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Effect of uremia and anephric state on the pharmacokinetics of sulindac and its metabolites in rats. II. Differential effects on the biliary excretion. 1985

J H Lin, and K C Yeh, and D E Duggan

The differential effects of experimental uremia and surgical anephric state on the biliary excretion of sulindac and its metabolites in rats were investigated. After concurrent administration of 14C-sulindac and 3H-sulfide (5 mg-eq/kg iv), the apparent biliary clearance of sulindac was significantly decreased in anephric rats relative to control rats, whereas the apparent biliary clearance of sulfide was increased in uremic rats as compared to that in control rats. There was a strong positive correlation between the irreversible elimination of sulindac (CLox) and the apparent biliary clearance (r = 0.942). Similarly, the irreversible elimination of sulfide (CLide) was positively correlated with the apparent biliary clearance of sulfide (r = 0.961). A partial explanation is thus provided for differences in the respective effects of uremic and anephric state upon observed CLox and CLide.

UI MeSH Term Description Entries
D007192 Indenes A family of fused-ring hydrocarbons isolated from coal tar that act as intermediates in various chemical reactions and are used in the production of coumarone-indene resins.
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001646 Bile An emulsifying agent produced in the LIVER and secreted into the DUODENUM. Its composition includes BILE ACIDS AND SALTS; CHOLESTEROL; and ELECTROLYTES. It aids DIGESTION of fats in the duodenum. Biliary Sludge,Sludge, Biliary
D013467 Sulindac A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects. Aclin,Apo-Sulin,Arthrobid,Arthrocine,Chibret,Clinoril,Copal,Kenalin,Klinoril,MK-231,Novo-Sundac,Nu-Sulindac,Sulindal,Apo Sulin,MK 231,MK231,Novo Sundac,Nu Sulindac
D014511 Uremia A clinical syndrome associated with the retention of renal waste products or uremic toxins in the blood. It is usually the result of RENAL INSUFFICIENCY. Most uremic toxins are end products of protein or nitrogen CATABOLISM, such as UREA or CREATININE. Severe uremia can lead to multiple organ dysfunctions with a constellation of symptoms. Uremias
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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