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(Hypertension. 2006;48:205.)
© 2006 American Heart Association, Inc.

Editorial Commentaries

Drospirenone

An Antihypertensive in Waiting

Domenic A. Sica

From the Section of Clinical Pharmacology and Hypertension, Division of Nephrology, Virginia Commonwealth University Health System, Richmond.

Correspondence to Domenic A. Sica, Section of Clinical Pharmacology and Hypertension, Division of Nephrology, Box 980160, MCV Station, 1101 East Marshall St, Sanger Hall, Room 8-062, Virginia Commonwealth University Health System, Richmond, VA 23298-0160. E-mail dsica@hsc.vcu.edu

An extract of the first 250 words of the full text is provided, because this article has no 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 17- 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 to young women resulted in a negative . . . [Full Text of this Article]

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Hypertension 2006 48: 246-253. [Abstract] [Full Text] [PDF]

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