Oxidation of reduced haloperidol to haloperidol: involvement of human P450IID6 (sparteine/debrisoquine monooxygenase).

abstract：AIMS:5-HT1B-receptor mediated vasoconstriction of cranial arteries is a potential mechanism by which 5-HT1B/1D-receptor agonists such as sumatriptan produce their antimigraine effects. 5-HT1B-receptors exist in other blood vessels which may give rise to unwanted vascular effects. Therefore we examined the distribution ...

journal_title：British journal of clinical pharmacology

authors： Razzaque Z,Pickard JD,Ma QP,Shaw D,Morrison K,Wang T,Longmore J

更新日期：2002-03-01 00:00:00

abstract：:1. A 1.25 mg dose of cilazapril, a new angiotensin-converting enzyme (ACE) inhibitor, was administered orally to two groups of hypertensive patients, five with normal renal function (NRF) and seven with impaired renal function (IRF), once daily for 5 or 8 consecutive days. Blood pressure, heart rate and serum ACE acti...

journal_title：British journal of clinical pharmacology

authors： Shionoiri H,Gotoh E,Sugimoto K,Takasaki I,Minamisawa K,Ishii M

更新日期：1989-01-01 00:00:00

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

authors： Virk SJ,Davies MK

更新日期：1989-01-01 00:00:00

abstract：:Self-poisoning by ingestion or inhalation is common, and it is important to study its various epidemiological manifestations with clear definitions. Data on fatal self-poisonings are recorded nationally within the UK and are codified according to the International Classification of Diseases (ICD) revision relevant at ...

journal_title：British journal of clinical pharmacology

authors： Camidge DR,Wood RJ,Bateman DN

更新日期：2003-12-01 00:00:00

abstract：:1. We report a method for measuring the concentrations of haloperidol (HL) and its major active metabolite, reduced haloperidol (RHL), in human scalp hair. 2. Hair samples were obtained from 59 patients who had been taking HL at fixed daily doses for more than 4 months and whose compliance was good. A morning pre-dose...

journal_title：British journal of clinical pharmacology

authors： Matsuno H,Uematsu T,Nakashima M

更新日期：1990-02-01 00:00:00

abstract：:1. The inhibitory effect of sufotidine, a new histamine H2-receptor antagonist, on gastric secretion of acid and pepsin was studied in six healthy male volunteers. This was a three-way, cross-over, randomized, double-blind study. On each of 3 study days, the drug in a dose of 600 mg, or placebo, was administered eithe...

journal_title：British journal of clinical pharmacology

authors： Johnston DA,Wormsley KG

更新日期：1989-10-01 00:00:00

abstract：AIM:To use non-linear mixed effects modelling and simulation techniques to predict whether PF-04878691, a toll-like receptor 7 (TLR7) agonist, would produce sufficient antiviral efficacy while maintaining an acceptable side effect profile in a 'proof of concept' (POC) study in chronic hepatitis C (HCV) patients. METHO...

journal_title：British journal of clinical pharmacology

authors： Jones HM,Chan PL,van der Graaf PH,Webster R

更新日期：2012-01-01 00:00:00

abstract：:The effects of intravenous boluses of adenosine on respiration and heart rate were compared in young and elderly individuals. Respiratory stimulation and biphasic changes in heart rate were confirmed. The dose-response relationship for the effects of adenosine on respiration and heart-rate did not differ significantly...

journal_title：British journal of clinical pharmacology

authors： Watt AH,Bayer A,Routledge PA,Swift CG

更新日期：1989-02-01 00:00:00

abstract：:1. Relative rates of absorption of enteric and non-enteric preparations of prednisolone were measured in five renal transplant recipients. 2. The absorption of the enteric coated preparation is delayed and the peak plasma concentration is much lower than that attained using the same dose of the uncoated material. 3. T...

journal_title：British journal of clinical pharmacology

authors： Hulme B,James VH,Rault R

更新日期：1975-08-01 00:00:00

abstract：AIMS:To study reporting of hypoglycaemia in angiotensin receptor blocker (ARB) users, and to investigate the possibility of confounding. METHODS:The French pharmacovigilance database was examined for an association between hypoglycaemia and ARBs or other drugs using reports notified between 1996 and 2005. This associa...

journal_title：British journal of clinical pharmacology

authors： Grégoire F,Pariente A,Fourrier-Reglat A,Haramburu F,Bégaud B,Moore N

更新日期：2008-07-01 00:00:00

abstract：WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT:• The CYP3A4 inhibition by lipophilic statins may attenuate the effectiveness of clopidogrel. • No studies have measured drug exposure in a time-varying manner that detects discontinuation and restart of clopidogrel and statin therapy, allowing clinical quantification of the int...

journal_title：British journal of clinical pharmacology

authors： Schmidt M,Johansen MB,Maeng M,Kaltoft A,Jensen LO,Tilsted HH,Bøtker HE,Baron JA,Sørensen HT

更新日期：2012-07-01 00:00:00

abstract：AIMS:To compare the effects of nabumetone and meloxicam, two cyclo-oxygenase-2 (COX-2) preferential nonsteroidal anti-inflammatory drugs (NSAIDs), on platelet COX-1 activity and platelet function. METHODS:Twelve healthy volunteers (3 male, 9 female, median age 22 years) participated in an open, randomized, cross-over ...

journal_title：British journal of clinical pharmacology

authors： van Kraaij DJ,Hovestad-Witterland AH,de Metz M,Vollaard EJ

更新日期：2002-06-01 00:00:00

abstract：:Residual effects of brotizolam (0.25 mg) and flurazepam (30 mg) were studied in healthy young adults. Performance and subjective assessments were observed from 7 to 8 h after overnight ingestion, and effects were compared with that of placebo. Visuo-motor coordination, visuo-mental processing time, visuo-motor reactio...

journal_title：British journal of clinical pharmacology

authors： Krueger H,Müller-Limmroth W

更新日期：1983-01-01 00:00:00

abstract：:The importance of number of tablets for patient compliance was investigated in 160 patients with mild-moderate essential hypertension treated with a beta-adrenoceptor blocker and a thiazide diuretic. Mean BP at entry 146 +/- 16/92 +/- 8 mm Hg. All patients were given pindolol 10 mg and clopamide 5 mg in one combinatio...

journal_title：British journal of clinical pharmacology

authors： Asplund J,Danielson M,Ohman P

更新日期：1984-05-01 00:00:00

abstract：:Alpha 1-acid glycoprotein (AAG) concentrations and propranolol binding were investigated in the serum of elderly hospitalized patients with acute illness, and healthy elderly and young subjects. Significantly greater AAG concentrations and reduced unbound propranolol fraction were observed in the elderly with acute di...

journal_title：British journal of clinical pharmacology

authors： Paxton JW,Briant RH

更新日期：1984-11-01 00:00:00

abstract：AIMS:The role of CYP pharmacogenetics in the bioactivation of cyclophosphamide is still controversial. Recent clinical studies have suggested a role for either CYP2C19 or CYP2B6. The aim of this study was to clarify the role of these pharmacogenes. METHODS:We used a combined in vitro-in vivo approach to determine the ...

journal_title：British journal of clinical pharmacology

authors： Helsby NA,Hui CY,Goldthorpe MA,Coller JK,Soh MC,Gow PJ,De Zoysa JZ,Tingle MD

更新日期：2010-12-01 00:00:00

abstract：AIMS:There are no specific criteria for a step-down or withdrawal dose of omalizumab (OMA). Our purpose was to evaluate the viability of a protocol for OMAlizumab DOse REduction (the OMADORE study) in severe allergic asthma (SAA). METHODS:The study population included 35 SAA patients treated during a minimum period of...

journal_title：British journal of clinical pharmacology

authors： Domingo C,Pomares X,Navarro A,Amengual MJ,Montón C,Sogo A,Mirapeix RM

更新日期：2018-02-01 00:00:00

abstract：AIMS:The aim of this work is to understand the process of drug administration and identify points in the workflow that resulted in interventions by clinical information systems in order to improve patient safety. METHODS:To identify a generic way to structure the drug administration process we performed peer-group dis...

journal_title：British journal of clinical pharmacology

authors： Seidling HM,Lampert A,Lohmann K,Schiele JT,Send AJ,Witticke D,Haefeli WE

更新日期：2013-09-01 00:00:00

abstract：:Eight healthy normal subjects (19-23 years) received graded intravenous isoprenaline infusions PRE- and POST-atropine, 0.04 mg/kg i.v. The adequacy of atropinization was tested with bolus intravenous injections of phenylephrine. PRE-atropine, isoprenaline caused an increase in heart rate and systolic pressure, but a d...

journal_title：British journal of clinical pharmacology

authors： Arnold JM,McDevitt DG

更新日期：1984-09-01 00:00:00

abstract：:1 Measurements of the binding of 12-alpha-[3H]-digoxin to the membranes of intact erythrocytes, erythrocyte 86rubidium uptake and intraerythrocytic sodium concentrations have been made in the red cells of various groups of patients--those who have not received digoxin, those during the early phases of treatment, those...

journal_title：British journal of clinical pharmacology

authors： Ford AR,Aronson JK,Grahame-Smith DG,Carver JG

更新日期：1979-08-01 00:00:00

abstract：:The elimination of the cardioselective beta-adrenoceptor antagonist atenolol has been studied in 35 neonates by measuring drug concentration in cord blood and in blood obtained at 24 h by heel stab. Elimination rate was assessed by calculating the slopes of lines joining these two concentration points. The slopes had ...

journal_title：British journal of clinical pharmacology

authors： Rubin PC,Butters L,Reynolds B,Evans J,Sumner D,Low RA,Reid JL

更新日期：1983-12-01 00:00:00

abstract：:1. The pharmacokinetics of methylprednisolone (MP) were studied in five normal subjects following intravenous doses of 20, 40 and 80 mg methylprednisolone sodium succinate (MPSS) and an oral dose of 20 mg methylprednisolone as 4 x 5 mg tablets. Plasma concentrations of MP and MPSS were measured by both high performanc...

journal_title：British journal of clinical pharmacology

authors： Al-Habet SM,Rogers HJ

更新日期：1989-03-01 00:00:00

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

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

abstract：:Plasma concentrations of isoniazid and N-acetylisoniazid were measured at varying times after addition of both compounds to plasma (5 micrograms/ml) and storage at several different temperatures (-70 degrees C, -20 degrees C, 4 degrees C and 20 degrees C). The concentration of both compounds declined log-linearly with...

journal_title：British journal of clinical pharmacology

authors： Hutchings A,Monie RD,Spragg B,Routledge PA

更新日期：1983-02-01 00:00:00

abstract：:Activated platelets stimulate thrombus formation in response to rupture of an atherosclerotic plaque or endothelial cell erosion, promoting atherothrombotic disease. Multiple pathways contribute to platelet activation. Aspirin, an irreversible inhibitor of thromboxane A2 synthesis, in combination with clopidogrel, an ...

journal_title：British journal of clinical pharmacology

authors： Tello-Montoliu A,Tomasello SD,Ueno M,Angiolillo DJ

更新日期：2011-10-01 00:00:00

abstract：AIMS:To identify the enzymes involved in the metabolism of CMV423, a new anticytomegalovirus molecule, to evaluate its in vitro clearance and to investigate its potential involvement in drug/drug interactions that might occur in the clinic. METHODS:The enzymes involved in and the kinetics of CMV423 biotransformation w...

journal_title：British journal of clinical pharmacology

authors： Bournique B,Lambert N,Boukaiba R,Martinet M

更新日期：2001-07-01 00:00:00

abstract：:1. Twenty-two patients with moderately severe essential hypertension were treated for a period of 12 months with guanfacine (BS 100-141), a new centrally-acting antihypertensive agent. A twice daily schedule was followed and the dose range of guanfacine was 1-8 mg daily. 2. In twenty patients satisfactory blood pressu...

journal_title：British journal of clinical pharmacology

authors： Higuchi M,Overlack A,Stumpe KO

更新日期：1980-01-01 00:00:00

abstract：:1. Fifty-four depressive in-patients aged 18-45 yr, were treated at random, in double-blind conditions, with mianserin 60 mg daily or imipramine 150 mg daily in three divided doses for 4 weeks. Nitrazepam and diazepam were also allowed if necessary. 2. There was no significant difference in antidepressant efficacy bet...

journal_title：British journal of clinical pharmacology

authors： Pichot P,Dreyfus JF,Pull C

更新日期：1978-01-01 00:00:00

abstract：:The in vitro conversion of enalapril (MK421) to enalaprilic acid (MK422) in human autopsy tissues was examined. MK422 was measured by radioimmunoassay. Human cadaver liver was the only tissue in which significant conversion was demonstrated. The esterase activity was stable after post mortem. Autopsy liver tissues fro...

journal_title：British journal of clinical pharmacology

authors： Larmour I,Jackson B,Cubela R,Johnston CI

更新日期：1985-05-01 00:00:00

abstract：AIMS:The pharmacokinetics and dose proportionality of rizatriptan single oral doses from 2.5 to 15 mg administered as solutions to healthy volunteers were studied. METHODS:In a randomized, crossover study with four periods, twenty-four healthy volunteers (12 males and 12 females) took single oral doses of 2.5, 5, 10, ...

journal_title：British journal of clinical pharmacology

authors： Lee Y,Conroy JA,Stepanavage ME,Mendel CM,Somers G,McLoughlin DA,Olah TV,De Smet M,Keymeulen B,Rogers JD

更新日期：1999-04-01 00:00:00