Chronopharmacology of verapamil in Stage I-II arterial hypertension

Aim. To compare the pharmacokinetics and pharmacodynamics of verapamil retard, regularly taken by patients  with Stage I-II arterial hypertension (AH). Material and methods. The effects of the administration time (morning vs. evening) on verapamil retard pharmacokinetics were investigated. This open...

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Main Authors: V. G. Belolipetskaya, D. F. Guranda, E. Yu. Fedorova, V. M. Gorbunov, N. A. Belolipetsky, A. V. Zhezlova, O. Yu. Isaykina, E. A. Zhabina, I. E. Koltunov
Format: Article
Language:Russian
Published: «SILICEA-POLIGRAF» LLC 2009-08-01
Series:Кардиоваскулярная терапия и профилактика
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Online Access:https://cardiovascular.elpub.ru/jour/article/view/1352
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author V. G. Belolipetskaya
D. F. Guranda
E. Yu. Fedorova
V. M. Gorbunov
N. A. Belolipetsky
A. V. Zhezlova
O. Yu. Isaykina
E. A. Zhabina
I. E. Koltunov
author_facet V. G. Belolipetskaya
D. F. Guranda
E. Yu. Fedorova
V. M. Gorbunov
N. A. Belolipetsky
A. V. Zhezlova
O. Yu. Isaykina
E. A. Zhabina
I. E. Koltunov
author_sort V. G. Belolipetskaya
collection DOAJ
description Aim. To compare the pharmacokinetics and pharmacodynamics of verapamil retard, regularly taken by patients  with Stage I-II arterial hypertension (AH). Material and methods. The effects of the administration time (morning vs. evening) on verapamil retard pharmacokinetics were investigated. This open, randomised, cross-over study included 14 patients with Stage I-II AH,  who were regularly administered verapamil retard for 3 weeks. Before the active therapy started, all antihypertensive medications were withdrawn, with an exception of short-acting agents (“wash-out” period). Two weeks later,  the patients were administered verapamil retard, according to the randomisation scheme, and were recommended  to take one tablet in the morning or evening, at the same time every day. The first administration was at the clinic,  under medical supervision. Three weeks later, the participants were hospitalised for pharmacokinetics assessment. Seven days after the end of the first treatment course, a second course started, with an inverted time of verapamil retard administration. Blood concentration of non-modified verapamil was measured by high-performance liquid chromatography with fluorescent detection.Results. Significant differences in pharmacokinetics were observed for morning vs. evening verapamil administration. The respective maximal verapamil concentrations were 239,7±152,3 vs. 148,6±107,4 ng/ml (p<0,01), and respective half-life times were 12,50±3,48 vs. 22,57±15,24 hours (p<0,05). For other parameters, the difference was non-significant.Conclusion. In Stage I-II AH patients, the morning administration of Isoptin SR resulted in accelerated increase of its plasma concentration. At the same time, the evening administration was associated with increased half-life time and higher “concentration-effect” correlation, which makes the latter variant more rational.
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publishDate 2009-08-01
publisher «SILICEA-POLIGRAF» LLC
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series Кардиоваскулярная терапия и профилактика
spelling doaj-art-e7d0f9574dd0416da33a7f819838228f2025-08-20T02:59:53Zrus«SILICEA-POLIGRAF» LLCКардиоваскулярная терапия и профилактика1728-88002619-01252009-08-018813181062Chronopharmacology of verapamil in Stage I-II arterial hypertensionV. G. Belolipetskaya0D. F. Guranda1E. Yu. Fedorova2V. M. Gorbunov3N. A. Belolipetsky4A. V. Zhezlova5O. Yu. Isaykina6E. A. Zhabina7I. E. Koltunov8State Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesA.N. Belozersky Research Institute of Physical & Chemical Biology, M.V. Lomonosov Moscow State UniversityState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesState Research Centre for Preventive Medicine, Federal Agency on High Medical TechnologiesAim. To compare the pharmacokinetics and pharmacodynamics of verapamil retard, regularly taken by patients  with Stage I-II arterial hypertension (AH). Material and methods. The effects of the administration time (morning vs. evening) on verapamil retard pharmacokinetics were investigated. This open, randomised, cross-over study included 14 patients with Stage I-II AH,  who were regularly administered verapamil retard for 3 weeks. Before the active therapy started, all antihypertensive medications were withdrawn, with an exception of short-acting agents (“wash-out” period). Two weeks later,  the patients were administered verapamil retard, according to the randomisation scheme, and were recommended  to take one tablet in the morning or evening, at the same time every day. The first administration was at the clinic,  under medical supervision. Three weeks later, the participants were hospitalised for pharmacokinetics assessment. Seven days after the end of the first treatment course, a second course started, with an inverted time of verapamil retard administration. Blood concentration of non-modified verapamil was measured by high-performance liquid chromatography with fluorescent detection.Results. Significant differences in pharmacokinetics were observed for morning vs. evening verapamil administration. The respective maximal verapamil concentrations were 239,7±152,3 vs. 148,6±107,4 ng/ml (p<0,01), and respective half-life times were 12,50±3,48 vs. 22,57±15,24 hours (p<0,05). For other parameters, the difference was non-significant.Conclusion. In Stage I-II AH patients, the morning administration of Isoptin SR resulted in accelerated increase of its plasma concentration. At the same time, the evening administration was associated with increased half-life time and higher “concentration-effect” correlation, which makes the latter variant more rational.https://cardiovascular.elpub.ru/jour/article/view/1352chronopharmacokineticsverapamil retardarterial hypertension24-hour blood pressure monitoring
spellingShingle V. G. Belolipetskaya
D. F. Guranda
E. Yu. Fedorova
V. M. Gorbunov
N. A. Belolipetsky
A. V. Zhezlova
O. Yu. Isaykina
E. A. Zhabina
I. E. Koltunov
Chronopharmacology of verapamil in Stage I-II arterial hypertension
Кардиоваскулярная терапия и профилактика
chronopharmacokinetics
verapamil retard
arterial hypertension
24-hour blood pressure monitoring
title Chronopharmacology of verapamil in Stage I-II arterial hypertension
title_full Chronopharmacology of verapamil in Stage I-II arterial hypertension
title_fullStr Chronopharmacology of verapamil in Stage I-II arterial hypertension
title_full_unstemmed Chronopharmacology of verapamil in Stage I-II arterial hypertension
title_short Chronopharmacology of verapamil in Stage I-II arterial hypertension
title_sort chronopharmacology of verapamil in stage i ii arterial hypertension
topic chronopharmacokinetics
verapamil retard
arterial hypertension
24-hour blood pressure monitoring
url https://cardiovascular.elpub.ru/jour/article/view/1352
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