London R S
Department of Obstetrics and Gynecology, Kaiser-Permanente Medical Group (CAPMG), Baltimore, MD 21207.
Obstet Gynecol Surv. 1992 Nov;47(11):777-82. doi: 10.1097/00006254-199211000-00014.
The latest advance in the 30-year evolution of oral contraceptives (OCs) is the development of three new progestogens: desogestrel, norgestimate, and gestodene. These three new agents are derivatives of levonorgestrel, a gonane hormone, and have been used to develop pills that provide effective pregnancy prevention at lower doses than oral contraceptives using the older steroids. Desogestrel is a prohormone that must first be metabolized into its biologically active form. Norgestimate is already active, but it will be metabolized in part to levonorgestrel. Gestodene is biologically active in its native form. Among the improvements in metabolic parameters seen with this new generation of progestogens are a lack of impact on blood pressure, a balanced effect on coagulation, and a reduced impact on carbohydrate metabolism compared with earlier, higher-dose formulations. The new pills also seem to produce no negative effects on lipid and lipoprotein biosynthesis, and perhaps even improve the ratio of low-density lipoprotein to high-density lipoprotein. Cycle control with all three progestogens is improved, with much lower incidence of intermenstrual bleeding (IMB). Efficacy is as good as with other OCs. Another benefit of the new low-dose progestogens, however, is the low incidence of minor side effects observed in women using these contraceptives. Low incidences of weight gain, headache, and nausea were reported, and the dropout rate because of side effects was low in both international and US trials. Serious side effects are rarely seen with pills containing the new progestogens.(ABSTRACT TRUNCATED AT 250 WORDS)
口服避孕药(OCs)30年发展历程中的最新进展是三种新型孕激素的研发:去氧孕烯、诺孕酯和孕二烯酮。这三种新型药物是左旋炔诺孕酮(一种孕烷激素)的衍生物,已被用于开发比使用旧类固醇的口服避孕药剂量更低却能有效预防妊娠的药丸。去氧孕烯是一种前体激素,必须先代谢为其生物活性形式。诺孕酯已经具有活性,但会部分代谢为左旋炔诺孕酮。孕二烯酮以其天然形式就具有生物活性。与早期高剂量配方相比,新一代孕激素在代谢参数方面的改善包括对血压无影响、对凝血有平衡作用以及对碳水化合物代谢的影响降低。这些新型药丸似乎对脂质和脂蛋白生物合成也没有负面影响,甚至可能改善低密度脂蛋白与高密度脂蛋白的比例。使用这三种孕激素时的月经周期控制都有所改善,经间期出血(IMB)的发生率大大降低。其有效性与其他口服避孕药相当。然而,新型低剂量孕激素的另一个好处是,使用这些避孕药的女性出现轻微副作用的发生率较低。据报道,体重增加、头痛和恶心的发生率较低,在国际和美国的试验中,因副作用导致的停药率都很低。含新型孕激素的药丸很少出现严重副作用。(摘要截选至250字)