[Hepatic mono-oxygenases]. 1988

A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
Département d'Anesthésiologie, Hospices Civils de Strasbourg.

Most drugs and xenobiotics are lipid-soluble compounds that need to be transformed into more polar water-soluble molecules by a system of hepatic monoxygenases in order to be excreted by the kidney and the liver. This system is also called cytochrome P-450. It is found in animals, as well as plants. It is located in the cellular endoplasmic reticulum of numerous tissues, but it is most active in the liver. It is made up of several isoenzymes differing from one another by the structure of their apoproteins, their immunological characteristics and their affinity for various substrates. Cytochrome P-450 has great variability, being influenced by exogenous factors (drug intake, ionizing radiation, stress, diet) and individual endogenous factors (age, sex, genetic factors). Several non specific tests exploring the system are available. They include: direct investigations carried out on liver biopsies, which are seldom used in clinical practice, and indirect investigations, such as the measurement of the clearance of exogenous substances, of urinary metabolites of endogenous substances and of specific enzymes. Induction and inhibition of microsomal activity are of the utmost interest to the clinician in various fields such as toxicology, carcinogenesis, drug interactions or drug habituation, metabolic regulations and maintenance of body homeostasis. Seven classes of enzyme inducers have been defined, but the exact mechanism of this has only been identified for two of them (the barbiturate and polycyclic hydrocarbon groups). Several drugs have been identified as enzyme inhibitors, the best known to the anaesthesiologist being macrolide antibiotics, imidazole derivatives, cimetidine, chloramphenicol and isonazide.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007093 Imidazoles Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
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
D002927 Cimetidine A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output. Altramet,Biomet,Biomet400,Cimetidine HCl,Cimetidine Hydrochloride,Eureceptor,Histodil,N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)guanidine,SK&F-92334,SKF-92334,Tagamet,HCl, Cimetidine,Hydrochloride, Cimetidine,SK&F 92334,SK&F92334,SKF 92334,SKF92334
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
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004364 Pharmaceutical Preparations Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form. Drug,Drugs,Pharmaceutical,Pharmaceutical Preparation,Pharmaceutical Product,Pharmaceutic Preparations,Pharmaceutical Products,Pharmaceuticals,Preparations, Pharmaceutical,Preparation, Pharmaceutical,Preparations, Pharmaceutic,Product, Pharmaceutical,Products, Pharmaceutical
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
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000617 Aminoglycosides Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS. Aminoglycoside

Related Publications

A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
January 1972, Biochemical Society symposium,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
April 1976, Comptes rendus hebdomadaires des seances de l'Academie des sciences. Serie D: Sciences naturelles,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
July 1985, Xenobiotica; the fate of foreign compounds in biological systems,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
January 1986, IARC scientific publications,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
October 2013, Current opinion in structural biology,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
January 1993, Vestnik Rossiiskoi akademii meditsinskikh nauk,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
February 2016, Biochemical Society transactions,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
January 1994, Eksperimental'naia i klinicheskaia farmakologiia,
A Robillart, and M Zeisser, and B Vailly, and J P Dupeyron
May 1992, Biochemical Society transactions,
Copied contents to your clipboard!