Intrauterine progestins, progesterone antagonists, and receptor modulators: a review of gynecologic applications

American Journal of Obstetrics and Gynecology

Volumn 202, Issue 5, 2010, Pages 420-428

  Rodriguez, Maria Isabel ^a   Warden, Meredith ^a   Darney, Philip D ^a  

^a SAN FRANCISCO GENERAL HOSPITAL   (United States)

Author keywords

intrauterine progestin; leiomyomas; levonorgestrel intrauterine device; menorrhagia; progesterone receptor modulators

Indexed keywords

11BETA (4 ACETYLPHENYL) 17BETA HYDROXY 17ALPHA (1,1,2,2,2 PENTAFLUOROETHYL)ESTRA 4,9 DIEN 3 ONE; ANTIGESTAGEN; ASOPRISNIL; CBD 2914; GESTAGEN; GONADOTROPIN DERIVATIVE; LEVONORGESTREL; MIFEPRISTONE; PLACEBO; PROGESTERONE RECEPTOR MODULATOR; TAMOXIFEN; UNCLASSIFIED DRUG;

ABORTION; ABSENCE OF SIDE EFFECTS; ADENOMYOSIS; AMENORRHEA; ANTIPROLIFERATIVE ACTIVITY; ARTERY BLOOD FLOW; BREAST CANCER; CLINICAL TRIAL; COST EFFECTIVENESS ANALYSIS; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG PROTEIN BINDING; DRUG TOLERABILITY; ECHOGRAPHY; ENDOMETRIAL DISEASE; ENDOMETRIOSIS; ENDOMETRIUM ABLATION; ENDOMETRIUM HYPERPLASIA; ESTROGEN DEFICIENCY; HORMONAL CONTRACEPTION; HORMONE SUBSTITUTION; HUMAN; HYSTERECTOMY; INTERMETHOD COMPARISON; LAPAROSCOPY; LOW DRUG DOSE; MENORRHAGIA; NONHUMAN; PATIENT COUNSELING; PELVIS PAIN SYNDROME; POLYP; POSTMENOPAUSE; PRIORITY JOURNAL; QUALITY OF LIFE; REVIEW; UTERINE ARTERY BLOOD FLOW; UTERINE HYPERPLASIA; UTERUS DISEASE; UTERUS MYOMA;

ADMINISTRATION, TOPICAL; ENDOMETRIOSIS; FEMALE; HUMANS; HYSTERECTOMY; INTRAUTERINE DEVICES, MEDICATED; LEIOMYOMA; MENORRHAGIA; PROGESTINS; RECEPTORS, PROGESTERONE; REPRODUCTIVE MEDICINE; UTERINE NEOPLASMS;

EID: 77951880664     PISSN: 00029378     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ajog.2009.10.863     Document Type: Review

References (73)

1. Pintiaux A., Chabbert-Buffet N., and Foidart J.M. Gynaecological uses of a new class of steroids: the selective progesterone receptor modulators. Gynecol Endocrinol 25 (2009) 67-73
2. Speroff L., and Darney P.F. A clinical guide for contraception (2005), Lippincott Williams & Wilkins, Philadelphia
3. Harper C.C., Blum M., de Bocanegra H.T., et al. Challenges in translating evidence to practice: the provision of intrauterine contraception. Obstet Gynecol 111 (2008) 1359-1369
4. Frank E. Contraceptive use by female physicians in the United States. Obstet Gynecol 94 (1999) 666-671
5. American College of Obstetricians and Gynecologists. Gallup survey reveals women Ob-Gyns benefit from "insider knowledge.". Vol 2009 (2003), American College of Obstetricians and Gynecologists, Washington, DC
6. Inki P. Long-term use of the levonorgestrel-releasing intrauterine system. Contraception 75 (2007) S161-S166
7. Chabbert-Buffet N., Meduri G., Bouchard P., and Spitz I.M. Selective progesterone receptor modulators and progesterone antagonists: mechanisms of action and clinical applications. Hum Reprod Update 11 (2005) 293-307
8. Bahamondes L., Petta C.A., Fernandes A., and Monteiro I. Use of the levonorgestrel-releasing intrauterine system in women with endometriosis, chronic pelvic pain and dysmenorrhea. Contraception 75 (2007) S134-S139
9. Leonhardt S.A., and Edwards D.P. Mechanism of action of progesterone antagonists. Exp Biol Med (Maywood) 227 (2002) 969-980
10. 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
11. Smith C.L., and O'Malley B.W. Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr Rev 25 (2004) 45-71
12. Stewart A., Cummins C., Gold L., Jordan R., and Phillips W. The effectiveness of the levonorgestrel-releasing intrauterine system in menorrhagia: a systematic review. BJOG 108 (2001) 74-86
13. Milsom I. The levonorgestrel-releasing intrauterine system as an alternative to hysterectomy in peri-menopausal women. Contraception 75 (2007) S152-S154
14. Hurskainen R., Teperi J., Aalto A.M., et al. Levonorgestrel-releasing intrauterine system or hysterectomy in the treatment of essential menorrhagia: predictors of outcome. Acta Obstet Gynecol Scand 83 (2004) 401-403
15. Andersson J.K., and Rybo G. Levonorgestrel-releasing intrauterine device in the treatment of menorrhagia. Br J Obstet Gynaecol 97 (1990) 690-694
16. Hurskainen R., and Paavonen J. Levonorgestrel-releasing intrauterine system in the treatment of heavy menstrual bleeding. Curr Opin Obstet Gynecol 16 (2004) 487-490
17. Milsom I., Andersson K., Andersch B., and Rybo G. A comparison of flurbiprofen, tranexamic acid, and a levonorgestrel-releasing intrauterine contraceptive device in the treatment of idiopathic menorrhagia. Am J Obstet Gynecol 164 (1991) 879-883
18. Reid P.C., and Virtanen-Kari S. Randomised comparative trial of the levonorgestrel intrauterine system and mefenamic acid for the treatment of idiopathic menorrhagia: a multiple analysis using total menstrual fluid loss, menstrual blood loss and pictorial blood loss assessment charts. BJOG 112 (2005) 1121-1125
19. Busfield R.A., Farquhar C.M., Sowter M.C., et al. A randomised trial comparing the levonorgestrel intrauterine system and thermal balloon ablation for heavy menstrual bleeding. BJOG 113 (2006) 257-263
20. Brown P.M., Farquhar C.M., Lethaby A., Sadler L.C., and Johnson N.P. Cost-effectiveness analysis of levonorgestrel intrauterine system and thermal balloon ablation for heavy menstrual bleeding. BJOG 113 (2006) 797-803
21. Shaw R.W., Symonds I.M., Tamizian O., Chaplain J., and Mukhopadhyay S. Randomised comparative trial of thermal balloon ablation and levonorgestrel intrauterine system in patients with idiopathic menorrhagia. Aust N Z J Obstet Gynaecol 47 (2007) 335-340
22. Kaunitz A.M., Meredith S., Inki P., Kubba A., and Sanchez-Ramos L. Levonorgestrel-releasing intrauterine system and endometrial ablation in heavy menstrual bleeding: a systematic review and meta-analysis. Obstet Gynecol 113 (2009) 1104-1116
23. Lahteenmaki P., Haukkamaa M., Puolakka J., et al. Open randomised study of use of levonorgestrel releasing intrauterine system as alternative to hysterectomy. BMJ 316 (1998) 1122-1126
24. Hurskainen R., Teperi J., Rissanen P., et al. Clinical outcomes and costs with the levonorgestrel-releasing intrauterine system or hysterectomy for treatment of menorrhagia: randomized trial 5-year follow-up. JAMA 291 (2004) 1456-1463
25. 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 (2007) 2515-2522
26. Ozkan S., and Arici A. Advances in treatment options of endometriosis. Gynecol Obstet Invest 67 (2009) 81-91
27. Petta C.A., Ferriani R.A., Abrao M.S., et al. Randomized clinical trial of a levonorgestrel-releasing intrauterine system and a depot GnRH analogue for the treatment of chronic pelvic pain in women with endometriosis. Hum Reprod 20 (2005) 1993-1998
28. Vercellini P., Aimi G., Panazza S., De Giorgi O., Pesole A., and Crosignani P.G. A levonorgestrel-releasing intrauterine system for the treatment of dysmenorrhea associated with endometriosis: a pilot study. Fertil Steril 72 (1999) 505-508
29. Petta C.A., Ferriani R.A., Abrao M.S., et al. A 3-year follow-up of women with endometriosis and pelvic pain users of the levonorgestrel-releasing intrauterine system. Eur J Obstet Gynecol Reprod Biol 143 (2009) 128-129
30. Vercellini P., Frontino G., De Giorgi O., Aimi G., Zaina B., and Crosignani P.G. Comparison of a levonorgestrel-releasing intrauterine device versus expectant management after conservative surgery for symptomatic endometriosis: a pilot study. Fertil Steril 80 (2003) 305-309
31. Lockhat F.B., Emembolu J.O., and Konje J.C. The efficacy, side-effects and continuation rates in women with symptomatic endometriosis undergoing treatment with an intra-uterine administered progestogen (levonorgestrel): a 3 year follow-up. Hum Reprod 20 (2005) 789-793
32. Chwalisz K., Perez M.C., Demanno D., Winkel C., Schubert G., and Elger W. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Endocr Rev 26 (2005) 423-438
33. Ferenczy A. Pathophysiology of adenomyosis. Hum Reprod Update 4 (1998) 312-322
34. Fong Y.F., and Singh K. Medical treatment of a grossly enlarged adenomyotic uterus with the levonorgestrel-releasing intrauterine system. Contraception 60 (1999) 173-175
35. Cho S., Nam A., Kim H., et al. Clinical effects of the levonorgestrel-releasing intrauterine device in patients with adenomyosis. Am J Obstet Gynecol 198 (2008) 373.e1-373.e7
36. Fedele L., Bianchi S., Raffaelli R., Portuese A., and Dorta M. Treatment of adenomyosis-associated menorrhagia with a levonorgestrel-releasing intrauterine device. Fertil Steril 68 (1997) 426-429
37. Bragheto A.M., Caserta N., Bahamondes L., and Petta C.A. Effectiveness of the levonorgestrel-releasing intrauterine system in the treatment of adenomyosis diagnosed and monitored by magnetic resonance imaging. Contraception 76 (2007) 195-199
38. Sheng J., Zhang W.Y., Zhang J.P., and Lu D. The LNG-IUS study on adenomyosis: a 3-year follow-up study on the efficacy and side effects of the use of levonorgestrel intrauterine system for the treatment of dysmenorrhea associated with adenomyosis. Contraception 79 (2009) 189-193
39. Buttram Jr. V.C., and Reiter R.C. Uterine leiomyomata: etiology, symptomatology, and management. Fertil Steril 36 (1981) 433-445
40. Kaunitz A.M. Progestin-releasing intrauterine systems and leiomyoma. Contraception 75 (2007) S130-S133
41. Grigorieva V., Chen-Mok M., Tarasova M., and Mikhailov A. Use of a levonorgestrel-releasing intrauterine system to treat bleeding related to uterine leiomyomas. Fertil Steril 79 (2003) 1194-1198
42. Gunes M., Ozdegirmenci O., Kayikcioglu F., Haberal A., and Kaplan M. The effect of levonorgestrel intrauterine system on uterine myomas: a 1-year follow-up study. J Minim Invasive Gynecol 15 (2008) 735-738
43. Magalhaes J., Aldrighi J.M., and de Lima G.R. Uterine volume and menstrual patterns in users of the levonorgestrel-releasing intrauterine system with idiopathic menorrhagia or menorrhagia due to leiomyomas. Contraception 75 (2007) 193-198
44. Mercorio F., De Simone R., Di Spiezio Sardo A., et al. The effect of a levonorgestrel-releasing intrauterine device in the treatment of myoma-related menorrhagia. Contraception 67 (2003) 277-280
45. Soysal S., and Soysal M.E. The efficacy of levonorgestrel-releasing intrauterine device in selected cases of myoma-related menorrhagia: a prospective controlled trial. Gynecol Obstet Invest 59 (2005) 29-35
46. Rosa e Silva J.C., de Sa Rosa e Silva A.C., Candido dos Reis F.J., Manetta L.A., Ferriani R.A., and Nogueira A.A. Use of a levonorgestrel-releasing intrauterine device for the symptomatic treatment of uterine myomas. J Reprod Med 50 (2005) 613-617
47. Maruo T., Ohara N., Matsuo H., et al. Effects of levonorgestrel-releasing IUS and progesterone receptor modulator PRM CDB-2914 on uterine leiomyomas. Contraception 75 (2007) S99-S103
48. Rizkalla H.F., Higgins M., Kelehan P., and O'Herlihy C. Pathological findings associated with the presence of a mirena intrauterine system at hysterectomy. Int J Gynecol Pathol 27 (2008) 74-78
49. Fong Y.F., and Singh K. Effect of the levonorgestrel-releasing intrauterine system on uterine myomas in a renal transplant patient. Contraception 60 (1999) 51-53
50. Inki P., Hurskainen R., Palo P., et al. Comparison of ovarian cyst formation in women using the levonorgestrel-releasing intrauterine system vs. hysterectomy. Ultrasound Obstet Gynecol 20 (2002) 381-385
51. Gardner F.J., Konje J.C., Abrams K.R., et al. Endometrial protection from tamoxifen-stimulated changes by a levonorgestrel-releasing intrauterine system: a randomised controlled trial. Lancet 356 (2000) 1711-1717
52. Tasci Y., Caglar G.S., Kayikcioglu F., Cengiz H., Yagci B., and Gunes M. Treatment of menorrhagia with the levonorgestrel releasing intrauterine system: effects on ovarian function and uterus. Arch Gynecol Obstet 280 (2009) 39-42
53. Monteiro I., Bahamondes L., Diaz J., Perrotti M., and Petta C. Therapeutic use of levonorgestrel-releasing intrauterine system in women with menorrhagia: a pilot study (1). Contraception 65 (2002) 325-328
54. DeManno D., Elger W., Garg R., et al. Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy. Steroids 68 (2003) 1019-1032
55. Steinauer J., Pritts E.A., Jackson R., and Jacoby A.F. Systematic review of mifepristone for the treatment of uterine leiomyomata. Obstet Gynecol 103 (2004) 1331-1336
56. Fiscella K., Eisinger S.H., Meldrum S., Feng C., Fisher S.G., and Guzick D.S. Effect of mifepristone for symptomatic leiomyomata on quality of life and uterine size: a randomized controlled trial. Obstet Gynecol 108 (2006) 1381-1387
57. Ohara N., Morikawa A., Chen W., et al. Comparative effects of SPRM asoprisnil (J867) on proliferation, apoptosis, and the expression of growth factors in cultured uterine leiomyoma cells and normal myometrial cells. Reprod Sci 14 (2007) 20-27
58. Levens E.D., Potlog-Nahari C., Armstrong A.Y., et al. CDB-2914 for uterine leiomyomata treatment: a randomized controlled trial. Obstet Gynecol 111 (2008) 1129-1136
59. Chwalisz K., DeManno D., Garg R., Larsen L., Mattia-Goldberg C., and Stickler T. Therapeutic potential for the selective progesterone receptor modulator asoprisnil in the treatment of leiomyomata. Semin Reprod Med 22 (2004) 113-119
60. Chwalisz K., Larsen L., Mattia-Goldberg C., Edmonds A., Elger W., and Winkel C.A. A randomized, controlled trial of asoprisnil, a novel selective progesterone receptor modulator, in women with uterine leiomyomata. Fertil Steril 87 (2007) 1399-1412
61. Wildemeersch D., and Dhont M. Treatment of nonatypical and atypical endometrial hyperplasia with a levonorgestrel-releasing intrauterine system. Am J Obstet Gynecol 188 (2003) 1297-1298
62. Varma R., Soneja H., Bhatia K., et al. The effectiveness of a levonorgestrel-releasing intrauterine system (LNG-IUS) in the treatment of endometrial hyperplasia-a long-term follow-up study. Eur J Obstet Gynecol Reprod Biol 139 (2008) 169-175
63. Wildemeersch D., Janssens D., Pylyser K., et al. Management of patients with non-atypical and atypical endometrial hyperplasia with a levonorgestrel-releasing intrauterine system: long-term follow-up. Maturitas 57 (2007) 210-213
64. Wheeler D.T., Bristow R.E., and Kurman R.J. Histologic alterations in endometrial hyperplasia and well-differentiated carcinoma treated with progestins. Am J Surg Pathol 31 (2007) 988-998
65. Orbo A., Arnes M., Hancke C., Vereide A.B., Pettersen I., and Larsen K. Treatment results of endometrial hyperplasia after prospective D-score classification: a follow-up study comparing effect of LNG-IUD and oral progestins versus observation only. Gynecol Oncol 111 (2008) 68-73
66. Vereide A.B., Arnes M., Straume B., Maltau J.M., and Orbo A. Nuclear morphometric changes and therapy monitoring in patients with endometrial hyperplasia: a study comparing effects of intrauterine levonorgestrel and systemic medroxyprogesterone. Gynecol Oncol 91 (2003) 526-533
67. Varma R., Sinha D., and Gupta J.K. Non-contraceptive uses of levonorgestrel-releasing hormone system (LNG-IUS)-a systematic enquiry and overview. Eur J Obstet Gynecol Reprod Biol 125 (2006) 9-28
68. Mutter G.L., Bergeron C., Deligdisch L., et al. The spectrum of endometrial pathology induced by progesterone receptor modulators. Mod Pathol 21 (2008) 591-598
69. Ioffe O.B., Zaino R.J., and Mutter G.L. Endometrial changes from short-term therapy with CDB-4124, a selective progesterone receptor modulator. Mod Pathol 22 (2009) 450-459
70. Cohen I. Endometrial pathologies associated with postmenopausal tamoxifen treatment. Gynecol Oncol 94 (2004) 256-266
71. Kesim M.D., Aydin Y., Atis A., and Mandiraci G. Long-term effects of the levonorgestrel-releasing intrauterine system on serum lipids and the endometrium in breast cancer patients taking tamoxifen. Climacteric 11 (2008) 252-257
72. ACOG committee opinion. No. 336: tamoxifen and uterine cancer. Obstet Gynecol 107 (2006) 1475-1478
73. Chan S.S., Tam W.H., Yeo W., et al. A randomised controlled trial of prophylactic levonorgestrel intrauterine system in tamoxifen-treated women. BJOG 114 (2007) 1510-1515