Acute and chronic effects of flosequinan on resting and exercise haemodynamics in congestive heart failure.

Abstract:

:1 The acute and chronic (8 weeks) haemodynamic responses to oral flosequinan have been investigated in 12 male patients of mean age 58.9 years with congestive heart failure of N.Y.H.A. classes II and III. 2 Flosequinan 125 mg orally significantly reduced right atrial pressure, pulmonary artery pressure and pulmonary wedge pressure prior to and following 8 weeks chronic treatment (125 mg daily). A significant decrease in systemic pressure and an increase in heart rate were also observed with acute flosequinan prior to chronic treatment. A reduction in systemic vascular resistance and an increase in cardiac index reached significance in response to flosequinan 125 mg orally following 8 weeks of therapy. 3 In the erect position, flosequinan reduced pulmonary wedge pressure and tended to reduce systemic vascular resistance, without decreasing mean arterial pressure. 4 Following chronic treatment, there was a trend towards a reduction in pulmonary wedge pressure and an increase in cardiac index, otherwise resting and exercise haemodynamics were unchanged. 5 The response to flosequinan was similar at week 1 and after 8 weeks of treatment for all of the haemodynamic parameters. 6 Flosequinan increased bicycle exercise times and attenuated exercise-induced increases in pulmonary arterial and systemic pressures. There was a trend towards an increase in treadmill exercise time. 7 Sublingual glyceryl trinitrate (0.5 mg) and oral flosequinan (125 mg) had similar effects on right atrial pressure, pulmonary arterial and pulmonary wedge pressures at 5 min and 2 h respectively post-dosing. A small additive effect on pulmonary arterial and wedge pressures was observed.

journal_name

Br J Clin Pharmacol

authors

Thomas P,O'Gorman DJ,Sheridan DJ

doi

10.1111/j.1365-2125.1993.tb00412.x

keywords:

subject

Has Abstract

pub_date

1993-12-01 00:00:00

pages

539-46

issue

6

eissn

0306-5251

issn

1365-2125

journal_volume

36

pub_type

杂志文章
  • Evaluation of the effect on heart rate variability of a beta2-adrenoceptor agonist and antagonist using non-linear scatterplot and sequence methods.

    abstract:AIMS:To examine the impact on heart rate variability (HRV), of agonism or antagonism at the cardiac beta2-adrenoceptor in healthy volunteers, using standard time-domain summary statistics and non-linear methods (scatterplot and quadrant analysis). METHODS:Under double-blind and randomised conditions (Latin square desi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.1365-2125.1999.00862.x

    authors: Hanratty CG,Silke B,Riddell JG

    更新日期:1999-02-01 00:00:00

  • A placebo-controlled study of effects of oral progesterone on performance and mood.

    abstract::1. Oral micronized progesterone (P) is proposed for the treatment of certain endocrine gynaecological disorders. To examine the effects of P on performance and mood, a randomized, placebo-controlled study of 24 healthy females ages 18-24 years on low-dose oral contraceptives was conducted. 2. Subjects were admitted to...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1992.tb04038.x

    authors: Freeman EW,Weinstock L,Rickels K,Sondheimer SJ,Coutifaris C

    更新日期:1992-03-01 00:00:00

  • Use of statins and risk of haematological malignancies: a meta-analysis of six randomized clinical trials and eight observational studies.

    abstract:AIMS:Statins have been suggested to prevent haematological malignancies. Several epidemiological studies have evaluated this association, while randomized controlled trials (RCTs) on cardiovascular outcomes have provided relevant data as secondary end-points. Our aim was to examine the strength of this association thro...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析,评审

    doi:10.1111/j.1365-2125.2007.02959.x

    authors: Bonovas S,Filioussi K,Tsantes A,Sitaras NM

    更新日期:2007-09-01 00:00:00

  • The effect of propranolol on paracetamol metabolism in man.

    abstract::Ten healthy volunteers were treated for 4 days with 160 mg propranolol HCl and placebo in random order. At the end of each treatment salivary antipyrine kinetics and the plasma kinetics and urinary excretion of paracetamol and its major metabolites were measured following a 1500 mg oral dose. Propranolol prolonged the...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1990.tb03631.x

    authors: Baraka OZ,Truman CA,Ford JM,Roberts CJ

    更新日期:1990-02-01 00:00:00

  • Measurement of blood concentrations of FK506 (tacrolimus) and its metabolites in seven liver graft patients after the first dose by h.p.l.c.-MS and microparticle enzyme immunoassay (MEIA).

    abstract::1. Blood and urine concentrations of the macrolide immunosuppressant FK506 and its metabolites were measured in seven orthotopic liver transplant patients after the first oral dose of FK506 (0.04 +/- 0.02 mg kg-1) used as primary immunosuppressant. A specific h.p.l.c.-MS assay was used, allowing the measurement of par...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1994.tb04398.x

    authors: Gonschior AK,Christians U,Braun F,Winkler M,Linck A,Baumann J,Sewing KF

    更新日期:1994-12-01 00:00:00

  • Efficacy, safety and pharmacokinetics of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control.

    abstract:AIMS:The objectives were to investigate the pharmacokinetics, pharmacodynamics and safety of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control, and then recommend the dosage regimen for Phase 2b/3 studies. METHODS:Three clinical studies were performed. First, 16 healthy subject...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/bcp.14076

    authors: Wang H,Shao F,Liu X,Xu W,Ou N,Qin X,Liu F,Hou X,Hu H,Jiang J

    更新日期:2019-11-01 00:00:00

  • Stereoselective disposition of ibuprofen in patients with compromised renal haemodynamics.

    abstract::1. The primary aim of this study was to assess the impact of renal haemodynamics on the pharmacokinetic behaviour of ibuprofen enantiomers. Thirty-two patients and ten age-matched healthy volunteers participated in this study. These patients had at least one of the following risk factors for cardiovascular disorders: ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1995.tb04536.x

    authors: Chen CY,Chen CS

    更新日期:1995-07-01 00:00:00

  • Effects of cardiac output on disposition kinetics of sorbitol: recirculatory modelling.

    abstract::1. The purpose of this study was to determine the effects of cardiac output on distribution and elimination kinetics of the marker compound sorbitol. 2. The disposition kinetics of sorbitol were investigated after rapid intravenous injection and arterial sampling in nine patients who had undergone cardiac catheterizat...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.1996.03121.x

    authors: Weiss M,Hübner GH,Hübner IG,Teichmann W

    更新日期:1996-04-01 00:00:00

  • Betaxolol and glucose-insulin relationships: studies in normal subjects taking glibenclamide or metformin.

    abstract::1. The potential interaction between selective beta 1-adrenoceptor blockers and sulphonylureas or biguanides was studied by comparing the beta 1-adrenoceptor antagonist betaxolol with placebo in 12 normal subjects taking glibenclamide or metformin in a single-blind crossover group study. 2. After a 4 day run-in period...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1990.tb03838.x

    authors: Sinclair AJ,Davies IB,Warrington SJ

    更新日期:1990-11-01 00:00:00

  • Tolerance and safety of enalapril.

    abstract::Enalapril is the result of a targeted research programme to develop a non-mercapto converting enzyme inhibitor with a long duration of action and an improved safety profile for use in the therapy of hypertension and congestive heart failure. Over 3500 patients world-wide have received enalapril or enalaprilat. Long-te...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1984.tb02604.x

    authors: McFate Smith W,Davies RO,Gabriel MA,Kramsch DM,Moncloa F,Rush JE,Walker JF

    更新日期:1984-01-01 00:00:00

  • Ipratropium bromide and fenoterol by aerosolized solution.

    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

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1982.tb04946.x

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

    更新日期:1982-07-01 00:00:00

  • Acute hypotensive effect of captopril in man modified by prostaglandin synthesis inhibition.

    abstract::1 A study was carried out to investigate the possible contribution of prostaglandins in captopril-induced hypotension. 2 Healthy volunteers and patients with essential hypertension were given single oral doses of 25 mg and 50 mg captopril respectively before and after cyclo-oxygenase inhibition with indomethacin. 3 Th...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1982.tb02063.x

    authors: Silberbauer K,Stanek B,Templ H

    更新日期:1982-01-01 00:00:00

  • Lack of systematic effects of the 5-hydroxytryptamine 3 receptor antagonist ICS 205-930 on gastric emptying and antral motor activity in patients with primary anorexia nervosa.

    abstract::1. The 5-hydroxytryptamine 3 receptor antagonist, ICS 205-930, has been reported to have potent effects on gastric smooth muscle and to enhance gastric emptying in animals, but findings in man have been inconsistent. 2. This study investigated the effects of ICS 205-930 on gastric emptying of an isotopically labelled ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Stacher G,Bergmann H,Granser-Vacariu GV,Wiesnagrotzki S,Wenzelabatzi TA,Gaupmann G,Kugi A,Steinringer H,Schneider C,Höbart J

    更新日期:1991-12-01 00:00:00

  • Effect of netazepide, a gastrin/CCK2 receptor antagonist, on gastric acid secretion and rabeprazole-induced hypergastrinaemia in healthy subjects.

    abstract:AIMS:To compare gastric acid suppression by netazepide, a gastrin/CCK2 receptor antagonist, with that by a proton pump inhibitor (PPI), and to determine if netazepide can prevent the trophic effects of PPI-induced hypergastrinaemia. METHODS:Thirty healthy subjects completed a double-blind, randomized, parallel group t...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/bcp.12534

    authors: Boyce M,Dowen S,Turnbull G,van den Berg F,Zhao CM,Chen D,Black J

    更新日期:2015-05-01 00:00:00

  • Model informed dosing of hydroxycholoroquine in COVID-19 patients: Learnings from the recent experience, remaining uncertainties and gaps.

    abstract:AIMS:In the absence of a commonly agreed dosing protocol based on pharmacokinetic (PK) considerations, the dose and treatment duration for hydroxychloroquine (HCQ) in COVID-19 disease currently vary across national guidelines and clinical study protocols. We have used a model-based approach to explore the relative impa...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.14436

    authors: Thémans P,Dauby N,Schrooyen L,Lebout F,Delforge M,Nasreddine R,Libois A,Payen MC,Konopnicki D,Wuillaume F,Lescrainier C,Verlinden V,Dogné JM,Hamdani J,Musuamba FT

    更新日期:2020-06-19 00:00:00

  • Rituximab in the treatment of autoimmune haemolytic anaemia.

    abstract::Rituximab is a B-cell depleting monoclonal antibody that is gaining popularity as an effective therapy for many autoimmune cytopenias. This article systematically evaluates its therapeutic efficacy in the treatment of different types of autoimmune haemolytic anaemia. We conclude that there is sufficient evidence to re...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.12498

    authors: Rodrigo C,Rajapakse S,Gooneratne L

    更新日期:2015-05-01 00:00:00

  • Autoinhibitory properties of the parent but not of the N-oxide metabolite contribute to infusion rate-dependent voriconazole pharmacokinetics.

    abstract:AIMS:The pharmacokinetics of voriconazole show a nonlinear dose-exposure relationship caused by inhibition of its own CYP3A-dependent metabolism. Because the magnitude of autoinhibition also depends on voriconazole concentrations, infusion rate might modulate voriconazole exposure. The impact of four different infusion...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.13297

    authors: Hohmann N,Kreuter R,Blank A,Weiss J,Burhenne J,Haefeli WE,Mikus G

    更新日期:2017-09-01 00:00:00

  • Involvement of CYP2C9 and UGT2B7 in the metabolism of zaltoprofen, a nonsteroidal anti-inflammatory drug, and its lack of clinically significant CYP inhibition potential.

    abstract:AIMS:To identify the cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) isoforms responsible for the formation of the primary metabolite(s) of zaltoprofen, and to predict possible drug interactions by investigating the inhibition of CYP isoforms in vitro. METHODS:The metabolism of zaltoprofen was studied in v...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.2002.01649.x

    authors: Furuta S,Akagawa N,Kamada E,Hiyama A,Kawabata Y,Kowata N,Inaba A,Matthews A,Hall M,Kurimoto T

    更新日期:2002-09-01 00:00:00

  • Lack of ethnic differences in the pharmacokinetics and pharmacodynamics of evolocumab between Caucasian and Asian populations.

    abstract:AIMS:To evaluate the potential ethnic differences in the pharmacokinetics (PK) and pharmacodynamics (PD) of evolocumab in Caucasian and Asian populations using population PK/PD modelling analysis. METHODS:Data from different ethnic groups in 5 Phase I clinical trials, including two American studies, one Japanese study...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.13767

    authors: Wang C,Zheng Q,Zhang M,Lu H

    更新日期:2019-01-01 00:00:00

  • Comparative wheal and flare study of mizolastine vs terfenadine, cetirizine, loratadine and placebo in healthy volunteers.

    abstract::1. Mizolastine, a new benzimidazole derivative with potent selective, non-sedative H1-histamine antagonist activity was compared with terfenadine, cetirizine and loratadine using the histamine-induced wheal and flare model in healthy volunteers. 2. Study design was a five way double-blind crossover design using a sing...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Rosenzweig P,Caplain H,Chaufour S,Ulliac N,Cabanis MJ,Thebault JJ

    更新日期:1995-11-01 00:00:00

  • Interaction of St John's wort with low-dose oral contraceptive therapy: a randomized controlled trial.

    abstract:AIMS:Breakthrough bleeding or even unwanted pregnancies have been reported in women during concomitant therapy with oral contraceptives and St John's wort extract. The aim of the present study was to investigate the effects of St John's wort extract on oral contraceptive therapy with respect to ovarian activity, breakt...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.1365-2125.2003.02005.x

    authors: Pfrunder A,Schiesser M,Gerber S,Haschke M,Bitzer J,Drewe J

    更新日期:2003-12-01 00:00:00

  • Continued use of non-steroidal anti-inflammatory drugs: an index of clinical efficacy.

    abstract::1 A double-blind entry to a trial of an active non-steroidal anti-inflammatory drug, flurbiprofen against placebo was undertaken until 100 patients with classical rheumatoid arthritis had been allocated to each treatment. 2 Each patient was given a long-term supply of drug and was asked to vary their own dosage within...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1978.tb01654.x

    authors: Rooney PJ,Capell HA,Paterson S,Buchanan WW,Dick WC

    更新日期:1978-05-01 00:00:00

  • Oral bioavailability of dabigatran etexilate (Pradaxa(®) ) after co-medication with verapamil in healthy subjects.

    abstract:AIM:To investigate the effect of the P-glycoprotein inhibitor verapamil on the pharmacokinetics and pharmacodynamics of dabigatran etexilate (DE). METHOD:In this two part multiple crossover trial in 40 healthy subjects, DE 150 mg was given alone or with verapamil at different doses, duration of treatment (single vs. m...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.2012.04453.x

    authors: Härtter S,Sennewald R,Nehmiz G,Reilly P

    更新日期:2013-04-01 00:00:00

  • Pilot drug and therapeutic committee program in Sierra Leone: a descriptive mixed method study.

    abstract:INTRODUCTION:Irrational medicine use is a global crisis, but incidences are proportionately higher in low and middle-income countries like Sierra Leone. This study explores the structure, functions, and challenges of Drug and Therapeutics Committees (DTC) an intervention towards irrational medicines use recently pilote...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.14716

    authors: Kabba JA,Koroma MM,James PB,Kitchen C,Xu S,Chang J,Saeed A,Malik UR,Jiang M,Fang Y

    更新日期:2021-01-04 00:00:00

  • Cardiovascular effects of eating, atenolol and their interaction: beta1-adrenergic modulation does not play a predominant role in the genesis of postprandial effects.

    abstract::1. Eight healthy subjects were investigated on four occasions at least 1 week apart when they either ate a standard 3100 kJ cold meal or fasted. One hour earlier, either 50 mg atenolol or placebo was administered. 2. Eating was followed by prominent changes of systolic cardiovascular function: a rise of heart rate (+7...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1993.tb00391.x

    authors: De Mey C,Enterling D,Meineke I

    更新日期:1993-11-01 00:00:00

  • A placebo-controlled study of interaction between nabumetone and acenocoumarol.

    abstract:AIMS:The use of nonsteroidal anti-inflammatory drugs (NSAIDs) in patients treated with oral anticoagulants is generally discouraged due to the risk of interactions that could increase the risk of bleeding complications. Available data suggest the NSAID, nabumetone, does not produce such an interaction. We investigated ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.1365-2125.1999.00916.x

    authors: Pardo A,García-Losa M,Fernández-Pavón A,del Castillo S,Pascual-García T,García-Méndez E,Dal-Ré R

    更新日期:1999-04-01 00:00:00

  • The potent calcitonin gene-related peptide receptor antagonist, telcagepant, does not affect nitroglycerin-induced vasodilation in healthy men.

    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

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.2010.03869.x

    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

  • Impaired theophylline clearance in patients with cor pulmonale.

    abstract::1 The relationship between serum theophylline concentration and daily dose was studied in 45 patients receiving aminophylline orally and in 36 patients receiving it by constant intravenous infusion. 2 Patients were categorized as uncomplicated chronic obstructive pulmonary disease (COPD) or COPD with cor pulmonale (...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1979.tb00893.x

    authors: Vicuna N,McNay JL,Ludden TM,Schwertner H

    更新日期:1979-01-01 00:00:00

  • Multicentre 12-week double-blind comparison of doxazosin, prazosin and placebo in patients with mild to moderate essential hypertension.

    abstract::A 12-week double-blind study was performed to compare the safety and efficacy of doxazosin, prazosin and placebo in 172 patients with essential hypertension. According to response, patients received doxazosin 1-16 mg once daily, prazosin 0.5-10 mg twice daily, or placebo. Mean final daily doses were doxazosin 11.3 mg ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1986.tb02856.x

    authors: Torvik D,Madsbu HP

    更新日期:1986-01-01 00:00:00

  • The effects of beta-adrenoceptor blockade on renin, angiotensin, aldosterone and catecholamines at rest and during exercise.

    abstract::1 beta-adrenoceptor blockade with metoprolol provoked, both at rest and during exercise, a decrease of 'active' renin and angiotensin II together with an increase of 'inactive' renin and unchanged 'total' renin. The significant exercise-provoked increases in angiotensin II, plasma renin activity and 'active', 'inactiv...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1979.tb00918.x

    authors: Lijnen PJ,Amery AK,Fagard RH,Reybrouck TM,Moerman EJ,De Schaepdryver AF

    更新日期:1979-02-01 00:00:00