Gustafsson L L, Post C, Edvardsen B, Ramsay C H
Anesthesiology. 1985 Nov;63(5):483-9. doi: 10.1097/00000542-198511000-00003.
Morphine and meperidine distribution in the neuroaxis were studied in rats after intrathecal injection through catheters ending at the lumbar level. 14C-Morphine and 3H-meperidine were injected with pharmacologic doses of each drug. Radioactivity was measured in spinal cord segments at different times. At 14 min the segment with maximum morphine concentration (T11-12) contained 8.6 +/- 2.4 (mean +/- SD) pmol/mg, a value 215 times higher than would be observed if distribution in the body were homogeneous. The ratio between concentration in the most rostral segment (C3-4) and in the segment with maximal concentration was 0.21 +/- 0.10. At 14 min the segment with maximum meperidine concentration (T9-10) contained 161.4 +/- 33.9 pmol/mg wet tissue, a value 75 times higher than would be seen with even distribution in the body. The ratio (C3-4 vs. T9-10) was 0.10 +/- 0.04 at this time. The distribution of 14C-morphine in the whole central nervous system (CNS) was studied in mice by whole body autoradiography after intrathecal injections of 5 microliters at the L5-6 level. High levels of radioactivity were detected in the whole spinal cord and in brain regions close to the basal cisterns until 2 h after injection. At 4 h only the caudal part of the spinal cord had detectable levels of radioactivity. The per cent of the injected dose of morphine that was recovered from the spinal cord was 26.5 +/- 4.5 at 14 min, 19.9 +/- 8.8 at 44 min, and 4.5 +/- 1.7 at 179 min after injection.(ABSTRACT TRUNCATED AT 250 WORDS)
通过末端位于腰段的导管向大鼠鞘内注射后,研究了吗啡和哌替啶在神经轴中的分布情况。分别以药理剂量注射了¹⁴C - 吗啡和³H - 哌替啶。在不同时间测量脊髓节段中的放射性。在14分钟时,吗啡浓度最高的节段(T11 - 12)含有8.6±2.4(平均值±标准差)pmol/mg,该值比假设药物在体内均匀分布时所观察到的值高215倍。最靠前节段(C3 - 4)与浓度最高节段之间的比值为0.21±0.10。在14分钟时,哌替啶浓度最高的节段(T9 - 10)含有161.4±33.9 pmol/mg湿组织,该值比药物在体内均匀分布时所观察到的值高75倍。此时(C3 - 4与T9 - 10的)比值为0.10±0.04。通过在L5 - 6水平鞘内注射5微升后进行全身放射自显影,研究了¹⁴C - 吗啡在小鼠整个中枢神经系统(CNS)中的分布。注射后2小时内,在整个脊髓以及靠近脑基底池的脑区检测到高水平放射性。在4小时时,仅脊髓尾部有可检测到的放射性水平。注射后14分钟从脊髓回收的吗啡注射剂量百分比为26.5±4.5,44分钟时为19.9±8.8,179分钟时为4.5±1.7。(摘要截断于250字)