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过量服用时维拉帕米对映体浓度的监测。

Monitoring of verapamil enantiomers concentration in overdose.

作者信息

Wilimowska Jolanta, Piekoszewski Wojciech, Krzyanowska-Kierepka Ewa, Florek Ewa

机构信息

Department of Analytical Toxicology and Therapeutic Drug Monitoring, Collegium Medicum, Jagiellonian University, Krakow, Poland.

出版信息

Clin Toxicol (Phila). 2006;44(2):169-71. doi: 10.1080/15563650500514541.

DOI:10.1080/15563650500514541
PMID:16615674
Abstract

A 52-year-old woman with a history of depression and personality disorders, hypertension, coronary disease and asthma was admitted to the Department of Clinical Toxicology after taking 60 tablets of Staveran (immediate release verapamil), and 4 tablets of acetaminophen. One and a half hours after ingestion her condition was critical. She required endotracheal intubation and artificial respiration. Her heart rate was 75 beats per minute, (bpm) and her blood pressure dropped from 70/50 to 50/00 mmHg. Additionally, drowsiness and headache were observed. On admission, R-(+)- and S-(-)-verapamil serum concentrations were 2252 ng/ml and 810 ng/ ml, respectively. Monitoring of the verapamil serum concentration was carried out over 74 h. Terminal elimination half-lives were 18.7 (21.3) and 17.0 (18.5) hours, respectively, for R-(+)- and S-(-)-verapamil. Monitoring of verapamil enantiomers concentrations in serum indicated a higher concentration of the less active form and slightly faster elimination of the more active enantiomer. The data-support a stereoselective difference between first pass clearance and later systemic clearance of verapamil, when taken in overdose.

摘要

一名52岁女性,有抑郁症、人格障碍、高血压、冠心病和哮喘病史,在服用60片速释维拉帕米(Staveran)和4片对乙酰氨基酚后被收入临床毒理学部门。摄入药物一个半小时后,她的情况危急。她需要气管插管和人工呼吸。她的心率为每分钟75次,血压从70/50毫米汞柱降至50/00毫米汞柱。此外,还观察到嗜睡和头痛。入院时,R-(+)-维拉帕米和S-(-)-维拉帕米的血清浓度分别为2252纳克/毫升和810纳克/毫升。对维拉帕米血清浓度进行了74小时的监测。R-(+)-和S-(-)-维拉帕米的终末消除半衰期分别为18.7(21.3)小时和17.0(18.5)小时。对血清中维拉帕米对映体浓度的监测表明,活性较低的形式浓度较高,而活性较高的对映体消除略快。这些数据支持了过量服用维拉帕米时首过清除率和随后全身清除率之间的立体选择性差异。

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