Absorption, distribution, metabolism and excretion of the cholecystokinin-1 antagonist dexloxiglumide in the rat

European Journal of Drug Metabolism and Pharmacokinetics
C WebberL F Chasseaud

Abstract

Single oral doses of 14C-dexloxiglumide were rapidly and extensively absorbed in rats, and eliminated more slowly by females than by males. The respective half-lives were about 4.9 and 2.1 h. Following single intravenous doses, dexloxiglumide was characterised as a drug having a low clearance (6.01 and about 1.96 ml/min/kg in males and females respectively), a moderate volume of distribution (Vss, 0.98 and about 1.1 L/kg in males and females respectively) and a high systemic availability. It was extensively bound to plasma proteins (97%). Dexloxiglumide is mainly cleared by the liver. Its renal clearance was minor. In only the liver and gastrointestinal tract, were concentrations of 14C generally greater than those in plasma. Peak 14C concentrations generally occurred at 1-2 h in males and at 2-4 h in females. Tissue 14C concentrations then declined by severalfold during 24 h although still present in most tissues at 24 h but only in a few tissues (such as the liver and gastrointestinal tract) at 168 h. Decline of 14C was less rapid in the tissues of females than in those of males. Single intravenous or oral doses were mainly excreted in the faeces (87-92%), mostly during 24 h and more slowly from females than from males. Urine...Continue Reading

References

Jan 1, 1991·Annual Review of Pharmacology and Toxicology·G N Woodruff, J Hughes
Jul 1, 1993·Pharmaceutical Research·B Davies, T Morris
Jul 10, 2003·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·C WebberLucio C Rovati

Citations

May 21, 2004·European Journal of Drug Metabolism and Pharmacokinetics·C WebberL F Chasseaud
Jun 15, 2012·AAPS PharmSciTech·Yardi SaibiHidehisa Tachiki
Nov 23, 2006·Clinical Pharmacokinetics·Stefano PersianiLucio C Rovati

Related Concepts

dexloxiglumide
Process of Absorption
Metazoa
Biological Availability
Pentanoic Acids
Drug or Chemical Tissue Distribution
Rats, Holtzman
Cholecystokinin A Receptor
Rats, Laboratory

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