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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0001175,
umls-concept:C0007806,
umls-concept:C0012634,
umls-concept:C0030705,
umls-concept:C0031327,
umls-concept:C0032105,
umls-concept:C0035647,
umls-concept:C0087111,
umls-concept:C0185125,
umls-concept:C0205314,
umls-concept:C0280039,
umls-concept:C0439849,
umls-concept:C0445223,
umls-concept:C0449435,
umls-concept:C0679622,
umls-concept:C1552599,
umls-concept:C1704787
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pubmed:issue |
4
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pubmed:dateCreated |
1987-5-8
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pubmed:abstractText |
We investigated the clinical pharmacokinetics of azidothymidine (N3TdR) as part of a phase I/II trial in the treatment of acquired immunodeficiency syndrome and related diseases. During the 6-week course of therapy, drug levels in plasma, cerebrospinal fluid, and urine were determined by HLPC. The plasma half-life of N3TdR was 1.1 hour. The total body clearance was 1.3 L/kg/hr. At intravenous doses of 5 mg/kg or oral doses of 10 mg/kg, plasma levels were continuously maintained above the target level of 1 mumol/L. Oral bioavailability was 63% +/- 13%. Substantial penetration of N3TdR into cerebrospinal fluid was demonstrated. At doses of 5 mg/kg intravenously or 10 mg/kg orally, cerebrospinal fluid drug levels exceeded and were maintained close to 1 mumol/L. Nineteen percent of the administered dose was excreted unchanged into the urine. Renal clearance was 0.23 L/kg/hr. N3TdR possesses pharmacokinetic properties that would facilitate the long-term treatment of patients with acquired immunodeficiency syndrome: it can be given orally and it penetrates the central nervous system.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
AIM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0009-9236
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
41
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
407-12
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:3549120-Acquired Immunodeficiency Syndrome,
pubmed-meshheading:3549120-Administration, Oral,
pubmed-meshheading:3549120-Biological Availability,
pubmed-meshheading:3549120-Chromatography, High Pressure Liquid,
pubmed-meshheading:3549120-Clinical Trials as Topic,
pubmed-meshheading:3549120-Drug Evaluation,
pubmed-meshheading:3549120-Half-Life,
pubmed-meshheading:3549120-Humans,
pubmed-meshheading:3549120-Infusions, Intravenous,
pubmed-meshheading:3549120-Kinetics,
pubmed-meshheading:3549120-Thymidine,
pubmed-meshheading:3549120-Zidovudine
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pubmed:year |
1987
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pubmed:articleTitle |
Plasma and cerebrospinal fluid pharmacokinetics of 3'-azido-3'-deoxythymidine: a novel pyrimidine analog with potential application for the treatment of patients with AIDS and related diseases.
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pubmed:publicationType |
Journal Article,
Clinical Trial
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