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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1985-2-11
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pubmed:abstractText |
In the first of two successive studies, four healthy male subjects received 500 mg of 14C-labeled imipenem alone and together with 500 mg of unlabeled cilastatin sodium. In the second study, the same subjects were given 250 mg of 14C-labeled cilastatin sodium alone and together with 250 and 1,000 mg of cold imipenem. Concentrations of imipenem and cilastatin in plasma, urine, and feces were assayed by high-pressure liquid chromatography and radiometry. Plasma concentrations of imipenem assayed radiometrically were higher than those measured by high-pressure liquid chromatography. In one subject studied at the end of drug administration, the open lactam metabolite of imipenem represented 9% of the radioactivity. Plasma levels of cilastatin determined by high-pressure liquid chromatography and radiometry were virtually identical. Urinary recovery of imipenem varied between 12 and 42% of the dose when that drug was given alone but increased to between 64 and 75% when administered with cilastatin sodium at a 1:1 ratio. Almost all radioactivity of imipenem was recovered in the urine within 96 h after drug administration. The open lactam metabolite, resulting from the metabolism of imipenem in the kidneys by a dipeptidase, dehydropeptidase-I, represented 80 to 90% of the effluent radioactivity when imipenem was given alone and about 20% when cilastatin sodium was coadministered. Renal excretion of cilastatin followed closely that of imipenem. Almost all of the administered radioactivity was recovered in 24 h, and about 75% of the dose was recovered as unchanged cilastatin within 6 h. The N-acetyl metabolite of cilastatin was found to represent about 12% of the total radioactivity.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6264844,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6365872,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6573156,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6573157,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6583195,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-6931549,
http://linkedlifedata.com/resource/pubmed/commentcorrection/6595962-7125632
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Bacterial Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cilastatin,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclopropanes,
http://linkedlifedata.com/resource/pubmed/chemical/Imipenem,
http://linkedlifedata.com/resource/pubmed/chemical/Thienamycins
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0066-4804
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
26
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
707-14
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:6595962-Adult,
pubmed-meshheading:6595962-Anti-Bacterial Agents,
pubmed-meshheading:6595962-Chromatography, High Pressure Liquid,
pubmed-meshheading:6595962-Cilastatin,
pubmed-meshheading:6595962-Cyclopropanes,
pubmed-meshheading:6595962-Drug Tolerance,
pubmed-meshheading:6595962-Feces,
pubmed-meshheading:6595962-Glomerular Filtration Rate,
pubmed-meshheading:6595962-Humans,
pubmed-meshheading:6595962-Imipenem,
pubmed-meshheading:6595962-Kinetics,
pubmed-meshheading:6595962-Male,
pubmed-meshheading:6595962-Thienamycins
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pubmed:year |
1984
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pubmed:articleTitle |
Disposition of radiolabeled imipenem and cilastatin in normal human volunteers.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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