Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia
We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiortho...
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Veröffentlicht in: | Bulletin of experimental biology and medicine 2020-02, Vol.168 (4), p.465-469 |
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description | We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiorthostatic hypokinesia, a tendency to a decrease in half-elimination period, mean retention time, and volume of distribution and an increase in the rate of absorption, ratio of maximum concentrations, and relative rate of absorption of verapamil and propranolol were revealed. For ethacizine, a statistically significant increase in the time of attaining maximum concentration and volume of distribution and a decrease in the maximum concentration, rate of absorption, ratio of maximum concentrations, and relative rate of absorption under conditions of antiorthostatic hypokinesia were found. |
doi_str_mv | 10.1007/s10517-020-04732-w |
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V. ; Svistunov, A. A. ; Kondratenko, S. N. ; Kovachevich, I. V. ; Repenkova, L. G. ; Savelyeva, M. I. ; Kukes, V. G.</creator><creatorcontrib>Polyakov, A. V. ; Svistunov, A. A. ; Kondratenko, S. N. ; Kovachevich, I. V. ; Repenkova, L. G. ; Savelyeva, M. I. ; Kukes, V. G.</creatorcontrib><description>We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiorthostatic hypokinesia, a tendency to a decrease in half-elimination period, mean retention time, and volume of distribution and an increase in the rate of absorption, ratio of maximum concentrations, and relative rate of absorption of verapamil and propranolol were revealed. For ethacizine, a statistically significant increase in the time of attaining maximum concentration and volume of distribution and a decrease in the maximum concentration, rate of absorption, ratio of maximum concentrations, and relative rate of absorption under conditions of antiorthostatic hypokinesia were found.</description><identifier>ISSN: 0007-4888</identifier><identifier>EISSN: 1573-8221</identifier><identifier>DOI: 10.1007/s10517-020-04732-w</identifier><identifier>PMID: 32146624</identifier><language>eng</language><publisher>New York: Springer US</publisher><subject>Adult ; Analysis ; Area Under Curve ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Cardiovascular Agents - blood ; Cardiovascular Agents - pharmacokinetics ; Cell Biology ; Half-Life ; Humans ; Hypokinesia - blood ; Hypokinesia - drug therapy ; Internal Medicine ; Laboratory Medicine ; Life Sciences & Biomedicine ; Male ; Medicine, Research & Experimental ; Middle Aged ; Pathology ; Phenothiazines - blood ; Phenothiazines - pharmacokinetics ; Propranolol - blood ; Propranolol - pharmacokinetics ; Propranolol hydrochloride ; Research & Experimental Medicine ; Science & Technology ; Verapamil - blood ; Verapamil - pharmacokinetics ; Weightlessness Simulation - methods</subject><ispartof>Bulletin of experimental biology and medicine, 2020-02, Vol.168 (4), p.465-469</ispartof><rights>Springer Science+Business Media, LLC, part of Springer Nature 2020</rights><rights>COPYRIGHT 2020 Springer</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>2</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000527541200011</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c378t-ec310f8ae818b9196f9d3b7e6d2e46e28e2e45300099267da34b9e80fc72de553</citedby><cites>FETCH-LOGICAL-c378t-ec310f8ae818b9196f9d3b7e6d2e46e28e2e45300099267da34b9e80fc72de553</cites><orcidid>0000-0002-2373-2250 ; 0000-0003-1323-7894</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10517-020-04732-w$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10517-020-04732-w$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>315,781,785,27929,27930,28253,41493,42562,51324</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/32146624$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Polyakov, A. V.</creatorcontrib><creatorcontrib>Svistunov, A. A.</creatorcontrib><creatorcontrib>Kondratenko, S. N.</creatorcontrib><creatorcontrib>Kovachevich, I. V.</creatorcontrib><creatorcontrib>Repenkova, L. G.</creatorcontrib><creatorcontrib>Savelyeva, M. I.</creatorcontrib><creatorcontrib>Kukes, V. G.</creatorcontrib><title>Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia</title><title>Bulletin of experimental biology and medicine</title><addtitle>Bull Exp Biol Med</addtitle><addtitle>B EXP BIOL MED</addtitle><addtitle>Bull Exp Biol Med</addtitle><description>We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiorthostatic hypokinesia, a tendency to a decrease in half-elimination period, mean retention time, and volume of distribution and an increase in the rate of absorption, ratio of maximum concentrations, and relative rate of absorption of verapamil and propranolol were revealed. For ethacizine, a statistically significant increase in the time of attaining maximum concentration and volume of distribution and a decrease in the maximum concentration, rate of absorption, ratio of maximum concentrations, and relative rate of absorption under conditions of antiorthostatic hypokinesia were found.</description><subject>Adult</subject><subject>Analysis</subject><subject>Area Under Curve</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Cardiovascular Agents - blood</subject><subject>Cardiovascular Agents - pharmacokinetics</subject><subject>Cell Biology</subject><subject>Half-Life</subject><subject>Humans</subject><subject>Hypokinesia - blood</subject><subject>Hypokinesia - drug therapy</subject><subject>Internal Medicine</subject><subject>Laboratory Medicine</subject><subject>Life Sciences & Biomedicine</subject><subject>Male</subject><subject>Medicine, Research & Experimental</subject><subject>Middle Aged</subject><subject>Pathology</subject><subject>Phenothiazines - blood</subject><subject>Phenothiazines - pharmacokinetics</subject><subject>Propranolol - blood</subject><subject>Propranolol - pharmacokinetics</subject><subject>Propranolol hydrochloride</subject><subject>Research & Experimental Medicine</subject><subject>Science & Technology</subject><subject>Verapamil - blood</subject><subject>Verapamil - pharmacokinetics</subject><subject>Weightlessness Simulation - methods</subject><issn>0007-4888</issn><issn>1573-8221</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>AOWDO</sourceid><sourceid>EIF</sourceid><recordid>eNqNkM1u1DAUhS1ERaeFF2CBvGKDAv5JYmc5BEqRKrVSy9py7JsZl4w9spOOZsuT40ygS8TCutfSd46PD0JvKflICRGfEiUVFQVhpCCl4Kw4vEArWgleSMboS7QimSpKKeU5ukjpcb6Smr5C55zRsq5ZuUK_7sBMg9PRjQ4SDj2-2-q40yb8dB5GZxLW3uLPLugn7QbducGNx5m7DzvArY7WhSedsomO-EucNglP3kLEbfA2mwZ_cl37vMZxG9Kosyu-Pu5PLySnX6OzXg8J3vyZl-jH1deH9rq4uf32vV3fFIYLORZgOCW91CCp7Bra1H1jeSegtgzKGpiEPCueP9k0rBZW87JrQJLeCGahqvgler_4bvQAagt6GLcpDNMpo1rXTBKRzwyyBTQxpBShV_vodjoeFSVqbl4tzavcvDo1rw5Z9G4R7aduB_ZZ8rfqDMgFOEAX-mQceAPPWI5dMVGVlOWN0tbNNQXfhsmPWfrh_6WZ5gudMuE3ENVjmKLP1f4r_2_U5LJc</recordid><startdate>20200201</startdate><enddate>20200201</enddate><creator>Polyakov, A. V.</creator><creator>Svistunov, A. A.</creator><creator>Kondratenko, S. N.</creator><creator>Kovachevich, I. V.</creator><creator>Repenkova, L. G.</creator><creator>Savelyeva, M. I.</creator><creator>Kukes, V. G.</creator><general>Springer US</general><general>Springer Nature</general><general>Springer</general><scope>AOWDO</scope><scope>BLEPL</scope><scope>DTL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0002-2373-2250</orcidid><orcidid>https://orcid.org/0000-0003-1323-7894</orcidid></search><sort><creationdate>20200201</creationdate><title>Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia</title><author>Polyakov, A. V. ; Svistunov, A. A. ; Kondratenko, S. N. ; Kovachevich, I. V. ; Repenkova, L. G. ; Savelyeva, M. I. ; Kukes, V. G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c378t-ec310f8ae818b9196f9d3b7e6d2e46e28e2e45300099267da34b9e80fc72de553</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Adult</topic><topic>Analysis</topic><topic>Area Under Curve</topic><topic>Biological Availability</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Cardiovascular Agents - blood</topic><topic>Cardiovascular Agents - pharmacokinetics</topic><topic>Cell Biology</topic><topic>Half-Life</topic><topic>Humans</topic><topic>Hypokinesia - blood</topic><topic>Hypokinesia - drug therapy</topic><topic>Internal Medicine</topic><topic>Laboratory Medicine</topic><topic>Life Sciences & Biomedicine</topic><topic>Male</topic><topic>Medicine, Research & Experimental</topic><topic>Middle Aged</topic><topic>Pathology</topic><topic>Phenothiazines - blood</topic><topic>Phenothiazines - pharmacokinetics</topic><topic>Propranolol - blood</topic><topic>Propranolol - pharmacokinetics</topic><topic>Propranolol hydrochloride</topic><topic>Research & Experimental Medicine</topic><topic>Science & Technology</topic><topic>Verapamil - blood</topic><topic>Verapamil - pharmacokinetics</topic><topic>Weightlessness Simulation - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Polyakov, A. V.</creatorcontrib><creatorcontrib>Svistunov, A. A.</creatorcontrib><creatorcontrib>Kondratenko, S. N.</creatorcontrib><creatorcontrib>Kovachevich, I. V.</creatorcontrib><creatorcontrib>Repenkova, L. G.</creatorcontrib><creatorcontrib>Savelyeva, M. I.</creatorcontrib><creatorcontrib>Kukes, V. G.</creatorcontrib><collection>Web of Science - Science Citation Index Expanded - 2020</collection><collection>Web of Science Core Collection</collection><collection>Science Citation Index Expanded</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Bulletin of experimental biology and medicine</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Polyakov, A. V.</au><au>Svistunov, A. A.</au><au>Kondratenko, S. N.</au><au>Kovachevich, I. V.</au><au>Repenkova, L. G.</au><au>Savelyeva, M. I.</au><au>Kukes, V. G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia</atitle><jtitle>Bulletin of experimental biology and medicine</jtitle><stitle>Bull Exp Biol Med</stitle><stitle>B EXP BIOL MED</stitle><addtitle>Bull Exp Biol Med</addtitle><date>2020-02-01</date><risdate>2020</risdate><volume>168</volume><issue>4</issue><spage>465</spage><epage>469</epage><pages>465-469</pages><issn>0007-4888</issn><eissn>1573-8221</eissn><abstract>We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity. Under conditions of antiorthostatic hypokinesia, a tendency to a decrease in half-elimination period, mean retention time, and volume of distribution and an increase in the rate of absorption, ratio of maximum concentrations, and relative rate of absorption of verapamil and propranolol were revealed. For ethacizine, a statistically significant increase in the time of attaining maximum concentration and volume of distribution and a decrease in the maximum concentration, rate of absorption, ratio of maximum concentrations, and relative rate of absorption under conditions of antiorthostatic hypokinesia were found.</abstract><cop>New York</cop><pub>Springer US</pub><pmid>32146624</pmid><doi>10.1007/s10517-020-04732-w</doi><tpages>5</tpages><orcidid>https://orcid.org/0000-0002-2373-2250</orcidid><orcidid>https://orcid.org/0000-0003-1323-7894</orcidid></addata></record> |
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subjects | Adult Analysis Area Under Curve Biological Availability Biomedical and Life Sciences Biomedicine Cardiovascular Agents - blood Cardiovascular Agents - pharmacokinetics Cell Biology Half-Life Humans Hypokinesia - blood Hypokinesia - drug therapy Internal Medicine Laboratory Medicine Life Sciences & Biomedicine Male Medicine, Research & Experimental Middle Aged Pathology Phenothiazines - blood Phenothiazines - pharmacokinetics Propranolol - blood Propranolol - pharmacokinetics Propranolol hydrochloride Research & Experimental Medicine Science & Technology Verapamil - blood Verapamil - pharmacokinetics Weightlessness Simulation - methods |
title | Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia |
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