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拉贝洛尔(Labetalol)用于治疗高血压和冠心病。它是四个对映异构体的外消旋物。这四个对映异构体中有两个无药理作用,其余两个分别有阻断α受体和β受体的活性;均在肝脏代谢。使用拉贝洛尔使肝酶值可逆性增加。 1985～1989年间,美国报道11例用拉贝洛尔致严重肝损害,其中3人死亡,5人严重肝硬化。85%病人为女性。剂量在推荐范围内。用药后3周至6个月(平均60天)出现综合征。虽然变态反应的临床综合征(发烧、嗜曙红细胞增多、皮肤发红)没有发现或极其轻微,但不排除存在免疫机理。也有认
Labetalol is used to treat high blood pressure and coronary heart disease. It is a racemate of the four enantiomers. Two of these four enantiomers have no pharmacological effect, and the remaining two have the activity of blocking both the alpha receptor and the beta receptor; both are metabolized in the liver. The use of labetalol reversibly increases hepatic enzyme activity. Between 1985 and 1989, the United States reported 11 cases of serious liver damage caused by labetalol, 3 of which were killed and 5 of whom had severe cirrhosis. 85% of patients are women. The dosage is within the recommended range. Syndromes occurred 3 weeks to 6 months after treatment (average 60 days). Although clinical syndromes of allergy (fever, eosinophilia, redness of the skin) are not found or are extremely mild, the immune mechanism is not ruled out. There are also recognized