Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat
Identifieur interne : 000041 ( Istex/Corpus ); précédent : 000040; suivant : 000042Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat
Auteurs : Evan W. Mcchesney ; William F. Banks Jr. ; Raymond J. FabianSource :
- Toxicology and Applied Pharmacology [ 0041-008X ] ; 1967.
English descriptors
- Teeft :
- Actual plasma concentration, Albino, Albino albino albino, Albino rats, Antimalarial, Antimalarial metabolism, Approximate proportions, Available data, Average weight, Biochemical properties, Body weight, Charles river, Chloroquine, Control groups, Corresponding data, Daily dosage, Daily dose, Daily intakes, Daily medication, Daily medication days, Dosage, Drug intake, Food consumption, Food intake, Growth rates, Heart tissue, Hooded, Hooded rats, Hydroxychloroquine, Initial weight, Last dose, Last week, Mcchesney, Medication, Medication period, Ocular concentration, Other tissues, Plasma concentration ratios, Plasma concentrations, Plasma levels, Plasma ratios, Rat, Recent dose, Schmidt, Schmidt group, Spleen, Standard error, Stomach tube, Sulfate salt, Tissue concentration, Tissue concentrations, Tissue distribution, Tissue levels, Total retention, Total retentions, Trade name, Turnover rate, Warrant recording, Weight gains, Winthrop laboratories, Withdrawal period.
Abstract
Abstract: Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney et al., 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.
Url:
DOI: 10.1016/0041-008X(67)90089-0
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<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title>Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title><author><name sortKey="Mcchesney, Evan W" sort="Mcchesney, Evan W" uniqKey="Mcchesney E" first="Evan W." last="Mcchesney">Evan W. Mcchesney</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author><author><name sortKey="Banks Jr, William F" sort="Banks Jr, William F" uniqKey="Banks Jr W" first="William F." last="Banks Jr.">William F. Banks Jr.</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author><author><name sortKey="Fabian, Raymond J" sort="Fabian, Raymond J" uniqKey="Fabian R" first="Raymond J." last="Fabian">Raymond J. Fabian</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:D5F5D2915C7A5B862E5F4A337F1923A32EACC62A</idno><date when="1967" year="1967">1967</date><idno type="doi">10.1016/0041-008X(67)90089-0</idno><idno type="url">https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">000041</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000041</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a">Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title><author><name sortKey="Mcchesney, Evan W" sort="Mcchesney, Evan W" uniqKey="Mcchesney E" first="Evan W." last="Mcchesney">Evan W. Mcchesney</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author><author><name sortKey="Banks Jr, William F" sort="Banks Jr, William F" uniqKey="Banks Jr W" first="William F." last="Banks Jr.">William F. Banks Jr.</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author><author><name sortKey="Fabian, Raymond J" sort="Fabian, Raymond J" uniqKey="Fabian R" first="Raymond J." last="Fabian">Raymond J. Fabian</name><affiliation><mods:affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation><affiliation><mods:affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</mods:affiliation></affiliation></author></analytic><monogr></monogr><series><title level="j">Toxicology and Applied Pharmacology</title><title level="j" type="abbrev">YTAAP</title><idno type="ISSN">0041-008X</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1967">1967</date><biblScope unit="volume">10</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="501">501</biblScope><biblScope unit="page" to="513">513</biblScope></imprint><idno type="ISSN">0041-008X</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0041-008X</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Actual plasma concentration</term><term>Albino</term><term>Albino albino albino</term><term>Albino rats</term><term>Antimalarial</term><term>Antimalarial metabolism</term><term>Approximate proportions</term><term>Available data</term><term>Average weight</term><term>Biochemical properties</term><term>Body weight</term><term>Charles river</term><term>Chloroquine</term><term>Control groups</term><term>Corresponding data</term><term>Daily dosage</term><term>Daily dose</term><term>Daily intakes</term><term>Daily medication</term><term>Daily medication days</term><term>Dosage</term><term>Drug intake</term><term>Food consumption</term><term>Food intake</term><term>Growth rates</term><term>Heart tissue</term><term>Hooded</term><term>Hooded rats</term><term>Hydroxychloroquine</term><term>Initial weight</term><term>Last dose</term><term>Last week</term><term>Mcchesney</term><term>Medication</term><term>Medication period</term><term>Ocular concentration</term><term>Other tissues</term><term>Plasma concentration ratios</term><term>Plasma concentrations</term><term>Plasma levels</term><term>Plasma ratios</term><term>Rat</term><term>Recent dose</term><term>Schmidt</term><term>Schmidt group</term><term>Spleen</term><term>Standard error</term><term>Stomach tube</term><term>Sulfate salt</term><term>Tissue concentration</term><term>Tissue concentrations</term><term>Tissue distribution</term><term>Tissue levels</term><term>Total retention</term><term>Total retentions</term><term>Trade name</term><term>Turnover rate</term><term>Warrant recording</term><term>Weight gains</term><term>Winthrop laboratories</term><term>Withdrawal period</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Abstract: Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney et al., 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.</div></front></TEI><istex><corpusName>elsevier</corpusName><keywords><teeft><json:string>albino</json:string><json:string>mcchesney</json:string><json:string>hooded</json:string><json:string>chloroquine</json:string><json:string>daily dose</json:string><json:string>tissue concentrations</json:string><json:string>albino rats</json:string><json:string>hydroxychloroquine</json:string><json:string>antimalarial</json:string><json:string>turnover rate</json:string><json:string>body weight</json:string><json:string>tissue concentration</json:string><json:string>daily intakes</json:string><json:string>spleen</json:string><json:string>last dose</json:string><json:string>total retention</json:string><json:string>standard error</json:string><json:string>schmidt</json:string><json:string>plasma ratios</json:string><json:string>stomach tube</json:string><json:string>recent dose</json:string><json:string>withdrawal period</json:string><json:string>tissue distribution</json:string><json:string>ocular concentration</json:string><json:string>schmidt group</json:string><json:string>medication</json:string><json:string>rat</json:string><json:string>dosage</json:string><json:string>hooded rats</json:string><json:string>trade name</json:string><json:string>biochemical properties</json:string><json:string>tissue levels</json:string><json:string>winthrop laboratories</json:string><json:string>corresponding data</json:string><json:string>total retentions</json:string><json:string>average weight</json:string><json:string>daily medication</json:string><json:string>sulfate salt</json:string><json:string>weight gains</json:string><json:string>charles river</json:string><json:string>initial weight</json:string><json:string>other tissues</json:string><json:string>food intake</json:string><json:string>warrant recording</json:string><json:string>drug intake</json:string><json:string>plasma concentrations</json:string><json:string>heart tissue</json:string><json:string>actual plasma concentration</json:string><json:string>albino albino albino</json:string><json:string>antimalarial metabolism</json:string><json:string>control groups</json:string><json:string>approximate proportions</json:string><json:string>food consumption</json:string><json:string>plasma concentration ratios</json:string><json:string>daily dosage</json:string><json:string>available data</json:string><json:string>growth rates</json:string><json:string>plasma levels</json:string><json:string>daily medication days</json:string><json:string>last week</json:string><json:string>medication period</json:string></teeft></keywords><author><json:item><name>Evan W. McChesney</name><affiliations><json:string>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string><json:string>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string></affiliations></json:item><json:item><name>William F. Banks, Jr.</name><affiliations><json:string>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string><json:string>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string></affiliations></json:item><json:item><name>Raymond J. Fabian</name><affiliations><json:string>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string><json:string>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</json:string></affiliations></json:item></author><arkIstex>ark:/67375/6H6-1XQQQ8KT-M</arkIstex><language><json:string>eng</json:string></language><originalGenre><json:string>Full-length article</json:string></originalGenre><abstract>Abstract: Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney et al., 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.</abstract><qualityIndicators><score>8.836</score><pdfWordCount>3836</pdfWordCount><pdfCharCount>27012</pdfCharCount><pdfVersion>1.3</pdfVersion><pdfPageCount>13</pdfPageCount><pdfPageSize>507 x 720 pts</pdfPageSize><refBibsNative>true</refBibsNative><abstractWordCount>327</abstractWordCount><abstractCharCount>1979</abstractCharCount><keywordCount>0</keywordCount></qualityIndicators><title>Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title><pmid><json:string>6059665</json:string></pmid><pii><json:string>0041-008X(67)90089-0</json:string></pii><genre><json:string>research-article</json:string></genre><host><title>Toxicology and Applied Pharmacology</title><language><json:string>unknown</json:string></language><publicationDate>1967</publicationDate><issn><json:string>0041-008X</json:string></issn><pii><json:string>S0041-008X(00)X0295-5</json:string></pii><volume>10</volume><issue>3</issue><pages><first>501</first><last>513</last></pages><genre><json:string>journal</json:string></genre></host><namedEntities><unitex><date><json:string>9 and 16-18</json:string><json:string>1967</json:string></date><geogName></geogName><orgName><json:string>Division of Sterling Drug Inc</json:string><json:string>Winthrop Laboratories</json:string></orgName><orgName_funder></orgName_funder><orgName_provider></orgName_provider><persName><json:string>Albino Albino</json:string><json:string>Charles E. Hunt</json:string><json:string>Charles River</json:string><json:string>WILLIAM Hydroxychloroquine</json:string><json:string>L. Bolinsky</json:string><json:string>FABIAN Sections</json:string></persName><placeName><json:string>New Aralen</json:string><json:string>York</json:string><json:string>New Plaquenil</json:string></placeName><ref_url></ref_url><ref_bibl><json:string>Rubin et al., 1963</json:string><json:string>McChesney et al. (1966)</json:string><json:string>Bernstein et al. (1963)</json:string><json:string>McChesney et al</json:string><json:string>McChesney et al., 1962</json:string><json:string>Perez et al., 1964</json:string><json:string>Whitehouse and Bostrom (1965)</json:string><json:string>McChesney et al. ( 1965)</json:string><json:string>Schmidt et al. (1953)</json:string><json:string>Ray, 1966</json:string><json:string>Sams and Epstein, 1965</json:string><json:string>Schmidt et al. ( 1953)</json:string><json:string>McChesney et al, 1965</json:string><json:string>McChesney et al., 1965</json:string></ref_bibl><bibl></bibl></unitex></namedEntities><ark><json:string>ark:/67375/6H6-1XQQQ8KT-M</json:string></ark><categories><wos><json:string>1 - science</json:string><json:string>2 - toxicology</json:string><json:string>2 - pharmacology & pharmacy</json:string></wos><scienceMetrix><json:string>1 - health sciences</json:string><json:string>2 - biomedical research</json:string><json:string>3 - toxicology</json:string></scienceMetrix><scopus><json:string>1 - Life Sciences</json:string><json:string>2 - Pharmacology, Toxicology and Pharmaceutics</json:string><json:string>3 - Pharmacology</json:string><json:string>1 - Life Sciences</json:string><json:string>2 - Pharmacology, Toxicology and Pharmaceutics</json:string><json:string>3 - Toxicology</json:string></scopus><inist><json:string>1 - sciences appliquees, technologies et medecines</json:string><json:string>2 - sciences biologiques et medicales</json:string><json:string>3 - sciences medicales</json:string><json:string>4 - pharmacologie. traitements medicamenteux</json:string></inist></categories><publicationDate>1967</publicationDate><copyrightDate>1967</copyrightDate><doi><json:string>10.1016/0041-008X(67)90089-0</json:string></doi><id>D5F5D2915C7A5B862E5F4A337F1923A32EACC62A</id><score>1</score><fulltext><json:item><extension>pdf</extension><original>true</original><mimetype>application/pdf</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/fulltext.pdf</uri></json:item><json:item><extension>zip</extension><original>false</original><mimetype>application/zip</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/bundle.zip</uri></json:item><istex:fulltextTEI uri="https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/fulltext.tei"><teiHeader><fileDesc><titleStmt><title level="a">Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title></titleStmt><publicationStmt><authority>ISTEX</authority><publisher scheme="https://scientific-publisher.data.istex.fr">ELSEVIER</publisher><availability><licence><p>elsevier</p></licence></availability><p scheme="https://loaded-corpus.data.istex.fr/ark:/67375/XBH-HKKZVM7B-M"></p><date>1967</date></publicationStmt><notesStmt><note type="research-article" scheme="https://content-type.data.istex.fr/ark:/67375/XTP-1JC4F85T-7">research-article</note><note type="journal" scheme="https://publication-type.data.istex.fr/ark:/67375/JMC-0GLKJH51-B">journal</note></notesStmt><sourceDesc><biblStruct type="inbook"><analytic><title level="a">Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title><author xml:id="author-0000"><persName><forename type="first">Evan W.</forename><surname>McChesney</surname></persName><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation></author><author xml:id="author-0001"><persName><forename type="first">William F.</forename><surname>Banks, Jr.</surname></persName><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation></author><author xml:id="author-0002"><persName><forename type="first">Raymond J.</forename><surname>Fabian</surname></persName><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation></author><idno type="istex">D5F5D2915C7A5B862E5F4A337F1923A32EACC62A</idno><idno type="ark">ark:/67375/6H6-1XQQQ8KT-M</idno><idno type="DOI">10.1016/0041-008X(67)90089-0</idno><idno type="PII">0041-008X(67)90089-0</idno></analytic><monogr><title level="j">Toxicology and Applied Pharmacology</title><title level="j" type="abbrev">YTAAP</title><idno type="pISSN">0041-008X</idno><idno type="PII">S0041-008X(00)X0295-5</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1967"></date><biblScope unit="volume">10</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="501">501</biblScope><biblScope unit="page" to="513">513</biblScope></imprint></monogr></biblStruct></sourceDesc></fileDesc><profileDesc><creation><date>1967</date></creation><langUsage><language ident="en">en</language></langUsage><abstract xml:lang="en"><p>Abstract: Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney et al., 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.</p></abstract></profileDesc><revisionDesc><change when="1967">Published</change></revisionDesc></teiHeader></istex:fulltextTEI><json:item><extension>txt</extension><original>false</original><mimetype>text/plain</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/fulltext.txt</uri></json:item></fulltext><metadata><istex:metadataXml wicri:clean="Elsevier, elements deleted: tail"><istex:xmlDeclaration>version="1.0" encoding="utf-8"</istex:xmlDeclaration><istex:docType PUBLIC="-//ES//DTD journal article DTD version 4.5.2//EN//XML" URI="art452.dtd" name="istex:docType"></istex:docType><istex:document><converted-article version="4.5.2" docsubtype="fla"><item-info><jid>YTAAP</jid><aid>67900890</aid><ce:pii>0041-008X(67)90089-0</ce:pii><ce:doi>10.1016/0041-008X(67)90089-0</ce:doi><ce:copyright type="unknown" year="1967"></ce:copyright></item-info><head><ce:title>Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</ce:title><ce:author-group><ce:author><ce:given-name>Evan W.</ce:given-name><ce:surname>McChesney</ce:surname><ce:cross-ref refid="AFF1"><ce:sup>a</ce:sup></ce:cross-ref><ce:cross-ref refid="AFF2"><ce:sup>b</ce:sup></ce:cross-ref></ce:author><ce:author><ce:given-name>William F.</ce:given-name><ce:surname>Banks</ce:surname><ce:suffix>Jr.</ce:suffix><ce:cross-ref refid="AFF1"><ce:sup>a</ce:sup></ce:cross-ref><ce:cross-ref refid="AFF2"><ce:sup>b</ce:sup></ce:cross-ref></ce:author><ce:author><ce:given-name>Raymond J.</ce:given-name><ce:surname>Fabian</ce:surname><ce:cross-ref refid="AFF1"><ce:sup>a</ce:sup></ce:cross-ref><ce:cross-ref refid="AFF2"><ce:sup>b</ce:sup></ce:cross-ref></ce:author><ce:affiliation id="AFF1"><ce:label>a</ce:label><ce:textfn>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</ce:textfn></ce:affiliation><ce:affiliation id="AFF2"><ce:label>b</ce:label><ce:textfn>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</ce:textfn></ce:affiliation></ce:author-group><ce:date-received day="17" month="1" year="1967"></ce:date-received><ce:abstract><ce:section-title>Abstract</ce:section-title><ce:abstract-sec><ce:simple-para>Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney <ce:italic>et al.</ce:italic>, 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.</ce:simple-para></ce:abstract-sec></ce:abstract></head></converted-article></istex:document></istex:metadataXml><mods version="3.6"><titleInfo><title>Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title></titleInfo><titleInfo type="alternative" contentType="CDATA"><title>Tissue distribution of chloroquine, hydroxychloroquine, and desethylchloroquine in the rat</title></titleInfo><name type="personal"><namePart type="given">Evan W.</namePart><namePart type="family">McChesney</namePart><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><role><roleTerm type="text">author</roleTerm></role></name><name type="personal"><namePart type="given">William F.</namePart><namePart type="family">Banks, Jr.</namePart><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><role><roleTerm type="text">author</roleTerm></role></name><name type="personal"><namePart type="given">Raymond J.</namePart><namePart type="family">Fabian</namePart><affiliation>Section of Biochemistry, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><affiliation>Section of Toxicology, Sterling-Winthrop Research Institute, A Division of Sterling Drug Inc., Rensselaer, New York 12144 USA</affiliation><role><roleTerm type="text">author</roleTerm></role></name><typeOfResource>text</typeOfResource><genre type="research-article" displayLabel="Full-length article" authority="ISTEX" authorityURI="https://content-type.data.istex.fr" valueURI="https://content-type.data.istex.fr/ark:/67375/XTP-1JC4F85T-7">research-article</genre><originInfo><publisher>ELSEVIER</publisher><dateIssued encoding="w3cdtf">1967</dateIssued><copyrightDate encoding="w3cdtf">1967</copyrightDate></originInfo><language><languageTerm type="code" authority="iso639-2b">eng</languageTerm><languageTerm type="code" authority="rfc3066">en</languageTerm></language><abstract lang="en">Abstract: Chloroquine was administered to albino rats in the diet for 32 weeks at levels estimated to provide daily intakes of 1.9, 5.6, or 16.8 mg/kg. At the conclusion of the experiment the amount of drug retained in the tissues analyzed ranged from 28 to 37% of the intake for 1 day, and the order of increasing tissue concentrations was: muscle, eye, heart, liver = lung, kidney, and spleen. Hydroxychloroquine was similarly administered to albino rats for 30 weeks at levels estimated to provide daily intakes of 7.8, 19.4, or 48.4 mg/kg. At the conclusion of the experiment the amount of HCQ retained in the tissues ranged from 22 to 31% of the intake for 1 day and the order of increasing concentrations was generally: muscle, eye, heart, kidney, liver, lung, spleen. Chloroquine and desethylchloroquine were administered to albino and pigmented rats (by stomach tube) at a dosage of 40 mg/kg/day of base, 6 days per week for one month. Twenty-four hours after the last dose these animals also retained in the tissues analyzed amounts of these drugs equivalent to about 33% of one daily dose. The order of increasing tissue concentration of CQ in both strains at this time was essentially the same as previously reported (McChesney et al., 1965) except for a reversal of the positions of liver and lung. The order of increasing tissue concentration of desethylchloroquine in both strains was much the same as for chloroquine; i.e., in the albinos it was muscle, eye, heart, kidney, lung, liver = spleen; while in the pigmented rats it was muscle, heart, kidney, lung = liver, spleen, eye. The decrease in tissue concentrations of chloroquine following discontinuance of medication indicated a half-life of 1.5 days, while the corresponding data for desethylchloroquine indicated a half-life of 2.3 days. Tissue concentrations of both of these drugs were generally higher in the females than in the males, but in the case of chloroquine the difference was much more marked.</abstract><relatedItem type="host"><titleInfo><title>Toxicology and Applied Pharmacology</title></titleInfo><titleInfo type="abbreviated"><title>YTAAP</title></titleInfo><genre type="journal" authority="ISTEX" authorityURI="https://publication-type.data.istex.fr" valueURI="https://publication-type.data.istex.fr/ark:/67375/JMC-0GLKJH51-B">journal</genre><originInfo><publisher>ELSEVIER</publisher><dateIssued encoding="w3cdtf">1967</dateIssued></originInfo><identifier type="ISSN">0041-008X</identifier><identifier type="PII">S0041-008X(00)X0295-5</identifier><part><date>1967</date><detail type="volume"><number>10</number><caption>vol.</caption></detail><detail type="issue"><number>3</number><caption>no.</caption></detail><extent unit="issue-pages"><start>413</start><end>684</end></extent><extent unit="pages"><start>501</start><end>513</end></extent></part></relatedItem><identifier type="istex">D5F5D2915C7A5B862E5F4A337F1923A32EACC62A</identifier><identifier type="ark">ark:/67375/6H6-1XQQQ8KT-M</identifier><identifier type="DOI">10.1016/0041-008X(67)90089-0</identifier><identifier type="PII">0041-008X(67)90089-0</identifier><recordInfo><recordContentSource authority="ISTEX" authorityURI="https://loaded-corpus.data.istex.fr" valueURI="https://loaded-corpus.data.istex.fr/ark:/67375/XBH-HKKZVM7B-M">elsevier</recordContentSource></recordInfo></mods><json:item><extension>json</extension><original>false</original><mimetype>application/json</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-1XQQQ8KT-M/record.json</uri></json:item></metadata><serie></serie></istex></record>Pour manipuler ce document sous Unix (Dilib)
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