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British Journal of Clinical Pharmacology Sep 19881. The effects of single oral doses of 10 mg bisoprolol and 400 mg acebutolol on respiratory function were studied in nine smokers with airway obstruction in a... (Clinical Trial)
Clinical Trial Comparative Study
1. The effects of single oral doses of 10 mg bisoprolol and 400 mg acebutolol on respiratory function were studied in nine smokers with airway obstruction in a double-blind, placebo-controlled experiment. 2. The effects of the drugs were assessed by measuring specific airway conductance (sGaw) for 3 h after their administration and by studying their interaction with the bronchodilator response to inhaled salbutamol. 3. sGaw did not change for 3 h after bisoprolol or acebutolol administration. The bronchodilator response to inhaled salbutamol was not affected by bisoprolol but significantly reduced by acebutolol (P less than 0.05 vs placebo). 4. Under these conditions, bisoprolol behaves like a selective beta 1-adrenoceptor antagonist but acebutolol exhibits less beta 1-adrenoceptor selectivity.
Topics: Acebutolol; Adrenergic beta-Antagonists; Adult; Bisoprolol; Blood Pressure; Female; Heart Rate; Humans; Lung Diseases, Obstructive; Male; Middle Aged; Propanolamines; Respiration; Smoking
PubMed: 2902873
DOI: 10.1111/j.1365-2125.1988.tb05278.x -
British Journal of Clinical Pharmacology Nov 1980The ability of propranolol, metoprolol, acebutolol, atenolol and practolol to reverse the stimulant effect of 10 M isoprenaline on lymphocyte cyclic AMP levels was...
The ability of propranolol, metoprolol, acebutolol, atenolol and practolol to reverse the stimulant effect of 10 M isoprenaline on lymphocyte cyclic AMP levels was determined. The ratios of doses required to produce 50% inhibition as compared with propranolol were 1:316 for metoprolol 1:1780 for acebutolol and 1:2820 for atenolol. No ratio could be calculated for practolol as it never produced more than 35% inhibition possibly because of its intrinsic sympathomimetic activity. This rank order of antagonist potencies suggest the lymphocyte β-receptor has β selectivity. For peripheral airway smooth muscle isoprenaline, adrenaline and noradrenaline had relative ECs of 1:25:9290 respectively in the absence of uptake blockade. However, the ECs changed to 1:15:82 in the presence of neuronal uptake blockade and x-adrenoceptor blockade. These observations are consistent with β selectivity. Salbutamol behaved as a partial agonist on peripheral airway smooth muscle. It was possible to demonstrate competitive antagonism to isoprenaline. Estimates of the dissociation constant of salbutamol were obtained (6.6 ± 0.02) × 10 M, =4, mean ± s.e. mean). A novel technique for determining the pA is described which is particularly useful on peripheral airway smooth muscle. Values obtained for propranolol and practolol using this technique were: propranolol pA 7.83 ± 0.14; slope=0.97 ± 0.05 (=4), practolol pA 5.62 ± 0.15; slope=1.17 ± 0.17 (=4) These values support the β selectivity suggested by the agonist studies. The cyclic AMP response of lung parenchyma to β-adrenoceptor agonists and antagonists (in the presence of isoprenaline demonstrated β selectivity. Salbutamolol appeared to be a partial agonist when compared with the cyclic AMP response to isoprenaline. The β-adrenoceptors of the lymphocyte, bronchial smooth muscle and lung parenchyma have β selectivity although they differ somewhat quantitatively from each other.
Topics: Bronchi; Cyclic AMP; Histamine; Humans; In Vitro Techniques; Isoproterenol; Lung; Lymphocytes; Muscle Contraction; Muscle, Smooth; Receptors, Adrenergic; Receptors, Adrenergic, beta
PubMed: 6254550
DOI: 10.1111/j.1365-2125.1980.tb01783.x -
Endocrinologia Japonica Jun 1988A patient with essential hypertension receiving the oral administration of acebutolol, a beta 1-selective adrenergic blocker, showed a marked increase in urinary...
A patient with essential hypertension receiving the oral administration of acebutolol, a beta 1-selective adrenergic blocker, showed a marked increase in urinary 17-ketosteroid (17-KS) excretion determined by Zimmermann's method. Since the normal concentration of each fraction of 17-KS was found in this case by gas chromatography, the possibility of an abnormality in steroid metabolism could be excluded from the mechanism of the increase in the measured value for urinary 17-KS. In the urine samples from patients treated with acebutolol, acebutolol and acetylated acebutolol, a main metabolite of acebutolol, were found equally among them. Moreover, acebutolol or acetylated acebutolol resulted in a dose-dependent increase in 17-KS by Zimmermann's method in phosphate buffered saline or in a urine sample. However, the other beta-blockers, such as propranolol, alprenolol and oxprenolol did not show any effect on the determined value for urinary 17-KS. Thus it was concluded that the activated methylene group of acebutolol and acetylated acebutolol may interfere with the measured values obtained by Zimmermann's method.
Topics: 17-Ketosteroids; Acebutolol; Drug Interactions; Female; Humans; Hypertension; Methods; Middle Aged
PubMed: 3197660
DOI: 10.1507/endocrj1954.35.485 -
Chemistry Central Journal Feb 2012A validated simple, rapid, sensitive and specific square-wave voltammetric technique is described for the determination of acebutolol (AC) following its accumulation...
A validated simple, rapid, sensitive and specific square-wave voltammetric technique is described for the determination of acebutolol (AC) following its accumulation onto a hanging mercury drop electrode in a Britton-Robinson universal buffer of pH 7.5. The optimal procedural conditions were: accumulation potential Eacc = - 0.8 V versus Ag/AgCl/KCl, accumulation duration tacc = 30 s, pulse-amplitude = 70 mV, scan rate = 100 mV/s, frequency = 30 Hz, surface area of the working electrode = 0.6 mm2 and the convection rate = 2000 rpm. Under these optimized conditions, the adsorptive stripping voltammetry (AdSV) peak current was proportional over the concentration range 5 × 10-7 - 6 × 10-6 M (r = 0.999). Recoveries for acebutolol from human plasma and urine were in the range 97-103% and 96-104% respectively. The method proved to be precise (intra-day precision expressed as %RSD in human plasma ranged from 2.9 - 3.2% and inter-day precision expressed as %RSD ranged from 3.4 - 3.8%) and accurate (intra-day accuracies expressed as % error in human urine ranged from -3.3 - 2.8% and inter-day accuracies ranged from -3.3 - 1.7%). The limit of quantitation (LOQ) and limit of detection (LOD) for acebutolol were 1.7 × 10-7 and 5 × 10-7 M, respectively. Possible interferences by substances usually present in the pharmaceutical formulations were investigated with a mean recovery of 101.6 ± 0.64%. Results of the developed square-wave adsorptive stripping voltammetry (SW-AdSV) method were comparable with those obtained by reference analytical method.
PubMed: 22353684
DOI: 10.1186/1752-153X-6-15 -
Molecules (Basel, Switzerland) Jun 2024The sustainable catalytic efficacy of transition metal oxides (TMO) and rare earth element-based oxides positions them as pivotal materials for effectively treating...
The sustainable catalytic efficacy of transition metal oxides (TMO) and rare earth element-based oxides positions them as pivotal materials for effectively treating contaminated wastewater. This study successfully synthesized a series of Ce@MnO photocatalysts using a straightforward hydrothermal method. These photocatalysts were thoroughly characterized for their optical properties, structural morphology, and phase purity. Among the synthesized materials, the Ce@MnO (40:60) exhibited the highest photocatalytic activity for the degradation of Acebutolol (ACB), achieving a remarkable degradation efficiency of 92.71% within 90 min under visible light irradiation. This superior performance is attributed to the increased presence of active species and the efficient separation of photogenerated carriers. Additionally, the photocatalytic reaction mechanism was elucidated, highlighting the catalyst's surface charge properties which significantly enhanced performance in a solution with pH 8. The outstanding photo-response in the visible spectrum renders this method not only cost-effective but also environmentally benign, presenting a promising approach for large-scale water purification.
PubMed: 38930919
DOI: 10.3390/molecules29122854 -
British Medical Journal Sep 1977Metoprolol and acebutolol, two supposedly cardioselective beta-adrenoceptor antagonists, were tested in 11 healthy men against propranolol, a non-selective drug, for... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Metoprolol and acebutolol, two supposedly cardioselective beta-adrenoceptor antagonists, were tested in 11 healthy men against propranolol, a non-selective drug, for their effect on plasma free fatty acid concentrations before and after insulin. The fasting concentrations of free fatty acid were significantly reduced after acebutolol and propranolol, and their return to normal after insulin was delayed. Metoprolol had no significant effect on free fatty acid levels either before or after insulin. Although both selective and non-selective beta-blocking drugs should be expected to delay the return of free fatty acid values to normal after insulin, in contrast to propranolol and acebutolol, metoprolol had no such effect. This suggests that metoprolol may not be as effective as the other two drugs in controlling lipid metabolism during long-term treatment with beta-adrenoceptor antagonists.
Topics: Acebutolol; Adult; Fatty Acids, Nonesterified; Humans; Insulin; Lipid Metabolism; Male; Metoprolol; Propanolamines; Propranolol
PubMed: 901996
DOI: 10.1136/bmj.2.6087.601 -
Annals of the Royal College of Surgeons... Mar 1985Twenty eight patients were randomly allocated into treatment or placebo groups. The treatment group received a single 400 mg oral dose of acebutolol, the placebo group... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Twenty eight patients were randomly allocated into treatment or placebo groups. The treatment group received a single 400 mg oral dose of acebutolol, the placebo group an identical inert prepation. A blood sample from each patient was subsequently analysed for plasma concentrations of acebutolol and diacetolol, and the electrocardiogram was continuously monitored for changes of rate and rhythm. The plasma concentrations of acebutolol and diacetolol were all above the previously reported minimum levels for effective dysrhythmia control and the nine patients in whom irregularities of rhythm occurred were all in the placebo group. One patient in the treatment group, who was 58 years old, required intravenous injection of atropine for bradycardia and hypotension after induction of anaesthesia. It is suggested that in patients with small body weights and in those patients over 50 years of age the predmedication dose of acebutolol should be reduced to 200 mg.
Topics: Acebutolol; Administration, Oral; Adult; Arrhythmias, Cardiac; Blood Pressure; Clinical Trials as Topic; Female; Heart Rate; Humans; Intraoperative Complications; Male; Middle Aged; Premedication; Random Allocation; Tooth Extraction
PubMed: 3883878
DOI: No ID Found -
British Journal of Clinical Pharmacology 1982Eleven β-adrenoceptor blocking agents (propranolol, oxprenolol, penbutolol, carteolol, bupranolol, bufetolol, pindolol, atenolol, metoprolol, acebutolol and labetalol)...
Eleven β-adrenoceptor blocking agents (propranolol, oxprenolol, penbutolol, carteolol, bupranolol, bufetolol, pindolol, atenolol, metoprolol, acebutolol and labetalol) were orally administered to 144 patients with essential hypertension for 5 weeks to assess their antihypertensive effects. In addition haemodynamic responses were measured non-invasively using radioactive iodinated human serum albumin. In a second study central haemodynamic changes in response to intravenous injection of propranolol (0.4 mg/kg) were assessed in 21 untreated patients with essential hypertension and compared with those induced by short-time therapy with propranolol, acebutolol or pindolol. During short term (5 weeks) oral therapy all the antagonists with the exception of pindolol and carteolol, showed a tendency to reduce heart rate. The effects on blood pressure were not uniform and for each drug a subgroup of responders (defined as those showing 10 mmHg or more reduction of mean arterial blood pressure) was separately analysed. The responders to antihypertensive therapy showed a wide spectrum of haemodynamic responses. The results would be compatible with the hypothesis that in addition to the reduction in cardiac output, the β-adrenoceptor blockers lower blood pressure by at least one, as yet unknown, mechanism leading to a reduction in total peripheral resistance. The antagonists tested demonstrate a variety of ancillary properties and some differences were apparent between the haemodynamic responses to the different drugs. Cardioselective β-adrenoceptor blockers caused a significant decrease in cardiac index; however no significant change in total peripheral resistance was observed. These effects may be attributable to their weak vascular β-adrenoceptor blockade. In the case of labetalol the additional α-adrenoceptor blocking activity of the drug was reflected by a fall in total peripheral resistance resulting from blockade of the vasoconstrictor effects of neuronal noradrenaline. Pindolol, because of its pronounced ISA, showed qualitative differences from the other antagonists, its antihypertensive effects being accompanied by significant falls of total peripheral resistance and increases in cardiac output. During short term (5 weeks) oral therapy with propranolol, acebutolol or pindolol no marked central haemodynamic changes occurred and in particular, no significant increase in cardiopulmonary blood volume was detected.
Topics: Adrenergic beta-Antagonists; Adult; Aged; Blood Pressure; Cardiac Output; Female; Hemodynamics; Humans; Hypertension; Male; Middle Aged; Pulse; Vascular Resistance
PubMed: 6125176
DOI: 10.1111/j.1365-2125.1982.tb01924.x -
Turkish Journal of Pharmaceutical... Dec 2020Acebutolol HCl (ABL) is a selective β-adrenergic receptor blocking agent that is preferably administered by the oral route despite its low bioavailability (30-50%). The...
OBJECTIVES
Acebutolol HCl (ABL) is a selective β-adrenergic receptor blocking agent that is preferably administered by the oral route despite its low bioavailability (30-50%). The purpose of this study was to evaluate the effect of verapamil HCl (VER) [as P-glycoprotein inhibitor (P-gp)] on the intestinal absorption of ABL by comparing the changes in the absorption rate constant (k) of ABL.
MATERIALS AND METHODS
intestinal perfusion was conducted in healthy male Wistar albino rats to study the absorption phase of ABL. Eighteen rats were divided into three groups. The first group (the control group) was perfused with ABL alone (260 μg/mL). The second and third groups were perfused with ABL (260 μg/mL) in combination with VER at different concentrations (200 and 400 μg/mL, respectively). The analysis was performed using a simple, rapid, and validated spectroscopic method.
RESULTS
The absorption study showed that k of ABL in the first group was 0.47±0.045 h-. In the third group k increased 3-fold (1.37±0.031 h-); however, the second group showed a statistically insignificant change in k (0.39±0.076 h-).
CONCLUSION
The results revealed that VER at a concentration of 400 μg/mL has a pronounced effect on the absorption kinetics of ABL (increased k). This could be linked to the inhibition of P-gp, which is considered a contributing factor in low bioavailability of ABL.
PubMed: 33389978
DOI: 10.4274/tjps.galenos.2019.59862 -
Developmental Cell Mar 2004In the sea urchin embryo, the oral-aboral axis is specified after fertilization by mechanisms that are largely unknown. We report that early sea urchin embryos express... (Comparative Study)
Comparative Study
In the sea urchin embryo, the oral-aboral axis is specified after fertilization by mechanisms that are largely unknown. We report that early sea urchin embryos express Nodal and Antivin in the presumptive oral ectoderm and demonstrate that these genes control formation of the oral-aboral axis. Overexpression of nodal converted the whole ectoderm into oral ectoderm and induced ectopic expression of the orally expressed genes goosecoid, brachyury, BMP2/4, and antivin. Conversely, when the function of Nodal was blocked, by injection of an antisense Morpholino oligonucleotide or by injection of antivin mRNA, neither the oral nor the aboral ectoderm were specified. Injection of nodal mRNA into Nodal-deficient embryos induced an oral-aboral axis in a largely non-cell-autonomous manner. These observations suggest that the mechanisms responsible for patterning the oral-aboral axis of the sea urchin embryo may share similarities with mechanisms that pattern the dorsoventral axis of other deuterostomes.
Topics: Acebutolol; Amphibians; Animals; Body Patterning; Bone Morphogenetic Proteins; Cell Differentiation; Chlorides; Ectoderm; Embryo, Nonmammalian; Embryonic Induction; Endoderm; Gene Expression Regulation, Developmental; Goosecoid Protein; Homeodomain Proteins; In Situ Hybridization; Left-Right Determination Factors; Lithium; Mice; Microinjections; Models, Biological; Molecular Sequence Data; Morphogenesis; Nickel; Nodal Protein; Oligoribonucleotides, Antisense; Phenotype; Repressor Proteins; Reverse Transcriptase Polymerase Chain Reaction; Sea Urchins; Sequence Alignment; Signal Transduction; Transcription Factors; Transforming Growth Factor beta; Zebrafish; Zebrafish Proteins; Zinc Compounds
PubMed: 15030762
DOI: 10.1016/s1534-5807(04)00056-5