Absorption, pharmacokinetics and excretion of levovirin in rats, dogs and Cynomolgus monkeys
The absorption, pharmacokinetics and excretion of levovirin were studied in Sprague–Dawley rats (30 mg/kg) and Beagle dogs (30 mg/kg) following intravenous (iv) and oral administration of [3H]levovirin, and in Cynomolgus monkeys following iv and oral administration of [14C]levovirin. Oral absorption...
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| Veröffentlicht in: | Journal of antimicrobial chemotherapy 2003-01, Vol.51 (1), p.93-99 |
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| creator | Lin, Chin-Chung Luu, Trong Lourenco, David Yeh, Li-Tain Lau, Johnson Y. N. |
| description | The absorption, pharmacokinetics and excretion of levovirin were studied in Sprague–Dawley rats (30 mg/kg) and Beagle dogs (30 mg/kg) following intravenous (iv) and oral administration of [3H]levovirin, and in Cynomolgus monkeys following iv and oral administration of [14C]levovirin. Oral absorption was 31.3% in rats, 67.3% in dogs and 17.5% in monkeys, and the bioavailability was 29.3% in rats, 51.3% in dogs and 18.4% in monkeys. After iv administration, the elimination half-life (t1/2) was 1.47 h in rats, 3.70 h in dogs and 3.50 h in monkeys. The total body clearance was 8.24, 2.96 and 2.58 mL/min per kg, respectively, in rats, dogs and monkeys and the apparent volume of distribution was 0.79, 0.95 and 0.65 L/kg. No metabolite was detected in plasma or urine of rats, dogs or monkeys, indicating negligible metabolism of levovirin in these animals. Excretion of total radioactivity in urine after oral dosing accounted for 15.4% of the administered dose in rats, 49.9% in dogs and 21.4% in monkeys. Biliary excretion did not play a significant role in the elimination of levovirin. |
| doi_str_mv | 10.1093/jac/dkg046 |
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N.</creator><creatorcontrib>Lin, Chin-Chung ; Luu, Trong ; Lourenco, David ; Yeh, Li-Tain ; Lau, Johnson Y. N.</creatorcontrib><description>The absorption, pharmacokinetics and excretion of levovirin were studied in Sprague–Dawley rats (30 mg/kg) and Beagle dogs (30 mg/kg) following intravenous (iv) and oral administration of [3H]levovirin, and in Cynomolgus monkeys following iv and oral administration of [14C]levovirin. Oral absorption was 31.3% in rats, 67.3% in dogs and 17.5% in monkeys, and the bioavailability was 29.3% in rats, 51.3% in dogs and 18.4% in monkeys. After iv administration, the elimination half-life (t1/2) was 1.47 h in rats, 3.70 h in dogs and 3.50 h in monkeys. The total body clearance was 8.24, 2.96 and 2.58 mL/min per kg, respectively, in rats, dogs and monkeys and the apparent volume of distribution was 0.79, 0.95 and 0.65 L/kg. No metabolite was detected in plasma or urine of rats, dogs or monkeys, indicating negligible metabolism of levovirin in these animals. Excretion of total radioactivity in urine after oral dosing accounted for 15.4% of the administered dose in rats, 49.9% in dogs and 21.4% in monkeys. Biliary excretion did not play a significant role in the elimination of levovirin.</description><identifier>ISSN: 0305-7453</identifier><identifier>ISSN: 1460-2091</identifier><identifier>EISSN: 1460-2091</identifier><identifier>DOI: 10.1093/jac/dkg046</identifier><identifier>PMID: 12493792</identifier><identifier>CODEN: JACHDX</identifier><language>eng</language><publisher>Oxford: Oxford University Press</publisher><subject>Absorption - drug effects ; Absorption - physiology ; Administration, Oral ; Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiviral agents ; Biological and medical sciences ; Biological Availability ; Dogs ; Feces - chemistry ; hepatitis C ; Injections, Intravenous ; levovirin ; Macaca fascicularis ; Male ; Medical sciences ; metabolism ; pharmacokinetics ; Pharmacology. Drug treatments ; Rats ; Rats, Sprague-Dawley ; Ribavirin - administration & dosage ; Ribavirin - blood ; Ribavirin - pharmacokinetics ; Ribavirin - urine ; Stereoisomerism</subject><ispartof>Journal of antimicrobial chemotherapy, 2003-01, Vol.51 (1), p.93-99</ispartof><rights>2003 INIST-CNRS</rights><rights>Copyright Oxford University Press(England) Jan 2003</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c445t-2a25617f2722cf82f3bd4e20ebcbe5f8447920430f2cd46c0cb9813d5ea0740e3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,4009,27902,27903,27904</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14482567$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12493792$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lin, Chin-Chung</creatorcontrib><creatorcontrib>Luu, Trong</creatorcontrib><creatorcontrib>Lourenco, David</creatorcontrib><creatorcontrib>Yeh, Li-Tain</creatorcontrib><creatorcontrib>Lau, Johnson Y. N.</creatorcontrib><title>Absorption, pharmacokinetics and excretion of levovirin in rats, dogs and Cynomolgus monkeys</title><title>Journal of antimicrobial chemotherapy</title><addtitle>J. Antimicrob. Chemother</addtitle><description>The absorption, pharmacokinetics and excretion of levovirin were studied in Sprague–Dawley rats (30 mg/kg) and Beagle dogs (30 mg/kg) following intravenous (iv) and oral administration of [3H]levovirin, and in Cynomolgus monkeys following iv and oral administration of [14C]levovirin. Oral absorption was 31.3% in rats, 67.3% in dogs and 17.5% in monkeys, and the bioavailability was 29.3% in rats, 51.3% in dogs and 18.4% in monkeys. After iv administration, the elimination half-life (t1/2) was 1.47 h in rats, 3.70 h in dogs and 3.50 h in monkeys. The total body clearance was 8.24, 2.96 and 2.58 mL/min per kg, respectively, in rats, dogs and monkeys and the apparent volume of distribution was 0.79, 0.95 and 0.65 L/kg. No metabolite was detected in plasma or urine of rats, dogs or monkeys, indicating negligible metabolism of levovirin in these animals. Excretion of total radioactivity in urine after oral dosing accounted for 15.4% of the administered dose in rats, 49.9% in dogs and 21.4% in monkeys. Biliary excretion did not play a significant role in the elimination of levovirin.</description><subject>Absorption - drug effects</subject><subject>Absorption - physiology</subject><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Dogs</subject><subject>Feces - chemistry</subject><subject>hepatitis C</subject><subject>Injections, Intravenous</subject><subject>levovirin</subject><subject>Macaca fascicularis</subject><subject>Male</subject><subject>Medical sciences</subject><subject>metabolism</subject><subject>pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Ribavirin - administration & dosage</subject><subject>Ribavirin - blood</subject><subject>Ribavirin - pharmacokinetics</subject><subject>Ribavirin - urine</subject><subject>Stereoisomerism</subject><issn>0305-7453</issn><issn>1460-2091</issn><issn>1460-2091</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0ctq3DAUBmBRWppJ0k0foJhCsyhxo6slL5NJ00kJZNELoRSELEtTzdjSVLJD5u2jwUMC3RQEWpyPI53zA_AWwU8I1uRspfRZu15CWr0AM0QrWGJYo5dgBglkJaeMHIDDlFYQwopV4jU4QJjWhNd4Bn6fNynEzeCCPy02f1TslQ5r583gdCqUbwvzoKPZ1Ytgi87ch3sXnS_yiWpIp0UblhOcb33oQ7ccU9EHvzbbdAxeWdUl82Z_H4EfV5-_zxflze2X6_n5TakpZUOJFWYV4hZzjLUV2JKmpQZD0-jGMCsozV-FlECLdUsrDXVTC0RaZhTkFBpyBE6mvpsY_o4mDbJ3SZuuU96EMUmOheAk7-F_EAlRY85whu__gaswRp-HkBjxShCKeEYfJ6RjSCkaKzfR9SpuJYJyl4zMycgpmYzf7TuOTW_aZ7qPIoMPe6CSVp2NymuXnh2lIq9p92o5OZcG8_BUV3Etc5Uzubj7Jb_-ZJdk8e1OXpBHZdemNQ</recordid><startdate>200301</startdate><enddate>200301</enddate><creator>Lin, Chin-Chung</creator><creator>Luu, Trong</creator><creator>Lourenco, David</creator><creator>Yeh, Li-Tain</creator><creator>Lau, Johnson Y. N.</creator><general>Oxford University Press</general><general>Oxford Publishing Limited (England)</general><scope>BSCLL</scope><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>7QL</scope><scope>7QO</scope><scope>7T7</scope><scope>7U7</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>NAPCQ</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>200301</creationdate><title>Absorption, pharmacokinetics and excretion of levovirin in rats, dogs and Cynomolgus monkeys</title><author>Lin, Chin-Chung ; Luu, Trong ; Lourenco, David ; Yeh, Li-Tain ; Lau, Johnson Y. N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c445t-2a25617f2722cf82f3bd4e20ebcbe5f8447920430f2cd46c0cb9813d5ea0740e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Absorption - drug effects</topic><topic>Absorption - physiology</topic><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antiviral agents</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Dogs</topic><topic>Feces - chemistry</topic><topic>hepatitis C</topic><topic>Injections, Intravenous</topic><topic>levovirin</topic><topic>Macaca fascicularis</topic><topic>Male</topic><topic>Medical sciences</topic><topic>metabolism</topic><topic>pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Ribavirin - administration & dosage</topic><topic>Ribavirin - blood</topic><topic>Ribavirin - pharmacokinetics</topic><topic>Ribavirin - urine</topic><topic>Stereoisomerism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lin, Chin-Chung</creatorcontrib><creatorcontrib>Luu, Trong</creatorcontrib><creatorcontrib>Lourenco, David</creatorcontrib><creatorcontrib>Yeh, Li-Tain</creatorcontrib><creatorcontrib>Lau, Johnson Y. 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N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Absorption, pharmacokinetics and excretion of levovirin in rats, dogs and Cynomolgus monkeys</atitle><jtitle>Journal of antimicrobial chemotherapy</jtitle><addtitle>J. Antimicrob. Chemother</addtitle><date>2003-01</date><risdate>2003</risdate><volume>51</volume><issue>1</issue><spage>93</spage><epage>99</epage><pages>93-99</pages><issn>0305-7453</issn><issn>1460-2091</issn><eissn>1460-2091</eissn><coden>JACHDX</coden><abstract>The absorption, pharmacokinetics and excretion of levovirin were studied in Sprague–Dawley rats (30 mg/kg) and Beagle dogs (30 mg/kg) following intravenous (iv) and oral administration of [3H]levovirin, and in Cynomolgus monkeys following iv and oral administration of [14C]levovirin. Oral absorption was 31.3% in rats, 67.3% in dogs and 17.5% in monkeys, and the bioavailability was 29.3% in rats, 51.3% in dogs and 18.4% in monkeys. After iv administration, the elimination half-life (t1/2) was 1.47 h in rats, 3.70 h in dogs and 3.50 h in monkeys. The total body clearance was 8.24, 2.96 and 2.58 mL/min per kg, respectively, in rats, dogs and monkeys and the apparent volume of distribution was 0.79, 0.95 and 0.65 L/kg. No metabolite was detected in plasma or urine of rats, dogs or monkeys, indicating negligible metabolism of levovirin in these animals. Excretion of total radioactivity in urine after oral dosing accounted for 15.4% of the administered dose in rats, 49.9% in dogs and 21.4% in monkeys. Biliary excretion did not play a significant role in the elimination of levovirin.</abstract><cop>Oxford</cop><pub>Oxford University Press</pub><pmid>12493792</pmid><doi>10.1093/jac/dkg046</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Absorption - drug effects Absorption - physiology Administration, Oral Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences Biological Availability Dogs Feces - chemistry hepatitis C Injections, Intravenous levovirin Macaca fascicularis Male Medical sciences metabolism pharmacokinetics Pharmacology. Drug treatments Rats Rats, Sprague-Dawley Ribavirin - administration & dosage Ribavirin - blood Ribavirin - pharmacokinetics Ribavirin - urine Stereoisomerism |
| title | Absorption, pharmacokinetics and excretion of levovirin in rats, dogs and Cynomolgus monkeys |
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