The acute changes seen in cardiac glycoside receptor sites, 86rubidium uptake and intracellular sodium concentrations in the erythrocytes of patients during the early phases of digoxin therapy are not found during chronic therapy: pharmacological and ther

abstract：:1 The disposition in urine of debrisoquine and its hydroxylated metabolites has been studied in subjects of the 'extensive metabolizer' (EM; n = 5) and 'poor metabolizer' (PM; n = 5) phenotypes. The 4-hydroxylation of debrisoquine by PM subjects following a 10 mg oral dose was capacity-limited and displayed significan...

journal_title：British journal of clinical pharmacology

authors： Sloan TP,Lancaster R,Shah RR,Idle JR,Smith RL

更新日期：1983-04-01 00:00:00

abstract：:1. Using human mononuclear leucocytes as target cells, we have investigated the bioactivation of dapsone (DDS) to a cytotoxic metabolite in the presence of microsomes from nine human livers. Values for NADPH dependent toxicity ranged from 8.8-27% (15.8 +/- 5.9%) and were similar to those for microsomes from control mi...

journal_title：British journal of clinical pharmacology

authors： Coleman MD,Breckenridge AM,Park BK

更新日期：1989-10-01 00:00:00

abstract：:1 Aspirin is partly hydrolyzed to salicylic acid during absorption. Absorbed aspirin is rapidly hydrolyzed systemically. Salicylic acid elimination kinetics are dependent on drug concentration due to the limited capacity of two major biotransformation pathways: formation of salicyluric acid and of salicylphenolic gluc...

journal_title：British journal of clinical pharmacology

authors： Levy G

更新日期：1980-10-01 00:00:00

abstract：AIMS:Women experience more adverse drug reactions (ADR) to antiretroviral therapy than men. This may be attributed to higher plasma concentrations of protease inhibitors due to pharmacokinetic interactions with hormonal preparations. Thus, in the present study we aimed to investigate the influence of oral contraceptive...

journal_title：British journal of clinical pharmacology

authors： Fröhlich M,Burhenne J,Martin-Facklam M,Weiss J,von Wolff M,Strowitzki T,Walter-Sack I,Haefeli WE

更新日期：2004-03-01 00:00:00

abstract：AIMS:There is a trend for more flexibility in timing of evidence generation in relation to marketing authorization, including the option to complete phase III trials after authorization or not at all. This paper investigated the relation between phase II and III clinical trial efficacy in oncology. METHODS:All oncolog...

journal_title：British journal of clinical pharmacology

authors： Vreman RA,Belitser SV,Mota ATM,Hövels AM,Goettsch WG,Roes KCB,Leufkens HGM,Mantel-Teeuwisse AK

更新日期：2020-07-01 00:00:00

abstract：:1. A two compartment system, comprising two adjacent teflon chambers separated by a semi-permeable membrane, has been devised with which to investigate the generation of drug metabolites that are toxic to human cells in vitro. 2. Compartment A contained a drug-metabolising system (human liver microsomes +/- NADPH) and...

journal_title：British journal of clinical pharmacology

authors： Riley RJ,Roberts P,Coleman MD,Kitteringham NR,Park BK

更新日期：1990-09-01 00:00:00

abstract：:Scientific advice (SA) is an important tool offered by regulators to help developers generate robust evidence on a medicine's benefits and risks. Drawing on accumulated experience and looking at the SA provided by the European Medicines Agency in 2018 to advanced therapy medicinal products originally developed by publ...

journal_title：British journal of clinical pharmacology

authors： Tavridou A,Rogers D,Bonelli M,Schiel A,Hidalgo-Simon A

更新日期：2020-11-25 00:00:00

abstract：AIM:Amiselimod (MT-1303) is a selective sphingosine 1-phosphate 1 (S1P1 ) receptor modulator which is currently being developed for the treatment of various autoimmune diseases. Unlike some other S1P receptor modulators, amiselimod seemed to show a favourable cardiac safety profile in preclinical, phase I and II studie...

journal_title：British journal of clinical pharmacology

authors： Harada T,Wilbraham D,de La Borderie G,Inoue S,Bush J,Camm AJ

更新日期：2017-05-01 00:00:00

abstract：WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT:Performance-enhancing dietary supplements have not been clinically tested for safety or efficacy. In clinical trials performed under resting conditions, performance-enhancing supplements raise blood pressure and affect glucose homeostasis. The effect of exercise on the pharmacok...

journal_title：British journal of clinical pharmacology

authors： Haller CA,Duan M,Jacob P 3rd,Benowitz N

更新日期：2008-06-01 00:00:00

abstract：:The deployment of artesunate for severe malaria and the artemisinin combination therapies (ACTs) for uncomplicated malaria has been a major advance in antimalarial therapeutics. These drugs have reduced treated mortality, accelerated recovery and reduced treatment failure rates and transmission from the treated infect...

journal_title：British journal of clinical pharmacology

authors： Hanboonkunupakarn B,White NJ

更新日期：2020-07-12 00:00:00

abstract：:This double-blind study in 60 hospitalized female patients comparing midazolam 15 mg, oxazepam 15 mg and placebo, demonstrated an inter-group difference in favour of midazolam with regard to efficacy. The sleep parameters of onset latency and duration were improved by midazolam. All three compounds were very well tole...

journal_title：British journal of clinical pharmacology

authors： Fischbach R

更新日期：1983-01-01 00:00:00

abstract：AIMS:5-hydroxytryptamine3 receptor antagonists act antiemetically and slow colonic transit. This study evaluated effects of the high-affinity 5-HT3 antagonist, cilansetron, on fasting, meal-and anticholinesterase-stimulated phasic contractile activity of the human sigmoid colon as well as on bowel habits and stool cons...

journal_title：British journal of clinical pharmacology

authors： Stacher G,Weber U,Stacher-Janotta G,Bauer P,Huber K,Holzäpfel A,Krause G,Steinborn C

更新日期：2000-05-01 00:00:00

abstract：AIM:We investigated whether moxifloxacin-induced QTc prolongations in Japanese and Caucasian healthy male volunteers were significantly different. METHODS:A two period, randomized, crossover, ICH-E14-compliant thorough QT (TQT) study compared placebo-corrected changes in QTc interval from baseline (ΔΔQTc F) and concen...

journal_title：British journal of clinical pharmacology

authors： Morganroth J,Wang Y,Thorn M,Kumagai Y,Harris S,Stockbridge N,Kleiman R,Shah R

更新日期：2015-09-01 00:00:00

abstract：:1. N-hydroxylation is thought to be an essential step in the haemotoxicity of dapsone (DDS). To investigate both metabolism-dependent and cell-selective drug toxicity in vitro we have developed a three-compartment system in which an hepatic drug metabolizing system is contained within a central compartment separated b...

journal_title：British journal of clinical pharmacology

authors： Tingle MD,Park BK

更新日期：1993-07-01 00:00:00

abstract：:1. The 5-hydroxytryptamine (5-HT3) receptor antagonist, GR 38032F, which possesses potent anti-emetic properties in vomiting induced by cancer chemotherapeutic drugs, has been tested to determine its value in the prophylaxis of motion sickness induced by cross-coupled stimulation. The double-blind trial compared GR 38...

journal_title：British journal of clinical pharmacology

authors： Stott JR,Barnes GR,Wright RJ,Ruddock CJ

更新日期：1989-02-01 00:00:00

abstract：:1 The anticholinergic effects of atropine and two antihistamines (terfenadine and mequitazine) were investigated vs placebo in a double-blind study. 2 Salivary secretion, basal pupil diameter, pilocarpine (0.25%) induced miosis and heart rate were determined in eight healthy volunteers, seven male and one female, aged...

journal_title：British journal of clinical pharmacology

authors： Brion N,Beaumont D,Advenier C

更新日期：1988-01-01 00:00:00

abstract：:1 Methimazole plasma concentrations were measured in two groups of hyperthyroid subjects after the oral administration of either carbimazole or methimazole. 2 With the HPLC method it was also possible to measure the concentration of a methimazole metabolite, 3-methyl-2-thiohydantoin in one patient. 3 Large interindivi...

journal_title：British journal of clinical pharmacology

authors： Skellern GG,Knight BI,Low CK,Alexander WD,McLarty DG,Kalk WJ

更新日期：1980-02-01 00:00:00

abstract：:1. The pharmacokinetics of didanosine, trimethoprim, and sulphamethoxazole were evaluated in ten HIV seropositive asymptomatic patients as single agents and upon coadministration of single doses. 2. Using a randomized, balanced incomplete block crossover study with at least a 1-week washout period between successive t...

journal_title：British journal of clinical pharmacology

authors： Srinivas NR,Knupp CA,Batteiger B,Smith RA,Barbhaiya RH

更新日期：1996-03-01 00:00:00

abstract：:1 The effects of oxprenolol 80 mg and propranolol 80 mg on resting forearm blood flow (RFBF) and skin temperature were compared in seven normotensive subjects, for 4 h after an oral dose. 2 There was a significant fall of RFBF after propranolol (mean +/- s.e. mean 0.74 +/- 0.24 ml 100 g-1 min-1) compared to a smaller ...

journal_title：British journal of clinical pharmacology

authors： Vandenburg MJ,Conlon C,Ledingham JM

更新日期：1981-05-01 00:00:00

abstract：:1. The pharmacokinetics of proguanil were evaluated in patients with acute P. falciparum malaria receiving concomitantly proguanil hydrochloride and atovaquone. The population consisted of 203 Blacks, 112 Orientals and 55 Malays; 274 males and 96 females. Of the 370 patients, 114 and 256 patients were classified as 'p...

journal_title：British journal of clinical pharmacology

authors： Hussein Z,Eaves CJ,Hutchinson DB,Canfield CJ

更新日期：1996-11-01 00:00:00

abstract：:Ipratropium bromide (0.5 mg) and fenoterol (2 mg) produced equivalent peak bronchodilatation between 1 and 2 h after administration to eight patients with chronic partially reversible airways obstruction. The duration of action compared with saline was 6 h for ipratropium and 4 h for fenoterol. Both drugs in combinati...

journal_title：British journal of clinical pharmacology

authors： Jenkins CR,Chow CM,Fisher BL,Marlin GE

更新日期：1982-07-01 00:00:00

abstract：:1 The plasma levels of disopyramide and mono-N-dealkyldisopyramide were measured from 118 patients, and the protein binding of both drugs from 50 patients during chronic oral disopyramide therapy. 2 No significant correlation was seen between the daily dose of disopyramide and the achieved plasma drug concentration. 3...

journal_title：British journal of clinical pharmacology

authors： Aitio ML

更新日期：1981-04-01 00:00:00

abstract：AIMS:In vitro data indicate that imipramine (IMI), a widely used tricyclic antidepressant drug, is N-demethylated by several isoforms of cytochrome P450, which include CYP3A4. The aim of this study was to investigate the role of CYP3A in the in vivo N-demethylation of IMI. METHODS:Healthy subjects were given troleando...

journal_title：British journal of clinical pharmacology

authors： Wang JS,Wang W,Xie HG,Huang SL,Zhou HH

更新日期：1997-08-01 00:00:00

abstract：AIMS:We investigated the effect of angiotensin converting enzyme inhibitors (ACEIs) on postsynaptic adrenoceptor sensitivity and compared the effect of the lipophilic ACEI, quinapril, and that of hydrophilic agent, enalapril in human vessels. METHODS:Alpha-adrenoceptor sensitivity was evaluated using the dorsal hand v...

journal_title：British journal of clinical pharmacology

authors： Kimura M,Umemura K,Kosuge K,Nishimoto M,Ohashi K,Nakashima M

更新日期：1998-12-01 00:00:00

abstract：:In a randomised crossover study in volunteers plasma midazolam levels were estimated for 24 h following 15 mg by mouth, either preceded by no medication or following 24 h therapy with ranitidine. Administration of the H2-receptor blocker significantly increased bioavailability of the benzodiazepine and resulted in hig...

journal_title：British journal of clinical pharmacology

authors： Elwood RJ,Hildebrand PJ,Dundee JW,Collier PS

更新日期：1983-06-01 00:00:00

abstract：:1. The effect of nomifensine on the uptake of 5-hydroxytryptamine (5-HT) and dopamine (DA) into human platelet-rich plasma has been studied. 2. A significant inhibition of DA uptake was observed at nomifensine 10(-6) M. 3. 5-HT uptake was significantly inhibited only at nomifensine 10(-4) M or more. 4. These results a...

journal_title：British journal of clinical pharmacology

authors： Ehsanullah RS,Turner P

更新日期：1977-01-01 00:00:00

abstract：:Three hypothalamic regulatory hormones, thyrotrophin-releasing hormone (TRH), luteinizing hormone/follicle-stimulating hormone-releasing hormone (LH/FSH-RH) and growth hormone-release inhibiting hormone (GH-RIH) given intravenously had no effect on the electroencephalographic response known as the contingent negative ...

journal_title：British journal of clinical pharmacology

authors： Ashton H,Millman JE,Telford R,Thompson JW,Davies TF,Hall R

更新日期：1976-08-01 00:00:00

abstract：AIMS:To assess the effect of the calcitonin gene-related peptide (CGRP) receptor antagonist, telcagepant, on the haemodynamic response to sublingual nitroglycerin (NTG). METHODS:Twenty-two healthy male volunteers participated in a randomized, placebo-controlled, double-blind, two-period, crossover study. Subjects rece...

journal_title：British journal of clinical pharmacology

authors： Van der Schueren BJ,Blanchard R,Murphy MG,Palcza J,De Lepeleire I,Van Hecken A,Depré M,de Hoon JN

更新日期：2011-05-01 00:00:00

abstract：:1. The in vitro metabolism of omeprazole was studied in human liver microsomes in order to define the secondary metabolic pathways and identify the cytochrome P450 (CYP) isoforms responsible for the formation of the secondary metabolites of omeprazole. 2. The major secondary omeprazole metabolite was the hydroxysulpho...

journal_title：British journal of clinical pharmacology

authors： Andersson T,Miners JO,Veronese ME,Birkett DJ

更新日期：1994-06-01 00:00:00

abstract：AIMS:To quantify usage of COX-2 inhibitors compared with nonselective NSAIDs and to determine their impact (including financial) on the co-prescription of antipeptic ulcer (anti-PU) drugs. METHODS:The Irish General Medical Services prescription database (covering 1.2 million people) was examined for NSAID prescription...

journal_title：British journal of clinical pharmacology

authors： Teeling M,Bennett K,Feely J

更新日期：2004-03-01 00:00:00