Drospirenone (DRSP) is used by itself as a progestogen-only birth control pill, in combination with the estrogens ethinylestradiol (EE) or estetrol (E4), with or without supplemental folic acid (vitamin B), as a combined birth control pill, and in combination with the estrogen estradiol (E2) for use in menopausal hormone therapy. A birth control pill with low-dose ethinylestradiol is also indicated for the treatment of moderate acne, premenstrual syndrome (PMS), premenstrual dysphoric disorder (PMDD), and dysmenorrhea (painful menstruation). For use in menopausal hormone therapy, E2/DRSP is specifically approved to treat moderate to severe vasomotor symptoms (hot flashes), vaginal atrophy, and postmenopausal osteoporosis. The drospirenone component in this formulation is included specifically to prevent estrogen-induced endometrial hyperplasia. Drospirenone has also been used in combination with an estrogen as a component of hormone therapy for transgender women.
Studies have found that EE/DRSP is superior to placebo in reducing premenstrual emotional and physical symptoms while also improving quality of life. E2/DRSP has been found to increase bone mineral density and to reduce the occurrence of bone fractures in postmenopausal women. In addition, E2/DRSP has a favorable influence on cholesterol and triglyceride levels and decreases blood pressure in women with high blood pressure. Due to its antimineralocorticoid activity, drospirenone opposes estrogen-induced salt and water retention and maintains or slightly reduces body weight.