Abstract:
:The disposition of caspofungin, a parenteral antifungal drug, was investigated. Following a single, 1-h, intravenous infusion of 70 mg (200 microCi) of [(3)H]caspofungin to healthy men, plasma, urine, and feces were collected over 27 days in study A (n = 6) and plasma was collected over 26 weeks in study B (n = 7). Supportive data were obtained from a single-dose [(3)H]caspofungin tissue distribution study in rats (n = 3 animals/time point). Over 27 days in humans, 75.4% of radioactivity was recovered in urine (40.7%) and feces (34.4%). A long terminal phase (t(1/2) = 14.6 days) characterized much of the plasma drug profile of radioactivity, which remained quantifiable to 22.3 weeks. Mass balance calculations indicated that radioactivity in tissues peaked at 1.5 to 2 days at approximately 92% of the dose, and the rate of radioactivity excretion peaked at 6 to 7 days. Metabolism and excretion of caspofungin were very slow processes, and very little excretion or biotransformation occurred in the first 24 to 30 h postdose. Most of the area under the concentration-time curve of caspofungin was accounted for during this period, consistent with distribution-controlled clearance. The apparent distribution volume during this period indicated that this distribution process is uptake into tissue cells. Radioactivity was widely distributed in rats, with the highest concentrations in liver, kidney, lung, and spleen. Liver exhibited an extended uptake phase, peaking at 24 h with 35% of total dose in liver. The plasma profile of caspofungin is determined primarily by the rate of distribution of caspofungin from plasma into tissues.
journal_name
Antimicrob Agents Chemotherjournal_title
Antimicrobial agents and chemotherapyauthors
Stone JA,Xu X,Winchell GA,Deutsch PJ,Pearson PG,Migoya EM,Mistry GC,Xi L,Miller A,Sandhu P,Singh R,deLuna F,Dilzer SC,Lasseter KCdoi
10.1128/aac.48.3.815-823.2004subject
Has Abstractpub_date
2004-03-01 00:00:00pages
815-23issue
3eissn
0066-4804issn
1098-6596journal_volume
48pub_type
临床试验,杂志文章abstract::The effectiveness of Staphylococcus aureus strain 8325-4 as a recipient for the transduction of methicillin resistance requires the presence of a penicillinase plasmid but was found to be independent of the lysogenic state of the recipient. Effectiveness is conferred by the plasmid in either the autonomous or integrat...
journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
doi:10.1128/aac.18.3.424
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abstract::Ten patients with acquired immunodeficiency syndrome with newly diagnosed cytomegalovirus (CMV) retinitis were treated with an induction regimen of intravenous foscarnet, 60 mg/kg of body weight, administered as a 2-h infusion and repeated every 8 h for 14 days. At the end of induction, 9 of 10 patients had stabilized...
journal_title:Antimicrobial agents and chemotherapy
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doi:10.1128/aac.33.5.736
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journal_title:Antimicrobial agents and chemotherapy
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doi:10.1128/aac.19.2.309
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doi:10.1128/aac.36.8.1677
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journal_title:Antimicrobial agents and chemotherapy
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doi:10.1128/AAC.00952-08
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journal_title:Antimicrobial agents and chemotherapy
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doi:10.1128/AAC.01447-06
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journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
doi:10.1128/aac.36.9.2054
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doi:10.1128/aac.25.1.7
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pub_type: 杂志文章
doi:10.1128/AAC.00851-07
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
doi:10.1128/AAC.49.2.827-829.2005
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journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
doi:10.1128/aac.37.6.1318
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journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
doi:10.1128/AAC.00320-12
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journal_title:Antimicrobial agents and chemotherapy
pub_type: 杂志文章
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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journal_title:Antimicrobial agents and chemotherapy
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