phkineticaФармакокинетика и ФармакодинамикаPharmacokinetics and Pharmacodynamics2587-78362686-8830ООО «Издательство ОКИ»phkinetica-170Research ArticleИССЛЕДОВАНИЯ ФАРМАКОКИНЕТИКИPHARMACOKINETICS STUDIESN-ацетилцистеин: фармакокинетические параметры и влияние на концентрацию эндогенных аминотиоловN-acetylcysteine: pharmacokinetic parameters and the effect on the concentration of endogenous aminothiolsДутовА. А.DutovA. A.dutovaa@yandex.ruНикитинД. А.NikitinD. A.noemail@neicon.ruЛукьяноваЮ. Л.LukianovaJ. L.noemail@neicon.ruШемякинаН. А.ShemyakinaN. A.noemail@neicon.ruЕрмолинаА. В.ErmolinaA. V.noemail@neicon.ruМищенкоМ. Н.MishchenkoM. N.noemail@neicon.ruФГБОУ ВО Читинская государственная медицинская академияРоссияFSEI HE State Medical AcademyRussian FederationФГБОУ ВПО Забайкальский государственный университетРоссияSEI HPE Zabaikalsky State UniversityRussian FederationГУЗ Городская клиническая больница № 1РоссияSII City Clinical Hospital № 1Russian FederationНУЗ «Дорожная клиническая больница на ст. Чита-2 ОАО «РЖД»РоссияPHI Road Clinical Hospital. Chita-2, «Russian Railways»Russian Federation201609032016022630Copyright © Дутов А.А., Никитин Д.А., Лукьянова Ю.Л., Шемякина Н.А., Ермолина А.В., Мищенко М.Н., 20162016Дутов А.А., Никитин Д.А., Лукьянова Ю.Л., Шемякина Н.А., Ермолина А.В., Мищенко М.Н.Dutov A.A., Nikitin D.A., Lukianova J.L., Shemyakina N.A., Ermolina A.V., Mishchenko M.N.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.pharmacokinetica.ru/jour/article/view/170

Исследовали фармакокинетические параметры N-ацетилцистеина при однократном пероральном и в/в введении у здоровых добровольцев. Период полувыведения (t1/2) в пределах 2 ч, максимальная концентрация в крови (Cmax) через 1 ч после введения была более чем в 10 раз выше при в/в введении по сравнению с пероральным. Также изучено влияние курсового в/в введения N-ацетилцистеина (1 200 мг/сут в течение одной недели) на концентрацию эндогенных аминотиолов у пациентов с заболеваниями, сопровождающимися оксидативным стрессом (ишемический инсульт и сосудистые осложнения сахарного диабета). На примере ишемического инсульта показано, что концентрация цистеина в плазме возрастала в 1,6 раза, а уровень гомоцистеина не менялся, как и соотношение восстановленного и окисленного цистеина (CysSH/CysSSCys). Содержание общего и свободного глутатиона в эритроцитах достоверно не менялось, зато значительно возрастал коэффициент GSH/GSSG, характеризующий антиоксидантный потенциал клеток. Таким образом, включение в схемы терапии N-ацетилцистеина указанных заболеваний сопровождается более благоприятным клиническим исходом за счёт значительного увеличения антиоксидантного потенциала клеток и тканей.

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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The authors declare that there are no conflicts of interest present.