Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria
Multiple dose pharmacokinetics of artemether and dihydroartemisinin were investigated in chinese patients treated for malaria. They received over 2 days either 4×80 mg artemether orally ( n=48) or 4×80–480 mg co-artemether ( n=40), a combination of artemether and lumefantrine (benflumetol). Lag time...
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| Veröffentlicht in: | International journal of antimicrobial agents 1999-07, Vol.12 (2), p.151-158 |
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| container_title | International journal of antimicrobial agents |
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| creator | van Agtmael, M.A Cheng-Qi, Shan Qing, Jiao Xiu Mull, R van Boxtel, C.J |
| description | Multiple dose pharmacokinetics of artemether and dihydroartemisinin were investigated in chinese patients treated for malaria. They received over 2 days either 4×80 mg artemether orally (
n=48) or 4×80–480 mg co-artemether (
n=40), a combination of artemether and lumefantrine (benflumetol). Lag time=0.48 h (mean),
C
max after first dose=157 ng/ml,
t
max=1.73 h and elimination half-life=1.16 h. The lag and absorption times were 0.5 h longer for co-artemether compared with artemether. Dihydroartemisinin paralleled artemether pharmacokinetics. Artemether
C
max after the last dose was one-third of the
C
max after the first dose while, inversely, dihydroartemisinin
C
max increased over time. We suggest that auto-induction of gut mucosa enzymes and/or liver enzymes causes a time-dependent increase in first-pass metabolisation of artemether. |
| doi_str_mv | 10.1016/S0924-8579(99)00063-1 |
| format | Article |
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n=48) or 4×80–480 mg co-artemether (
n=40), a combination of artemether and lumefantrine (benflumetol). Lag time=0.48 h (mean),
C
max after first dose=157 ng/ml,
t
max=1.73 h and elimination half-life=1.16 h. The lag and absorption times were 0.5 h longer for co-artemether compared with artemether. Dihydroartemisinin paralleled artemether pharmacokinetics. Artemether
C
max after the last dose was one-third of the
C
max after the first dose while, inversely, dihydroartemisinin
C
max increased over time. We suggest that auto-induction of gut mucosa enzymes and/or liver enzymes causes a time-dependent increase in first-pass metabolisation of artemether.</description><identifier>ISSN: 0924-8579</identifier><identifier>EISSN: 1872-7913</identifier><identifier>DOI: 10.1016/S0924-8579(99)00063-1</identifier><identifier>PMID: 10418761</identifier><language>eng</language><publisher>London: Elsevier B.V</publisher><subject>Adolescent ; Adult ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antimalarials - pharmacokinetics ; Antimalarials - therapeutic use ; Antiparasitic agents ; Artemether ; Artemisinins ; Auto-induction ; Benflumetol ; Biological and medical sciences ; China ; Double-Blind Method ; Drug Evaluation ; Drug Therapy, Combination ; Ethanolamines - pharmacokinetics ; Ethanolamines - therapeutic use ; Female ; Fluorenes - pharmacokinetics ; Fluorenes - therapeutic use ; General pharmacology ; Humans ; Lumefantrine ; Malaria ; Malaria, Falciparum - blood ; Malaria, Falciparum - drug therapy ; Male ; Medical sciences ; Middle Aged ; Models, Chemical ; Pharmacognosy. Homeopathy. Health food ; Pharmacokinetics ; Pharmacology. Drug treatments ; Plasmodium falciparum ; Sesquiterpenes - pharmacokinetics ; Sesquiterpenes - therapeutic use ; Time Factors</subject><ispartof>International journal of antimicrobial agents, 1999-07, Vol.12 (2), p.151-158</ispartof><rights>1999 Elsevier Science B.V.</rights><rights>1999 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c421t-7d46cb970890b69529687745cd675d367868b5320cf083699be6f073482503923</citedby><cites>FETCH-LOGICAL-c421t-7d46cb970890b69529687745cd675d367868b5320cf083699be6f073482503923</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0924-8579(99)00063-1$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,777,781,3537,27905,27906,45976</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1899406$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10418761$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>van Agtmael, M.A</creatorcontrib><creatorcontrib>Cheng-Qi, Shan</creatorcontrib><creatorcontrib>Qing, Jiao Xiu</creatorcontrib><creatorcontrib>Mull, R</creatorcontrib><creatorcontrib>van Boxtel, C.J</creatorcontrib><title>Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria</title><title>International journal of antimicrobial agents</title><addtitle>Int J Antimicrob Agents</addtitle><description>Multiple dose pharmacokinetics of artemether and dihydroartemisinin were investigated in chinese patients treated for malaria. They received over 2 days either 4×80 mg artemether orally (
n=48) or 4×80–480 mg co-artemether (
n=40), a combination of artemether and lumefantrine (benflumetol). Lag time=0.48 h (mean),
C
max after first dose=157 ng/ml,
t
max=1.73 h and elimination half-life=1.16 h. The lag and absorption times were 0.5 h longer for co-artemether compared with artemether. Dihydroartemisinin paralleled artemether pharmacokinetics. Artemether
C
max after the last dose was one-third of the
C
max after the first dose while, inversely, dihydroartemisinin
C
max increased over time. We suggest that auto-induction of gut mucosa enzymes and/or liver enzymes causes a time-dependent increase in first-pass metabolisation of artemether.</description><subject>Adolescent</subject><subject>Adult</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antimalarials - pharmacokinetics</subject><subject>Antimalarials - therapeutic use</subject><subject>Antiparasitic agents</subject><subject>Artemether</subject><subject>Artemisinins</subject><subject>Auto-induction</subject><subject>Benflumetol</subject><subject>Biological and medical sciences</subject><subject>China</subject><subject>Double-Blind Method</subject><subject>Drug Evaluation</subject><subject>Drug Therapy, Combination</subject><subject>Ethanolamines - pharmacokinetics</subject><subject>Ethanolamines - therapeutic use</subject><subject>Female</subject><subject>Fluorenes - pharmacokinetics</subject><subject>Fluorenes - therapeutic use</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Lumefantrine</subject><subject>Malaria</subject><subject>Malaria, Falciparum - blood</subject><subject>Malaria, Falciparum - drug therapy</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>Models, Chemical</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Plasmodium falciparum</subject><subject>Sesquiterpenes - pharmacokinetics</subject><subject>Sesquiterpenes - therapeutic use</subject><subject>Time Factors</subject><issn>0924-8579</issn><issn>1872-7913</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEurFDEQRoMo3nH0JyhZiOiiNek8ayUy-IIrLtR1SKermWi_TNKK_97MnUHduSqoOl9VcQh5yNlzzrh-8YlBKxurDDwFeMYY06Lht8iOW9M2Bri4TXZ_kCtyL-evjHElpLpLrjiTldN8R4YP21jiOiLtl4x0Pfo0-bB8izOWGDJdBupTwQnLERONMz0c6-hE-hJxLpn-jOVItzks0zrG4Av2dPBjiKtP20QnP_oU_X1ypzYzPrjUPfny5vXnw7vm-uPb94dX102QLS-N6aUOHRhmgXUaVAvaGiNV6LVRvdDGatsp0bIwMCs0QId6YEZI2yomoBV78uS8d03L9w1zcVPMAcfRz7hs2XHTaqskVFCdwZCWnBMObk1x8umX48ydBLsbwe5kzwG4G8GO19yjy4Gtm7D_J3U2WoHHF8Dn4Mch-TnE_JezALKu2pOXZwyrjR8Rk8uh-gzYx4ShuH6J__nkN6Yzl30</recordid><startdate>19990701</startdate><enddate>19990701</enddate><creator>van Agtmael, M.A</creator><creator>Cheng-Qi, Shan</creator><creator>Qing, Jiao Xiu</creator><creator>Mull, R</creator><creator>van Boxtel, C.J</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</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><scope>M7N</scope></search><sort><creationdate>19990701</creationdate><title>Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria</title><author>van Agtmael, M.A ; Cheng-Qi, Shan ; Qing, Jiao Xiu ; Mull, R ; van Boxtel, C.J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c421t-7d46cb970890b69529687745cd675d367868b5320cf083699be6f073482503923</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Adolescent</topic><topic>Adult</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antimalarials - pharmacokinetics</topic><topic>Antimalarials - therapeutic use</topic><topic>Antiparasitic agents</topic><topic>Artemether</topic><topic>Artemisinins</topic><topic>Auto-induction</topic><topic>Benflumetol</topic><topic>Biological and medical sciences</topic><topic>China</topic><topic>Double-Blind Method</topic><topic>Drug Evaluation</topic><topic>Drug Therapy, Combination</topic><topic>Ethanolamines - pharmacokinetics</topic><topic>Ethanolamines - therapeutic use</topic><topic>Female</topic><topic>Fluorenes - pharmacokinetics</topic><topic>Fluorenes - therapeutic use</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Lumefantrine</topic><topic>Malaria</topic><topic>Malaria, Falciparum - blood</topic><topic>Malaria, Falciparum - drug therapy</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>Models, Chemical</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Plasmodium falciparum</topic><topic>Sesquiterpenes - pharmacokinetics</topic><topic>Sesquiterpenes - therapeutic use</topic><topic>Time Factors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>van Agtmael, M.A</creatorcontrib><creatorcontrib>Cheng-Qi, Shan</creatorcontrib><creatorcontrib>Qing, Jiao Xiu</creatorcontrib><creatorcontrib>Mull, R</creatorcontrib><creatorcontrib>van Boxtel, C.J</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><jtitle>International journal of antimicrobial agents</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>van Agtmael, M.A</au><au>Cheng-Qi, Shan</au><au>Qing, Jiao Xiu</au><au>Mull, R</au><au>van Boxtel, C.J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria</atitle><jtitle>International journal of antimicrobial agents</jtitle><addtitle>Int J Antimicrob Agents</addtitle><date>1999-07-01</date><risdate>1999</risdate><volume>12</volume><issue>2</issue><spage>151</spage><epage>158</epage><pages>151-158</pages><issn>0924-8579</issn><eissn>1872-7913</eissn><abstract>Multiple dose pharmacokinetics of artemether and dihydroartemisinin were investigated in chinese patients treated for malaria. They received over 2 days either 4×80 mg artemether orally (
n=48) or 4×80–480 mg co-artemether (
n=40), a combination of artemether and lumefantrine (benflumetol). Lag time=0.48 h (mean),
C
max after first dose=157 ng/ml,
t
max=1.73 h and elimination half-life=1.16 h. The lag and absorption times were 0.5 h longer for co-artemether compared with artemether. Dihydroartemisinin paralleled artemether pharmacokinetics. Artemether
C
max after the last dose was one-third of the
C
max after the first dose while, inversely, dihydroartemisinin
C
max increased over time. We suggest that auto-induction of gut mucosa enzymes and/or liver enzymes causes a time-dependent increase in first-pass metabolisation of artemether.</abstract><cop>London</cop><cop>Amsterdam</cop><cop>New York, NY</cop><pub>Elsevier B.V</pub><pmid>10418761</pmid><doi>10.1016/S0924-8579(99)00063-1</doi><tpages>8</tpages></addata></record> |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Adolescent Adult Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarials - pharmacokinetics Antimalarials - therapeutic use Antiparasitic agents Artemether Artemisinins Auto-induction Benflumetol Biological and medical sciences China Double-Blind Method Drug Evaluation Drug Therapy, Combination Ethanolamines - pharmacokinetics Ethanolamines - therapeutic use Female Fluorenes - pharmacokinetics Fluorenes - therapeutic use General pharmacology Humans Lumefantrine Malaria Malaria, Falciparum - blood Malaria, Falciparum - drug therapy Male Medical sciences Middle Aged Models, Chemical Pharmacognosy. Homeopathy. Health food Pharmacokinetics Pharmacology. Drug treatments Plasmodium falciparum Sesquiterpenes - pharmacokinetics Sesquiterpenes - therapeutic use Time Factors |
| title | Multiple dose pharmacokinetics of artemether in Chinese patients with uncomplicated falciparum malaria |
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