Contraception
Volume 81, Issue 1 , Pages 8-15 , January 2010

Review of clinical experience with estradiol in combined oral contraceptives

  • Franca Fruzzetti

      Affiliations

    • Department of Obstetrics and Gynecology, Ospedale S. Chiara, 56100 Pisa, Italy
    • Corresponding Author InformationCorresponding author. Tel.: +39 050 992 801; fax: +39 050 553410.
    • ,
  • Johannes Bitzer

      Affiliations

    • Universitätsspital Basel, Frauenklinik, 4031 Basel, Switzerland

Received 25 March 2009 ,Revised 1 July 2009 ,Accepted 19 August 2009.

References 

  1. Trussell J. Contraceptive efficacy. In:  Hatcher RA,  Trussell J,  Stewart F, et al. editor. Contraceptive Technology. 18th ed.. New York (NY): Irvington Publishers; 2004;p. 773–845
  2. Dusterberg B, Ellman H, Muller U, Rowe E, Muhe B. A three-year clinical investigation into efficacy, cycle control and tolerability of a new low-dose monophasic oral contraceptive containing gestodene. Gynecol Endocrinol. 1996;10:33–39
  3. Huber J, Foidart JM, Wuttke W, et al. Efficacy and tolerability of a monophasic oral contraceptive containing ethinylestradiol and drospirenone. Eur J Contracept Reprod Health Care. 2000;5:25–34
  4. Sitruk-Ware R. New progestagens for contraceptive use. Hum Reprod Update. 2006;12:169–178
  5. Spona J, Feichtinger W, Kindermann C, et al. Modulation of ovarian function by an oral contraceptive containing 30 micrograms ethinyl estradiol in combination with 2.00 mg dienogest. Contraception. 1997;56:185–191
  6. Krattenmacher R, Knauthe R, Parczyk K, Walker A, Hilgenfeldt U, Fritzemeier KH. Estrogen action on hepatic synthesis of angiotensinogen and IGF-I: direct and indirect estrogen effects. J Steroid Biochem Mol Biol. 1994;48:207–214
  7. Lindberg UB, Crona N, Stigendal L, Teger-Nilsson AC, Silfverstolpe G. A comparison between effects of estradiol valerate and low dose ethinyl estradiol on haemostasis parameters. Thromb Haemost. 1989;61:65–69
  8. Toy JL, Davies JA, Hancock KW, McNicol GP. The comparative effects of a synthetic and a 'natural' oestrogen on the haemostatic mechanism in patients with primary amenorrhoea. Br J Obstet Gynaecol. 1978;85:359–362
  9. Wiegratz I, Lee JH, Kutschera E, Winkler UH, Kuhl H. Effect of four oral contraceptives on hemostatic parameters. Contraception. 2004;70:97–106
  10. Bottiger LE, Boman G, Eklund G, Westerholm B. Oral contraceptives and thromboembolic disease: effects of lowering oestrogen content. Lancet. 1980;1:1097–1101
  11. Farmer RDT, Preston TD. The risk of venous thromboembolism associated with low oestrogen oral contraceptives. J Obstet Gynaecol. 1995;14:195–200
  12. Gallo MF, Nanda K, Grimes DA, Schulz KF. 20 mcg versus >20 mcg estrogen combined oral contraceptives for contraception. Cochrane Database Syst Rev. 2005;CD003989
  13. Dinger JC, Heinemann LA, Kuhl-Habich D. The safety of a drospirenone-containing oral contraceptive: final results from the European Active Surveillance Study on oral contraceptives based on 142,475 women-years of observation. Contraception. 2007;75:344–354
  14. Speroff L, Fritz MA. In: Clinical Gynecologic Endocrinology and Infertility. 7th ed.. Philadelphia, PA: Lippincott Williams & Wilkins; 2005;p. 866
  15. Bostofte E, Hemmingsen L, Moller KJ, Serup J, Weber T. Serum lipids and lipoproteins during treatment with oral contraceptives containing natural and synthetic oestrogens. A controlled double-blind investigation. Acta Endocrinol (Copenh). 1978;87:855–864
  16. Helgason S. Estrogen replacement therapy after the menopause. Estrogenicity and metabolic effects. Acta Obstet Gynecol Scand Suppl. 1982;107:1–29
  17. Mashchak CA, Lobo RA, Dozono-Takano R, et al. Comparison of pharmacodynamic properties of various estrogen formulations. Am J Obstet Gynecol. 1982;144:511–518
  18. World Health Organization Task Force on Oral Contraception . A randomized, double-blind study of two combined oral contraceptives containing the same progestogen, but different estrogens. Contraception. 1980;21:445–459
  19. Serup J, Bostofte E, Larsen S, Westergaard J. Effectivity and acceptability of oral contraceptives containing natural and artificial estrogens in combination with a gestagen. A controlled double-blind investigation. Acta Obstet Gynecol Scand. 1981;60:203–206
  20. Serup J, Bostofte E, Larsen S, Westergaard J, Lebech PE. Natural oestrogens for oral contraception. Lancet. 1979;2:471–472
  21. Wenzl R, Bennink HC, van Beek A, Spona J, Huber J. Ovulation inhibition with a combined oral contraceptive containing 1 mg micronized 17 beta-estradiol. Fertil Steril. 1993;60:616–619
  22. Kivinen S, Saure A. Efficacy and tolerability of a combined oral contraceptive containing 17 beta-estradiol and desogestrel (Abstract). Eur J Contracept Reprod Health Care. 1996;1:183
  23. Astedt B, Jeppsson S, Liedholm P, Rannevik G, Svanberg L. Clinical trial of a new oral contraceptive pill containing the natural oestrogen 17 beta-oestradiol. Br J Obstet Gynaecol. 1979;86:732–736
  24. Schubert W, Cullberg G. Ovulation inhibition with 17 beta-estradiol cyclo-octyl acetate and desogestrel. Acta Obstet Gynecol Scand. 1987;66:543–547
  25. Csemiczky G, Dieben T, Coeling Bennink HJ, Landgren BM. The pharmacodynamic effects of an oral contraceptive containing 3 mg micronized 17 beta-estradiol and 0.150 mg desogestrel for 21 days, followed by 0.030 mg desogestrel only for 7 days. Contraception. 1996;54:333–338
  26. Hirvonen E, Stenman UH, Malkonen M, Rasi V, Vartiainen E, Ylostalo P. New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women. Maturitas. 1988;10:201–213
  27. Hirvonen E, Allonen H, Anttila M, et al. Oral contraceptive containing natural estradiol for premenopausal women. Maturitas. 1995;21:27–32
  28. Dusterberg B, Nishino Y. Pharmacokinetic and pharmacological features of oestradiol valerate. Maturitas. 1982;4:315–324
  29. Timmer CJ, Geurts TB. Bioequivalence assessment of three different estradiol formulations in postmenopausal women in an open, randomized, single-dose, 3-way cross-over study. Eur J Drug Metab Pharmacokinet. 1999;24:47–53
  30. Kuhnz W, Blode H, Zimmermann H. Pharmacokinetics of exogenous natural and synthetic estrogens and antiestrogens. In:  Oettel M,  Schillinger E editor. Handbook of Experimental Pharmacology, Estrogens and Antiestrogens II. Berlin: Springer Verlag; 1999;p. 261–322
  31. Kovacs L, Hoffmann H. A new low-dose oral contraception containing ethinylestradiol, estradiol and dienogest: first experience of its clinical use. In:  Elstein M editors. Extragenital effects of oral contraceptives. Carnforth: Parthenon; 1997;p. 39–44
  32. Hoffmann H, Moore C, Kovacs L, et al. Alternatives of the replacement of ethinylestradiol by natural 17beta-estradiol in dienogest-containing oral contraceptives. Drugs of Today. 1999;35:105–113
  33. Hoffmann H, Moore C, Zimmermann H, et al. Approaches to the replacement of ethinylestradiol by natural 17beta-estradiol in combined oral contraceptives. Exp Toxicol Pathol. 1998;50:458–464
  34. Oettel M, Breitbarth H, Elger W, et al. The pharmacological profile of dienogest. Eur J Contracept Reprod Health Care. 1999;4:2–13
  35. Oettel M, Graeser T, Hoffmann H, Moore C, Zimmermann H, Zimmermann T. The preclinical and clinical profile of dienogest. A short overview. Drugs Today. 1999;35:3–12
  36. Sasagawa S, Shimizu Y, Kami H, et al. Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008;73:222–231
  37. Oettel M, Bervoas-Martin S, Elger W, et al. A 19-norprogestin without 17alpha-ethinyl group I: dienogest from a pharmacokinetic point of view. Drugs Today. 1995;31:499–516
  38. Golbs S, Domhardt R, Presl J, Ganev M, Wisser KH, Zimmermann T. Clinical findings with the oral contraceptive combination ethinylestradiol/dienogest in the Czech Republic. Methods Find Exp Clin Pharmacol. 2002;24:689–696
  39. Golbs S, Domhardt R, Radowicky S, Kaluzny Z, Wisser KH, Zimmermann T. Clinical findings with the oral contraceptive combination ethinylestradiol/dienogest in Poland. Methods Find Exp Clin Pharmacol. 2002;24:585–592
  40. Zimmermann T, Dietrich H, Wisser KH, Hoffmann H. The efficacy and tolerability of Valette: a postmarketing surveillance study. Eur J Contracept Reprod Health Care. 1999;4:155–164
  41. Endrikat J, Parke S, Trummer D, Schmidt W, Duijkers I, Klipping C. Ovulation inhibition with four variations of a four-phasic estradiol valerate/dienogest combined oral contraceptive: results of two prospective, randomized, open-label studies. Contraception. 2008;78:218–225
  42. Nahum GG, Parke S, Wildt L, Palacios S, Roemer T, Bitzer J. Efficacy and tolerability of a new oral contraceptive containing estradiol and dienogest. Obstet Gynecol. 2008;111(4 Suppl):15S
  43. Parke S, Makalova D, Ahrendt HJ, Mansour D. Bleeding patterns and cycle control with a novel four-phasic combined oral contraceptive containing estradiol valerate and dienogest. Eur J Contracept Reprod Health Care. 2008;13(Suppl):94
  44. Parke S, Junge W, Mellinger U, Duijkers I, Klipping C. Comparative effects of a four-phasic regimen of estradiol valerate/dienogest versus ethinylestradiol/levonorgestrel on haemostatic parameters. Hum Reprod Update. 2008;23(Suppl 1):i78–i79
  45. Parke S, Nahum G, Mellinger U, Junge W. Metabolic effects of a new four-phasic oral contraceptive containing estradiol valerate and dienogest. Obstet Gynecol. 2008;111(4 Suppl):12S–13S
  46. Longcope C, Williams KI. The metabolism of estrogens in normal women after pulse injections of 3H-estradiol and 3H-estrone. J Clin Endocrinol Metab. 1974;38:602–607

PII: S0010-7824(09)00384-9

doi: 10.1016/j.contraception.2009.08.010

Contraception
Volume 81, Issue 1 , Pages 8-15 , January 2010

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