Effect of fluvastatin, an inhibitor of 3-hydroxy-3-methyl glutaryl CoA reductase, on drug-metabolizing enzymes in rats.

Abstract:

:Fluvastatin (FV), a new cholesterol-lowering agent, has been studied for its effects on hepatic microsomal drug-metabolizing enzymes in male rats. FV was orally administered in dosages of 1, 5, and 30 mg/kg/day for 7 consecutive days. 3-Hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase activities were markedly decreased at all dose levels. The amount of microsomal protein and the contents of cytochromes P450 and b5 did not change. No induction of aniline hydroxylase, aminopyrine N-demethylase, testosterone hydroxylases (15 alpha-, 7 alpha-, 6 beta-, 16 alpha-, and 16 beta-), and UDP-glucuronosyltransferase were found. On the other hand, 7-ethoxycoumarin o-deethylase activity was slightly increased and lauric acid omega-1-hydroxylase activity tended to be decreased after treatment with FV.

authors

Ohtawa M,Masuda N,Karasawa Y,Tojo H

doi

10.1007/BF03189669

subject

Has Abstract

pub_date

1995-07-01 00:00:00

pages

191-6

issue

3

eissn

0378-7966

issn

2107-0180

journal_volume

20

pub_type

杂志文章
  • Effect of Tamarindus indica. L on the bioavailability of ibuprofen in healthy human volunteers.

    abstract::The influence of Tamarindus indica L fruit extract incorporated in a traditional meal on the bioavailability of Ibuprofen tablets 400 mg dose when given concurrently was studied in 6 healthy human volunteers. There was a statistically significant increase in the plasma levels of Ibuprofen and its metabolites hydroxy-i...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190483

    authors: Garba M,Yakasai IA,Bakare MT,Munir HY

    更新日期:2003-07-01 00:00:00

  • Multidose studies in the human metabolism of pentobarbitone.

    abstract::The metabolism of pentobarbitone has been investigated in two healthy volunteers, and the urinary excretion of unchanged drug, and the products of omega- and (omega-1)-oxidation, quantified for four days after each of three doses to each volunteer. The rates of excretion are discussed in terms which include enzyme ind...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189449

    authors: Baldeo WC,Gilbert JN,Powell JW

    更新日期:1980-01-01 00:00:00

  • Lipid kinetics in obese patients undergoing laparoscopy. The impact of cortisol inhibition by etomidate.

    abstract::The aim of this study was to investigate the response of cortisol, insulin and lipid parameters [serum Lipoprotein Lipase activity, choleseryl-ester transfer protein, triglycerides, total Cholesterol, High Density Lipoprotein, Free Fatty Acids] during the perioperative period in obese patients undergoing laparoscopic ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190596

    authors: Saranteas T,Voukena V,Zotos N,Stranomiti J,Kondadaki A,Tachmintzi A,Pantos C,Tesseromatis C,Dimitriou V

    更新日期:2004-07-01 00:00:00

  • Changes in cyclosporine A kinetics after experimental reduction of renal parenchyma.

    abstract::Experimental chronic renal insufficiency (produced by 5/6 ablation of renal parenchyma) is associated with changes in the kinetics of oral (intragastric) cyclosporine A (CyA). Compared with animals with intact renal parenchyma, significantly lower levels of CyA are reached under these conditions. The factors responsib...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189808

    authors: Schück O,Bohdanecká M,Sedivý J,Krajícková M,Chadimová M,Matousovic K

    更新日期:1997-07-01 00:00:00

  • Hydrolysis of haloperidol decanoate in vitro by cultured cells.

    abstract::[14C]Haloperidol decanoate was hydrolysed by partially purified carboxylesterase but not in plasma, blood, lymph and lymphatic liquid. These fluids inhibited the enzyme-mediated hydrolysis of the ester. Within the same incubation period as above, the ester was found hydrolysed to various extents in cell cultures of is...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189895

    authors: Oh-e Y,Miyazaki H,Matsunaga Y,Nambu K,Kobayashi N,Hashimoto M

    更新日期:1987-07-01 00:00:00

  • Parameterization of Microsomal and Cytosolic Scaling Factors: Methodological and Biological Considerations for Scalar Derivation and Validation.

    abstract::Mathematical models that can predict the kinetics of compounds have been increasingly adopted for drug development and risk assessment. Data for these models may be generated from in vitro experimental systems containing enzymes contributing to metabolic clearance, such as subcellular tissue fractions including micros...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-020-00666-w

    authors: Doerksen MJ,Jones RS,Coughtrie MWH,Collier AC

    更新日期:2020-12-19 00:00:00

  • Population Pharmacokinetic Modeling of Azithromycin Eyedrops in Tears Following Single-Dose Topical Administration in Healthy Volunteers.

    abstract:BACKGROUND AND OBJECTIVES:The disposition of azithromycin in the human eye following topical administration has not been fully explored. Population pharmacokinetic (PopPK) modeling can allow useful conclusions to be drawn based on limited tear sampling data. The aim of this study was therefore to develop and evaluate a...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/s13318-018-0522-6

    authors: Wu F,Zhao X,Li X,Cui Y

    更新日期:2019-06-01 00:00:00

  • Determination of the Pharmacokinetics and Tissue Distribution of Methyl 3,4-Dihydroxybenzoate (MDHB) in Mice Using Liquid Chromatography-Tandem Mass Spectrometry.

    abstract:BACKGROUND AND OBJECTIVES:Methyl 3,4-dihydroxybenzoate (MDHB) has the potential to prevent neurodegenerative diseases (NDDs). The present work aims to reveal the pharmacokinetics and tissue distribution characteristics of MDHB. METHODS:The pharmacokinetics and tissue distribution of MDHB were analyzed using LC-MS/MS a...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-0512-8

    authors: Wang JH,Hu SH,Su JY,Pan JP,Mi XN,Geng HJ,Zhang W,Cai L,Su CF,Hong AH,Luo HM

    更新日期:2019-04-01 00:00:00

  • Hepatic clearance of gitoxin: pharmacokinetic study on rabbit isolated liver. Influence of protein binding and comparison with digoxin.

    abstract::Hepatic clearance of gitoxin has been studied in the rabbit and compared with that of digoxin using an isolated perfused liver technique. During 1.5 hour perfusions with a modified Krebs-Henseleit solution, gitoxin perfusate levels decreased biexponentially; the distribution and elimination half-lives were estimated t...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189574

    authors: Pellegrin P,Lesne M

    更新日期:1983-01-01 00:00:00

  • Isolation and determination of bile acids.

    abstract::In this article, the methods of isolation and determination of bile acids are reviewed. Methods for separation of bile acids from cattle and pig bile are given in detail. Isolation of a mixture of cholic acid and deoxycholic acids from cattle bile and their subsequent purification are described. The isolation and puri...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章,评审

    doi:10.1007/BF03190712

    authors: Kandrac J,Kevresan S,Gu JK,Mikov M,Fawcett JP,Kuhajda K

    更新日期:2006-07-01 00:00:00

  • Impact of Efavirenz Metabolism on Loss to Care in Older HIV+ Africans.

    abstract::BACKGROUND AND OBJECTIVE: Efavirenz is commonly used in Africa and is frequently associated with neurocognitive toxicity, which may compromise clinical outcomes. Older individuals are at increased risk for drug toxicity and clinical outcomes may be worse in older age, particularly among those individuals with cytochro...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-0507-5

    authors: Torgersen J,Bellamy SL,Ratshaa B,Han X,Mosepele M,Zuppa AF,Vujkovic M,Steenhoff AP,Bisson GP,Gross R

    更新日期:2019-04-01 00:00:00

  • Comparative bioavailability and in-vitro antimicrobial activity of two different brands of rifampicin.

    abstract::A comparative bioavailability study was undertaken between a new formulation of rifampicin 'Famcin' and a standard formulation of rifampicin 'R-cin' in eight healthy male volunteers at two dose levels: 300 mg and 450 mg given orally under both single dose and steady state conditions. Plasma rifampicin was assayed spec...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189964

    authors: Garg SK,Chakrabarti A,Panigrahi D,Sharma M,Talwar P,Kumar N,Sharma PL

    更新日期:1991-07-01 00:00:00

  • Effects of Phenothiazines on Aldehyde Oxidase Activity Towards Aldehydes and N-Heterocycles: an In Vitro and In Silico Study.

    abstract:BACKGROUND:Aldehyde oxidase (AOX) is an important molybdenum-containing enzyme with high similarity with xanthine oxidase (XO). AOX involved in the metabolism of a large array of aldehydes and N-heterocyclic compounds and its activity is highly substrate-dependent. OBJECTIVES:The aim of this work was to study the effe...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-018-0514-6

    authors: Deris-Abdolahpour F,Abdolalipouran-Sadegh L,Dastmalchi S,Hamzeh-Mivehroud M,Zarei O,Dehgan G,Rashidi MR

    更新日期:2019-04-01 00:00:00

  • Pharmacokinetics of nefazodone in the dog following single oral administration.

    abstract::The pharmacokinetics of nefazodone (NEF) and two of its pharmacologically active metabolites viz hydroxynefazodone (HO-NEF) and m-chlorophenylpiperazine (mCPP) were determined following single oral administration of 100, 200 and 400 mg NEF to 6 beagle dogs in a three-way crossover study. Blood samples were collected f...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190163

    authors: Shukla UA,Marathe PH,Labudde JA,Pittman KA,Barbhaiya RH

    更新日期:1992-10-01 00:00:00

  • In vitro binding of lidocaine to liver tissue under the influence of propranolol: another mechanism of interaction?

    abstract::The co-administration of lidocaine and propranolol leads to significant drug-drug interactions. Beta-blockers decrease liver perfusion and inhibit the activity of hepatic microsomal lidocaine metabolizing enzymes of the P450_2D subfamily. Hence, there is a resulting reduction in the hepatic breakdown of lidocaine and ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03191006

    authors: Tesseromatis C,Kotsiou A,Tsagataki M,Tigka E,Vovou J,Alevizou A,Perisanidis C,Saranteas T,Karakitsos D,Karabinis A,Kostopanagiotou G

    更新日期:2007-10-01 00:00:00

  • 4-Amino-3-(3'-methoxycarbonyl-2'-thioureido)benzophenone, a prodrug of mebendazole.

    abstract::The compound 4-amino-3-(3'-methoxycarbonyl-2'-thioureido) benzophenone has shown promise as a prodrug of the anthelmintic mebendazole. The compound is stable in acid and neutral media and is rapidly hydrolysed in base. An HPLC assay procedure for mebendazole, the prodrug and their known or expected metabolites and deg...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03188765

    authors: Dawson M,Watson TR

    更新日期:1983-10-01 00:00:00

  • Effects of silymarin on the pharmacokinetics of atorvastatin in diabetic rats.

    abstract::The effect of silymarin (SMN) on the pharmacokinetics of atorvastatin in diabetic rats was evaluated. Male Wistar rats were assigned into two major groups and then sub-grouped according to the purposes of the study. The first major group was subdivided into three groups (n = 6) including control, non-treated diabetic ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-013-0166-5

    authors: Malekinejad H,Rokhsartalab-Azar S,Hassani-Dizaj S,Alizadeh-Fanalou S,Rezabakhsh A,Amniattalab A

    更新日期:2014-12-01 00:00:00

  • The pharmacokinetics of lisuride hydrogen maleate in rat, rabbit and rhesus monkey.

    abstract::The pharmacokinetics of lisuride hydrogen maleate (LHM) were investigated in rat, rabbit and rhesus monkey. Experiments were designed to meet not only the requirements of drug registration but also to serve other preclinical disciplines (toxicology, pharmacology). LHM is absorbed almost completely at a dose level of 1...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189490

    authors: Humpel M,Toda T,Oshino N,Pommerenke G

    更新日期:1981-01-01 00:00:00

  • The influence of herbal medicine ursolic acid on the uptake of rosuvastatin mediated by OATP1B1*1a and *5.

    abstract::Chinese herbal medicines such as hawthorn, salvia, etc., are frequently combined with statins so as to treat cardiovascular diseases more effectively. Chinese herbal medicines contain many kinds of active components, which may have drug-drug interactions with statins. This study aims to explore the effect and mechanis...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-014-0187-8

    authors: Hua WJ,Hua WX,Nan FY,Jiang WA,Yan C

    更新日期:2014-09-01 00:00:00

  • Hepatobiliary transport of YM466, a novel factor Xa inhibitor, in rats.

    abstract::YM466, a novel factor Xa inhibitor, is a hydrophilic compound with a carboxylic acid moiety. Previous studies in rats have shown that YM466 does nor undergo metabolism but is excreted into the bile and urine in unchanged form. Thus, in this study, we investigated in vivo hepatobiliary transport, focusing in particular...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03191128

    authors: Mano Y,Usui T,Kamimura H

    更新日期:2006-04-01 00:00:00

  • Rapid determination of functional liver plasma flow in ICU patients by a modified hepatic D-sorbitol plasma clearance method.

    abstract::Changes in liver perfusion may have a substantial influence on the pharmacokinetics of drugs with flow-controlled metabolism. This may have important implications for drug dosage in patients in an intensive care unit (ICU). The hepatic D-sorbitol plasma clearance has been suggested as a non-invasive test for evaluatin...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190181

    authors: Köppel C,Pohle S,Müller C

    更新日期:1993-10-01 00:00:00

  • Pharmacokinetic study of doxycycline polyphosphate (PPD), hydrochloride (CHD) and base (DB).

    abstract::Six healthy volunteers received the same oral dose of doxycycline, base (200 mg). Each received two of the three preparations at two-week intervals. Experimental results were interpreted on the basis of one or two-compartment models. The three preparations gave the elimination constants of the same order of magnitude ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189510

    authors: Saux MC,Mosser J,Pontagnier H,Leng B

    更新日期:1981-01-01 00:00:00

  • Alterations in central monoaminergic neurotransmission induced by polycyclic aromatic hydrocarbons in rats.

    abstract::Benzo[alpha]pyrene (B[a]P) is a product derived from incomplete combustion of organic material and is considered responsible for chemically-induced cancer in humans. In the present study, the levels of noradrenaline (NA), dopamine (DA), dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), 5-hydroxytryptamine (...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189998

    authors: Stephanou P,Konstandi M,Pappas P,Marselos M

    更新日期:1998-10-01 00:00:00

  • Pharmacokinetic studies of flumecinol in man and dog.

    abstract::The pharmacokinetics of flumecinol (Zixoryn) a new hepatic enzyme inducer has been studied in four beagle dogs and six healthy volunteers. The beagle dogs and the volunteers received the drug orally in a dose of 40 mg/kg of body weight and of 100 mg single dose respectively. Flumecinol was extracted from plasma with d...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03188725

    authors: Klebovich I,Vereczkey L,Kerpel-Fronius S,Ringwald G,Bodrogligeti I

    更新日期:1982-01-01 00:00:00

  • Stereoselective Pharmacokinetics of Ketoprofen After Oral Administration of Modified-Release Formulations in Caucasian Healthy Subjects.

    abstract:BACKGROUND AND OBJECTIVES:Ketoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation ...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/s13318-015-0313-2

    authors: Lorier M,Magallanes L,Ibarra M,Guevara N,Vázquez M,Fagiolino P

    更新日期:2016-12-01 00:00:00

  • Effects of potassium ethylxanthogenate and 2,3-dimercaptopropane sulphonate sodium on the pentobarbital pharmacokinetics and metabolism in male mice.

    abstract::The effects of potassium ethylxanthogenate (PEX) and 2,3-Dimercaptopropane sulphonate sodium (Unithiol) on the pentobarbital (40 mg/kg, body weight i.v.) (PB) sleeping time, pharmacokinetics, and metabolism, were studied in comparative experiments on male albino mice. It was established that the pretreatment of animal...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03189539

    authors: Yanev S,Janku I,Stoytchev T,Havlik I,Krebs V

    更新日期:1982-01-01 00:00:00

  • Pharmacokinetics of vitexin-4″-O-glucoside in rats after intravenous application.

    abstract::Vitexin-4″-O-glucoside (VOG), being a main component in the leaves of Crataegus pinnatifida Bge. var. major, was isolated and then three different doses (20, 40, and 60 mg/kg) of VOG were administered intravenously to rats. To study its pharmacokinetics, a simple and rapid HPLC method was developed using hesperidin as...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/s13318-011-0071-8

    authors: Ying XX,Wang F,Cheng ZZ,Zhang WJ,Li HB,Du Y,Liu X,Wang SY,Kang TG

    更新日期:2012-06-01 00:00:00

  • The effect of food and antacids on lansoprazole absorption and disposition.

    abstract::Bioavailability of lansoprazole, a new gastric proton pump inhibitor, was investigated in 12 healthy subjects. Each subject received in random order, lansoprazole (30 mg) alone or associated with standard meal or with antacids (aluminium and magnesium hydroxides) or one hour later than antacids. Lansoprazole and metab...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Delhotal-Landes B,Cournot A,Vermerie N,Dellatolas F,Benoit M,Flouvat B

    更新日期:1991-01-01 00:00:00

  • Dissolution kinetics of bezafibrate in two solid forms for oral administration.

    abstract::The dissolution kinetics of two solid and oral formulations of bezafibrate have been studied. These preparations are available in the Spanish market. Both of them are tablets, one conventional-release (A) and the other slow-release formulation (C). Dissolution studies have been performed using the system proposed by t...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:

    authors: Cadorniga R,Hernanez MT,Negro S,Burgos ML,Molina IT

    更新日期:1991-01-01 00:00:00

  • Pharmacokinetics of recombinant human basic fibroblast growth factor in mice using a radioiodination method combined with SDS-PAGE and a sandwich enzyme-linked immunosorbent assay.

    abstract::Pharmacokinetics of recombinant human basic fibroblast growth factor (rhbFGF) in mice were studied by using a radioiodination method combined with sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and a sandwich enzyme-Linked immunosorbent assay (ELISA). RhbFGF concentration in serum were dertermine...

    journal_title:European journal of drug metabolism and pharmacokinetics

    pub_type: 杂志文章

    doi:10.1007/BF03190593

    authors: Zhang Q,Wang GJ,Sun JG

    更新日期:2004-07-01 00:00:00