[舌下硝酸甘油:长期使用三硝基龙和硝皮tts治疗后的药代动力学变化]。

Farmakologiia i toksikologiia Pub Date : 1991-07-01
S V Blagodatskikh, V K Piotrovskiĭ, V I Metelitsa, S Iu Martsevich, O S Riabokon'
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引用次数: 0

摘要

研究了长期使用含硝酸甘油(NG)-三硝基龙和硝酸甘油- tts的长效制剂对舌下NG药代动力学的影响。长期用三硝基龙治疗和用硝皮治疗后舌下使用NG的药代动力学参数发生了显著变化:两种情况下NG从血浆中半释放时间和平均滞留时间增加,浓度-时间曲线下面积显著增加,药物清除率降低(三硝基龙的清除率差异显著)。当结合两种药物的数据时,最后两个参数的差异也变得显著。观察到的消除速度减缓可能是长期治疗中对NH产生耐受性的原因,因为根据现代观念,影响的程度是由NG代谢率决定的。
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[Sublingual nitroglycerin: the pharmacokinetic changes following long-term treatment with trinitrolong and nitroderm-TTS].

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.

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