Pharmacologic actions of 4-aminoquinoline compounds
Identifieur interne : 000018 ( Istex/Corpus ); précédent : 000017; suivant : 000019Pharmacologic actions of 4-aminoquinoline compounds
Auteurs : Allen H. MackenzieSource :
- The American Journal of Medicine [ 0002-9343 ] ; 1983.
English descriptors
- Teeft :
- Acid hydrolases, American journal, Antimalarial, Antimalarial drugs, Arthritis, Arthritis rheum, Autophagic vacuoles, Biochem pharmacol, Cell biol, Cell surface, Cell surface receptors, Chloroquine, Chloroquine phosphate, Ciliary body, Cleveland clinic foundation, Clin, Concentration range, Dosage regimens, Early sign, Epithelium, Excessive dosage, Further studies, Higher concentrations, Human fibroblasts, Hydroxychloroquine, Hydroxychloroquine sulfate, Immunologic disease, Lysosomal, Lysosomal actions, Lysosomal function, Lysosomal storage disease, Lysosome, Macrophage, Pharmacologic actions, Plaquenil, Plasma membrane, Proc natl acad, Receptor, Retinal, Rheum, Rheumatoid, Rheumatoid arthritis, Rheumatologic effectiveness, Serum concentration, Serum levels, Side chain, Systemic lupus erythematosus, Toxicity, Vesicle, Vesicle fusion.
Abstract
Abstract: The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. Dosages ranging from 3.5 to 4.0 mg/kg per day for chloroquine and 6.0 to 6.5 mg/kg per day for hydroxychloroquine are clinically safe.
Url:
DOI: 10.1016/0002-9343(83)91264-0
Links to Exploration step
ISTEX:D5E8C31BA7999187B9DB886DF26381C86BDE3503Le document en format XML
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Mackenzie</name><affiliation><mods:affiliation>Cleveland, Ohio, USA</mods:affiliation></affiliation></author></analytic><monogr></monogr><series><title level="j">The American Journal of Medicine</title><title level="j" type="abbrev">AJM</title><idno type="ISSN">0002-9343</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1983">1983</date><biblScope unit="volume">75</biblScope><biblScope unit="issue">1</biblScope><biblScope unit="supplement">P1</biblScope><biblScope unit="page" from="5">5</biblScope><biblScope unit="page" to="10">10</biblScope></imprint><idno type="ISSN">0002-9343</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0002-9343</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Acid hydrolases</term><term>American journal</term><term>Antimalarial</term><term>Antimalarial drugs</term><term>Arthritis</term><term>Arthritis rheum</term><term>Autophagic vacuoles</term><term>Biochem pharmacol</term><term>Cell biol</term><term>Cell surface</term><term>Cell surface receptors</term><term>Chloroquine</term><term>Chloroquine phosphate</term><term>Ciliary body</term><term>Cleveland clinic foundation</term><term>Clin</term><term>Concentration range</term><term>Dosage regimens</term><term>Early sign</term><term>Epithelium</term><term>Excessive dosage</term><term>Further studies</term><term>Higher concentrations</term><term>Human fibroblasts</term><term>Hydroxychloroquine</term><term>Hydroxychloroquine sulfate</term><term>Immunologic disease</term><term>Lysosomal</term><term>Lysosomal actions</term><term>Lysosomal function</term><term>Lysosomal storage disease</term><term>Lysosome</term><term>Macrophage</term><term>Pharmacologic actions</term><term>Plaquenil</term><term>Plasma membrane</term><term>Proc natl acad</term><term>Receptor</term><term>Retinal</term><term>Rheum</term><term>Rheumatoid</term><term>Rheumatoid arthritis</term><term>Rheumatologic effectiveness</term><term>Serum concentration</term><term>Serum levels</term><term>Side chain</term><term>Systemic lupus erythematosus</term><term>Toxicity</term><term>Vesicle</term><term>Vesicle fusion</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Abstract: The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. Dosages ranging from 3.5 to 4.0 mg/kg per day for chloroquine and 6.0 to 6.5 mg/kg per day for hydroxychloroquine are clinically safe.</div></front></TEI><istex><corpusName>elsevier</corpusName><keywords><teeft><json:string>chloroquine</json:string><json:string>vesicle</json:string><json:string>receptor</json:string><json:string>lysosomal</json:string><json:string>antimalarial</json:string><json:string>hydroxychloroquine</json:string><json:string>lysosome</json:string><json:string>arthritis rheum</json:string><json:string>rheumatoid arthritis</json:string><json:string>epithelium</json:string><json:string>rheumatoid</json:string><json:string>rheum</json:string><json:string>clin</json:string><json:string>macrophage</json:string><json:string>plaquenil</json:string><json:string>toxicity</json:string><json:string>vesicle fusion</json:string><json:string>american journal</json:string><json:string>higher concentrations</json:string><json:string>arthritis</json:string><json:string>antimalarial drugs</json:string><json:string>biochem pharmacol</json:string><json:string>cell surface</json:string><json:string>hydroxychloroquine sulfate</json:string><json:string>cell biol</json:string><json:string>systemic lupus erythematosus</json:string><json:string>chloroquine phosphate</json:string><json:string>autophagic vacuoles</json:string><json:string>retinal</json:string><json:string>side chain</json:string><json:string>serum concentration</json:string><json:string>immunologic disease</json:string><json:string>concentration range</json:string><json:string>cleveland clinic foundation</json:string><json:string>rheumatologic effectiveness</json:string><json:string>early sign</json:string><json:string>excessive dosage</json:string><json:string>plasma membrane</json:string><json:string>cell surface receptors</json:string><json:string>acid hydrolases</json:string><json:string>lysosomal function</json:string><json:string>lysosomal storage disease</json:string><json:string>pharmacologic actions</json:string><json:string>lysosomal actions</json:string><json:string>dosage regimens</json:string><json:string>ciliary body</json:string><json:string>further studies</json:string><json:string>human fibroblasts</json:string><json:string>serum levels</json:string><json:string>proc natl acad</json:string></teeft></keywords><author><json:item><name>Allen H. Mackenzie M.D.</name><affiliations><json:string>Cleveland, Ohio, USA</json:string></affiliations></json:item></author><articleId><json:string>83912640</json:string></articleId><arkIstex>ark:/67375/6H6-QJ3RBWS1-Q</arkIstex><language><json:string>eng</json:string></language><originalGenre><json:string>Full-length article</json:string></originalGenre><abstract>Abstract: The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. 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Mackenzie, Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio 44106.</note><note type="biography">From the Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, Cleveland, Ohio.</note><affiliation>Requests for reprints should be addressed to Dr. Allen H. Mackenzie, Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio 44106.</affiliation><affiliation>From the Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, Cleveland, Ohio.</affiliation><affiliation>Cleveland, Ohio, USA</affiliation></author><idno type="istex">D5E8C31BA7999187B9DB886DF26381C86BDE3503</idno><idno type="ark">ark:/67375/6H6-QJ3RBWS1-Q</idno><idno type="DOI">10.1016/0002-9343(83)91264-0</idno><idno type="PII">0002-9343(83)91264-0</idno><idno type="article-id">83912640</idno></analytic><monogr><title level="j">The American Journal of Medicine</title><title level="j" type="abbrev">AJM</title><idno type="pISSN">0002-9343</idno><idno type="PII">S0002-9343(00)X0600-6</idno><meeting><addName>A Reassessment of Plaquenil in the Treatment of Rheumatoid Arthritis, Cleveland, Ohio</addName><date>19821203</date></meeting><imprint><publisher>ELSEVIER</publisher><date type="published" when="1983"></date><biblScope unit="volume">75</biblScope><biblScope unit="issue">1</biblScope><biblScope unit="supplement">P1</biblScope><biblScope unit="page" from="5">5</biblScope><biblScope unit="page" to="10">10</biblScope></imprint></monogr></biblStruct></sourceDesc></fileDesc><profileDesc><creation><date>1983</date></creation><langUsage><language ident="en">en</language></langUsage><abstract xml:lang="en"><p>Abstract: The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. Dosages ranging from 3.5 to 4.0 mg/kg per day for chloroquine and 6.0 to 6.5 mg/kg per day for hydroxychloroquine are clinically safe.</p></abstract></profileDesc><revisionDesc><change when="1983">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-QJ3RBWS1-Q/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" xml:lang="en"><item-info><jid>AJM</jid><aid>83912640</aid><ce:pii>0002-9343(83)91264-0</ce:pii><ce:doi>10.1016/0002-9343(83)91264-0</ce:doi><ce:copyright type="unknown" year="1983"></ce:copyright></item-info><head><ce:title>Pharmacologic actions of 4-aminoquinoline compounds</ce:title><ce:author-group><ce:author><ce:given-name>Allen H.</ce:given-name><ce:surname>Mackenzie</ce:surname><ce:degrees>M.D.</ce:degrees><ce:cross-ref refid="COR1"><ce:sup loc="post">∗</ce:sup></ce:cross-ref><ce:cross-ref refid="FN1"><ce:sup loc="post">1</ce:sup></ce:cross-ref></ce:author><ce:affiliation><ce:textfn>Cleveland, Ohio, USA</ce:textfn></ce:affiliation><ce:correspondence id="COR1"><ce:label>∗</ce:label><ce:text>Requests for reprints should be addressed to Dr. Allen H. Mackenzie, Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio 44106.</ce:text></ce:correspondence><ce:footnote id="FN1"><ce:label>1</ce:label><ce:note-para>From the Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, Cleveland, Ohio.</ce:note-para></ce:footnote></ce:author-group><ce:abstract class="author"><ce:section-title>Abstract</ce:section-title><ce:abstract-sec><ce:simple-para view="all" id="simple-para.0010">The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. Dosages ranging from 3.5 to 4.0 mg/kg per day for chloroquine and 6.0 to 6.5 mg/kg per day for hydroxychloroquine are clinically safe.</ce:simple-para></ce:abstract-sec></ce:abstract></head></converted-article></istex:document></istex:metadataXml><mods version="3.6"><titleInfo lang="en"><title>Pharmacologic actions of 4-aminoquinoline compounds</title></titleInfo><titleInfo type="alternative" lang="en" contentType="CDATA"><title>Pharmacologic actions of 4-aminoquinoline compounds</title></titleInfo><name type="personal"><namePart type="given">Allen H.</namePart><namePart type="family">Mackenzie</namePart><namePart type="termsOfAddress">M.D.</namePart><affiliation>Cleveland, Ohio, USA</affiliation><description>Requests for reprints should be addressed to Dr. Allen H. Mackenzie, Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, 9500 Euclid Avenue, Cleveland, Ohio 44106.</description><description>From the Department of Rheumatic and Immunologic Disease, Cleveland Clinic Foundation, Cleveland, Ohio.</description><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">1983</dateIssued><copyrightDate encoding="w3cdtf">1983</copyrightDate></originInfo><language><languageTerm type="code" authority="iso639-2b">eng</languageTerm><languageTerm type="code" authority="rfc3066">en</languageTerm></language><abstract lang="en">Abstract: The pharmacokinetics, physiologic effects, and the metabolization of chloroquine and hydroxychloroquine are all similar. Their concentrations in plasma and tissue are directly related to daily dosing. The highest concentrations are found in melanin-containing tissues, particularly the choroid and ciliary body of the eye. The pharmacologic effects of 4-aminoquinoline compounds are reviewed in detail. It is likely that the rheumatologic effectiveness of these agents is primarily related to lysosomal actions. The drug-induced lysosomal abnormalities include diminished vesicle fusion, diminished exocytosis, and reversible “lysosomal storage disease.” It is likely that the retinal toxicity of these drugs is one manifestation of the altered lysosomal physiology involving the retinal pigmented epithelium. Tissue of retinal pigmented epithelium is similar to that of the bone-marrow-derived macrophage. Depression of extra-oculogram is an early sign of excessive dosage and can be used to measure potential toxicity during therapy with 4-aminoquinolines. 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