The pharmacokinetics of 1,3-di(4-imidazolino-2-methoxyphenoxy) propane.lactate (DMP.lactate), a new agent against opportunistic infections, in male beagle dogs. | |
MedLine Citation:
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PMID: 8013279 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The pharmacokinetics and oral bioavailability of 1,3-di(4-imidazolino-2-methoxyphenoxy) propane.lactate (DMP) was determined in male dogs following iv and po administrations of DMP.lactate containing trace amounts of [14C]DMP.HCl. Following the iv administration of [14C]DMP.lactate (2.5 mg/kg), plasma concentrations of DMP declined in a biexponential manner and were measurable to 48 hr. The terminal elimination half-life was 37.7 hr. The mean AUC0-infinity of DMP was 1.58 micrograms.hr/ml. The volume of distribution was 89 liters/kg and the body clearance was 27 ml/min/kg. The disposition of total radioactivity was similar to that of DMP. Approximately 14% of the dose was eliminated in urine as DMP or total radioactivity. Renal clearance was 10% of the body clearance. Following the po administration of [14C]DMP.lactate (14 mg/kg) the mean Cmax of total radioactivity and DMP was 0.20 and 0.17 micrograms/ml, respectively. The respective mean AUC0-T was 0.37 and 0.21 micrograms.hr/ml. The mean oral bioavailability based on DMP plasma concentrations was 2.4%. The mean Cmax of DMP following a 100 mg/kg po dose of DMP.lactate was 14 micrograms/ml and the AUC0-T was 1.87 micrograms.ml/hr; the bioavailability was 3.2%. Approximately 1% of the orally administered dose was eliminated in urine as DMP. |
Authors:
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I Bekersky; R J Puhl; G Hanson; S Mong |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Drug metabolism and disposition: the biological fate of chemicals Volume: 22 ISSN: 0090-9556 ISO Abbreviation: Drug Metab. Dispos. Publication Date: 1994 Mar-Apr |
Date Detail:
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Created Date: 1994-07-26 Completed Date: 1994-07-26 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 9421550 Medline TA: Drug Metab Dispos Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 233-6 Citation Subset: IM |
Affiliation:
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Department of Pharmacology and Toxicology, Fujisawa Pharmaceutical Company, Deerfield, Illinois 60015. |
Export Citation:
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MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Anti-Infective Agents / blood, pharmacokinetics*, urine Biological Availability Chromatography, High Pressure Liquid Dogs Half-Life Injections, Intravenous Male Opportunistic Infections / drug therapy* Pentamidine / analogs & derivatives*, blood, pharmacokinetics, urine |
Chemical | |
Reg. No./Substance:
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0/Anti-Infective Agents; 100-33-4/Pentamidine; 109444-03-3/1,3-di-(4-imidazolino-2-methoxyphenoxy)propane |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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