轻度镇痛药的生物分布。
Biodistribution of mild analgesics.
作者信息
Brune K, Rainsford K D, Schweitzer A
出版信息
Br J Clin Pharmacol. 1980 Oct;10 Suppl 2(Suppl 2):279S-284S. doi: 10.1111/j.1365-2125.1980.tb01810.x.
Abstract
1 Macro-autoradiographic methods were used to assess the biodistribution of [3H]-, or [14C]-acidic (aspirin, indomethacin, phenylbutazone) and non-acidic (antipyrine, aminopyrine, paracetamol) mild analgesics in rats with carrageenan-induced inflammation. 2 At anti-inflammatory doses all the acidic drugs (and/or their metabolites) were found to reach high concentrations in the stomach wall, liver, blood and bone marrow, kidney cortex and the inflamed tissue, that is, the tissues in which these drugs exert their therapeutic or side-effects. 3 In contrast, at analgesic doses, the non-acidic mild analgesics (and/or their metabolites) are equally distributed throughout the body with the exception of the gastro-intestinal lumen and the liver. This distribution pattern correlates well with the lack of acute side-effects and anti-inflammatory action of these drugs at therapeutic doses.
摘要
- 采用宏观放射自显影法评估了[3H]-或[14C]-酸性（阿司匹林、吲哚美辛、保泰松）和非酸性（安替比林、氨基比林、对乙酰氨基酚）轻度镇痛药在角叉菜胶诱导的炎症大鼠体内的生物分布。2. 在抗炎剂量下，所有酸性药物（和/或其代谢产物）在胃壁、肝脏、血液、骨髓、肾皮质和炎症组织中达到高浓度，即这些药物发挥治疗作用或副作用的组织。3. 相比之下，在镇痛剂量下，除胃肠道管腔和肝脏外，非酸性轻度镇痛药（和/或其代谢产物）在全身均匀分布。这种分布模式与这些药物在治疗剂量下缺乏急性副作用和抗炎作用密切相关。
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