Estradiol Valerate/Dienogest: A Novel Combined Oral Contraceptive

Clinical Therapeutics

Volumn 34, Issue 1, 2012, Pages 37-55

  Borgelt, Laura M ^a   Martell, Chad W ^b  

^a UNIVERSITY OF COLORADO   (United States)

^b REGIS UNIVERSITY   (United States)

Author keywords

Combined oral contraceptives; Contraception; Dienogest; Estradiol valerate; Oral contraceptives

Indexed keywords

CYTOCHROME P450 3A4; DIENOGEST PLUS ESTRADIOL VALERATE; ESTROGEN; GESTAGEN; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HUMAN IMMUNODEFICIENCY VIRUS PROTEINASE INHIBITOR; PROGESTERONE; THYROID HORMONE;

ABDOMINAL PAIN; ACNE; AREA UNDER THE CURVE; BLOOD PRESSURE; BODY MASS; CLINICAL EFFECTIVENESS; DEPRESSION; DIARRHEA; DRUG ABSORPTION; DRUG COST; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG METABOLISM; DRUG STRUCTURE; DRUG TOLERABILITY; DYSMENORRHEA; ECONOMIC ASPECT; EDEMA; ESTROGEN BLOOD LEVEL; EYE IRRITATION; GESTAGEN BLOOD LEVEL; HEADACHE; HUMAN; KIDNEY DISEASE; LACTATION; LIVER DISEASE; MASTALGIA; MENTAL INSTABILITY; MULTIPLE CYCLE TREATMENT; NAUSEA; OBESITY; ORAL CONTRACEPTION; OVARY CYST; OVULATION INHIBITION; PATIENT SATISFACTION; PHARMACODYNAMICS; PREGNANCY; PROGESTERONE BLOOD LEVEL; REVIEW; SIDE EFFECT; WEIGHT; WITHDRAWAL BLEEDING;

ADMINISTRATION, ORAL; ANIMALS; CONTRACEPTIVES, ORAL, COMBINED; CONTRACEPTIVES, ORAL, HORMONAL; DRUG ADMINISTRATION SCHEDULE; DRUG COSTS; ESTRADIOL; FEMALE; HUMANS; NANDROLONE; PREGNANCY; TREATMENT OUTCOME;

EID: 84856172988     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2011.11.006     Document Type: Review

References (56)

1. Dhont M. History of oral contraception. Eur J Contracept Reprod Health Care 2010, 15(Suppl 2):S12-S18.
2. Djerassi C. Chemical birth of the pill. Am J Obstet Gynecol 2006, 194:290-298.
3. Nelson A. Combined oral contraceptives. Contraceptive Technology 2007, 193-270. Ardent Media Inc, New York, NY. 19th ed. R.A. Hatcher, J. Trussel, A.L. Nelson (Eds.).
4. Barbieri R. In the news, now on the shelf: a novel estradiol-based OC. OBG Management 2010, 22:6. 10-11, Accessed January 4, 2011. http://www.obgmanagement.com.
5. Alsina J.C. After 50 years of ethinylestradiol, another oestrogen in combined oral contraceptives. Eur J Contracept Reprod Health Care 2010, 15:1-3.
6. 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.
7. Hoffmann H., Moore C., Kovacs L., et al. Alternatives of the replacement of ethinylestradiol by natural 17beta-estradiol in dienogest-containing oral contraceptives. Drugs Today 1999, 35:105-113.
8. Sitruk-Ware R., Nath A. The use of newer progestins for contraception. Contraception 2010, 82:410-417.
9. Natazia (estradiol valerate/dienogest) May 2010, [package insert], Bayer HealthCare Pharmaceuticals, Wayne, NJ.
10. Mishell D.R. Rationale for decreasing the number of days of the hormone-free interval with use of low-dose oral contraceptive formulations. Contraception 2005, 71:304-305.
11. Read C.M. New regimens with combined oral contraceptive pills-moving away from traditional 21/7 cycles. Eur J Contracept Reprod Health Care 2010, 15(Suppl 2):S32-S41.
12. In brief: facts on contraceptive use in the United States, 2010 Guttmacher Institute, Accessed January 4, 2011. http://www.guttmacher.org/pubs/fb_contr_use.html.
13. Speroff L., Fritz M.A. Oral contraception. Clinical Gynecologic Endocrinology and Infertility 2005, 861-942. Lippincott Williams & Wilkins, Philadelphia, Pa. 7th ed.
14. Jensen J.T. Evaluation of a new estradiol oral contraceptive: estradiol valerate and dienogest. Expert Opin Pharmacother 2010, 11:1147-1157.
15. Zeun S., Lu M., Uddin A., Zeiler B., Morrison D., Blode H. Pharmacokinetics of an oral contraceptive containing oestradiol valerate and dienogest. Eur J Contracept Reprod Health Care 2009, 14:221-232.
16. Perez-Campos E.F. Ethinylestradiol/dienogest in oral contraception. Drugs 2010, 70:681-689.
17. Hoy S.M., Scott L.J. Estradiol valerate/dienogest: in oral contraception. Drugs 2009, 69:1635-1646.
18. Dusterberg B., Nishino Y. Pharmacokinetic and pharmacological features of oestradiol valerate. Maturitas 1982, 4:315-324.
19. 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.
20. Oettel M., Breitbarth H., Elger W. The pharmacological profile of dienogest. Eur J Contracept Reprod Health Care 1999, 4(Suppl 1):2-13.
21. Dickinson B.D., Altman R.D., Nielsen N.H., Sterling M.L. Drug interactions between oral contraceptives and antibiotics. Obstet Gynecol 2001, 98:853-860.
22. Sparrow M.J. Pill method failure. N Z Med J 1987, 100:102-105.
23. Kakouris H., Kovacs G.T. Pill failure and non-use of secondary precautions. Br J Fam Plan 1992, 18:41-44.
24. Kovacs G.T., Riddoch G., Duncombe P., et al. Inadvertent pregnancies in oral contraceptive users. Med J Aust 1989, 150:549-551.
25. Neely J., Abate M., Swinker M., D'angio R. The effect of doxycycline on serum levels of ethinyl estradiol, norethindrone, and endogenous progesterone. Obstet Gynecol 1991, 77:416-420.
26. Murphy A.A., Zacur H.A., Charache P., Burkman R.T. The effect of tetracycline on levels of oral contraceptives. Am J Obstet Gynecol 1991, 164(1 Pt 1):28-33.
27. Friedman C.I., Huneke A.L., Kim M.H. The effect of ampicillin on oral contraceptive effectiveness. Obstet Gynecol 1980, 55:33-37.
28. Hoogland H.J., Skouby S.O. Ultrasound evaluation of ovarian activity under oral contraceptives. Contraception 1993, 47:583-590.
29. Spona J., Feichtinger W., Kindermann C., Wunsch C., Brill K. Inhibition of ovulation by an oral contraceptive containing 100 micrograms levonorgestrel in combination with 20 micrograms ethinylestradiol. Contraception 1996, 54:299-304.
30. Palacios S., Wildt L., Parke S., Machlitt A., Romer T., Bitzer J. 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, 149:57-62.
31. The safety and contraceptive efficacy of a 24-day low-dose oral contraceptive regimen containing gestodene 60 microg and ethinylestradiol 15 microg. Eur J Contracept Reprod Health Care 1999, 4(Suppl 2):9-15.
32. Ahrendt H.J., Nisand I., Bastianelli C., et al. Efficacy, acceptability and tolerability of the combined contraceptive ring, NuvaRing, compared with an oral contraceptive containing 30 microg of ethinyl estradiol and 3 mg of drospirenone. Contraception 2006, 74:451-457.
33. Bachmann G., Sulak P.J., Sampson-Landers C., Benda N., Marr J. 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.
34. A randomized, double-blind study of two combined oral contraceptives containing the same progestogen, but different estrogens. Contraception 1980, 21:445-459. World Health Organization Task Force on Oral Contraception.
35. 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.
36. Hirvonen E., Allonen H., Anttila M., et al. Oral contraceptive containing natural estradiol for premenopausal women. Maturitas 1995, 21:27-32.
37. Serup J., Bostofte E., Larsen S., Westergaard J., Lebech P.E. Natural oestrogens for oral contraception. Lancet 1979, 2:471-472.
38. 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 ethinyl estradiol/levonorgestrel. Contraception 2009, 80:436-444.
39. Nelson A, Sampson-Landers C, Parke S, Jensen JT. Efficacy of estradiol valerate/dienogest OC: results of 3 large studies in North America and Europe. Abstract and poster presented at: 57th Annual Clinical Meeting of the American Congress of Obstetricians and Gynecologists; May 2-6, 2009; Chicago, Ill.
40. Anttila L., Backhmann G., Hernadi L., Kunz M., Marr J., Klipping C. Contraceptive efficacy of a combined oral contraceptive containing ethinylestradiol 20 mcg/drosperinone 3 mg administered in a 24/4 regimen: a pooled analysis of four open-label studies. Eur J Obstet Gynecol Reprod Biol 2011, 155:180-182.
41. Dando T.M., Curran M.P. Low-dose ethinylestradiol/levonorgestrel. Drugs 2005, 65:2299-2306.
42. Bitzer J., Parke S., Roemer T., Serrani M. Endometrial safety of an oral contraceptive containing estradiol valerate and dienogest. Int J Womens Health 2011, 3:127-132.
43. Wenzl R., Bennink H.C., 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.
44. Schubert W., Cullberg G. Ovulation inhibition with 17 beta-estradiol cyclo-octyl acetate and desogestrel. Acta Obstet Gynecol Scand 1987, 66:543-547.
45. Fraser I., 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: World Congress of the International Federation of Gynecology and Obstetrics (FIGO) 4-9 October 2009. Int J Gynecol Obstet 2009, 107(Suppl 2):S183.
46. Jensen J., Parke S., Mellinger U., Machlitt A., Fraser I. Effective treatment of heavy menstrual bleeding with estradiol valerate and dienogest: a randomized controlled trial. Obstet Gynecol 2011, 117:777-787.
47. Wasiak R, Filonenko A, Jensen J, Law A, Jeddi M, Stull D. Impact of estradiol valerate/dienogest (E2V/DNG) on work productivity (WP) and activities of daily living (ADL) impairment in North American women with heavy and/or prolonged menstrual bleeding (HPMP). Paper presented at: American Society for Reproductive Medicine (ASRM) 66th Annual Meeting; October 23-27, 2010; Denver, Colo.
48. 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.
49. Wiegratz I., Kutschera E., Lee J.H., et al. Effect of four different oral contraceptives on various sex hormones and serum-binding globulins. Contraception 2003, 67:25-32.
50. Wiegratz I., Lee J.H., Kutschera E., et al. Effect of dienogest-containing oral contraceptives on lipid metabolism. Contraception 2002, 65:223-229.
51. Wiegratz I., Kutschera E., Lee J.H., et al. Effect of four oral contraceptives on thyroid hormones, adrenal and blood pressure parameters. Contraception 2003, 67:361-366.
52. Klipping C., Duijkers I., Parke S., et al. Hemostatic effects of a novel estradiol-based oral contraceptive: an open-label, randomized, crossover study of estradiol valerate/dienogest versus ethinylestradiol/levonorgestrel. Drugs R D 2011, 11:159-170.
53. Drug prices and information, 2011 Accessed July 11, 2011. http://www.drugstore.com.
54. van Hylckama Vlieg A., Helmerhorst F.M., Vandenbroucke J.P., Doggen C.J., Rosendaal F.R. 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.
55. Nelson A., Stewart F. Menopause and perimenopausal health. Contraceptive Technology 2007, 699-745. Ardent Media Inc, New York, NY. R.A. Hatcher, J. Trussel, A.L. Nelson (Eds.).
56. Rosenberg M., Waugh M.S. Causes and consequences of oral contraceptive noncompliance. Am J Obstet Gynecol 1999, 180(2 Pt 2):276-279.