慢性高剂量口服后人体内硝酸异山梨酯及其代谢产物的血浆浓度。
Plasma concentrations of isosorbide dinitrate and its metabolites after chronic high oral dosage in man.
作者信息
Shane S J, Iazzetta J J, Chisholm A W, Berka J F, Leung D
出版信息
Br J Clin Pharmacol. 1978 Jul;6(1):37-41. doi: 10.1111/j.1365-2125.1978.tb01679.x.
Abstract
1 We have previously reported that vasodilator headache due to isosorbide dinitrate (ISDN) can be circumvented by using small 'priming' doses for an induction period of 1-2 weeks, after which it is possible to increase to dose rapidly to 360-720 mg, daily without recurrence of headache and without toxicity. The present study corroborates this earlier finding. 2. Chronic oral administration of doses of ISDN of this order of magnitude results in prolonged high plasma concentrations of the parent compound, as well as higher levels of the metabolites 2-ISMN and 5-ISMN. 3. It is our thesis that chronic high oral dosage of ISDN saturates the intrahepatic biotransformation process, and allows high concentrations of ISDN and its metabolites to enter the systemic circulation.
摘要
- 我们之前曾报道，通过在1 - 2周的诱导期使用小剂量“起始”剂量的硝酸异山梨酯（ISDN），可以避免因ISDN引起的血管舒张性头痛，之后可以迅速将剂量增加至每日360 - 720毫克，而不会再次出现头痛且无毒性。本研究证实了这一早期发现。2. 长期口服这种数量级剂量的ISDN会导致母体化合物的血浆浓度长时间维持在较高水平，同时代谢物2 - ISMN和5 - ISMN的水平也会升高。3. 我们的论点是，长期高剂量口服ISDN会使肝内生物转化过程饱和，并使高浓度的ISDN及其代谢物进入体循环。
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