Abstract：
:Drug binding in the interstitial fluid as well as in the plasma must be taken into account when considering the pharmacokinetics of drugs which are highly bound to plasma proteins and have a relatively small apparent volume of distribution (V). The half-life and apparent volume of distribution of such a drug can be affected significantly by changes in the extent of binding of the drug in both the plasma and the interstitial fluid. An alteration in the fraction of drug in the tissues which is unbound will primarily affect the pharmacokinetics of drugs which have a relatively large apparent volume of distribution. The effect of changes in the plasma free fraction of drug (fP) on tissue binding can be deduced from a plot of fP versus V, but not from a plot of fP versus beta.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Faed EMdoi
10.1007/BF00609592subject
Has Abstractpub_date
1981-01-01 00:00:00pages
77-81issue
1eissn
0031-6970issn
1432-1041journal_volume
21pub_type
杂志文章abstract：BACKGROUND:Zolmitriptan is a 5HT(1B/1D) receptor agonist effective in the acute treatment of migraine. Clinical trials in the USA and Europe have demonstrated the optimal oral therapeutic dose to be 2.5 mg. The 2.5-mg oral tablet has recently been licensed in Japan. OBJECTIVE:To compare the pharmacokinetics of zolmitr...
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/s00228-002-0461-6
更新日期：2002-07-01 00:00:00
abstract：OBJECTIVE:Troglitazone is an agonist of the peroxisome proliferator-activated receptor-gamma (PPAR-gamma), which has been shown to improve the metabolic control of type 2 diabetes. Troglitazone undergoes hepatic metabolism to an inactive sulphate conjugate and an oxidative quinone metabolite with minor activity. The ob...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s002280050514
更新日期：1998-09-01 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：:We report the first placebo controlled parallel group study of once daily endralazine (5-20 mg) in hypertension uncontrolled by a beta-blocker plus a diuretic. Following a 4-week run-in period 22 patients with a sitting mean arterial pressure (MAP) greater than 110 mm Hg were entered into the study and received either...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00613452
更新日期：1985-01-01 00:00:00
abstract：OBJECTIVES:To compare the systemic exposure for intranasal mometasone furoate (MF) and fluticasone propionate (FP) aqueous nasal sprays (ANS) in terms of serum and urinary cortisol parameters and plasma pharmacokinetics. METHODS:Twelve healthy subjects completed this three-way, cross-over study. They received FPANS (5...
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/s00228-004-0763-y
更新日期：2004-06-01 00:00:00
abstract：:Changes in phenytoin concentrations caused by switching valproate formulations with different absorption rates were retrospectively investigated in eleven epileptic patients receiving treatment with both drugs. Total plasma phenytoin concentrations were measured before and after a standard tablet of valproate was repl...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00202174
更新日期：1995-01-01 00:00:00
abstract：:The pharmacokinetics of isosorbide-5-mononitrate (IS-5-MN) has been studied in two groups of healthy volunteers after oral (n = 20) and intravenous (n = 11) administration of 20 mg, which had previously been proved to be as effective as 20 mg sustained-release isosorbide dinitrate (ISDN). IS-5-MN in serum was measured...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00618777
更新日期：1981-01-01 00:00:00
abstract：OBJECTIVE:More than 11% of the Caucasian population are heterozygous or homozygous carriers of thiopurine S-methyltransferase (TPMT) mutants and are at risk for toxic side effects when treated with thiopurine drugs. Therefore, screening for TPMT polymorphisms in a patient prior to prescribing these agents is recommende...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-004-0728-1
更新日期：2004-03-01 00:00:00
abstract：:We have found transient circulating neutropenia and pulmonary sequestration of neutrophils after the intravenous injection of vindesine, a microtubule disruptor. Experiment 1 Ten patients with lung cancer were given a bolus intravenous injection of 3 mg.m-2 vindesine (Fildesine(r)). In all patients, total leukocyte an...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00193474
更新日期：1994-01-01 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：PURPOSE:The quality of drug therapy is an important issue for nursing homes. This study aimed to assess the prevalence of polypharmacy and potentially inappropriate medications (PIMs) in a large sample of nursing home residents by using the data recorded during the preparation of pill dispensers. METHODS:This is a cro...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-016-2193-z
更新日期：2017-05-01 00:00:00
abstract：:The debrisoquine/sparteine-type polymorphism of drug oxidation and the polymorphism for acetylation are two common inherited variations in human drug metabolism. The phenotypes for hydroxylation and acetylation can be predicted be newly developed methods based on mutation-specific amplification of DNA by the polymeras...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF02220616
更新日期：1992-01-01 00:00:00
abstract：:The effects of intravenous strophanthin K (0.125 and 0.25 MG) and lanatoside C (0.4, 0.8 and 1.6 mg) on systolic time intervals (STI) and impedance plethysmographic (IP)P values were studied in ten patients with compensated coronary heart disease. The heart rate decreased significantly during a two-hour study in the l...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00613426
更新日期：1975-10-10 00:00:00
abstract：:We have studied the pharmacodynamic effects of ramipril, propranolol, and their combination, as well as the effect of propranolol on the pharmacokinetics of ramipril in 12 healthy men (age 24 (SD 6) y, weight 72 (7) kg). Propranolol and placebo, ramipril and placebo, or propranolol and ramipril were given orally for f...
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/BF00315392
更新日期：1993-01-01 00:00:00
abstract：OBJECTIVE:Spontaneous reporting is the most common method used in pharmacovigilance and the best one to generate signals on new or rare adverse drug reactions (ADRs). Under-reporting is a major drawback of this system. The objective of this study was to quantify the extent of under-reporting in general practice and to ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280050498
更新日期：1998-08-01 00:00:00
abstract：OBJECTIVE:To study the influence of CYP3A4 inhibition by ketoconazole on the disposition of venlafaxine in individuals with different CYP2D6 pheno- and genotypes. METHODS:In an open two-phase study, 21 healthy volunteers with known CYP2D6 pheno- and genotype [14 extensive metabolisers (EMs), 7 poor metabolisers (PMs)]...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-003-0627-x
更新日期：2003-09-01 00:00:00
abstract：OBJECTIVE:The aim of this study was to clarify the effect of genetic polymorphisms of CYP2C19 on the pharmacokinetics of phenobarbitone (PB) using a nonlinear mixed-effects model (NONMEM) analysis in Japanese adults with epilepsy. METHODS:A total of 144 serum PB concentrations were obtained from 74 subjects treated wi...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s002280050703
更新日期：2000-02-01 00:00:00
abstract：:We have studied the kinetics of a single oral dose of mefloquine (750 mg) in 12 Thai patients with falciparum malaria and have compared the results with those of a previous study in 12 healthy Thai volunteers. All the patients responded to treatment with a mean parasite clearance time of 66.6 h and a mean fever cleara...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00637607
更新日期：1988-01-01 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：PURPOSE:Anaphylaxis is a potentially fatal systemic adverse drug reaction (ADR). It is an unpredictable and mostly dose-independent event that occurs suddenly following exposure to the causative drug. Our objective was to characterize a case series of anaphylactic reactions reported to the Portuguese Pharmacovigilance ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-012-1376-5
更新日期：2013-03-01 00:00:00
abstract：:In this paper pharmaceutical and biopharmaceutical aspects on the development of long-acting nitrate delivery systems are reviewed. Basic considerations and requirements are also discussed. Recent product development activities are presented, with an emphasis on nitroglycerin in transdermal form and oral isosorbide-5-...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,评审
doi：10.1007/BF01417560
更新日期：1990-01-01 00:00:00
abstract：:The pharmacokinetics of amoxycillin in normal male volunteers was studied during the states of bedrest, sleep and ambulation. The absorption and disposition of amoxycillin in ambulatory subjects was found to be comparable to that reported previously by other workers. Serum amoxycillin concentrations were found to be s...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00561587
更新日期：1980-08-01 00:00:00
abstract：:This study examined dosage prescribing patterns and steady-state oxipurinol plasma concentrations in 66 patients receiving chronic allopurinol therapy. Most patients (65%) were taking 300 mg allopurinol daily, although renal impairment was common. Using published guidelines, it was estimated that 35% of patients were ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00315424
更新日期：1990-01-01 00:00:00
abstract：:The efficacy of bopindolol and atenolol in the treatment of patients with chronic stable angina pectoris have been compared in a double blind, randomized study. Both bopindolol 1 mg and atenolol 100 mg for 6 weeks increased mean exercise time (25% and 22%, respectively, compared to placebo), time to angina (27% and 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/BF00314809
更新日期：1990-01-01 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：: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：: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：AIMS:The study aimed to identify and describe adverse drug reactions and adherence to clinical guidelines in patients receiving treatment for type 2 diabetes mellitus (T2DM) in Cameroon. METHODS:The method used was a cross-sectional study at a tertiary diabetes care service in Yaoundé, Cameroon. Adult T2DM patients at...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-020-02949-2
更新日期：2020-11-01 00:00:00
abstract：:The possible interaction between cetirizine 2 HCl and alcohol was studied in a double-blind, cross-over trial in 36 healthy volunteers. The performance of each volunteer was tested with a battery of five objective psychometric tests, and their subjective feelings were evaluated by visual analogue scales, and by extens...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00615227
更新日期：1988-01-01 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
