Genetic CYP2C19 polymorphism dependent non-responders to clopidogrel therapy--does structural design, dosing and induction strategies have a role to play?

abstract：:Although the application of medical marijuana and cannabinoid drugs is controversial, it is a part of modern-day medicine. The list of diseases in which cannabinoids are promoted as a treatment is constantly expanding. Cases of significant improvement in patients with a very poor prognosis of glioma or epilepsy have a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Hryhorowicz S,Walczak M,Zakerska-Banaszak O,Słomski R,Skrzypczak-Zielińska M

更新日期：2018-02-01 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：:Penbutolol is a not cardioselective beta-adrenergic blocking drug; it is lipid soluble and differs in its protein binding from the other members of its group because shows linkage to alpha 1-glycoprotein, with no detectable binding to albumin. AAG levels change during pregnancy and so the binding of [3H]-penbutolol wa...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Aquirre C,Rodriguez-Sasiain JM,Navajas P,Calvo R

更新日期：1988-01-01 00:00:00

abstract：:This paper deals with press-coated modified release tablets in which the drug dose is situated in the core or is divided between the core and the coat. The coat contains polymer (sodium alginate or hydroxypropylmethyl cellulose, HPMC) to control drug release. The main objective was to investigate how the pharmacokinet...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Halsas M,Ervasti P,Veski P,Jürjenson H,Marvola M

更新日期：1998-04-01 00:00:00

abstract：:The pharmacokinetics of tolbutamide (TB) have been studied in endotoxin pretreated rats with the aim of evaluating TB as a marker for endotoxin effects. Endotoxin dose of 10 mg/kg resulted in a 50% rate of mortality. TB was i.v. administered 24 h. after endotoxin dosing. Clearance (Cl) decreased by approximately 2/3 o...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Kaka JS,al-Khamis K,Tanira MO

更新日期：1990-07-01 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：:The technique of differential display reverse transcription-polymerase chain reaction (ddRT-PCR) has been used to produce unique profiles of up-regulated and down-regulated gene expression in the liver of male Wistar rats following short term exposure to the non-genotoxic hepatocarcinogens, phenobarbital and WY-14,643...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Rockett JC,Esdaile DJ,Gibson GG

更新日期：1997-10-01 00:00:00

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

authors： Dawson M,Watson TR

更新日期：1983-10-01 00:00:00

abstract：:A rapid and sensitive procedure is described for the quantitation of levamisole in plasma using high-performance liquid chromatography (HPLC). The procedure involves sample preparation using a reverse-phase C18 cartridge prior to chromatography and quantitation using peak area ratios (UV absorbance detection, 225 nm) ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vandamme TF,Demoustier M,Rollmann B

更新日期：1995-04-01 00:00:00

abstract：:This study describes an approach permitting the determination of compartmental concentration and drug kinetics in the case of chronobiological variations of elimination rate. ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Merabet-Atmani G,Aliguechi-Bouhadja S,Redouane A,Filali T,Mansour K

更新日期：1999-10-01 00:00:00

abstract：:This study examined the effects of the absorption enhancers, acylcarnitines, on efflux transporting systems, including P-glycoprotein (P-gp) and other efflux transporters, and elucidated the importance of acyl chain length and the concentration of acylcarnitine on the activity of efflux transport. The effects of two a...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Tomita M,Doi N,Hayashi M

更新日期：2010-09-01 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：:A multicompartmental pharmacokinetic model is presented, which based upon data from a previous study, describes the effects of ethanol (60 mM) on the metabolism of codeine (10 microM) in isolated rat hepatocytes. According to this model, about one third of codeine metabolized was transformed to morphine (13%) and norc...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Bodd E,Green MH,Drevon CA,Mørland J

更新日期：1986-07-01 00:00:00

abstract：:Pharmacokinetics of ketoprofen (KTP) enantiomers has been studied in patients with rheumatoid arthritis (RA) following administration of a single oral dose of 100 mg rac-KTP during multidrug therapy taking into consideration the genotype of RA patients Concentrations of (-)-R and (+)-S enantiomers of KTP in plasma, ur...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Główka F,Karaźniewicz-Łada M,Grześkowiak E,Rogozinska D,Romanowski W

更新日期：2011-09-01 00:00:00

abstract：:Pomegranate juice (PJ) is known to be a potent inhibitor of human cytochrome enzymes. The purpose of this study was to investigate the effect of acute and chronic PJ on the pharmacokinetics of oral nitrendipine (10 mg/kg) in rabbits. Male New Zealand rabbits were pretreated with PJ for 1 week and on the last day, a si...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Voruganti S,Rapolu K,Tota S,Yamsani SK,Yamsani MR

更新日期：2012-06-01 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：:The transdermally applied dopamine receptor agonist rotigotine is extensively metabolized in the liver. An open-label, parallel-group study was conducted to evaluate the effects of moderate hepatic impairment on the pharmacokinetics, safety and tolerability of rotigotine. Eight subjects with normal hepatic function an...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Cawello W,Fichtner A,Boekens H,Braun M

更新日期：2014-09-01 00:00:00

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

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

更新日期：2014-09-01 00:00:00

abstract：:A single oral dose of 300 mg of nizatidine was administered to two groups of volunteers: a first group of 12 young healthy subjects and a second group of 12 elderly patients, in order to compare the pharmacokinetic parameters and to verify a possible influence of the age on nizatidine's kinetics. Blood samples were co...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Villani P,Regazzi MB,Pecorini M,Tizzoni M,Savio D

更新日期：1991-01-01 00:00:00

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

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

更新日期：2003-07-01 00:00:00

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

authors： Wu F,Zhao X,Li X,Cui Y

更新日期：2019-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Effective management of immunosuppressants is extemely important to improve prognosis of heart transplant recipients. We aim to investigate the effects of cytochrome P450 (CYP) 3A5 (rs776746) single nucleotide polymorphisms (SNPs) on serum tacrolimus concentrations/doses (C/Ds, ng/mL per mg/kg...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Liu BY,Chen WQ,Chen ZG,Huang J,Liao ZK,Liu Q,Zheng Z,Song YH,Wang W,Hu SS

更新日期：2019-12-01 00:00:00

abstract：:There is current emphasis for extended integration of pharmacokinetics (PK) and pharmacodynamics (PD) into all phases of new drug development, including large-scale clinical trials. In this paper, we focus on study design and data analysis issues for the investigation of pharmacokinetic/pharmacodynamic and blood level...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Steimer JL,Ebelin ME,Van Bree J

更新日期：1993-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Polyethylene glycol-modified canine uricase (PEG-UHC) prepared with a lower-molecular-weight (5 kDa) PEG is used to treat gout. This study investigated the comparative pharmacokinetics of single and multiple doses of PEG-UHC administered intravenously and a single dose of uricase (UHC) administ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Li H,Huo J,Sun D,Jiang L,Hu C,Bai Y,Ma X,Zhang H,Shi X,Zhao Z,Zhou J,Lu Y,Zhang C

更新日期：2020-08-01 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

abstract：:The kinetics of five cisplatin analogs binding to human plasma fractions possessing a molecular weight greater than 50,000 daltons were studied. Each drug solution in plasma ultrafiltrate or phosphate buffer (pH = 7.4, mu = 0.154) was mixed with human plasma and filterable platinum concentrations were measured versus ...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Momburg R,Bourdeaux M,Sarrazin M,Roux F,Briand C

更新日期：1985-01-01 00:00:00

abstract：:The metabolic fate of the anti-Parkinsonian drug budipine was studied in rats after oral administration. The presence of an aromatic hydroxylation product, metabolite M1, and its O-sulphate conjugate was confirmed. Three new minor metabolites, budipine N-oxide, metabolite M1 N-oxide and a secondary metabolite derived ...

journal_title：European journal of drug metabolism and pharmacokinetics

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

更新日期：1991-04-01 00:00:00

abstract：:The biotransformation of 1-(3-butoxy-2-carbamoyloxypropyl)-5-ethyl-5-phenyl-(1H,3H,5H)-pyrimidine-2,4,6-trione (febarbamate) has been investigated in man. Human volunteers received a single oral dose of 15 mg/kg febarbamate. Twenty two metabolites found in urine were separated and purified by means of an extraction wi...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Vachta J,Valter K,Gold-Aubert P

更新日期：1983-07-01 00:00:00

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

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

更新日期：1981-01-01 00:00:00

abstract：:Lisofylline (LSF), is the R-(-) enantiomer of the metabolite M1 of pentoxifylline, and is currently under development for the treatment of type 1 diabetes. The aim of the study was to develop a physiologically based pharmacokinetic (PBPK) model of LSF in mice and to perform simulations in order to predict LSF concentr...

journal_title：European journal of drug metabolism and pharmacokinetics

authors： Wyska E,Świerczek A,Pociecha K,Przejczowska-Pomierny K

更新日期：2016-08-01 00:00:00