Drospirenone/ethinylestradiol: A review on efficacy and noncontraceptive benefits

Women's Health

Volumn 7, Issue 1, 2011, Pages 19-30

  Machado, Rogério Bonassi ^c   De Melo Pompei, Luciano ^a   Giribela, Arcia Galvão ^b   Giribela, Cassiana Galvão ^b  

^a FACULDADE DE MEDICINA DO ABC   (Brazil)

^b UNIVERSITY OF SÃO PAULO   (Brazil)

^c NONE

Author keywords

drospirenone; efficacy; ethinylestradiol; noncontraceptive benefits; oral contraception; premenstrual dysphoric syndrome

Indexed keywords

ALDOSTERONE; CYPROTERONE ACETATE; DROSPIRENONE; DROSPIRENONE PLUS ETHINYLESTRADIOL; ETHINYLESTRADIOL; ETHINYLESTRADIOL PLUS LEVONORGESTREL; NANDROLONE DERIVATIVE; ORAL CONTRACEPTIVE AGENT; PLACEBO; POTASSIUM; PROGESTERONE RECEPTOR; RENIN; SODIUM; SPIRONOLACTONE;

ACNE; AMENORRHEA; ANTIANDROGEN THERAPY; AREA UNDER THE CURVE; BINDING AFFINITY; CLINICAL TRIAL; DEPRESSION; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG EFFECT; DRUG EFFICACY; DRUG FECES LEVEL; DRUG HALF LIFE; DRUG INDICATION; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG TOLERABILITY; DRUG URINE LEVEL; DRUG WITHDRAWAL; DYSMENORRHEA; EDEMA; FLUID RETENTION; HEADACHE; HORMONE SUBSTITUTION; HUMAN; KALIURESIS; LOW DRUG DOSE; MASTALGIA; MAXIMUM PLASMA CONCENTRATION; METRORRHAGIA; MOOD CHANGE; MULTIPLE CYCLE TREATMENT; NATRIURESIS; NAUSEA; NONHUMAN; ORAL CONTRACEPTION; OVARY CYCLE; OVULATION INHIBITION; PATIENT COMPLIANCE; PREGNANCY OUTCOME; PREMENSTRUAL DYSPHORIC DISORDER; PSYCHOLOGICAL WELL BEING; RENIN ANGIOTENSIN ALDOSTERONE SYSTEM; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; SKIN DISEASE; SPOTTING; TREATMENT OUTCOME; UTERINE CERVIX MUCUS; VAGINA BLEEDING; WEIGHT GAIN; WEIGHT REDUCTION;

ACNE VULGARIS; ALDOSTERONE ANTAGONISTS; ANDROSTENES; CONTRACEPTIVES, ORAL, COMBINED; DYSMENORRHEA; ENDOMETRIUM; ETHINYL ESTRADIOL; FEMALE; HUMANS; PREMENSTRUAL SYNDROME;

EID: 78650656131     PISSN: 17455057     EISSN: 17455065     Source Type: Journal    
DOI: 10.2217/whe.10.84     Document Type: Review

References (50)

1. Petitti DB: Clinical practice. Combination estrogen-progestin oral contraceptives. N. Engl. J. Med. 349(15), 1443-1450 (2003).
2. Sitruk-Ware R: New progestagens for contraceptive use. Hum. Reprod. Update 12(2), 169-178 (2006).
3. Pearlstein TB, Bachmann GA, Zacur HA, Yonkers KA: Treatment of premenstrual dysphoric disorder with a new drospirenone-containing oral contraceptive formulation. Contraception 72(6), 414-421 (2005).
4. Yonkers KA, Brown C, Pearlstein TB, Foegh M, Sampson-Landers C, Rapkin A: Efficacy of a new low-dose oral contraceptive with drospirenone in premenstrual dysphoric disorder. Obstet. Gynecol. 106(3), 492-501 (2005).
5. Blode H, Wuttke W, Loock W, Röll G, Heithecker R: A 1-year pharmacokinetic investigation of a novel oral contraceptive containing drospirenone in healthy female volunteers. Eur. J. Contracept. Reprod. Health Care 5(4), 256-264 (2000). (Pubitemid 32165464)
6. Kuhnz W, Blode H, Zimmermann H: Pharmacokinetics of exogenous natural and synthetic estrogens and antiestrogens. In: Handbook of experimental Pharmacology. Oettel M, Schillinger E (Eds.). Springer-Verlag, Berlin, 281-291 (1999).
7. Blode H: Pharmacokinetics of drospirenone. Gynaecol. Forum 7(1), 18-22 (2002).
8. Keam SJ, Wagstaff AJ: Ethinylestradiol/ drospirenone: a review of its use as an oral contraceptive. Treat. Endocrinol. 2(1), 49-70 (2003).
9. Muhn P, Krattenmacher R, Beier S, Elger W, Schillinger E: Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Pharmacological characterization in animal models. Contraception 51(2), 99-110 (1995).
10. Krattenmacher R: Drospirenone: pharmacology and pharmacokinetics of a unique progestogen. Contraception 62(1), 29-38 (2000).
11. Rosenbaum P, Schmidt W, Helmerhorst FM et al.: Inhibition of ovulation by a novel progestogen (drospirenone) alone or in combination with ethinylestradiol. Eur. J. Contracept. Reprod. Health Care 5(1), 16-24 (2000).
12. Endrikat J, Gerlinger C, Plettig K et al.: A meta-analysis on the correlation between ovarian activity and the incidence of intermenstrual bleeding during low-dose oral contraceptive use. Gynecol. Endocrinol. 17(2), 107-114 (2003).
13. Klipping C, Marr J, Korner P: Ovulation inhibition effects of two low-dose oral contraceptive dosing regimens following intentional dosing errors. Presented at: The American College of Obstetricians and Gynecologists 54th Annual Clinical Meeting. Washington, USA, 6-10 May (2006).
14. Goldzieher JW: Pharmacology of contraceptive steroids: a brief review. Am. J. Obstet. Gynecol. 160(5 Pt 2), 1260-1264 (1989).
15. Muhn P, Fuhrmann U, Fritzemeier KH, Krattenmacher R, Schillinger E: Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Ann. N. Y. Acad. Sci. 761, 311-335 (1995).
16. Fuhrmann U, Krattenmacher R, Slater EP, Fritzemeier KH: The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception 54(4), 243-251 (1996).
17. Oelkers W, Foidart JM, Dombrovicz N, Welter A, Heithecker R: Effects of a new oral contraceptive containing an antimineralocorticoid progestogen, drospirenone, on the renin-aldosterone system, body weight, blood pressure, glucose tolerance, and lipid metabolism. J. Clin. Endocrinol. Metab. 80(6), 1816-1821 (1995).
18. Oelkers W, Berger V, Bolik A et al.: Dihydrospirorenone, a new progestogen with antimineralocorticoid activity: effects on ovulation, electrolyte excretion, and the renin- aldosterone system in normal women. J. Clin. Endocrinol. Metab. 73(4), 837-842 (1991).
19. Oelkers W, Helmerhorst FM, Wuttke W, Heithecker R: Effect of an oral contraceptive containing drospirenone on the renin- angiotensin-aldosterone system in healthy female volunteers. Gynecol. Endocrinol. 14(3), 204-213 (2000). (Pubitemid 30449898)
20. Van Vloten WA, van Haselen CW, van Zuuren EJ, Gerlinger C, Heithecker R: The effect of 2 combined oral contraceptives containing either drospirenone or cyproterone acetate on acne and seborrhea. Cutis 69(Suppl. 4), 2-15 (2002).
21. Bachmann G, Sulak PJ, Sampson-Landers C, Benda N, Marr J: Efficacy and safety of a low-dose 24-day combined oral contraceptive containing 20 mcg ethinylestradiol and 3 mg drospirenone. Contraception 70(3), 191-198 (2004).
22. Hernádi L, Marr J, Trummer D, De Leo V, Petraglia F: Efficacy and safety of a low-dose combined oral contraceptive containing drospirenone 3 mg and ethinylestradiol 20 mcg in a 24/4-day regimen. Contraception 80(1), 18-24 (2009).
23. Koltun W, Lucky AW, Thiboutot D et al.: Efficacy and safety of 3 mg drospirenone/ 20 mcg ethinylestradiol oral contraceptive administered in 24/4 regimen in the treatment of acne vulgaris: a randomized, double-blind, placebo-controlled trial. Contraception 77(4), 249-256 (2008).
24. Maloney JM, Dietze P Jr, Watson D et al.: Treatment of acne using a 3-milligram drospirenone/20-microgram ethinyl estradiol oral contraceptive administered in a 24/4 regimen: a randomized controlled trial. Obstet. Gynecol. 112(4), 773-781 (2008).
25. Cibula D, Karck U, Weidenhammer HG, Kunz J, Alincic S, Marr J: Efficacy and safety of a low-dose 21-day combined oral contraceptive containing ethinylestradiol 20microg and drospirenone 3mg. Clin. Drug Investig. 26(3), 143-150 (2006).
26. Anttila L, Kunz M, Marr J: Bleeding pattern with drospirenone 3 mg+ethinyl estradiol 20 mcg 24/4 combined oral contraceptive compared with desogestrel 150 mcg+ethinyl estradiol 20 mcg 21/7 combined oral contraceptive. Contraception 80(5), 445-451 (2009).
27. Klipping C, Marr J: Effects of two combined oral contraceptives containing ethinyl estradiol 20 microg combined with either drospirenone or desogestrel on lipids, hemostatic parameters and carbohydrate metabolism. Contraception. 71(6), 409-416 (2005).
28. Parsey KS, Pong A: An open-label, multicenter study to evaluate Yasmin, a low-dose combination oral contraceptive containing drospirenone, a new progestogen. Contraception 61(2), 105-111 (2000).
29. Endrikat JS, Milchev NP, Kapamadzija A et al.: Bleeding pattern, tolerance and patient satisfaction with a drospirenone-containing oral contraceptive evaluated in 3488 women in Europe, the Middle East and Canada. Contraception 79(6), 428-432 (2009).
30. Short M: User satisfaction with the combined oral contraceptive drospirenone 3 mg/ ethinylestradiol 20 microg (Yasminelle) in clinical practice: a multi-country, questionnaire-based study. Clin. Drug Investig. 29(3), 153-159 (2009).
31. Apter D, Borsos A, Baumgrtner W et al.: Effect of an oral contraceptive containing drospirenone and ethinylestradiol on general well-being and fluid-related symptoms. Eur. J. Contracept. Reprod. Health Care 8(1), 37-51 (2003).
32. Oelkers W: Drospirenone - a new progestogen with antimineralocorticoid activity, resembling natural progesterone. Eur. J. Contracept. Reprod. Health Care 5(Suppl. 3), 17-24 (2000).
33. Sangthawan M, Taneepanichskul S: A comparative study of monophasic oral contraceptives containing either drospirenone 3 mg or levonorgestrel 150 g on premenstrual symptoms. Contraception 71(1), 1-7 (2005)
34. Machado RB, Tachotti F, Cavenague G, Maia E: Effects of two different oral contraceptives on total body water: a randomized study. Contraception 73(4), 344-347 (2006).
35. Rosenberg MJ, Waugh MS, Meehan TE: Use and misuse of oral contraceptives: risk indicators for poor pill taking and discontinuation. Contraception 51(5), 283-288 (1995).
36. Hoppe G: Gestoden, an innovative progestogen. Contraception 37(5), 493-501 (1988).
37. Gestodene Study Group: Cycle control, safety and efficacy of a 24-day regimen of gestodene 60 microg/ ethinylestradiol 15 g and a 21-day regimen of desogestrel 150 g/ ethinylestradiol 20 g. Eur. J. Contracept. Reprod. Health Care 4(Suppl 2), 17-25 (1999).
38. Bckström T, Hansson-Malmström Y, Lindhe BA, Cavalli-Björkman B, Nordenström S: Oral contraceptives in premenstrual syndrome: a randomized comparison of triphasic and monophasic preparations. Contraception 46(3), 253-268 (1992).
39. Graham CA, Sherwin BB: A prospective treatment study of premenstrual symptoms using a triphasic oral contraceptive. J. Psychosom. Res. 36(3), 257-266 (1992).
40. Eriksson E, Sundblad C, Lisjö P, Modigh K, Andersch B: Serum levels of androgens are higher in women with premenstrual irritability and dysphoria than in controls. Psychoneuroendocrinology 17(2-3), 195-204 (1992).
41. Dougherty DM, Bjork JM, Moeller FG, Swann AC: The influence of menstrual-cycle phase on the relationship between testosterone and aggression. Physiol. Behav. 62(2), 431-435 (1997).
42. Sulak PJ, Scow RD, Preece C, Riggs MW, Kuehl TJ: Hormone withdrawal symptoms in oral contraceptive users. Obstet. Gynecol. 95(2), 261-266 (2000).
43. Sillem M, Schneidereit R, Heithecker R, Mueck AO: Use of an oral contraceptive containing drospirenone in an extended regimen. Eur. J. Contracept. Reprod. Health Care 8(3), 162-169 (2003).
44. Machado RB, de Melo NR, Maia H Jr: Bleeding patterns and menstrual-related symptoms with the continuous use of a contraceptive combination of ethinylestradiol and drospirenone: a randomized study. Contraception 81(3), 215-222 (2010).
45. Shrader SP, Dickerson LM: Extended- and continuous-cycle oral contraceptives. Pharmacotherapy 28(8), 1033-1040 (2008).
46. Cremer M, Phan-Weston S, Jacobs A: Recent innovations in oral contraception. Semin. Reprod. Med. 28(2), 140-146 (2010).
47. Coffee AL, Sulak PJ, Kuehl TJ: Long-term assessment of symptomatology and satisfaction of an extended oral contraceptive regimen. Contraception 75(6), 444-449 (2007).
48. Kwiecien M, Edelman A, Nichols MD, Jensen JT: Bleeding patterns and patient acceptability of standard or continuous dosing regimens of a low-dose oral contraceptive: a randomized trial. Contraception 67(1), 9-13 (2003).
49. Archer DF, Jensen JT, Johnson JV, Borisute H, Grubb GS, Constantine GD: Evaluation of a continuous regimen of levonorgestrel/ethinyl estradiol: Phase 3 study results. Contraception 74(6), 439-445 (2006).
50. Vercellini P, Frontino G, De Giorgi O, Pietropaolo G, Pasin R, Crosignani PG: Continuous use of an oral contraceptive for endometriosis-associated recurrent dysmenorrhea that does not respond to a cyclic pill regimen. Fertil. Steril. 80(3), 560-563 (2003).