Forsman A, Larsson M, Lundborg H, Renstrom P
Eur J Drug Metab Pharmacokinet. 1981;6(4):249-53. doi: 10.1007/BF03189521.
A single oral dose of haloperidol was given to 19 patients prior to cholecystectomy. The concentration of haloperidol was assessed in serum, urine, fatty tissue, liver tissue, choledochal bile and bile bladder contents. The biological half-life of the drug in the serum was 25.1 +/- 12.9 hours, which is comparable to that in healthy volunteers. Only minute amounts of the drug were excreted with the urine. The drug concentration was only slightly elevated in choledochal bile but in the bile bladder contents it was about 11 times higher than that in the serum. The low concentration of haloperidol in the bile indicated that there was no substantial enterohepatic recirculation of the drug in this patient material. The concentration of haloperidol in fatty tissue was about 20 times, and in liver tissue 900 times higher than that in the serum. The corresponding figures for intramuscular administration of haloperidol were 10 and 325, respectively. A possible relationship between the side-effects and the route of administration is discussed.
在胆囊切除术之前,给19名患者单次口服了氟哌啶醇。对血清、尿液、脂肪组织、肝脏组织、胆总管胆汁和胆囊内容物中的氟哌啶醇浓度进行了评估。该药物在血清中的生物半衰期为25.1±12.9小时,这与健康志愿者中的情况相当。只有极少量的药物随尿液排出。胆总管胆汁中的药物浓度仅略有升高,但胆囊内容物中的药物浓度约为血清中的11倍。胆汁中氟哌啶醇浓度较低表明,在该患者群体中该药物没有大量的肝肠循环。脂肪组织中氟哌啶醇的浓度约为血清中的20倍,肝脏组织中则为血清中的900倍。氟哌啶醇肌肉注射时的相应倍数分别为10倍和325倍。文中讨论了副作用与给药途径之间可能存在的关系。