| Serum protein binding of lomefloxacin, a new antimicrobial agent, and its related quinolones. | |
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MedLine Citation:
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PMID: 2760827 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The serum protein binding of lomefloxacin (LFLX), a new quinolone (pyridonecarboxylic acid), and its related analogues was studied by an ultrafiltration technique. The extent of binding of quinolones was independent of the concentration of quinolones below 100 micrograms/mL in rat serum; but, above this concentration, the binding decreased with increased drug concentration in the case of nalidixic acid and analogue 3. The extent of binding in rat serum differed widely among the quinolones examined [i.e., from 15% (norfloxacin) to 84% (nalidixic acid) at concentrations of 0.4-10.0 micrograms/mL]. Lomefloxacin was bound to serum proteins to the extent of 28.1, 20.1, and 20.6% in the sera of rats, dogs, and humans, respectively. The binding of nalidixic acid with rat serum albumin, which was very similar to that in rat serum, was concentration dependent. Some quinolone derivatives with a piperazinyl group or a relatively large-sized substituent at the 7-position exhibited a percentage unbound of approximately 70-80%, while some derivatives with small-sized substituents gave a low percentage unbound of 20-30%. This suggests that there is a steric effect of the substituents at the 7-position of quinolones on their binding characteristics with serum proteins. The results of the present study indicate that quinolones bind mainly with albumin among serum proteins and that the remarkable difference of the extent of binding of quinolone analogues is related to the size of the substituent at the 7-position of the molecule, possibly due to its steric effect. |
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Authors:
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E Okezaki; T Terasaki; M Nakamura; O Nagata; H Kato; A Tsuji |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: 78 ISSN: 0022-3549 ISO Abbreviation: J Pharm Sci Publication Date: 1989 Jun |
Date Detail:
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Created Date: 1989-09-21 Completed Date: 1989-09-21 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 504-7 Citation Subset: IM |
Affiliation:
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Central Research Laboratory, Hokuriku Seiyaku Co., Ltd., Fukui, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Infective Agents / blood*, pharmacokinetics Blood Proteins / metabolism Dogs Fluoroquinolones* Humans Nalidixic Acid / blood, pharmacokinetics Ofloxacin / blood, metabolism Protein Binding Quinolones* Rats Species Specificity |
| Chemical | |
Reg. No./Substance:
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0/Anti-Infective Agents; 0/Blood Proteins; 0/Fluoroquinolones; 0/Quinolones; 389-08-2/Nalidixic Acid; 82419-36-1/Ofloxacin; 98079-51-7/lomefloxacin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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