Bruguerolle B, Prat M
Medical Pharmacology Laboratory, Faculty of Medicine, Marseille, France.
Chronobiol Int. 1992 Dec;9(6):448-52. doi: 10.3109/07420529209064558.
The aim of this study was to investigate the possible influence of the time of administration on bupivacaine (B), etidocaine (E), and mepivacaine (M) protein and tissue (brain and heart) binding. For each anesthetic agent, a single dose of B (20 mg/kg), E (40 mg/kg), or M (60 mg/kg) was administered intraperitoneally at 10:00, 16:00, 22:00, and 04:00 h. Blood and tissue samples were collected 15 min after drug administration. This study documents significant circadian variations in protein and tissue binding of the three local anesthetic agents. We did not demonstrate a temporal relationship between the respective free and tissue levels. Thus, the temporal variations of free plasma, brain, and heart levels do not seem to be involved in the temporal changes of induced mortality.
本研究的目的是调查给药时间对布比卡因（B）、依替卡因（E）和甲哌卡因（M）蛋白质及组织（脑和心脏）结合的可能影响。对于每种麻醉剂，在10:00、16:00、22:00和04:00时腹腔注射单剂量的B（20mg/kg）、E（40mg/kg）或M（60mg/kg）。给药后15分钟采集血液和组织样本。本研究记录了三种局部麻醉剂蛋白质及组织结合的显著昼夜变化。我们未证明各自游离水平与组织水平之间存在时间关系。因此，游离血浆、脑和心脏水平的时间变化似乎与诱导死亡率的时间变化无关。
