References

diaendo

Сахарный диабет

Diabetes mellitus

2072-03512072-0378

Endocrinology research centre

10.14341/2072-0351-6230

diaendo-6230

Research Article

Статьи

Articles

Глибенкламид - профиль эффективности и безопасности

Glibenclamide - profile of efficacy and safety

Недосугова

Людмила Викторовна

Nedosugova

Lyudmila Viktorovna

profmila@rambler.ru

ГОУ ВПО Первый Московский государственный медицинский университет им. И.М. Сеченова, МоскваI.M.Sechenov First Moscow State Medical University, Moscow

2011

15092011

143

№3 (2011)

8590

2011

Недосугова Л.В.

Nedosugova L.V.

Данная работа распространяется под лицензией Creative Commons Attribution 4.0.

This work is licensed under a Creative Commons Attribution 4.0 License.

https://www.dia-endojournals.ru/jour/article/view/6230

В арсенале пероральных сахароснижающих препаратов глибенкламид сохраняет лидирующие позиции как наиболее эффективноепо своей гипогликемизирующей активности средство. Эффективность препарата обусловлена его уникальной химической структу-рой, содержащей не только сульфонилмочевинное кольцо, но и бензамидную группировку в боковой цепи, что обеспечивает максимальноесродство к SUR 1 на ?-клетке и возможность связывания с SUR 2А на клетках периферических тканей, таких как кардиомиоциты, гладкомышечные клетки сосудистой стенки и адипоциты. Вместе с тем данная особенность может повышать риск гипогликемическихсостояний и оказывать негативный эффект на сердечно-сосудистую систему. Рассматриваются данные клинических исследований, доказывающих эффективность и безопасность препарата, получившего в 2010 году Премию Лекарственных Средств Г.Г. Крейтцфельдта,на основе доказательной базы долгосрочных наблюдений, продемонстрировавших снижение риска сосудистых осложнений сахарногодиабета, возможность легко комбинироваться с препаратами других групп, назначения пожилым и мультиморбидным пациентам. Глибенкламид - единственный из препаратов сульфонилмочевины внесен в список Жизненно Важных Лекарственных Средств ВсемирнойОрганизации Здравоохранения.

Glibenclemide is the most effective drug among oral hypoglycemic ones. The efficacy of this drug is determined by its unique chemical structure thatcontains sulfonylurea, not only ring, but also benzamid group in the side chain. This provides the maximum affinity for SUR 1 on the betbeta-cell ATP-dependentK+ channels and ability to associate with SUR 2A cells in the peripheral tissues such as cardiomyocytes, smooth muscle cells of the vascular walland adipocytes. However, this feature can increase the risk of hypoglycemic states and have a negative effect on the cardiovascular system. We considerdata from clinical studies proving the efficacy and safety of the drug, which were based on evidence of long-term observations, and which demonstratedreduced risk of vascular complications of diabetes, compatibility with drugs of other groups, and possibility to use in elderand multimorbid patients. Glibenclamidewas evaluated by prestigious H.G. Creutzfeldt Drug Prize in 2010. It is the only SCI listed essential medicine of the World Health Organization.

терапия сахарного диабета 2 типасекреция инсулинарецептор сульфонилмочевины - SURАТФ зависимые К+-каналыишемическое прекондиционированиегипогликемические состояния

type 2 diabetes treatmentinsulin secretionsulfonylurea receptor - SURK + ATP channelsischemic preconditioninghypoglycemia

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