Pharmacokinetics of Fluconazole and Fosfluconazole after Intraperitoneal Administration to Peritoneal Dialysis Rats
Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD)...
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| Veröffentlicht in: | DRUG METABOLISM AND PHARMACOKINETICS 2005, Vol.20 (6), p.485-490 |
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| container_title | DRUG METABOLISM AND PHARMACOKINETICS |
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| creator | Aoyama, Takahiko Ogata, Kazuhiro Shimizu, Makiko Hatta, Shigeo Masuhara, Keiso Shima, Yoshinori Kimura, Kenjirou Matsumoto, Yoshiaki |
| description | Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study were to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations were analyzed using a two-compartment model in which the distribution volume of the peripheral compartment was fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients. |
| doi_str_mv | 10.2133/dmpk.20.485 |
| format | Article |
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Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study were to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations were analyzed using a two-compartment model in which the distribution volume of the peripheral compartment was fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients.</description><identifier>ISSN: 1347-4367</identifier><identifier>EISSN: 1880-0920</identifier><identifier>DOI: 10.2133/dmpk.20.485</identifier><identifier>PMID: 16415533</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Acute Kidney Injury - metabolism ; Algorithms ; Alkaline Phosphatase - metabolism ; Animals ; Antifungal Agents - administration & dosage ; Antifungal Agents - pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Data Interpretation, Statistical ; fluconazole ; Fluconazole - administration & dosage ; Fluconazole - analogs & derivatives ; Fluconazole - pharmacokinetics ; fosfluconazole ; Injections, Intraperitoneal ; Injections, Intravenous ; intraperitoneal administration ; Male ; Organophosphates - administration & dosage ; Organophosphates - pharmacokinetics ; peritoneal dialysis ; Peritoneal Dialysis, Continuous Ambulatory ; rat ; Rats ; Rats, Wistar</subject><ispartof>DRUG METABOLISM AND PHARMACOKINETICS, 2005, Vol.20 (6), p.485-490</ispartof><rights>2005 The Japanese Society for the Study of Xenobiotics</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c502t-4268fb6da98fdf14595603225f20b9f0da14511c126d064fe02a4c1bef76fb7f3</citedby><cites>FETCH-LOGICAL-c502t-4268fb6da98fdf14595603225f20b9f0da14511c126d064fe02a4c1bef76fb7f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,4010,27900,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16415533$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Aoyama, Takahiko</creatorcontrib><creatorcontrib>Ogata, Kazuhiro</creatorcontrib><creatorcontrib>Shimizu, Makiko</creatorcontrib><creatorcontrib>Hatta, Shigeo</creatorcontrib><creatorcontrib>Masuhara, Keiso</creatorcontrib><creatorcontrib>Shima, Yoshinori</creatorcontrib><creatorcontrib>Kimura, Kenjirou</creatorcontrib><creatorcontrib>Matsumoto, Yoshiaki</creatorcontrib><creatorcontrib>School of Medicine</creatorcontrib><creatorcontrib>School of Medicine and Hospital</creatorcontrib><creatorcontrib>Showa Pharmaceutical University</creatorcontrib><creatorcontrib>Department of Clinical Pharmacology and Toxicology</creatorcontrib><creatorcontrib>St. Marianna University</creatorcontrib><creatorcontrib>Department of Pharmacy</creatorcontrib><creatorcontrib>Division of Nephrology and Hypertension</creatorcontrib><creatorcontrib>College of Pharmacy</creatorcontrib><creatorcontrib>Nihon University</creatorcontrib><title>Pharmacokinetics of Fluconazole and Fosfluconazole after Intraperitoneal Administration to Peritoneal Dialysis Rats</title><title>DRUG METABOLISM AND PHARMACOKINETICS</title><addtitle>Drug Metab Pharmacokinet</addtitle><description>Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study were to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations were analyzed using a two-compartment model in which the distribution volume of the peripheral compartment was fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients.</description><subject>Acute Kidney Injury - metabolism</subject><subject>Algorithms</subject><subject>Alkaline Phosphatase - metabolism</subject><subject>Animals</subject><subject>Antifungal Agents - administration & dosage</subject><subject>Antifungal Agents - pharmacokinetics</subject><subject>Area Under Curve</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Data Interpretation, Statistical</subject><subject>fluconazole</subject><subject>Fluconazole - administration & dosage</subject><subject>Fluconazole - analogs & derivatives</subject><subject>Fluconazole - pharmacokinetics</subject><subject>fosfluconazole</subject><subject>Injections, Intraperitoneal</subject><subject>Injections, Intravenous</subject><subject>intraperitoneal administration</subject><subject>Male</subject><subject>Organophosphates - administration & dosage</subject><subject>Organophosphates - pharmacokinetics</subject><subject>peritoneal dialysis</subject><subject>Peritoneal Dialysis, Continuous Ambulatory</subject><subject>rat</subject><subject>Rats</subject><subject>Rats, Wistar</subject><issn>1347-4367</issn><issn>1880-0920</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkE1rFTEUhoMo9kNX7mVWbmRuT5JJZmZZWq8WCi3SrkMmH5h2JrkmmUL99Z5yL9SFm7zhnIeH5CXkE4UNo5yf2WX3uGGw6QbxhhzTYYAWRgZv8c67vu247I_ISSkPAJyLjr0nR1R2VAjOj0m5_aXzok16DNHVYEqTfLOdV5Oi_pNm1-hom20q_t-Rry43V7FmvXM51BSdnptzu4QYCg5rSLGpqbl9XV4GPT-XUJqfupYP5J3Xc3EfD3lK7rff7i5-tNc3368uzq9bI4DVtmNy8JO0ehy89bQTo5DAGROewTR6sBpnlBrKpAXZeQdMd4ZOzvfST73np-TL3rvL6ffqSlVLKMbNs44urUXJEWTfA0Pw6x40OZWSnVe7HBadnxUF9dKxeulYMVDYMdKfD9p1Wpx9ZQ-lIrDdA7gNRs8pzliuekhrjvhfZRJdXNUTCkEoAAyJMSpAPR4j9IPk44gisRc5bOkpuKyKCS4a1GZnqrIp_PeFfwGou6L1</recordid><startdate>2005</startdate><enddate>2005</enddate><creator>Aoyama, Takahiko</creator><creator>Ogata, Kazuhiro</creator><creator>Shimizu, Makiko</creator><creator>Hatta, Shigeo</creator><creator>Masuhara, Keiso</creator><creator>Shima, Yoshinori</creator><creator>Kimura, Kenjirou</creator><creator>Matsumoto, Yoshiaki</creator><general>Elsevier Ltd</general><general>Japanese Society for the Study of Xenobiotics</general><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>7X8</scope></search><sort><creationdate>2005</creationdate><title>Pharmacokinetics of Fluconazole and Fosfluconazole after Intraperitoneal Administration to Peritoneal Dialysis Rats</title><author>Aoyama, Takahiko ; 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Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study were to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations were analyzed using a two-compartment model in which the distribution volume of the peripheral compartment was fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>16415533</pmid><doi>10.2133/dmpk.20.485</doi><tpages>6</tpages></addata></record> |
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| subjects | Acute Kidney Injury - metabolism Algorithms Alkaline Phosphatase - metabolism Animals Antifungal Agents - administration & dosage Antifungal Agents - pharmacokinetics Area Under Curve Chromatography, High Pressure Liquid Data Interpretation, Statistical fluconazole Fluconazole - administration & dosage Fluconazole - analogs & derivatives Fluconazole - pharmacokinetics fosfluconazole Injections, Intraperitoneal Injections, Intravenous intraperitoneal administration Male Organophosphates - administration & dosage Organophosphates - pharmacokinetics peritoneal dialysis Peritoneal Dialysis, Continuous Ambulatory rat Rats Rats, Wistar |
| title | Pharmacokinetics of Fluconazole and Fosfluconazole after Intraperitoneal Administration to Peritoneal Dialysis Rats |
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