Third-generation oral contraceptives: Future implications of current use

Expert Review of Obstetrics and Gynecology

Volumn 3, Issue 2, 2008, Pages 189-201

  Ouzounian, Sophie ^a   Verstraete, Lieve ^b   Chabbert Buffet, Nathalie ^b,c  

^a HÔPITAL SAINT ANTOINE   (France)

^b ASSISTANCE PUBLIQUE HÔPITAUX DE PARIS   (France)

^c SORBONNE UNIVERSITÉ   (France)

Author keywords

Breast cancer; Cardiovascular risk; Contraception; Estradiol; Metabolic risk; Non oral hormonal contraceptive; Progestin; SPRM; Thrombosis

Indexed keywords

ACTIVATED PROTEIN C; ANDROGEN RECEPTOR; ANTIGESTAGEN; CHLORMADINONE; CHLORMADINONE ACETATE; CORTICOSTEROID DERIVATIVE; CYPROTERONE ACETATE; DESOGESTREL; DROSPIRENONE; ESTRADIOL; ESTRANE DERIVATIVE; ESTROGEN; ESTROGEN DERIVATIVE; ESTROGEN RECEPTOR; ETHINYLESTRADIOL; ETONOGESTREL; GESTAGEN; GESTODENE; LEVONORGESTREL; MEDROXYPROGESTERONE ACETATE; NOMEGESTROL; NORETHISTERONE; NORETHISTERONE ACETATE; NORGESTIMATE; ORAL CONTRACEPTIVE AGENT; PROGESTERONE DERIVATIVE; PROGESTERONE RECEPTOR; PROMEGESTONE; TESTOSTERONE DERIVATIVE; UNINDEXED DRUG;

ANTICOAGULATION; ARTERY DISEASE; ARTERY THROMBOSIS; BLEEDING DISORDER; BODY WEIGHT; BONE DENSITY; BREAKTHROUGH BLEEDING; BREAST CANCER; CEREBROVASCULAR ACCIDENT; CIGARETTE SMOKING; CLINICAL TRIAL; DEEP VEIN THROMBOSIS; DRUG EFFICACY; DRUG FATALITY; DRUG INFORMATION; DRUG MEGADOSE; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG TOLERABILITY; DRUG WITHDRAWAL; ENDOMETRIUM CANCER; FIBRINOLYSIS; FRACTURE; HEART INFARCTION; HIGH RISK PATIENT; HIRSUTISM; HORMONAL CONTRACEPTION; HUMAN; HYPERTENSION; ISCHEMIC HEART DISEASE; LOW DRUG DOSE; LUNG EMBOLISM; METABOLIC DISORDER; NAUSEA; OVARY CANCER; OVULATION INHIBITION; PATIENT COMPLIANCE; REVIEW; SIDE EFFECT; SPOTTING; STRUCTURE ANALYSIS; THROMBOEMBOLISM; THROMBOPHILIA; UTERINE CERVIX CANCER; UTERINE CERVIX CARCINOMA IN SITU; VASCULAR DISEASE; VASCULARIZATION; VENOUS THROMBOEMBOLISM; WITHDRAWAL BLEEDING;

EID: 49149128903     PISSN: 17474108     EISSN: None     Source Type: Journal    
DOI: 10.1586/17474108.3.2.189     Document Type: Review

References (97)

1. Practice Committee of the American Society for Reproductive Medicine. Hormonal contraception: recent advances and controversies. Fertil. Steril. 86(5 Suppl.), S229-S235 (2006).
2. Cerel-Suhl SL, Yeager BE Update on oral contraceptive pills. Am. Fam. Physician 60(7), 2073-2084 (1999).
3. Poindexter A. The emerging use of the 20-microg oral contraceptive. Fertil. Steril. 75(3), 457-465 (2001).
4. Rosenberg MJ, Meyers A, Roy V. Efficacy, cycle control, and side effects of low-and lower dose oral contraceptives: a randomized trial of 20 micrograms and 35 micrograms estrogen preparations. Contraception 60(6), 321-329 (999).
5. Hammond GL, Rabe T, Wagner JD. Preclinical profiles of progestins used in formulations of oral contraceptives and hormone replacement therapy. Am. J. Obstet. Gynecol. 185(2 Suppl.), S24-S31 (2001).
6. Maitra N, Kulier R, Bloemenkamp KW, Helmerhorst FM, Gulmezoglu AM. Progestogens in combined oral contraceptives for contraception. Cochrane Database Syst. Rev. 3, CD004861 (2004).
7. Moreau C, Trussell J, Gilbert F, Bajos N, Bouyer J. Oral contraceptive tolerance: does the type of pill matter? Obstet. Gynecol. 109(6), 1277-1285 (2007).
8. Jordan W. Pulmonary embolism. Lancet 2, 1146-1147 (1961).
9. World Health Organization Collaborative Study of Cardiovascular Disease and Steroid Hormone Contraception. Effect of different progestagens in low oestrogen oral contraceptives on venous thromboembolic disease. Lancet 346(8990), 1582-1588 (1995).
10. Hannaford PC, Owen-Smith V. Using epidemiological data to guide clinical practice: review of studies on cardiovascular disease and use of combined oral contraceptives. BMJ 316(7136), 984-987 (1998).
11. Jick H, Jick SS, Gurewich V, Myers MW, Vasilakis C. Risk of idiopathic cardiovascular death and nonfatal venous thromboembolism in women using oral contraceptives with differing progestagen components. Lancet 346(8990), 1589-1593 (1995).
12. Spitzer WO, Lewis MA, Heinemann LA, Thorogood M, MacRae KD. Third generation oral contraceptives and risk of venous thromboembolic disorders: an international case-control study. Transnational Research Group on Oral Contraceptives and the Health of Young Women. BMJ 312(7023), 83-88 (1996).
13. Vandenbroucke JP, Rosing J, Bloemenkamp KW et al. Oral contraceptives and the risk of venous thrombosis. N. Engl. J. Med. 344(20), 1527-1535 (2001).
14. Jick SS, Vasilakis C, Jick H. Pregnancies and terminations after 1995 warning about third-generation oral contraceptives. Lancet 351(9113), 1404-1405 (1998).
15. O'Brien PA. The third generation oral contraceptive controversy. The evidence shows they are less safe than second generation pills. BMJ 319(7213), 795-796 (1999).
16. Medicines Commission. Combined oral contraceptives containing desogestrel or gestodene and the risk of venous thromboembolism. Curr. Probl. Pharmacovigilance 25, 12 (1999).
17. Middeldorp S, Meijers JC, van den Ende AE et al. Effects on coagulation of levonorgestrel- and desogestrel-containing low dose oral contraceptives: a cross-over study. Thromb. Haemost. 84(1), 4-8 (2000).
18. Rosing J, Middeldorp S, Curvers J et al. Low-dose oral contraceptives and acquired resistance to activated protein C: a randomised cross-over study. Lancet 354(9195), 2036-2040 (1999).
19. Farley TM, Meirik O, Collins J. Cardiovascular disease and combined oral contraceptives: reviewing the evidence and balancing the risks. Hum. Reprod. Update 5(6), 721-735 (1999).
20. World Health Organization Collaborative Study of Cardiovascular Disease and us Steroid Hormone Contraception. Cardiovascular disease and use of oral injectable progestogen-only contraceptives and combined injectable contraceptives. Results of an international, multicenter, case control study. Contraception 57, 315-324 (1998).
21. Boyce J, Fawcett J, Noall E. Coronary thrombosis and Conovid. Lancet 1, 111 (1963).
22. Tanis BC, van den Bosch MA, Kemmeren JM et al. Oral contraceptives and the risk of myocardial infarction. N. Engl. J. Med. 345(25), 1787-1793 (2001).
23. Dunn N, Thorogood M, Faragher B et al. Oral contraceptives and myocardial infarction: results of the MICA case-control study. BMJ 318(7198), 157-1583 (1,999).
24. Khader YS, Rice J, John L, Abueita O. Oral contraceptives use and the risk of myocardial infarction: a meta-analysis. Contraception 68(1), 11-17 (2003).
25. Baillargeon JP, McClish DK, Essah PA, Nestler JE. Association between the current use of low-dose oral contraceptives and cardiovascular arterial disease: a meta-analysis. J. Clin. Endocrinol. Metab. 90(7), 3863-3870 (2005).
26. Kemmeren JM, Tanis BC, van den Bosch MA et al. Risk of Arterial Thrombosis in Relation to Oral Contraceptives (RATIO) study: oral contraceptives and the risk of ischemic stroke. Stroke 33(5), 1202-1208 (2002).
27. Collaborative Group on Hormonal Factors in Breast Cancer. Breast cancer and hormonal contraceptives: collaborative reanalysis of individual data on 53,297 women with breast cancer and 100 239 women without breast cancer from 54 epidemiological studies. Lancet 347(9017), 1713-1727 (1996).
28. Newcomb PA, Longnecker MP, Storer BE et al. Recent oral contraceptive use and risk of breast cancer (United States). Cancer Causes Control 7(5), 525-532 (1996).
29. Brinton LA, Gammon MD, Malone KE et al. Modification of oral contraceptive relationships on breast cancer risk by selected factors among younger women. Contraception 55(4), 197-203 (1997).
30. McCredie MR, Dite GS, Giles GG, Hopper JL. Breast cancer in Australian women under the age of 40. Cancer Causes Control 9(2), 189-198 (1998).
31. Ursin G, Ross RK, Sullivan-Halley J et al. Use of oral contraceptives and risk of breast cancer in young women. Breast Cancer Res. Treat. 50(2), 175-184 (1998).
32. Marchbanks PA, McDonald JA, Wilson HG et al. Oral contraceptives and the risk of breast cancer. N. Engl J. Med. 346(26), 2025-2032 (2002).
33. Kumle M, Weiderpass E, Braaten T et al. Use of oral contraceptives and breast cancer risk: The Norwegian-Swedish Women's Lifestyle and Health Cohort Study. Cancer Epidemiol. Biomarkers Prev. 11(11), 1375-1381 (2002).
34. Magnusson C, Baron JA, Correia N et al. Breast-cancer risk following long-term oestrogen- and oestrogen-progestin-replacement therapy. Int. J. Cancer 81 (3), 339-344 (1999).
35. Grabrick DM, Hartmann LC, Cerhan JR et al. Risk of breast cancer with oral contraceptive use in women with a family history of breast cancer. JAMA 284(14), 1791-1798 (2000).
36. Narod SA, Dube MP, Klijn J et al. Oral contraceptives and the risk of breast cancer in BRCA1 and BRCA2 mutation carriers. J. Natl Cancer Inst. 94(23), 1773-1779 (2002).
37. Schlesselman J, Collins J. The influence of steroids on gynecoogic cancers. In: Estrogens and Progestogens in Clinical Practice. Fraser IS (Ed.). Churchill-Livingstone, London, UK (1999).
38. The Cancer and Steroid Hormone Study of the Centers for Disease Control and the National Institute of Child Health and Human Development. The reduction in risk of ovarian cancer associated with oral contraceptive use. N. Engl. J. Med. 316, 650-655 (1987).
39. Schildkraut JM, Calingaert B, Marchbanks PA, Moorman PG, Rodriguez GC. Impact of progestin and estrogen potency, in oral contraceptives on ovarian cancer risk. J. Natl Cancer Inst. 94(1), 32-38 (2002).
40. Modan B, Hartge P, Hirsh-Yechezkel G et al. Panty, oral contraceptives, and the risk of ovarian cancer among carriers and noncarriers of a BRCA1 or BRCA2 mutation. N. Engl. J. Med. 345(4), 235-240 (2001).
41. Weiderpass E, Adami HO, Baron JA et al. Use of oral contraceptives and endometrial cancer risk (Sweden). Cancer Causes Control 10(4), 277-284 (1999).
42. Hormonal contraception: recent advances and controversies. Fertil. Steril. 86(5 Suppl. 1), S229-S235 (2006).
43. Polatti F, Perotti F, Filippa N, Gallina D, Nappi RE. Bone mass and long-term monophasic oral contraceptive treatment in young women. Contraception 51(4), 221-224 (1995).
44. Elgan C, Dykes AK, Samsioe G. Bone mineral density changes in young women: a two year study. Gynecol. Endocrinol. 19(4), 169-177 (2004).
45. Prior JC, Kirkland SA, Joseph L et al. Oral contraceptive use and bone mineral density in premenopausal women: cross-sectional, population-based data from the Canadian Multicentre Osteoporosis Study. CMAJ 165(8), 1023-1029 (2001),
46. Cooper C, Hannaford P, Croft P, Kay CR. Oral contraceptive pill use and fractures in women: a prospective study. Bone 14(1), 4145 (1993).
47. Hartard M, Kleinmond C, Kirchbichler A et al. Age at first oral contraceptive use as a major determinant of vertebral bone mass in female endurance athletes. Bone 35(4), 836-841 (2004).
48. Hartard M, Kleinmond C, Wiseman M et al. Detrimental effect of oral contraceptives on parameters of bone mass and geometry in a cohort of 248 young women. Bone 40(2), 444-450 (2007).
49. d'Arcangues C. WHO statement on hormonal contraception and bone health. Cantraception 73(5), 443-444 (2006).
50. World Health Organization Reproductive Health and Research. Medical Eligibility Criteria for Contraceptive Use. WHO, Geneva, Switzerland (2004).
51. O'Malley BW. Coregulators: from whence came these "master genes". Mol Endocrinol. 21(5), 1009-1013 (2007).
52. Georgiakaki M, Chabbert-Buffet N, Dasen B et al. Ligand-controlled interaction of histone acetyltransferase binding to ORC-1 (HBO1) with the N-terminal transactivating domain of progesterone receptor induces steroid receptor coactivator 1-dependent coactivation of transcription. Mol. Endocrinol. 20(9), 2122-2140 (2006).
53. Mulac-Jericevic B, Conneely OM. Reproductive tissue selective actions of progesterone receptors. Reproduction 128(2), 139-146 (2004).
54. Pascual-Le Tallec L, Lombes M. The mineralocorticoid receptor: a journey exploring its diversity and specificity of action. Mol. Endocrinol. 19(9), 2211-2221 (2005).
55. Duma D, Jewell CM, Cidlowski JA. Multiple glucocorticoid receptor isoforms and mechanisms of post-translational modification. J. Steroid Biochem. Mol. Biol. 102(1-5), 11-21 (2006).
56. Zerr-Fouineau M, Chataigneau M, Blot C, Schini-Kerth VB. Progestins overcome inhibition of platelet aggregation by endothelial cells by down-regulating endothelial NO synthase via glucocorticoid receptors. FASEB J. 21(1), 265-273 (2007).
57. Chataigneau T, Zerr M, Chataigneau M et al. Chronic treatment with progesterone but not medroxyprogesterone acetate restores the endothelial control of vascular tone in the mesenteric artery of ovariectomized rats. Menopause 11(3), 255-263 (2004).
58. Finlay IG, Scott MG. Patterns of contraceptive pill taking in an inner city practice. Br. Med. J. 293(6547), 601-602 (1986).
59. van Heusden AM, Fauser BC. Residual ovarian activity during oral steroid contraception. Hum. Reprod. Update 8(4), 345-358 (2002).
60. Barbosa IC, Filho CI, Faggion D Jr, Baracat EC. Prospective, open-label, noncomparative study to assess cycle control, safety and acceptability of a new oral contraceptive containing gestodene 60 microg and ethinylestradiol 15 microg (Minesse). Contraception 73(1), 30-33 (2006).
61. Sabatini R, Cagiano R. Comparison profiles of cycle control, side effects and sexual satisfaction of three hormonal contraceptives. Contraception 74(3), 220-223 (2006).
62. Edelman A, Gallo MF, Nichols MD et al. Continuous versus cyclic use of combined oral contraceptives for contraception: systematic Cochrane review of randomized controlled trials. Hum. Reprod. 21(3), 573-578 (2006).
63. Canonico M, Oger E, Plu-Bureau G et al. Hormone therapy and venous thromboembolism among postmenopausal women: impact of the route of estrogen administration and progestogens: the ESTHER study. Circulation 115(7), 840-845 (2007).
64. Sitruk-Ware R, Plu-Bureau G, Menard J et al. Effects of oral and transvaginal ethinyl estradiol on hemostatic factors and hepatic proteins in a randomized, crossover study. J. Clin. Endocrinol. Metab. 92(6), 2074-2079 (2007).
65. O'Connell K, Burkman RT. The transdermal contraceptive patch: an updated review of the literature. Clin. Obstet. Gynecol. 50(4), 918-926 (2007).
66. Gompel A, Carpentier S, Frances C, Piette JC. Risk of venous thromboembolism and oral contraceptives. Lancet 359(9314), 1348-1349 (2002).
67. Vasilakis-Scaramozza C, Jick H. Risk of venous thromboembolism with cyproterone or levonorgestrel contraceptives. Lancet 358(9291), 1427-1429 (2001).
68. Seaman HE, de Vries CS, Farmer RD. The risk of venous thromboembolism in women prescribed cyproterone acetate in combination with ethinyl estradiol: a nested cohort analysis and case-control study. Hum. Reprod. 18(3), 522-526 (2003).
69. Spitzer WO. Cyproterone acetate with ethinylestradiol as a risk factor for venous thromboembolism: an epidemiological evaluation. J. Obstet. Gynaecol. Can. 25(12), 1011-1018 (2003).
70. Mastorakos G, Kohopoulos C, Deligeoroglou E, Diamanti-Kandarakis E, Creatsas G. Effects of two forms of combined oral contraceptives on carbohydrate metabolism in adolescents with polycystic ovary syndrome. Fertil. Steril. 85(2), 420-427 (2006).
71. Bouchard P. Chlormadinone Acetate (CMA) in oral contraception. A new opportunity. Fertil. Contracept. 10(Suppl. 1), 7-11 (2005).
72. Conard J, Plu-Bureau G, Bahi N et al. Progestogen-onlycontraception in women at high risk of venous thromboembolism. Contraception 70(6), 437-441 (2004).
73. Krattenmacher R. Drospirenone: pharmacology and pharmacokioetics of a unique progestogen. Contraception 62(1), 29-38 (2000).
74. Fenton C, Wellington K, Moen MD, Robinson DM. Drospirenone/ ethinylestradiol 3mg/20microg (24/4 day regimen): a review of its use in Contraception premenstrual dysphoric disorder and moderate acne vulgaris. Drugs 67(12), 1749-1765 (2007).
75. Seeger JD, Loughlin J, Eng PM et al. Risk of thromboembolism in women taking ethinylestradiol/drospirenone and other oral contraceptives. Obstet. Gynecol. 110(3), 587-593 (2007).
76. Bazin B, Thevenot R, Bursaux C, Paris J. Effect of nomegestrol acetate, a new 19-nor-progesterone derivative, on pituitary-ovarian function in women. Br. J. Obstet. Gynaecol. 94(12), 1199-1204 (1987).
77. Jamin C, Batallan A, Madelenat P. Antigonadotropic effects of a 19-nor-progesterone derivative: the example of nomegestrol acetate. Gynecol. Obstet. Fertil. 31, 70-83 (2003).
78. Couzinet B, Young J, Kujas, M et al. The antigonadotropic activity of a 19-nor-progesterone derivative is exerted both at the hypothalamic and pituitary levels in women. J. Clin. Endocrinol. Metab. 84(11), 4191-4196 (1999).
79. Korver T, Klipping C, Heger-Mahn D et al. Maintenance of ovulation inhibition with the 75-microg desogestrel-only contraceptive pill (Cerazette) after scheduled 12-h delays in tablet intake. Contraception 71(1), 8-13 (2005).
80. Meirik O, Farley TM, Sivin I. Safety and efficacy of levonorgestrel implant, intrauterine device, and sterilization. Obstet. Gynecol., 97(4), 539 547 (2001).
81. Glasier A. Implantable contraceptives for women: effectiveness, discontinuation rates, return of fertility, and outcome of pregnancies. Contraception 65(1), 29-37 (2002).
82. Kovacs G, Progestogen-only pills and bleeding disturbances. Hum. Reprod. 11(Suppl. 2), 20-23 (1996).
83. Verbost PM, Hanssen RG, Korver GH, Mulders TM. ORG 33628 and ORG 31710 to control vaginal bleeding in progestin-only contraceptive regimens. Semin. Reprod. Med. 23(1), 101-111 (2005).
84. Croxatto HB, Salvatierra AM, Fuentealba B, Massai R. Contraceptive potential of a mifepristone-nomegestrol acetate sequential regimen in women. Hum. Reprod. 13(12), 3297-3302 (1998).
85. Cheng L, Zhu H, Wang A et al. Once a month administration of mifepristone improves bleeding patterns in women using subdermal contraceptive implants releasing levonorgestrel. Hum. Reprod. 15(9), 1969-1972 (2000).
86. Weisberg E, Hickey M, Palmer D et al. A pilot study to assess the effect of three short-term treatments on frequent and/or prolonged bleeding compared to placebo in women using Implanon. Hum. Reprod. 21(1), 295-302 (2006).
87. Spitz IM, Van Look PF, Coelingh Bennink HJ. The use of progesterone antagonists and progesterone receptor modulators in contraception. Steroids 65(10-11), 817-823 (2000).
88. Ledger WL, Sweeting VM, Hillier H, Baird DT. Inhibition of ovulation by low-dose mifepristone (RU 486). Hum. Reprod. 7(7), 945-950 (1992).
89. Brown A, Cheng L, Lin S, Baird DT. Daily low-dose mifepristone has contraceptive potential by suppressing ovulation and menstruation: a double-blind randomized control trial of 2 and 5 mg per day for 120 days. J. Clin. Endocrinol. Metab. 87(1), 63-70 (2002).
90. Pei K, Xiao B, Jing X et al. Weekly contraception with mifepristone. Contraception 75(1), 40-44 (2007).
91. Chabbert-Buffet N, Pintiaux-Kairis A, Bouchard P. Effects of the progesterone receptor modulator VA2914 in a continuous low dose on the hypothalamic-pituitary-ovarian axis and endometrium in normal women: a prospective, randomized, placebo-controlled trial. J. Clin. Endocrinol. Metab. 92(9), 3582-3589 (2007).
92. Steinauer J, Pritts EA, Jackson R, Jacoby AF. Systematic review of mifepristone for the treatment of uterine leiomyomata. Obstet. Gynecol. 103(6), 1331-1336 (2004).
93. Lakha F, Ho PC, Van der Spuy ZM et al. A novel estrogen-free oval contraceptive pill for women: multicentre, double-blind, randomized controlled trial of mifepristone and progestogen-only pill (levonorgestrel). Hum. Reprod. 22(9), 2428-2436 (2007).
94. Williams AR, Critchley HO, Osei J et al. The effects of the selective progesterone receptor modulator asoprisnil on the morphology of uterine tissues after 3 months treatment in patients with symptomatic uterine leiomyomata. Hum. Reprod 22(6), 1696-1704 (2007).
95. Horne FM, Blithe DL. Progesterone receptor modulators and the endometrium: changes and consequences. Hum. Reprod Update 13(6), 567-580 (2007).
96. Heikinheimo O, Vani S, Carpen O et al. Intrauterine release of progesterone antagonist ZK230211 is feasible and results in novel endometrial effects: a pilot study. Hum. Reprod 22(9), 2515-2522 (2007).
97. Sitruk-Ware R. Vaginal delivery of contraceptives. Expert Opin. Drug Delivery, 2(4), 729-736 (2005).