Kraus M, Breuel H P, Lücker P W, Fleck B
Arzneimittelforschung. 1982;32(5):537-42.
A new non-invasive clinical pharmacological model, developed at the Institut für Klinische Pharmakologie, Bobenheim (FR Germany), is reported. The principle of the model is the photographic determination of the diameter of the pupilla before and after administration of drugs active at the pupillar muscle. The area of the pupilla as a parameter of drug effect can be proceeded mathematically. With the reported model the area under the time curve, the pupillary index and the mean myotic or mydriatic time is determined. The area under the curve gives information about the extent of the drug effect. The pupillary index takes the maximum diameter into account and is even more sensitive than the area under the curve, correcting steep and flat profiles of the time curve. The mean mydriatic or myotic time gives a robust measurement concerning the duration of the drug effect. To prove the relevance of our model we used N,N-diethyl-N-(2-[alpha-(tricyclo(2.2.1.02.6)hept-3-ylidene)-benzyloxy]-ethyl)- amine hydrochloride (treptilamine hydrochloride, Asta S 5521) in four different dosages orally and intravenously. The results show: 1. The model is appropriate to show the effect of drugs on the smooth pupillary muscle concerning rate and extent. 2. The drug treptilamine hydrochloride does change the diameter of the pupils. 3. The drug is active after oral application.
据报道,德国博本海姆临床药理学研究所开发了一种新的非侵入性临床药理学模型。该模型的原理是通过拍照测定在瞳孔肌上起作用的药物给药前后瞳孔的直径。作为药物效应参数的瞳孔面积可以进行数学处理。利用所报道的模型,可以确定时间曲线下面积、瞳孔指数以及平均缩瞳或散瞳时间。曲线下面积提供了有关药物效应程度的信息。瞳孔指数考虑了最大直径,比曲线下面积更敏感,可校正时间曲线的陡峭和平缓轮廓。平均散瞳或缩瞳时间给出了关于药物效应持续时间的可靠测量值。为了证明我们模型的相关性,我们口服和静脉注射了四种不同剂量的N,N - 二乙基 - N - (2 - [α - (三环(2.2.1.02.6)庚 - 3 - 亚基) - 苄氧基] - 乙基) - 胺盐酸盐(盐酸曲替拉明,阿斯塔S 5521)。结果表明:1. 该模型适用于显示药物对瞳孔平滑肌的速率和程度方面的效应。2. 盐酸曲替拉明确实会改变瞳孔直径。3. 该药物口服后有活性。