Benagiano G, Primiero F M
Drugs. 1983 Jun;25(6):570-609. doi: 10.2165/00003495-198325060-00003.
Long acting injectable hormonal contraceptives are among the most effective fertility regulating agents developed; yet they are also among the most controversial because of animal data indicating a possible carcinogenic potential in several species. A critical analysis of these animal findings has revealed, in all instances, the existence of specific mechanisms not occurring in the human. For this reason, most national and international scientific bodies who have reviewed this issue have concluded that there are no toxicological reasons for not using long acting hormonal contraceptives. Long acting agents can be divided into 2 separate groups: those having a duration of action of one month, which are composed of a long acting oestrogen and a progestagen, and those lasting for several months which consist of only a progestagen. Among the injectable progestagen-only contraceptives tested, only 2 have so far reached the international market: depot medroxyprogesterone acetate (DMPA), which has been administered at 3- or 6-month intervals and norethisterone enanthate, which has been injected at intervals ranging between 2 and 3 months. The most important side effect observed with these 2 agents is a complete disruption of the menstrual bleeding pattern, leading - in some cases - to total amenorrhoea, which is more frequent with depot medroxyprogesterone acetate than with norethisterone enanthate. The latter, however, has a shorter duration of action with a higher pregnancy rate than the former. Other adverse reactions are rare and of no real importance. Metabolic effects with progestagen-only injectable preparations are, in general, mild and less marked than with combined oestrogen-progestagen formulations. Recent investigations have shown that the return of fertility following their use is delayed but in no way impaired. Monthly injectable oestrogen-progestagen combinations have been tested to a more limited extent and these agents are available only in a very few countries. Their main advantage over progestagen-only preparations is that they allow a reasonable menstrual bleeding pattern in the majority of cases. Their obvious disadvantage is that they contain a long acting oestrogen.
长效注射用激素避孕药是已研发出的最有效的生育调节药物之一;然而,由于动物实验数据表明在多个物种中可能存在致癌潜力,它们也是最具争议的药物之一。对这些动物实验结果的批判性分析表明,在所有情况下,都存在人类不会出现的特定机制。因此,大多数审查过此问题的国家和国际科学机构都得出结论,没有毒理学理由不使用长效激素避孕药。长效制剂可分为两类:一类作用持续时间为一个月,由长效雌激素和孕激素组成;另一类持续数月,仅由孕激素组成。在已测试的仅含孕激素的注射用避孕药中,到目前为止只有两种进入了国际市场:醋酸甲羟孕酮长效避孕针(DMPA),每3或6个月注射一次;庚酸炔诺酮,每隔2至3个月注射一次。使用这两种药物观察到的最重要的副作用是月经出血模式完全紊乱,在某些情况下会导致完全闭经,醋酸甲羟孕酮长效避孕针导致闭经的情况比庚酸炔诺酮更常见。然而,后者的作用持续时间较短,妊娠率比前者高。其他不良反应很少见且并不严重。一般来说,仅含孕激素的注射用制剂的代谢作用比雌激素 - 孕激素联合制剂轻微且不明显。最近的研究表明,使用这些药物后生育能力的恢复会延迟,但不会受到损害。每月注射一次的雌激素 - 孕激素联合制剂的测试范围较有限,这些药物仅在极少数国家有售。它们相对于仅含孕激素制剂的主要优点是,在大多数情况下能使月经出血模式较为正常。其明显的缺点是含有长效雌激素。