Liu G Z, Lyle K C, Cao J
Peking Union Medical College Hospital, China.
Am J Obstet Gynecol. 1987 Oct;157(4 Pt 2):1079-81. doi: 10.1016/s0002-9378(87)80136-9.
In 1981 to 1983 we performed a clinical study with gossypol involving 152 participants, and in 1983 to 1985 we conducted another study of 120 participants. The first study was aimed at confirming gossypol's antifertility efficacy and determining the existence of side effects. The objective of the latter study was to find out whether the addition of a potassium salt supplement or a potassium-sparing agent could alleviate the side effect of hypokalemia. In both studies, the participants took a gossypol pill, 20 mg/day for 60 to 75 days for loading, and 50 mg/wk for maintenance. All participants were followed up for a year. The antifertility efficacy was found to be more than 90%, and the chief side effect was lowered serum potassium. In our 1983 to 1985 study, we concluded that since neither potassium supplementation nor triamterene solved the problem, it is very likely that gossypol is a nephrotoxic agent. With 1 year of gossypol treatment, serum testosterone and serum luteinizing hormone showed no change, whereas serum follicle-stimulating hormone showed some elevation after 6 months. The Shanghai researchers found that in their gossypol users, plasma and urinary beta 2-microglobulin levels were elevated to a certain extent. However, 25 subjects in our 1983 to 1985 study showed no appreciable change. Our volunteers had stopped taking gossypol for more than 1 year. In 1986 we started a third study, which was aimed at finding the lowest antifertility dose to minimize possible renal toxicity.
1981年至1983年，我们对152名受试者进行了一项关于棉酚的临床研究；1983年至1985年，我们又对120名受试者进行了另一项研究。第一项研究旨在证实棉酚的抗生育功效并确定是否存在副作用。后一项研究的目的是探究补充钾盐或保钾剂是否能减轻低钾血症的副作用。在两项研究中，受试者均服用棉酚片，负荷量为每日20毫克，持续60至75天，维持量为每周50毫克。所有受试者均接受了一年的随访。结果发现抗生育功效超过90%，主要副作用是血清钾降低。在我们1983年至1985年的研究中，我们得出结论，由于补钾和氨苯蝶啶均未能解决问题，棉酚很可能是一种肾毒性药物。经过一年的棉酚治疗，血清睾酮和血清黄体生成素未发生变化，而血清卵泡刺激素在6个月后有所升高。上海的研究人员发现，他们的棉酚使用者血浆和尿β2-微球蛋白水平有一定程度的升高。然而，在我们1983年至1985年的研究中，25名受试者未出现明显变化。我们的志愿者已停止服用棉酚超过一年。1986年，我们开始了第三项研究，旨在找到最低的抗生育剂量，以尽量减少可能的肾毒性。
