Source:http://linkedlifedata.com/resource/pubmed/id/10434231
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
8
|
| pubmed:dateCreated |
1999-10-13
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| pubmed:abstractText |
As a result of the low oral bioavailability of ganciclovir, a prodrug was developed to improve the bioavailability of ganciclovir. This study was designed to investigate the fasting, single-dose pharmacokinetics as well as the absolute and relative bioavailability of a valine ester prodrug of ganciclovir, valganciclovir, as compared to oral and intravenous ganciclovir in asymptomatic HIV+ and CMV+ subjects. In this open-label, randomized, three-period crossover study, 18 subjects received, in random order, single oral doses of valganciclovir 360 mg and ganciclovir 1000 mg and an intravenous infusion of ganciclovir 5 mg/kg over 1 hour. Valganciclovir was rapidly and extensively hydrolyzed to ganciclovir, resulting in significantly greater bioavailability compared to 1000 mg oral ganciclovir (60.9% vs. 5.6%, respectively). Higher peak serum concentrations were reached earlier following valganciclovir (ganciclovir [2.98 +/- 0.77 micrograms/mL at 1.0 +/- 0.3 h]) than following oral ganciclovir (0.47 +/- 0.17 microgram/mL and 2.2 +/- 1.0 h). Mean total ganciclovir AUCs following oral ganciclovir (1000 mg) and 360 mg valganciclovir (3.8 +/- 1.2 and 10.8 +/- 1.9 micrograms-h/mL) were less than that following a standard 5 mg/kg intravenous infusion of ganciclovir (25.1 +/- 3.8 micrograms-h/mL). In summary, valganciclovir is a prodrug with a favorable safety profile with enhanced bioavailability and significantly higher serum concentrations of ganciclovir than following oral administration of ganciclovir itself.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-HIV Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Ganciclovir,
http://linkedlifedata.com/resource/pubmed/chemical/Prodrugs,
http://linkedlifedata.com/resource/pubmed/chemical/valganciclovir
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| pubmed:status |
MEDLINE
|
| pubmed:month |
Aug
|
| pubmed:issn |
0091-2700
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
39
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
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| pubmed:pagination |
800-4
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| pubmed:dateRevised |
2004-11-17
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| pubmed:meshHeading |
pubmed-meshheading:10434231-Adult,
pubmed-meshheading:10434231-Anti-HIV Agents,
pubmed-meshheading:10434231-Antiviral Agents,
pubmed-meshheading:10434231-Area Under Curve,
pubmed-meshheading:10434231-Biological Availability,
pubmed-meshheading:10434231-Cross-Over Studies,
pubmed-meshheading:10434231-Cytomegalovirus Infections,
pubmed-meshheading:10434231-Diarrhea,
pubmed-meshheading:10434231-Dizziness,
pubmed-meshheading:10434231-Dyspnea,
pubmed-meshheading:10434231-Exanthema,
pubmed-meshheading:10434231-Female,
pubmed-meshheading:10434231-Fever,
pubmed-meshheading:10434231-Ganciclovir,
pubmed-meshheading:10434231-HIV Seropositivity,
pubmed-meshheading:10434231-Headache,
pubmed-meshheading:10434231-Humans,
pubmed-meshheading:10434231-Hypertension,
pubmed-meshheading:10434231-Male,
pubmed-meshheading:10434231-Metabolic Clearance Rate,
pubmed-meshheading:10434231-Middle Aged,
pubmed-meshheading:10434231-Pain,
pubmed-meshheading:10434231-Prodrugs,
pubmed-meshheading:10434231-Syncope
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| pubmed:year |
1999
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| pubmed:articleTitle |
Single-dose pharmacokinetics of valganciclovir in HIV- and CMV-seropositive subjects.
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| pubmed:affiliation |
Roche Global Development, Palo Alto, California, USA.
|
| pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial
|