| Pharmacokinetics of dicrofenac after its intrarectal and intracolostomal administration to rabbits with rectal resection or colostoma construction. | |
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MedLine Citation:
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PMID: 11745905 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We investigated the pharmacokinetics of diclofenac, one of the important analgesics in palliative care, after its intrarectal and intracolostomal administration to rabbits with rectal resection or colostoma construction. In rectal-resected rabbits, its bioavailability after rectal administration was significantly lower than that in normal rabbits, and furthermore that after intracolostomal administration was significantly lower than that in rectal-resected rabbits. This decreased bioavailability in rabbits with rectal resection and colostoma construction was thought to be due to the increased first-pass effect. With increase in the dose up to 1.5-fold, the plasma concentrations in both rectal-resected and colostoma-constructed rabbits increased to the normal rabbit level. These results indicate that the bioavailability of diclofenac sodium after its rectal and intracolostomal administration decreases, and that an increased dose can restore the decreased plasma concentration. There was no difference in the plasma concentration with diclofenac sodium suppositories between administration into the normal rectum and the remaining rectum following colostoma construction, and the remaining rectum was found to be a useful administration route for suppositories. Therefore, it was indicated that when administering diclofenac sodium suppositories to rectal-resected and colostoma-constructed patients, the dose should be increased, because the pharmacokinetics of diclofenac was similar in rabbits and human. |
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Authors:
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K Nagasawa; H Nakanishi; T Matsuda; K Takara; N Ohnishi; T Yokoyama; S Fujimoto |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Biopharmaceutics & drug disposition Volume: 22 ISSN: 0142-2782 ISO Abbreviation: Biopharm Drug Dispos Publication Date: 2001 Jan |
Date Detail:
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Created Date: 2001-12-17 Completed Date: 2002-01-15 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 7911226 Medline TA: Biopharm Drug Dispos Country: England |
Other Details:
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Languages: eng Pagination: 31-9 Citation Subset: IM |
Copyright Information:
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Copyright 2001 John Wiley & Sons, Ltd. |
Affiliation:
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Department of Environmental Biochemistry, Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi, Yamashina-ku, Kyoto 607-8414, Japan. nagasawa@mb.kyoto-phu.ac.jp |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Administration, Rectal Animals Anti-Inflammatory Agents, Non-Steroidal / administration & dosage, blood, pharmacokinetics* Biological Availability Colostomy* Diclofenac / administration & dosage, blood, pharmacokinetics* Injections, Intravenous Male Rabbits Rectum / drug effects, metabolism*, surgery* |
| Chemical | |
Reg. No./Substance:
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0/Anti-Inflammatory Agents, Non-Steroidal; 15307-86-5/Diclofenac |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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