via anti-inflammatory) effects?
Definition
  • Inflammation is associated with extravasation and infiltration of leukocytes into affected tissue.
    • Mediated by complex interactions of white cell adhesion molecules with those of endothelial cells.
    • Glucocorticoids inhibit this.
    • One injection of glucocorticoid decreases circulating numbers of lymphocytes, monocytes, eosinophils, and basophils.
    • One injection increases circulating neutrophils.
Term
What type of agent has important dose-related effects on carbohydrate, protein and fat metabolism?
Definition
Glucocorticoids
Term
What type of agents influence gluconeogenesis, glycogen synthesis, and many other metabolic events?
Definition
Glucocorticoids.
Term
What type of agents have catabolic and antianabolic effects in lymphoid and connective tissue, muscle, fat, and skin? In what way may this effect bone?
Definition

Glucocorticoids

  • These effects may cause osteoporosis in Cushing's syndrome.
Term
What type of agents may reduce growth in children? What may be done to counteract this?
Definition

Glucocorticoids.

  • Growth hormone may be needed in children receiving glucocorticoid therapy.
Term
What are some natural and synthetic corticosteroids? List them with ranking in terms of relative duration.
Definition
  • Short-acting:
    • Cortisone (Cortone Acetate)
    • Prednisone (Meticorten)
  • Intermediate-acting:
    • Triamcinolone (Aristocort, Kenacort)
  • Long-acting:
    • Dexamethasone (Decadron)
Term
What are the effects of aldosterone?
Definition
  • Promotes reabsorption of sodium from the distal convoluted and cortical collecting renal tubules.
  • Promotes sodium reabsorption in the sweat gland, slivary glands, GI mucosa, and across cell membranes in many tissues.
Term
Deoxycortisone (DOC):
Definition
  • A precursor for aldosterone with similar effects.
  • Secreted in much smaller amounts than aldosterone
Term
Fludrocortisone (Florinef Acetate):
Definition
  • A potent synthetic steroid with glucocorticoid and mineralocorticoid activity.
Term
What is mineralocorticoid deficiency?
Definition
  • Adrenocortical insufficiency.
  • Potent salt-retain activity
Term
What are the uses of Dehydroepiandrosterone? What is it?
Definition
  • An adrenal androgen
  • Converted to androstenedione, testosterone, and androsterone.
  • Has been advocated for weight loss, tx of CV disease, aging and other conditions.
    • Jury still out on efficacy.
Term
What is Metyrapone? Use & ADR?
Definition
  • A synthesis inhibitor (antagonist of adrenocortical agents)
  • Selective inhibitor of steroid synthesis (cortisol and corticosterone)
  • Uses:
    • Diagnostic use is to determine capacity of anterior pituitary to produce ACTH and to test adrenal fct.
    • Rarely used to treat Cushing's disease.
  • ADR: Salt and water retention. Hirsutism.
Term
What is Aminoglutethimide (Cytadren)? MOA & use?
Definition
  • Antagonist of adrenocortical agents: Synthesis inhibitor
  • Blocks conversion of cholesterol to pregnenolone causing decrease in synthesis of all steroids.
  • Uses: Has been used to reduce estrogen production in breast cancer.
  • Replaced tamoxifen or aromatase inhibitors.
Term
What is Ketoconazole (Nizoral)? MOA, use & ADR?
Definition
  • Antagonist of Adrenocortical Agents: Synthesis inhibitor
  • Potent, nonselective inhibitor of adrenal and gonadal steroid synthesis.
  • Use: Has been used for tx of Cushing's Syndrome
  • ADR: Hepatotoxicity.
Term
What is Mifepristone? MOA & use?
Definition
  • Antagonist of Adrenocortical Agents: Glucocorticoid antagonist
  • Has strong antiprogestin activity.
  • High affinity antagonist of glucocorticoid receptor.
  • Use:
    • Useful in treating Cushing's syndrome due to ectopic ACTH production or adrenal carcinoma.
    • Used for contraception and postcoital contraception
Term
What is spironalactone? MOA, use & ADR?
Definition
  • Mineralocorticoid antagonist
  • Competes w/ aldosterone for binding sites on receptors.
  • Uses:
    • Used to treat primary aldosteronism.
    • Also an androgen antagonist and can be used to treat hirsutism.
    • Also used as a diuretic.
  • ADR: Hyperkalemia, gynecomastia, sedation
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