Mifepristone: bioavailability, pharmacokinetics and use-effectiveness

Nandini Sarkar1
1Department of Reproductive Biology, All India Institute of Medical Sciences, Ansarinagar, New Delhi 110029, India

Tóm tắt

Từ khóa


Tài liệu tham khảo

Herrman, 1982, Effect d’um steroide antiprogesterone chez la femme: interruption dy cucle menstruel et dela grossese an bedut, CR Acad. Sci. Paris, 294, 933

Spitz, 1993, Clinical pharmacology of RU486: an anti-progestin and anti-glucocorticoid, Contraception, 48, 403, 10.1016/0010-7824(93)90133-R

Murray, 1996, Mifepristone and first trimester abortion, Clin. Obstet. Gynecol., 39, 474, 10.1097/00003081-199606000-00021

Robbins, 1996, Mifepristone: clinical pharmacolgy, Clin. Obstet. Gynecol., 39, 436, 10.1097/00003081-199606000-00017

Yong-en, 1993, Pharmocokinetic study of RU486 and its metabolites after oral administration of single doses to pregnant and non-pregnant women, Contraception, 48, 133, 10.1016/0010-7824(93)90004-Q

Swahn, 1986, Plasma levels of anti progestin RU486 following oral administration to non-pregnant and early pregnant women, Contraception, 34, 469, 10.1016/0010-7824(86)90056-9

Liu, 1988, Pharmacokinetics of antiprogesterone RU486 in women after oral administration, Fertil Steril, 50, 245, 10.1016/S0015-0282(16)60067-5

Heikinheimo, 1989, Pharmacokinetics of the antiprogestin RU486 in women during multiple doses administration, J. Steroid Biochem, 32, 21, 10.1016/0022-4731(89)90008-3

Heikinheimo, 1986, Quantitation of RU486 in human plasma by HPLC and RIA after column chromatography, Contraception, 34, 613, 10.1016/S0010-7824(86)80017-8

Foldesi, 1996, Determination of RU486 (mifepristone) in blood by radioreceptor assay: a pharmacokinetic study, Contraception, 56, 27, 10.1016/0010-7824(96)00116-3

Van Look, 1989, Antiprogestational steroids: a new dimension in fertility regulation, Oxf Rev. Reprod. Biol., 11, 1

Sartos, 1996, Mifepristone: antineoplastic studies, Clin. Obstet Gynecol, 39, 498, 10.1097/00003081-199606000-00023

Heikinheimo, 1989, Distribution of RU486 and its demethylated metabolites in human, J. Clin. Endocrinol. Metab., 68, 270, 10.1210/jcem-68-2-270

Heikinheimo, 1987, Plasma concentrations and receptor binding of RU486 and its metabolites in human, J. Steriod Biochem, 26, 279, 10.1016/0022-4731(87)90083-5

Croxatto, 1993, Effect of continuous treatment with low dose mifepristone throughout one menstrual cycle, Hum Reprod., 8, 201, 10.1093/oxfordjournals.humrep.a138022

Kekkonen, 1996, Pharmacokinetics of mifepristone after low oral doses, Contraception, 54, 229, 10.1016/S0010-7824(96)00193-X

Heikinheimo, 1993, Dose response relationship of RU486, Ann. Med., 25, 71, 10.3109/07853899309147861

Changhai, 1989, Phrmacokinetic study of orally administered RU486 in non-pregnant women, Contraception, 40, 449, 10.1016/0010-7824(89)90052-8

Foldesi, 1994, Pharmacokinetics of RU486 and its active metabolites in humans, Acta Pharma Hung, 64, 17

Cekan, 1989, Levels of antiprogestin RU486 and its metabolites in human blood and follicular fluid following oral administration of a single dose, Hum Repro, 4, 131, 10.1093/oxfordjournals.humrep.a136857

Heikinheimo, 1997, Clinical pharmacokinetics of mifepristone, Clin. Pharmacokinet, 33, 7, 10.2165/00003088-199733010-00002

Pinter, 1996, Progesterone receptors: expression and regulation in the mammalian ovary, Clin. Obstet. Gynecol., 39, 424, 10.1097/00003081-199606000-00016

Williams, 1998, Atomic structure of progesterone complexed with its receptors, Nature, 393, 392, 10.1038/30775

Tsai, 1994, Molecular mechanism of action of steroid/thyroid receptor super family members, Annu. Rev. Biochem., 63, 451, 10.1146/annurev.bi.63.070194.002315

DeMarzo, 1991, Dimerization of mammalian progesterone receptors occurs in the absence of DNA and is related to the release of the 90-kDa heat shock protein, Proc. Natl. Acad. Sci. U.S.A., 88, 72, 10.1073/pnas.88.1.72

DeMarzo, 1992, Effects of the steroid antagonist RU486 on dimerization of the human progesterone receptor, Biochemistry, 31, 10491, 10.1021/bi00158a012

Benhamou, 1992, A single amino acid that determines the sensitivity of progesterone receptors to RU486, Science, 255, 206, 10.1126/science.1372753

Ulman, 1994, RU486: the French experience, Hum. Reprod., 9, 126, 10.1093/humrep/9.suppl_1.126

Urguhart, 1997, The efficacy and tolerance of mifepristone and prostaglandin in termination of pregnancy less than 63 days gestation: UK multicentre study-final results, Contraception, 55, 1, 10.1016/S0010-7824(96)00252-1

WHO. Termination of pregnancy with reduced doses of mifepristone. Br Med J 1993;307:532-7.

WHO. Pregnancy termination with mifepristone and gemeprost: a multicentre comparison between repeated doses and a single dose of mifepristone, Fertil Steril 1991;56:32-40.

Sang, 1994, Termination of early pregnancy by two regimens of mifepristone with misoprostol and mifepristone with PGO5: a multicentre clinical trial in China, Contraception, 50, 501, 10.1016/0010-7824(94)90009-4

Prasad, 1996, Termination of early human pregnancy with either 50 or 200 mg single oral dose of mifepristone (RU486) in combination with either 0.5 mg or 1 mg vaginal gemeprost, Aust. N. Z. J. Obstet. Gynecol., 36, 20, 10.1111/j.1479-828X.1996.tb02915.x

Winikoff, 1997, Safety efficacy and acceptability of medical abortion in China Cuba and India. A comparative trial of mifepristone–misoprostol versus surgical abortion, Am. J. Obstet. Gynecol., 176, 431, 10.1016/S0002-9378(97)70511-8

Brogden, 1993, Mifepristone: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential, Drugs, 45, 384, 10.2165/00003495-199345030-00007

Prasad, 1995, Blood loss in termination of early pregnancy with mifepristone and gemeprost, Aust. N.Z.J. Obstet. Gynecol., 35, 329, 10.1111/j.1479-828X.1995.tb01996.x

Harper, 1998, Blood loss with mifepristone–misoprostol abortion; measures from a trial in China, Cuba and India, Int. J. Gynecol. Obstet., 63, 39, 10.1016/S0020-7292(98)00102-7

Elul, 1999, Side effects of mifepristone–misoprostol abortion versus surgical abortion. Data from a trial in China, Cuba and India, Contraception, 59, 107, 10.1016/S0010-7824(99)00003-7

Jensen, 1999, Outcome of suction curettage and mifepristone abortion in the United States. A prospective comparison study, Contraception, 59, 153, 10.1016/S0010-7824(99)00016-5

Spitz, 1998, Early pregnancy ternnnation with mifepristone and misoprostol in the United States, N. Engl. J. Med., 338, 1214, 10.1056/NEJM199804303381801

Sandstrom, 1999, Interruption of early pregnancy with mifepristone in combination with gemeprost, Acta. Obstet. Gynecol. Scand., 78, 806, 10.1080/j.1600-0412.1999.780913.x

Ashok, 1998, An effective regimen for early medical abortion: report of 2000 consecutive cases, Hum. Reprod., 13, 2962, 10.1093/humrep/13.10.2962

Schaff, 1999, Low-dose mifepristone 200 mg and vaginal misoprostol for abortion, Contraception, 59, 1, 10.1016/S0010-7824(98)00150-4

WHO task force on post-ovulatory methods of fertility regulations. Comparison of two doses of mifepristone in combination with misoprostol for early medical abortion:a randomised trial. Br J Obstet Gynecol 2000;107:524-30.

Schaff, 2000, Low-dose mifepristone followed by vaginal misoprostol at 48 hours for abortion up to 63 days, Contraception, 61, 41, 10.1016/S0010-7824(99)00119-5

Schaff, 2000, A comparison of the abortion rights mobilization and population council trials, J. Am. Med. Women’s Assoc., 55, 137

von-Hertzen, 2000, Research on regimens for early nedical abortion, J. Am. Med. Women’s Assoc., 55, 133

Kahn, 2000, The efficacy of medical abortion: a meta-analysis, Contraception, 61, 29, 10.1016/S0010-7824(99)00115-8

Creinin, 1997, Misoprostol for medical evacuation of early pregnancy failure, Obstet. Gynecol., 89, 768, 10.1016/S0029-7844(97)81438-X

Danielsson, 1999, Comparison between oral and vaginal administration of misoprostol on uterine contractility, Obstet. Gynecol., 93, 275, 10.1016/S0029-7844(98)00436-0

Zieman, 1997, Absorption kinetics of misoprostol with oral or vaginal administration, Obstet. Gynecol., 90, 88, 10.1016/S0029-7844(97)00111-7

Heikinheimo, 1990, Phmmacokinetics of antiprogesterone RU486; no correlation to clinical perforrnance of RU486, Acta. Endocrinol. Copenh., 123, 298, 10.1530/acta.0.1230298

Baulieu, 1989, Contragestion and other clinical applications of RU486, an anti-progesterone at the receptor, Science, 245, 1351, 10.1126/science.2781282

Glacier, 1992, Mifepristrone (RU486) compared with high-dose estrogen and progestogen for emergency post-coital contraception, N. Engl. J. Med., 327, 1041, 10.1056/NEJM199210083271501

Webb, 1992, Comparison of Yuzpe regimen, danazol and mifepristone (RU486) in oral post-coital contraception, Br. Med. J., 305, 927, 10.1136/bmj.305.6859.927

Paychoyos, 1995, Hormonal anti-implantation agents, anti progestins, Hum. Reprod., 10, 140, 10.1093/humrep/10.suppl_2.140

Swahn, 1996, Contraception with anti-progesterone, Baillieres. Clin. Obstet. Gynecol., 10, 43, 10.1016/S0950-3552(96)80061-7

Han, 1996, Emergency contraception with mifepristone and anordin, Chang Hua-Fu-Chan-Ko-Tsa-Chih, 31, 526

WHO: task force on post-ovulatory methods of fertility regulation. Comparison of three single doses of mifepristone as emergency contraception: a randomised trial, Lancet 1999;353:697-702.

Danielsson, 1996, Effect of low weekly doses of mifepristone on ovarian function and endometrial development, Hum. Reprod., 11, 256, 10.1093/HUMREP/11.2.256

Danielsson, 1997, Effect of low daily doses of mifepristone on ovarian function and endometrial development, Hum. Reprod., 12, 124, 10.1093/humrep/12.1.124

Nayak, 1998, Antinidatory effect of luteal phase administration of mifepristone (RU486) is associated with changes in endometrial prostaglandins during implantation window, Contraception, 58, 111, 10.1016/S0010-7824(98)00068-7

Bygdernan, 1997, The possible use of anti-progestins for contraception, Acta. Obstet. Gynecol. Scand. Suppl., 164, 75

Chen, 1997, Effect of once weekly administration of mifepristone on ovarian function in normal women, Contraception, 56, 175, 10.1016/S0010-7824(97)00115-7

Croxatto, 1998, Effect of long-term low-dose mifepristone on reproductive function in women, Hum. Reprod., 13, 793, 10.1093/humrep/13.4.793

Marions, 1998, Contraceptive efficacy of low doses of mifepristone, Fertil. Steril., 70, 813, 10.1016/S0015-0282(98)00306-9

Danielsson, 1993, Early luteal phase treatment with mifepristone (RU486) for fertility regulation, Hum. Reprod., 8, 870, 10.1093/oxfordjournals.humrep.a138157

Bygdeman, 1999, Comparative use of anti-progestin, Eur. J. Contracept. Reprod. Health Care, 4, 103, 10.3109/13625189909064011

Sarkar, 2000, Mifepristone as abortifacient and contraceptive drug: attitude, efficacy and acceptability, Int. Med. J., 7, 67