Evaluation of Strategies for the Assessment of Drug-Drug Interactions Involving Cytochrome P450 Enzymes.

abstract：BACKGROUND AND OBJECTIVES:Doxorubicin plays an essential role in the treatment of paediatric cancers. Defining genotypes with a higher risk for developing anthracycline-induced cardiotoxicity could help to reduce cardiotoxicity. METHODS:Data originated from a phase II study assessing the pharmacokinetics of doxorubici...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hellmann F,Völler S,Krischke M,Jamieson D,André N,Bisogno G,Boddy A,Hempel G

更新日期：2020-06-01 00:00:00

abstract：:We have studied the metabolism of doxorubicin in rat and mouse liver, heart and hepatocytes. Doxorubicinol was present in all cases at very low levels and 7-deoxyaglycones were present only in extraphysiological conditions: no aglycones were found either in fresh livers or in hearts of animals treated with the drug, b...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vrignaud P,Londos-Gagliardi D,Robert J

更新日期：1986-04-01 00:00:00

abstract：:This study investigated the effect of diltiazem on the bioavailability of oral and intravenous cyclosporine (CsA) in rats. While control rats received normal saline, experimental groups received 60 or 90 mg/kg diltiazem orally for 3 days. Each group divided into 2 equal groups that received a single oral dose or i.v. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kalkan S,Gumustekin M,Aygoren O,Tuncok Y,Gelal A,Guven H

更新日期：2004-04-01 00:00:00

abstract：:The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Aitio A,Ahotupa M,Parkki MG

更新日期：1980-01-01 00:00:00

abstract：:The disposition of RS-tocainide in three healthy volunteers has been studied after oral administration of a pseudoracemic mixture containing S(+) [3H] tocainide as a radioactive tracer together with a therapeutic dose of the racemate. Analytical methods based on HPLC have been developed to measure S(+) and R(-) tocain...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hoffmann KJ,Renberg L,Bäärnhielm C

更新日期：1984-07-01 00:00:00

abstract：:Tectorigenin (Te) is a main active component in the flowers of Pueraria thomsonii Benth. and the rhizomes of Belamcanda chinensis (L.) DC. Previously, we have reported the pharmacokinetic properties of Te in rat plasma. The purpose of this study was to investigate the urinary excretion of Te after oral administration ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Shi Z,Zhang G,Zhao L,Wang S,Kano Y,Yuan D

更新日期：2015-09-01 00:00:00

abstract：BACKGROUND:Omadacycline is a semisynthetic aminomethylcycline antibacterial derived from the tetracycline class. It is approved in the USA to treat adults with acute bacterial skin and skin-structure infections and community-acquired bacterial pneumonia. OBJECTIVES:This phase I, open-label study evaluated the effect o...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hunt TL,Tzanis E,Bai S,Manley A,Chitra S,McGovern PC

更新日期：2021-01-01 00:00:00

abstract：:Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Milosevic N,Popovic J,Grujic Z,Rapaic M

更新日期：2011-09-01 00:00:00

abstract：:The metabolic fate of anti-inflammatory agent 2-(5-ethylpyridin-2-yl)benzimidazole (KB-1043) was studied in rats after oral administration. An average of 12.2 +/- 1.5% of the dose was excreted in the urine in the course of 0-48 h; 56.7 +/- 2.6% with feces. Two metabolites were also detected in the urine and isolated b...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Caputo O,Grosa G,Ceruti M,Viola F,Rocco F

更新日期：1989-10-01 00:00:00

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

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

更新日期：1982-01-01 00:00:00

abstract：:This study developed a physiologically based pharmacokinetic (PBPK) model in intraabdominally infected rats and extrapolated it to humans to predict the levofloxacin pharmacokinetics and penetration into tissues. Twelve male rats with intraabdominal infections induced by Escherichia coli received a single dose of 50 m...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zhu L,Zhang Y,Yang J,Wang Y,Zhang J,Zhao Y,Dong W

更新日期：2016-08-01 00:00:00

abstract：:Glutathione S-transferases (GSTs) play an important role in the biotransformation of endogenous compounds and xenobiotics as well as in the metabolic inactivation of pharmacologically active substances, including anticancer drugs. Using cisplatin as the prototype drug, we investigated if any correlation exists between...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Nagar R,Khan AR,Poonia A,Mishra PK,Singh S

更新日期：2015-03-01 00:00:00

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

authors： Baldeo WC,Gilbert JN,Powell JW

更新日期：1980-01-01 00:00:00

abstract：:A remarkably large species difference in cinchonidine oxidation activity catalyzed by aldehyde oxidase (AO) has been known, in particular between rabbit and monkey. As the first step in clarifying the phenomenon from the view point of structures of the active site, we attempted to construct an expression system of rab...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu P,Liang S,Wang BJ,Guo RC

更新日期：2009-07-01 00:00:00

abstract：:Weibull function C = Bts-1exp(-lambda ts) was used to describe plasma concentration-time data of ribavirin in 6 healthy subjects following an i.v. dose of 600 mg. A good fit was found in each of the subjects, where the coefficients of determination r2 were > 0.99. The parameters estimated were as follows: B, 5.90 +/- ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu XD,Xie L,Han KQ,Liu GQ

更新日期：1996-07-01 00:00:00

abstract：:Angiogenesis is integral to tumour growth and invasion, and is a key target for cancer therapeutics. However, for many of the licensed indications, only a modest clinical benefit has been observed for both monoclonal antibody and small-molecule tyrosine kinase inhibitor anti-angiogenic therapy. Pre-clinical and clinic...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Morotti M,Dass PH,Harris AL,Lord S

更新日期：2018-04-01 00:00:00

abstract：:Urodynamic model was developed which, in conjunction with a compartmental pharmacokinetic model, was used for study of factors influencing drug concentrations in urine: urine flow rate, residual bladder urine, maximal bladder urine, stage of renal failure, and elimination kinetics of drugs. Norfloxacin (NOR) was used ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Primozic S,Karba R,Mrhar A,Drinovec J,Kozjek F

更新日期：1991-01-01 00:00:00

abstract：:The development of peptide therapeutics has increased enormously in recent decades. Many of the peptide drugs and antibody fragments that lack Fc backbone have a short half-life in circulation. In general, the half-life supports the design of the dosing regimen and frequency of administration, which are key aspects in...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hijazi Y

更新日期：2021-01-01 00:00:00

abstract：:We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metab...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bernareggi A,Crema A,Carlesi RM,Castoldi D,Ratti E,Renoldi MI,Ratti D,Ceserani R,Tognella S

更新日期：1995-10-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and huma...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bairam AF,Rasool MI,Kurogi K,Liu MC

更新日期：2017-10-01 00:00:00

abstract：:A generic drug product (test product) is bioequivalent to an innovator product (reference product) when their bioavailabilities in the same molar dose are similar. Bioavailability is expressed by pharmacokinetic parameters such as the area under plasma concentration-time curve (AUC), the maximum plasma concentration (...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zintzaras E

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Daire JL,Leporq B,Vilgrain V,Van Beers BE,Schmidt S,Pastor CM

更新日期：2017-08-01 00:00:00

abstract：:The binding of three digitalis glycosides, digitoxin, digoxin and gitoxin, to human serum albumin was studied in vitro by equilibrium dialysis. The results obtained showed that binding is a non saturable process and that probably the same binding mechanism is involved for each of the three drugs. Their binding sites s...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tillement JP,Zini R,Lecomte M,d'Athis P

更新日期：1980-01-01 00:00:00

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

authors： Pellegrin P,Lesne M

更新日期：1983-01-01 00:00:00

abstract：:The pharmacokinetic-pharmacodynamic (PK-PD) relationship of the proton pump inhibitor rabeprazole in healthy Chinese volunteers was characterized via a population approach. Healthy Chinese male volunteers were enrolled in the clinical trial. Subjects were divided into three groups by their CYP2C19 genotype. Serum conc...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Chen ZY,Xie HT,Zheng QS,Sun RY,Hu G

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Acetaminophen (APAP, paracetamol) is currently the principal cause of acute liver failure in both the USA and the UK. However, relatively little is known about the influence of genes and race/ethnicity on the disposition of APAP and the extent to which genetic variation and ethnicity may predi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Zurlinden TJ,Reisfeld B

更新日期：2017-02-01 00:00:00

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

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

更新日期：2006-07-01 00:00:00

abstract：:The disposition kinetics of the N-oxide of picobenzide were studied after administration to rabbits at a bolus dose of 30 mg/kg of picobenzide intravenously. The biotransformation process fits a first-order kinetic process, and the metabolite shows good access capacity to the peripheral compartment. The N-oxide of pic...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Santos Buelga D,Mariño EL,Domínguez-Gil A

更新日期：1989-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmaco...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bursi R,Piana C,Grevel J,Huntjens D,Boesl I

更新日期：2017-10-01 00:00:00

abstract：:Tritiated tetrahydro-tetramethyl-naphthalenyl-propenyl benzoic acid (TTNPB; Ro 13-7410) was administered as a single oral bolus to pregnant hamsters (day 8) to determine the maternal plasma pharmacokinetic profile and peripheral tissue distribution patterns. Blood and tissue, including embryo or fetus, were collected ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Howard WB,Willhite CC,Sharma RP,Omaye ST,Hatori A

更新日期：1989-04-01 00:00:00