Drospirenone

Abstract

Drospirenone (DRSP) is a compound with mingled identities having been viewed as a diuretic,1 a progestational agent,2 and/or an antimineralocorticoid agent with an ability to reduce blood pressure (BP).3–6 The multiple personalities of this compound can be seen by examining the position adopted by the United States Anti-Doping Agency on its use as a diuretic in athletes. Until January 2005, athletes were prohibited from using the fixed-dose combination contraceptive product (3-mg DRSP/0.03-mg ethinylestradiol [EE]) in or out of competition specifically because it contained the diuretic DRSP, albeit a compound with very weak diuretic properties.1 This restriction on DRSP use in athletes has been lifted, although the use of spironolactone is still outlawed. More recently, DRSP has gained some momentum as an antihypertensive agent.3–6 All along, DRSP has been a progestational agent used in combination with estrogen for birth control or treatment of vasomotor symptoms relating to menopause.2 DRSP, formerly called dihydrospirorenone, is chemically related to 17α- spironolactone. It is a synthetic progestogen, which more closely resembles natural progesterone than conventional synthetic progestogens. As such, it possesses clinically recognizable antimineralocorticoid activity and is estimated to be 8 times more potent than spironolactone (3 mg of DRSP=25 mg of spironolactone).7 DRSP pharmacokinetics are such that it has an oral bioavailability of &80%, a half-life of 30 to 35 hours, and is without active metabolites, a characteristic that distinguishes it from spironolactone.7 In early studies, administration of 2 mg of DRSP daily for 6 days …