Evaluation of the antimuscarinic activity of atropine, terfenadine and mequitazine in healthy volunteers.

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 between 23 and 35 years. Each volunteer received all four separate courses of treatment: i.e. terfenadine 60 mg or mequitazine 5 mg twice daily for 3 days, and one single dose on the day of the trial; for the placebo or atropine courses they received the placebo twice daily during 3 days and, on the morning of test day, either the placebo again or atropine 1 mg. Pupillary diameter was measured under standardized conditions using a pupil gauge (Smith and Nephew Pharmaceuticals Ltd). 3 Atropine significantly reduced salivary output (-2.25 +/- 0.36 ml from control values of 4.17 +/- 0.42 ml, P less than 0.001) and heart rate (-9.7 +/- 3.7 beats min-1 from 77.5 +/- 2.7, P less than 0.05). These maximal effects were observed 3 h after atropine dosing for salivary secretion and 1 h for heart rate. Atropine did not affect basal pupil diameter or pilocarpine-induced miosis. 4 Mequitazine and terfenadine did not affect salivary flow, heart rate or pilocarpine-induced miosis. 5 Terfenadine and mequitazine had no anticholinergic effect in these tests involving a limited number of subjects.

journal_name

Br J Clin Pharmacol

authors

Brion N,Beaumont D,Advenier C

doi

10.1111/j.1365-2125.1988.tb03278.x

subject

Has Abstract

pub_date

1988-01-01 00:00:00

pages

27-32

issue

1

eissn

0306-5251

issn

1365-2125

journal_volume

25

pub_type

临床试验,杂志文章
  • Pinacidil monotherapy for hypertension.

    abstract::Ten patients with mild to moderate hypertension were treated for 9 weeks with a tablet formulation of pinacidil. Mean supine blood pressure fell from 174/100 to 148/84 mm Hg and mean supine pulse increased by 3 beats/min. Daily dosage was 40-100 mg, given in two or three divided doses. Plasma urea increased significan...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1984.tb02456.x

    authors: Ward JW

    更新日期:1984-08-01 00:00:00

  • Evaluation of a long acting formulation of nicardipine in hypertension by clinic and home recorded blood pressures and Doppler aortovelography.

    abstract::1. A novel formulation of nicardipine (50% standard (short acting), 50% sustained release) was evaluated in mild hypertension in a double-blind, randomized, placebo-controlled study, using clinic measurements (Hawksley) augmented by home recorded blood pressures (Copal UA 251). 2. Nicardipine 60 mg twice daily for 28 ...

    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.1365-2125.1989.tb03418.x

    authors: Webster J,Witte K,Rawles J,Petrie JC,Jeffers TA

    更新日期:1989-05-01 00:00:00

  • Targeting mTOR for the treatment of B cell malignancies.

    abstract::Mechanistic target of rapamycin (mTOR) is a serine/threonine kinase that functions as a key regulator of cell growth, division and survival. Many haematologic malignancies exhibit elevated or aberrant mTOR activation, supporting the launch of numerous clinical trials aimed at evaluating the potential of single agent m...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.12888

    authors: Lee JS,Vo TT,Fruman DA

    更新日期:2016-11-01 00:00:00

  • The influence of naloxone on the circulatory effects of captopril.

    abstract::The fall in blood pressure produced by captopril is not accompanied by a compensatory tachycardia. Angiotensin converting enzyme may participate in the metabolism of endogenous opioids and these substances can lower blood pressure without reflex tachycardia. It is therefore possible that the hypotensive effect of capt...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1984.tb02408.x

    authors: Rubin PC,Millar JA,Sturani S,Lawrie C,Reid JL

    更新日期:1984-06-01 00:00:00

  • Altered pharmacokinetics of oral flecainide by cimetidine.

    abstract::A potential kinetic interaction between cimetidine and flecainide has been studied in eight healthy males receiving flecainide (200 mg) orally on three occasions: before any treatment and on day 2 and day 7 of 8 days' cimetidine maintenance treatment at 1 g daily. Six days pretreatment with cimetidine induced the foll...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Tjandra-Maga TB,van Hecken A,van Melle P,Verbesselt R,de Schepper PJ

    更新日期:1986-07-01 00:00:00

  • 2-Hydroxylation of ethinyloestradiol in relation to the oxidation of sparteine and antipyrine.

    abstract::The metabolism of [3H]ethinyloestradiol (EE2) was investigated in six male subjects who had been phenotyped with respect to sparteine metabolism (three metabolizers and three non-metabolizers). Urinary metabolite profiles of EE2 were virtually identical. Following enzyme hydrolysis of sulphate and glucuronide conjugat...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1984.tb02511.x

    authors: Back DJ,Maggs JL,Purba HS,Newby S,Park BK

    更新日期:1984-10-01 00:00:00

  • Effect of an alpha- and beta-adrenoceptor-blocking agent (labetalol) on haemodynamics in hypertension.

    abstract::1 The effect of an intravenous bolus of labetalol (0.6-1.6 mg/kg body weight) on central and peripheral haemodynamics was studied in nine subjects with essential hypertension and in eleven subjects with chronic renal disease and hypertension. 2 The BP reduction amounting to 20/13 mmHg was entirely due to the lowering ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1979.tb04764.x

    authors: Bahlmann J,Brod J,Hubrich W,Cachovan M,Pretschner P

    更新日期:1979-04-01 00:00:00

  • No relevant pharmacokinetic interaction between pantoprazole and mycophenolate in renal transplant patients: a randomized crossover study.

    abstract:AIMS:Mycophenolic acid (MPA) suppresses lymphocyte proliferation through inosine monophosphate dehydrogenase (IMPDH) inhibition. Two formulations have been approved: mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS). Pantoprazole (PAN) inhibits gastric acid secretion, which may alter MPA expo...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/bcp.12664

    authors: Rissling O,Glander P,Hambach P,Mai M,Brakemeier S,Klonower D,Halleck F,Singer E,Schrezenmeier EV,Dürr M,Neumayer HH,Budde K

    更新日期:2015-11-01 00:00:00

  • First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G-protein-biased sphingosine-1 phosphate receptor-1 agonist for endothelial protection.

    abstract:AIMS:SAR247799 is a selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist with potential to restore endothelial function in vascular pathologies. SAR247799, a first-in-class molecule differentiated from previous S1P1 -desensitizing molecules developed for multiple sclerosis, can activate S1P1 wi...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.14422

    authors: Bergougnan L,Armani S,Golor G,Tardat A,Vitse O,Hurbin F,Scemama M,Poitiers F,Radzik D,Gaudin C,Hovsepian L,Muslin AJ,Kirkesseli S,Deutsch P,Parkar AA

    更新日期:2020-06-10 00:00:00

  • Effect of candesartan, a type 1 angiotensin II receptor antagonist, on bronchial hyper-responsiveness to methacholine in patients with bronchial asthma.

    abstract:AIMS:Angiotensin II is a putative mediator in bronchial asthma. There have been very few studies investigating the involvement of angiotensin II receptors in bronchial hyper-responsiveness in asthmatic patients. We examined the effect of candesartan cilexetil, a specific angiotensin II type 1 (AT1) receptor antagonist,...

    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.1365-2125.2002.t01-4-01689.x

    authors: Myou S,Fujimura M,Kamio Y,Kita T,Watanabe K,Ishiura Y,Hashimoto T,Nakao S

    更新日期:2002-12-01 00:00:00

  • Ventilatory responses of healthy subjects to intravenous combinations of morphine and oxycodone under imposed hypercapnic and hypoxaemic conditions.

    abstract:AIMS:Previous isobolographic analysis revealed that coadministration of morphine and oxycodone produces synergistic antinociception in laboratory rodents. As both opioids can produce ventilatory depression, this study was designed to determine whether their ventilatory effects were synergistic when coadministered to he...

    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.1365-2125.2005.02368.x

    authors: Ladd LA,Kam PC,Williams DB,Wright AW,Smith MT,Mather LE

    更新日期:2005-05-01 00:00:00

  • Von Willebrand factor and fibrinolytic parameters during the desmopressin test in patients with Cushing's disease.

    abstract:WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT:Desmopressin is a known haemostatic agent and is also being used, albeit at lower doses, during the diagnostic work-up of Cushing's syndrome, a condition characterized by excess cortisol concentrations and frequent thromboembolic events. No study has yet evaluated whether admini...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2010.03812.x

    authors: Pecori Giraldi F,Ambrogio AG,Fatti LM,Rubini V,Cozzi G,Scacchi M,Federici AB,Cavagnini F

    更新日期:2011-01-01 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

  • Concomitant overdosing of other drugs in patients with paracetamol poisoning.

    abstract:AIMS:Paracetamol is frequently involved in intended self-poisoning, and concomitant overdosing of other drugs is commonly reported. The purpose of the study was to investigate further concomitant drug overdose in patients with paracetamol poisoning and to evaluate its effects on the outcome of the paracetamol intoxicat...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.2002.01564.x

    authors: Schmidt LE,Dalhoff K

    更新日期:2002-05-01 00:00:00

  • The effect of isoxicam on neutrophil and monocyte function.

    abstract::1 Isoxicam was found to inhibit monocyte and neutrophil cell chemotaxis at therapeutic concentrations. 2 The effect was observed after in vitro incubation of normal cells and in vivo in patients with rheumatoid arthritis. 3 Compared to other NSAIDs studied in our laboratory, isoxicam was shown to have a broader spectr...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1986.tb02991.x

    authors: Martinez JG,Murakami SI,Scheinberg MA

    更新日期:1986-01-01 00:00:00

  • Brotizolam and chronic insomnia: a multi-centre study.

    abstract::A double-blind, crossover study was carried out on the acceptability of three doses of brotizolam (0.125, 0.25 and 0.5 mg) in chronic insomniacs aged between 21 and 75 years (33 men: 42 women). Patients reported a shorter time to fall asleep and less nocturnal awakenings. Improvement in sleep was evident during the fi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1983.tb02319.x

    authors: Fritz-Osner A,Arias-Ortiz JL,Dorantes JF,Rabago-Sánchez J,Rodríguez-Tenorio A,Sánchez-Martinez J

    更新日期:1983-01-01 00:00:00

  • The pharmacokinetics of nortriptyline in patients with chronic renal failure.

    abstract::1 The pharmacokinetics of single oral doses of nortriptyline were studied in twenty patients with chronic renal failure, eight of whom were receiving treatment with haemodialysis. 2 The median nortriptyline half-life was 25.2 h (range 14.5-140.0 h) and the median nortriptyline clearance was 32.3 l/h (range 8.1-122.0 l...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1981.tb01852.x

    authors: Dawlilng S,Lynn K,Rosser R,Braithwaite R

    更新日期:1981-07-01 00:00:00

  • Microsomal prediction of in vivo clearance of CYP2C9 substrates in humans.

    abstract:AIMS:To assess the utility of human hepatic microsomes for predicting in vivo intrinsic clearance (CLint ) via the use of four cytochrome P450 2C9 substrates: phenytoin, tolbutamide (S)-ibuprofen (two pathways) and diclofenac, and to examine the role of exogenous albumin within the microsomal incubation. METHODS:V max...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.1999.00935.x

    authors: Carlile DJ,Hakooz N,Bayliss MK,Houston JB

    更新日期:1999-06-01 00:00:00

  • Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers.

    abstract::Twelve healthy volunteers were given orally placebo, itraconazole 100 mg or terbinafine 250 mg for 4 days. Midazolam 7.5 mg was ingested on the fourth day, after which plasma samples were collected and psychomotor performance tests carried out for 17 h. Itraconazole increased the area under the midazolam concentration...

    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: Ahonen J,Olkkola KT,Neuvonen PJ

    更新日期:1995-09-01 00:00:00

  • The immunocytochemical localisation and distribution of cytochrome P-450 in normal human hepatic and extrahepatic tissues with a monoclonal antibody to human cytochrome P-450.

    abstract::1. The localisation and distribution of cytochrome P-450 in human tissues has been studied by immunocytochemistry using a monoclonal antibody to a major form of human hepatic cytochrome P-450, P-450hA7, which is closely related to cytochromes P-450 HLp and P-450NF. 2. Strong immunoreactivity was identified in hepatocy...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1988.tb03331.x

    authors: Murray GI,Barnes TS,Sewell HF,Ewen SW,Melvin WT,Burke MD

    更新日期:1988-04-01 00:00:00

  • Patients' attitudes to participation in clinical trials.

    abstract::1. In order to assess attitudes of patients to participation in therapeutic trials 197 patients underwent structured interviews conducted by a single observer. Of these patients 66 were previous or current participants in clinical trials (group A), 12 had declined participation in a trial (group B), and 119 had never ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Bevan EG,Chee LC,McGhee SM,McInnes GT

    更新日期:1993-02-01 00:00:00

  • Effects of xamoterol on resting and exercise haemodynamics in patients with chronic heart failure.

    abstract::1. A bicycle exercise test was used to investigate functional capability and haemodynamics in 30 patients with heart failure (13 NYHA Class II, 17 Class III), before and after i.v. xamoterol (Corwin, Carwin, Corwil, Xamtol, ICI 118,587) 0.2 mg kg-1. 2. Resting heart rate fell from 78 to 74 beats min-1 (P less than 0.0...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Virk SJ,Davies MK

    更新日期:1989-01-01 00:00:00

  • Experience with the use of a corticosteroid aerosol.

    abstract::1. In 48 patients with chronic asthma who had been receiving treatment with beclomethasone dipropionate aerosol (BDA) at a daily dose of 400 microgram for several years, observations were made on the effect of increasing the dose to 800 microgram daily for 6 months. 2. There was subjective improvement in 37 of the 48 ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1977.tb04516.x

    authors: Chatterjee SS

    更新日期:1977-01-01 00:00:00

  • The effect of inhaled 5-hydroxytryptamine (5-HT, serotonin) on airway calibre in man.

    abstract::Since platelet activation has been incriminated in the pathogenesis of asthma, we have investigated the effect of one of its major granule-derived mediators, 5-hydroxytryptamine (5-HT, serotonin) on airway calibre in normal (12), atopic non-asthmatic (12) and atopic asthmatic subjects (16). On separate days subjects i...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1986.tb02923.x

    authors: Cushley MJ,Wee LH,Holgate ST

    更新日期:1986-10-01 00:00:00

  • Therapeutic interventions in acute stroke.

    abstract::1. Potential therapies for ischaemic stroke include agents to reduce oedema, to improve cerebral perfusion, to reduce excitotoxic damage, to minimise free-radical induced injury and to reduce complications such as deep venous thrombosis. 2. Of the anti-oedema drugs, steroids are ineffective and possibly dangerous; int...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1365-2125.1992.tb05655.x

    authors: Lees KR

    更新日期:1992-12-01 00:00:00

  • Central nervous system toxicity of mefenamic acid overdose compared with other NSAIDs: an analysis of cases reported to the United Kingdom National Poisons Information Service.

    abstract:AIMS:Case reports and small case series suggest increased central nervous system (CNS) toxicity, especially convulsions, after overdose of mefenamic acid, compared with other nonsteroidal anti-inflammatory drugs (NSAIDs), although comparative epidemiological studies have not been conducted. The current study compared r...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.13169

    authors: Kamour A,Crichton S,Cooper G,Lupton DJ,Eddleston M,Vale JA,Thompson JP,Thomas SH

    更新日期:2017-04-01 00:00:00

  • Non-invasive measurement of the haemodynamic effects of inhaled salbutamol, intravenous L-arginine and sublingual nitroglycerin.

    abstract:AIMS:To examine the effects of salbutamol and L-arginine, two compounds acting largely on the endothelium, and the endothelium-independent agent nitroglycerin on blood pressure, arterial compliance, cardiac function and vascular resistance. METHODS:Continuous radial pulse wave analysis, whole-body impedance cardiograp...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2009.03434.x

    authors: Tahvanainen A,Leskinen M,Koskela J,Ilveskoski E,Alanko J,Kähönen M,Kööbi T,Lehtimäki L,Moilanen E,Mustonen J,Pörsti I

    更新日期:2009-07-01 00:00:00

  • Contrasts between pindolol and propranolol concentration-response relationships.

    abstract::The plasma concentration-response relationships of oral and intravenous pindolol and propranolol have been studied in a group of eight healthy male subjects who received each dosage form in a randomized single-blind cross-over manner. Despite similar elimination half-lives, the duration of action of pindolol was longe...

    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.1365-2125.1985.tb05088.x

    authors: Carruthers SG,Pacha WL,Aellig WH

    更新日期:1985-10-01 00:00:00

  • Bioavailability and disposition of azelastine and fluticasone propionate when delivered by MP29-02, a novel aqueous nasal spray.

    abstract:WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT:• The topical second generation anti-histamine azelastine hydrochloride (AZE) and the potent corticosteroid fluticasone propionate (FP) are well established first-line treatments in allergic rhinitis (AR). • MP29-02, a novel intranasal AZE and FP formulation, has been shown to c...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.2012.04222.x

    authors: Derendorf H,Munzel U,Petzold U,Maus J,Mascher H,Hermann R,Bousquet J

    更新日期:2012-07-01 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