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Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?

BACKGROUND: Despite several decades of use of calcium channel blockers, the side effect of edema persists as a class effect, and its mechanism is unresolved. Amlodipine has effects on hemorheology (HR), and its hemodilutory property may partly contribute to its antihypertensive action. This aspect i...

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Autores principales: Ravindra, R.P., Arunkumar, S., Puniyani, R.R., Padgaonkar, K., Vadivelu, Ramalingam, Sharma, Rajeev, Panicker, Gopi, Lokhandwala, Yash
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6477139/
https://www.ncbi.nlm.nih.gov/pubmed/31000180
http://dx.doi.org/10.1016/j.ihj.2018.10.417
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author Ravindra, R.P.
Arunkumar, S.
Puniyani, R.R.
Padgaonkar, K.
Vadivelu, Ramalingam
Sharma, Rajeev
Panicker, Gopi
Lokhandwala, Yash
author_facet Ravindra, R.P.
Arunkumar, S.
Puniyani, R.R.
Padgaonkar, K.
Vadivelu, Ramalingam
Sharma, Rajeev
Panicker, Gopi
Lokhandwala, Yash
author_sort Ravindra, R.P.
collection PubMed
description BACKGROUND: Despite several decades of use of calcium channel blockers, the side effect of edema persists as a class effect, and its mechanism is unresolved. Amlodipine has effects on hemorheology (HR), and its hemodilutory property may partly contribute to its antihypertensive action. This aspect is not well studied, and the literature is sparse in this regard. OBJECTIVE: This experiment was planned to determine effect of a single-dose administration of amlodipine on HR parameters in normal human volunteers. METHODS AND RESULTS: Amlodipine (5 mg) or S (-) amlodipine (2.5 mg) was administered to 27 normal human volunteers. Whole-blood viscosity (WBV) at different shear rates, plasma viscosity (PV), red cell rigidity (RCR), red cell aggregation (RCA), hematocrit (Hct), plasma hemoglobin, along with plasma drug concentration were determined at time intervals, t = 0, 4, 8, 12, and 24 h. Statistically significant reductions were observed at t(max) = 4 h in WBV at shear rates of 0.512 s(–1) (p < 0.005), WBV at shear rates of 5.26 s(–1) (p < 0.01), PV (p < 0.05), and Hct (p < 0.01). At t = 8 h, as drug concentration reduced, some of the changes persisted and later slowly decreased with the decreasing drug concentration till t = 24 h. Red blood cell–related parameters such as RCA and RCR remained unaltered. WBV values at all shear rates, when corrected for Hct = 0.45, did not show deviation from their original values at any time. CONCLUSIONS: Amlodipine causes a reduction in Hct and blood viscosity, along with hemodilution. These effects persist as long as the drug remains in plasma. Edema resulting from chronic dosing may be explained by the aforementioned effects. It is possible that antihypertensive action of the drug may be due to a combination of vasodilatation and an improvement in the HR properties.
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spelling pubmed-64771392020-01-01 Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema? Ravindra, R.P. Arunkumar, S. Puniyani, R.R. Padgaonkar, K. Vadivelu, Ramalingam Sharma, Rajeev Panicker, Gopi Lokhandwala, Yash Indian Heart J Original Article BACKGROUND: Despite several decades of use of calcium channel blockers, the side effect of edema persists as a class effect, and its mechanism is unresolved. Amlodipine has effects on hemorheology (HR), and its hemodilutory property may partly contribute to its antihypertensive action. This aspect is not well studied, and the literature is sparse in this regard. OBJECTIVE: This experiment was planned to determine effect of a single-dose administration of amlodipine on HR parameters in normal human volunteers. METHODS AND RESULTS: Amlodipine (5 mg) or S (-) amlodipine (2.5 mg) was administered to 27 normal human volunteers. Whole-blood viscosity (WBV) at different shear rates, plasma viscosity (PV), red cell rigidity (RCR), red cell aggregation (RCA), hematocrit (Hct), plasma hemoglobin, along with plasma drug concentration were determined at time intervals, t = 0, 4, 8, 12, and 24 h. Statistically significant reductions were observed at t(max) = 4 h in WBV at shear rates of 0.512 s(–1) (p < 0.005), WBV at shear rates of 5.26 s(–1) (p < 0.01), PV (p < 0.05), and Hct (p < 0.01). At t = 8 h, as drug concentration reduced, some of the changes persisted and later slowly decreased with the decreasing drug concentration till t = 24 h. Red blood cell–related parameters such as RCA and RCR remained unaltered. WBV values at all shear rates, when corrected for Hct = 0.45, did not show deviation from their original values at any time. CONCLUSIONS: Amlodipine causes a reduction in Hct and blood viscosity, along with hemodilution. These effects persist as long as the drug remains in plasma. Edema resulting from chronic dosing may be explained by the aforementioned effects. It is possible that antihypertensive action of the drug may be due to a combination of vasodilatation and an improvement in the HR properties. Elsevier 2019 2018-12-04 /pmc/articles/PMC6477139/ /pubmed/31000180 http://dx.doi.org/10.1016/j.ihj.2018.10.417 Text en © 2018 Cardiological Society of India. Published by Elsevier B.V. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Ravindra, R.P.
Arunkumar, S.
Puniyani, R.R.
Padgaonkar, K.
Vadivelu, Ramalingam
Sharma, Rajeev
Panicker, Gopi
Lokhandwala, Yash
Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title_full Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title_fullStr Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title_full_unstemmed Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title_short Amlodipine alters hemorheological parameters: Increased efficacy at the cost of edema?
title_sort amlodipine alters hemorheological parameters: increased efficacy at the cost of edema?
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6477139/
https://www.ncbi.nlm.nih.gov/pubmed/31000180
http://dx.doi.org/10.1016/j.ihj.2018.10.417
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