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https://www.readbyqxmd.com/read/28107561/beta-blockers-for-hypertension
#1
REVIEW
Charles S Wiysonge, Hazel A Bradley, Jimmy Volmink, Bongani M Mayosi, Lionel H Opie
BACKGROUND: Beta-blockers refer to a mixed group of drugs with diverse pharmacodynamic and pharmacokinetic properties. They have shown long-term beneficial effects on mortality and cardiovascular disease (CVD) when used in people with heart failure or acute myocardial infarction. Beta-blockers were thought to have similar beneficial effects when used as first-line therapy for hypertension. However, the benefit of beta-blockers as first-line therapy for hypertension without compelling indications is controversial...
January 20, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28101724/drug-drug-multicomponent-solid-forms-cocrystal-coamorphous-and-eutectic-of-three-poorly-soluble-antihypertensive-drugs-using-mechanochemical-approach
#2
Jamshed Haneef, Renu Chadha
The present study deals with the application of mechanochemical approach for the preparation of drug-drug multicomponent solid forms of three poorly soluble antihypertensive drugs (telmisartan, irbesartan and hydrochlorothiazide) using atenolol as a coformer. The resultant solid forms comprise of cocrystal (telmisartan-atenolol), coamorphous (irbesartan-atenolol) and eutectic (hydrochlorothiazide-atenolol). The study emphasizes that solid-state transformation of drug molecules into new forms is a result of the change in structural patterns, diminishing of dimers and creating new facile hydrogen bonding network based on structural resemblance...
January 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28089688/functional-identification-of-plasma-membrane-monoamine-transporter-pmat-slc29a4-as-an-atenolol-transporter-sensitive-to-flavonoids-contained-in-apple-juice
#3
Yoshihisa Mimura, Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
The intestinal absorption of atenolol has recently been reported to be reduced by simultaneous ingestion of fruit juices, such as apple juice. This finding implies a possibility that an unidentified carrier-mediated transport system, which could be interfered by some components of those juices, might be involved in atenolol absorption. In an attempt to explore that possibility, we successfully identified plasma membrane monoamine transporter (PMAT/SLC29A4) as a transporter that can operate for cellular atenolol uptake in the intestine, using Madin-Darby canine kidney II cells stably expressing PMAT...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28073770/impact-of-beta-blocker-initiation-timing-on-mortality-risk-in-patients-with-diabetes-mellitus-undergoing-noncardiac-surgery-a-nationwide-population-based-cohort-study
#4
Ray-Jade Chen, Hsi Chu, Lung-Wen Tsai
BACKGROUND: Relevant clinical studies have been small and have not convincingly demonstrated whether the perioperative initiation of beta-blockers should be considered in patients with diabetes mellitus undergoing noncardiac surgery. METHODS AND RESULTS: In this nationwide propensity score-matched study, we included patients with diabetes mellitus undergoing noncardiac surgery between 2000 and 2011 from Taiwan's National Health Insurance Research Database. Patients were classified as beta-blocker and non-beta-blocker cohorts...
January 10, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28065821/an-evaluation-of-the-utility-of-lvdp-dt40-qa-interval-lvdp-dtmin-and-tau-as-indicators-of-drug-induced-changes-in-contractility-and-lusitropy-in-dogs
#5
Michael K Pugsley, Brian Guth, Alan Y Chiang, Jennifer M Doyle, Michael Engwall, Jean-Michel Guillon, Peter K Hoffmann, John E Koerner, Scott W Mittelstadt, Jennifer Beck Pierson, Eric I Rossman, Dustan R Sarazan, Stanley T Parish
INTRODUCTION: The importance of drug-induced effects on the inotropic state of the heart is well known. Unlike hemodynamic and cardiac electrophysiological methods, which have been routinely used in drug safety testing for years, the non-clinical assessment of drug effects on myocardial contractility is used less frequently with no established translation to humans. The goal of these studies was to determine whether assessment of alternate measures of cardiac inotropy could detect drug-induced changes in the contractile state of the heart using drugs known to have clinically relevant positive and negative effects on myocardial contractility...
January 5, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28054999/interaction-between-dna-and-drugs-having-protonable-basic-groups-characterization-through-affinity-constants-drug-release-kinetics-and-conformational-changes
#6
Liliana P Alarcón, Yolima Baena, Rubén H Manzo
This paper reports the in vitro characterization of the interaction between the phosphate groups of DNA and the protonated species of drugs with basic groups through the determination of the affinity constants, the reversibility of the interaction, and the effect on the secondary structure of the macromolecule. Affinity constants of the counterionic condensation DNA-drug were in the order of 10⁶. The negative electrokinetic potential of DNA decreased with the increase of the proportion of loading drugs. The drugs were slowly released from the DNA-drug complexes and had release kinetics consistent with the high degree of counterionic condensation...
January 4, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28045944/pharmaceutical-metabolism-in-fish-using-a-3-d-hepatic-in-vitro-model-to-assess-clearance
#7
Matthew G Baron, Kate S Mintram, Stewart F Owen, Malcolm J Hetheridge, A John Moody, Wendy M Purcell, Simon K Jackson, Awadhesh N Jha
At high internal doses, pharmaceuticals have the potential for inducing biological/pharmacological effects in fish. One particular concern for the environment is their potential to bioaccumulate and reach pharmacological levels; the study of these implications for environmental risk assessment has therefore gained increasing attention. To avoid unnecessary testing on animals, in vitro methods for assessment of xenobiotic metabolism could aid in the ecotoxicological evaluation. Here we report the use of a 3-D in vitro liver organoid culture system (spheroids) derived from rainbow trout to measure the metabolism of seven pharmaceuticals using a substrate depletion assay...
2017: PloS One
https://www.readbyqxmd.com/read/28043207/behavior-of-pharmaceuticals-in-uv-photoreactors-fed-with-sewage-treated-by-anaerobic-aerobic-system
#8
Bruna Coelho Lopes, Ananda Lima Sanson, Sérgio Francisco de Aquino, Cláudio Leite de Souza, Carlos Augusto de Lemos Chernicharo, Robson José de Cássia Franco Afonso
This work has assessed the seasonal changes and the dynamics in the concentration of six pharmaceutical compounds during photolysis as a tertiary treatment of sewage previously treated by an anaerobic/aerobic system comprising a UASB (Upflow Anaerobic Sludge Blanket) reactor and a trickling filter (TF). The target compounds were four antibiotics (ciprofloxacin (CPF), clindamycin (CLM), sulfamethoxazole (SMX), and trimetoprim), one β-blocker (atenolol), and one anti-inflammatory (diclofenac (DCF)). Six hydraulic retention times (HRTs) were evaluated (5, 10, 20, 40, 80, and 160 min) with the intent of varying the ultraviolet C (UVC) radiation doses applied to the effluent from biological treatment containing the target contaminants...
January 19, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28034694/single-jugular-vein-cannulated-rats-may-not-be-suitable-for-intravenous-pharmacokinetic-screening-of-high-logp-compounds
#9
Nilesh Gaud, Anoop Kumar, Muralikrishna Matta, Prashant Kole, Srikanth Sridhar, Sandhya Mandlekar, Vinay K Holenarsipur
Rat is commonly used for pharmacokinetic screening during pharmaceutical lead optimization. To handle the large number of compounds, rats with a single jugular vein cannulation are commonly utilized for intravenous pharmacokinetic studies, where the same cannula is used both for dose administration and blood sampling. We demonstrate that the single cannula method is not suitable for all compounds, especially for high logP compounds. We propose an alternative dual cannulation technique in which two cannulas are placed in the same jugular vein, thus avoiding an additional surgery...
December 26, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28027919/physicochemical-characterisation-and-investigation-of-the-bonding-mechanisms-of-api-titanate-nanotube-composites-as-new-drug-carrier-systems
#10
Barbara Sipos, Klára Pintye-Hódi, Zoltán Kónya, András Kelemen, Géza Regdon, Tamás Sovány
Titanate nanotube (TNT) has recently been explored as a new carrier material for active pharmaceutical ingredients (API). The aim of the present work was to reveal the physicochemical properties of API-TNT composites, focusing on the interactions between the TNTs and the incorporated APIs. Drugs belonging to different Biopharmaceutical Classification System (BCS) classes were loaded into TNTs: diltiazem hydrochloride (BCS I.), diclofenac sodium (BCS II.), atenolol (BCS III.) and hydrochlorothiazide (BCS IV...
December 24, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28011585/the-role-of-sympathetic-and-vagal-cardiac-control-on-complexity-of-heart-rate-dynamics
#11
Luiz Eduardo Virgilio Silva, Carlos Alberto Aguiar Silva, Helio C Salgado, Rubens Fazan
Analysis of heart rate variability (HRV) by nonlinear approaches has been gaining interest due to their ability to extract additional information from heart rate (HR) dynamics, not detectable by traditional approaches. Nevertheless, the physiological interpretation of nonlinear approaches remains unclear. Therefore, we propose long-term (60 min) protocols involving selective blockade of cardiac autonomic receptors to investigate the contribution of sympathetic and parasympathetic function upon nonlinear dynamics of HRV...
December 23, 2016: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/27982380/access-to-and-use-of-high-blood-pressure-medications-in-brazil
#12
Sotero Serrate Mengue, Andréa Dâmaso Bertoldi, Luiz Roberto Ramos, Mareni Rocha Farias, Maria Auxiliadora Oliveira, Noemia Urruth Leão Tavares, Paulo Sergio Dourado Arrais, Vera Lucia Luiza, Tatiane da Silva Dal Pizzol
OBJECTIVE: To analyze the access to and use of medicines for high blood pressure among the Brazilian population according to social and demographic conditions. METHODS: Analysis of data from Pesquisa Nacional Sobre Acesso, Utilização e Promoção do Uso Racional de Medicamentos (PNAUM - National Survey on Access, Use and Promotion of Rational Use of Medicines), a nationwide cross-sectional, population-based study, with probability sampling, carried out between September 2013 and February 2014 in urban households in the five Brazilian regions...
December 2016: Revista de Saúde Pública
https://www.readbyqxmd.com/read/27957711/the-role-of-beta-blockers-in-the-treatment-of-hypertension
#13
John M Cruickshank
IMPORTANCE: Two major guide-line committees (JNC-8 and NICE UK) have dropped beta-blockers as first-line therapy in the treatment of hypertension. Also, recent meta-analyses (that do not take age into account) have concluded that beta-blockers are inappropriate first-line agents in the treatment of hypertension. This review seeks to shed some light on the "rights and wrongs" of such actions and conclusions. OBJECTIVES: Because the pathophysiology of primary/essential hypertension differs in elderly and younger subjects, the latter being closely linked to obesity and increased sympathetic nerve activity, the author sought to clarify the efficacy of beta-blockers in the younger/middle-aged group in reducing the risk of death, and cardiovascular end-points...
December 13, 2016: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/27956919/cardiovascular-effects-of-the-essential-oil-of-croton-argyrophylloides-in-normotensive-rats-role-of-the-autonomic-nervous-system
#14
Thayane Rebeca Alves-Santos, Rodrigo José Bezerra de Siqueira, Gloria Pinto Duarte, Saad Lahlou
Cardiovascular effects of the essential oil of Croton argyrophylloides Muell. Arg. (EOCA) were investigated in normotensive rats. In saline-pretreated anesthetized or conscious rats, intravenous (i.v.) injection of the EOCA induced dose-dependent hypotension. Dose-dependent tachycardia was observed only in conscious rats. In anesthetized rats, cervical bivagotomy failed to enhance EOCA-induced hypotension but unmasked significant bradycardia. In conscious rats, i.v. pretreatment with methylatropine, but not with atenolol or L-NAME, reduced both hypotensive and tachycardiac responses to EOCA...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27939084/hazard-screening-of-photo-transformation-products-from-pharmaceuticals-application-to-selective-%C3%AE-1-blockers-atenolol-and-metoprolol
#15
Anju Priya Toolaram, Jakob Menz, Tushar Rastogi, Christoph Leder, Klaus Kümmerer, Mandy Schneider
The identification of toxic components in cocktail mixtures of pollutants, their metabolites and transformation products (TPs) generated from environmental and treatment processes remains an arduous task. This study expanded in this area by applying a combination of chemical analytics, a battery of in vitro bioassays and an in silico "testing battery" to UV photolysis mixtures of active pharmaceutical ingredients. The objectives were to understand the toxic nature of the mixtures and to prioritize photo-TPs for risk analysis...
February 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/27915141/a-review-of-the-occurrence-of-pharmaceuticals-and-personal-care-products-in-indian-water-bodies
#16
REVIEW
Keshava Balakrishna, Amlan Rath, Yerabham Praveenkumarreddy, Keerthi Siri Guruge, Bikram Subedi
Little information exists on the occurrence and the ultimate fate of pharmaceuticals in the water bodies in India despite being one of the world leaders in pharmaceutical production and consumption. This paper has reviewed 19 published reports of pharmaceutical occurrence in the aquatic environment in India [conventional activated sludge wastewater treatment plants (WTPs), hospital WTPs, rivers, and groundwater]. Carbamazepine (antipsychoactive), atenolol (antihypertensive), triclocarban and triclosan (antimicrobials), trimethoprim and sulfamethoxazole (antibacterials), ibuprofen and acetaminophen (analgesics), and caffeine (stimulant) are the most commonly detected at higher concentrations in Indian WTPs that treat predominantly the domestic sewage...
March 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27913078/pulmonary-artery-dissection-following-balloon-valvuloplasty-in-a-dog-with-pulmonic-stenosis
#17
K A Grint, H B Kellihan
A 3-month-old, 9.9 kg, male pit bull cross was referred for evaluation of collapse. A left basilar systolic heart murmur graded V/VI and a grade IV/VI right basilar systolic heart murmur were ausculted. Echocardiography showed severe pulmonic stenosis characterized by annular hypoplasia, leaflet thickening, and leaflet fusion. After 1 month of atenolol therapy, a pulmonic valve balloon valvuloplasty procedure was performed, and the intra-operative right ventricular pressure was reduced by 43%. Echocardiography, performed the following day, showed apparent rupture of a pulmonary valve leaflet and a membranous structure within the pulmonary artery consistent with a dissecting membrane...
November 30, 2016: Journal of Veterinary Cardiology: the Official Journal of the European Society of Veterinary Cardiology
https://www.readbyqxmd.com/read/27871747/impact-of-external-carbon-dose-on-the-removal-of-micropollutants-using-methanol-and-ethanol-in-post-denitrifying-moving-bed-biofilm-reactors
#18
Elena Torresi, Mònica Escolà Casas, Fabio Polesel, Benedek G Plósz, Magnus Christensson, Kai Bester
Addition of external carbon sources to post-denitrification systems is frequently used in wastewater treatment plants to enhance nitrate removal. However, little is known about the fate of micropollutants in post-denitrification systems and the influence of external carbon dosing on their removal. In this study, we assessed the effects of two different types and availability of commonly used carbon sources -methanol and ethanol- on the removal of micropollutants in biofilm systems. Two laboratory-scale moving bed biofilm reactors (MBBRs), containing AnoxKaldnes K1 carriers with acclimated biofilm from full-scale systems, were operated in continuous-flow using wastewater dosed with methanol and ethanol, respectively...
January 1, 2017: Water Research
https://www.readbyqxmd.com/read/27862262/different-effects-of-selective-%C3%AE-1-adrenoceptor-antagonists-nebivolol-or-atenolol-in-acetaminophen-induced-heptatotoxicity-of-rats
#19
Remon R Rofaeil, Maha Yehia Kamel, Walaa Yehia Abdelzaher
Acetaminophen (APAP) overdose is a common cause of acute liver failure and beta blockers are commonly used drugs in clinical practice. This study aims to evaluate the effect of two different beta blockers agents as nebivolol and atenolol against APAP-induced hepatotoxicity. Male wistar rats were treated with APAP (2 g/kg/day, p.o.) to induce hepatotoxicity. Our results showed that nebivolol and atenolol reduced heart rate and blood pressure. Nebivolol (5 mg/kg /day, p.o.) for 14 days has a hepatoprotective effect shown by significant decrease in hepatic injury parameters (serum AST and ALT) with significant suppression of hepatic malondialdehyde (MDA) and nitric oxide (NO) which were elevated with APAP administration...
November 14, 2016: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/27857521/global-chemical-reactivity-parameters-for-several-chiral-beta-blockers-from-the-density-functional-theory-viewpoint
#20
Mona Maria Talmaciu, Ede Bodoki, Radu Oprean
BACKGROUND AND AIM: Beta-adrenergic antagonists have been established as first line treatment in the medical management of hypertension, acute coronary syndrome and other cardiovascular diseases, as well as for the prevention of initial episodes of gastrointestinal bleeding in patients with cirrhosis and esophageal varices, glaucoma, and have recently become the main form of treatment of infantile hemangiomas. The aim of the present study is to calculate for 14 beta-blockers several quantum chemical descriptors in order to interpret various molecular properties such as electronic structure, conformation, reactivity, in the interest of determining how such descriptors could have an impact on our understanding of the experimental observations and describing various aspects of chemical binding of beta-blockers in terms of these descriptors...
2016: Clujul Medical (1957)
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