Adrenal Corticosteroid Pharmacology Flashcards
Endogenous Corticosteroids
Examples (2), Receptors (2), Common Applications (5)
Cortisol
Aldosterone
Glucocorticoid Receptors (alpha and beta) Mineralocorticoid Receptors (equal affinity for cortisol and aldosterone)
Primary Adrenal Insufficiency (Addison’s)
Congenital Adrenal Hyperplasia
Immunosuppression, Allergies, Inflammation
11-Beta-Hydroxysteroid Dehydrogenase Type 2
Action, Deficiency Effects (2), Inhibitor
Turns active steroids (cortisol, corticosterone, prednisolone) into Inert steroids (cortisone, 11-dehydrocorticosterone, prednisone)
Excessive activation of mineralocorticoid receptor by cortisol
Causes increased Na+/Water retention leading to HTN
Glycyrrhizin (licorice root extract)
Glucocorticoid Drugs
Examples with Length of Action and Potency
Short (5) Intermediate, Long (2)
Short last 8-12 hours Lowest Potency Hydrocortisone Cortisone Prednisone Prednisolone Methylprednisolone
Intermediate last 12-36 hours
Medium Potency
Triamcinolone
Long last 36-72 hours
Highest Potency
Betamethasone
Dexamethasone
Glucocorticoid Side Effects (7)
Infection susceptibility Myopathies Osteoporosis Hyperglycemia HPA insufficiency Cataracts/Glaucoma Hypertension
Glucocorticoid Intermediary Metabolism Effects (5)
Antagonize actions of insulin causing Hyperglycemia
Increased gluconeogenesis
Decreased glucose uptake and glycogen synthesis
Increased proteolysis
Increased lipolysis
Glucocorticoid Immune System Effects (5)
Decreased Prostaglandins and Leukotrienes Decreased immune cell production Decreased cytokines Decreased immune cell transmigration Decreased cell adhesion molecules
Glucocorticoid Dosing Considerations (4) and Adrenal Cancer Drug
Avoid systemic distribution
Give single dose in the morning
Give every other day
Taper patient off steroids to avoid adrenal crisis
Mitotane used for adrenal cancer
Mifepristone
Use and Adverse Effect
Medical abortion
Vaginal bleeding
Fludrocortisone
Use, Pharmacokinetics and Adverse Effects (2)
Addison’s Disease
Long duration of action
Salt and water retention
Exacerbation of CHF
Metyrapone Uses (2)
Diagnosis of adrenal insufficiency
Treatment of Cushing’s disease
Mineralocorticoid Antagonists
Examples (2), Uses (2/1) Pharmacokinetics and Adverse Effects (2/2)
Spironolactone
Uses: Hyperaldosteronism and Hypokalemia
Slow onset and long half-life (24-48 hours)
AE’s: Hyperkalemia and Gynecomastia
Eplerenone
Use: Hypertension
CYP450 3A4 metabolized
AE’s: Hyperkalemia and Increased creatinine
Ketaconazole
Mechanisms of Action (2) Adverse Effects (2)
Blocks steroid hormone synthesis in mammals
Blocks ergosterol in fungi
Hepatic dysfunction
CYTP450 inhibition causing many drug interactions
Contraindications to Use of Glucocorticoids (7)
Immunocompromised patient (HIV/AIDS) Diabetics Peptic Ulcers Cardiovascular conditions (CHF, Angina) Psychiatric conditions Osteoporosis Children
