常用生殖激素药物__培训课件.ppt

* * * * 倍美力是多种成份的结合物，包括雌酮、雌二醇、马烯雌酮等等。 倍美力的临床活性基于其完整的组成，并非其组份中的某一部分。 * * 与微粒化E2（17-β E2）制剂比较，E2V 既有与 其相同的快速溶解的优点，又有其不具备的优点。由于 酯化作用，E2V 平缓地转变为17-β E2，避免了出现 E2 高峰浓度，从而也避免了非生理性高峰带来的不良反 应 * * 请注意烯丙雌醇是一种雌烷,属于19-去甲基睾酮类 孕激素类药物分为天然孕激素和合成孕激素. 合成孕激素的结构接近于要么与黄体酮要么接近于睾酮. References Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH. Classification and pharmacology of progestins. Maturitas. 2003 Dec 10;46 Suppl 1:S7-S16 Lobo RA, Stanczyk FZ. New knowledge in the physiology of hormonal contraceptives. Am J Obstet Gynecol. 1994;170:1499-1507. Stanczyk FZ. Pharmacology, pharmacokinetics and pharmacodynamics: pharmacokinetics of progestogens. Int Proc J. 1989;1:11-20. Rebar RW, Zeserson K. Characteristics of the new progestogens in combination oral contraceptives. Contraception. 1991;44:1-10. Philibert D, Bouchoux F, Degryse M, et al. The pharmacological profile of a novel norpregnane progestin (trimegestone). Gynecol Endocrinol. 1999;13:316-326. Muhn P, Krattenmacher R, Beier S, et al. Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity: pharmacological characterization in animal models. Contraception. 1995;51:99-110. * This slide shows the chemical structures of progesterone and Duphaston? (dydrogesterone), and illustrates the presence of a second double bond between C6 and C7 in the Duphaston? molecule. It should be noted that the carboxyl groups at position C10 and the Hydrogen molecule at position C9 extend on opposite sides of the molecule in Duphaston? in comparison to progesterone. This leads to Duphaston? have a bent shape. * * * * References: Dydrogesterone monograph; Prometrium (progesterone) monograph Fertil Steril. 1986 Dec;46(6):1062-6. Assessment of the potency of orally administered progestins in women.King RJ, Whitehead MI.The effects of at least three doses of each of five orally administered progestins on estrogen-primed, postmenopausal endometrial biochemistry and morp