-
British Journal of Clinical Pharmacology Nov 1986The effects of single oral doses of atenolol 50 mg and xamoterol 200 mg (a recently developed partial beta 1-adrenoceptor agonist) on lung function, heart rate and blood... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The effects of single oral doses of atenolol 50 mg and xamoterol 200 mg (a recently developed partial beta 1-adrenoceptor agonist) on lung function, heart rate and blood pressure were investigated in 11 patients with asthma. Xamoterol caused a significant increase in heart rate and systolic blood pressure, which changes are consistent with the partial beta 1-adrenoceptor agonist activity of this drug. Atenolol induced a significant decrease in FEV1 and the forced vital capacity (FVC); there was a non-significant change in FEV1 and FVC after xamoterol. There was no significant difference between the effects of atenolol and xamoterol of FEV1 and FVC. Bronchospasm induced by atenolol 50 mg and xamoterol 200 mg was completely reversed by inhalation of the beta 2-adrenoceptor agonist terbutaline to a cumulative dose of 4.0 mg.
Topics: Adrenergic beta-Agonists; Adult; Asthma; Atenolol; Blood Pressure; Double-Blind Method; Forced Expiratory Volume; Heart Rate; Hemodynamics; Humans; Lung; Male; Middle Aged; Peak Expiratory Flow Rate; Propanolamines; Random Allocation; Terbutaline; Vital Capacity; Xamoterol
PubMed: 2878680
DOI: 10.1111/j.1365-2125.1986.tb02940.x -
British Journal of Clinical Pharmacology Jun 19821 The effects of 4 week treatment periods of once-daily atenolol 100 mg, nadolol 80 mg, nadolol 160 mg and placebo on resting and exercise heart rate and blood pressure... (Clinical Trial)
Clinical Trial Comparative Study
1 The effects of 4 week treatment periods of once-daily atenolol 100 mg, nadolol 80 mg, nadolol 160 mg and placebo on resting and exercise heart rate and blood pressure were compared in a single-blind crossover trial in fifteen patients with essential hypertension. 2 Both atenolol and nadolol, irrespective of dose, reduced resting and exercise blood pressures to the same extent. 3 Nadolol caused a greater bradycardia both at rest and during exercise than did atenolol, thereby effecting a greater reduction in double-product. 4 During progressive treadmill exercise neither atenolol nor nadolol prevented a linear increase in heart rate and blood pressure which were parallel to, but at a lower level than, that produced by placebo. 5 In each individual patient the magnitude of the hypotensive effect produced by one drug was similar to that produced by the other. 6 All the treatment periods resulted in the same linear increase in the patients' perceived exertion scores during exercise despite marked differences in haemodynamic responses evoked by the beta-adrenoceptor blockers compared with placebo. 7 Neither atenolol or nadolol produced any significant change in peak expiratory flow rate compared with placebo.
Topics: Adrenergic beta-Antagonists; Adult; Atenolol; Blood Pressure; Exercise Test; Heart Rate; Humans; Hypertension; Middle Aged; Nadolol; Peak Expiratory Flow Rate; Physical Exertion; Propanolamines
PubMed: 6124268
DOI: 10.1111/j.1365-2125.1982.tb01876.x -
Prediction of in vivo atenolol removal by high-permeability hemodialysis based on an in vitro model.Journal of Pharmacy & Pharmaceutical... 2013In order to update our data on drug dialyzability using the high-permeability dialysis membranes, atenolol elimination by an in vitro dialysis model was compared to that... (Clinical Trial)
Clinical Trial
PURPOSE
In order to update our data on drug dialyzability using the high-permeability dialysis membranes, atenolol elimination by an in vitro dialysis model was compared to that observed in six patients during high-permeability hemodialysis (HD), and the predictive value of the model was evaluated.
METHODS
Atenolol clearance was evaluated in six patients undergoing chronic HD. They were considered as eligible candidates if they were between 18 and 80 years of age, had a body mass index between 19 and 30 kg/m2, underwent HD and were taking atenolol on a regular basis in oral tablet form for at least 1 month before the study started. Atenolol clearance was also evaluated in three in vitro dialysis sessions with high-permeability polysulfone membrane. Atenolol was dissolved in 6 L of Krebs-Henseleit buffer with bovine serum albumin. Dialysis parameters were set to mirror as much as possible the patients' parameters (flow rate: 300 mL/min, dialyzate flow: 500 mL/min). After sample collection, drug concentrations were measured with high performance liquid chromatography. The comparison between in vivo and in vitro atenolol elimination kinetics was performed by drawing the curve fittings of concentrations vs. time on SigmaPlot 12, and adding a 95% prediction interval to each elimination curve fitting.
RESULTS
Mean dialysis clearance of atenolol in vitro and in vivo was 198 ± 4 and 235 ± 53 mL/min, respectively. Atenolol was significantly removed within the study time period in both in vitro and in vivo experiments. By the end of in vitro dialysis, atenolol remaining in the drug reservoir was less than 2% of initial arterial concentration.
CONCLUSION
Our study has indicated that atenolol is almost entirely cleared during high-permeability hemodialysis. Furthermore, the in vitro prediction interval of the drug elimination curve fitting could forecast its in vivo elimination especially at the end of dialysis.
Topics: Adrenergic beta-1 Receptor Antagonists; Adult; Aged; Atenolol; Female; Humans; Male; Membranes, Artificial; Middle Aged; Models, Biological; Permeability; Renal Dialysis
PubMed: 24393549
DOI: 10.18433/j3930s -
Journal of Pharmacy & Pharmaceutical... 2001The beta-blockers comprise a group of drugs that are mostly used to treat cardiovascular disorders such as hypertension, cardiac arrhythmia, or ischemic heart disease.... (Review)
Review
The beta-blockers comprise a group of drugs that are mostly used to treat cardiovascular disorders such as hypertension, cardiac arrhythmia, or ischemic heart disease. Each of these drugs possesses at least one chiral center, and an inherent high degree of enantioselectivity in binding to the beta-adrenergic receptor. For beta-blockers with a single chiral center, the (-) enantiomer possesses much greater affinity for binding to the beta-adrenergic receptors than antipode. The enantiomers of some of these drugs possess other effects, such as antagonism at alpha-adrenergic receptors or Class III antiarrhythmic activity. However, these effects generally display a lower level of stereoselectivity than the beta-blocking activity. Except for timolol, all of these drugs used systemically are administered clinically as the racemate. As a class, the beta blockers are quite diverse from a pharmacokinetic perspective, as they display a high range of values in plasma protein binding, percent of drug eliminated by metabolism or unchanged in the urine, and in hepatic extraction ratio. With respect to plasma concentrations attained after oral or intravenous dosing, in most cases the enantiomers of the beta-blockers show only a modest degree of stereoselectivity. However, the relative magnitude of the concentrations of the enantiomers in plasma is not constant in all situations and varies from drug to drug. Further, various factors related to the drug (e.g., dosing rate or enantiomer-enantiomer interaction) or the patient (e.g., racial background, cardiovascular function, or the patient metabolic phenotype) may affect the stereospecific pharmacokinetics and pharmacodynamics of beta-blockers. An understanding of the stereospecific pharmacokinetics and pharmacodynamics of beta-blockers may help clinicians to interpret and predict differences among patients in pharmacologic responses to these drugs.
Topics: Absorption; Adrenergic beta-Antagonists; Age Factors; Atenolol; Cardiovascular Diseases; Humans; Metoprolol; Molecular Conformation; Propanolamines; Propranolol; Sex Factors; Tissue Distribution
PubMed: 11466176
DOI: No ID Found -
British Journal of Clinical Pharmacology 1984Pharmacological interactions in both directions between phenprocoumon and atenolol and metoprolol were investigated using a crossover trial. Co-administration of...
Pharmacological interactions in both directions between phenprocoumon and atenolol and metoprolol were investigated using a crossover trial. Co-administration of phenprocoumon did not significantly affect Cmax, tmax, t1/2,22, AUC for atenolol or metoprolol. Co-administration of metoprolol, but not atenolol, increased mean plasma phenprocoumon concentrations 4 and 6 h after dosing and was caused by a decrease in the apparent volume of distribution. This increase in plasma phenprocoumon was not associated with an increase in prothrombin time or in the total area under the concentration-time curve. Although the transient increase of phenprocoumon plasma levels caused by metoprolol may be of little clinical significance after a single dose of phenprocoumon, a more important alteration in phenprocoumon disposition and effect should be considered in individual patients on long-term therapy.
Topics: 4-Hydroxycoumarins; Adult; Atenolol; Blood Coagulation; Drug Interactions; Female; Humans; Kinetics; Male; Metoprolol; Phenprocoumon
PubMed: 6743480
DOI: 10.1111/j.1365-2125.1984.tb02439.x -
American Journal of Hypertension Apr 2014Night blood pressure (BP) predicts patient outcomes. Variables associated with night BP response to antihypertensive agents have not been fully evaluated in essential... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Night blood pressure (BP) predicts patient outcomes. Variables associated with night BP response to antihypertensive agents have not been fully evaluated in essential hypertension.
METHODS
We sought to measure night BP responses to hydrochlorothiazide (HCTZ), atenolol (ATEN), and combined therapy using ambulatory blood pressure (ABP) monitoring in 204 black and 281 white essential hypertensive patients. Initial therapy was randomized; HCTZ and ATEN once daily doses were doubled after 3 weeks and continued for 6 more weeks with the alternate medication added for combined therapy arms. ABP was measured at baseline and after completion of each drug. Night, day, and night/day BP ratio responses (treatment - baseline) were compared in race/sex subgroups.
RESULTS
Baseline night systolic BP and diastolic BP, and night/day ratios were greater in blacks than whites (P < 0.01, all comparisons). Night BP responses to ATEN were absent and night/day ratios increased significantly in blacks (P < 0.05). At the end of combined therapy, women, blacks, and those starting with HCTZ as opposed to ATEN had significantly greater night BP responses (P < 0.01). Variables that significantly associated with ATEN response differed from those that associated with HCTZ response and those that associated with night BP response differed from those that associated with day BP response.
CONCLUSIONS
In summary, after completion of HCTZ and ATEN therapy, women, blacks, and those who started with HCTZ had greater night BP responses. Reduced night BP response and increased night/day BP ratios occured with ATEN in blacks. Given the prognostic significance of night BP, strategies for optimizing night BP antihypertensive therapy should be considered.
CLINICAL TRIAL REGISTRATION
Clinicaltrials.gov identifier NCT00246519.
Topics: Adolescent; Adult; Aged; Antihypertensive Agents; Atenolol; Black People; Blood Pressure; Blood Pressure Monitoring, Ambulatory; Circadian Rhythm; Drug Therapy, Combination; Essential Hypertension; Female; Humans; Hydrochlorothiazide; Hypertension; Male; Middle Aged; White People
PubMed: 23886594
DOI: 10.1093/ajh/hpt124 -
British Journal of Clinical Pharmacology 1984Treatment of angina pectoris with beta-adrenoceptor antagonists and verapamil in combination is effective and increasingly common. The study reported here was designed...
Treatment of angina pectoris with beta-adrenoceptor antagonists and verapamil in combination is effective and increasingly common. The study reported here was designed to show whether the pharmacokinetics of verapamil are influenced by concurrent treatment with three different beta-adrenoceptor blockers, and whether there is any pharmacodynamic interaction between these drugs. Twelve healthy volunteers (eight men, four women) aged 21-25 years and weighing 48-82 kg consented to participate in the study. They received verapamil 50 mg three times daily for four 1-week periods, each separated by a 1 week 'washout' period. During three of the four treatment periods, the subjects took either atenolol 100 mg once daily, metoprolol 100 mg twice daily or propranolol 80 mg twice daily; in the remaining period they took verapamil alone. The concentration/time curve and plasma elimination half-life of verapamil and norverapamil, its major metabolite, were not influenced by 1 weeks co-administration atenolol, metoprolol or propranolol. As expected, co-administration of each of the beta-adrenoceptor blockers significantly reduced exercise heart rate when compared with verapamil alone.
Topics: Adrenergic beta-Antagonists; Adult; Atenolol; Blood Pressure; Drug Interactions; Female; Half-Life; Heart Diseases; Heart Rate; Humans; Kinetics; Male; Metoprolol; Propranolol; Verapamil
PubMed: 6146339
DOI: 10.1111/j.1365-2125.1984.tb02426.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 -
Basic & Clinical Pharmacology &... Apr 2022
Topics: Adrenergic beta-Antagonists; Atenolol; Drug-Related Side Effects and Adverse Reactions; Female; Humans; Hypertension; Japan; Male; Renal Insufficiency, Chronic
PubMed: 35174631
DOI: 10.1111/bcpt.13717 -
BioMed Research International 2014The objective of the present study was to develop bilayer tablets of atorvastatin and atenolol that are characterized by initial fast-release of atorvastatin in the...
The objective of the present study was to develop bilayer tablets of atorvastatin and atenolol that are characterized by initial fast-release of atorvastatin in the stomach and comply with the release requirements of sustained-release of atenolol. An amorphous, solvent evaporation inclusion complex of atorvastatin with β -cyclodextrin, present in 1 : 3 (drug/cyclodextrin) molar ratio, was employed in the fast-release layer to enhance the dissolution of atorvastatin. Xanthan gum and guar gum were integrated in the sustained-release layer. Bilayer tablets composed of sustained-release layer (10% w/w of xanthan gum and guar gum) and fast-release layer [1 : 3 (drug/cyclodextrin)] showed the desired release profile. The atorvastatin contained in the fast-release layer showed an initial fast-release of more than 60% of its drug content within 2 h, followed by sustained release of the atenolol for a period of 12 h. The pharmacokinetic study illustrated that the fast absorption and increased oral bioavailability of atorvastatin as well as therapeutic concentration of atenolol in blood were made available through adoption of formulation strategy of bilayer tablets. It can be concluded that the bilayer tablets of atorvastatin and atenolol can be successfully employed for the treatment of hypertension and hypercholesterolemia together through oral administration of single tablet.
Topics: Administration, Oral; Atenolol; Atorvastatin; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Combinations; Heptanoic Acids; Humans; Hypercholesterolemia; Hypertension; Pyrroles; Solubility
PubMed: 24527446
DOI: 10.1155/2014/396106