Aldosterone antagonists - Nonmercurial diuretics

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Chapter: Medicinal Chemistry : Diuretics

Nonmercurial diuretics : Aldosterone antagonists: Spironolactone (Aldactone) - Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Nonmercurial diuretics

Aldosterone antagonists

Mode of action: Aldosterone inhibitors inhibit the aldosterone action on mineralocorticoid receptor, where aldosterone generates aldosterone-induced proteins along with Na+ K+ ATPase and amiloride sensitive Na+ channels that leads to the reabsorption of Na+. Aldosterone inhibitors limit the reabsorption by binding with mineralocorticoid receptor. Spironolactone is the only available aldosterone antagonist ; a metabolite of spironolactone, canrenone is also active.


i. Spironolactone (Aldactone)


Synthesis


Properties and uses: Spironolactone is a white or yellowish-white powder, practically insoluble in water and soluble in alcohol. It is a synthetic steroid that acts as a competitive antagonist of the potent, endogenous mineralocorticosteroid, aldosterone. It has a slower onset of action than triamterene or amiloride, but its natriuretic effect is slightly greater during long-term therapy. It is indicated in the treatment of essential hypertension, oedema associated with congestive heart failure, hepatic cirrhosis with ascites, the nephritic syndrome and hypokalemia, and in the diagnosis of primary aldosteronism. It is useful in the treatment of cirrhosis of liver, aldosterone secreting tumours, and high-renin hypertension.

Assay: Dissolve the sample in methanol and measure the absorbance of the solution after suitable dilution at the maxima of 238 nm using ultraviolet-spectrophotometer.

Diuretic-induced hypokalemia: Adult: 25–100 mg daily. Child: Neonates: 1–2 mg/kg daily; 1month-12 years; 1–3mg/kg daily: 12–18 years: 50–100 mg daily. To be given in 1–2 divided dose. Elderly: Dosing adjustment may be required.

Hirsutism in women: Adult: 50–200 mg daily. Elderly: Dosing adjustment may be required.

Dosage forms: Spironolactone tablets I.P., B.P.


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