Abstract:
:The beta-adrenoceptor blocking activity of the new Class Ic-antiarrhythmic drug diprafenone has been determined in man in comparison with that of propranolol, using the standardized isoproterenol test. Following placebo, the dose of isoproterenol which increased the heart rate by 25 beats.min-1 (CD25) was 0.84 (0.1-2.72) micrograms (median and range). Two hours following single oral doses of 200 mg diprafenone (3.61 micrograms; 1.53-44.15) or 40 mg propranolol (16.06 micrograms; 9.15-27.04) significantly higher CD25-values were found. The affinity constants for the beta-adrenergic receptors calculated on the basis of free drug in the plasma were similar for propranolol and diprafenone (2.79 vs. 2.60 nM-1, respectively). Thus, diprafenone showed a definite degree of beta-blocking activity in a clinically relevant range of plasma concentrations.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Wagner F,Jähnchen E,Trenk Ddoi
10.1007/BF00637739subject
Has Abstractpub_date
1989-01-01 00:00:00pages
579-82issue
6eissn
0031-6970issn
1432-1041journal_volume
36pub_type
临床试验,杂志文章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: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:PURPOSE:The aim of this study was to investigate the contributions of non-genetic and genetic factors on the variability of stable warfarin doses in Thai patients. METHODS:A total of 250 Thai patients with stable warfarin doses were enrolled in the study. Demographics and clinical data, e.g., age, body mass index, ind...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-017-2265-8
更新日期:2017-08-01 00:00:00
abstract::The cleansing effects on pus and debris of streptokinase-streptodornase and of stabilized crystalline trypsin were compared in 40 patients (12 males, 28 females) with necrotic varicose or arteriosclerotic leg ulcers. Both preparations produced significant partial or total cleansing of the ulcers of necrotic material, ...
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/BF00542211
更新日期:1983-01-01 00:00:00
abstract:OBJECTIVE:NXY-059 is a nitrone-based, free-radical trapping agent being developed for the treatment of acute ischaemic stroke. Elimination of NXY-059 is primarily renal. The objective of the study was to investigate the pharmacokinetics of NXY-059 in subjects with renal impairment. METHODS:Twenty-four subjects with a ...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-002-0478-x
更新日期:2002-09-01 00:00:00
abstract:PURPOSE:To investigate pharmacokinetics (PK) of encapsulated CPT-11, released CPT-11 and the active metabolite SN-38 following administration of IHL-305 and to identify factors that may influence IHL-305 PK. METHODS:Plasma samples from 39 patients with solid tumors were collected in a phase I study. IHL-305 was admini...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-013-1580-y
更新日期:2013-12-01 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:OBJECTIVE:After liver transplantation (LT), genotypic differences between the recipient and the transplanted liver, medications and post-LT complications may all affect drug metabolism. We have studied the effect of two CYP2D6 mutations in the donor and the recipient on post-LT CYP2D6 phenotype. METHOD:The CYP2D6 phen...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050419
更新日期:1998-03-01 00:00:00
abstract:OBJECTIVE:Biotransformation of metoprolol to alpha-hydroxymetoprolol (HM) and O-demethylmetoprolol (ODM) is mediated by CYP2D6. The selective serotonin reuptake inhibitors (SSRIs) are known to inhibit CYP2D6. The aim was to study in vitro the potential inhibitory effect of SSRIs on metoprolol biotransformation. METHOD...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050456
更新日期:1998-05-01 00:00:00
abstract::The pharmacokinetics of metoclopramide has been studied after acute IV administration to 12 patients with hepatic cirrhosis (6 with and 6 without ascites) and 6 control subjects. The elimination half-life was significantly longer in patients (11.4 h and 9.9 h in those with and without ascites, respectively, vs 6.4 h i...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00265857
更新日期:1991-01-01 00:00:00
abstract::Individual variation in the half-life of caffeine in the body was measured by HPLC analysis of saliva samples. The mean for adult males and non-pregnant females was 3.4 h (range 2-5 h, n = 25), and 8.3 h (range 3-16 h, n = 57) for pregnant women. After delivery, in most cases the values returned to normal within one m...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00637512
更新日期:1981-01-01 00:00:00
abstract::The duration and extent of cardiac beta-blockade and their relationship to propranolol pharmacokinetics were assessed in nine healthy volunteers. Each subject received 160 mg of regular propranolol (R), 160 mg of sustained-release propranolol (SR) and no drug (control), both as single doses and once daily for 7 days. ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00637569
更新日期:1987-01-01 00:00:00
abstract:PURPOSE:To investigate associations between antidepressant use patterns and risk of fatal and non-fatal suicidal behaviours in older adults who initiated antidepressant therapy. METHOD:A national population-based cohort study conducted among Swedish residents aged ≥ 75 years who initiated antidepressant treatment. Pat...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-017-2360-x
更新日期:2018-02-01 00:00:00
abstract::The aim of the study was to examine the effect of chronic angiotensin converting enzyme inhibition on haemodynamics and left ventricular performance during long-lasting exercise at the anaerobic threshold. For this purpose exercise haemodynamics and left ventricular performance were assessed in 14 physically trained h...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00194331
更新日期:1995-01-01 00:00:00
abstract::We have studied the pharmacokinetics of fluconazole in five patients on long-term haemodialysis. The single-pass extraction rate of the dialyzer was 59 (3.5)% (n = 4), and the serum concentration was reduced by haemodialysis for 3 or 4 h by 26 (3.2)% (n = 5) and 39 (2.2)% (n = 9) respectively. The estimated amount ext...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00265934
更新日期:1992-01-01 00:00:00
abstract:OBJECTIVES:To assess relative roles of the intestinal and hepatic stereoselective metabolism of nicardipine in an oral first-pass disposal with and without grapefruit juice intake. METHODS:The kinetic profiles of (+)- and (-)-nicardipine were studied in the six normal healthy male volunteers who received oral (40 mg) ...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s002280000235
更新日期:2000-12-01 00:00:00
abstract::The sulphation of (+) and (-) terbutaline was investigated in specimens of human intestinal mucosa isolated from the duodenum, ileum, ascending colon and sigmoid colon and in specimens of liver and lung. The lung specimens came from 8 current smokers and 11 ex-smokers, the latter having stopped at least 3 months befor...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00315522
更新日期:1993-01-01 00:00:00
abstract::Plasma aspirin, salicylate and salicyluric acid concentrations were monitored in young, elderly and alcoholic subjects after ingestion of a single 1.2 g dose of soluble aspirin. The plasma aspirin, salicylate and unbound salicylate concentration-time profiles varied considerably between individual subjects. Most of th...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00543800
更新日期:1983-01-01 00:00:00
abstract:OBJECTIVE:We investigated whether interindividual differences in the pharmacokinetic disposition of lansoprazole are attributed to the genetic polymorphism of CYP2C19 which occurred by two mutations. CYP2C19m1 and CYP2C19m2, in 20 Japanese subjects. METHODS:Polymerase chain reaction (PCR) restriction fragment length p...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050307
更新日期:1997-01-01 00:00:00
abstract:PURPOSE:Propofol anesthesia is usually accompanied by hypotensive responses, which are at least in part mediated by nitric oxide (NO). Arginase I (ARG1) and arginase II (ARG2) compete with NO synthases for their common substrate L-arginine, therefore influencing the NO formation. We examined here whether ARG1 and ARG2 ...
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: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::The pharmacokinetics of mexiletine, a Class I antiarrhythmic drug, was investigated in 6 healthy volunteers after single oral doses and 15 min intravenous infusions of 3 mg/kg. Cimetidine and ranitidine are commonly used H2-receptor antagonists, which interact adversely with many drugs, e.g. inhibition of the metaboli...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00558298
更新日期:1989-01-01 00:00:00
abstract::The relationship between the serum protein binding of carbamazepine (CBZ) and carbamazepine-10,11 epoxide (CBZ-E) and the concentration of alpha 1-acid glycoprotein (AAG) and albumin (HSA) was examined in 39 CBZ-treated epileptic children aged 4 months to 12 years. A significant inverse correlation was found between t...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00547424
更新日期:1985-01-01 00:00:00
abstract::We have previously shown that inhaled salbutamol further increases the bronchodilator response after the maximum effect of theophylline has been obtained in patients with severe chronic bronchitis. We now report the results of adding maximally effective doses of theophylline to the maximum response obtainable from sal...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00542540
更新日期:1982-01-01 00:00:00
abstract::The effect of ethanol intake on disopyramide elimination was examined in an open crossover study in six healthy volunteers. No effect of ethanol on the elimination half-life or total body clearance of disopyramide was found, although it did decrease the percentage of mono-N-dealkylated disopyramide excreted in the uri...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00544024
更新日期:1983-01-01 00:00:00
abstract::The cellular sources or molecular mechanisms responsible for the derangement of vasoactive prostanoid levels during immunosuppressive cyclosporin (CSA) therapy have not been defined. Using cultured rat glomerular mesangial cells (MC), the cytostatic, cytotoxic and prostanoid synthesis modulating effects of CSA and FK-...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF01428385
更新日期:1993-01-01 00:00:00
abstract:PURPOSE:To gain insight into the experiences and handling of adverse drug reactions (ADRs) by the staffs of public primary healthcare (PHC) clinics in Eastern Cape Province, South Africa, as well as their perceptions of related adherence challenges in the treatment and follow-up of human immunodeficiency virus (HIV)-po...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-012-1254-1
更新日期:2012-09-01 00:00:00
abstract::The antihypertensive effect of labetalol (L) was compared with that of clonidine (C) in a randomized cross-over study in 17 hypertensive outpatients on bendrofluazide (B). After treatment for two weeks with B(5 mg qd), either L (100 mg tid) or C (0.1 mg tid) was given and their doses were titrated at 2-weekly visits u...
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/BF00542319
更新日期:1982-01-01 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: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