Packard C J, Shepherd J
Institute of Biochemistry, Royal Infirmary, Glasgow, UK.
Acta Obstet Gynecol Scand Suppl. 1994;159:35-40.
Danazol, a weakly androgenic, heterocyclic compound with anabolic properties, is used primarily in the treatment of endometriosis and other gynecological complaints. Early reports indicated that the drug had little effect on plasma lipid (cholesterol and triglyceride) levels but recently concern has been expressed over more subtle changes reported in plasma lipid and lipoprotein metabolism after danazol treatment. Therapy produces a rapid reduction in high density lipoprotein (HDL) cholesterol (particularly in the putatively cardioprotective HDL2 subfraction) coupled with a rise in the pro-atherogenic low density lipoprotein (LDL). These apparently unwanted actions are balanced against a possibly beneficial reduction in the atherogenic lipoprotein(a) fraction. The mechanism of these changes induced by danazol is unknown but probably relates to effects on hepatic lipase, LDL receptor and lecithin cholesterol acyl transferase activity. While it is prudent to recognize the potential detriment that may follow these perturbations, concern is only warranted where therapy is prolonged (> 12 months) or given to subjects with a high background risk of ischemic heart disease.
达那唑是一种具有合成代谢特性的弱雄激素性杂环化合物，主要用于治疗子宫内膜异位症和其他妇科疾病。早期报告表明该药物对血浆脂质（胆固醇和甘油三酯）水平影响不大，但最近人们对达那唑治疗后血浆脂质和脂蛋白代谢中报告的更细微变化表示关注。治疗会使高密度脂蛋白（HDL）胆固醇迅速降低（特别是在假定具有心脏保护作用的HDL2亚组分中），同时促动脉粥样硬化的低密度脂蛋白（LDL）升高。这些明显不良的作用与动脉粥样硬化性脂蛋白（a）组分可能的有益降低相平衡。达那唑引起这些变化的机制尚不清楚，但可能与对肝脂肪酶、LDL受体和卵磷脂胆固醇酰基转移酶活性的影响有关。虽然认识到这些干扰可能带来的潜在危害是谨慎的，但只有在治疗时间延长（>12个月）或给予有缺血性心脏病高背景风险的受试者时才需要关注。
