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 effects of late pregnancy and also oestrogen supplementation on the CYP2C19-mediated biotransformation of proguanil (PG) to its active antifol triazine metabolite cycloguanil (CG). METHODS:Case control study conducted on the NW border of Thailand; a single dose of PG (4 mg/kg) was administer...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-003-0651-x
更新日期：2003-10-01 00:00:00
abstract：:Drug utilization was studied in children below 14 years of age in Tenerife, Canary Islands, who were seen as outpatients by 15 paediatricians and 10 general practitioners. Data on diagnosis, previous drug exposure and prescriptions were collected from a random sample of 1327 children. Nose and throat infections (40.1%...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF01046708
更新日期：1988-01-01 00:00:00
abstract：:The pharmacokinetics of phenylethylmalonamide (PEMA) were studied in 6 elderly men after oral administration of a single 400 mg dose. Peak PEMA serum levels were obtained within 4 h of intake, half-life values ranged from 30.7-57.9 h in these elderly men. The elimination half-life was twice as long when compared to a ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00637644
更新日期：1987-01-01 00:00:00
abstract：:The influence of a benzodiazepine (triazolam) on the body temperature of poor sleepers during nights disturbed by airplane noises has been examined. Subjects were divided into 3 groups each of 8 men. Following a double-blind design, Group A (controls) received a placebo for 6 consecutive nights, Group B received 0.25 ...
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/BF00544042
更新日期：1984-01-01 00:00:00
abstract：:The debrisoquine hydroxylation phenotype was studied in 152 unselected healthy Tasmanian subjects, who were mostly Caucasians of British ancestry. Following a 10 mg oral dose of debrisoquine (D), the ratio of D/4-hydroxydebrisoquine excreted in 8-h urine (metabolic ratio, MR) was determined. MR values were bimodally d...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00315235
更新日期：1991-01-01 00:00:00
abstract：:Acute studies of clonidine suggest that it lowers blood pressure by central enhancement of baroreflex sensitivity coupled with diminished evidence of sympathetic outflow, but longterm clonidine data have not been conclusive. We examined effects of one month of low dose clonidine (0.4 +/- 0.15 mg/day) alone in 13 essen...
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/BF00558378
更新日期：1981-01-01 00:00:00
abstract：:To elucidate the effect of Nicorandil on myocardial energy metabolism and myocardial sympathetic activity, we administered Nicorandil orally to eight patients with angina pectoris prior to exercise testing. Arterial and coronary sinus levels of lactate, ammonia, hypoxanthine (HX), adrenaline and noradrenaline were mea...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00198297
更新日期：1995-01-01 00:00:00
abstract：:The antihypertensive effect of a new vasodilator with betablocking properties (SK & F 92657) was investigated in 10 patients with mild to moderate essential hypertension. After a mean treatment period of 26,5 weeks (6,5-49 weeks) blood pressure was significantly reduced, from 168 +/- 22/106 +/- 6 mmHg to 144 +/- 19/94...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00605990
更新日期：1982-01-01 00:00:00
abstract：:The kinetics of triamterene and its active phase II metabolite were studied in 32 patients with various degrees of impaired renal function; the creatinine clearances ranged from 135 to 10 ml/min. The area under the plasma concentration-time curves (AUC) for triamterene were not influenced by kidney function, but the A...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00609885
更新日期：1983-01-01 00:00:00
abstract：:The peripheral histamine-inhibiting and central sedative effects of single oral doses (SOD) and of repeated administration for one week (steady state, SS), of 20 mg hydroxyzine HCL and 10 mg cetirizine have been assessed in 12 healthy volunteers, in a double-blind placebo-controlled cross-over study. Peripheral H1-rec...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00626365
更新日期：1991-01-01 00:00:00
abstract：OBJECTIVE:To examine the effect of fluconazole, a potent inhibitor of CYP2C9 and CYP2C19, on the pharmacokinetics of rosuvastatin in healthy volunteers. Significantly increased plasma concentrations of fluvastatin have been observed following co-administration with fluconazole. METHODS:This was a randomised, double-bl...
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/s00228-002-0508-8
更新日期：2002-11-01 00:00:00
abstract：:As a target group, geriataric patients were selected for pharmacokinetic studies with terodiline (Mictrol), an anticholinergic and calcium antagonist drug effective in the treatment of urinary incontinence. The single-dose kinetics in the geriatric patients (mean age 82 years) differed significantly from that previous...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00540958
更新日期：1988-01-01 00:00:00
abstract：OBJECTIVE:To describe the epidemiology of psychotropic drug use in a sample of Italian outpatient psychiatric services. METHODS:Drug-utilisation survey conducted within the framework of a broader prospective follow-up study with 67 Italian outpatient psychiatric services. RESULTS:The data concern 2322 patients recrui...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,多中心研究
doi：10.1007/s002280050694
更新日期：1999-11-01 00:00:00
abstract：:The pharmacokinetic profiles of transdermal timolol 6 and 24 mg (as 5 and 20% w/v patches) was studied in four healthy young volunteers. To assess its bioavailability, the pharmacokinetics of an IV infusion of timolol maleate 5 mg was also determined in the same subjects. When the 20% (w/v) timolol patch was applied, ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00315551
更新日期：1993-01-01 00:00:00
abstract：:The effect of menstrual cycle on the pharmacokinetics of theophylline has been studied in 9 female asthmatic patients. At three different times during the cycle (first, tenth and twentieth days) each subject received an i.v. infusion of 240 mg theophylline. Significant changes were found in the kinetics of theophyllin...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF02657059
更新日期：1990-01-01 00:00:00
abstract：PURPOSE:Perhexiline is a prophylactic anti-ischaemic agent with weak calcium antagonist effect which has been increasingly utilised in the management of refractory angina. The metabolic clearance of perhexiline is modulated by CYP2D6 metaboliser status and stereoselectivity. The current study sought to (1) determine wh...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1007/s00228-015-1934-8
更新日期：2015-12-01 00:00:00
abstract：OBJECTIVE:To describe trends in opioid consumption in Israel (morphine, methadone, oxycodone, pethidine, fentanyl, buprenorphine, codeine, and dextropropoxyphene) over the 9 years, 2000-2008, and to explore explanations for changes in consumption, in amounts and the pattern. METHODS:Data for the 2000-2008 period (all ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-010-0932-0
更新日期：2011-02-01 00:00:00
abstract：:Verapamil, 0.1 mg/kg body wt, was injected i.v. over 2 minutes in 8 subjectively healthy middle-aged men, followed by a continuous infusion of 0.007 mg/kg body wt per minute. Prior to the injection several of the subjects had raised pulmonary or systemic arterial pressures. At rest, the central pressures increased sli...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00562656
更新日期：1975-06-13 00:00:00
abstract：:We have studied the pharmacokinetics of methotrexate in patients with rheumatoid arthritis concurrently treated with choline magnesium trisalicylate, ibuprofen, naproxen, or a non-NSAID analgesic (control treatment). The apparent systemic clearance of methotrexate was significantly reduced by all three treatments. Tri...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00278469
更新日期：1992-01-01 00:00:00
abstract：OBJECTIVE:To study the effects of possible interactions between levosimendan and warfarin on pharmacokinetics and pharmacodynamics. Furthermore, the effects of levosimendan on blood coagulation were investigated. METHODS:Open, randomised cross-over design with two treatment phases was used. During one phase, levosimen...
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/s002280000204
更新日期：2000-12-01 00:00:00
abstract：:The pharmacokinetics of intravenous enprofylline has been studied in 8 children with asthma. The mean plasma half-life of enprofylline (1.0 h) was considerably shorter than that previously reported in adults. The half-life determined from log urine excretion rate data was identical to the plasma half-life, so urine ex...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00637683
更新日期：1987-01-01 00:00:00
abstract：:The relation between plasma concentration of theophylline and number of apnea preterm infants was studied in six patients. The apnea frequency was monitored after cessation of theophylline treatment and plotted against the log plasma concentration of theophylline. It was calculated that at an average plasma concentrat...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00561480
更新日期：1980-07-01 00:00:00
abstract：:The cardiovascular and central nervous system effects of the kappa opioid receptor agonist U-62066E were investigated in ten normal male subjects who received U-62066E or placebo with low or high dose naloxone in a randomized, double blind study. Blood pressure and heart rate in the supine and standing position, plasm...
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/BF00192549
更新日期：1994-01-01 00:00:00
abstract：:Amitriptyline has clinically important interactions with ethanol. Five healthy volunteers received 25 mg of amitriptyline orally, preceded by one hour and followed for eight hours by oral ethanol (or juice), dosed to achieve and maintain blood ethanol concentrations of 800 mg/l. In the presence of ethanol, amitriptyli...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF01037943
更新日期：1983-01-01 00:00:00
abstract：PURPOSE:To develop a limited sampling strategy (LSS) to predict area under the concentration-time curve (AUC) ratios of omeprazole (AUC(OPZ)) to its metabolites 5-hydroxyomeprazole (AUC(5OH)) and omeprazole sulfone (AUC(SUL)) as phenotyping parameters for cytochrome P450 (CYP) 2C19 and 3A. METHODS:Data were obtained f...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-011-1136-y
更新日期：2012-04-01 00:00:00
abstract：OBJECTIVE:Iloprost is a potent PGI2 mimetic, which has been shown to be therapeutically effective in several vascular disorders. Due to its rapid clearance from the central compartment, iloprost is administered mainly by i.v. infusion, which limits its use to hospitalized patients. In order to improve pharmacotherapeut...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,多中心研究
doi：10.1007/s002280050336
更新日期：1997-01-01 00:00:00
abstract：:Unstable angina is a clinical syndrome characterized by increased rate and severity of angina pectoris attacks and, sometimes but not always, accompanied by ECG changes similar to those seen in coronary insufficiency. According to the present conception of the pathogenesis, ruptures at points of high-grade stenosis in...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,评审
doi：10.1007/BF01417569
更新日期：1990-01-01 00:00:00
abstract：PURPOSE:To investigate possible differences in the time course of vasodilating effects of atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP) in humans. METHODS:We measured forearm blood flow (FBF) by strain gauge plethymography and cyclic GMP spillover during and after intra-arterial infusions of BNP...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-008-0516-4
更新日期：2008-09-01 00:00:00
abstract：:The effect beta-adrenoceptor blockade on the pressor response to tyramine has been investigated in 6 healthy volunteers, each submitted to an i.v. tyramine pressor test before and after 7 days of propranolol 40 mg b.d. or indenolol 60 mg o.d. Tyramine was given as i.v. boluses of 1-6 mg, alternating with saline, in a ...
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/BF00540953
更新日期：1988-01-01 00:00:00
abstract：:The effect of drinking grapefruit juice on the acute pharmacokinetic and haemodynamic actions of the dihydropyridine calcium antagonist felodipine given as a 5 mg plain tablet has been studied in nine, healthy, middle-aged males. Compared to water, grapefruit juice caused an increase in Cmax from mean 6 to 16 nmol.l-1...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00266354
更新日期：1992-01-01 00:00:00
