Abstract：
OBJECTIVE:In order to document the stereoselective distribution in joints of a chiral nonsteroidal anti-inflammatory drug, the relative affinities of the enantiomers of tiaprofenic acid in synovium and for cartilage were compared. METHODS:The distribution of tiaprofenic acid in synovium and in cartilage was studied 25 h after administering the racemic drug for 2 days (600 mg of a sustained-release preparation, once daily), in 12 inpatients with osteoarthritis of the hip requiring arthroplasty. Enantiomers were quantified in plasma and freeze-ground tissues by a chiral HPLC assay. RESULTS:Plasma concentrations of the dextrorotatory (R) enantiomer (0.40 microgram/ml) were higher than those of its antipode. The concentration of racemate in synovium (in dried and fresh tissues, 150% and 40%, respectively, of the concentration in plasma) was much higher than that in cartilage (in dried tissues 32% of the plasma concentration). The ratio of the active, dextrorotatory (R) enantiomer to its antipode was higher in synovial tissue than in plasma. CONCLUSION:Tiaprofenic acid is distributed stereoselectively in plasma and synovium, which contain a higher concentration of the active, dextrorotatory (R) enantiomer. In cartilage, it reaches only a very low concentration.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Lapicque F,Mainard D,Gillet P,Payan E,Bannwarth B,Netter Pdoi
10.1007/s002280050109subject
Has Abstractpub_date
1996-01-01 00:00:00pages
283-7issue
4eissn
0031-6970issn
1432-1041journal_volume
50pub_type
杂志文章abstract：OBJECTIVE:To determine the possible interaction between the antihypertensive agent cicletanine and the hypoglycaemic drug tolbutamide. METHODS:Time-courses of glycaemia and serum immunoreactive insulin (IRI) were followed in 10 healthy subjects after two tolbutamide infusions in each volunteer; initially alone and 9 d...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280050127
更新日期：1996-01-01 00:00:00
abstract：BACKGROUND:A four-drug cytochrome P450 (CYP) phenotyping cocktail was developed to rapidly and safely determine CYP2D6, CYP2C19, CYP2C9 and CYP1A2 enzyme activity and phenotype. METHODS:The cocktail consisted of the single CYP phenotyping probes of 50 mg tramadol (CYP2D6), 20 mg omeprazole (CYP2C19), 25 mg losartan (C...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-013-1561-1
更新日期：2013-12-01 00:00:00
abstract：OBJECTIVE:The aim of this study was to compare the effects of benazepril and amlodipine in monotherapy versus in combination with plasma t-PA and PAI-1 activity in hypertensive type-2 diabetic patients. METHODS:After an initial 6-week wash-out, single-blind placebo period, 38 patients, 17 men and 21 females, were rand...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/s00228-003-0621-3
更新日期：2003-08-01 00:00:00
abstract：OBJECTIVE:This multicenter, double-blind, placebo-controlled, parallel-group study was designed to assess the acute effects of intravenous mibefradil on the electrophysiologic characteristics of the human heart. METHODS:Seventy-one patients referred for routine electrophysiologic testing were randomized to receive one...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,多中心研究,随机对照试验
doi：10.1007/s002280050241
更新日期：1997-01-01 00:00:00
abstract：:For model identification and parameter estimation in the framework of linear pharmacokinetics it is most often assumed that the disposition function is a finite sum of exponential functions with time constants lambda i and associated coefficients Ci. Least-square fitting procedures are used to estimate the coefficient...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00315312
更新日期：1993-01-01 00:00:00
abstract：:The pharmacokinetics of a new sustained-release preparation of theophylline (Dilatrane à Action Prolongée capsules filled with homogenous microgranules) has been after its studied administration to 7 healthy volunteers at 8 p.m. in order to achieve therapeutic levels at night and in the morning. In separate trials the...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00542169
更新日期：1984-01-01 00:00:00
abstract：:The acute effects on monophasic action potentials (MAP), QT interval, and right ventricle effective refractory period (V-ERP) of propranolol 0.2 mg.kg-1 body weight have been studied in 10 patients with coronary artery disease. The median duration of MAP at 90% repolarization (MAP90) was shortened from 238 to 228 ms a...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00280044
更新日期：1990-01-01 00:00:00
abstract：OBJECTIVE:To assess the pharmacokinetics, safety and tolerability of escalating oral doses of GW420867X, a non-nucleoside reverse transcriptase inhibitor, was investigated in healthy male volunteers in a randomized, double-blind placebo-controlled study. METHODS:Study subjects were divided into four groups of 12 subje...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/s002280000224
更新日期：2001-01-01 00:00:00
abstract：:Since little is known of the number and types of binding sites on alpha 1-acid glycoprotein (AAG) and because drug-drug protein binding interactions often fail to fit a simple model, a study of the effect of 9 known AAG binding drugs on lidocaine free fraction (LFF) was performed. Serum was obtained from 10 healthy ma...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF01037957
更新日期：1983-01-01 00:00:00
abstract：:The function of the hepatic P450 enzyme system was evaluated by measuring the kinetics of antipyrine and serum sex hormone levels were determined in 12 male patients with epilepsy during carbamazepine medication, and two and six months after changing their medication to oxcarbazepine. Antipyrine t1/2 increased and ant...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00196862
更新日期：1995-01-01 00:00:00
abstract：PURPOSE:Our aim was to observe the impact of CYP3A4*1G genetic polymorphism on lipid-lowering efficacy of statins. METHODS:We studied 217 unrelated hyperlipidemic patients who prospectively received atorvastatin and 199 patients who received simvastatin as a single-agent therapy (20 mg day(-1) p.o.) for 4 weeks. Genot...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-008-0502-x
更新日期：2008-09-01 00:00:00
abstract：:Procainamide was given to 20 patients with normal renal function as an i.v. bolus of 500 mg followed by 1.0 or 1.5 g eight-hourly by mouth in the form of a slow release preparation (Durules). 97.6 +/- 27.1 (SD)% of the oral procainamide was absorbed, the absorption half life being 1.54 h. The elimination half life fol...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00560459
更新日期：1978-12-01 00:00:00
abstract：OBJECTIVES:The objective of this study was to describe determinants of current and subsequent benzodiazepine use in an elderly population, the Paquid cohort. METHODS:The study was conducted on a cohort of 2,792 community-dwelling subjects 65 years of age or more living in the Gironde department, southwestern France. B...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280100326
更新日期：2001-08-01 00:00:00
abstract：:We have studied 16 healthy men to evaluate preliminary pharmacodynamics and kinetics of BW443C given by i.v. infusions. Four volunteers received escalating doses at weekly intervals, starting at 0.1 microgram.kg-1 for 60 min and increasing to a maximum of 2.0 micrograms.kg-1.min-1 for 180 min. Subsequently 12 differen...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF01061420
更新日期：1988-01-01 00:00:00
abstract：:The pharmacokinetics of enprofylline, a new potent antiasthmatic, has been studied in 20 healthy, elderly subjects, aged 65 to 81 years, and in 7 young adult controls, aged 23 to 37 years. The dose of 1 mg/kg body weight was given as an i.v. infusion. Plasma levels of enprofylline were followed for about 7 h and urine...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00609959
更新日期：1987-01-01 00:00:00
abstract：PURPOSE:Older people with several chronic conditions require multiple drugs from different classes to be adequately treated. This study aims to: (i) measure medication adherence across multiple conditions and therapeutic drug groups in older community-dwelling patients, and (ii) examine the effect of multimorbidity on ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,多中心研究
doi：10.1007/s00228-017-2388-y
更新日期：2018-03-01 00:00:00
abstract：:The pharmacokinetics and metabolism of quinidine were investigated in extensive and poor metabolisers of sparteine. No differences in plasma clearance, terminal half life, volume of distribution or cumulative urinary excretion of quinidine, 3-hydroxyquinidine and quinidine-N-oxide were observed between phenotypes. Thu...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00870989
更新日期：1986-01-01 00:00:00
abstract：OBJECTIVE:To describe the frequency and types of drug-related problems (DRPs) in hospitalised patients, and to identify risk factors for DRPs and the drugs most frequently causing them. METHODS:From May to December 2002, 827 patients from six internal medicine and two rheumatology departments in five hospitals in Norw...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,多中心研究
doi：10.1007/s00228-004-0830-4
更新日期：2004-11-01 00:00:00
abstract：PURPOSE:To investigate the characteristics of ADRs in patients admitting at the emergency room of a tertiary hospital. METHODS:We collected the patient records of 1600 emergency room visits of a university hospital in 2018. The patient files were studied retrospectively and all possible ADRs were identified and regist...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-020-03043-3
更新日期：2020-11-13 00:00:00
abstract：:We have studied the pharmacokinetics of tulobuterol given transdermally or by aerosol inhalation in healthy male volunteers. Tulobuterol was rapidly absorbed after inhalation, with a tmax of 0.8-1.5 h. The Cmax and the AUC increased linearly with dose. Tulobuterol was well absorbed after transdermal administration, wi...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00316473
更新日期：1993-01-01 00:00:00
abstract：PURPOSE:To investigate adherence rates to hospital drug formularies (HDFs) and cost of drugs in hospitals. METHODS:Data on drugs used during 2010 were analyzed for ten hospitals (two hospitals from each of the five regions), constituting 30 % of hospitals and 45 % of hospital beds in Denmark. Drug use data from indivi...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-013-1540-6
更新日期：2013-10-01 00:00:00
abstract：OBJECTIVE:To investigate if an intervention aimed at improving the quality of the diagnostic procedures in Spanish general practice could lower antibiotic prescribing in patients with respiratory tract infections (RTIs). METHODS:GPs in the intervention group (n=17) registered all patients with RTIs during a 3-week per...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-006-0187-y
更新日期：2006-11-01 00:00:00
abstract：:In a double-blind, placebo-controlled cross-over study, the plasma atrial natriuretic peptide (ANP) levels of nine young and ten elderly hypertensive patients were compared after placebo and after treatment with 120 mg verapamil given three times daily over 4 weeks. During placebo, plasma ANP levels proved to be highe...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF01409206
更新日期：1990-01-01 00:00:00
abstract：:Right ventricular repolarisation and refractoriness after therapeutic doses of disopyramide have been studied in 10 patients with coronary artery disease by recording monophasic action potentials (MAP) during programmed stimulation. Using 2 catheters, with the tip of one in the apex and the other in the outflow tract ...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF00558240
更新日期：1988-01-01 00:00:00
abstract：PURPOSE:This study aimed to test the applicability and effectiveness of the principles and informed consent form (ICF) template proposed by the Strategic Initiative for Developing Capacity in Ethical Review (SIDCER) across multiple clinical trials involving Thai research participants with various conditions. METHODS:A...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1007/s00228-016-2159-1
更新日期：2017-02-01 00:00:00
abstract：PURPOSE:Sacubitril/valsartan (LCZ696) is a first-in-class angiotensin receptor neprilysin inhibitor (ARNI) indicated to reduce the risk of cardiovascular death and hospitalization for heart failure in patients with chronic heart failure (NYHA class II-IV) and reduced ejection fraction. This study was aimed to evaluate ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1007/s00228-016-2062-9
更新日期：2016-08-01 00:00:00
abstract：:The linearity of the pharmacokinetics of the metamizol metabolites 4-methyl-amino-antipyrine (4-MAA), 4-amino-antipyrine (4-AA), 4-formyl-aminoantipyrine (4-FAA), and 4-acetyl-amino-antipyrine (4-AcAA) has been studied after administration to 15 healthy male volunteers of single oral doses of 750, 1500, and 3000 mg me...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF00314805
更新日期：1990-01-01 00:00:00
abstract：PURPOSE:Sitagliptin, a dipeptidyl peptidase (DPP)-IV inhibitor approved for the treatment of type 2 diabetes, is reported to be more efficacious in Indian patients than non-Indian patient population. The objective of the study was to evaluate pharmacokinetic and pharmacodynamic (PK/PD) parameters of single-dose sitagli...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1007/s00228-018-2433-5
更新日期：2018-05-01 00:00:00
abstract：:The pharmacokinetics of cephacetrile were studied after its administration as a single i.v. bolus injection of 15 mg/kg body weight to 11 patients with terminal renal inpairment undergoing haemodialysis for 6 h. A two-compartment kinetic model was used to describe the biphasic decrease in plasma concentration. The qua...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00644966
更新日期：1979-08-01 00:00:00
abstract：OBJECTIVE/METHODS:The metabolism of chloramphenicol succinate (CAPS) by human bone marrow was studied in vitro using 75 marrow samples. Whole marrow samples were incubated with CAPS with or without reduced nicotinamide adenine dinucleotide phosphate for 1, 2 and 3 h at 37 degrees C. Ficoll-paque-separated marrow mononu...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280000143
更新日期：2000-08-01 00:00:00
