| 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 |
Related Documents
:
|
535599 - Disposition and metabolism of [14c]loperamide in rats. 1642669 - Metabolic fate of the new angiotensin-converting enzyme inhibitor imidapril in animals.... 15893299 - Determination of the tissue distribution and excretion by accelerator mass spectrometry... 8355589 - Adipose glycerolipid formation: effect of nutritional and hormonal states. 2712419 - Pharmacokinetics of oxytetracycline in the turkey: evaluation of biliary and urinary ex... 581939 - Further absorption studies with the anti-diarrhoeal agent ethacridine lactate in the dog. 19324279 - Evaluation of the hsp90 inhibitor nvp-auy922 in multicellular tumour spheroids with res... 10688339 - A double-blind placebo-controlled study of botulinum toxin in upper limb spasticity aft... 25191739 - Variation of rabbit sperm physiologic parameters after the x-ray exposure. |
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. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| 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
Previous Document: Bile flow but not enterohepatic recirculation influences the pharmacokinetics of ranitidine in the r...
Next Document: Metabolic kinetics of pseudoracemic propranolol in human liver microsomes. Enantioselectivity and qu...