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[舌下硝酸甘油:长期使用长效硝酸甘油和硝酸甘油透皮贴剂治疗后的药代动力学变化]

[Sublingual nitroglycerin: the pharmacokinetic changes following long-term treatment with trinitrolong and nitroderm-TTS].

作者信息

Blagodatskikh S V, Piotrovskiĭ V K, Metelitsa V I, Martsevich S Iu, Riabokon' O S

出版信息

Farmakol Toksikol. 1991 Jul-Aug;54(4):62-6.

PMID:1786833
Abstract

The effect of the long-term use of prolonged medicinal forms containing nitroglycerin (NG)--trinitrolong and nitroderm-TTS on the pharmacokinetics of sublingual NG was studied. A significant change of the pharmacokinetic parameters at the sublingual use of NG both after the long-term treatment with trinitrolong and after therapy with nitroderm was observed: in both cases the time of half-release of NG from plasma and the average time of retention increased, the area under the curve of concentration-time significantly increased and the drug clearance decreased (for trinitrolong the difference in the clearance parameter is significant). While combining the data on both drugs the difference in the last two parameters also becomes significant. The observed slowing of elimination is probably the cause of the development of tolerance to NH at the long-term treatment, since according to the modern notions the degree of the effect is determined by the rate of NG metabolism.

摘要

研究了长期使用含硝酸甘油(NG)的长效剂型——长效硝酸甘油和硝酸甘油透皮贴剂对舌下含服NG药代动力学的影响。观察到在长期使用长效硝酸甘油治疗后以及使用硝酸甘油透皮贴剂治疗后,舌下含服NG时药代动力学参数发生了显著变化:在这两种情况下,NG从血浆中半衰期释放时间和平均保留时间均增加,浓度-时间曲线下面积显著增加,药物清除率降低(长效硝酸甘油清除参数差异显著)。综合两种药物的数据,后两个参数的差异也变得显著。观察到的消除减慢可能是长期治疗时对硝酸甘油产生耐受性的原因,因为根据现代观点,效应程度由NG代谢速率决定。

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