Pyykkö I, Padoan S, Schalén L, Lyttkens L, Magnusson M, Henriksson N G
Aviat Space Environ Med. 1985 Aug;56(8):777-82.
The effects of TTS-scopolamine, dimenhydrinate, lidocaine, and tocainide on motion sickness and vertigo and on caloric and postrotatory nystagmus were evaluated in healthy volunteers. TTS-scopolamine was administered transdermally (delivering approximately 10 micrograms X h-1 scopolamine base) and 100 mg dimenhydrinate orally. Lidocaine and tocainide were administered intravenously (average plasma concentration of lidocaine 6 mol X L-1 and of tocainide 20 mol X L-1). TTS-scopolamine and dimenhydrinate significantly reduced vertigo induced by calorization of the ears, nausea provoked with Coriolis maneuvre, and nystagmus in caloric and rotatory tests. During treatment with lidocaine and tocainide no alleviation of vertigo and nausea was observed. Caloric nystagmus was reduced but rotation induced nystagmus was virtually unchanged. Presumably the motion sickness drugs act at the brain stem where TTS-scopolamine and dimenhydrinate have their target cells in the vestibular nuclei. Furthermore, the alleviation of motion sickness was linked to a decline of nystagmus. Lidocaine and tocainide, the action of which in vertigo and nausea in patients is proposed to be on the vestibular end organs and the supratentorial brain structures, consistently failed to alleviate motion sickness.
在健康志愿者中评估了经皮给药的东莨菪碱、茶苯海明、利多卡因和妥卡尼对晕动病和眩晕以及对冷热试验和转椅试验后眼震的影响。经皮给予东莨菪碱(输送约10微克/小时的东莨菪碱碱),口服100毫克茶苯海明。静脉注射利多卡因和妥卡尼(利多卡因平均血浆浓度为6微摩尔/升,妥卡尼为20微摩尔/升)。经皮给药的东莨菪碱和茶苯海明显著减轻了耳部冷热试验诱发的眩晕、科里奥利试验诱发的恶心以及冷热试验和转椅试验中的眼震。在利多卡因和妥卡尼治疗期间,未观察到眩晕和恶心减轻。冷热试验眼震减轻,但转椅试验诱发的眼震基本未变。推测晕动病药物作用于脑干,经皮给药的东莨菪碱和茶苯海明在前庭核中有其靶细胞。此外,晕动病的减轻与眼震减弱有关。利多卡因和妥卡尼在患者眩晕和恶心方面的作用被认为是在前庭终器和幕上脑结构,但始终未能减轻晕动病。