Spiroxasone
A synthetic steroidal antimineralocorticoid and antiandrogen
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Spiroxasone is a synthetic steroidal antimineralocorticoid and antiandrogen that was developed for the treatment of conditions such as hypertension and heart failure. It is a derivative of spironolactone, a well-known potassium-sparing diuretic.
Pharmacology
Mechanism of Action
Spiroxasone acts as an antagonist of the mineralocorticoid receptor, which is responsible for the effects of aldosterone in the body. By blocking this receptor, spiroxasone reduces sodium reabsorption and increases potassium retention, leading to a diuretic effect. Additionally, it has antiandrogenic properties, which means it can block the effects of androgens like testosterone.
Pharmacokinetics
The pharmacokinetic profile of spiroxasone includes its absorption, distribution, metabolism, and excretion. Like other steroidal antimineralocorticoids, it is metabolized in the liver and excreted primarily in the urine.
Clinical Use
Spiroxasone was investigated for use in conditions such as hypertension, heart failure, and hirsutism. However, it was never marketed, and its clinical use remains limited to research settings.
Side Effects
Potential side effects of spiroxasone include hyperkalemia, gynecomastia, and menstrual irregularities. These are similar to those observed with other antimineralocorticoids and antiandrogens.
Chemical Structure
Spiroxasone is a synthetic steroid with a chemical structure similar to that of spironolactone. It contains a lactone ring and a thioacetate group, which are characteristic of this class of compounds.
Related Compounds
Spiroxasone is related to other antimineralocorticoids such as spironolactone and eplerenone. These compounds share similar mechanisms of action and therapeutic uses.
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