Steroids Flashcards
What are the two goals of steroid administration
Replacement therapy for primary adrenal insufficiency- glucocorticoid and mineralcorticoids must be replaced
Suppres inflammation and immune responses
What are the two classes of glucocorticoids
11-hydroxy-glucocorticoids (intrinsic activity)
11-keto-glucocorticoids ( inactive)
What enzyme activates 11-keto glucocorticoids
11B-HSD 1
- prednisone to prednisolone
- cortisone to cortisol
The DOA of glucocorticoids depends on what four variables
Protein binding
affinity of the drug for 11-HSD 2 (in kidney)
lipophilicity of drug
affinity of drug for glucocorticoid receptor
What syndrome is associated with glucocorticoid administration
Iatrogenic Cushing’s syndrome
What are the S/S of Iatrogenic Cushing’s syndrome
Infection Hyperglycemia Osteoporosis Muscle weakness Periperal wasting with central obesity Fat redistribution-Moon face/buffalo hump Peptic ulcers Acute psychosis/depression
Acute withdrawal of glucocorticoid tx can result in
adrenal insufficiency-Addison’s disease
What is the typical Stress dose replacement
hydrocortisone 100 mg before, during, and after surgery
Cautious administration of glucocorticoids should be used in which patients
Heart disease/HTN/HF
DM
Infectious disease processes
Name the short acting synthetic steroids and their relative potencies with respect to glucocorticoid and mineralcorticoid activity
Gluco/Mineral
Hydrocortisone (cortisol) 1.0/1.0
* Cortisone 0.8/0.8
Prednisone 4.0/0.3
Prednisolone 4.0/0.3
* Methylprednisolone 5.0/0.25
Name the intermediate-acting synthetic steroids and it’s relative potencies with respect to gluc/minercorticoid activity
Gluco/Mineral
Triamcinolone 5.0/0
Name the long- acting synthetic steroids and their relative potencies with respect to glucocorticoid and mineralcorticoid activity
Gluco/Mineral
Dexamethasone 30.0/0
Betamethasone 40/0
Name the inhaled glucocorticoids
Fluticasone
Beclomethasone
Flunisolide
Triamcinolone
What are the clinical uses and SE associated with glucocorticoid receptor agonists
clinical uses: inflammation, autoimmune disease, and prevention of transfusion rxn
SE- Iatrogenic Cushing’s syndrome
What are the clinical uses and SE associated with the inhaled steroids
Clinical uses- asthma, allergic rhinitis
SE- oropharyngeal candidiasis
Can aldosterone be given as a tx for hypoaldosteronism
No, because it has a high hepatic first-pass metabolism of 75%
What is the main drug for replacing mineracorticoids and it’s SE
Fludrocortisone
SE- HTN, hypokalemia, and cardiac failure
What are the three different classes of adrenal steroid INHIBITORS
Inhibitors of Adrenocorticol hormone synthesis
Glucocorticoid receptor antagonists
mineralocorticoid receptor antagonists
Name the inhibitors of adrenocortical hormone synthesis and the pathway it effects
Mitotane effects salt, sugar, and sex s/s/s
Aminoglutethimide effects s/s/s
Ketoconazole decreases male sex hormones but increases all other pathways
Metyrapone 11B-hydroxylase inhibitor which effects cortisol synthesis
Trilostane effects both cortisol and aldosterone synthesis
SE: Hypercholesterolemia, gynecosmastia, N/D, pruitus, CNS depression
Name the glucocorticoid receptor antagonists and the pathways effected
Mifepristone (RU-486) effects progesterone receptors (induces abortion) and glucocorticoid receptors ( treats life-threatening steroid levels)
*SE- HYPOTHYROIDISM (inhibits T4 to T3 conversion)
Name the mineralcorticoid receptor antagonists and the pathways effected
Sprironolactone competes with aldosterone to lower bp and tx HTN
Eplerenone binds only to mineralcorticoid receptors to tx HTN and HF
- SE include gynecomastia, hyperkalemia, metabolic acidosis
- Don’t use in patient’s with Renal failure
