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血液和尿液中硫利达嗪的测定。

Measurement of thioridazine in blood and urine.

作者信息

Ng C H, Crammer J L

出版信息

Br J Clin Pharmacol. 1977 Apr;4(2):173-83. doi: 10.1111/j.1365-2125.1977.tb00691.x.

Abstract

1 Thioridazine can be specifically, simply, and reliably measured in plasma and urine by gas chromatography using hexane extraction and prochlorperazine as internal standard; fluorimetry is non-specific. 2 The method can also measure thioridazine ring sulphoxide, and mesoridazine-plus-sulphoridazine (M/S). 3 After single doses plasma sometimes shows M/S in addition to thioridazine itself; it always does so on continued treatment. There is great individual variation in both components, and evidence of changes in metabolism during the early weeks. 4 Urinary excretion may be influenced by pH, but between pH 6.0-7.0 about 1% of the daily dose appears in 24 h urine as the following: free thioridazine in microng quantities, M/S and ring sulphoxide each in mg amounts. 5 Patients attain steady state conditions, although plasma levels rise considerably after each dose and settle again in about 10 h. After chronic treatment is stopped to half-life is at about 30 h. 6 Plasma levels cannot be related to therapeutic response when this is slow, as in schizophrenia, but interpretations are complicated by the production of clinically active metabolites, and by plasma protein binding.

摘要
  1. 采用己烷萃取并用丙氯拉嗪作为内标,通过气相色谱法可在血浆和尿液中特异性、简单且可靠地测定硫利达嗪;荧光测定法是非特异性的。2. 该方法还可测定硫利达嗪环亚砜以及美索达嗪加硫利达嗪(M/S)。3. 单次给药后,血浆中除硫利达嗪本身外有时还会出现M/S;持续治疗时则总会出现。两种成分个体差异很大,且在最初几周有代谢变化的证据。4. 尿液排泄可能受pH值影响,但在pH 6.0至7.0之间,约1%的日剂量会在24小时尿液中以如下形式出现:微量的游离硫利达嗪、毫克量的M/S和环亚砜。5. 患者达到稳态,尽管每次给药后血浆水平会大幅上升并在约10小时后再次稳定。长期治疗停药后,半衰期约为30小时。6. 当治疗反应缓慢时,如在精神分裂症中,血浆水平与治疗反应无关,但由于临床活性代谢物的产生以及血浆蛋白结合,解释变得复杂。

相似文献

1
Measurement of thioridazine in blood and urine.血液和尿液中硫利达嗪的测定。
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本文引用的文献

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Theoretical changes in drug distribution resulting from changes in binding to plasma proteins and to tissues.
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Gas chromatographic identification of thioridazine in plasma, and a method for routine assay of the drug.
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