Kanto J, Klotz U
Department of Anaesthesiology, Turku University, Finland.
Acta Anaesthesiol Scand. 1988 Feb;32(2):69-78. doi: 10.1111/j.1399-6576.1988.tb02691.x.
Several specific and sensitive new methods for determining atropine and its metabolites in biological fluids have increased the possibility to characterise the pharmacokinetic properties of this antimuscarinic agent. Following i.v. injection, atropine disappears very quickly from the circulation, resembling its fast onset of action. Age, but not sex, appears to have a clear effect on its kinetics, explaining at least partly the higher sensitivity of very young and very old patients to this anticholinergic agent. Following i.m. or oral atropine administration, typical anticholinergic effects coincide quite well with the absorption rate of the drug, indicating that the premedication should be given about 1 and 2 h before induction of anaesthesia. A sufficient absorption after rectal administration offers an alternative treatment, especially in children. Differing from its placental transfer, atropine has a delayed and incomplete lumbar cerebrospinal fluid penetration, indicating a fundamental difference between these two biological membranes. Oropharyngeally administered atropine has a very variable absorption, but inhaled or intratracheally given drug has produced interesting new results, e.g. pulmonary atropine administration appears to have clinical significance in special situations, such as cardiac arrest and organophosphate poisoning (military personnel). Depending on the method used, different data on the metabolism and excretion for atropine have been reported and therefore further studies are needed in this respect. The pharmacokinetics of scopolamine and glycopyrrolate and their relation to clinical response are poorly understood.
几种用于测定生物体液中阿托品及其代谢物的特异性强且灵敏的新方法，增加了表征这种抗毒蕈碱药物药代动力学特性的可能性。静脉注射后，阿托品从循环中消失得非常快，这与其起效迅速相一致。年龄而非性别似乎对其动力学有明显影响，这至少部分解释了非常年幼和非常年老的患者对这种抗胆碱能药物更高的敏感性。肌内或口服阿托品给药后，典型的抗胆碱能作用与药物的吸收速率相当吻合，这表明术前用药应在麻醉诱导前约1小时和2小时给予。直肠给药后有足够的吸收，这提供了一种替代治疗方法，尤其适用于儿童。与胎盘转运不同，阿托品在腰椎脑脊液中的渗透延迟且不完全，这表明这两种生物膜之间存在根本差异。经口咽给药的阿托品吸收情况差异很大，但吸入或气管内给药产生了有趣的新结果，例如肺内给予阿托品在特殊情况下似乎具有临床意义，如心脏骤停和有机磷中毒（军事人员）。根据所使用的方法，已报道了关于阿托品代谢和排泄的不同数据，因此在这方面还需要进一步研究。东莨菪碱和格隆溴铵的药代动力学及其与临床反应的关系尚不清楚。
