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Neuroscience 2019 Feb 13. Epub 2019 Feb 13.

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 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

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

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

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

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

Water Res 2019 Feb 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

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

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

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

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

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

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

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

1 Division of Pulmonary and Critical Care.

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

J Transl Med 2018 Aug 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

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

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

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

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

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

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

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

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

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

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

Mol Pharm 2018 Jul 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

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

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

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

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

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

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

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

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

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

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

Cardiol Res 2018 Feb 11;9(1):46-49. Epub 2018 Feb 11.

Division of Gastroenterology, Department of Medicine, Bronx Lebanon Hospital Center, Bronx, NY, USA.

Calcium channel blocker (CCB ) overdose, whether intentional or accidental, is a common clinical scenario and can be very lethal. Conventional treatments for CCB overdose include intravenous (IV) fluids, calcium salts, dopamine, dobutamine, norepinephrine, phosphodiesterase inhibitors, and glucagon. However, the conventional therapies are unsuccessful in reversing the cardiovascular toxicity of CCB, so they commonly fail to improve the hemodynamic condition of the patient. Read More

J Intensive Care Soc 2018 Feb 13;19(1):50-55. Epub 2017 Jun 13.

Department of Intensive Care, Royal Surrey County Hospital, Guildford, UK.

We present the case of a 51-year-old woman admitted to our intensive care unit following an intentional overdose of a calcium channel antagonist and a beta blocker. The resultant hypotension was reversed with glucagon, noradrenaline, calcium and high-dose insulin. Despite these interventions, she remained vasoplegic and received a delayed, standard dose of intralipid. Read More

Cell Stress Chaperones 2018 07 12;23(4):695-702. Epub 2018 Feb 12.

Department of Neurology, Liaocheng People's Hospital, No. 67 Dongchang West Road, Dongchangfu District, Liaocheng, Shandong, 252000, China.

Mutations in amyloid precursor protein (APP) and presenilin1 result in overproduction and accumulation of β-amyloid (Aβ) peptide, which has been shown to play an important role in Alzheimer's disease (AD) pathogenesis. Carvedilol, a nonselective β-adrenergic receptor blocker used for treatment for heart failure and hypertension, has displayed its neuroprotective capacity due to its antioxidant property. In this study, we investigated whether Carvedilol has a neuronal protective effect against endogenous Aβ neurotoxicity in mouse Neuro2a (N2a) cells transfected with Swedish amyloid precursor protein (Swe-APP) mutant and Presenilin exon9 deletion mutant (N2a/Swe. Read More

Pharmacol Res Perspect 2018 02;6(1)

Department of Anatomic and Molecular Pathology, Faculty of Basic Medical Sciences, College of Medicine, University of Lagos, Lagos, Nigeria.

This study investigated the protective effects of carvedilol alone and coadministered with prednisolone and diltiazem on doxorubicin (DOX) and 5-fluorouracil (5-FU)-induced toxicity. Each of 2 pools of 70 female rats were randomly allotted into 10 groups of 7 animals each and treated as follows: Group 1: normal saline (10 mL/kg); Group 2: normal saline and DOX (40 mg/kg)/5-FU (20 mg/kg) alone; Group 3: gallic acid (200 mg/kg) and DOX/5-FU; Group 4: carvedilol (0.075 mg/kg) and DOX/5-FU; Group 5: carvedilol (0. Read More

Int J Cardiol 2018 03 28;254:195-202. Epub 2018 Jan 28.

First Department of Medicine, Faculty of Medicine, University Medical Centre Mannheim (UMM), University of Heidelberg, Mannheim, Germany; DZHK (German Center for Cardiovascular Research), Partner Sites, Heidelberg-Mannheim and Göttingen, Mannheim, Germany.

Background And Purpose: Previous studies revealed that Takotsubo cardiomyopathy (TTC), a transient disorder of ventricular dysfunction affecting predominantly postmenopausal women, is associated with acquired long QT syndrome and arrhythmias, but the exact pathophysiologic mechanism is unknown. Our aim is to investigate the electrophysiological mechanism for QT-prolongation in TTC-patients by using human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs).

Methods: hiPSC-CMs, which were generated from human skin fibroblasts of three healthy donors, were treated by estradiol (10μM for one week) and a toxic concentration of isoprenaline (Iso, 1mM for 2h). Read More

Cell Physiol Biochem 2018 24;45(2):446-457. Epub 2018 Jan 24.

Jiangxi Key Laboratory of Organic Chemistry, Jiangxi Science & Technology Normal University, Nanchang, China.

Background/aims: Islet beta cells (β-cells) are unique cells that play a critical role in glucose homeostasis by secreting insulin in response to increased glucose levels. Voltage-gated ion channels in β-cells, such as K+ and Ca2+ channels, contribute to insulin secretion. The response of voltage-gated Na+ channels (VGSCs) in β-cells to the changes in glucose levels remains unknown. Read More

Int J Nanomedicine 2018 12;13:415-428. Epub 2018 Jan 12.

Guangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Department of Pharmaceutics, Guangdong Pharmaceutical University.

Background: Glaucoma is a serious eye disease that can lead to loss of vision. Unfortunately, effective treatments are limited by poor bioavailability of antiglaucoma medicine due to short residence time on the preocular surface.

Materials And Methods: To solve this, we successfully prepared novel controlled-release ion-exchange microparticles to deliver betaxolol hydrochloride (BH). Read More

Clin Exp Emerg Med 2018 Jan 31. Epub 2018 Jan 31.

Department of Internal Medicine, University of California Davis Medical Center, Sacramento, CA, USA.

Cardiovascular and central nervous system (CNS) toxicity, including tachydysrhythmia, agitation, and seizures, may arise from cocaine or bupropion use. We report acute toxicity from the concomitant use of cocaine and bupropion in a 25-year-old female. She arrived agitated and uncooperative, with a history of possible antecedent cocaine use. Read More

Sci Rep 2018 01 26;8(1):1657. Epub 2018 Jan 26.

Department of Obstetrics, Gynecology, and Reproductive Sciences, Division of Maternal-Fetal Medicine, Rutgers Robert Wood Johnson Medical School, New Brunswick, New Jersey, USA.

The non-canonical NF-κB signaling (RelB/p52) pathway drives pro-labor genes in the human placenta, including corticotropin-releasing hormone (CRH) and cyclooxygenase-2 (COX-2), making this a potential therapeutic target to delay onset of labor. Here we sought to identify small molecule compounds from a pre-existing chemical library of orally active drugs that can inhibit this NF-κB signaling, and in turn, human placental CRH and COX-2 production. We used a cell-based assay coupled with a dual-luciferase reporter system to perform an in vitro screening of a small molecule library of 1,120 compounds for inhibition of the non-canonical NF-κB pathway. Read More

Naunyn Schmiedebergs Arch Pharmacol 2018 02 11;391(2):207-217. Epub 2018 Jan 11.

Department of Pharmacology, Al-Ameen College of Pharmacy, Bengaluru, India.

Metabolic abnormalities including hyperglycemia, hyperlipidemia, and oxidative-nitrosative stress are involved in the progression of diabetic neuropathy. In the present study, we targeted oxidative-nitrosative stress using nebivolol, a β-receptor antagonist with vasodilator and antioxidant property, to evaluate its neuroprotective effect in streptozotocin-induced diabetic neuropathy in rats. Diabetic neuropathy develops within 4-6 weeks after administration of streptozotocin (55 mg/kg, i. Read More

Med Res Rev 2018 07 5;38(4):1332-1403. Epub 2018 Jan 5.

Department of Pharmacology, Faculty of Medicine in Hradec Králové, Charles University, Hradec Králové, Czech Republic.

Cardiovascular diseases are a leading cause of morbidity and mortality in most developed countries of the world. Pharmaceuticals, illicit drugs, and toxins can significantly contribute to the overall cardiovascular burden and thus deserve attention. The present article is a systematic overview of drugs that may induce distinct cardiovascular toxicity. Read More

Toxicol Appl Pharmacol 2018 01 13;339:161-171. Epub 2017 Dec 13.

Environmental Public Health Division, National Health and Environmental Effects Research Laboratory, U.S. Environmental Protection Agency, Research Triangle Park, NC, United States. Electronic address:

Recent studies showed that the circulating stress hormones, epinephrine and corticosterone/cortisol, are involved in mediating ozone-induced pulmonary effects through the activation of the sympathetic-adrenal-medullary (SAM) and hypothalamus-pituitary-adrenal (HPA) axes. Hence, we examined the role of adrenergic and glucocorticoid receptor inhibition in ozone-induced pulmonary injury and inflammation. Male 12-week old Wistar-Kyoto rats were pretreated daily for 7days with propranolol (PROP; a non-selective β adrenergic receptor [AR] antagonist, 10mg/kg, i. Read More

Clin Hypertens 2017 30;23:25. Epub 2017 Nov 30.

Department of Internal Medicine, University of Florida College of Medicine, 4th Fl. LRC Building, 653 W 8th St, Jacksonville, Fl 32209 USA.

Background: Carvedilol is used in the management of hypertension, ischemic heart disease, heart failure and most recently, portal hypertension. It has been associated with improved outcomes regarding variceal bleeding, hepatic decompensation and death when compared to propranolol and endoscopic band ligation. The main cause of portal hypertension is cirrhosis and therefore carvedilol is increasingly used in these patients. Read More

Biomed Res Int 2017 24;2017:4754701. Epub 2017 Oct 24.

Department of Neurology and Pediatric Neurology, Iuliu Haţieganu University of Medicine and Pharmacy Cluj-Napoca, Victor Babeş Str., No. 43, 400012 Cluj-Napoca, Romania.

Objective: Our study aimed to investigate the analgesic and antioxidative stress effects of Curcumin (CC) in experimental migraine induced by Nitroglycerin (NTG) on rats, compared with Indomethacin (ID) and Propranolol (PP) treatments.

Material And Methods: Five groups of 10 rats treated i.p. Read More

Curr Drug Abuse Rev 2017 ;10(1):25-30

Department of Health Science, School of Medicine, University of Catanzaro, Clinical Pharmacology and Pharmacovigilance Unit, Mater Domini Hospital Catanzaro, Catanzaro, Italy.

Background: Drug-Drug Interactions (DDIs) represent a common problem in clinical practice during drug treatments. DDIs can both induce the development of adverse drug reactions or reduce the clinical efficacy of each drug.

Objectives: The main objective of this review was to analyze the pharmacokinetic and pharmacodynamic DDIs in cocaine consumers, focusing the interest on their clinical implications. Read More

J Toxicol Sci 2017 ;42(6):755-761

Medical-Industrial Translational Research Center, Fukushima Medical University.

In recent years, human-induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) have been widely used to develop evaluation systems for drug cardiotoxicity, including the arrhythmia caused by QT prolongation. To accurately assess the arrhythmogenic potential of drugs, associated with QT prolongation, we developed an evaluation system using hiPS-CMs and gene expression analysis. hiPS-CMs were treated with 8 arrhythmogenic and 17 non-arrhythmogenic drugs at several concentrations for 24 hr to comprehensively analyze gene expression. Read More