Document Detail


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:
PMID:  8013279     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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:
I Bekersky; R J Puhl; G Hanson; S Mong
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Publication Detail:
Type:  Journal Article    
Journal Detail:
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:
Created Date:  1994-07-26     Completed Date:  1994-07-26     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  9421550     Medline TA:  Drug Metab Dispos     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  233-6     Citation Subset:  IM    
Affiliation:
Department of Pharmacology and Toxicology, Fujisawa Pharmaceutical Company, Deerfield, Illinois 60015.
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MeSH Terms
Descriptor/Qualifier:
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:
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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