1,942 results match your criteria Toxicity Beta-blocker


Amyloid β-dependent mitochondrial toxicity in mouse microglia requires P2X7 receptor expression and is prevented by nimodipine.

Sci Rep 2019 Apr 24;9(1):6475. Epub 2019 Apr 24.

Department of Morphology, Surgery and Experimental Medicine, University of Ferrara, Ferrara, Italy.

Previous data from our laboratory show that expression of the P2X7 receptor (P2X7R) is needed for amyloid β (Aβ)-stimulated microglia activation and IL-1β release in vitro and in vivo. We also showed that Aβ-dependent stimulation is inhibited by the dihydropyridine nimodipine at an intracellular site distal to the P2X7R. In the present study, we used the N13 microglia cell line and mouse primary microglia from wt and P2rx7-deleted mice to test the effect of nimodipine on amyloid β (Aβ)-dependent NLRP3 inflammasome expression and function, and on mitochondrial energy metabolism. Read More

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http://dx.doi.org/10.1038/s41598-019-42931-2DOI Listing

Clinical toxicology of beta-blocker overdose in adults.

Basic Clin Pharmacol Toxicol 2019 Mar 27. Epub 2019 Mar 27.

Mainz Poison Center, Mainz, Germany.

Beta-blocker overdose is potentially harmful due to the strong blood pressure-lowering and heart rate-lowering effects. However, conflicting data exist as to their differential toxicity, single-substance exposures and the effect of co-exposure with additional antihypertensive medication. For this, a 10-year retrospective, explorative analysis of the Mainz Poison Center/Germany database with regard to circumstances of beta-blocker exposure, doses, symptoms and treatment was carried out. Read More

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http://dx.doi.org/10.1111/bcpt.13231DOI Listing
March 2019
10 Reads

A Swine Model of Severe Propranolol Toxicity Permitting Direct Measurement of Brain Tissue Oxygenation.

J Med Toxicol 2019 Mar 20. Epub 2019 Mar 20.

Department of Emergency Medicine, Regions Hospital, 640 Jackson St., St. Paul, MN, 55101, USA.

Introduction: High-dose insulin (HDI) therapy has been used successfully for beta-blocker toxicity, but needs further study when hypotension persists despite HDI. The objective was to develop a model of propranolol toxicity with persistent hypotension despite HDI and to develop means to measure cerebral oxygen tension (PbrO).

Methods: Eight anesthetized Yorkshire pigs were instrumented with a tracheostomy, Swan-Ganz catheter, arterial catheter, and intra-cerebral pressure and oxygen monitor. Read More

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http://dx.doi.org/10.1007/s13181-019-00707-0DOI Listing
March 2019
1 Read

Dual Effect of Doxazosin: Anticancer Activity on SH-SY5Y Neuroblastoma Cells and Neuroprotection on an In Vitro Model of Alzheimer's Disease.

Neuroscience 2019 Apr 14;404:314-325. Epub 2019 Feb 14.

Programa de Pós-Graduação em Ciências Biológicas-Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.

Several studies have demonstrated the antitumor effect of doxazosin, an α1-adrenergic blocker, against glioma and breast, bladder and prostate cancers. Doxazosin is also being evaluated as a treatment for posttraumatic stress disorder (PTSD) and alcoholism, and α1-adrenergic blockers have been linked to neuroprotection in neurodegenerative disorders, such as Alzheimer's Disease (AD). Cancer and AD have an inverse relationship in many aspects, with several factors that contribute to apoptosis inhibition and proliferation being increased in cancers but decreased in AD. Read More

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http://dx.doi.org/10.1016/j.neuroscience.2019.02.005DOI Listing
April 2019
1 Read

Irbesartan suppresses cardiac toxicity induced by doxorubicin via regulating the p38-MAPK/NF-κB and TGF-β1 pathways.

Naunyn Schmiedebergs Arch Pharmacol 2019 Feb 7. Epub 2019 Feb 7.

Department of Pharmacology and Toxicology, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, P.N. 11754, Egypt.

Doxorubicin (DOX) so far continues to be one of the most potent and effective anticancer drugs. Therefore, it is still needed to search for a safe and effective therapy that can opposite DOX-induced cardiotoxicity. Irbesartan (IRB), an angiotensin II receptor blocker, has a wide-ranging variety of biological activities. Read More

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http://dx.doi.org/10.1007/s00210-019-01624-3DOI Listing
February 2019
3 Reads

Fungal treatment of metoprolol and its recalcitrant metabolite metoprolol acid in hospital wastewater: Biotransformation, sorption and ecotoxicological impact.

Water Res 2019 Apr 10;152:171-180. Epub 2019 Jan 10.

Catalan Institute for Water Research (ICRA), H(2)O Building, Scientific and Technological Park of the University of Girona, Emili Grahit 101, E-17003, Girona, Spain; Water and Soil Quality Research Group, Department of Environmental Chemistry, (IDAEA-CSIC), Jordi Girona 18-26, E-08034, Barcelona, Spain.

Hospital wastewater (HWW) effluents represent an important source of contaminants such as pharmaceutical compounds and their human metabolites. To better evaluate dedicated treatment of hospital effluents for pollutant mitigation, not only the parent compounds should be considered but also the intermediates generated during treatment. The metabolite metoprolol acid (MTPA) has been found in urban wastewaters at higher concentration than its parent compound metoprolol (MTP), being more recalcitrant to biodegradation. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00431354193001
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http://dx.doi.org/10.1016/j.watres.2018.12.054DOI Listing
April 2019
12 Reads

The Use of High-dose Insulin Infusion and Lipid Emulsion Therapy in Concurrent Beta-blocker and Calcium Channel Blocker Overdose.

Cureus 2018 Nov 1;10(11):e3534. Epub 2018 Nov 1.

Pulmonology and Critical Care, Abington Hospital - Jefferson Health, Abington, USA.

Patients admitted with the presumed coingestion of beta-blockers (BBs) and calcium channel blockers (CCBs) should be initially managed in accordance with standardized resuscitation protocols (the airway, breathing, and circulation (ABC) approach). Additionally, more specific interventions should be promptly attempted. Intravenous glucagon and calcium salts have long been used in the treatment of BB and CCB toxicities. Read More

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http://dx.doi.org/10.7759/cureus.3534DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6318115PMC
November 2018
3 Reads

Effect of electrolytes on the simultaneous electrochemical oxidation of sulfamethoxazole, propranolol and carbamazepine: behaviors, by-products and acute toxicity.

Environ Sci Pollut Res Int 2019 Mar 11;26(7):6855-6867. Epub 2019 Jan 11.

Mexican Institute of Water Technology (IMTA), Paseo Cuauhnahuac 8532, Progreso, 62550, Jiutepec, Morelos, Mexico.

In this work, the effect of supporting electrolytes on the simultaneous electrochemical oxidation of the pharmaceuticals sulfamethoxazole (SMX), propranolol (PRO), and carbamazepine (CBZ) in aqueous solutions has been studied. Based on the identified by-products, the degradation mechanisms were proposed and the acute toxicity was evaluated for each electrolyte. Assays were carried out in batch mode in a 2 L undivided reactor using a niobium coated with boron-doped diamond (Nb/BDD) mesh anode and Ti cathode at 2. Read More

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http://dx.doi.org/10.1007/s11356-018-4020-9DOI Listing
March 2019
3 Reads

The role of freshwater copepods in the environmental risk assessment of caffeine and propranolol mixtures in the surface water bodies of Spain.

Chemosphere 2019 Apr 18;220:227-236. Epub 2018 Dec 18.

Cavanilles Institute of Biodiversity and Evolutionary Biology, University of Valencia, José Beltrán Martínez, 2, 46980, Paterna, Valencia, Spain; University of Gdańsk, Faculty of Biology, Department of Genetics and Biosystematics, Wita Stwosza 59, 80-308, Gdańsk, Poland.

In this study we aimed at assessing: (i) the environmental risk posed by mixtures of caffeine and propranolol to the freshwater ecosystems of Spain; (ii) the sensitivity of freshwater copepod species to the two compounds; (iii) if the toxicity of caffeine and propranolol to freshwater copepods contributes to the environmental risk posed by the two compounds in the freshwater bodies of Spain. The environmental risk was computed as the ratio of MECs (i.e. Read More

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http://dx.doi.org/10.1016/j.chemosphere.2018.12.117DOI Listing
April 2019
3 Reads

Gelatinized core liposomes: A new Trojan horse for the development of a novel timolol maleate glaucoma medication.

Int J Pharm 2019 Feb 12;556:192-199. Epub 2018 Dec 12.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, African Union Authority Street, Abbassia, 11566 Cairo, Egypt.

Glaucoma treatment with ocular medications requires overcoming the corneal barrier to drug penetration. Liposomes have a great corneal penetration ability and affinity while suffering from poor stability and low entrapment of hydrophilic drugs accompanied by rapid drug release. This work aims to develop a new, effective and stable glaucoma medication with sustained drug release properties; Timolol maleate gelatinized core liposomes. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2018.12.015DOI Listing
February 2019
4 Reads

Crystal structure of the complex between venom toxin and serum inhibitor from Viperidae snake.

J Biol Chem 2019 01 30;294(4):1250-1256. Epub 2018 Nov 30.

Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan, and

Venomous snakes have endogenous proteins that neutralize the toxicity of their venom components. We previously identified five small serum proteins (SSP-1-SSP-5) from a highly venomous snake belonging to the family Viperidae as inhibitors of various toxins from snake venom. The endogenous inhibitors belong to the prostate secretory protein of 94 amino acids (PSP94) family. Read More

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http://dx.doi.org/10.1074/jbc.RA118.006840DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6349104PMC
January 2019
3 Reads

Propranolol Promotes Glucose Dependence and Synergizes with Dichloroacetate for Anti-Cancer Activity in HNSCC.

Cancers (Basel) 2018 Nov 30;10(12). Epub 2018 Nov 30.

Cancer Biology and Immunotherapies Group, Sanford Research, 2301 East 60th St North, Sioux Falls, SD 57104, USA.

Tumor cell metabolism differs from that of normal cells, conferring tumors with metabolic advantages but affording opportunities for therapeutic intervention. Accordingly, metabolism-targeting therapies have shown promise. However, drugs targeting singular metabolic pathways display limited efficacy, in part due to the tumor's ability to compensate by using other metabolic pathways to meet energy and growth demands. Read More

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http://dx.doi.org/10.3390/cancers10120476DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6316475PMC
November 2018
4 Reads

Comparative study on degradation of propranolol and formation of oxidation products by UV/HO and UV/persulfate (PDS).

Water Res 2019 02 24;149:543-552. Epub 2018 Oct 24.

State Key Laboratory of Urban Water Resource and Environment, Harbin Institute of Technology, Harbin, 150090, China.

The frequent detection of propranolol, a widely used β-blocker, in wastewater effluents and surface waters has raised serious concern, due to its adverse effects on organisms. UV/hydrogen peroxide (UV/HO) and UV/persulfate (UV/PDS) processes are efficient in eliminating propranolol in various waters, but the formation of oxidation products in these processes, as well as the assessment of their toxicity, has not been systematically addressed. In this study, we identified and compared transformation products of propranolol produced by hydroxyl radical (OH) and sulfate radical (SO). Read More

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http://dx.doi.org/10.1016/j.watres.2018.08.074DOI Listing
February 2019
5 Reads

Carvedilol suppresses malignant proliferation of mammary epithelial cells through inhibition of the ROS‑mediated PI3K/AKT signaling pathway.

Oncol Rep 2019 Feb 19;41(2):811-818. Epub 2018 Nov 19.

The Second Hospital of Shandong University, Jinan, Shandong 250033, P.R. China.

Reactive oxygen species (ROS) cause oncogenic mutations through direct interaction with DNA. Carvedilol (CAR) exhibits antioxidative activity, and pre‑clinical studies have identified that CAR may prevent malignant transformation in certain carcinogenic models. This suggests that CAR may be a potential agent in cancer prevention. Read More

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http://dx.doi.org/10.3892/or.2018.6873DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6312993PMC
February 2019
3 Reads

Cytotoxicity of new psychoactive substances and other drugs of abuse studied in human HepG2 cells using an adopted high content screening assay.

Toxicol Lett 2019 Feb 19;301:79-89. Epub 2018 Nov 19.

Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, Center for Molecular Signaling (PZMS), Saarland University, Homburg, Germany. Electronic address:

New psychoactive substances (NPS) are still an emerging issue in clinical and forensic toxicology. Information about their cytotoxic potential is limited or even unavailable before distribution and thus their intake can be of high risk for consumers. The aim of the presented study was to develop a strategy to identify cytotoxic potential of NPS based on a high content screening assay (HCSA) using HepG2 cell line and four fluorescent dyes, namely Hoechst33342, TMRM, CAL-520, and TOTO-3. Read More

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http://dx.doi.org/10.1016/j.toxlet.2018.11.007DOI Listing
February 2019
23 Reads

LC-MS/MS analysis of the plasma concentrations of a cocktail of 5 cytochrome P450 and P-glycoprotein probe substrates and their metabolites using subtherapeutic doses.

J Pharm Biomed Anal 2019 Feb 28;164:430-441. Epub 2018 Oct 28.

School of Pharmaceutical Sciences of Ribeirão Preto, Department of Clinical Analysis, Toxicology and Food Science, University of São Paulo, Brazil; Ribeirão Preto Medical School, Department of Internal Medicine, University of São Paulo, Brazil. Electronic address:

Drug transporters and CYP enzymes are important sources of pharmacokinetics (PK) variability in drug responses and can cause various pharmacological and toxicological consequences, leading to either toxicity or an insufficient pharmacological effect. In recent years, the cocktail approach was developed to determine in vivo CYP and transporters activities, but these approaches are somewhat limited. We described the development and validation of three sensitive and specific LC-MS/MS assays for the determination of P-gp and major human CYP isoenzyme activities following oral administration of a drug cocktail of subtherapeutic doses (lower than 10 times) of caffeine (CAF), omeprazole (OME), losartan (LOS), midazolam (MDZ), metoprolol (METO) and fexofenadine (FEX) in healthy volunteers. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S07317085183106
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http://dx.doi.org/10.1016/j.jpba.2018.10.029DOI Listing
February 2019
7 Reads

Carvedilol (CAR) combined with carnosic acid (CAA) attenuates doxorubicin-induced cardiotoxicity by suppressing excessive oxidative stress, inflammation, apoptosis and autophagy.

Biomed Pharmacother 2019 Jan 2;109:71-83. Epub 2018 Nov 2.

Department of Cardiology, Affiliated Hospital of Jining Medical University, 272000, China. Electronic address:

Doxorubicin (DOX) is a wide spectrum antitumor drug. However, its clinical application is limited due to the cardiotoxicity. Carvedilol (CAR) is a β-blocker used to treat high blood pressure and heart failure. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S07533322183079
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http://dx.doi.org/10.1016/j.biopha.2018.07.037DOI Listing
January 2019
16 Reads

Oxidative treatments for atenolol removal in water: Elucidation by mass spectrometry and toxicity evaluation of degradation products.

Rapid Commun Mass Spectrom 2019 Feb;33(3):303-313

Chemistry Department, Universidade Federal de Ouro Preto, Ouro Preto, MG, 35400-000, Brazil.

Rationale: The presence of pharmaceuticals in water is a worldwide concern due to potential damage to human and environmental health. For example, compounds such as the β-blocker atenolol (ATE), widely used for the treatment of cardiac disease, are detected in drinking water since conventional water treatment plants are not designed to remove them. Thus, the evaluation of ATE removal at different water oxidative treatment processes, identification of its degradation products and evaluation of their toxicity is necessary. Read More

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http://doi.wiley.com/10.1002/rcm.8338
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http://dx.doi.org/10.1002/rcm.8338DOI Listing
February 2019
22 Reads

Effects of timolol on Ca handling and viability in human prostate cancer cells.

Toxicol Mech Methods 2019 Feb 10;29(2):138-145. Epub 2019 Jan 10.

c Department of Medical Education and Research, Kaohsiung Veterans General Hospital , Kaohsiung , Taiwan.

Timolol is a medication used widely to treat glaucoma. Regarding Ca signaling, timolol was shown to modulate Ca-related physiology in various cell types, however, the effect of timolol on Ca homeostasis and cell viability has not been explored in human prostate cancer cells. The aim of this study was to explore the effect of timolol on intracellular Ca concentrations ([Ca]) and viability in PC3 human prostate cancer cells. Read More

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http://dx.doi.org/10.1080/15376516.2018.1540024DOI Listing
February 2019
19 Reads

Dopamine promotes cathepsin B-mediated amyloid precursor protein degradation by reactive oxygen species-sensitive mechanism in neuronal cell.

Mol Cell Biochem 2019 Apr 22;454(1-2):153-163. Epub 2018 Oct 22.

Special Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi, 110067, India.

Recent literature suggested an important function of native amyloid precursor protein (APP) as amine oxidase implicating in protection of brain cells from catecholamine-induced toxicity. However, any role of catecholamines on regulation of native APP has not been explored. Here we report that dopamine (DA), one of the most prominent catecholamine neurotransmitters in brain, down-modulates native APP protein in several neuronal cell types. Read More

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http://dx.doi.org/10.1007/s11010-018-3460-3DOI Listing
April 2019
12 Reads

Improving the Reliability and Utility of Streptozotocin-Induced Rat Diabetic Model.

J Diabetes Res 2018 23;2018:8054073. Epub 2018 Sep 23.

Department of Therapeutics, Chromocell Corporation, 685 U.S. Highway One, North Brunswick, NJ 08902, USA.

The Streptozotocin- (STZ-) induced diabetic model is widely used; however, unexplained acute toxicity has given the model an unreliable reputation. To improve the reliability and utility of this model, we characterize the age dependence of STZ toxicity and introduce novel endpoints to assess diabetic complications and reveal possible mechanisms for diabetic development. Diabetes was induced by STZ injection into male, 6 to 23 weeks old, Sprague-Dawley rats. Read More

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https://www.hindawi.com/journals/jdr/2018/8054073/
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http://dx.doi.org/10.1155/2018/8054073DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6174751PMC
January 2019
23 Reads

Effects of early intravenous low-dose of metoprolol on cardiac sympathetic activities and electrophysiological properties in myocardial infarction heart.

Exp Ther Med 2018 Nov 4;16(5):4114-4118. Epub 2018 Sep 4.

Department of Cardiology, Shanghai Changzheng Hospital, Shanghai 200433, P.R. China.

This study observed the effects of early intravenous low-doses of metoprolol on cardiac sympathetic activities and electrophysiological properties in myocardial infarction (MI) dogs. Thirty two mongrel dogs with the first diagonal branch of the left anterior descending coronary artery ligated were randomly divided into three groups: The low-dose group was given metoprolol 0.6 mg/kg immediately by intravenous injection (n=12); the target-dose group was given metoprolol 1. Read More

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http://dx.doi.org/10.3892/etm.2018.6695DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6176129PMC
November 2018
30 Reads

The impact of propranolol, 17α-ethinylestradiol, and gemfibrozil on early life stages of marine organisms: effects and risk assessment.

Environ Sci Pollut Res Int 2018 Nov 16;25(32):32196-32209. Epub 2018 Sep 16.

Physical Chemical Department, Institute of Marine Research (INMAR), International Campus of Excellence of the Sea (CEIMAR), Faculty of Marine and Environmental Sciences, University of Cadiz, 11510, Puerto Real, Cadiz, Spain.

Pharmaceuticals are ubiquitously detected in the marine environment at the ng-μg/L range. Given their biological activity, these compounds are known to induce detrimental effects on biota at relatively low exposure levels; however, whether they affect early life stages of marine species is still unclear. In this study, a set of bioassays was performed to assess the effects of propranolol (PROP), 17-α ethinylestradiol (EE2), and gemfibrozil (GEM) on gamete fertilization and embryonic development of mussels (Mytilus galloprovincialis) and sea urchins (Paracentrotus lividus), and on the survival of seabream (Sparus aurata) larvae. Read More

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http://dx.doi.org/10.1007/s11356-018-3185-6DOI Listing
November 2018
4 Reads

A Young Woman with Bradycardia and Hypotension.

Ann Am Thorac Soc 2018 Sep;15(9):1092-1095

1 Division of Pulmonary and Critical Care.

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http://dx.doi.org/10.1513/AnnalsATS.201802-142CCDOI Listing
September 2018
2 Reads

Low dose Intralipid resuscitation improves survival compared to ClinOleic in propranolol overdose in rats.

PLoS One 2018 30;13(8):e0202871. Epub 2018 Aug 30.

Department of Anesthesiology and Pain Medicine, University of Alberta, Edmonton, Alberta, Canada.

Background: Medication overdose is a prevalent issue and despite mixed reports of efficacy, the use of intravenous lipid emulsions, notably Intralipid®, for the management of toxicity from lipid-soluble drugs is becoming increasingly prevalent. Whether alternative lipid emulsion formulations have similar efficacy for resuscitation compared to Intralipid is not known. Here, we compared the efficacy of Intralipid and ClinOleic® for resuscitation following overdose with the lipid-soluble beta-adrenergic antagonist propranolol. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0202871PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6116996PMC
February 2019
22 Reads

Large-scale in silico identification of drugs exerting sex-specific effects in the heart.

J Transl Med 2018 08 29;16(1):236. Epub 2018 Aug 29.

Department of Physiology and Pathophysiology, MOE Key Lab of Cardiovascular Sciences, School of Basic Medical Sciences, Peking University, 38 Xueyuan Rd, Beijing, 100191, China.

Background: Major differences exist between men and women in both physiology and pathophysiology. Dissecting the underlying processes and contributing mechanisms of sex differences in health and disease represents a crucial step towards precision medicine. Considering the significant differences between men and women in the response to pharmacotherapies, our aim was to develop an in silico model able to predict sex-specific drug responses in a large-scale. Read More

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http://dx.doi.org/10.1186/s12967-018-1612-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6116388PMC
August 2018
21 Reads
3.930 Impact Factor

An Overview of Hyperinsulinemic-Euglycemic Therapy in Calcium Channel Blocker and β-blocker Overdose.

Pharmacotherapy 2018 Nov 4;38(11):1130-1142. Epub 2018 Oct 4.

Purdue University College of Pharmacy, West Lafayette, Indiana.

Both calcium channel blockers (CCBs) and β blockers (BBs) are associated with fatal substance exposures within the United States. Cases of overdose with these agents have the potential to be both complex and difficult to manage. A variety of pharmacologic treatment options are available for clinicians to use to help mitigate harm from these poisonings. Read More

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http://dx.doi.org/10.1002/phar.2177DOI Listing
November 2018
7 Reads

Behavior and histopathology as biomarkers for evaluation of the effects of paracetamol and propranolol in the neotropical fish species Phalloceros harpagos.

Environ Sci Pollut Res Int 2018 Oct 9;25(28):28601-28618. Epub 2018 Aug 9.

Departamento de Biologia, Universidade de Aveiro, Campus de Santiago, 3810-193, Aveiro, Portugal.

Pharmaceutical drugs in the aquatic environment can induce adverse effects on nontarget organisms. This study aimed to assess the short-term effects of sublethal concentrations of both paracetamol and propranolol on the fish Phalloceros harpagos, specifically light/dark preference, swimming patterns, skin pigmentation, histopathology, and liver glycogen levels. Fish were acutely exposed to sublethal concentrations of both paracetamol (0. Read More

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http://dx.doi.org/10.1007/s11356-018-2839-8DOI Listing
October 2018
1 Read

Design, synthesis, and in silico studies of novel eugenyloxy propanol azole derivatives having potent antinociceptive activity and evaluation of their β-adrenoceptor blocking property.

Mol Divers 2019 Feb 9;23(1):147-164. Epub 2018 Aug 9.

Faculty of Pharmacy, Shiraz University of Medical Science, Medicinal and Natural Products Chemistry Research Center, P.O.Box 71345-1149, Shiraz, Iran.

The design, synthesis, antinociceptive and β-adrenoceptor blocking activities of several eugenyloxy propanol azole derivatives have been described. In this synthesis, the reaction of eugenol with epichlorohydrin provided adducts 3 and 4 which were N-alkylated by diverse azoles to obtain the eugenyloxy propanol azole analogues in good yields. Adducts 3 and 4 were also reacted with azide ion to obtain the corresponding azide 6. Read More

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http://dx.doi.org/10.1007/s11030-018-9867-7DOI Listing
February 2019
6 Reads

Conduction and contraction properties of human iPS cell-derived cardiomyocytes: analysis by motion field imaging compared with the guinea-pig isolated heart model.

J Toxicol Sci 2018 ;43(8):493-506

Research Division, Chugai Pharmaceutical Co., Ltd.

We used motion field imaging to characterize the conduction and contraction of a sheet of cardiomyocytes derived from human induced pluripotent stem cells (hiPS-CMs). A hiPS-CMs sheet of 2.8 mm × 2. Read More

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http://dx.doi.org/10.2131/jts.43.493DOI Listing
August 2018
6 Reads

Labrasol-Enriched Nanoliposomal Formulation: Novel Approach to Improve Oral Absorption of Water-Insoluble Drug, Carvedilol.

AAPS PharmSciTech 2018 Oct 20;19(7):2961-2970. Epub 2018 Jul 20.

Department of Pharmaceutics, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism. Conventional and various surfactant-enriched carvedilol-loaded liposomes were prepared by thin film hydration technique and physicochemical properties of liposomes (including size, encapsulation efficiency, release behavior, and morphology) were evaluated. To assess the oral bioavailability, in vivo studies were carried out in eight groups of male Wistar rats (n = 6) and the drug plasma concentration was determined. Read More

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http://link.springer.com/10.1208/s12249-018-1118-9
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http://dx.doi.org/10.1208/s12249-018-1118-9DOI Listing
October 2018
30 Reads

Small molecules bind human mTOR protein and inhibit mTORC1 specifically.

Biochem Pharmacol 2018 09 17;155:298-304. Epub 2018 Jul 17.

Department of Molecular Biosciences, 1089 Veterinary Medicine Dr., VM3B, UC Davis, CA 95616, USA. Electronic address:

Inhibition of mTOR activity (mechanistic target of rapamycin) is an anti-cancer therapeutic strategy. mTOR participates in two functional complexes, mTORC1 and mTORC2. Since mTORC1 is specifically activated in multiple tumors, novel molecules that inhibit mTORC1 could be therapeutically important. Read More

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http://dx.doi.org/10.1016/j.bcp.2018.07.013DOI Listing
September 2018
19 Reads

Inhibitory effect of timolol on topical glucocorticoid‑induced skin telangiectasia.

Mol Med Rep 2018 Sep 9;18(3):2823-2831. Epub 2018 Jul 9.

Department of Dermatology, Renmin Hospital of Wuhan University, Wuhan, Hubei 430060, P.R. China.

The aim of the present study wasto investigate the potential inhibitory effect of timolol on topical glucocorticoid‑induced skin telangiectasia. In rabbits, flumethasone ointment was used to induce skin telangiectasia in the inner ear. Subsequently, timolol maleate (0. Read More

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http://dx.doi.org/10.3892/mmr.2018.9266DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6102693PMC
September 2018
4 Reads

Utilizing recycled LiFePO from batteries in combination with B@CN and CuFeO as sustainable nano-junctions for high performance degradation of atenolol.

Chemosphere 2018 Oct 18;209:457-469. Epub 2018 Jun 18.

College of Materials Science and Engineering, Shenzhen Key Laboratory of Polymer Science and Technology, Guangdong Research Center for Interfacial Engineering of Functional Materials, Nanshan District Key Laboratory for Biopolymers and Safety Evaluation, Shenzhen University, Shenzhen, 518060, PR China. Electronic address:

In this report recycled LiFePO (LFP) from exhaust batteries was utilized to form B@CN/LiFePO/CuFeO (BLC) nano-junction as a visible active photocatalyst. The junction synthesized by two routes: Using as extracted LFP and forming LFP by extracted FePO and LiCO via in-situ deposition method. The two ternary junctions BLC and BLC (E) (utilizing as extracted LFP) were utilized for visible and solar powered degradation of beta-blocker drug Atenolol (ATL). Read More

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http://dx.doi.org/10.1016/j.chemosphere.2018.06.117DOI Listing
October 2018
6 Reads
3.340 Impact Factor

Sublethal metabolic responses to contaminant mixture toxicity in Daphnia magna.

Environ Toxicol Chem 2018 09 30;37(9):2448-2457. Epub 2018 Jul 30.

Environmental NMR Centre and Department of Physical and Environmental Sciences, University of Toronto, Toronto, Ontario, Canada.

Anthropogenic activity is increasing the presence of contaminants that enter waterways through wastewater effluent and urban and/or agricultural runoff, generally in complex mixtures. Depending on the mode of action of the individual contaminant within the mixture, toxicity can occur due to contaminants having similar or dissimilar modes of action. However, it is unknown how the metabolome responds to sublethal contaminant mixtures in the keystone genus Daphnia. Read More

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http://dx.doi.org/10.1002/etc.4208DOI Listing
September 2018
2 Reads

Effect of β-adrenergic receptor agents on cardiac structure and function and whole-body gene expression in Daphnia magna.

Environ Pollut 2018 Oct 12;241:869-878. Epub 2018 Jun 12.

School of Earth Science and Environmental Engineering, Gwangju Institute of Science and Technology (GIST), 123 Cheomdan-gwagiro, Buk-gu, Gwangju, 61005, South Korea. Electronic address:

Propranolol (PRO), a human β-AR (β-adrenergic receptor) antagonist, is considered to result in specific effects in a non-target species, D. magna, based on our previous studies. The present study investigated the effects of β-AR agents, including an antagonist and agonist using pharmacologically relevant endpoints as well as a more holistic gene expression approach to reveal the impacts and potential mode of actions (MOAs) in the model non-target species. Read More

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http://dx.doi.org/10.1016/j.envpol.2018.06.026DOI Listing
October 2018
12 Reads

Influence of pH on the uptake and toxicity of β-blockers in embryos of zebrafish, Danio rerio.

Aquat Toxicol 2018 Aug 28;201:129-137. Epub 2018 May 28.

Department Cell Toxicology, Helmholtz-Centre for Environmental Research - UFZ, Permoserstr. 15, 04318 Leipzig, Germany. Electronic address:

ß-Blockers are weak bases with acidity constants related to their secondary amine group. At environmental pH they are protonated with the tendency to shift to their neutral species at more alkaline pH. Here we studied the influence of pH from 5. Read More

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http://dx.doi.org/10.1016/j.aquatox.2018.05.020DOI Listing
August 2018
24 Reads

Zumba-induced Takotsubo cardiomyopathy: a case report.

J Med Case Rep 2018 Jun 10;12(1):160. Epub 2018 Jun 10.

Department of Internal Medicine, Wayne State University School of Medicine, Rochester Hills, MI, USA.

Background: Takotsubo cardiomyopathy or stress cardiomyopathy is characterized by transient left ventricular apical ballooning in the absence of coronary occlusion. The underlying pathophysiological mechanism is still unclear but possible causes have been proposed mainly catecholamine cardiotoxicity, followed by metabolic disturbance, coronary microvascular impairment, and multivessel epicardial coronary artery vasospasm. Takotsubo cardiomyopathy accounts for 1-2% of patients presenting with acute coronary syndrome with the majority of patients diagnosed with Takotsubo cardiomyopathy being women > 55 years of age. Read More

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http://dx.doi.org/10.1186/s13256-018-1696-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5994255PMC
June 2018
9 Reads

No obvious sympathetic excitation after massive levothyroxine overdose: A case report.

Medicine (Baltimore) 2018 Jun;97(23):e10909

Department of Urology, Peking Union Medical College Hospital, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing, China.

Rationale: Thyrotoxicosis from an overdose of medicinal thyroid hormone is a condition that may be associated with a significant delay in onset of toxicity. However, limited literature is available regarding thyrotoxicosis attributed to excessive ingestion of exogenous thyroid hormone and most cases described were pediatric clinical researches. Herein, we presented the course of a patient who ingested a massive amount of levothyroxine with no obvious sympathetic excited symptoms exhibited and reviewed feasible treatment options for such overdoses. Read More

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http://dx.doi.org/10.1097/MD.0000000000010909DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5999513PMC
June 2018
6 Reads

The Effects of Lipid Emulsion, Magnesium Sulphate and Metoprolol in Amitriptyline-Induced Cardiovascular Toxicity in Rats.

Cardiovasc Toxicol 2018 12;18(6):547-556

Department of Emergency Medicine, Health Science University İzmir Bozyaka Research and Training Hospital, Izmir, Turkey.

The aim of this study was to evaluate the effects of metoprolol, lipid emulsion and MgSO which can be recommended for prevention of long QT that is one of the lethal consequences of amitriptyline intoxication. Thirty Sprague-Dawley male rats were included. Five groups respectively received the following: saline intraperitoneally (i. Read More

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http://dx.doi.org/10.1007/s12012-018-9466-yDOI Listing
December 2018
5 Reads

Unsuspected Clenbuterol Toxicity in a Patient Using Intramuscular Testosterone.

Clin Pract Cases Emerg Med 2017 Aug 23;1(3):197-200. Epub 2017 May 23.

University of Massachusetts School of Medicine, Department of Emergency Medicine, Division of Toxicology, Worcester, Massachusetts.

Clenbuterol is a beta-agonist that has been abused by fitness-oriented individuals for muscle growth and weight loss. We report a case of a 46-year-old man who presented tachycardic, hypokalemic, and hyperglycemic after injecting testosterone obtained from Brazil. He developed refractory hypotension and was started on an esmolol infusion for suspected beta-agonist toxicity. Read More

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http://dx.doi.org/10.5811/cpcem.2017.2.33318DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5965169PMC
August 2017
3 Reads

DenTimol as A Dendrimeric Timolol Analogue for Glaucoma Therapy: Synthesis and Preliminary Efficacy and Safety Assessment.

Mol Pharm 2018 07 30;15(7):2883-2889. Epub 2018 May 30.

Department of Chemical & Life Science Engineering , Virginia Commonwealth University , Richmond , Virginia 23219 , United States.

In this work, we report the synthesis and characterization of DenTimol, a dendrimer-based polymeric timolol analog, as a glaucoma medication. A timolol precursor ( S)-4-[4-(oxiranylmethoxy)-1,2,5-thiadiazol-3-yl]morpholine (OTM) was reacted with the heterobifunctional amine polyethylene glycol acetic acid (amine-PEG-acetic acid, M = 2000 g/mol) via a ring opening reaction of an epoxide by an amine to form the OTM-PEG conjugate. OTM-PEG was then coupled to an ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimer G3 to generate DenTimol using the N-(3-(dimethylamino)propyl)- N'-ethylcarbodiimide hydrochloride (EDC)/ N-hydroxysuccinimide (NHS) coupling reaction. Read More

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http://pubs.acs.org/doi/10.1021/acs.molpharmaceut.8b00401
Publisher Site
http://dx.doi.org/10.1021/acs.molpharmaceut.8b00401DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6075655PMC
July 2018
29 Reads

Bucindolol attenuates the vascular remodeling of pulmonary arteries by modulating the expression of the endothelin-1 A receptor in rats with pulmonary arterial hypertension.

Biomed Pharmacother 2018 Mar 20;99:704-714. Epub 2018 Feb 20.

Laboratory of Cardiovascular Physiology and Reactive Oxygen Species, Institute of Basic Health Science, Universidade Federal do Rio Grande do Sul, Rio Grande do Sul, Brazil. Electronic address:

The aim of this study was to investigate the role of the ß-adrenergic blocker bucindolol on endothelial dysfunction and pulmonary vascular remodeling in rats with pulmonary arterial hypertension (PAH). Male Wistar rats were divided into four groups: control, monocrotaline (MCT), control?+?bucindolol and monocrotaline?+?bucindolol (MCT?+?BCD). PAH was induced by an injection of monocrotaline (60?mg/kg i. Read More

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http://dx.doi.org/10.1016/j.biopha.2018.01.127DOI Listing
March 2018
6 Reads

Exploring gelatin nanoparticles as novel nanocarriers for Timolol Maleate: Augmented in-vivo efficacy and safe histological profile.

Int J Pharm 2018 Jul 27;545(1-2):229-239. Epub 2018 Apr 27.

Department of Pharmaceutical Technology, Faculty of Pharmacy and Biotechnology, German University in Cairo, Cairo, Egypt; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

The use of gelatin has been gaining recognition in ocular delivery for its safety profile and biocompatible properties. Timolol Maleate (TM) is an anti-glaucoma drug possessing poor corneal penetration while causing eye irritation making it an ideal candidate for novel nanoparticulate systems. Timolol Maleate loaded Gelatin Nanoparticles (GNPs) were prepared using the double desolvation method utilizing glutaraldehyde as the crosslinking agent. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2018.04.059DOI Listing
July 2018
8 Reads
3.650 Impact Factor

Association between hyperinsulinemia-euglycemia therapy and hyponatremia.

Am J Health Syst Pharm 2018 04;75(7):422

Division of Allergy/Pulmonary and Critical Care MedicineVanderbilt University School of MedicineNashville, TN.

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http://dx.doi.org/10.2146/ajhp170898DOI Listing
April 2018
5 Reads

Association between hyperinsulinemia-euglycemia therapy and hyponatremia.

Am J Health Syst Pharm 2018 04;75(7):420-422

Florida/USVI Poison Information Center-JacksonvilleUFHealth Jacksonville/University of Florida Health ScienceCenterJacksonville, FL.

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http://dx.doi.org/10.2146/ajhp170849DOI Listing
April 2018
5 Reads

Proposal of degradation pathway with toxicity prediction for hydrolytic and photolytic degradation products of timolol.

J Pharm Biomed Anal 2018 May 28;154:7-15. Epub 2018 Feb 28.

National Centre for Mass Spectrometry, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana 500007, India.

Timolol (TIM) is a potent β-adrenergic blocker, useful in treatment of ocular hypertension or open-angle glaucoma. Development and validation of stability indicating LCMS assay method for TIM was accomplished coherent with ICH guideline. Successful chromatographic separation of TIM with its four degradation products was attained by using gradient elution mode on reverse phase column using ammonium acetate buffer, pH 4. Read More

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http://dx.doi.org/10.1016/j.jpba.2018.02.057DOI Listing
May 2018
19 Reads

Left Ventricular Dysfunction and Chemotherapeutic Agents.

Curr Cardiol Rep 2018 03 8;20(4):20. Epub 2018 Mar 8.

Advanced Heart Failure in the Division of Cardiology, Hospital of the University of Pennsylvania, Philadelphia, PA, 19104, USA.

Purpose Of Review: We aim to summarize the effect of cancer therapy-related cardiotoxicity on the development of left ventricular (LV) dysfunction.

Recent Findings: We discuss commonly used cancer therapeutics that have the potential for both acute and delayed cardiotoxicity. LV dysfunction from cancer therapies may be found by routine cardiac imaging prior to clinical manifestations of heart failure (HF) and we discuss the current multi-modality approaches for early detection of toxicity with the use of advanced echocardiographic parameters including strain techniques. Read More

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http://dx.doi.org/10.1007/s11886-018-0967-xDOI Listing
March 2018
3 Reads

Oxidation of the β-blocker propranolol by UV/persulfate: Effect, mechanism and toxicity investigation.

Chemosphere 2018 Jun 1;201:50-58. Epub 2018 Mar 1.

State Key Laboratory of Pollution Control and Resource Reuse, College of Environmental Science and Engineering, Tongji University, Shanghai, 200092, China.

In this study, the degradation of propranolol (PRO) by UV/persulfate process was systematically investigated. Direct photolysis of PRO was limited due to its low quantum yield, while the PRO degradation efficiency can be greatly promoted by the combination of persulfate and UV irradiation. Radical scavenging tests showed that both SO and OH contributed to the removal of PRO, with SO playing a more important role. Read More

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http://dx.doi.org/10.1016/j.chemosphere.2018.02.158DOI Listing
June 2018
5 Reads

Metoprolol induces oxidative damage in common carp (Cyprinus carpio).

Aquat Toxicol 2018 Apr 18;197:122-135. Epub 2018 Feb 18.

Laboratorio de Toxicología Ambiental, Facultad de Química, Universidad Autónoma del Estado de México, Paseo Colón intersección Paseo Tollocan s/n. Col. Residencial Colón, 50120, Toluca, Estado de México, México. Electronic address:

During the last decade, β-blockers such as metoprolol (MTP) have been frequently detected in surface water, aquatic systems and municipal water at concentrations of ng/L to μg/L. Only a small number of studies exist on the toxic effects induced by this group of pharmaceuticals on aquatic organisms. Therefore, the present study aimed to evaluate the oxidative damage induced by MTP in the common carp Cyprinus carpio, using oxidative stress biomarkers. Read More

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http://dx.doi.org/10.1016/j.aquatox.2018.02.012DOI Listing
April 2018
5 Reads