Adrenal Steroids 2 Flashcards
Betamethasone - MoA
Promotes fetal lung maturation
Betamethasone - Clinical use
Prevent RDS in premature infants by leading to lung maturation, psoriasis, seborrheic/atopic dermatitis, neurodermatitis
Betamethasone - Special considerations
Can enter placenta, used systemically and topically
Budesonide - Clinical use
Ulcerative colitis
Asthma
Ciclesonide - Clinical use
Hay fever/ allergic rhinitis
Beclomethasone, Flunisolide and Mometasone furoate - Clinical use
Extremely good for asthma, allergic rhinitis
Topical steroids
Loteprednol Difluprednate Desonide Hydrocortisone Dexamethasone Fluticasone Triamcinolone Desoximethasone Fluocinonide Clobetasol Betamethasone Dipropionate
Low-potensy topical steroids
Desonide
Hydrocortisone
Dexamethasone
Medium-potensy topical steroids
Fluticasone
Triamcinolone
High-potency topical steroids
Desoximethasone
Fluocinonide
Very-high-potency topical steroids
Clobetasol
Betamethasone
Dipropionate
Topical corticosteroids - Special consideration
Ointment: dry, cracked, scaly or hardened skin.
Lotions and gels: hairy areas
Ophthalmis cortisol preparations
Loteprednol
Difluprednate
Loteprednol - Clinical use
With tobramycin for corneal inflammation and keratitis
Difluprednate - Clinical use
Pain and inflammation associated with ocular surgery
Desonide,
Hydrocortisone,
Dexamethasone - Clinical use
Fluticasone - Clinical use
Redness, swelling, itching in various skin conditions (Atopic dermatitis, seborrheic dermatitis, contact dermatitis, and psoriasis)
Asthma
Low potency steroids used in what kind of areas?
Areas with thinner skin and intertriginous areas where skin is folded or overlapped.
Low to medium potency used in what kind of areas?
ears, trunk, arms, legs and scalp.
Medium to very high potency are used in what kind of areas?
thicker skin.
Mineralocorticoids - MoA
Na+ reabsorption coupled (loosely) with K+ & H+ excretion. Binds to mineralocorticoid receptors in cytoplasm causing increased expression of Na/K-ATPase & epithelial sodium channels. (Receptors have same affinity for cortisol, but in kidney cortisol is converted to cortisone with lower affinity)
Mineralocorticoids - Adverse Effects
Hypokalemia, metabolic alkalosis, Increased plasma volume, hypertension
Fludrocortisone - MoA
Both glucocorticoid and mineralocorticoid actions
Potent salt retaining activity
Fludrocortisone - Clinical use
Primary adrenal insufficiency (Addison`s disease)
Preferred in replacement therapy in adenectomy
CAH in combo with hydrocortisone.
Fludrocortisone - Special considerations
Also glucocorticoid activity, but 20 times more potent salt-retaining activity
Only oral adm
Adrenal androgens
DHEA (Dehydroepiandrosterone)
DHEA - Clinical use
USED IN ALTERNATIVE MEDICINE
Studies indicate: protective for DM, immune disorders, cancer, weight gain, increased muscle mass and sexual function, and prolong life.
DHEA - Contraindication and Special consideration
Prostate cancer (because it is a weak androgen)
Extremely weak androgen, partly converted to testosterone.
DHEA - Adverse effects
Mild acne, seborrhea, and facial hair growth
Corticosteroid receptor antagonists
Spironolactone
Eplerenone
Mifepristone
Spironolactone - MoA
Competitive inhibition of mineralocorticoids receptors in the kidney
Spironolactone - Clinical use
Used as potassium-sparing diuretic,
Primary hyperaldosteronism (DOC)– diagnostic & therapeutic,
Secondary hyperaldosteronism (with heart failure, Bartter syndrome)
Hirsutism in women
Spironolactone - Special consideration
Reduce mortality in heart failure
Potassium-sparing diuretic.
Spironolactone - Adverse Effect
Hyperkalemia, cardiac arrhythmias, menstrual abnormalities, gynecomastia, sedation, headache, GI disturbances, skin rashes
Eplerenone - Clinical use
Hypertension
Eplerenone - Special consideration
Reduce mortality in heart failure
No effect on androgen receptors
Eplerenone - Adverse effects
Hyperkalemia (usually mild)
Mifepristone - MoA
It antagonizes both progesterone and glucocorticoid receptors
Mifepristone - Clinical use
Cushing’s syndrome (esp. hyperglycemia in patients with cushing syndrome)
Mifepristone - Special consideration
Strong antiprogestin activity (first intended to be contraceptive)
Corticosteroid synthesis inhibitors
Ketoconazole
Fluconazole
Aminoglutethimide
Metyrapone
Ketoconazole and Fluconazole - MoA
Inhibits steroid production by inhibiting 11β-hydroxylase (fungal cytochrome P450 enzyme)
Ketoconazole and Fluconazole - Clinical use
Cushing syndrome
Adrenal carcinoma, hirsutism, breast & prostate cancer.
Ketoconazole and Fluconazole - Adverse effects
Hepatotoxicity
Gynecomastia
Aminoglutethimide - MoA
Blocks conversion of cholesterol to pregnenolone & inhibits synthesis of all hormonally active steroids
Aminoglutethimide - Clinical use
- Reduce estrogen production in pt with breast cancer (in combo with dexamethasone and hydrocortisone)
- Reduce steroid secretion in pt with Cushing`s syndrome due to adrenocortical cancer who do not respond to mitotane (in combo with metyrapone or ketoconazole)
Aminoglutethimide - Adverse effects and interactions
High doses: Lethargy and skin rash
Interactions: increased Metabolism of dexamethasone
Metyrapone - MoA
Inhibits glucocorticoid synthesis by selectively inhibiting 11β-hydroxylation, shifts production to adrenal androgens
Metyrapone - Clinical use
Diagnostic test of adrenal function
Pregnant women with Cushing syndrome (ONLY drug for this).
Cushing syndrome in pt whose condition is refractory to other treatments and who are not candidates for surgery
Preparation for surgery
Metyrapone - Special consideration
Not normally used for Cushing syndrome (only choice for pregnancy. Also if other drugs failed and not candidate for surgery)
Metyrapone - Adverse effects
Transient dizziness and GI disturbances
Salt and water retention
Hirsutism
