Evaluation of a new estradiol oral contraceptive: Estradiol valerate and dienogest

Expert Opinion on Pharmacotherapy

Volumn 11, Issue 7, 2010, Pages 1147-1157

  Jensen, Jeffrey T ^a  

^a OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

Contraception; Dienogest; Estradiol valerate; Heavy menstrual bleeding; Menorrhagia

Indexed keywords

DIANE; DIENOGEST; DIENOGEST PLUS ESTRADIOL VALERATE; ESTRADIOL VALERATE; ESTRIOL; ESTROGEN; ETHINYLESTRADIOL; ETHINYLESTRADIOL PLUS LEVONORGESTREL; FEMILAR; NORETHISTERONE ACETATE; PLACEBO; PROGESTERONE; QLAIRA; UNCLASSIFIED DRUG;

AMENORRHEA; BLEEDING; BREAST DISEASE; CLINICAL TRIAL; COMPETITIVE INHIBITION; DEEP VEIN THROMBOSIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG DOSE REDUCTION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG METABOLISM; DRUG STRUCTURE; HEART INFARCTION; HUMAN; INCIDENCE; LIVER HYPERPLASIA; LOW DRUG DOSE; MENSTRUAL CYCLE; MENSTRUATION; MENSTRUATION DISORDER; META ANALYSIS; METRORRHAGIA; OCULAR HISTOPLASMOSIS; ORAL CONTRACEPTION; OVARY CYST; REVIEW; SYSTEMATIC REVIEW; THERAPY EFFECT; TREATMENT INDICATION; UTERUS MYOMA;

ADOLESCENT; ADULT; CLINICAL TRIALS AS TOPIC; CONTRACEPTIVES, ORAL, COMBINED; DRUG COMBINATIONS; DRUG DESIGN; ESTRADIOL; FEMALE; HUMANS; MENORRHAGIA; NANDROLONE; PREGNANCY; PREGNANCY, UNPLANNED; YOUNG ADULT;

EID: 77951287402     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656561003724713     Document Type: Review

References (47)

1. Speroff L. A good man. Portland, OR: Arnica Pub, Inc, 2009
2. Speroff L, Darney P. A clinical guide for contraception, 4th edn. Philadelphia, PA: Lippincott, Williams & Wilkins, 2005
3. Zeun S, Lu M, Uddin A, et al. Pharmacokinetics of an oral contraceptive containing oestradiol valerate and dienogest. Eur J Contracept Reprod Health Care 2009;14:221-232
4. Mosher WD, Martinez GM, Chandra A, et al. Use of contraception and use of family planning services in the United States: 1982-2002. Adv Data 2004;350:1-36
5. Rosenberg MJ, Burnhill MS, Waugh MS, et al. Compliance and oral contraceptives: a review. Contraception 1995;52:137-141
6. Jensen JT, Speroff L. Health benefits of oral contraceptives. Obstet Gynecol Clin North Am 2000;27:705-721
7. Gallo MF, Nanda K, Grimes DA, Schulz KF. 20 mcg versus >20 mcg estrogen combined oral contraceptives for contraception. Cochrane Database Syst Rev 2005;2:CD003989
8. Astedt B, Jeppsson S, Liedholm P, et al. Clinical trial of a new oral contraceptive pill containing the natural oestrogen 17 beta-oestradiol. Br J Obstet Gynaecol 1979;86:732-736 (Pubitemid 9245029)
9. 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
10. Hirvonen E, Stenman UH, Malkonen M, et al. New natural oestradiol/cyproterone acetate oral contraceptive for pre-menopausal women. Maturitas 1988;10:201-213
11. 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 (Pubitemid 26412416)
12. Oettel M, Breitbarth H, Elger W, et al. The pharmacological profile of dienogest. Eur J Contracept Reprod Health Care 1999;4(1 Suppl 1):2-13
13. 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;78:218-225
14. Rivera R, Yacobson I, Grimes D. The mechanism of action of hormonal contraceptives and intrauterine contraceptive devices. Am J Obstet Gynecol 1999;181:1263-1269
15. Speroff L, Fritz M. Clinical gynecologic endocrinology and infertility, 7th edn. Lippincott, Williams & Wilkins, 2004
16. Sulak P, Scow R, Preece C, et al. Hormone withdrawal symptoms in oral contraceptive users. Obstet Gynecol 2000;95:261-266 (Pubitemid 30045651)
17. Pearlstein TB, Bachmann GA, Zacur HA, Yonkers KA. Treatment of premenstrual dysphoric disorder with a new drospirenone-containing oral contraceptive formulation. Contraception 2005;72:414-421 (Pubitemid 41676830)
18. Sulak PJ, Kuehl TJ, Ortiz M, Shull BL. Acceptance of altering the standard 21-day/7-day oral contraceptive regimen to delay menses and reduce hormone withdrawal symptoms. Am J Obstet Gynecol 2002;186:1142-1149 (Pubitemid 34665050)
19. 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 2003;67:9-13 (Pubitemid 36084281)
20. Dusterberg B, Nishino Y. Pharmacokinetic and pharmacological features of oestradiol valerate. Maturitas 1982;4:315-324 (Pubitemid 13189102)
21. Ben-Rafaelf Z, Mastroianni L, Meloni F, et al. Total estradiol, free estradiol, sex hormone-binding globulin, and the fraction of estradiol bound to sex hormone-binding globulin in human follicular fluid. J Clin Endocrinol Metab 1986;63:1106-1111 (Pubitemid 17173045)
22. Lievertz RW. Pharmacology and pharmacokinetics of estrogens. Am J Obstet Gynecol 1987;156:1289-1293
23. Lindberg UB, Crona N, Stigendal L, et al. A comparison between effects of estradiol valerate and low dose ethinyl estradiol on haemostasis parameters. Thromb Haemost 1989;61:65-69 (Pubitemid 19092670)
24. Lee AJ, Cai MX, Thomas PE, et al. Characterization of the oxidative metabolites of 17{beta}-estradiol and estrone formed by 15 selectively expressed human cytochrome P450 isoforms. Endocrinology 2003;144:3382-3398
25. Goldzieher JW. Pharmacology of contraceptive steroids: a brief review. Am J Obstet Gynecol 1989;160:1260-1264
26. Gommaa AA, Osman FH. Influence of acetaminophen-induced hepatic necrosis on the pharmacokinetics of levonorgestrel. Contraception 1983;28:149-157
27. Ahrendt HJ, Makalova D, Parke S, et al. 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;80:436-444
28. Palacios S, Wildt L, Parke S, et al. Efficacy and safety of a novel oral contraceptive based on oestradiol (oestradiol valerate/dienogest): a Phase III trial. Eur J Obstet Gynecol Reprod Biol 2010;149(1):57-62
29. Nelson A, Sampson-Landers C, Parke S, Jensen J. Efficacy of estradiol valerate/ dienogest OC: results of 3 large studies in North America and Europe [abstract and poster]. Presented at the 57th Annual Clinical Meeting of the American College of Obstetricians & Gynecologists, 2-6 May 2009, Chicago, IL, USA
30. Qlaira- Summary of Product Characteristics. 22 Dec 2009. Available from: http://emc. medicines.org.uk/medicine/21700/SPC/ Qlaira/ [Last accesssed 22 Dec 2009]
31. Belsey EM. Vaginal bleeding patterns among women using one natural and eight hormonal methods of contraception. Contraception 1988;38:181-206
32. Archer DF, Jensen JT, Johnson JV, et al. Evaluation of a continuous regimen of levonorgestrel/ethinyl estradiol: phase III study results. Contraception 2006;74:439-445
33. Bachmann G, Sulak PJ, Sampson-Landers C, et al. Efficacy and safety of a low-dose 24-day combined oral contraceptive containing 20 micrograms ethinylestradiol and 3 mg drospirenone. Contraception 2004;70:191-198 (Pubitemid 39119980)
34. Nakajima ST, Archer DF, Ellman H. Efficacy and safety of a new 24-day oral contraceptive regimen of norethindrone acetate 1 mg/ethinyl estradiol 20 micro g (Loestrin 24 Fe). Contraception 2007;75:16-22 (Pubitemid 44854856)
35. 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):12-13
36. Hallberg L, Hogdahl AM, Nilsson L, Rybo G. Menstrual blood loss and iron deficiency. Acta Med Scand 1966;180:639-650
37. National Collaborating Centre for Women's and Children's Health. Heavy menstrual bleeding. Commissioned by the National Institute for Health and Clinical Excellence. Available from: http://wwwniceorguk/nicemedia/pdf/ CG44FullGuidelinepdf [Last accessed 28 October 2009]
38. Fraser IS, McCarron G. Randomized trial of 2 hormonal and 2 prostaglandin-inhibiting agents in women with a complaint of menorrhagia. Aust NZ J Obstet Gynaecol 1991;31:66-70
39. Fraser IS, Zeun S, Machlitt A, Mellinger U. A novel oral contraceptive comprising estradiol valerate/dienogest for the treatment of heavy and/or prolonged menstrual bleeding without organic cause: a double-blind, randomised, placebo-controlled trial. Int J Gynecol Obstet 2009;107(Suppl 2):S183
40. Jensen J, Machlitt A, Mellinger U, et al. A multicenter, double-blind, randomized, placebo-controlled study of oral estradiol valerate/dienogest for the treatment of heavy and/or prolonged menstrual bleeding. Fertil Steril 2009;92:S32
41. Goebelsmann U, Mashchak CA, Mishell DR Jr. Comparison of hepatic impact of oral and vaginal administration of ethinyl estradiol. Am J Obstet Gynecol 1985;151:868-877 (Pubitemid 15237723)
42. Jick SS, Kaye JA, Russmann S, Jick H. Risk of nonfatal venous thromboembolism in women using a contraceptive transdermal patch and oral contraceptives containing norgestimate and 35 microg of ethinyl estradiol. Contraception 2006;73:223-228 (Pubitemid 43202170)
43. Eilertsen AL, Hoibraaten E, Os I, et al. The effects of oral and transdermal hormone replacement therapy on C-reactive protein levels and other inflammatory markers in women with high risk of thrombosis. Maturitas 2005;52:111-118 (Pubitemid 41368033)
44. van Hylckama Vlieg A, Helmerhorst FM, Vandenbroucke JP, et al. The venous thrombotic risk of oral contraceptives, effects of oestrogen dose and progestogen type: results of the MEGA case-control study. BMJ 2009;339:b2921
45. Lidegaard O, Lokkegaard E, Svendsen AL, Agger C. Hormonal contraception and risk of venous thromboembolism: national follow-up study. BMJ 2009;339:b2890
46. 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 (Pubitemid 46551071)
47. Seeger JD, Loughlin J, Eng PM, et al. Risk of thromboembolism in women taking ethinylestradiol/drospirenone and other oral contraceptives. Obstet Gynecol 2007;110:587-593 (Pubitemid 47359582)