1995
DOI: 10.1128/aac.39.11.2401
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Clinical pharmacokinetics of adefovir in human immunodeficiency virus type 1-infected patients

Abstract: The pharmacokinetics and bioavailability of adefovir [9-[2-(phosphonomethoxy)ethyl]adenine] were examined at two dose levels in three phase I/II studies in 28 human immunodeficiency type 1-infected patients. The concentrations of adefovir in serum following the intravenous infusion of 1.0 or 3.0 mg/kg of body weight were dose proportional and declined biexponentially, with an overall mean ؎ standard deviation terminal half-life of 1.6 ؎ 0.5 h (n ‫؍‬ 28). Approximately 90% of the intravenous dose was recovered … Show more

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Cited by 126 publications
(81 citation statements)
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“…The histopathologies of the three animals that were euthanized after chronic dosing with PMPA at 30 mg/kg revealed renal tubular atrophy and degeneration as common lesions. This toxicity of PMPA is probably related to its renal clearance; studies with animals and humans indicate that PMPA and its related nucleotide analogs are excreted in unchanged form in urine through a combination of renal filtration and active tubular secretion (10,14,15,16). Thus, accumulation of drug in tubular epithelial cells (due to more drug uptake from plasma than secretion into the tubular lumen) may be the direct cause of these renal effects.…”
Section: Discussionmentioning
confidence: 99%
“…The histopathologies of the three animals that were euthanized after chronic dosing with PMPA at 30 mg/kg revealed renal tubular atrophy and degeneration as common lesions. This toxicity of PMPA is probably related to its renal clearance; studies with animals and humans indicate that PMPA and its related nucleotide analogs are excreted in unchanged form in urine through a combination of renal filtration and active tubular secretion (10,14,15,16). Thus, accumulation of drug in tubular epithelial cells (due to more drug uptake from plasma than secretion into the tubular lumen) may be the direct cause of these renal effects.…”
Section: Discussionmentioning
confidence: 99%
“…Preliminary data in animals also indicates that the bioavailability of alamifovir may decrease when it is given with food. In contrast, the oral bioavailability of the broad-spectrum antiviral adefovir was approximately 4% in cynomolgus monkeys (5,17) and less than 12% in humans (4). Therefore, in comparison to adefovir, alamifovir has shown greater oral bioavailability.…”
mentioning
confidence: 86%
“…For study 1, serial venous blood samples (15 ml) for the determination of alamifovir, 602074, 602075, and 602076 concentrations in plasma were collected into glass tubes containing sodium heparin via an indwelling cannula. Blood samples were collected just prior to dose and at 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3,4,6,8,12,24,36,48, and 72 h postdose during each treatment period. Samples were immediately centrifuged for 10 min at 2,000 ϫ g and at 4°C.…”
Section: Methodsmentioning
confidence: 99%
“…4,5 Its oral pro-drug is adefovir dipivoxil, which is a butyl ester of PMEA. Therefore, PMEA is used in the treatment of chronic hepatitis B.…”
Section: 3mentioning
confidence: 99%