Angiotensin Ii Receptor Antagonists in the Treatment of Hypertension: Perspectives for Clinical Use

Потешкина, Н Г; Селиванова, Г. Б.; Жалсараев, Тимур Жаргалович

doi:10.18705/1607-419x-2013-19-2-117-124

Cited by 2 publications

(2 citation statements)

References 10 publications

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“…Заболевания сердечно-сосудистой системы являются одной из важнейших медико-социальных проблем в Российской Федерации. Смертность взрослого трудоспособного населения от инфаркта миокарда и нарушений мозгового кровообращения составляет около 40% в структуре всех причин смертности [1]. Одним из главных факторов риска этих заболеваний является артериальная гипертензия.…”

Section: оригинальные статьи / Original Articlesunclassified

“…Приведенные данные демонстрируют, что из группы АРА II чаще разрабатываются воспроизведенные препараты лозартана. При этом для лозартана характерен эффект первичного прохождения через печень, и лозартан метаболизируется с образованием активного карбоксильного метаболита ЕХР-3174, обладающего более выраженной антигипертензивной активностью (в 10-40 раз) 1 . Согласно данным литературы, лекарственные средства с пресистемным метаболизмом часто демонстрируют высокую внутрииндивидуальную вариабельность в исследованиях биоэквивалентности, что осложняет их оценку [3,4].…”

Section: оригинальные статьи / Original Articlesunclassified

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Expert Approaches to the Assessment of Losartan Drugs Bioequivalence

Ромодановский¹,

Горячев²

2020

Vedomosti Nauchnogo tsentra ekspertizy sredstv meditsinskogo pr

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Angiotensin II receptor antagonists (ARAs) are one of the most promising classes of antihypertensive drugs. They are most widely represented on the Russian market by losartan drugs which total 24 items. Therefore, it is crucial to analyse the factors that may affect the results of comparison of generic and reference losartan drugs.The aim of the study was to perform a retrospective analysis of bioequivalence studies of generic losartan drugs in order to develop approaches to expert evaluation of research protocols and reports.Materials and methods: the retrospective analysis covered the results of 27 bioequivalence studies of losartan and included the calculation of the pharmacokinetic parameters Cmax and AUC0-t, their intra-individual variability, and the weighted average of intra-individual variability. The calculations were made for the pooled population of men and women, as well as separately for each gender.Results: the data obtained indicate borderline high variability of losartan in bioequivalence studies (for Cmax in 50 % of the studies). It was demonstrated that losartan drugs may have different pharmacokinetics in men and women in terms of Cmax and AUC0-t. The retrospective analysis of the data made it possible to formulate relevant expert approaches to evaluation of protocols and reports of bioequivalence studies of losartan drugs.Conclusions: Bioequivalence of losartan should be evaluated in three- or four-period, double crossover, two-sequence replicate design studies. The study has to determine the pharmacokinetic parameters of the starting compound and its active metabolite; the period of determination of analytes should be at least 36 hours; the washout period of 7 days is sufficient; blood sampling should be more frequent during the first hour after administration for losartan and during the first 3–4 hours for the metabolite. When determining the sample size, the weighted average of the coefficient of intra-individual variability of Cmax of losartan (33 %) should be taken into account. The bioequivalence margins for Cmax can be scaled up.

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Section: оригинальные статьи / Original Articlesunclassified

Expert Approaches to the Assessment of Losartan Drugs Bioequivalence

Ромодановский¹,

Горячев²

2020

Vedomosti Nauchnogo tsentra ekspertizy sredstv meditsinskogo pr

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Fixed drug combinations as a way of complex antihypertensive therapy optimization: focus on the combination of amlodipine, indapamide, perindopril

Поветкин

Корнилов

2022

Arter. gipertenz.

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This article is an analysis of current data on arterial hypertension (HTN) as a leading risk factor for premature death. We discuss the reasons of the failure to achieve target levels of blood pressure, and the available approaches to HTN pharmacological treatment by the main classes of antihypertensive drugs in accordance with current clinical guidelines. We show the advantages of fixed combinations (FC) of antihypertensive drugs and the ways to optimize antihypertensive treatment by administration of a triple FC, containing amlodipine, indapamide and perindopril.

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Angiotensin Ii Receptor Antagonists in the Treatment of Hypertension: Perspectives for Clinical Use

Cited by 2 publications

References 10 publications

Expert Approaches to the Assessment of Losartan Drugs Bioequivalence

Expert Approaches to the Assessment of Losartan Drugs Bioequivalence

Fixed drug combinations as a way of complex antihypertensive therapy optimization: focus on the combination of amlodipine, indapamide, perindopril

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