Laurikainen E, Koulu M, Kaila T, Scheinin M, Isalo E
Dept. of Otorhinolaryngology, Turku University Hospital, Finland.
Rhinology. 1988 Jun;26(2):133-8.
Plasma concentrations of nasally inhaled ipratropium bromide were analyzed in eight healthy volunteers by using a sensitive radioreceptor assay (RRA). The rate of saliva secretion, heart rate and changes in visual accommodation were quantitated in order to measure possible systemic anticholinergic drug effects. 240 micrograms of ipratropium bromide (40 micrograms each nostril, repeated twice at 15 min intervals) were inhaled nasally in a double blind, randomized, placebo-controlled experiment. Ipratropium bromide absorbed fast, and peak plasma concentrations of the drug (257 +/- 55 pg/ml) were detected as soon as 5 min after the last inhalation (at 35 min from the beginning). The plasma levels of ipratropium bromide decreased rapidly, being only 86 +/- 7 pg/ml one hour after the last inhalation. These low concentrations of ipratropium bromide indicate that only a small portion of it absorbs after nasal application, which is consistent with the lack of any systemic anticholinergic drug effects in our subjects. It is concluded that nasally applied ipratropium bromide is not likely to cause systemic anticholinergic side-effects, even in doses exceeding the therapeutic recommendations.
采用灵敏的放射受体分析法（RRA）对8名健康志愿者吸入鼻用异丙托溴铵后的血浆浓度进行了分析。为了测定可能的全身抗胆碱能药物效应，对唾液分泌速率、心率及视觉调节变化进行了定量分析。在一项双盲、随机、安慰剂对照实验中，志愿者经鼻吸入240微克异丙托溴铵（每侧鼻孔40微克，每隔15分钟重复一次，共两次）。异丙托溴铵吸收迅速，在最后一次吸入后5分钟（即从开始起35分钟）就检测到该药物的血浆浓度峰值（257±55皮克/毫升）。异丙托溴铵的血浆水平迅速下降，最后一次吸入1小时后仅为86±7皮克/毫升。这些低浓度的异丙托溴铵表明，经鼻给药后只有一小部分被吸收，这与我们研究对象中未出现任何全身抗胆碱能药物效应是一致的。得出的结论是，即使经鼻应用的异丙托溴铵剂量超过治疗推荐剂量，也不太可能引起全身抗胆碱能副作用。
