Adrenal Steroids 2 Flashcards by David Sisa Gangai

Betamethasone - MoA

Promotes fetal lung maturation

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Betamethasone - Clinical use

Prevent RDS in premature infants by leading to lung maturation, psoriasis, seborrheic/atopic dermatitis, neurodermatitis

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Betamethasone - Special considerations

Can enter placenta, used systemically and topically

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Budesonide - Clinical use

Ulcerative colitis

Asthma

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Ciclesonide - Clinical use

Hay fever/ allergic rhinitis

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Beclomethasone, Flunisolide and Mometasone furoate - Clinical use

Extremely good for asthma, allergic rhinitis

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Topical steroids

Loteprednol
Difluprednate
Desonide 
Hydrocortisone
Dexamethasone
Fluticasone
Triamcinolone
Desoximethasone
Fluocinonide 
Clobetasol
Betamethasone
Dipropionate

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Low-potensy topical steroids

Desonide
Hydrocortisone
Dexamethasone

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Medium-potensy topical steroids

Fluticasone

Triamcinolone

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High-potency topical steroids

Desoximethasone

Fluocinonide

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Very-high-potency topical steroids

Clobetasol
Betamethasone
Dipropionate

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Topical corticosteroids - Special consideration

Ointment: dry, cracked, scaly or hardened skin.

Lotions and gels: hairy areas

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Ophthalmis cortisol preparations

Loteprednol

Difluprednate

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Loteprednol - Clinical use

With tobramycin for corneal inflammation and keratitis

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Difluprednate - Clinical use

Pain and inflammation associated with ocular surgery

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Desonide,
Hydrocortisone,
Dexamethasone - Clinical use

Fluticasone - Clinical use

Redness, swelling, itching in various skin conditions (Atopic dermatitis, seborrheic dermatitis, contact dermatitis, and psoriasis)

Asthma

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Low potency steroids used in what kind of areas?

Areas with thinner skin and intertriginous areas where skin is folded or overlapped.

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Low to medium potency used in what kind of areas?

ears, trunk, arms, legs and scalp.

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Medium to very high potency are used in what kind of areas?

thicker skin.

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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)

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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