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Clinical Pharmacology in Drug... May 2024Atenolol, a cardioselective β1-blocker, exhibits efficacy in treating cardiovascular diseases. We conducted a single-center, randomized, open, single-dose,...
Atenolol, a cardioselective β1-blocker, exhibits efficacy in treating cardiovascular diseases. We conducted a single-center, randomized, open, single-dose, 2-preparation, 2-cycle, 2-sequence, double-crossover trial with a 7-day washout period to investigate the pharmacokinetics, bioequivalence (BE), and safety of test and reference atenolol tablets (25 mg) in healthy Chinese volunteers. Forty-eight healthy participants were randomized into the fasting and fed arms. After administering a single oral dose of the test or reference formulation (25 mg), plasma atenolol concentrations were measured using liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were obtained from concentration-time profiles. In total, 23 and 24 individuals were included in the fasting and fed arms, respectively. The mean concentration-time profiles for both formulations were similar, and C, AUC, and AUC were within the BE range of 80%-125%. Thirteen adverse events (AEs) were observed in 7 participants in the fasting arm; 1 withdrew from the trial early owing to an AE. In the fed arm, 20 AEs were observed in 8 participants, and none withdrew from the trial. All adverse reactions were grade I, with no serious AEs or deaths. Therefore, the 2 tablets are bioequivalent in healthy Chinese individuals under fasting and fed conditions, supporting their further clinical development.
PubMed: 38742472
DOI: 10.1002/cpdd.1414 -
Cureus Apr 2024I, the author of this case report, was on beta blockers, initially atenolol and later on nebivolol, for my "systemic hypertension" illness. After attending the National...
I, the author of this case report, was on beta blockers, initially atenolol and later on nebivolol, for my "systemic hypertension" illness. After attending the National Pulmonary Conference, I fell during the return journey on the express highway, became unconscious, and reached the tertiary care hospital of the medical college at the end of the day. The electrocardiogram was suggestive of a "complete heart block.". They immediately implanted a temporary pacemaker and transferred me to the cardiac care unit. I was discharged after five days of stay in the hospital, as the Holter study concluded to be normal. After about two weeks, I felt lightheadedness and giddiness for a fraction of a second. An eminent senior cardiologist in my hometown advised Holter's study; this time, it was suggestive of long pauses. A permanent pacemaker was implanted with the diagnosis of sick sinus syndrome. This autobiographical case report hopes to shed light on more advanced cardiac screening in the search for the etiology of clinical symptoms.
PubMed: 38738068
DOI: 10.7759/cureus.58017 -
Journal of Veterinary Cardiology : the... Jun 2024A nine-year-old spayed female domestic shorthair cat with a previous diagnosis of hypertrophic cardiomyopathy and treated for one month with atenolol (6.25 mg q 12 h)...
A nine-year-old spayed female domestic shorthair cat with a previous diagnosis of hypertrophic cardiomyopathy and treated for one month with atenolol (6.25 mg q 12 h) was referred for respiratory distress and anorexia. The cat was diagnosed with pulmonary oedema secondary to obstructive hypertrophic cardiomyopathy. After stabilisation, she was discharged with furosemide (1 mg/kg q 12 h), clopidogrel (18.75 mg q 24 h), atenolol (6.25 mg q 12 h), and mirtazapine (2 mg/cat q 24 h) to increase appetite. At recheck, the cat was lethargic and presented with severe bradycardia with a junctional escape rhythm and ventriculoatrial conduction. The mirtazapine was discontinued due to its possible side-effects on cardiac rhythm. After three days, the atenolol was halved because the bradyarrhythmia was still present. After 10 days, the rhythm returned to sinus; atenolol was reintroduced twice daily with no further side-effects. The absence of a sinus rhythm with a junctional escape rhythm and P' retroconduction is compatible with a third-degree sinus block or a sinus standstill; the differentiation of these rhythm disturbances is impossible, based on the surface electrocardiogram (ECG). The sinus rhythm was restored after mirtazapine was withdrawn. However, it is not possible to rule out the role of the atenolol or the combined effect of the two drugs. The cat was affected by hypertrophic cardiomyopathy, and the role of myocardial remodelling cannot be excluded. This is the first time that a bradyarrhythmia consequent to the treatment with atenolol and mirtazapine was described in a cat.
Topics: Female; Mirtazapine; Animals; Atenolol; Cats; Cat Diseases; Cardiomyopathy, Hypertrophic; Bradycardia; Mianserin; Adrenergic beta-1 Receptor Antagonists
PubMed: 38735230
DOI: 10.1016/j.jvc.2024.03.003 -
International Journal of Cardiology Aug 2024The aim of this study is to evaluate the effect of beta-blockers and angiotensin receptor blockers in reducing the aortic growth rate in children with bicuspid aortic... (Observational Study)
Observational Study
AIMS
The aim of this study is to evaluate the effect of beta-blockers and angiotensin receptor blockers in reducing the aortic growth rate in children with bicuspid aortic valve (BAV)-related aortopathy and ascending phenotype.
METHODS
Consecutive paediatric patients (≤16 years) with BAV and ascending aorta (AsAo) dilation (z-score > 3) were enrolled in this observational retrospective cohort study. Patients receiving prophylactic treatment with either atenolol (0.5 to 1.0 mg/kg/daily) or losartan (0.7 to 1.4 mg/kg/daily) were compared with those who did not receive medical prophylaxis (control group). The primary outcome of interest was the annual rate of change in maximal AsAo diameter z-score in the treatment and control groups.
RESULTS
From a cohort of 1005 patients, 120 (mean age 11.3 ± 4.5 years, 82% males) fulfilled the inclusion criteria and were included in the study. Patients in the treatment and control group had similar age, sex, family history of BAV, BAV morphology, and baseline AsAo diameter. During a median follow-up of 7.1 years (interquartile range 3.8-10.2), no differences were observed in the annual growth rate of aortic diameter z-score between patients on treatment and controls. The prevalence of aortic diameter progression was similar in the treatment and control groups, and treatment with atenolol or losartan was not associated with a lower rate of aortic disease progression.
CONCLUSIONS
The findings revealed no significant difference in the annual aortic growth rate between treated and untreated patients. Larger cohort studies or, ideally, randomized clinical controlled trials are needed to validate these findings.
Topics: Humans; Male; Female; Bicuspid Aortic Valve Disease; Child; Retrospective Studies; Adolescent; Adrenergic beta-Antagonists; Aortic Valve; Angiotensin Receptor Antagonists; Losartan; Follow-Up Studies; Cohort Studies; Atenolol; Treatment Outcome; Aorta; Aortic Valve Disease; Heart Valve Diseases; Angiotensin II Type 1 Receptor Blockers
PubMed: 38714235
DOI: 10.1016/j.ijcard.2024.132067 -
The Journal of the Association of... Sep 2023β-adrenergic blocker group of medicines has been traditionally used to control high blood pressure since propranolol was discovered by Sir James Black almost 50 years...
β-adrenergic blocker group of medicines has been traditionally used to control high blood pressure since propranolol was discovered by Sir James Black almost 50 years ago. They were the drug of choice in hypertension (HTN) associated with ischemic heart disease, tachyarrhythmias including atrial fibrillation (AF), and anxiety. Congestive cardiac failure was a relative contraindication, but with major advances in science, it became an absolute indication. However, with the advent of newer antihypertensives, especially calcium channel blocker (CCBs) and renin-angiotensin-aldosterone inhibitors, comparative studies were done, and depending on the outcomes of these trials, β-blockers (BBs) were downgraded to fourth or fifth-line therapy, except in the conditions mentioned above, along with HTN in pregnancy. But clinicians never rejected BBs as important antihypertensives, as evidenced by various real-world data. Also, many investigators found the unfairness of the trial designs where BBs were poor performers. The fact that all BBs are not similar, and differ widely in various properties, added to the question of downgrading all BBs on the basis of trials mostly with atenolol, which is also used once daily. Moreover, trials like ASCOT could not show the reduction of most of the events after long-term follow-up with the use of newer antihypertensives. Added to the issue is the fact that the majority of the trials used BBs with diuretics, and selecting BBs as the sole nonperformer appears to be unjustified and illogical. The recent European Society of HTN (ESH) guideline reemphasized the fact that all the five major classes of antihypertensives, including BBs, can be used as first-line medicine and also can be used interchangeably. Moreover, apart from the traditional indications of BBs, this guideline listed nineteen other conditions, including high heart rate (HR), chronic obstructive pulmonary disease (COPD), and obstructive sleep apnoea, as the conditions where BBs are preferred agents as antihypertensive. So, the life history of BBs in HTN has completed a full cycle, and they are ready now for prime time again. How to cite this article: Ray S, Saboo B, Joshi S, β-blockers as the First Line of Treatment for Hypertension Management. J Assoc Physicians India 2023;71(9):95-100.
Topics: Humans; Adrenergic beta-Antagonists; Antihypertensive Agents; Hypertension; Evidence-Based Medicine; Practice Guidelines as Topic
PubMed: 38700308
DOI: 10.59556/japi.71.0341 -
Chemosphere Jun 2024Elevated usage of pharmaceutical products leads to the accumulation of emerging contaminants in sewage. In the current work, Ganoderma lucidum (GL) was used to remove...
Elevated usage of pharmaceutical products leads to the accumulation of emerging contaminants in sewage. In the current work, Ganoderma lucidum (GL) was used to remove pharmaceutical compounds (PCs), proposed as a tertiary method in sewage treatment plants (STPs). The PCs consisted of a group of painkillers (ketoprofen, diclofenac, and dexamethasone), psychiatrists (carbamazepine, venlafaxine, and citalopram), beta-blockers (atenolol, metoprolol, and propranolol), and anti-hypertensives (losartan and valsartan). The performance of 800 mL of synthetic water, effluent STP, and hospital wastewater (HWW) was evaluated. Parameters, including treatment time, inoculum volume, and mechanical agitation speed, have been tested. The toxicity of the GL after treatment is being studied based on exposure levels to zebrafish embryos (ZFET) and the morphology of the GL has been observed via Field Emission Scanning Electron Microscopy (FESEM). The findings conclude that GL can reduce PCs from <10% to >90%. Diclofenac and valsartan are the highest (>90%) in the synthetic model, while citalopram and propranolol (>80%) are in the real wastewater. GL effectively removed pollutants in 48 h, 1% of the inoculum volume, and 50 rpm. The ZFET showed GL is non-toxic (LC is 209.95 mg/mL). In the morphology observation, pellets GL do not show major differences after treatment, showing potential to be used for a longer treatment time and to be re-useable in the system. GL offers advantages to removing PCs in water due to their non-specific extracellular enzymes that allow for the biodegradation of PCs and indicates a good potential in real-world applications as a favourable alternative treatment.
Topics: Wastewater; Water Pollutants, Chemical; Animals; Zebrafish; Reishi; Waste Disposal, Fluid; Pharmaceutical Preparations; Malaysia; Sewage; Biodegradation, Environmental; Diclofenac
PubMed: 38697564
DOI: 10.1016/j.chemosphere.2024.142209 -
The Journal of Toxicological Sciences 2024Drug-induced convulsions are a major challenge to drug development because of the lack of reliable biomarkers. Using machine learning, our previous research indicated...
Drug-induced convulsions are a major challenge to drug development because of the lack of reliable biomarkers. Using machine learning, our previous research indicated the potential use of an index derived from heart rate variability (HRV) analysis in non-human primates as a biomarker for convulsions induced by GABA receptor antagonists. The present study aimed to explore the application of this methodology to other convulsants and evaluate its specificity by testing non-convulsants that affect the autonomic nervous system. Telemetry-implanted males were administered various convulsants (4-aminopyridine, bupropion, kainic acid, and ranolazine) at different doses. Electrocardiogram data gathered during the pre-dose period were employed as training data, and the convulsive potential was evaluated using HRV and multivariate statistical process control. Our findings show that the Q-statistic-derived convulsive index for 4-aminopyridine increased at doses lower than that of the convulsive dose. Increases were also observed for kainic acid and ranolazine at convulsive doses, whereas bupropion did not change the index up to the highest dose (1/3 of the convulsive dose). When the same analysis was applied to non-convulsants (atropine, atenolol, and clonidine), an increase in the index was noted. Thus, the index elevation appeared to correlate with or even predict alterations in autonomic nerve activity indices, implying that this method might be regarded as a sensitive index to fluctuations within the autonomic nervous system. Despite potential false positives, this methodology offers valuable insights into predicting drug-induced convulsions when the pharmacological profile is used to carefully choose a compound.
Topics: Animals; Male; Machine Learning; Seizures; Heart Rate; 4-Aminopyridine; Kainic Acid; Convulsants; Ranolazine; Bupropion; Electrocardiography; Dose-Response Relationship, Drug; Autonomic Nervous System; Telemetry; Biomarkers
PubMed: 38692910
DOI: 10.2131/jts.49.231 -
Water Research Jun 2024Separate collection and treatment of urine optimizes nutrient recovery and enhances micropollutant removal from municipal wastewater. One typical urine treatment train... (Comparative Study)
Comparative Study
Separate collection and treatment of urine optimizes nutrient recovery and enhances micropollutant removal from municipal wastewater. One typical urine treatment train includes nutrient recovery in three biological processes: anaerobic storage, followed by aerobic organics degradation concurrently with nitrification. These are usually followed by activated carbon adsorption to remove micropollutants. However, removing micropollutants prior to nitrification would protect nitrifiers from potential inhibition by pharmaceuticals. In addition, combining simplified biological treatment with activated carbon adsorption could offer a cheap and robust process for removing micropollutants where nutrient recovery is not the first priority, as a partial loss of ammonia occurs without nitrification. In this study, we investigated whether activated carbon adsorption could also take place between the three biological treatment steps. We tested the effectiveness of micropollutant removal with activated carbon after each biological treatment step by conducting experiments with anaerobically stored urine, organics-depleted urine, and nitrified urine. The urine solutions were spiked with 19 pharmaceuticals: amisulpride, atenolol, atenolol acid, candesartan, carbamazepine, citalopram, clarithromycin, darunavir, diclofenac, emtricitabine, fexofenadine, hydrochlorothiazide, irbesartan, lidocaine, metoprolol, N-acetylsulfamethoxazole, sulfamethoxazole, trimethoprim, venlafaxine, and two artificial sweeteners, acesulfame and sucralose. Batch experiments were conducted with powdered activated carbon (PAC) to determine how much activated carbon achieve which degree of micropollutant removal and how organics, pH, and speciation change from ammonium to nitrate influence adsorption. Micropollutant removal was also tested in granular activated carbon (GAC) columns, which is the preferred technology for micropollutant removal from urine. The carbon usage rates (CUR) per person were lower for all urine solutions than for municipal wastewater. The results showed that organics depletion would be needed when micropollutant removal was the sole aim of urine treatment, as the degradation of easily biodegradable organics prevented clogging of GAC columns. However, CUR did hardly improve with organics-depleted urine compared to stored urine. The lowest CUR was achieved with nitrified urine. This resulted from the additional organics removal during nitrification and not the lower pH or the partial conversion of ammonium to nitrate. In addition, we showed that the relative pharmaceutical removal in all solutions was independent of the initial pharmaceutical concentration unless the background organics matrix changed considerably. We conclude that removal of micropollutants in GAC columns from organics-depleted urine can be performed without clogging, but with the drawback of a higher carbon usage compared to removal from nitrified urine.
Topics: Adsorption; Water Pollutants, Chemical; Nitrification; Charcoal; Anaerobiosis; Waste Disposal, Fluid; Wastewater; Urine; Pharmaceutical Preparations; Water Purification
PubMed: 38692253
DOI: 10.1016/j.watres.2024.121615 -
Water Science and Technology : a... Apr 2024Nanofiltration (NF) membrane technology has been widely used in the removal of salts and trace organic pollutants, such as pharmaceuticals and personal care products...
Enhanced properties of a positive-charged nanofiltration membrane containing quaternarized chitosan through second interfacial polymerization for the removal of salts and pharmaceuticals.
Nanofiltration (NF) membrane technology has been widely used in the removal of salts and trace organic pollutants, such as pharmaceuticals and personal care products (PPCPs), due to its superiority. A positive-charged composite NF membrane with an active skin layer was prepared by polyethyleneimine (PEI), trimethyl benzene chloride, and quaternate chitosan (HTCC) through second interfacial polymerization on the polyethersulfone ultrafiltration membrane. The physicochemical properties of the nanocomposite membrane were investigated using surface morphology, hydrophilicity, surface charge, and molecular weight cut-off (MWCO). The influence of the concentration and reaction time of PEI and HTCC was documented. The optimized membrane had a MWCO of about 481 Da and possessed a pure water permeability of 25.37 L·m·h·MPa. The results also exhibited salt rejection ability as MgCl > CaCl > MgSO > NaSO > NaCl > KCl, showing a positive charge on the fabricated membrane. In addition, the membrane had higher rejection to atenolol, carbamazepine, amlodipine, and ibuprofen at 89.46, 86.02, 90.12, and 77.21%, respectively. Moreover, the anti-fouling performance and stability of the NF membrane were also improved.
Topics: Chitosan; Membranes, Artificial; Water Pollutants, Chemical; Pharmaceutical Preparations; Water Purification; Polymerization; Salts; Ultrafiltration; Filtration
PubMed: 38678406
DOI: 10.2166/wst.2024.109 -
Heliyon Apr 2024Torsades de Pointes (TdP) is a malignant polymorphic ventricular tachycardia with heart rate corrected QT interval (QTc) prolongation, which may be attributed to...
Case report: A 56-year-old woman presenting with torsades de pointes and cardiac arrest associated with levosimendan administration and underlying congenital long QT syndrome type 1.
Torsades de Pointes (TdP) is a malignant polymorphic ventricular tachycardia with heart rate corrected QT interval (QTc) prolongation, which may be attributed to congenital and acquired factors. Although various acquired factors for TdP have been summarized, levosimendan administration in complex postoperative settings is relatively uncommon. Timely identification of potential causes and appropriate management may improve the outcome. Herein, we describe the postoperative case of a 56-year-old female with initial normal QTc who accepted the administration of levosimendan for heart failure, suffered TdP, cardiac arrest, and possible Takotsubo cardiomyopathy, further genetically confirmed as long QT syndrome type 1 (LQT1). The patient was successfully treated with magnesium sulfate, atenolol, and implantable cardioverter defibrillator implantation. There should be a careful evaluation of the at-risk populations and close monitoring of the electrocardiograms, particularly the QT interval, to reduce the risk of near-fatal arrhythmias during the use of levosimendan.
PubMed: 38644859
DOI: 10.1016/j.heliyon.2024.e29300