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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:dateCreated |
1990-3-23
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pubmed:abstractText |
The pharmacokinetics of azithromycin, a new azalide antibiotic, were examined in man. Approximately 37% of a single oral dose of 500 mg was bioavailable and produced a peak serum concentration of 0.4 mg/l. Multiple dose regimens (two doses of 500 mg separated by 12 h and followed by 500 mg qds for five days, or two doses of 250 mg separated by 12 h and followed by 250 mg qds for nine days) produced only slight increases in peak serum concentrations. The serum protein binding of azithromycin declined from about 50% at 0.02 mg/l to 12% at 0.5 mg/l. Tissue concentrations of azithromycin were much higher than serum concentrations. After two 250 mg doses 12 h apart, peak azithromycin concentrations exceeded 3 mg/kg in prostate, tonsil and many other tissues. Concentrations in tissues declined with apparent half-lives of 2.3 days in prostate and 3.2 days in tonsil. The high tissue concentrations suggest that proposed standard dosage regimens of 500 mg qds on day 1 followed by 250 mg qds for four days, or three daily dosages of 500 mg, will produce tissue concentrations above 3 mg/kg in a variety of tissues. Since these tissue concentrations exceed the MICs of relevant pathogens, these dosage regimens should be effective against respiratory tract and soft-tissue infections. A single 1 g dose may be effective in the treatment of many sexually transmitted diseases.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0305-7453
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
25 Suppl A
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
73-82
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:2154441-Adolescent,
pubmed-meshheading:2154441-Adult,
pubmed-meshheading:2154441-Azithromycin,
pubmed-meshheading:2154441-Biological Availability,
pubmed-meshheading:2154441-Erythromycin,
pubmed-meshheading:2154441-Half-Life,
pubmed-meshheading:2154441-Humans,
pubmed-meshheading:2154441-Least-Squares Analysis,
pubmed-meshheading:2154441-Male,
pubmed-meshheading:2154441-Middle Aged,
pubmed-meshheading:2154441-Tissue Distribution
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pubmed:year |
1990
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pubmed:articleTitle |
The pharmacokinetics of azithromycin in human serum and tissues.
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pubmed:affiliation |
Drug Metabolism Department, Pfizer Central Research, Groton, CT 06340.
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pubmed:publicationType |
Journal Article
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