Antimineralocorticoid

Hyperkalemia Yasmin contains the progestin drospirenone that has antimineralocorticoid activity, including the potential for hyperkalemia in high-risk patients, comparable to a 25 mg dose of spironolactone. Yasmin should not be used in patients with conditions that predispose to hyperkalemia. Women receiving daily, long-term treatment for chronic conditions or diseases with medications that may increase serum potassium should have their serum potassium level checked during the first treatment cycle. 

The androgenic, anabolic, uterotropic, antioestrogenic, gestagenic, glucocorticoid, antiinflammatory, mineralocorticoid, antimineralocorticoid and adrenocorticoid activity of silatranes has been studied59. ... 

The antimineralocorticoidal activity of drospirenone is considered as a main benefit. It counteracts the salt and water retention effects of ethinylestradiol, the standard estrogen component in oral contraceptives [33]. 

Ulmann, A., Bertagna, C., Le Go, A., Husson, J.M., Tache, A., Sassano, P., Menard, J. and Corvol, P. (1985) Assessment of the antimineralocorticoid effect of RU 28318 in healthy men with induced exogenous and endogenous hypermineralocorticism. European Journal of Clinical Pharmacology, 28, 531-535. 

The syntheses of carbocyclic spiro-compounds via cycloaddition have been reviewed and some steroid examples are included. The synthesis of the antimineralocorticoid (379) was reported along with the syntheses of the 6/3-... 

Mineralocorticoids. Aldosterone [6251-69-0] (32), the most potent natural mineralocorticoid, also possesses a A4-3-one group, an oxygen substituent at Clip, and a C17p-2-hydroxyethan-l-one side chain. In addition, the C18 of aldosterone is oxidized to an aldehyde. Mineralocorticoids, particularly aldosterone, act to retain sodium and to prevent the retention of excess potassium. Antimineralocorticoids have been used therapeutically as diuretics and as agents that regulate blood pressure (63—65). 

Azidopyrimidines. The diuretic activity of a group of 2-amino-4-azido-6-phenylpyrimidines was found to depend upon the nature of the substituent in the S position [177,178], For example, the 2-ethoxyethyl derivative had general diuretic properties like the thiazides but in addition it was more potent than spironolactone as a mineralocorticoid antagonist. The 2-propynyl derivative Figure 1.14) was also a potent antimineralocorticoid but showed no general diuretic activity. Both compounds were potent antagonists of ADH. 

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