Injectable depot contraceptives on d-norgestrel basis II. Clinical pharmacokinetic studies with d-norgestrel undecylate in women

作者: J. Spona , E. Weiner , B. Nieuweboer , M. Hümpel , W.H.F. Schneider

DOI: 10.1016/0010-7824(77)90004-X

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摘要: Abstract The effect of a single intramuscular injection 100 mg d-norgestrel 17β-undecylate was investigated in 8 women. Levels radioimmunoassayable serum progesterone, 17β-estradiol and were studied for at least three months. Besides registration uterine bleeding, 5 out these subjects karyopyknotic index (KI) cervical function (CF) recorded. Six patients showed maximum levels between 400 700 pg/ml 24–48 hr after the ester. Thereafter, values dropped to constant varying 50 150 pg/ml, stayed 130 days. Two maximal dnorgestrel 1300 1500 10 19 days, respectively, injection. In this group 300 days treatment. All had normal pretreatment cycles. first treatment cycles followed by anovulatory other cycles, which ovulatory Poor bleeding control registered all patients. data suggest slow release ester from depot an insufficient cleavage into fatty acid resulting low progestagen bioavailability.

参考文章(13)
Daniel R. Mishell, Mary E. Lumkin, Contraceptive effect of varying dosages of progestogen in silastic vaginal rings. Fertility and Sterility. ,vol. 21, pp. 99- 103 ,(1970) , 10.1016/S0015-0282(16)37333-2
J.B. Foster, D.J. Newell, Henry Miller, L.J. Kinlen, MULTIPLE SCLEROSIS: A TRIAL OF TREATMENT WITH TOLBUTAMIDE The Lancet. ,vol. 1, pp. 915- 917 ,(1961) , 10.1016/S0140-6736(61)91773-1
Bernard F. Erlanger, Felix Borek, Sam M. Beiser, Seymour Lieberman, Steroid-protein conjugates. I. Preparation and characterization of conjugates of bovine serum albumin with testosterone and with cortisone. Journal of Biological Chemistry. ,vol. 228, pp. 713- 727 ,(1957) , 10.1016/S0021-9258(18)70654-6
Daniel R. Mishell, Mary Lumkin, Sergio Stone, Inhibition of ovulation with cyclic use of progestogen-impregnated intravaginal devices American Journal of Obstetrics and Gynecology. ,vol. 113, pp. 927- 932 ,(1972) , 10.1016/0002-9378(72)90658-8
Frank Z. Stanczyk, Masahiko Hiroi, Uwe Goebelsmann, Paul F. Brenner, Mary E. Lumkin, Daniel R. Mishell, Radioimmunoassay of serum d-norgestrel in women following oral and intravaginal administration Contraception. ,vol. 12, pp. 279- 298 ,(1975) , 10.1016/0010-7824(75)90088-8
GUY E. ABRAHAM, Solid-Phase Radioimmunoassay of Estradiol-17β The Journal of Clinical Endocrinology and Metabolism. ,vol. 29, pp. 866- 870 ,(1969) , 10.1210/JCEM-29-6-866
M.P. Vessey, Eleanor Mears, Lidija Andolšek, Majda Ogrinc-Oven, RANDOMISED DOUBLE-BLIND TRIAL OF FOUR ORAL PROGESTAGEN-ONLY CONTRACEPTIVES The Lancet. ,vol. 299, pp. 915- 922 ,(1972) , 10.1016/S0140-6736(72)91492-4
J. Spona, W. H. F. Schneider, Central and Peripheral Parameters of the Menstrual Cycle Under the Influence of a New Combined Oral Contraceptive Acta Obstetricia et Gynecologica Scandinavica. ,vol. 55, pp. 45- 50 ,(1976) , 10.3109/00016347609156448
Daniel R. Mishell, Mary Lumkin, Theodore Jackanicz, Initial clinical studies of intravaginal rings containing norethindrone and norgestrel Contraception. ,vol. 12, pp. 253- 260 ,(1975) , 10.1016/0010-7824(75)90086-4