Cocchiara G, Benedetti M S
Department of Pharmacokinetics and Metabolism, Farmitalia Carlo Erba, Erbamont Group, Milan, Italy.
Drug Metabol Drug Interact. 1992;10(3):199-211. doi: 10.1515/dmdi.1992.10.3.199.
After oral administration of [3H]cabergoline to man at a single nominal dose of 0.6 mg/subject radioactivity is mainly eliminated by the faecal route (72% of the dose after 10 days). Urine contains 18% of the dose after the same period. The unchanged drug and metabolites present in urine were identified by comparison with reference compounds and quantified by radio-TLC analysis. Cabergoline is extensively metabolized. Unchanged drug in 0-24 h urine represents less than 14% of urinary radioactivity, reaching 20% in 0-96 h urine. The acid derivative FCE 21589 is the main metabolite, amounting to 38% and 30% of the urinary radioactivity in 0-24 h and 0-96 h urine, respectively. The amide derivative FCE 21590 appears to be present in only a small amount, accounting for no more than 4% of the urinary radioactivity in the urine of the first 24 hours after administration and increasing to about 8% in the 0-96 h urine.
给人体口服单次标称剂量为0.6毫克/受试者的[3H]卡麦角林后，放射性主要通过粪便途径消除（10天后占剂量的72%）。同一时期尿液中含剂量的18%。通过与参考化合物比较鉴定尿液中未变化的药物和代谢物，并通过放射性薄层色谱分析进行定量。卡麦角林被广泛代谢。0 - 24小时尿液中未变化的药物占尿液放射性的比例不到14%，在0 - 96小时尿液中达到20%。酸性衍生物FCE 21589是主要代谢物，在0 - 24小时和0 - 96小时尿液中分别占尿液放射性的38%和30%。酰胺衍生物FCE 21590似乎仅少量存在，给药后最初24小时尿液中占尿液放射性不超过4%，在0 - 96小时尿液中增加到约8%。
