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Journal of Clinical Hypertension... Jan 2010Office, home, and ambulatory blood pressure (BP) demonstrate variable associations with outcomes. The authors sought to compare office BP (OBP), home BP (HBP), and... (Randomized Controlled Trial)
Randomized Controlled Trial
Office, home, and ambulatory blood pressure (BP) demonstrate variable associations with outcomes. The authors sought to compare office BP (OBP), home BP (HBP), and ambulatory BP (ABP) for measuring responses to hydrochlorothiazide (HCTZ), atenolol, and their combination. After completing washout, eligible patients were randomized to atenolol 50 mg or HCTZ 12.5 mg daily. Doses were doubled after 3 weeks and the alternate drug was added after 6 weeks if BP was >120/70 mm Hg (chosen to allow maximum opportunity to assess genetic associations with dual BP therapy in the parent study). OBP (in triplicate), HBP (twice daily for 5 days), and 24-hour ABP were measured at baseline, after monotherapy, and after combination therapy. BP responses were compared between OBP, HBP, and ABP for each monotherapy and combination therapy. In 418 patients, OBP overestimated BP response compared with HBP, with an average 4.6 mm Hg greater reduction in systolic BP (P<.0001) and 2.1 mm Hg greater reduction in diastolic BP (P<.0001) across all therapies. Results were similar for atenolol and HCTZ monotherapy. ABP response was more highly correlated with HBP response (r=0.58) than with OBP response (r=0.47; P=.04). In the context of a randomized clinical trial, the authors have identified significant differences in HBP, OBP, and ABP methods of measuring BP response to atenolol and HCTZ monotherapy.
Topics: Adolescent; Adult; Aged; Antihypertensive Agents; Atenolol; Blood Pressure; Blood Pressure Monitoring, Ambulatory; Drug Therapy, Combination; Female; Humans; Hydrochlorothiazide; Male; Middle Aged; Treatment Outcome
PubMed: 20047624
DOI: 10.1111/j.1751-7176.2009.00185.x -
British Journal of Clinical Pharmacology Mar 1985The pharmacokinetics and pharmacodynamics of atenolol and timolol were studied in six extensive and four poor metabolisers of debrisoquine. There was a significant... (Comparative Study)
Comparative Study
The pharmacokinetics and pharmacodynamics of atenolol and timolol were studied in six extensive and four poor metabolisers of debrisoquine. There was a significant correlation between the debrisoquine to 4-hydroxydebrisoquine ratio and the area under the plasma concentration time curve (AUC) for timolol (rs = 0.75, P less than 0.02). The mean of the AUC values for timolol was significantly greater in the poor metabolisers than in the extensive metabolisers (P less than 0.05). There was a significant correlation between the debrisoquine to 4-hydroxydebrisoquine ratio and beta-adrenoceptor blockade 24 h after dosing with timolol (rs = 0.66, P less than 0.05). The mean degree of beta-adrenoceptor blockade was significantly greater in the poor metabolisers than in the extensive metabolisers 24 h after dosing with timolol (P less than 0.01). There was no relation between the debrisoquine to 4-hydroxydebrisoquine ratio and the pharmacokinetics or pharmacodynamics of atenolol.
Topics: Adrenergic beta-Antagonists; Adult; Atenolol; Chromatography, High Pressure Liquid; Debrisoquin; Heart Rate; Humans; Kinetics; Male; Oxidation-Reduction; Phenotype; Physical Exertion; Spectrophotometry, Ultraviolet; Timolol
PubMed: 2859048
DOI: 10.1111/j.1365-2125.1985.tb02651.x -
The American Journal of Cardiology Oct 1999Vasovagal syncope is a common disorder of autonomic cardiovascular regulation. Many pharmacologic agents have been proposed as effective in the management of this... (Review)
Review
Vasovagal syncope is a common disorder of autonomic cardiovascular regulation. Many pharmacologic agents have been proposed as effective in the management of this condition based on nonrandomized clinical trials. Notably, only 3 agents--atenolol, midodrine, and paroxetine--have demonstrated efficacy in the treatment of vasovagal syncope in at least 1 prospective, randomized, placebo-controlled clinical trial. Other therapies commonly used in treating syncope include increased salt and fluid intake and fludrocortisone. In this review, we provide a summary of currently available data that support or question the use of various pharmacologic agents for treatment of vasovagal syncope.
Topics: Atenolol; Fludrocortisone; Humans; Midodrine; Paroxetine; Randomized Controlled Trials as Topic; Syncope, Vasovagal; Treatment Outcome
PubMed: 10568557
DOI: 10.1016/s0002-9149(99)00626-8 -
British Journal of Clinical Pharmacology Dec 19951. The effects of 4 week treatment with rilmenidine or atenolol on tests of mental stress, dynamic exercise, autonomic function and psychometric tests were evaluated in... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
1. The effects of 4 week treatment with rilmenidine or atenolol on tests of mental stress, dynamic exercise, autonomic function and psychometric tests were evaluated in a randomized, double-blind, placebo-controlled, cross-over study. 2. After a 4 week placebo run-in, 12 patients with essential hypertension (blood pressure [BP] 160/95 +/- 15/7 mmHg) received rilmenidine 1-2 mg day-1, and atenolol 50-100 mg day-1, each for 4 weeks, with a 4 week placebo wash-out between drug treatments. 3. Both agents produced a comparable reduction in supine and erect BP. During the mental arithmetic test, BP and heart rate (HR) responses were similar for rilmenidine and atenolol. 4. During bicycle exercise, the increase in HR was significantly greater after rilmenidine (+50 vs 41 beats min-1, P = 0.04). During recovery, the areas under the curve for diastolic BP (46,450 vs 51,400 mmHg s, P = 0.02) and HR (49,445 vs 63,597 beats min-1 s, P = 0.001) were significantly less with atenolol than rilmenidine. 5. Neither rilmenidine nor atenolol affected mental performance as judged by arithmetic and psychomotor tests. Physiological responses to autonomic function tests (deep breathing, facial immersion, isometric handgrip and cold pressor) were preserved with both drugs. The standing to lying ratio was higher on atenolol (P = 0.01) and Valsalva ratio was higher on rilmenidine (P = 0.03). 6. In conclusion, rilmenidine and atenolol exerted comparable antihypertensive effects both at rest and during mental and dynamic stress. Atenolol attenuated HR responses to dynamic exercise and the Valsalva manoeuvre; rilmenidine did not interfere with the physiological responses of BP and HR during autonomic function tests.
Topics: Adrenergic beta-Antagonists; Adult; Antihypertensive Agents; Atenolol; Blood Pressure; Cross-Over Studies; Double-Blind Method; Exercise; Heart Rate; Humans; Hypertension; Male; Middle Aged; Oxazoles; Rilmenidine; Stress, Psychological; Supine Position
PubMed: 8703663
DOI: 10.1111/j.1365-2125.1995.tb05801.x -
Vascular Pharmacology Oct 2022The mechanisms underlying the success of propranolol in the treatment of infantile hemangioma (IH) remain elusive and do not fully explain the rapid regression of...
UNLABELLED
The mechanisms underlying the success of propranolol in the treatment of infantile hemangioma (IH) remain elusive and do not fully explain the rapid regression of hemangiomatous lesions following drug administration. As autophagy is critically implicated in vascular homeostasis, we determined whether β-blockers trigger the autophagic flux on infantile hemangioma-derived endothelial cells (Hem-ECs) in vitro.
MATERIAL AND METHODS
Fresh tissue specimens, surgically removed for therapeutic purpose to seven children affected by proliferative IH, were subjected to enzymatic digestion. Cells were sorted with anti-human CD31 immunolabeled magnetic microbeads. Following phenotypic characterization, expanded Hem-ECs, at P2 to P6, were exposed to different concentrations (50 μM to 150 μM) of propranolol, atenolol or metoprolol alone and in combination with the autophagy inhibitor Bafilomycin A1. Rapamycin, a potent inducer of autophagy, was also used as control. Autophagy was assessed by Lysotracker Red staining, western blot analysis of LC3BII/LC3BI and p62, and morphologically by transmission electron microscopy.
RESULTS
Hem-ECs treated with either propranolol, atenolol or metoprolol displayed positive LysoTracker Red staining. Increased LC3BII/LC3BI ratio, as well as p62 modulation, were documented in β-blockers treated Hem-ECs. Abundant autophagic vacuoles and multilamellar bodies characterized the cytoplasmic ultrastructural features of autophagy in cultured Hem-ECs exposed in vitro to β-blocking agents. Importantly, similar biochemical and morphologic evidence of autophagy were observed following rapamycin while Bafilomycin A1 significantly prevented the autophagic flux promoted by β-blockers in Hem-ECs.
CONCLUSION
Our data suggest that autophagy may be ascribed among the mechanisms of action of β-blockers suggesting new mechanistic insights on the potential therapeutic application of this class of drugs in pathologic conditions involving uncontrolled angiogenesis.
Topics: Adrenergic beta-Antagonists; Amines; Atenolol; Autophagy; Cell Proliferation; Child; Endothelial Cells; Hemangioma; Humans; Macrolides; Metoprolol; Propranolol; Sirolimus
PubMed: 36103993
DOI: 10.1016/j.vph.2022.107110 -
Clinical Cardiology Dec 1994The effects of monotherapy with atenolol or diltiazem-SR on blood pressure, 24-h blood pressure (BP) load, and exercise capacity were tested in patients with mild to... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
The effects of monotherapy with atenolol or diltiazem-SR on blood pressure, 24-h blood pressure (BP) load, and exercise capacity were tested in patients with mild to moderate (stages I and II) essential hypertension. After 3-week single-blind placebo therapy, patients with sitting diastolic blood pressure (SDBP) of 94-114 mmHg were randomized to atenolol 50 mg/day (62 patients) or diltiazem-SR 90 mg b.i.d. (60 patients) in a double-blind parallel study. Depending on SDBP response, the dose was increased to 100 mg/day for atenolol and 180 mg b.i.d. for diltiazem-SR. Twenty-four-hour ambulatory blood pressure measurements and exercise tolerance test by the Bruce protocol were done at the end of placebo and active treatment. Compared with placebo, both atenolol and diltiazem-SR significantly decreased heart rate (HR), sitting systolic blood pressure (SSBP), SDBP, ambulatory BP, BP load for waking and sleeping hours, area under the BP curve, rate-pressure product (p < 0.001), and exercise time (NS). Atenolol exerted a greater effect on ambulatory BP, HR, rate-pressure product, waking diastolic BP load, and area under the 24-h BP curve. The drugs were well tolerated and caused no serious side effects necessitating discontinuation of treatment. These findings indicate that (1) monotherapy for hypertension with atenolol or diltiazem-SR is effective and well tolerated, (2) it decreases the 24-h BP load, (3) it does not interfere with exercise capacity.
Topics: Adult; Aged; Atenolol; Blood Pressure; Diltiazem; Dose-Response Relationship, Drug; Double-Blind Method; Exercise Tolerance; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged
PubMed: 7867240
DOI: 10.1002/clc.4960171209 -
Polimery W Medycynie 2017The use of mucoadhesive natural polymers in designing mucoadhesive patch systems has received much attention.
BACKGROUND
The use of mucoadhesive natural polymers in designing mucoadhesive patch systems has received much attention.
OBJECTIVES
The study involved the development and evaluation of buccal patches of atenolol using fenugreek (Trigonella foenum-graecum L.) seed mucilage with hydroxylpropyl methyl cellulose (HPMC K4M) and a backing membrane (ethyl cellulose 5% w/v).
MATERIAL AND METHODS
These atenolol-releasing buccal patches were prepared using a solvent casting technique. The buccal patches prepared were evaluated for average weight, thickness, drug content, folding endurance and moisture content. Ex vivo mucoadhesive strength, force of adhesion and bonding strength were determined using porcine buccal mucosa. The mucosal permeation of atenolol through the porcine buccal mucosa was carried out using a Franz diffusion cell in phosphate buffer saline, pH 6.8. These buccal patches were also characterized by SEM and FTIR spectroscopy.
RESULTS
The average weight, thickness, drug content, folding endurance and moisture content of these atenolol-releasing buccal patches were found satisfactory for all the patches. Amongst all, the F-4 buccal patch showed maximum mucoadhesive strength (31.12 ±1.86 g), force of adhesion (30.53 × 10-2 N) and bond strength (1748.89 N/m2). Ex vivo atenolol permeation from the buccal patches showed drug permeation across the excised porcine buccal mucosa over 12 h. The F-4 buccal patch showed maximum permeation flux (29.12 μg/cm2/h).
CONCLUSIONS
The developed atenolol-releasing buccal patches can be beneficial over the conventional drug delivery systems to decrease the dosing frequency and enhance patient compliance.
Topics: Animals; Atenolol; Drug Delivery Systems; Goats; Mouth Mucosa; Permeability; Plant Extracts; Polysaccharides; Swine; Trigonella
PubMed: 29160624
DOI: 10.17219/pim/70498 -
Journal of Veterinary Internal Medicine 2011Ivabradine is a novel negative chronotropic drug used for treatment of ischemic heart disease in people. Little is known about its effects and safety in cats. (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Ivabradine is a novel negative chronotropic drug used for treatment of ischemic heart disease in people. Little is known about its effects and safety in cats.
HYPOTHESIS/OBJECTIVES
Ivabradine is not inferior to atenolol with regard to clinical tolerance, heart rate (HR) reduction, and effects on cardiac function in healthy, lightly sedated cats.
ANIMALS
Ten healthy laboratory cats.
METHODS
Physical examination, systolic blood pressure measurement, and transthoracic echocardiography were performed in all cats at baseline and after oral administration (4 weeks each) of ivabradine (0.3 mg/kg q12h) and atenolol (6.25 mg/cat q12h; 1.0-1.7 mg/kg) in a prospective, double-blind, randomized, active-control, fully crossed study. A priori noninferiority margins for the effects of ivabradine compared with atenolol were set at 50% (f = 0.5) based on predicted clinical relevance, observer measurement variability, and in agreement with FDA guidelines. Variables were compared by use of 2-way repeated measures ANOVA.
RESULTS
Ivabradine was clinically well tolerated with no adverse events observed. HR (ivabradine, P < .001; atenolol, P < .001; ivabradine versus atenolol, P = .721) and rate-pressure product (RPP) (ivabradine, P < .001; atenolol, P = .001; ivabradine versus atenolol, P = .847) were not different between treatments. At the dosages used, ivabradine demonstrated more favorable effects than atenolol on echocardiographic indices of left ventricular (LV) systolic and diastolic function and left atrial performance.
CONCLUSIONS AND CLINICAL IMPORTANCE
Ivabradine is not inferior to atenolol with regard to effects on HR, RPP, LV function, left atrial performance, and clinical tolerance. Clinical studies in cats with hypertrophic cardiomyopathy are needed to validate these findings.
Topics: Animals; Anti-Arrhythmia Agents; Atenolol; Benzazepines; Blood Pressure; Cardiotonic Agents; Cats; Cross-Over Studies; Double-Blind Method; Female; Heart Rate; Ivabradine; Ventricular Function, Left
PubMed: 21418320
DOI: 10.1111/j.1939-1676.2011.0705.x -
British Journal of Clinical Pharmacology Sep 19911. The interactions between the dihydropyridine calcium antagonist nisoldipine and two beta-adrenoceptor blocker drugs (atenolol and propranolol) were investigated in... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
1. The interactions between the dihydropyridine calcium antagonist nisoldipine and two beta-adrenoceptor blocker drugs (atenolol and propranolol) were investigated in two groups of healthy normotensive subjects. 2. The steady state plasma concentrations of both beta-adrenoceptor blockers were significantly altered by the addition of nisoldipine: for propranolol there were significant increases in Cmax, by about 50%, and in AUC by about 30% and for atenolol there was a significant increase in Cmax, by about 20%. 3. The addition of nisoldipine was also associated with significant changes in apparent liver blood flow (measured by indocyanine green clearance) from 1.4 to 2.4 l min-1 in the atenolol group and from 1.3 to 2.3 l min-1 in the propranolol group. 4. Both nisoldipine-beta-adrenoceptor blocker combinations were associated with small enhanced blood pressure reductions e.g. from 104/60 with atenolol alone to 98/50 mm Hg with the combination but there was no alteration to the extent of beta-adrenoceptor blockade (as assessed by bicycle ergometry). 5. This pharmacodynamic profile in healthy normotensives is consistent with the known therapeutic efficacy of such combination treatments in patients with hypertension and angina. 6. It is suggested that there is a pharmacokinetic component to the efficacy of this type of combination, perhaps reflecting vasodilator-induced changes in drug absorption and/or hepatic extraction.
Topics: Adult; Atenolol; Blood Pressure; Drug Interactions; Exercise; Heart Rate; Humans; Kidney; Liver; Male; Nisoldipine; Propranolol; Reference Values; Regional Blood Flow
PubMed: 1777376
DOI: 10.1111/j.1365-2125.1991.tb03916.x -
The Cochrane Database of Systematic... Oct 2008Beta (ss) blockers are indicated for use in coronary artery disease (CAD). However, optimal therapy for people with CAD accompanied by intermittent claudication has been... (Meta-Analysis)
Meta-Analysis Review
BACKGROUND
Beta (ss) blockers are indicated for use in coronary artery disease (CAD). However, optimal therapy for people with CAD accompanied by intermittent claudication has been controversial due to the presumed peripheral haemodynamic consequences of beta blockers, leading to worsening symptoms of intermittent claudication.
OBJECTIVES
To quantify the potential harm of beta blockers on maximum walking distance, claudication distance, calf blood flow, calf vascular resistance, and skin temperature when used in patients with peripheral arterial disease (PAD).
SEARCH STRATEGY
The Cochrane Peripheral Vascular Diseases (PVD) Group searched for publications describing randomised controlled trials (RCTs) of beta blockers in PAD in their Trials Register (last searched 6 May 2008) and the Cochrane Central Register of Controlled Trials (CENTRAL) (last searched The Cochrane Library 2008, Issue 2). We handsearched relevant journals and conference proceedings.
SELECTION CRITERIA
Randomised controlled trials evaluating the role of both selective (beta1) and non-selective (beta1 and beta2) beta blockers compared with placebo. We excluded trials comparing different types of beta blockers.
DATA COLLECTION AND ANALYSIS
Primary outcome measures were claudication distance in metres, and the time to claudication in minutes, and maximum walking distance in metres and minutes (as assessed by treadmill).Secondary outcome measures were calf blood flow (ml/100 ml/min), calf vascular resistance, and skin temperature (degrees C).
MAIN RESULTS
We included six RCTs fulfilling the above criteria, with a total of 119 patients. The beta blockers studied were atenolol, propranolol, pindolol, and metoprolol. None of the trials showed a statistically significant worsening effect of beta blockers on either the primary or secondary outcomes. There were no reports of any adverse events with the beta blockers studied.
AUTHORS' CONCLUSIONS
There is currently no evidence that beta blockers adversely affect walking distance in people with intermittent claudication. However, due to the lack of large published trials beta blockers should be used with caution if clinically indicated.
Topics: Adrenergic beta-Antagonists; Atenolol; Humans; Intermittent Claudication; Metoprolol; Peripheral Vascular Diseases; Pindolol; Propranolol; Randomized Controlled Trials as Topic
PubMed: 18843692
DOI: 10.1002/14651858.CD005508.pub2