摘要:

B antagonists eye drops are most effective for the treatment of chronic open angle glaucoma. By this way of administration they have a very good systemic bioavailability.Bronchial, and cardiovascular effects of three of these topicals: timolol, carteolol and metipranolol have been evaluated in three parallel groups of asthmatic patients. The three topics induce bronchoconstriction without significant difference between them, and lower heart rate (sometimes very intensely) whatever the B antagonist studied.From these data, it is recommended to practitioners to follow carefully the rules of administration of B blockers, even in eye drops.

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03293.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

To study the sensitivity of atrioventricular (AV) node to diltiazem in seven patients with paroxysmal supraventricular tachycardia (PSVT), we analyzed the plasma concentration‐response relationship of this Ca‐antagonist using AH interval as an index for assessing its Ca channel blocking effect on the AV node after an IV infusion (0.4 mg/kg). The postdose AH intervals were prolonged compared with the baseline, and their percentage changes correlated significantly (P<0.01) with log‐diltiazem concentrations in all patients. However, drug concentrations associated with a 20% prolongation of AH interval differed considerably among the patients (range; 65 to 260 ng/ml), indicating a large interindividual variability in the sensitivity of AV node to diltiazem. These results suggest that the interindividual difference in the responsiveness of AV node to diltiazem‐induced Ca channel blocking effect may be one of the possible explanations for the therapeutic failure of this Ca‐antagonist for terminating PSVT or preventing its recurrences in certain

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03294.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

Although it is well known that calcium channel blockers can influence contraction of vascular smooth muscle, there is less knowledge on its effect on excitation contraction coupling in the endocrine glands and more specifically on insulin and glucagon release. In this study, nifedipine was administered in doses of 40 to 80 mg/day to 14 patients with essential hypertension, and its hemodynamic effects were evaluated by non‐invasive methods, and its effect on glucose metabolism by an arginine infusion test. Nifedipine produced a significant reduction in systolic and diastolic blood pressure, both after the first dose (30/12 mm Hg) and after 8 weeks of administration (19/12 mm Hg). There were no significant changes in cardiac output (5.1 to 4.9 L/min), muscle (2.4 to 3.2 mL/sec/min) or cutaneous basal flow (9.8 to 8.6 mL/100 mL) as measured non‐invasively by echocardiogram and by plethysmography. Insulin and glucagon release were evaluated by the arginine infusion test. Nifedipine produced a tendency towards an increase in glucagon release and a reduction in insulin release although these changes did not reach statistical significance. In this group of patients, nifedipine produced a significant reduction in systolic and diastolic pressure, but no significant changes in insulin or glucagon plasma lev

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03295.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The pharmacokinetics of a single intravenous dose of propafenone were studied in subjects with normal renal function (n = 5), renal insufficiency (n = 5), and renal failure (n = 3). No difference in central volume of distribution, total systemic clearance or terminal half‐life existed. None of the pharmacokinetic parameters examined correlated to creatinine clearance. Within the confines of the small number of patients studied, there does not appear to be any effect of renal insufficiency or failure on single‐dose propafenone disposit

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03296.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The effect of desipramine on chronic ventricular ectopic depolarizations (VEDs) was studied in 10 patients with at least 30 VEDs per hour. A single‐blind, placebo‐controlled, dose‐ranging protocol was followed. Efficacy was defined as a decrease in VED frequency of at least 75%, based on three 24 hour ambulatory ECGs obtained on each dose. Among seven patients with analyzable data, one responded to 75 mg daily, and three others responded to 150 mg daily. Six of the seven patients demonstrated decreases in VED frequency with increases in desipramine serum concentration. Among five patients with episodes of nonsustained ventricular tachycardia, desipramine completely abolished the episodes in two, and reduced the frequency of episodes by at least 90% in two others. Adverse reactions were common, and necessitated drug discontinuation or dose reduction in five patients. Desipramine has an antiarrhythmic effect in patients with chronic ventricular ectopy, but its clinical utility is limited by adverse ef

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03297.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The purpose of this study was to assess the effect of a daily low dose of the angiotensin‐converting enzyme (ACE) inhibitors, captopril or enalapril, in mild essential hypertension. Nine men with seated diastolic blood pressure between 95 and 104 mm Hg on placebo participated in the study. After one month of placebo, captopril 25 mg was administered; blood pressure, heart rate, ACE activity and plasma renin activity were measured hourly for 4 hours. Each patient then received captopril 50 mg once daily for 8 weeks and similar measurements were made 24 hours post‐dose every 2 weeks. After another month of placebo, the identical protocol was repeated after enalapril 5 mg. Although blood pressure and ACE activity decreased significantly (P<0.05) within 2–4 hours of the acute doses of each inhibitor, neither captopril or enalapril produced significant reductions 24 hours after the small daily dose. Thus, neither ACE inhibitor alone was adequate to control blood pressure in mild hypertension when given once daily during 8 weeks of trea

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03298.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The effects of doxazosin, a long‐acting alpha‐1 adrenoreceptor blocking drug, were observed upon blood pressure and serum lipoproteins. Thirty patients with supine diastolic blood pressure between 90 and 114 mm Hg during single‐blind placebo therapy were randomized to double‐blind treatment with either doxazosin or further placebo in a parallel‐design protocol. Starting at one mg, dosage was doubled every 2 weeks during a 10‐week treatment period to a maximum dose of 16 mg once daily. Blood was sampled in the fasting state before and during double‐blind therapy for measurement of total cholesterol and triglycerides, cholesterol in the lipoprotein fractions, and apolipoproteins A and B. At the end of 10 weeks of titration, systolic and diastolic blood pressure were each reduced by 14 mm Hg in the standing position when measured 24 hours following the previous dose. Supine pressure was lowered by 6 mm Hg systolic and by 5 mm Hg diastolic at the same time point. Measured hourly for 12 hours following the ingestion of doxazosin, blood pressure was lowered maximally at 4–5 hours when an additional decline of 14/6 mm Hg (systolic/diastolic) was observed in the standing position and 13/6 in the supine posture. Postural dizziness, the most frequent symptomatic complaint, was reported in 4 patients during doxazosin treatment. After brief interruption of treatment in one and dosage adjustment in another, titration was continued in all four and no patient was withdrawn because of side effects. Concerning lipoproteins, the ratio of total cholesterol to HDL cholesterol and of LDL to HDL cholesterol both improved during treatment with doxazosin. Although these changes did not differ from those in the placebo group, the findings indicate that both blood pressure and lipoprotein concentrations respond favorably during treatment with doxazosin. This favorable combination of effects on CHD risk factors is matched by few other classes of antihypertensive drugs. In this way doxazosin offers a distinct advantage as first‐line therap

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03299.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The disposition of a single 25 mg oral dose of guanadrel was evaluated in 22 subjects with various degrees of renal function. The terminal elimination half‐life was significantly prolonged in subjects with a creatinine clearance (ClCr)80 mL/min/1.73 m.2Apparent total body clearance (Clp/F) was also progressively lower in the patients with decreased renal function and the decline was significantly correlated with ClCr(Clp/F = 0.0294 + 0.0236 ClCr, r = 0.74, P = 0.002). Renal clearance and apparent nonrenal clearance also declined as creatinine clearance decreased and both were significantly correlated with the observed ClCr. Apparent volume of distribution averaged 11.5 ± 8.9 L/kg and did not differ in patients with decreased renal function compared to those with normal renal function. Thus, the disposition of guanadrel is significantly altered in the presence of renal insufficiency and dosage adjustments may be necessary, especially in patients with ClCr<50 ml

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03300.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

Sixteen of 22 elderly male patients (aged 60–74 years) who had previously taken only hydrochlorothiazide 50 mg completed a study evaluating the safety, efficacy, and tolerability of 12–20 weeks of transdermal clonidine (Catapres TTSR) as monotherapy for mild hypertension. Thirteen of the sixteen patients (81%) responded to transdermal clonidine which was begun after 28 days of placebo. Five patients discontinued transdermal clonidine therapy because of intolerable skin irritation, and one because of daytime fatigue. Clonidine caused none of the metabolic effects we observed with hydrochlorothiazide: no change in serum potassium, uric acid, cholesterol, or triglyceride. Eleven of the 22 patients (50%) who began the study experienced a skin reaction under the transdermal clonidine patch. The incidence of dry mouth and fatigue in patients using transdermal clonidine was dose‐related and similar to reports of dry mouth and fatigue in patients taking oral clonidine tablets. Rebound hypertension occurred in one patient upon withdrawal of transdermal clonidine. There was no effect of transdermal clonidine or hydrochlorothiazide on cognitive function or emotional state tested with three questionnaires. Overall, transdermal clonidine, in various doses, was as effective as hydrochlorothiazide in elderly male hypertensive patients. The effectiveness of both was inversely proportional to the level of untreated blood pressure. The high incidence of skin reactions limited prolonged use of transdermal clonidine in our pat

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03301.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY

摘要:

The peritoneal clearance of gentamicin was studied in 11 chronic uremic patients who undergoing intermittent peritoneal dialysis. Gentamicin was significantly removed by peritoneal dialysis with a clearance value of 9.75 ± 3.78 ml/min. The serum half life was 14.08 ± 3.57 hr, a value significantly less than that of non dialysed end stage renal disease patients. The mean apparent volume of distribution of the drug in these patient was about 27% of body weight. The derived value for gentamicin peritoneal clearance and volume of distribution can be used to calculate maintenance dose during intermittent peritoneal dialysis. In order to achieve the peak level of 8 ug/ml, supplementary dose compensated for the loss during peritoneal dialysis is approximately 40% of loading dose 0.8 mg/kg every 12 hour

ISSN:0091-2700    

DOI:10.1002/j.1552-4604.1989.tb03302.x

出版商:Blackwell Publishing Ltd    

年代:1989

数据来源: WILEY