Spironolactone is a 7α-acetylthiospirolactone. Its onset of action is slow, and the effects last for 2–3 days after the drug is discontinued. It is used in the treatment of primary aldosteronism in dosages of 50–100 mg/d. This agent reverses many of the manifestations of aldosteronism. It has been useful in establishing the diagnosis in some patients and in ameliorating the signs and symptoms when surgical removal of an adenoma is delayed. When used diagnostically for the detection of aldosteronism in hypokalemic patients with hypertension, dosages of 400–500 mg/d for 4–8 days—with an adequate intake of sodium and potassium—restore potassium levels to or toward normal. Spironolactone is also useful in preparing these patients for surgery. Dosages of 300–400 mg/d for 2 weeks are used for this purpose and may reduce the incidence of cardiac arrhythmias.
Spironolactone is also an androgen antagonist and as such is sometimes used in the treatment of hirsutism and acne in women. Dosages of 50–200 mg/d cause a reduction in the density, diameter, and rate of growth of facial hair in patients with idiopathic hirsutism or hirsutism secondary to androgen excess. The effect can usually be seen in 2 months and becomes maximal in about 6 months.
Spironolactone as a diuretic is discussed in Chapter 15. The drug has benefits in heart failure greater than those predicted from its diuretic effects alone (see Chapter 13). Adverse effects reported for spironolactone include hyperkalemia, cardiac arrhythmia, menstrual abnormalities, gynecomastia, sedation, headache, gastrointestinal disturbances, and skin rashes.
Eplerenone, another aldosterone antagonist, is approved for the treatment of hypertension and heart failure (see Chapters 11, 13, and 15). Like spironolactone, eplerenone has also been found to reduce mortality in heart failure. This aldosterone receptor antagonist is somewhat more selective than spironolactone and has no reported effects on androgen receptors. The standard dosage in hypertension is 50–100 mg/d. The most common toxicity is hyperkalemia, but this is usually mild.
Drospirenone, a progestin, is an oral contraceptive (see Chapter 40), and also antagonizes the effects of aldosterone.
Betamethasone sodium phosphate Generic, Celestone Phosphate
Budesonide Generic, Entocort EC
Dexamethasone Generic, Decadron
Hydrocortisone (cortisol) Generic, Cortef
Hydrocortisone sodium succinate Generic, Solu-Cortef, others
Methylprednisolone Generic, Medrol
Methylprednisolone acetate Generic, Depo-Medrol
Methylprednisolone sodium Generic, Solu-Medrol, others succinate
Prednisolone Generic, Prelone, others
Prednisolone acetate Generic, Flo-Pred
Prednisolone sodium phosphate Generic, Hydeltrasol
Prednisone Generic, Deltasone, Prednicot
Triamcinolone acetonide Generic, Kenalog, Azmacort
Ketoconazole Generic, Nizoral
Mifepristone Mifeprex, Korlym
Glucocorticoids for respiratory use: See Chapter 20. Glucocorticoids for dermatologic use: See Chapter 61. Glucocorticoids for gastrointestinal use: See Chapter 62.
Alesci S et al: Glucocorticoid-induced osteoporosis: From basic mechanisms to clinical aspects. Neuroimmunomodulation 2005;12:1.