Chronic experimental diabetes accelerates urinary elimination of deprenyl and its metabolites.

Q2 Pharmacology, Toxicology and Pharmaceutics Open Medicinal Chemistry Journal Pub Date : 2008-01-10 DOI:10.2174/1874104500802010001
Ernest Adeghate, Péter Sótonyi, Huba Kalász
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Abstract

Many diabetic patients take several medications to treat diabetes-associated complications and other ailments. The mode of elimination of these drugs and their metabolites are poorly understood. The elimination of deprenyl, a MAO-B inhibitor, used for the treatment of the early stage of Parkinson's disease and senile dementia was investigated using thin layer chromatography.Male Wistar rats (180-200 g) were rendered diabetic by streptozotocin (STZ) treatment (60 mg/kg, i.v.). Rats having at least three times higher plasma glucose level than the normal were considered diabetic. Rats were treated with a single oral dose of 5 mg/kg (14)C-(methyl)-labeled (-)-deprenyl, 98 microCi/mg. Diabetic rats excreted the majority of urinary radioactivity in 8 hours, while control rats did it in 16 hours. The approximate ratio of major metabolites as determined using thin-layer chromatography did not change. In conclusion, diabetic rats excreted radiolabelled-deprenyl more rapidly compared to control animals. Increased elimination of deprenyl should be taken into account in the management of patients suffering from diabetes.

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慢性实验性糖尿病会加速去甲肾上腺素及其代谢物在尿液中的排出。
许多糖尿病患者服用多种药物来治疗糖尿病相关并发症和其他疾病。人们对这些药物及其代谢物的消除方式知之甚少。本研究使用薄层色谱法研究了用于治疗帕金森病早期和老年痴呆症的 MAO-B 抑制剂去甲肾上腺素的消除情况。大鼠的血浆葡萄糖水平至少比正常值高三倍,即为糖尿病大鼠。大鼠单次口服 5 mg/kg (14)C-(methyl)-labeled (-)-deprenyl (98 microCi/mg)。糖尿病大鼠在 8 小时内排出了尿液中的大部分放射性物质,而对照组大鼠则在 16 小时内排出了尿液中的大部分放射性物质。使用薄层色谱法测定的主要代谢物的大致比例没有变化。总之,与对照组动物相比,糖尿病大鼠排泄放射性标记的去甲肾上腺素的速度更快。在对糖尿病患者进行治疗时,应考虑到去甲肾上腺素排出量的增加。
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来源期刊
Open Medicinal Chemistry Journal
Open Medicinal Chemistry Journal Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.40
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0.00%
发文量
4
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