Фармакокинетика и Фармакодинамика (Mar 2016)
N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
Abstract
We studied the pharmacokinetic parameters of N-acetylcysteine at a single oral and intravenous administration of healthy volunteers. Elimination half-life (t1/2) within 2 hours and the maximum concentration in blood (Cmax) after 1 hour after administration was more than 10 times higher when intravenous on a comparison with oral administration. Effect of exchange rate on intravenous administration of N-acetylcysteine (1 200 mg/day for one week) the concentration of endogenous aminothiols in patients with diseases that are accompanied by oxidative stress (ischemic stroke and vascular complications of diabetes mellitus) are also studied. In ischemic stroke example it shows that the concentration of cysteine in plasma was increased by 1,6 times, and homocysteine levels did not change, as the ratio of reduced and oxidized cysteine (CysSH / CysSSCys). The content of total and free glutathione in red blood cells was not significantly changed, but significantly increased GSH / GSSG ratio, characterizing the antioxidant capacity of cells. We conclude that the inclusion in the scheme of N-acetylcysteine therapy of these diseases, accompanied by a more favorable clinical outcome due to a significant increase in antioxidant capacity of cells and tissues.
