Pharm 52: Adrenocorticosteroids
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14 terms
Terms | Definitions |
|---|---|
 Beclomethasone | MOA: Short acting synthetic glucocorticoid (10h) -> used aerosol, penetrates airway mucosa (low systemic toxicity) USE: Asthma |
| Methylprednisone, Prednisone (prodrug), Triamcinolone, Fluticasone | MOA: Synthetic glucocorticoids -> intermediate acting (24h) USE: CAH (21 hydroxylase def), inflammation, Anti-emetic, Hodgkins (prodrug), fetal lung maturity (IM), hematologic disorders, organ transplants (prevent rejection), renal disorders (nephrotic syndrome), hypercalcemia, mountain sickness, IBD |
| Hydrocortisone (Cortisol) | MOA: Naturally occurring glucocorticoid -> short duration of action (10h), diffuses poorly across skin unless inflamed, well across mucous membranes -> some salt retaining effects USE: #1 for Addison's (with fludrocortisone), #1 for acute adrenal insufficiency (parenteral), CAH (21 hydroxylase def), inflammation, fetal lung maturation, before and after surgery for Cushing's, stress dose for pts with adrenal insufficiency during serious illness or prior to surgery |
| Dexamethasone | MOA: long acting glucocorticoid (2 days) USE: potent anti-inflammatory action, #1 cerebral edema, CAH (21 hydroxylase def, protect fetus in high risk pregnancies by administration to mother), fetal lung maturation *used as a diagnostic tool for Cushing's syndrome, depressive psychiatric states AE: not used in Addison's |
| Aldosterone, Fludrocortisone | MOA: mineralocorticoids -> bind intracellular receptor and cause increased expression Na/K/ATPase and ENaC -> promote Na reabsorption from renal tubule, promote K+ and H+ excretion -> Salt-retaining hormones USE: Addison's, adrenal insufficiency (once stabilized), CAH (once stabilized) |
| Mifepristone | MOA: Glucocorticoid and progesterone antagonist USE: inoperable pts with ectopic ACTH syndrome (Cushing's) or adrenal carcinoma |
| Spironolactone | MOA: Mineralocorticoid antagonist - competitive inhibitor USE: aldosteronism (diagnosis and treament), hirsutism in women (acts as androgen antagonist), diuretic AE: Hyperkalemia*, cardiac arrhythmia, menstrual abnormalities, gynecomastia, sedation, headache, GI disturbances, skin rash |
| Ketoconazole | MOA: Corticosteroid Synthesis inhibitor -> potent and non-selective inhibitor of adrenal and gonadal steroid synthesis USE: Cushing's syndrome, prostate cancer |
| Aminoglutethimide | MOA: Corticosteroid Synthesis inhibitor -> blocks conversion of cholesterol to pregnenolone (desmolase) USE: Adrenal cancer (add hydrocortisone or dexamethasone) |
| Metyrapone | MOA: Corticosteroid synthesis inhibitor -> selective inhibitor of 11-hydroxylation -> interferes with cortisol and corticosterone synthesis USE: tests adrenal function, treat pregnant women with Cushing's AE: salt and water retention, Hirsutism, transient dizziness, GI disturbances |
| Metabolic/Catabolic effects of glucocorticoids | Steroid receptor complex enters nucleus and increases txn producing tissue specific responses Metabolic effects maintain adequate glucose supply to brain -> central fat redistribution, hyperglycemia -> Cushing's Catabolic effects (proteins, lymphoid, CT, muscle, peripheral fat and skin, bone) cause osteoporosis (give Ca and Vit D supplements), peripheral fat wasting and growth retardation in children, myopathy |
| Anti-inflammatory and immunosuppressive effects of glucocorticoids | increased neutrophils, decreased lymphocytes, inhibit PLA2/COX-2/PG, vasoconstriction due to suppression of mast cell degranulation Peptic ulcers (stimulation of gastric acid and suppression of immune response to H. pylori) |
| Other effects of glucocorticoids | CNS = behavioural changes (insomnia, euphoria leading to depression), increased ICP and intraocular pressure (glaucoma), cataracts Suppression of release of ACTH, GH, TSH, LH with chronic use Increased platelets and RBCs Deficiency causes renal impairment Development of fetal lungs sodium and fluid retention, loss of potassium -> give K+ supplement Adrenal suppression with abrupt withdrawal (taper dose) |
| Glucocorticoid contraindications | peptic ulcers heart disease/HTN with heart failure TB/VZV infections Psychoses Diabetes Osteoporosis Glaucoma |
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