Progestational effects of dydrogesterone in vitro, in vivo and on the human endometrium

Maturitas

Volumn 65, Issue SUPPL. 1, 2009, Pages

  Schindler, Adolf E ^a  

^a Institute for Medical Research and Education Essen   (Germany)

Author keywords

Dydrogesterone; Endometrium; Hormone replacement therapy; Progestational effect; Progesterone

Indexed keywords

CHLORMADINONE; CHLORMADINONE ACETATE; CYPROTERONE ACETATE; DNA; DROSPIRENONE; DYDROGESTERONE; ESTRADIOL; ESTROGEN; GESTAGEN; GESTODENE; LEVONORGESTREL; LYNESTRENOL; MEDROGESTONE; MEDROXYPROGESTERONE ACETATE; NANDROLONE; NOMEGESTROL ACETATE; NORETHISTERONE; PROGESTERONE; PROMEGESTONE; RALOXIFENE; TAMOXIFEN; TRIMEGESTONE;

AMENORRHEA; ARTICLE; BINDING AFFINITY; BREAST CANCER; DRUG ADMINISTRATION ROUTE; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG POTENCY; ENDOMETRIUM; ENDOMETRIUM HYPERPLASIA; ENDOTHELIUM CELL; HORMONE SUBSTITUTION; HUMAN; HYPOTHALAMUS HYPOPHYSIS SYSTEM; IN VITRO STUDY; IN VIVO STUDY; MENSTRUAL IRREGULARITY; NONHUMAN; OLIGOMENORRHEA; OVULATION; POSTMENOPAUSE; RABBIT; UTERUS; UTERUS BLEEDING;

ANIMALS; DYDROGESTERONE; ENDOMETRIAL HYPERPLASIA; ENDOMETRIUM; ESTRADIOL; ESTROGEN REPLACEMENT THERAPY; FEMALE; HUMANS; MENSTRUATION DISTURBANCES; PROGESTERONE; PROGESTINS;

ORYCTOLAGUS CUNICULUS;

EID: 72749119215     PISSN: 03785122     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.maturitas.2009.10.011     Document Type: Article

References (80)

1. Schindler A.E., Campagnoli C., Druckmann R., et al. Classification and pharmacology of progestins. Maturitas 61 (2008) 171-180
2. Jalkanen J. Interaction of 17 beta-estradiol and progesterone production in human granulosa-luteal cells. Eur J Obstet Gynecol Reprod Biol 37 (1990) 143-153
3. Lobb D.K., Soliman S.R., Daya S., and Younglai E.V. Steroidogenesis in luteinized granulosa cell cultures varies with follicular priming regimen. Hum Reprod 13 (1998) 2064-2067
4. Branchaud C.L., Goodyer C.G., and Lipowski L.S. Progesterone and estrogen production by placental monolayer cultures: effect of dehydroepiandrosterone and luteinizing hormone-releasing hormone. J Clin Endocrinol Metab 56 (1983) 761-766
5. Selvaraj N., Dantes A., and Amsterdam A. Establishment and characterization of steroidogenic granulosa cells expressing beta(2)-adrenergic receptor: regulation of adrenodoxin and steroidogenic acute regulatory protein by adrenergic agents. Mol Cell Endocrinol 168 (2000) 53-63
6. Devoto L., Kohen P., Vega M., et al. Control of human luteal steroidogenesis. Mol Cell Endocrinol 186 (2002) 137-141
7. Hillensjö T., Sjögren A., Strander B., et al. Effect of gonadotrophins on progesterone secretion by cultured granulosa cells obtained from human preovulatory follicles. Acta Endocrinol (Copenh) 110 (1985) 401-407
8. Wardell S.E., and Edwards D.P. Mechanisms controlling agonist and antagonist potential of selective progesterone receptor modulators (SPRMs). Semin Reprod Med 23 (2005) 9-21
9. Schindler A.E. Endocrinology of pregnancy: consequences for the diagnosis and treatment of pregnancy disorders. J Steroid Biochem Mol Biol 97 (2005) 386-388
10. Schindler A.E. Immunology and progestins in pregnancy. Gynecol Endocrinol 13 Suppl. 4 (1999) 47-50
11. Schindler A.E. Gestagene, endometrium und endometriose. Gestagene und endometrium. Zentralbl Gynakol 119 (1997) 59-63
12. Writing Group for the PEPI Trial. Effects of hormone replacement therapy on endometrial histology in postmenopausal women. The postmenopausal estrogen/progestin intervention trial. JAMA 275 (1996) 370-375
13. Tamaya T., Furuta N., Ohono Y., Ide N., Tsurusaki T., and Okada H. Chromatin transcription by progestogen-receptor in rabbit uterus. Endocrinol Jpn 26 (1979) 117-122
14. Tamaya T., Tsurusaki T., Ide N., et al. Nuclear translocation of progesterone receptor-progestogen complex in vitro. Acta Obstet Gynaecol Jpn 35 (1983) 77-82
15. Reerink E.H., Schöler H.F.L., Westerhof P., et al. A new class of hormonally active steroids. Nature 186 (1960) 168-169
16. Colombo D., Ferraboschi P., Prestileo P., and Toma L. A comparative molecular modeling study of dydrogesterone with other progestational agents through theoretical calculations and nuclear magnetic resonance spectroscopy. J Steroid Biochem Mol Biol 98 (2006) 56-62
17. Van Amsterdam P.H., Overmars H., Scherpenisse P.M., and de Bree H. Dydrogesterone: metabolism in man. Eur J Drug Metab Pharmacokinet 5 (1980) 173-184
18. Okada H., Iwasaki S., Take H., Matsuyoshi K., and Houki N. Liver metabolism of 6-dehydroretroprogesterone in rats. 1. Reduction of C20-ketone. Nippon Naibunpi Gakkai Zasshi 41 (1965) 856-859
19. Houki N. Study on the metabolism of progestins, pregnane compounds, in vivo. Nippon Naibunpi Gakkai Zasshi 42 (1966) 900-917
20. Queisser-Luft A. Dydrogesterone use during pregnancy: overview of birth defects reported since 1977. Early Hum Dev 85 (2009) 375-377
21. Balasch J., Vanrell J., Márquez M., and González-Merlo J. Dehydrogesterone treatment of endometrial luteal phase deficiency after ovulation induced by clomiphene citrate and human chorionic gonadotropin. Fertil Steril 40 (1983) 469-471
22. Cohen M.R., and Perez-Pelaez M. The effect of norethindrone acetate-ethinyl estradiol, clomiphene citrate, and dydrogesterone on spinnbarkeit. Fertil Steril 16 (1965) 141-150
23. Okada H. Metabolism, structure and biological activity of sex steroids. Folia Endocrinol 69 (1993) 67-79
24. Picolet H., Girard P., Nemoz C., and Boissel J.P. Effects of dydrogesterone on hydroelectrolytic metabolism: a randomized double-blind study. Gynecol Endocrinol 4 (1990) 219-224
25. Satake M., Sakai K., Takano J., et al. Urinary excretion of steroid hormones in menstruation disorders and its significance. Horumon To Rinsho 19 (1971) 548-552
26. Hulley S., Grady D., Bush T., et al. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women. Heart and Estrogen/progestin Replacement Study (HERS) Research Group. JAMA 280 (1998) 605-613
27. Grady D., Herrington D., Bittner V., et al. Cardiovascular disease outcomes during 6.8 years of hormone therapy: heart and estrogen/progestin replacement study follow-up (HERS II). JAMA 288 (2002) 49-57
28. Rossouw J.E., Anderson G.L., Prentice R.L., et al. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 288 (2002) 321-333
29. Beral V. Million Women Study Collaborators. Breast cancer and hormone-replacement therapy in the Million Women Study. Lancet 362 (2003) 419-427
30. Anderson G.L., Limacher M., Assaf A.R., et al. Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women's Health Initiative randomized controlled trial. JAMA 291 (2004) 1701-1712
31. Schindler A.E. Differential effects of progestins. Maturitas 46S1 (2003) S3-S5
32. European Progestin Club: Editorial. Progestins: present and future. J Steroid Biochem Mol Biol 59 (1996) 357-363
33. Junkmann K. Experimentelle Gesichtspunkte bei der Prüfung Synthetischer Gestagene. Dtsch Med Wschr 88 (1963) 629-638
34. Kontula K., Jänne O., Vihko R., de Jager E., de Visser J., and Zeelen F. Progesterone binding proteins: in vitro binding and biological activity of different steroidal ligands. Acta Endocrinol 78 (1975) 574-592
35. Wilks J.W., Spilman C.H., and Campbell J.A. Steroid binding specificity of the hamster uterine progesterone receptor. Steroids 35 (1980) 697-706
36. Meglioli G., and Desaulles P.A. Modifications induced by progestogen treatment in the action of rat uterine secretion on corona cells in vitro. Hormone Res 4 (1973) 288-292
37. Meglioli G., Kalvoda J., and Desaulles P.A. Effects of progestogenic substances on the uterine secretion of spayed rats primed with oestradiol. Hormone Res 4 (1973) 97-106
38. Saure A., Karjalainen O., and Teräväinen T. The effect of synthetic gestagens on progesterone formation in vitro in human corpus luteum of early pregnancy. Eur J Obstet Gynecol Reprod Biol 6 (1976) 223-234
39. Madjerek Z., and Smit-Vis J.H. Assessment of a bioassay of progestational activity. J Endocrinol 66 (1975) 135-136
40. Madjerek Z.S., and Smit-Vis J.H. Further studies on a new bioassay of progestational activity (Traumatic deciduoma formation in immature rats). Acta Morphol Neer-Scand 15 (1977) 65-74
41. Chetrite G.S., Thole H.H., Philippe J.C., and Pasqualini J.R. Dydrogesterone (Duphaston) and its 20-dihydro-derivative as selective estrogen enzyme modulators in human breast cancer cell lines. Effect on sulfatase and on 17beta-hydroxysteroid dehydrogenase (17beta-HSD) activity. Anticancer Res 24 (2004) 1433-1438
42. Pasqualini J.R., and Chetrite G.S. Recent insights on the control of enzymes involved in estrogen formation and transformation in human breast cancer. J Steroid Biochem Mol Biol 93 (2005) 221-236
43. Franke H.R., Kole S., Ciftci Z., Haanen C., and Vermes I. In vitro effects of estradiol, dydrogesterone, tamoxifen and cyclophosphamide on proliferation vs. death in human breast cancer cells. Cancer Lett 190 (2003) 113-118
44. Franke H.R., and Vermes I. Differential effects of progestogens on breast cancer cell lines. Maturitas 46S1 (2003) 55-58
45. Werner H.M., Franke H.R., and Vermes I. Apoptosis and proliferation in breast cancer cells, cultured in vitro: effects of SERMs. Climacteric 8 (2005) 294-299
46. Sugawa H., Moriyama I., and Kakita M. The action of delta-6-retroprogesterone (Duphaston) on DNA synthesis of the uterine endometrium. Clin Endocrinol 17 (1969) 876-877
47. Mattioli F., Garbero C., Gosmar M., et al. DNA fragmentation, DNA repair and apoptosis induced in primari rat hepatocytes by dienogest, dydrogesterone and 1,4,6-Androstatriene-17β-ol-3-one acetate. Mutat Res 564 (2004) 21-29
48. Simoncini T., Caruso A., Giretti M.S., et al. Effects of dydrogesterone and of its stable metabolite, 20-alpha-dihydrodydrogesterone, on nitric oxide synthesis in human endothelial cells. Fertil Steril 86 Suppl. 4 (2006) 1235-1242
49. Kumasaka T., Itoh E., Watanabe H., Hoshino K., Yoshinaka A., and Masawa N. Effects of various forms of progestin on the endometrium of the estrogen-primed, ovariectomized rat. Endocr J 41 (1994) 161-169
50. Neumann F. Chemische Konstitution und pharmakologische Wirkung. Handbuch der Experimentelle Pharmakologie (Handbook of Experimental Pharmacology), Kapitel VI, Teil 1, Die Gestagene (1968), Springer Verlag, Berlin, Heidelberg, New York
51. Joachim R., Zenclussen A.C., Polgar B., et al. The progesterone derivative dydrogesterone abrogates murine stress-triggered abortion by inducing a Th2 biased local immune response. Steroids 68 (2003) 931-940
52. Blois S.M., Joachim R., Kandil J., et al. Depletion of CD8+ cells abolishes the pregnancy protective effect of progesterone substitution with dydrogesterone in mice by altering the Th1/Th2 cytokine profile. J Immunol 172 (2004) 5893-5899
53. Raghupathy R., Al Mutawa E., Makhseed M., Azizieh F., and Szekeres-Bartho J. Modulation of cytokine production by dydrogesterone in lymphocytes from women with recurrent miscarriage. BJOG 112 (2005) 1096-1101
54. Swyer G.I.M. Small-scale clinical trials of progestogens for control of conception. Int J Fertil 9 (1964) 11-16
55. King R., and Whitehead M. Assessment of the potency of orally administered progestins in women. Fertil Steril 46 (1986) 1062-1066
56. Ryder T., Mobberley M., and Whitehead M. The endometrial nucleolar channel system as an indicator of progestin potency in HRT. Maturitas 22 (1995) 31-36
57. Lane G., Siddle N.C., Ryder T.A., Pryse-Davies J., King R.J., and Whitehead M.I. Effects of dydrogesterone on the oestrogenized postmenopausal endometrium. Br J Obstet Gynaecol 93 (1986) 55-62
58. Siddle N., Fraser D., Whitehead M., et al. Endometrial, physical and psychological effects of postmenopausal oestrogen therapy with added dydrogesterone. Br J Obstet Gynaecol 97 (1990) 1101-1107
59. Rees M., Leather A., Pryse-Davies J., Collins S.A., Barlow D.H., and Studd J.W. A first study to compare two dosages of dydrogesterone in opposing the 50 mg oestradiol implant. Maturitas 14 (1991) 9-15
60. Gelfand M., Fugère P., Bissonette F., et al. Conjugated estrogens combined with sequential dydrogesterone or medroxyprogesterone acetate in postmenopausal women: effects on lipoproteins, glucose tolerance, endometrial histology and bleeding. Menopause 4 (1997) 10-18
61. Burch D.J., Spowart K.J.M., Jesinger D.K., Randall S., and Smith S.K. A dose-ranging study of the use of cyclical dydrogesterone with continuous 17beta-oestradiol. Br J Obstet Gynaecol 102 (1995) 243-248
62. van der Mooren M.J., Hanselaar A.G.J.M., Borm G.F., and Rolland R. Changes in the withdrawal bleeding pattern and endometrial histology during 17beta-estradiol-dydrogesterone therapy in postmenopausal women: a 2-year prospective study. Maturitas 20 (1995) 175-180
63. Bergeron C., and Fox H. Low incidence of endometrial hyperplasia with acceptable bleeding patterns in women taking sequential hormone replacement therapy with dydrogesterone. Gynecol Endocrinol 14 (2000) 275-281
64. Ferenczy A., and Gelfand M.M. Endometrial histology and bleeding patterns in post-menopausal women taking sequential, combined estradiol and dydrogesterone. Maturitas 26 (1997) 219-226
65. ®-conti): endometrial safety and bleeding profile. Maturitas 53 (2006) 299-305
66. Bergeron C., and Ferenczy A. Endometrial safety of continuous combined hormone replacement therapy with 17beta-oestradiol (1 or 2 mg) and dydrogesterone. Maturitas 37 (2001) 191-199
67. Whitehead M.I., and Fraser D. The effects of estrogens and progestogens on the endometrium. Modern approach to treatment. Obstet Gynecol Clin North Am 14 (1987) 299-320
68. Delzanno G., Paoletti R., Gaudiano L., Bertinetti G., Ventrella C.A., and Dell'Elce C. Dihydrogesterone versus medroxyprogesterone acetate in association with transdermal oestradiol in postmenopausal replacement therapy. Minerva Ginecol 46 (1994) 179-182
69. Korhonen M.O., Symons J.P., Hyde B.M., Rowan J.P., and Wilborn W.H. Histologic classification and pathologic findings for endometrial biopsy specimens obtained from 2964 perimenopausal and postmenopausal women undergoing screening for continuous hormones as replacement therapy (CHART 2 Study). Am J Obstet Gynecol 176 (1997) 377-380
70. van de Weijer P.H.M., Scholten P.C., van der Mooren M.J., Barentsen R., and Kenemans P. Bleeding patterns and endometrial histology during administration of low-dose estradiol sequentially combined with dydrogesterone. Climacteric 2 (1999) 101-109
71. Woodruff J.D., and Pickar J.H. Incidence of endometrial hyperplasia in postmenopausal women taking conjugated estrogens (Premarin) with medroxyprogesterone acetate or conjugated estrogens alone. Am J Obstet Gynecol 170 (1994) 1213-1223
72. Modan B., Ron E., Lerner-Geva L., et al. Cancer incidence in a cohort of infertile women. Am J Epidemiol 147 (1998) 1038-1042
73. Panay N., Pritsch M., and Alt J. Cyclical dydrogesterone in secondary amenorrhea: results of a double-blind, placebo-controlled, randomized study. Gynecol Endocrinol 23 (2007) 611-618
74. Battino S., Ben-Ami M., Geslevich Y., Weiner E., and Shalev E. Factors associated with withdrawal bleeding after administration of oral dydrogesterone or medroxyprogesterone acetate in women with secondary amenorrhoea. Gynecol Obstet Invest 42 (1996) 113-116
75. Tabaste J.L., Servaud M., Steiner E., Dabir P., Bene B., and Pouzet M. Action of dydrogesterone in postpubertal menstruation disorders. Rev Fr Gynecol Obstet 79 (1984) 19-25
76. Sipowicz I., and Chomczyk I. The efficacy of dydrogesterone in the treatment of menstrual cycle disturbances in girls. Ginekol Pol 69 (1998) 767-770
77. Chomczyk I., Sipowicz M., and Sipowicz I. Dydrogesterone in the regulation of cycle disturbances in adolescence. Ginekol Pol 70 (1999) 343-347
78. Anklesaria B., Balamba P., and Banerjee B. Cycle regulation with dydrogesterone in Indian women. Obstet Gynaecol IV (1999) 559-564
79. Naib J.M., Siddiqui M.I., and Ajmal W. The role of dydrogesterone in the medical management of 100 cases of dysfunctional uterine bleeding (DUB) above 35 years of age. J Postgrad Med Inst Peshawar 17 2 (2003)
80. Dutta D.K. Management of luteal phase defect (LPD) in adolescent girls. Asian J Obstet Gynaecol Pract 5 (2001) 3-5