Mifepristone: Clinical pharmacology

Clinical Obstetrics and Gynecology

Volumn 39, Issue 2, 1996, Pages 436-450

  Robbins, Ann ^a   Spitz, Irving M ^a  

^a Ctr Biomed Res Pop C   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

11BETA [4 (DIMETHYLAMINO)PHENYL] 4',5' DIHYDRO 6BETA METHYLSPIRO[ESTRA 4,9 DIENE 17BETA,2'(3'H) FURAN] 3 ONE; ANTIGESTAGEN; LILOPRISTONE; MIFEPRISTONE; ONAPRISTONE; ORG 33628; PROGESTERONE RECEPTOR; UNCLASSIFIED DRUG;

CUSHING DISEASE; DOSE RESPONSE; DRUG ABSORPTION; DRUG CLEARANCE; DRUG CONFORMATION; DRUG EFFECT; DRUG HALF LIFE; DRUG RECEPTOR BINDING; ENDOMETRIOSIS; HORMONAL CONTRACEPTION; HORMONE INHIBITION; HUMAN; INDUCED ABORTION; NONHUMAN; RECEPTOR AFFINITY; REVIEW; STRUCTURE ACTIVITY RELATION; UTERUS MYOMA;

ANIMALS; BRAIN; ENDOMETRIUM; FEMALE; GENITALIA, FEMALE; HORMONE ANTAGONISTS; HUMANS; MALE; MIFEPRISTONE; OVARY; RECEPTORS, PROGESTERONE; SPERMATOZOA;

EID: 0029865951     PISSN: 00099201     EISSN: None     Source Type: Journal    
DOI: 10.1097/00003081-199606000-00017     Document Type: Review

References (21)

1. Spitz IM, Bardin CW. Mifepristone (RU 486) - a modulator of progestin and glucocorticoid action. New Engl J Med. 1993;329: 404-412.
2. Van Look PFA, von Hertzen H. Clinical uses of antiprogestins. Human Reprod Update. 1995;1:19-34.
3. Spitz IM, Croxatto HB, Robbins A. Antiprogestins - mechanism of action and contraceptive potential. Annu Rev Pharmacol Toxicol. 1996;36:47-81.
4. Glasier A, Thong KJ, Dewar M, Mackie M, Baird DT. Mifepristone (RU 486) compared with high-dose estrogen and progestogen for emergency postcoital contraception. New Engl J Med. 1992;327:1041-1044.
5. Spitz IM, Bardin CW. Clinical pharmacology of RU 486 - an antiprogestin and antiglucocorticoid. Contraception. 1993;48: 403-444.
6. Teutsch G, Philibert D. History and perspectives of antiprogestins from the chemist's point of view. In: Beier HM, Spitz IM, eds. Progesterone Antagonists in Reproductive Medicine and Oncology. Oxford: Oxford University Press, 1994:12-31.
7. Benhamou B, Garcia T, Lerouge T, et al. A single amino acid that determines the sensitivity of progesterone receptors to RU 486. Science. 1992;255:206-209.
8. Tsai M-J, O'Malley BW. Molecular mechanisms of action of steroid/thyroid receptor superfamily members. Annu Rev Biochem. 1994;63:451-486.
9. McDonnell DP. Unraveling the human progesterone receptor signal transduction pathways (insights into antiprogestin action). Trends Endocrinol Metab. 1995;6: 133-138.
10. Hodgen GD, van Uem JFHM, Chillik CF, et al. Non-competitive anti-oestrogenic activity of progesterone antagonists in primate models. In: Beier HM, Spitz IM, eds. Progesterone Antagonists in Reproductive Medicine and Oncology. Oxford: Oxford University Press, 1994:77-81.
11. Deraedt R, Bonnat C, Busigny M, et al. Pharmacokinetics of RU 486. In: Baulieu EE, Segal SJ, eds. The Antiprogestin Steroid RU 486 and Human Fertility Control. New York: Plenum Press, 1985:103-122.
12. Chwalisz K, Stöckemann K, Fuhrmann U, Fritzemeier KH, Einspanier A, Garfield RE. Mechanism of action of antiprogestins in the pregnant uterus. Ann NY Acad Sci. 1995;761:202-223.
13. Cho BN, Seong JY, Cho H, Kim K. Progesterone stimulates GnRH gene expression in the hypothalamus of ovariectomized, estrogen treated adult rats. Brain Res. 1994;652: 177-180.
14. Batista MC, Cartledge TP, Zellmer AW, Nieman LK, Loriaux DL, Merriam GR. The antiprogestin RU486 delays the midcycle gonadotropin surge and ovulation in gonadotropin-releasing hormone-induced cycles. Fertil Steril. 1994;62:28-34.
15. Murphy AA, Castellano PZ. RU486: pharmacology and potential use in the treatment of endometriosis and leiomyomata uteri. Curr Opin Obstet Gynecol. 1994;6:269-278.
16. Refaeli Y, Levy DN, Weiner DB. The glucocorticoid receptor type II complex is a target of the HIV-1 vpr gene product. Proc Natl Acad Sci USA. 1995;92:3621-3625.
17. Li Y, Huang C, Klindt J, Anderson LL. Stimulation of prolactin secretion in the pig: central effects of relaxin and the antiprogesterone RU 486. Endocrinology. 1993; 133:1205-1212.
18. Gemzell-Danielsson K, Swahn M-L, Svalander P, Bygdeman M. Early luteal phase treatment with mifepristone (RU 486) for fertility regulation. Human Reprod. 1993;8: 870-873.
19. Baird DT. Antigestogens. Br Med Bull. 1993;49:73-87.
20. Yang J, Serres C, Philibert D, Robel P, Baulieu E-E, Jouannet P. Progesterone and RU 486: opposing effects on human sperm. Proc Natl Acad Sci USA. 1994;91:529-533.
21. Parthasarathy S, Morales AJ, Murphy AA. Antioxidant: a new role for RU-486 and related compounds. J Clin Invest. 1994;94: 1990-1995.