Abstract:
OBJECTIVE:The pharmacokinetics of orally and intravenously administered valsartan were determined in two studies. In a first pilot study, three i.v. doses of valsartan were given in an ascending manner (5, 10 and 20 mg) to evaluate tolerability and basic pharmacokinetics of the i.v. formulation. In a second study, the absolute bioavailability of 80 mg valsartan from a capsule and a buffered solution was compared with a 20 mg i.v. dose. METHODS:The concentrations of valsartan in plasma and urine were measured using HPLC. The disposition of valsartan after an i.v. dose was characterized by biphasic decay kinetics, with a distribution phase (half-life 1.0 h), followed by a longer elimination phase (half-life 9.5 h). The volume of distribution at steady state was 16.9 l, and the total body clearance 2.2 l.h-1. 29% of the i.v. dose was recovered unchanged in the urine. RESULTS:Plasma levels peaked 2 h after oral administration of the 80 mg capsule. Thereafter, plasma levels declined biexponentially with a terminal t1/2 of 7.0 h. Cmax was reached 1 h after administration of the solution, and t1/2 was 7.5 h. On average 7.3% (capsule) and 12.6% (solution) of the dose was excreted in the urine as the unchanged drug. The fraction of dose absorbed and systemically available after oral administration was 0.23 for the capsule and 0.39 for the solution, based on AUC. Absorption appeared to follow two first-order processes. The first phase was rapid, with a half-life of 0.5 h and 0.9 h for solution and capsule, respectively. The slower absorption phase was characterized by a half-life of 6.5 h for the solution and 3.5 h for the capsule. Most of the drug was absorbed during the period 0.4 h to 3 h post-dosing, and 90% of the fraction absorbed from the capsule was absorbed within 5 h.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Flesch G,Müller P,Lloyd Pdoi
10.1007/s002280050259subject
Has Abstractpub_date
1997-01-01 00:00:00pages
115-20issue
2eissn
0031-6970issn
1432-1041journal_volume
52pub_type
临床试验,杂志文章,随机对照试验abstract:OBJECTIVE:In elderly patients, both falls and impaired memory are considerable medical problems. Hypnotics, which are frequently administered to this patient group for the treatment of insomnia, should ideally not impair equilibrium or memory functions. This double-blind, randomised, four-way, cross-over study investig...
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/s00228-003-0591-5
更新日期:2003-07-01 00:00:00
abstract:BACKGROUND:Xanthine oxidase (XO) is one of the two interconvertible forms of xanthine oxidoreductase and well-studied for its role in purine catabolism and that of other purine analogues, drugs especially. Our study investigated the incidence of polymorphism in phenotypes along with the influence of gender and age on e...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-015-1852-9
更新日期:2015-06-01 00:00:00
abstract:OBJECTIVE:To assess the haemodynamic effects of short-term treatment with dofetilide in comparison with sotalol in patients with ischaemic heart disease. METHODS:Twelve patients with ischaemic heart disease and sustained ventricular tachycardia were treated with dofetilide [500 microg twice daily (b.i.d.)] or sotalol ...
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/s00228-002-0464-3
更新日期:2002-06-01 00:00:00
abstract:OBJECTIVE:UDP-glucuronosyltransferases (UGTs) UGT1A9 and UGT2B7 are involved in the metabolism of antimalarial dihydroartemisinin and antiretroviral zidovudine. Our aim was to analyze the prevalence of UGT1A9 (chromosome 2) and UGT2B7 (chromosome 4) nonsynonymous single nucleotide polymorphisms (SNPs) in West African (...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-006-0206-z
更新日期:2007-01-01 00:00:00
abstract::The effects of single oral doses of mequitazine (5 and 10 mg), terfenadine (60 mg) and triprolidine (10 mg) as active controls, and placebo were evaluated on visuo-motor coordination, digit symbol substitution, critical flicker fusion and dynamic visual acuity, and on subjective assessments of mood and well-being in s...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00542129
更新日期:1983-01-01 00:00:00
abstract::The pharmacokinetics of lorazepam was examined in 10 male patients with insulin-dependent diabetes mellitus before and following treatment with neomycin and cholestyramine. Neomycin and cholestyramine were given in an attempt to block the enterohepatic circulation of lorazepam and so to permit an in vivo estimate of h...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00198307
更新日期:1995-01-01 00:00:00
abstract:PURPOSE:The purpose of this study is to investigate the association between polypharmacy with health-related quality of life (HRQoL) and medication regimen complexity with HRQoL in residential aged care facilities (RACFs). METHODS:A cross-sectional study of 383 residents from six Australian RACFs was conducted. The pr...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-016-2075-4
更新日期:2016-09-01 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::The systemic availability of oral zidovudine has been studied in 13 patients with the acquired immunodeficiency syndrome (AIDS) dosed either fasting or with breakfast. The mean peak plasma concentration and AUC of zidovudine were significantly 2.8- and 1.4-times higher in fasting patients than in those treated during ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00315215
更新日期:1991-01-01 00:00:00
abstract:PURPOSE:To investigate interindividual variability in response to pain treatment, we characterized postoperative patients for morphine metabolism and for COMT, OPRM1 and UGT2B7 polymorphisms. METHODS:A total of 109 patients treated with morphine were genotyped by DNA sequencing for 12 DNA polymorphisms of the COMT, OP...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-013-1523-7
更新日期:2013-09-01 00:00:00
abstract:UNLABELLED:The steady-state pharmacokinetics of nefazodone (NEF) and its metabolites hydroxynefazodone (HO-NEF) and m-chlorophenylpiperazine (mCPP) were compared in subjects with normal and impaired renal function. PATIENTS:The Study was of parallel group design which included 7 subjects with normal (NOR) renal functi...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00192384
更新日期:1995-01-01 00:00:00
abstract:PURPOSE:To conduct a mechanistic investigation of the interaction between aliskiren and grapefruit juice in healthy subjects. METHODS:Twenty-eight subjects received an oral dose of aliskiren 300 mg (highest recommended clinical dose) with 300 mL of either water or grapefruit juice in a two-way crossover design. Safety...
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/s00228-011-1167-4
更新日期:2012-05-01 00:00:00
abstract:INTRODUCTION:Deoxycytidine kinase (DCK) is the rate-limiting enzyme of the intracellular phosphorylation of nucleoside anticancer drugs, including gemcitabine and beta-arabinofuranosylcytosine, to their active triphosphates. This study was performed to assess the occurrence and frequency of DCK polymorphisms in a predo...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-006-0162-7
更新日期:2006-08-01 00:00:00
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journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-004-0859-4
更新日期:2005-02-01 00:00:00
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journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-006-0125-z
更新日期:2006-07-01 00:00:00
abstract::Enprofylline 1 mg/kg, a new potent antiasthmatic xanthine derivative, which is mainly eliminated by renal excretion, was given intravenously to 6 normal subjects with and without oral pretreatment with 1 g probenecid. The latter caused a drop in the average total body clearance of enprofylline from 21 to 9.8 l/h, and ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00614308
更新日期:1986-01-01 00:00:00
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...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050109
更新日期:1996-01-01 00:00:00
abstract:OBJECTIVE:The effect of age on the pharmacokinetics and pharmacodynamics of prazosin (alpha 1 adrenoceptor blocker) was studied in 20 healthy volunteers. PATIENTS:Ten elderly (61-81 y) and ten young (23-28 y) subjects were studied. All subjects received 1 mg of prazosin orally in a fasting state. Serial blood samples ...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s002280050067
更新日期:1996-01-01 00:00:00
abstract::The effect of the aminoglycosides amikacin, gentamicin, netilmicin sisomicin and tobramycin on the proximal tubule of the human kidney was investigated in 78 healthy subjects. Fifteen adults were each given gentamicin, sisomicin or tobramycin 3 mg/kg bodyweight, 10 subjects received netilmicin 3 mg/kg or amikacin 15 m...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00609758
更新日期:1978-05-17 00:00:00
abstract:OBJECTIVE:A prospective study was undertaken to determine the transcorneal penetration of three topically applied fluoroquinolones into aqueous humour. METHODS:Two hundred and twenty-four patients undergoing cataract extraction received 0.3% ciprofloxacin, norfloxacin or ofloxacin eye drops by two different administra...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:1997-01-01 00:00:00
abstract::The effect of the angiotensin converting enzyme inhibitor, perindopril, on autonomic function was assessed in a double blind, placebo controlled, crossover study in 10 normotensive males. Eight milligram of perindopril given orally lowered blood pressure without a change in heart rate. Perindopril enhanced the vagally...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00614298
更新日期:1986-01-01 00:00:00
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journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-03059-9
更新日期:2021-01-07 00:00:00
abstract::General equations are derived for the disposition functions of any compartment in a linear mammillary model, when the system input occurs into a peripheral compartment. Laplace transforms and matrix algebra are used to derive these equations. Equations describing the time-course of a drug in any compartment are readil...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00561564
更新日期:1975-02-28 00:00:00
abstract:PURPOSE:Drug-related problems (DRPs) are common in paediatric pharmacotherapy, but few studies describe them from the parents' perspective. In the present survey, we have investigated the lifetime prevalence and type of DRPs in children in Finland. METHODS:This was a population-based survey of a random sample of 6,000...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-012-1426-z
更新日期:2013-04-01 00:00:00
abstract::The interaction between the main components of the new glycopeptide antibiotic teicoplanin, A2-2, A2-3, A2-4, A2-5 and A3-1, and human serum albumin has been studied in vitro by equilibrium dialysis (pH 7.4, 37 degrees C). From Scatchard analysis of the data, the calculated association constants (Ka) were: A2-2, 2.47 ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00544566
更新日期:1987-01-01 00:00:00
abstract:PURPOSE:To assess the efficacy of acetylleucine to improve or stop an attack of vertigo and dizziness (vertigo/dizziness). METHODS:Systematic review by 2 independent reviewers. Consultation of the Medline, Cochrane and ClinicalTrials.gov databases until September 2018. Keywords used: Acetylleucine, Tanganil®, Acetyl-D...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,meta分析
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更新日期:2019-05-01 00:00:00
abstract:PURPOSE:Concomitant treatment with the glucose-lowering drug metformin and the platelet aggregation inhibitor dipyridamole often occurs in patients with type 2 diabetes mellitus who have suffered a cerebrovascular event. The gastrointestinal uptake of metformin is mediated by the human equilibrative nucleoside transpor...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-016-2039-8
更新日期:2016-06-01 00:00:00
abstract:PURPOSE:We proposed a statistical criterion to detect drug-drug interactions causing adverse drug reactions in spontaneous reporting systems. METHODS:The used criterion quantitatively measures the discrepancy between the observed and expected number of adverse events via chi-square statistics. We compared the performa...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-017-2233-3
更新日期:2017-06-01 00:00:00
abstract:OBJECTIVES:Methantheline is a strong muscarinic receptor blocking drug used in the treatment of overactive bladder syndrome, hypersalivation and hyperhidrosis. To provide basic information on the pharmacokinetics, magnitude of pharmacodynamic (PD) effects and their correlations with plasma concentrations, we performed ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-012-1286-6
更新日期:2012-11-01 00:00:00
abstract::The present study was designed to investigate the effects of raised intragastric pH on the absorption of theophylline from a sustained-release formulation. Six healthy male volunteers participated in the cross-over randomised study and on one of two occasions were pretreated with 240 mg omeprazole, administered in thr...
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/BF01740660
更新日期:1992-01-01 00:00:00