Fundamentall and clinical aspects of the use of natural estrogens in the composition of modern combiened hormonal contraception

Authors

  • Д. В. Лизнева IPO Samara State Medical University, Russian Federation
  • А. И. Синицына JSC "Medical Company IDK" Samara, Russian Federation

DOI:

https://doi.org/10.18370/2309-4117.2012.6.43-48

Abstract

This review presents recent data on the specifics aspects of the pharmacokinetics, metabolism and biological effects of natural estrogens used in combined oral contraceptives.

Author Biography

Д. В. Лизнева, IPO Samara State Medical University

PhD, Department of Obstetrics and Gynecology

References

  1. Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric 2005; 8 (Suppl 1): 3-63.
  2. Aedo A.R., Landgren B.M., Diczfalusy E. Pharmacokinetics and biotransformation of orally administered oestrone sulphate and oestradiol valerate in postmenopausal women. Maturitas 1990; 12: 333-43.
  3. Kuhnz W., Gansau C., Mahler M. Pharmacokinetics of estradiol, free and total estrone, in young women following single intravenous and oral administration of 17b-estradiol. Drug Res 1993; 43: 966-73.
  4. Stadberg E., Westlund P., Landgren B.M. et al. Bioavailability of norethisterone acetate alone and in combination with estradiol administered in single or multiple oral doses to postmenopausal
  5. women. Maturitas 1999; 33: 59-69.
  6. Endrikat J., Parke S., Trummer D. et al. 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 (3): 218-225.
  7. Sitruk-Ware R. Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct; 61 (1-2): 151-7.
  8. Jung-Hoffmann C., Fitzner M., Kuhl H. Oralcontraceptives containing 20 or 30 mg ethinylestradiol and 150 mg desogestrel: pharmacokinetics and pharmacodynamic parameters. Horm Res 1991; 36: 238-46.
  9. Sitruk-Ware R. New progestagens for contraceptive use. Hum. Reprod Update. 2006; 12: 169-78.
  10. Parke S., Nahum G.G., Mellinger U., Junge W. Metabolic effects of a new four-phasic oral contraceptive containing estradiol valerate and dienogest. Obstet Gynecol. 2008; 111: 15S.
  11. Sitruk-Ware R.L., Menard J., Rad M., Burggraaf J., de Kam M.L.,Tokay B.A. et al. Comparison of the impact of vaginal and oral administration of combined hormonal contraceptives on hepatic proteins sensitive to estrogen. Contraception. 2007; 75: 430-7.
  12. Odlind V., Milsom I., Persson I., Victor A. Can changes in sex hormone binding globulin predict the risk of venous thromboem-bolism with combined oral contraceptive pills? Acta Obstet Gynecol Scand. 2002; 81: 482-90.
  13. Wiegratz I., Lee J.H., Kutschera E., Winkler U.H., Kuhl H. Effect of four oral contraceptives on hemostatic parameters. Contraception. 2004; 70: 97-106.
  14. Wiegratz I., Stahlberg S., Manthey T., Sänger N., Mittmann K., Lange E. et al. Effects of conventional or extended-cycle regimen of an oral contraceptive containing 30 mcg ethinylestradiol and 2mg dienogest on various hemostasis parameters. Contraception. 2008; 78: 384-91.
  15. Newburger J., Castracane V.D., Moore Jr. P.H., Williams M.C., Goldzieher J.W. The pharmacokinetics and metabolism of ethinyl estradiol and its three sulfates in the baboon. Am J Obstet Gynecol. 1983; 146: 80-7.
  16. Steingold K.A., Cefalu W., Pardridge W., Judd H.L., Chaudhuri G. Enhanced hepatic extraction of estrogens used for replacement therapy. J Clin Endocrinol Metab. 1986; 62: 761-6.
  17. Goebelsmann U., Mashchak C.A., Mishell Jr. D.R. Comparison of hepatic impact of oral and vaginal administration of ethinyl estradiol. Am J Obstet Gynecol. 1985;151:868–77.
  18. Kuhl H. Effects of progestogens on haemostasis. Maturitas.1996; 24: 1-19.
  19. Mashchak C.A., Lobo R.A., Dozono-Takano R., Eggena P., Nakamura R.M., Brenner P.F. et al. Comparison of pharmacodynamic properties of various estrogen formulations. Am J Obstet Gynecol. 1982; 144: 511-8.
  20. Parke S., Junge W., Mellinger U., Duijkers., Klipping C. Oral Comparative effects of a four-phasic regimen of estradiol valerate/dienogest versus ethinylestradiol/levonorgestrel on haemostatic parameters. Hum Reprod. 2008; 23: i77.
  21. Jensen J. Evaluation of a new estradiol oral contraceptive:estradiol valerate and dienogest. Expert Opin Pharmacother. 2010; 11: 1147-57.
  22. Parke S., Nahum G.G., Mellinger U., Junge W. Metabolic effects of a new four-phasic oral contraceptive containing estradiol valerate and dienogest. Obstet Gynecol. 2008; 111: 15S.
  23. Caruso S., Agnello C., Intelisano G., Farina M., Di Mari L., Cianci A. Sexual behavior of women taking low-dose oral contraceptive containing 15 microg ethinylestradiol/60 microg gestodene. Contraception. 2004 Mar; 69 (3): 237-40.
  24. Bouchard C., Brisson J., Fortier M., Morin C., Blanchette C. Use of oral contraceptive pills and vulvar vestibulitis: a case-control study. Am J Epidemiol. 2002 Aug 1; 156 (3): 254-61.
  25. Cayan F.J. Comparison of the effects of hormone therapy regimens, oral and vaginal estradiol, estradiol + drospirenone and tibolone, on sexual function in healthy postmenopausal women. SEX MED. 2008 Jan; 5(1): 132-8.
  26. Caruso S., Agnello C., Romano M., Cianci S., Lo Presti L., Malandrino C. and Cianci A. Preliminary study on the effect of four-phasic estradiol valerate and dienogest (E2V/DNG) oral contraceptive on the quality of sexual life. J. Sex Med 2011; 8: 2841-2850.
  27. Rossella E. Nappi, Susan R. Davis, Susanne Parke, Uwe Mellinger and Marco Serrani. Effects of Estradiol Valerate/Dienogest Compared with Ethinyl Estradiol/Levonorgestrel on Libido. Endocr Rev, Vol. 32 (MeetingAbstracts): P1-315.
  28. Yen and Jaffe’s Reproductive Endocrinology: Physiology, Pathophysiology, and Clinical Management , 5th edition.Chapter 14. Menopause and aging. P. 421-452.
  29. McEwen B.S., Akama K.T., Spencer-Segal J.L., Milner T.A., Waters E.M. Estrogen effects on the brain: actions beyond the hypothalamus via novel mechanisms. Behav Neurosci. 2012 Feb; 126 (1): 4-16.
  30. Walf A.A., Frye C.A. A review and update of mechanisms of estrogen in the hippocampus and amygdala for anxiety and depression behavior. Neuropsychopharmacology. 2006 Jun; 31 (6): 1097-111.
  31. Gibbs R.B. Estrogen therapy and cognition: a review of the cholinergic hypothesis. Endocr Rev. 2010 Apr; 31(2): 224-53. Epub. 2009, Dec 17.
  32. Molina R.C., Sandoval J.Z., Montero A.V., Oyarzún P.G., Molina T.G., González E.A. Comparative performance of a combined injectable contraceptive (50 mg norethisterone enanthate plus 5mg estradiol valerate) and a combined oral contraceptive (0.15 mg levonorgestrel plus 0.03 mg ethinyl estradiol) in adolescents. Pediatr Adolesc Gynecol. 2009 Feb; 22 (1): 25-31.
  33. Ahrendt H.-J., Makalova D., Parke S., Mellinger U., Mansour D. Bleeding pattern and cycle control with an estradiol-based oral contraceptive: a seven-cycle, randomized comparative trial of estradiol valerate/dienogest and ethinylestradiol/levonorgestrel. Contraception 2009; 80:436-44.
  34. Jordan V.C., Mittal S., Gosden B., Koch R., Lieberman M.E. Structure-activity relationships of estrogens. Environ Health Perspect. 1985 Sep; 61: 97-110.
  35. Ahrendt H.J., Makalová D., Parke S., Mellinger U., Mansour D. Bleeding pattern and cycle control with an estradiol-based oral contraceptive: a seven-cycle, randomized comparative trial of estradiol valerate/dienogest and ethinyl estradiol/levonorgestrel. Contraception. 2009 Nov; 80 (5): 436-44. Epub 2009, May 13.
  36. Ma P.T., Yamamoto T., Goldstein J.L., Brown M.S. Increased mRNA for low density lipoprotein receptor in livers of rabbits treated with 17 alpha-ethinyl estradiol. Proc Natl Acad Sci USA. 1986; 83: 792-6.

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Published

2012-08-14

How to Cite

Лизнева, Д. В., & Синицына, А. И. (2012). Fundamentall and clinical aspects of the use of natural estrogens in the composition of modern combiened hormonal contraception. REPRODUCTIVE ENDOCRINOLOGY, (6), 43–48. https://doi.org/10.18370/2309-4117.2012.6.43-48

Issue

No. 6 (2012)

Section

Endocrine gynecology

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Copyright (c) 2014 Д. В. Лизнева, А. И. Синицына

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