Adverse effects

• Oral thrush

• Iatrogenic Cushing's

• Osteoporosis

• Hyperglycemia

Adverse effects

• Muscle wasting

• CNS effects (euphoria, depression, & psychosis)

• Glaucoma

• Increased incidence of cataracts

• Raised intra-cranial pressure

• Most important mineralocorticoid

• Promote the reabsorption of sodium from the distal part of the distal convoluted renal tubule and from the cortical collecting tubules

• Excessive secretion: hypokalemia, metabolic alkalosis, increased plasma volume, and hypertension

• Secreted at the rate of 100-200 mcg/d in normal individuals with a moderate dietary salt intake

• Half-life: 15-20 minutes

• Metabolism is similar to that of cortisol

• Precursor of aldosterone

• Normally secreted in amounts of about 200 mcg/d

• Half-life: 70 mins

• Plasma conc: 0.03mcg/dL

• Secretion is primarily under the control of ACTH

• Secretion of DOC may be markedly increased in abnormal conditions such as:

- Adrenocortical carcinoma

- Congenital adrenal hyperplasia with reduced P450c11 or P450c17 activity

• Potent steroid with both glucocorticoid and mineralocorticoid activity

• Most commonly-prescribed salt-retaining hormone

• Increases Na reabsorption in the distal tubules and increases K

and H efflux into the tubules

• Oral doses of 0.1 mg two to seven times weekly have potent salt-retaining activity and are used in the treatment of adrenocortical insufficiency associated with mineralocorticoid deficiency

- These dosages are too small to have important anti-inflammatory or antigrowth effects

MOA/PK

• Blocks the conversion of cholesterol to pregnenolone

• Increases the clearance of some steroids.

• Shown to enhance the metabolism of Dexamethasone, reducing its half-life from 4–5 hours to 2 hours

Indications

• Used in conjunction with dexamethasone or hydrocortisone to reduce or eliminate estrogen production in patients with carcinoma of the breast

Indications

• Used in conjunction with metyrapone or ketoconazole

to reduce steroid secretion in patients with Cushing’s syndrome

Adverse effects

- In higher doses: lethargy an skin rash

MOA/PK

• Antifungal imidazole derivative

• Potent and rather nonselective inhibitor of adrenal and gonadal steroid synthesis

Indications

• Treatment of patients with Cushing’s syndrome

Adverse effects

• Hepatotoxic

MOA/PK

• Substituted imidazole

• Inhibits adrenal steroidogenesis at the level of 11β- hydroxylase

Indications

• Induction of general anesthesia and sedation

Indications

• Only parenteral medication available in the treatment of severe Cushing’s syndrome

MOA/PK

• Relatively selective inhibitor of steroid 11-hydroxylation, interfering with cortisol and corticosterone synthesis

Indications

• May be useful in the management of severe manifestations of cortisol excess

• Commonly used in tests of adrenal function

Indications

• Only adrenal inhibiting medication that can be administered to pregnant women with Cushing’s syndrome

MOA/PK

• 3β -17 hydroxysteroid dehydrogenase inhibitor

• Interferes with the synthesis of adrenal and gonadal hormones

Indications

• Primary aldosteronism

• Comparable to aminoglutethimide

Adverse effects

• Gastrointestinal disturbances

- occurs in 50% of px

MOA/PK

• Newest of the steroid synthesis inhibitors

• Blocks 17α-hydroxylase (P450c17) and 17,20-lyase

• Orally active steroid prodrug

Indications

• Treatment of refractory prostate cancer

MOA/PK

• Pharmacologic antagonist at the steroid receptor

• Strong anti-progestin activity

• At high doses: exert anti-glucocorticoid activity by blocking the glucocorticoid receptor

• Causes generalized glucocorticoid resistance

MOA/PK

• Mean half-life: 20 hours

• Less than 1% of daily dose is excreted in the urine

• Long plasma half-life results from extensive and strong binding to plasma proteins

Indications

Given orally to inoperable patients with ectopic ACTH secretion or adrenal carcinoma who have failed to respond to other treatment

Indications

• Initially proposed as a contraceptive-contragestive agent

MOA/PK

• Non-selective cytotoxic action on the adrenal cortex in dogs and to a lesser extent in humans

• Inhibits CYP11A1

Indications

• Used to treat inoperable adrenocortical carcinoma

Dosing

• Administered orally in divided doses up to 12g daily

Adverse effects

• Diarrhea

• Nausea

• Vomiting

• Depression

• Somnolence

• Skin rashes

MOA/PK

• Compete with aldosterone for its receptor and decrease its effect peripherally

• Onset of actions is slow

• Effects last for 2-3 days after discontinuation

Indications

• Treatment of primary aldosteronism

• Treatment of hirsutism and acne in women

• Also, a diuretic

Adverse effects

• Hyperkalemia

• Cardiac arrhythmia

• Menstrual abnormalities

• Gynecomastia

• Sedation

• Headache

• GI disturbances

• Skin rashes

MOA/PK

• Aldosterone antagonist

Indications

• Treatment of hypertension and heart failure

• Used to treat Primary and Secondary Hyperaldosteronism

Adverse effects

• Cause fewer adverse effects

• Hyperkalemia

MOA/PK

• Aldosterone antagonist

Indications

• Oral contraceptive

• Good effect against acne in women