N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols

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 intraven...

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Main Authors: A. A. Dutov, D. A. Nikitin, J. L. Lukianova, N. A. Shemyakina, A. V. Ermolina, M. N. Mishchenko
Format: Article
Language:Russian
Published: LLC “Publisher OKI” 2016-03-01
Series:Фармакокинетика и Фармакодинамика
Subjects:
Online Access:https://www.pharmacokinetica.ru/jour/article/view/170
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author A. A. Dutov
D. A. Nikitin
J. L. Lukianova
N. A. Shemyakina
A. V. Ermolina
M. N. Mishchenko
author_facet A. A. Dutov
D. A. Nikitin
J. L. Lukianova
N. A. Shemyakina
A. V. Ermolina
M. N. Mishchenko
author_sort A. A. Dutov
collection DOAJ
description 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.
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institution Kabale University
issn 2587-7836
2686-8830
language Russian
publishDate 2016-03-01
publisher LLC “Publisher OKI”
record_format Article
series Фармакокинетика и Фармакодинамика
spelling doaj-art-ba0f4e98394f4cbeabe2d42bc8076db02025-08-20T03:57:48ZrusLLC “Publisher OKI”Фармакокинетика и Фармакодинамика2587-78362686-88302016-03-01022630169N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiolsA. A. Dutov0D. A. Nikitin1J. L. Lukianova2N. A. Shemyakina3A. V. Ermolina4M. N. Mishchenko5FSEI HE State Medical AcademySEI HPE Zabaikalsky State UniversitySII City Clinical Hospital № 1FSEI HE State Medical AcademyPHI Road Clinical Hospital. Chita-2, «Russian Railways»FSEI HE State Medical AcademyWe 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.https://www.pharmacokinetica.ru/jour/article/view/170n-ацетилцистеинфармакокинетикацистеинглутатионоксидативный стрессишемический инсультосложнения сахарного диабетаn-acetylcysteinepharmacokineticscysteineglutathioneoxidative stressischemic strokediabetes complications
spellingShingle A. A. Dutov
D. A. Nikitin
J. L. Lukianova
N. A. Shemyakina
A. V. Ermolina
M. N. Mishchenko
N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
Фармакокинетика и Фармакодинамика
n-ацетилцистеин
фармакокинетика
цистеин
глутатион
оксидативный стресс
ишемический инсульт
осложнения сахарного диабета
n-acetylcysteine
pharmacokinetics
cysteine
glutathione
oxidative stress
ischemic stroke
diabetes complications
title N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
title_full N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
title_fullStr N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
title_full_unstemmed N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
title_short N-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
title_sort n acetylcysteine pharmacokinetic parameters and the effect on the concentration of endogenous aminothiols
topic n-ацетилцистеин
фармакокинетика
цистеин
глутатион
оксидативный стресс
ишемический инсульт
осложнения сахарного диабета
n-acetylcysteine
pharmacokinetics
cysteine
glutathione
oxidative stress
ischemic stroke
diabetes complications
url https://www.pharmacokinetica.ru/jour/article/view/170
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AT jllukianova nacetylcysteinepharmacokineticparametersandtheeffectontheconcentrationofendogenousaminothiols
AT nashemyakina nacetylcysteinepharmacokineticparametersandtheeffectontheconcentrationofendogenousaminothiols
AT avermolina nacetylcysteinepharmacokineticparametersandtheeffectontheconcentrationofendogenousaminothiols
AT mnmishchenko nacetylcysteinepharmacokineticparametersandtheeffectontheconcentrationofendogenousaminothiols