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：:Serum and milk concentrations of aztreonam were studied in 12 lactating, healthy subjects over the 8 h period after the administration of a single intramuscular or intravenous 1 g dose. Milk concentrations of aztreonam were found to be much lower than serum concentrations at all time points after both routes of inject...

journal_title：British journal of clinical pharmacology

authors： Fleiss PM,Richwald GA,Gordon J,Stern M,Frantz M,Devlin RG

更新日期：1985-04-01 00:00:00

abstract：:To examine the importance of acute frusemide-induced renin release in the production of the acute peripheral venous and arterial responses to frusemide in man, the effects of two drugs, previously described as inhibitors of acute frusemide-induced renin release, propranolol and digoxin, were examined. Propranolol abol...

journal_title：British journal of clinical pharmacology

authors： Johnston GD,O'Connor PC,Nicholls DP,Leahey WJ,Finch MB

更新日期：1985-04-01 00:00:00

abstract：:The effects of separate 7 day pretreatments with sulphinpyrazone (800 mg daily) and cimetidine (1 g daily) on the disposition of (+/-)-verapamil have been examined in eight healthy volunteers (four male, four female). Each subject received single oral (80 mg) and intravenous (0.15 mg/kg) doses of verapamil on differen...

journal_title：British journal of clinical pharmacology

authors： Wing LM,Miners JO,Lillywhite KJ

更新日期：1985-03-01 00:00:00

abstract：:The effects of ranitidine on the pharmacokinetics of metoprolol were examined in two studies. In the first study, pharmacokinetics of single doses of metoprolol were examined in six subjects before, during and after ranitidine administration for 1 week. Peak concentrations of metoprolol were increased on ranitidine bu...

journal_title：British journal of clinical pharmacology

authors： Kelly JG,Salem SA,Kinney CD,Shanks RG,McDevitt DG

更新日期：1985-02-01 00:00:00

abstract：:In a double-blind, placebo-controlled, randomised, cross-over study of six healthy male subjects, the effect of nicardipine (5 mg h-1 for 3 h) on basal and stimulated pituitary hormone release was examined. Statistically significant differences between nicardipine and placebo were seen occasionally for follicle-stimul...

journal_title：British journal of clinical pharmacology

authors： Isles TE,Baty J,Dow RJ

更新日期：1985-01-01 00:00:00

abstract：:Three calcium antagonists, diltiazem, flunarizine and verapamil stimulated human sperm motility in vitro. Among them, diltiazem induced the largest amplitude of motility increase. The concentration-response curve of diltiazem was similar in shape to those of calcium chelators. EGTA, a calcium chelator, potentiated the...

journal_title：British journal of clinical pharmacology

authors： Hong CY,Chiang BN,Ku J,Wei YH,Fong JC

更新日期：1985-01-01 00:00:00

abstract：:The effects of intravenous nicardipine (2.5 mg) on the left ventricular (LV) inotropic state, LV metabolism, and coronary haemodynamics were analysed in 22 patients with angina pectoris. Measurements were made at fixed heart rate (atrial pacing), under basal state, and during a cold pressor test. After nicardipine, co...

journal_title：British journal of clinical pharmacology

authors： Rousseau MF,Vincent MF,Cheron P,van den Berghe G,Charlier AA,Pouleur H

更新日期：1985-01-01 00:00:00

abstract：:In a dog model of partial myocardial ischaemia, superimposed ST segment elevations in epicardial ECGs were inhibited by nicardipine over a cumulative i.v. dose range of 1-20 micrograms kg-1. Over the cumulative i.v. dose range of 0.5-166.5 micrograms kg-1, nicardipine had little overall effect on gross cardiac conduct...

journal_title：British journal of clinical pharmacology

authors： Alps BJ,Calder C,Wilson A

更新日期：1985-01-01 00:00:00

abstract：:The dose-response effects of oral nicardipine on the systemic blood pressure were examined in 54 patients with uncomplicated essential hypertension (DBP greater than or equal to 100 mm Hg). The study was designed in four sequential stages. A 2 week single-blind placebo run-in period was followed by dose titration with...

journal_title：British journal of clinical pharmacology

authors： Taylor SH,Frais MA,Lee P,Verma SP,Jackson N,Silke B

更新日期：1985-01-01 00:00:00

abstract：:A new osmotic drug delivery system (Oros) has been evaluated in multiple-dose studies in young healthy volunteers as a sustained-release vehicle for once-daily administration of oxprenolol. Two Oros systems were examined in two separate studies, one containing 170 mg oxprenolol succinate with an initial zero-order rel...

journal_title：British journal of clinical pharmacology

authors： Woods KL,Jack DB,Kendall MJ,Halsey A,O'Donnell ML,Warrington SJ,John VA

更新日期：1985-01-01 00:00:00

abstract：:The influence of food on the release, absorption and metabolism of metoprolol has been studied after single administration of a 19/190 Oros system to eight healthy volunteers on four occasions, once after an overnight fast, and just before each of three daily meals (breakfast, lunch and dinner). The plasma concentrati...

journal_title：British journal of clinical pharmacology

authors： Lecaillon JB,Massias P,Schoeller JP,Abadie F

更新日期：1985-01-01 00:00:00

abstract：:The effect of fatty degeneration of liver parenchyma on drug metabolism was investigated in 21 obese non-insulin-dependent diabetic subjects by measuring plasma antipyrine kinetics, hepatic cytochrome P-450, liver size and the extent of fatty infiltration. The hepatic drug metabolising capacity, as measured by total a...

journal_title：British journal of clinical pharmacology

authors： Pirttiaho HI,Salmela PI,Sotaniemi EA,Pelkonen RO,Pitkänen U,Luoma PV

更新日期：1984-12-01 00:00:00

abstract：:The effect of liver cirrhosis on plasma clearance and metabolite profile of i.v. administered antipyrine was studied in 23 patients with alcoholic liver cirrhosis (age 37-70 years) and 17 healthy subjects (age 28-55 years). Liver volume was also measured and was found to be larger in patients than in controls, mean va...

journal_title：British journal of clinical pharmacology

authors： Teunissen MW,Spoelstra P,Koch CW,Weeda B,van Duyn W,Janssens AR,Breimer DD

更新日期：1984-11-01 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：:To study the cardioselectivity of xamoterol, eight asthmatic patients took part in a randomised, double-blind, cross-over study, in which xamoterol or saline were infused, followed by four increasing doses of terbutaline i.v. Circulatory studies showed a significant increase of systolic blood pressure after xamoterol ...

journal_title：British journal of clinical pharmacology

authors： Löfdahl CG,Svedmyr N

更新日期：1984-10-01 00:00:00

abstract：:The binding of carbamazepine and carbamazepine 10,11-epoxide to serum, albumin and alpha 1-acid glycoprotein (AAG) was determined and compared at drug concentrations ranging from 0.5 to 400 mg/l using equilibrium dialysis and liquid chromatography. The total binding of carbamazepine in serum was determined primarily b...

journal_title：British journal of clinical pharmacology

authors： MacKichan JJ,Zola EM

更新日期：1984-10-01 00:00:00

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

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

更新日期：1984-10-01 00:00:00

abstract：:Eight psoriatic patients were treated with etretinate (50 mg daily) for 6 weeks. Skin chamber exudates from involved and uninvolved skin were assayed for arachidonic acid, 12-HETE, PGE2 and for neutrophil chemokinetic activity co-chromatographing with leukotriene B4, before and at weekly intervals during therapy. Pre-...

journal_title：British journal of clinical pharmacology

authors： Wong E,Barr RM,Brain SD,Greaves MW,Olins LA,Mallet AI

更新日期：1984-10-01 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：:The influence of cimetidine pretreatment on the pharmacokinetics of 5-fluorouracil (5FU) has been studied in 15 ambulant patients with carcinoma. Neither pretreatment with a single dose of cimetidine (400 mg) nor with daily treatment at 1000 mg for 1 week altered 5FU pharmacokinetics. Pretreatment with cimetidine for ...

journal_title：British journal of clinical pharmacology

authors： Harvey VJ,Slevin ML,Dilloway MR,Clark PI,Johnston A,Lant AF

更新日期：1984-09-01 00:00:00

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

authors： Ward JW

更新日期：1984-08-01 00:00:00

abstract：:Both the acute blood pressure lowering and renal effects of the calcium antagonist nicardipine and those after 1 week's treatment were investigated in 10 normotensive volunteers and in 10 patients with mild to moderate essential hypertension. After 1 week of placebo, nicardipine was administered orally for 1 week (20 ...

journal_title：British journal of clinical pharmacology

authors： van Schaik BA,van Nistelrooy AE,Geyskes GG

更新日期：1984-07-01 00:00:00

abstract：:In order to elucidate the mechanisms by which beta-adrenoceptor blockade leads to a reduction in portal pressure, we have measured portal pressure, heart rate and cardiac index in 17 patients with cirrhosis and portal hypertension following the oral administration of the selective beta 2-adrenoceptor blocking agent, I...

journal_title：British journal of clinical pharmacology

authors： Bihari D,Westaby D,Gimson A,Crossley I,Harry J,Williams R

更新日期：1984-06-01 00:00:00

abstract：:The effects of two single oral doses of ibopamine (150 and 600 mg) on heart rate, blood pressure, urine flow, sodium, potassium and creatinine excretion were studied in normal volunteers. No significant change was observed in urine flow, sodium, potassium or creatinine excretion at either dose. No significant change w...

journal_title：British journal of clinical pharmacology

authors： Harvey JN,Worth DP,Brown J,Lee MR

更新日期：1984-06-01 00:00:00

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

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

更新日期：1984-06-01 00:00:00

abstract：:The ability to recall details of current and prior drug therapy was evaluated in two studies employing a total of 94 patients with inflammatory polyarthritis. Ten per cent of patients were unable to completely recall the names of their current anti-inflammatory drugs and eighty-three per cent of patients to completely...

journal_title：British journal of clinical pharmacology

authors： Bellamy N,Grace E,Hanna B,Grant E,Tugwell P,Buchanan WW

更新日期：1984-06-01 00:00:00

abstract：:Medroxalol, a new drug which has been reported to possess both alpha- and beta-adrenoceptor antagonist properties, was compared with labetalol in single dose studies in normotensive males. Oral doses of 400 mg of each drug significantly reduced blood pressure, both supine and erect, without significant changes in hear...

journal_title：British journal of clinical pharmacology

authors： Elliott HL,McLean K,Meredith PA,Sumner DJ,Reid JL

更新日期：1984-05-01 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：:Theophylline clearance was studied in normal healthy volunteers before and after chronic oral dosing. Oral theophylline clearance showed a significant decrease (P less than 0.001) from 59.3 +/- 6.48 ml/min (mean +/- s.e. mean, n = 10) to 48.0 +/- 6.4 ml/min. Steady-state intravenous clearance decreased by 26 +/- 2% fr...

journal_title：British journal of clinical pharmacology

authors： Efthimiou H,Morgan DJ,Ioannides-Demos L,Raymond K,McLean AJ

更新日期：1984-05-01 00:00:00

abstract：:The effect of urinary pH on flecainide excretion has been evaluated in six healthy subjects after a single oral dose of 300 mg flecainide administered as the acetate salt. The cumulative urinary excretion of unchanged flecainide under acidic conditions (134.0 +/- 16.1 mg; mean +/- s.e. mean) was significantly higher t...

journal_title：British journal of clinical pharmacology

authors： Muhiddin KA,Johnston A,Turner P

更新日期：1984-04-01 00:00:00

abstract：:A method is described for the simultaneous determination of the carboxylic acid and N-acetyl-derivatives of primaquine, in plasma and urine. After oral administration of 45 mg primaquine, to five healthy volunteers, absorption was rapid, with peak primaquine levels of 153.3 +/- 23.5 ng/ml at 3 +/- 1 h, followed by an ...

journal_title：British journal of clinical pharmacology

authors： Mihaly GW,Ward SA,Edwards G,Orme ML,Breckenridge AM

更新日期：1984-04-01 00:00:00

abstract：:Propranolol induced changes in blood plasma chemistry were followed in thirty hypertensive patients (WHO I-II) who were seen each week during 14-15 weeks. The initial 4 weeks were a drug free period and the next 2 weeks were a drug adjustment period. After that the patients were on an unchanged propranolol dose for 8 ...

journal_title：British journal of clinical pharmacology

authors： Andreasen F,Jakobsen P,Kornerup HJ,Pedersen EB,Pedersen OL,Weeke J

更新日期：1984-03-01 00:00:00

abstract：:We have measured the psychological effects of acebutolol and atenolol in sixteen patients with essential hypertension. The drugs were administered in a randomized, placebo-controlled, double-blind manner, in single daily doses of 100 mg atenolol, 400 mg acebutolol or placebo for periods of 6 weeks, each drug period be...

journal_title：British journal of clinical pharmacology

authors： Lewis MJ,Jones DM,Dart AM,Henderson AH

更新日期：1984-03-01 00:00:00

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

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

abstract：:A possible route of metabolism of beta-adrenoceptor stimulating drugs used in obstetrics consists of conjugation by the enzyme phenol sulphotransferase. The substrate specificities of the platelet and the placental enzymes towards these drugs were tested. The specific activities of the beta-adrenoceptor agonists were ...

journal_title：British journal of clinical pharmacology

authors： Sodha RJ,Schneider H

更新日期：1984-01-01 00:00:00

abstract：:The degrees of interactions between the H2-receptor antagonists, cimetidine and ranitidine, and several beta-adrenoceptor blockers were investigated in healthy volunteers following 7 days of oral monotherapy with penbutolol, propranolol, metoprolol, pindolol and atenolol, and after co-administration with each of the H...

journal_title：British journal of clinical pharmacology

authors： Mutschler E,Spahn H,Kirch W

更新日期：1984-01-01 00:00:00

abstract：:Analysis of human horizontal saccadic eye movements can provide measurements of central nervous system depression and stimulation. Effects on saccadic eye movements have been observed in normal volunteers with barbiturates, benzodiazepines, opiates and related compounds, carbamazepine, amphetamine and ethanol. A suite...

journal_title：British journal of clinical pharmacology

authors： Griffiths AN,Marshall RW,Richens A

更新日期：1984-01-01 00:00:00

abstract：:The effect of acute migraine attack and rectally given metoclopramide on the absorption of orally given tolfenamic acid (300 mg) was investigated in seven female patients in a crossover study consisting of four phases, two without migraine and two during migraine. Metoclopramide hydrochloride (20 mg) or placebo was gi...

journal_title：British journal of clinical pharmacology

authors： Tokola RA,Neuvonen PJ

更新日期：1984-01-01 00:00:00

abstract：:Both empirical epidemiological data on the causes of traffic accidents and conceptual models of skilled human performance stress the central role of perception and cognition. This paper examines the effects of drugs on two major components of cognitive perceptual performance, namely, concentrated attention or vigilanc...

journal_title：British journal of clinical pharmacology

authors： Moskowitz H

更新日期：1984-01-01 00:00:00