METHYLENE-BLUE - EFFECTS AND DISPOSITION IN SHEEP
METHYLENE-BLUE - EFFECTS AND DISPOSITION IN SHEEP
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DOI：
10.1111/j.1365-2885.1984.tb00904.x
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发表时间：
1984-01-01
影响因子：
1.3
通讯作者：
BURROWS, GE
中科院分区：
文献类型：
--
作者：
BURROWS, GE
以15 mg/kg的剂量对成年母羊静脉注射美蓝后，测定了美蓝在绵羊体内的分布和尿药代动力学。在单独给予亚甲蓝或随后给予50 mg/kg亚硝酸钠之间进行比较。总消除速率常数（β）亚甲基蓝，0.0076 ±。0.0016/min，不受预先给予亚硝酸钠的影响。亚硝酸钠显著改变了分布速率。尽管亚甲基蓝的半衰期相对较短，但无论是完整的还是作为无色亚甲基蓝从尿液中消除的亚甲基蓝都非常少。使用LD 50测定、高铁血红蛋白生成和血液学效应作为评价参数进行毒理学评估。剂量高达50 mg/kg时，高铁血红蛋白的产生最小，在总剂量为30 mg/kg的亚甲蓝给药后4周内未观察到显著的血液学变化。静脉注射3%亚甲蓝溶液的24 h LD 50为42.3 mg/kg，95%置信区间限值为37.3 - 47.9 mg/kg。根据情况，在治疗重度高铁血红蛋白血症时，亚甲蓝的剂量可安全地增加至至少15 mg/kg。
The disposition and urinary excretion pharmacokinetics of methylene blue were determined after its i.v. administration at 15 mg/kg to mature female sheep. Comparisons were made between methylene blue administered alone or subsequent to 50 mg/kg sodium nitrite. The overall elimination rate constant (.beta.) of methylene blue, 0.0076 .+-. 0.0016/min, was not influenced by prior administration of sodium nitrite. The distribution rate was significantly altered by sodium nitrite. Very little of the methylene blue was eliminated in the urine either intact or as leucomethylene blue in spite of its relatively short half life. Toxicologic assessment was carried out using LD50 determination, methemoglobin production and hematologic effects as evaluation parameters. Methemoglobin production was minimal with doses as high as 50 mg/kg and no significant hematologic changes were seen up to 4 wk after a total dose of 30 mg/kg methylene blue. The 24 h LD50 for i.v. methylene blue administered as a 3% solution was 42.3 mg/kg with 95% confidence interval limits of 37.3 to 47.9 mg/kg. As conditions may warrant, the dosage of methylene blue may be safely increased up to at least 15 mg/kg in therapy of severe methemoglobinemias.