Review of clinical experience with estradiol in combined oral contraceptives

Contraception

Volumn 81, Issue 1, 2010, Pages 8-15

  Fruzzetti, Franca ^a   Bitzer, Johannes ^b  

^a SANTA CHIARA HOSPITAL   (Italy)

^b UNIVERSITY WOMEN S HOSPITAL   (Switzerland)

Author keywords

Bleeding outcomes; Dienogest; Estradiol; Estradiol valerate; Oral contraceptives; Progestin

Indexed keywords

CYPROTERONE ACETATE; DESOGESTREL; DIENOGEST; DIENOGEST PLUS ETHINYLESTRADIOL; ESTRADIOL; ESTRADIOL VALERATE; ESTRIOL; ETHINYLESTRADIOL; ETHINYLESTRADIOL PLUS NORETHISTERONE; FEMILAR; GESTAGEN; LEVONORGESTREL; NETAGEN 403; NETAGEN 423; NORETHISTERONE; NORETHISTERONE ACETATE; ORAL CONTRACEPTIVE AGENT; UNCLASSIFIED DRUG;

AMENORRHEA; CLINICAL TRIAL; DRUG ABSORPTION; DRUG RESEARCH; DRUG SAFETY; DRUG SYNTHESIS; DRUG WITHDRAWAL; HORMONAL CONTRACEPTION; HORMONE RESPONSE; HUMAN; MENSTRUAL CYCLE; MENSTRUAL IRREGULARITY; NAUSEA; OPTIMAL DRUG DOSE; ORAL CONTRACEPTION; OVULATION INHIBITION; REVIEW; SIDE EFFECT; SPOTTING; WEIGHT GAIN;

CLINICAL TRIALS AS TOPIC; CONTRACEPTIVES, ORAL, COMBINED; ESTRADIOL; FEMALE; HUMANS; TREATMENT OUTCOME;

EID: 71249120726     PISSN: 00107824     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.contraception.2009.08.010     Document Type: Review

References (46)

1. Trussell J. Contraceptive efficacy. In: Hatcher R.A., Trussell J., Stewart F., et al. (Eds). Contraceptive Technology. 18th ed. (2004), Irvington Publishers, New York (NY) 773-845
2. Dusterberg B., Ellman H., Muller U., Rowe E., and 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 10 (1996) 33-39
3. Huber J., Foidart J.M., Wuttke W., et al. Efficacy and tolerability of a monophasic oral contraceptive containing ethinylestradiol and drospirenone. Eur J Contracept Reprod Health Care 5 (2000) 25-34
4. Sitruk-Ware R. New progestagens for contraceptive use. Hum Reprod Update 12 (2006) 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 56 (1997) 185-191
6. Krattenmacher R., Knauthe R., Parczyk K., Walker A., Hilgenfeldt U., and Fritzemeier K.H. Estrogen action on hepatic synthesis of angiotensinogen and IGF-I: direct and indirect estrogen effects. J Steroid Biochem Mol Biol 48 (1994) 207-214
7. Lindberg U.B., Crona N., Stigendal L., Teger-Nilsson A.C., and Silfverstolpe G. A comparison between effects of estradiol valerate and low dose ethinyl estradiol on haemostasis parameters. Thromb Haemost 61 (1989) 65-69
8. Toy J.L., Davies J.A., Hancock K.W., and McNicol G.P. The comparative effects of a synthetic and a 'natural' oestrogen on the haemostatic mechanism in patients with primary amenorrhoea. Br J Obstet Gynaecol 85 (1978) 359-362
9. Wiegratz I., Lee J.H., Kutschera E., Winkler U.H., and Kuhl H. Effect of four oral contraceptives on hemostatic parameters. Contraception 70 (2004) 97-106
10. Bottiger L.E., Boman G., Eklund G., and Westerholm B. Oral contraceptives and thromboembolic disease: effects of lowering oestrogen content. Lancet 1 (1980) 1097-1101
11. Farmer R.D.T., and Preston T.D. The risk of venous thromboembolism associated with low oestrogen oral contraceptives. J Obstet Gynaecol 14 (1995) 195-200
12. Gallo M.F., Nanda K., Grimes D.A., and Schulz K.F. 20 mcg versus >20 mcg estrogen combined oral contraceptives for contraception. Cochrane Database Syst Rev (2005) CD003989
13. Dinger J.C., Heinemann L.A., and 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 75 (2007) 344-354
14. Speroff L., and Fritz M.A. Clinical Gynecologic Endocrinology and Infertility. 7th ed. (2005), Lippincott Williams & Wilkins, Philadelphia, PA 866
15. Bostofte E., Hemmingsen L., Moller K.J., Serup J., and Weber T. Serum lipids and lipoproteins during treatment with oral contraceptives containing natural and synthetic oestrogens. A controlled double-blind investigation. Acta Endocrinol (Copenh) 87 (1978) 855-864
16. Helgason S. Estrogen replacement therapy after the menopause. Estrogenicity and metabolic effects. Acta Obstet Gynecol Scand Suppl 107 (1982) 1-29
17. Mashchak C.A., Lobo R.A., Dozono-Takano R., et al. Comparison of pharmacodynamic properties of various estrogen formulations. Am J Obstet Gynecol 144 (1982) 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 21 (1980) 445-459
19. Serup J., Bostofte E., Larsen S., and 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 60 (1981) 203-206
20. Serup J., Bostofte E., Larsen S., Westergaard J., and Lebech P.E. Natural oestrogens for oral contraception. Lancet 2 (1979) 471-472
21. Wenzl R., Bennink H.C., van Beek A., Spona J., and Huber J. Ovulation inhibition with a combined oral contraceptive containing 1 mg micronized 17 beta-estradiol. Fertil Steril 60 (1993) 616-619
22. Kivinen S., and Saure A. Efficacy and tolerability of a combined oral contraceptive containing 17 beta-estradiol and desogestrel (Abstract). Eur J Contracept Reprod Health Care 1 (1996) 183
23. Astedt B., Jeppsson S., Liedholm P., Rannevik G., and Svanberg L. Clinical trial of a new oral contraceptive pill containing the natural oestrogen 17 beta-oestradiol. Br J Obstet Gynaecol 86 (1979) 732-736
24. Schubert W., and Cullberg G. Ovulation inhibition with 17 beta-estradiol cyclo-octyl acetate and desogestrel. Acta Obstet Gynecol Scand 66 (1987) 543-547
25. Csemiczky G., Dieben T., Coeling Bennink H.J., and Landgren B.M. 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 54 (1996) 333-338
26. Hirvonen E., Stenman U.H., Malkonen M., Rasi V., Vartiainen E., and Ylostalo P. New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women. Maturitas 10 (1988) 201-213
27. Hirvonen E., Allonen H., Anttila M., et al. Oral contraceptive containing natural estradiol for premenopausal women. Maturitas 21 (1995) 27-32
28. Dusterberg B., and Nishino Y. Pharmacokinetic and pharmacological features of oestradiol valerate. Maturitas 4 (1982) 315-324
29. Timmer C.J., and Geurts T.B. 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 24 (1999) 47-53
30. Kuhnz W., Blode H., and Zimmermann H. Pharmacokinetics of exogenous natural and synthetic estrogens and antiestrogens. In: Oettel M., and Schillinger E. (Eds). Handbook of Experimental Pharmacology, Estrogens and Antiestrogens II (1999), Springer Verlag, Berlin 261-322
31. Kovacs L., and Hoffmann H. A new low-dose oral contraception containing ethinylestradiol, estradiol and dienogest: first experience of its clinical use. In: Elstein M. (Ed). Extragenital effects of oral contraceptives (1997), Parthenon, Carnforth 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 35 (1999) 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 50 (1998) 458-464
34. Oettel M., Breitbarth H., Elger W., et al. The pharmacological profile of dienogest. Eur J Contracept Reprod Health Care 4 (1999) 2-13
35. Oettel M., Graeser T., Hoffmann H., Moore C., Zimmermann H., and Zimmermann T. The preclinical and clinical profile of dienogest. A short overview. Drugs Today 35 (1999) 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 73 (2008) 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 31 (1995) 499-516
38. Golbs S., Domhardt R., Presl J., Ganev M., Wisser K.H., and Zimmermann T. Clinical findings with the oral contraceptive combination ethinylestradiol/dienogest in the Czech Republic. Methods Find Exp Clin Pharmacol 24 (2002) 689-696
39. Golbs S., Domhardt R., Radowicky S., Kaluzny Z., Wisser K.H., and Zimmermann T. Clinical findings with the oral contraceptive combination ethinylestradiol/dienogest in Poland. Methods Find Exp Clin Pharmacol 24 (2002) 585-592
40. Zimmermann T., Dietrich H., Wisser K.H., and Hoffmann H. The efficacy and tolerability of Valette: a postmarketing surveillance study. Eur J Contracept Reprod Health Care 4 (1999) 155-164
41. Endrikat J., Parke S., Trummer D., Schmidt W., Duijkers I., and 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 78 (2008) 218-225
42. Nahum G.G., Parke S., Wildt L., Palacios S., Roemer T., and Bitzer J. Efficacy and tolerability of a new oral contraceptive containing estradiol and dienogest. Obstet Gynecol 111 4 Suppl (2008) 15S
43. Parke S., Makalova D., Ahrendt H.J., and 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 13 Suppl (2008) 94
44. Parke S., Junge W., Mellinger U., Duijkers I., and Klipping C. Comparative effects of a four-phasic regimen of estradiol valerate/dienogest versus ethinylestradiol/levonorgestrel on haemostatic parameters. Hum Reprod Update 23 Suppl 1 (2008) i78-i79
45. Parke S., Nahum G., Mellinger U., and Junge W. Metabolic effects of a new four-phasic oral contraceptive containing estradiol valerate and dienogest. Obstet Gynecol 111 4 Suppl (2008) 12S-13S
46. Longcope C., and Williams K.I. The metabolism of estrogens in normal women after pulse injections of 3H-estradiol and 3H-estrone. J Clin Endocrinol Metab 38 (1974) 602-607