Gonsalves S F, Gallager D W
Eur J Pharmacol. 1986 Feb 18;121(2):281-4. doi: 10.1016/0014-2999(86)90501-7.
Continuous release of diazepam from subcutaneously implanted silastic capsules provided significant protection against pentylenetetrazol seizures in rats for up to 3 weeks. However, the degree of protection seen after 3 weeks of exposure to diazepam was significantly less than after 1 h. These data suggest that continuous exposure to constant low levels of diazepam results in the development of partial tolerance which is not sufficient to eliminate significant anticonvulsant effects.
从皮下植入的硅橡胶胶囊中持续释放地西泮,能在长达3周的时间里为大鼠提供显著的抗戊四氮惊厥保护。然而,在接触地西泮3周后所观察到的保护程度明显低于接触1小时后的保护程度。这些数据表明,持续暴露于恒定低水平的地西泮会导致部分耐受性的产生,而这种耐受性不足以消除显著的抗惊厥作用。