Development and regression of the hepatic microsomal enzyme induction and stimulation of biliary excretion produced by phenobarbital in rats. 1980

E Fischer, and Z Gregus

The time-course effect of a single dose (75 mg/kg i.p.) of phenobarbital (PB) and that of prolonged PB treatment (75 mg/kg daily i.p., for 1 to 5 days) on the hepatic excretory and microsomal enzyme functions have been studied in rats. PB given in a single dose resulted in hypercholeresis 6 hr, an increase in the biliary excretion rate of bromcresol green and in hepatic cytochrome P-45 concentration 12 hr, and shortening of hexobarbital sleeping time 24 hr after the administration. All these changes, except the hypercholeresis, became gradually more apparent following the repeated daily administration of PB. Regression of the changes was faster in biliary excretory function than in microsomal function. Biliary flow and biliary output of bromcresol green returned to the control level at 72 hr after a single dose of PB or at 5 days after the cessation of a 5-day PB treatment, whereas enzyme induction was still apparent at those times. These results indicate that no close correlation in time exists between PB produced hepatic microsomal enzyme induction and the stimulatory effect of PB on biliary excretion.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D009929 Organ Size The measurement of an organ in volume, mass, or heaviness. Organ Volume,Organ Weight,Size, Organ,Weight, Organ
D010634 Phenobarbital A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations. Phenemal,Phenobarbitone,Phenylbarbital,Gardenal,Hysteps,Luminal,Phenobarbital Sodium,Phenobarbital, Monosodium Salt,Phenylethylbarbituric Acid,Acid, Phenylethylbarbituric,Monosodium Salt Phenobarbital,Sodium, Phenobarbital
D003577 Cytochrome P-450 Enzyme System A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism. Cytochrome P-450,Cytochrome P-450 Enzyme,Cytochrome P-450-Dependent Monooxygenase,P-450 Enzyme,P450 Enzyme,CYP450 Family,CYP450 Superfamily,Cytochrome P-450 Enzymes,Cytochrome P-450 Families,Cytochrome P-450 Monooxygenase,Cytochrome P-450 Oxygenase,Cytochrome P-450 Superfamily,Cytochrome P450,Cytochrome P450 Superfamily,Cytochrome p450 Families,P-450 Enzymes,P450 Enzymes,Cytochrome P 450,Cytochrome P 450 Dependent Monooxygenase,Cytochrome P 450 Enzyme,Cytochrome P 450 Enzyme System,Cytochrome P 450 Enzymes,Cytochrome P 450 Families,Cytochrome P 450 Monooxygenase,Cytochrome P 450 Oxygenase,Cytochrome P 450 Superfamily,Enzyme, Cytochrome P-450,Enzyme, P-450,Enzyme, P450,Enzymes, Cytochrome P-450,Enzymes, P-450,Enzymes, P450,Monooxygenase, Cytochrome P-450,Monooxygenase, Cytochrome P-450-Dependent,P 450 Enzyme,P 450 Enzymes,P-450 Enzyme, Cytochrome,P-450 Enzymes, Cytochrome,Superfamily, CYP450,Superfamily, Cytochrome P-450,Superfamily, Cytochrome P450
D004790 Enzyme Induction An increase in the rate of synthesis of an enzyme due to the presence of an inducer which acts to derepress the gene responsible for enzyme synthesis. Induction, Enzyme
D006591 Hexobarbital A barbiturate that is effective as a hypnotic and sedative. Evipan,Hexenal,Hexobarbitone,Sodium Hexobarbital,Hexobarbital, Sodium
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

Related Publications

E Fischer, and Z Gregus
June 1990, Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association,
E Fischer, and Z Gregus
December 1979, Clinical biochemistry,
E Fischer, and Z Gregus
August 1973, Anesthesiology,
E Fischer, and Z Gregus
January 1985, Archives of toxicology. Supplement. = Archiv fur Toxikologie. Supplement,
E Fischer, and Z Gregus
November 2001, Toxicology and applied pharmacology,
Copied contents to your clipboard!