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[单次或重复给药锂盐的药代动力学及一般药理作用]

[Pharmacokinetics and general pharmacological actions of lithium salts administered singly or repeatedly].

作者信息

Ozawa H, Nozu T, Aihara H, Akiyama F, Sasajima M

出版信息

Nihon Yakurigaku Zasshi. 1976 May;72(4):433-43.

PMID:987975
Abstract

Absorption, distribution and excretion after oral administration of lithium carbonate (Li2CO3) and/or lithium chloride (LiCl) were studied in Wistar rats and beagle dogs. The maximum level of concentration in the blood was seen within 4 hr after administration of Li2CO3, and a greater part of the orally dosed Li2CO3 was excreted into the urine. The blood and urine Li levels after the administration of LiCl were similar to those seen with Li2CO3. In dogs, Li2CO3 was more slowly excreted into the urine than it was in rats. Li was selectively incorporated into the thyroid and pituitary a short time after administration, and was not detected in any organ 7 days after cessation of repeated dosing for 19 days. The movement of Li into the brain was slow and relatively low levels were achieved after a single administration, but high and constant levels were shown after repeated administration. Effects of Li salts on behavior of ddy mice with repeated administration were investigated. The spontaneous motor activity was suppressed with Li2CO3 more strongly than with LiCl. The high dose of Li2CO3 suppressed not only the stimulating actions of methamphetamine and cocaine, but the ptotic and hypothermic action of reserpine. From these results, it is concluded that the repeated administration of Li salts reveals higher levels of Li ion in the brain than does a single administration, and also more responsive action on the central nervous system.

摘要

在Wistar大鼠和比格犬中研究了口服碳酸锂(Li2CO3)和/或氯化锂(LiCl)后的吸收、分布和排泄情况。口服Li2CO3后4小时内血液中出现最高浓度水平,且口服剂量的Li2CO3大部分经尿液排出。给予LiCl后血液和尿液中的锂水平与给予Li2CO3时相似。在犬中,Li2CO3经尿液排泄的速度比在大鼠中更慢。给药后短时间内锂被选择性地摄入甲状腺和垂体,在连续给药19天停止后7天,未在任何器官中检测到锂。锂进入大脑的速度较慢,单次给药后达到的水平相对较低,但重复给药后显示出高且稳定的水平。研究了锂盐重复给药对ddy小鼠行为的影响。Li2CO3比LiCl更强烈地抑制自发运动活动。高剂量的Li2CO3不仅抑制甲基苯丙胺和可卡因的兴奋作用,还抑制利血平的上睑下垂和体温过低作用。从这些结果得出结论,锂盐重复给药比单次给药在大脑中显示出更高水平的锂离子,并且对中枢神经系统的反应也更强。

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