Persistent Hyperinsulinemia Following High-Dose Insulin Therapy: A Case Report.
CONCLUSION: The kinetics of insulin following discontinuation of high-dose insulin therapy are largely unknown, but supraphysiologic insulin levels persist for some time following therapy; this may allow for simple discontinuation rather than titration of insulin at the end of therapy. Dextrose replacement is frequently needed; although the duration is often difficult to predict, prolonged infusions may not be necessary. PMID: 32656624 [PubMed - as supplied by publisher] (Source: Journal of Medical Toxicology)
Source: Journal of Medical Toxicology - July 11, 2020 Category: Toxicology Authors: Corcoran JN, Jacoby KJ, Olives TD, Bangh SA, Cole JB Tags: J Med Toxicol Source Type: research

Assessment of the safety of intravitreal injection of metoprolol tartrate in rabbits
ConclusionsThe intravitreal use of metoprolol at 50 and 100  µg dosages does not cause short-term retinal toxicity in rabbits. (Source: Documenta Ophthalmologica)
Source: Documenta Ophthalmologica - July 4, 2020 Category: Opthalmology Source Type: research

Effect of Naoxintong Capsules on the Activities of CYP450 and Metabolism of Metoprolol Tartrate in Rats Evaluated by Probe Cocktail and Pharmacokinetic Methods.
Authors: Ouyang H, Shen J, Huang X, Ma W, Jia Q, Yao G, Tang Z, Zhang D, Sun M, Teye Azietaku J, Hao J, Gao X, Chang Y, He J Abstract Naoxintong capsule (NXT), a prescribed Chinese medicine, has been used clinically for more than 20 years and is widely received by patients. We determined five probe drugs, namely, omeprazole (CYP2C19), midazolam (CYP3A4), phenacetin (CYP1A2), tolbutamide (CYP2C9), and dextromethorphan (CYP2D6) to study the potential influences of NXT on the activities of CYP enzymes and assessed the pharmacokinetics effect of NXT on metoprolol tartrate in rat plasma. The study showed that AUC(0-24) ...
Source: Evidence-based Complementary and Alternative Medicine - November 1, 2019 Category: Complementary Medicine Tags: Evid Based Complement Alternat Med Source Type: research

A High Throughput HPLC-MS/MS Method for Antihypertensive Drugs Determination in Plasma and Its Application on Pharmacokinetic Interaction Study with Shuxuetong Injection in Rats.
Abstract A high-throughput HPLC-MS/MS method was developed and validated for the determination of four antihypertensive drugs including metoprolol tartrate, hydrochlorothiazide, nifedipine, and valsartan in rat plasma. The Sprague-Dawley rats were randomly divided into three groups: A Group: gastric-administration of metoprolol tartrate, hydrochlorothiazide, nifedipine, or valsartan; B Group: a single intravenous injection of SXT, then dosing as the A group; C Group: daily injection of SXT through the tail vein for 8 consecutive days and dosing as the A group on the eighth day. For metoprolol tartrate and valsarta...
Source: Biomed Res - September 1, 2019 Category: Research Authors: Wei J, Ma W, Yao G, Jia Q, Cheng X, Ouyang H, Chang Y, Chen X, He J Tags: Biomed Res Int Source Type: research

Quantitative analysis of 3-isopropylamino-1,2-propanediol as a degradation product of metoprolol in pharmaceutical dosage forms by HILIC-CAD
Publication date: Available online 28 August 2019Source: Journal of Pharmaceutical AnalysisAuthor(s): Qun Xu, Shane TanAbstractAryloxypropanolamine is an essential structural scaffold for a variety of β-adrenergic receptor antagonists such as metoprolol. Molecules with such a structural motif tend to degrade into α, β–hydroxypropanolamine impurities via a radical–initiated oxidation pathway. These impurities are typically polar and nonchromophoric, and are thus often overlooked using traditional reversed phase chromatography and UV detection. In this work, stress testing of metoprolol confirmed ...
Source: Journal of Pharmaceutical Analysis - August 29, 2019 Category: Drugs & Pharmacology Source Type: research

Pore size effect on adsorption and release of metoprolol tartrate in mesoporous silica: Experimental and molecular simulation studies
In this study, two MCF-26 type MSNs were prepared with pore size of 11 or 15 nm, and used to conduct MPT release in comparison with MCM-41 and SBA-15. Both molecular simulation and MPT release experiments were performed to identify the pore size effect on adsorption and diffusion (release) of MPT in these MSNs. Finally, a kind of pH-sensitive MPT drug delivery system was obtained by coating the chosen MCF-26@MPT with an enteric polymer, which might find promising application in treating morning hypertension attack by orally administrating the drug delivery system before bedtime. (Source: Materials Science and Engineering: C)
Source: Materials Science and Engineering: C - March 23, 2019 Category: Materials Science Source Type: research

Advancing USP compendial methods for fixed dose combinations: a case study of metoprolol tartrate and hydrochlorothiazide tablets
Publication date: Available online 28 December 2018Source: Journal of Pharmaceutical AnalysisAuthor(s): Qun XuAbstractThe current United States Pharmacopeia–National Formulary (USP–NF) includes more than 250 monographs of fixed dose combinations (FDCs), and some of them need to be updated due to incompleteness of impurity profiles and obsolescence of analytical methodologies. A case study of metoprolol tartrate and hydrochlorothiazide tablets is presented to summarize challenges encountered during the USP monograph modernization initiative of FDCs and to highlight an “adoption and adaptation” approa...
Source: Journal of Pharmaceutical Analysis - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Detection of potential look-alike/sound-alike medication errors using Veterans Affairs administrative databases.
CONCLUSION: Through the use of administrative databases, potential LASA errors that could be reviewed for an actual error via chart review were identified. While a high rate of potential LASA errors was detected, the number of actual errors identified was low. PMID: 30257842 [PubMed - in process] (Source: American Journal of Health-System Pharmacy : AJHP)
Source: American Journal of Health-System Pharmacy : AJHP - September 29, 2018 Category: Drugs & Pharmacology Authors: Zacher JM, Cunningham FE, Zhao X, Burk ML, Moore VR, Good CB, Glassman PA, Aspinall SL Tags: Am J Health Syst Pharm Source Type: research

Impact of blend properties on die filling during tableting
Publication date: Available online 11 August 2018Source: International Journal of PharmaceuticsAuthor(s): B. Van Snick, W. Grymonpré, J. Dhondt, K. Pandelaere, G. Di Pretoro, J.P. Remon, T. De Beer, C. Vervaet, V. VanhoorneAbstractBased on characterization of a wide range of fillers and APIs, thirty divergent blends were composed and subsequently compressed on a rotary tablet press, varying paddle speed and turret speed. The tablet weight variability was determined of 20 grab samples consisting of each 20 tablets. Additionally, the bulk residence time, ejection force, pre-compression displacement, main compression f...
Source: International Journal of Pharmaceutics - August 12, 2018 Category: Drugs & Pharmacology Source Type: research

Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice.
Authors: Bialy LP, Wojcik C, Mlynarczuk-Bialy I Abstract Patients who are unable to receive oral medication (p.o.) are a major problem in outpatient settings, especially in home health care systems. Mucosal administration of drugs offers an alternative to the oral route, especially when the parenteral mode cannot be used. There are three main pathways of mucosal administration: sublingual/buccal, intranasal and rectal. We discuss the possibility of mucosal delivery of antihypertensive drugs. Perindopril arginine and Amlodipine besylate are registered in the EU as orodispersible tablets for oromucosal delivery, howe...
Source: Biomedical Papers of the Medical Faculty of the Univ Palacky Olomouc Czech Repub - May 18, 2018 Category: Biomedical Science Tags: Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub Source Type: research

A case report of apical aneurysms and myocardial perfusion deficit with myocardial necrosis due to hypertrophic cardiomyopathy
We present a relatively rare case of HCM patients with apical aneurysms, accompaning by myocardial necrosis markers increased due to ventricular muscle stress increases, rather than obstructive coronary artery disease. Interventions: The patient was prescribed aspirin, metoprolol tartrate, perindopril, and atorvastatin and was strongly advised to quit cigarettes and reduce weight. Outcomes: Follow-up at half a year turned out well. Lessons: LGE with a notable progression by ECG and SPECT along with an increase in myocardial necrosis markers in HCM patients with apical aneurysms, as was noted in the present case, i...
Source: Medicine - May 1, 2018 Category: Internal Medicine Tags: Research Article: Clinical Case Report Source Type: research

In Vitro Assessment of Nasal Insufflation of Comminuted Drug Products Designed as Abuse Deterrent Using the Vertical Diffusion Cell.
In this study, a vertical diffusion cell (VDC) was used to evaluate polyethylene oxide (PEO)-based tablets manipulated by three different forces. The commercially available products Oxycontin®, an ADF, Opana®, and metoprolol tartrate tablet formulations made in our laboratory were studied. Particle size distribution and percent recovery of manipulated tablets were measured. Grinding produced the lowest recovery and the smallest particle size distribution. Drug release was examined using a VDC by placing the dry comminuted particles on an enclosed wetted cellulose membrane. Dispensing dry particles on a VDC is atypi...
Source: AAPS PharmSciTech - March 26, 2018 Category: Drugs & Pharmacology Authors: Boyce H, Smith D, Byrn S, Saluja B, Qu W, Gurvich VJ, Hoag SW Tags: AAPS PharmSciTech Source Type: research

When drugs plasticize film coatings: Unusual formulation effects observed with metoprolol and Eudragit RS
Publication date: 25 March 2018 Source:International Journal of Pharmaceutics, Volume 539, Issues 1–2 Author(s): Youness Karrout, Florence Siepmann, Youcef Benzine, Laurent Paccou, Yannick Guinet, Alain Hedoux, Juergen Siepmann Metoprolol tartrate and metoprolol free base loaded pellet starter cores were coated with Eudragit RS, plasticized with 25% triethyl citrate (TEC). The initial drug loading and coating level were varied from 10 to 40 and 0 to 20%, respectively. Drug release was measured in 0.1 N HCl and phosphate buffer pH 7.4. The water uptake and swelling kinetics, mechanical properties and TEC leaching o...
Source: International Journal of Pharmaceutics - February 27, 2018 Category: Drugs & Pharmacology Source Type: research

The impact of the injection mold temperature upon polymer crystallization and resulting drug release from immediate and sustained release tablets
Publication date: 25 April 2018 Source:International Journal of Pharmaceutics, Volume 541, Issues 1–2 Author(s): Jeroen Van Renterghem, Heleen Dhondt, Glenn Verstraete, Michiel De Bruyne, Chris Vervaet, Thomas De Beer It was the aim of this study to elucidate the impact of the injection mold temperature upon the polymer crystallinity, its microstructure and the resulting drug release from immediate and sustained release tablets containing semi-crystalline polymers. The immediate release formulation contained 20% (w/w) ketoprofen (KETO) in poly (ethylene oxide) (PEO) and the sustained release formulation contained 20...
Source: International Journal of Pharmaceutics - February 24, 2018 Category: Drugs & Pharmacology Source Type: research

Hyponatremia induced by hyperinsulinemia-euglycemia therapy.
CONCLUSION: A woman who overdosed on amlodipine, metoprolol tartrate, and isosorbide mononitrate was treated with HIE therapy and developed symptomatic hyponatremia. Hyponatremia resolved after administration of dextrose with sodium bicarbonate infusion and 3% sodium chloride infusion and cessation of HIE therapy. PMID: 28687552 [PubMed - in process] (Source: American Journal of Health-System Pharmacy : AJHP)
Source: American Journal of Health-System Pharmacy : AJHP - July 10, 2017 Category: Drugs & Pharmacology Authors: Beavers JR, Stollings JL, Rice TW Tags: Am J Health Syst Pharm Source Type: research

Preparation and evaluation of metoprolol tartrate sustained-release pellets using hot melt extrusion combined with hot melt coating.
The objective of this study was to prepare and evaluate metoprolol tartrate sustained-release pellets. Cores were prepared by hot melt extrusion and coated pellets were prepared by hot melt coating. Cores were found to exist in a single-phase state and drug in amorphous form. Plasticizers had a significant effect on torque and drug content, while release modifiers and coating level significantly affected the drug release behavior. The mechanisms of drug release from cores and coated pellets were Fickian diffusion and diffusion-erosion, respectively. The coated pellets exhibited sustained-release properties in vitro and in ...
Source: Drug Development and Industrial Pharmacy - January 29, 2017 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Efficiency of La-doped TiO2 calcined at different temperatures in photocatalytic degradation of β-blockers
Publication date: Available online 17 January 2017 Source:Arabian Journal of Chemistry Author(s): Sanja J. Armaković, Mirjana Grujić-Brojčin, Maja Šćepanović, Stevan Armaković, Aleksandar Golubović, Biljana Babić, Biljana F. Abramović Photocatalytic activity of titania–based photocatalysts doped with 1% La have been tested in UVA radiation-induced degradation of two β-blockers – metoprolol tartrate (MET) and propranolol hydrochloride (PRO). Photocatalysts have been synthesized by sol–gel process followed by calcination at various temperatures in the range of 450−750 °C. The...
Source: Arabian Journal of Chemistry - January 17, 2017 Category: Chemistry Source Type: research

Older adults with heart failure treated with carvedilol, bisoprolol, or metoprolol tartrate: risk of mortality
ConclusionsOur evidence suggests no differential effect of β‐blockers on all‐cause mortality among older adults with HF. Copyright © 2016 John Wiley & Sons, Ltd. (Source: Pharmacoepidemiology and Drug Safety)
Source: Pharmacoepidemiology and Drug Safety - November 16, 2016 Category: Drugs & Pharmacology Authors: Sylvie Perreault, Simon Denus, Michel White, Brian White ‐Guay, Michel Bouvier, Marc Dorais, Marie‐Pierre Dubé, Jean‐Lucien Rouleau, Jean‐Claude Tardif, Sarah Jenna, Benjamin Haibe‐Kains, Richard Leduc, Denis Deblois Tags: Original Report Source Type: research

Stearic acid and high molecular weight PEO as matrix for the highly water soluble metoprolol tartrate in continuous twin-screw melt granulation
This study aims to investigate the continuous twin screw melt granulation technique to study the impact of a SA/PEO matrix on the dissolution rate of a highly water soluble drug (MPT). Decreasing the SA/PEO ratio improved the release-sustaining properties of the matrix. The solid state of the granules was characterized using differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), X-ray diffraction (XRD), Raman spectroscopy, Fourier transform infrared (FTIR) and near infrared chemical imaging (NIR-CI) in order to understand the dissolution behavior. The results revealed a preferential interaction of the M...
Source: International Journal of Pharmaceutics - August 30, 2016 Category: Drugs & Pharmacology Source Type: research

Improving performance of an accountable care organization on a quality measure assessing β-blocker use in systolic heart failure.
CONCLUSION: The performance on a Medicare Pioneer ACO quality measure evaluating β-blocker use in systolic heart failure improved in a one-year period after a clinical pharmacist-generated initiative was implemented at Atrius Health practice sites. PMID: 27543597 [PubMed - as supplied by publisher] (Source: American Journal of Health-System Pharmacy : AJHP)
Source: American Journal of Health-System Pharmacy : AJHP - August 22, 2016 Category: Drugs & Pharmacology Authors: Elman S, Zaiken K Tags: Am J Health Syst Pharm Source Type: research

Continuous melt granulation: Influence of process and formulation parameters upon granule and tablet properties.
Abstract The pharmaceutical industry has a growing interest in alternative manufacturing models allowing automation and continuous production in order to improve process efficiency and reduce costs. Implementing a switch from batch to continuous processing requires fundamental process understanding and the implementation of quality-by-design (QbD) principles. The aim of this study was to examine the relationship between formulation-parameters (type binder, binder concentration, drug-binder miscibility), process-parameters (screw speed, powder feed rate and granulation temperature), granule properties (size, size d...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 20, 2016 Category: Drugs & Pharmacology Authors: Monteyne T, Vancoillie J, Remon JP, Vervaet C, De Beer T Tags: Eur J Pharm Biopharm Source Type: research

Hybrid nanoadsorbents for the magnetically assisted removal of metoprolol from water
Publication date: 15 October 2016 Source:Chemical Engineering Journal, Volume 302 Author(s): Sofia F. Soares, Tânia R. Simões, Maria António, Tito Trindade, Ana L. Daniel-da-Silva Metoprolol (MTP) is known as one of the most frequently detected beta blockers in surface waters, with potentially harmful impact on environment and human health due to its widespread use and resistance to hydrolysis. The removal of MTP in wastewater treatment plants is still very low due to fairly ineffective conventional water treatment procedures and, therefore, more efficient treatments are needed. To tackle this ch...
Source: Chemical Engineering Journal - May 31, 2016 Category: Chemistry Source Type: research

Synchronous delivery of felodipine and metoprolol tartrate using monolithic osmotic pump technology.
Authors: Zhao S, Yu F, Liu N, Di Z, Yan K, Liu Y, Li Y, Zhang H, Yang Y, Yang Z, Li Z, Mei X Abstract The synchronous sustained-release of two drugs was desired urgently for patients needing combination therapy in long term. However, sophisticated technologies were used generally to realize the simultaneous delivery of two drugs especially those with different physico-chemical properties. The purpose of this study was to obtain the concurrent release of felodipine and metoprolol tartrate, two drugs with completely different solubilities, in a simple monolithic osmotic pump system (FMOP). Two types of blocking agent...
Source: Drug Development and Industrial Pharmacy - April 16, 2016 Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

Development of a controlled release formulation by continuous twin screw granulation: Influence of process and formulation parameters
Publication date: 30 May 2016 Source:International Journal of Pharmaceutics, Volume 505, Issues 1–2 Author(s): V. Vanhoorne, B. Vanbillemont, J. Vercruysse, F. De Leersnyder, P. Gomes, T. De Beer, J.P. Remon, C. Vervaet The aim of this study was to evaluate the potential of twin screw granulation for the continuous production of controlled release formulations with hydroxypropylmethylcellulose as hydrophilic matrix former. Metoprolol tartrate was included in the formulation as very water soluble model drug. A premix of metoprolol tartrate, hydroxypropylmethylcellulose and filler (ratio 20/20/60, w/w) was gr...
Source: International Journal of Pharmaceutics - April 6, 2016 Category: Drugs & Pharmacology Source Type: research

Comparison of metoprolol tartrate multiple-unit lipid matrix systems produced by different technologies.
t C, Dreu R Abstract The aim of this study was to develop, evaluate and compare extended release mini-matrices based on metoprolol tartrate (MPT) and either glyceryl behenate (GB) or glyceryl palmitostearate (GPS). Mini-matrices were produced by three different techniques: hot melt extrusion, compression of melt granulates and prilling. Hot-melt extrusion and compression of granules obtained from melted material proved to be reliable, robust and reproducible techniques with aim of obtaining extended release matrices. Prilling tended to be susceptible to increased melt viscosity. Direct compression was not applicab...
Source: European Journal of Pharmaceutical Sciences - March 12, 2016 Category: Drugs & Pharmacology Authors: Aleksovski A, Van Bockstal PJ, Roškar R, Sovány T, Regdon G, De Beer T, Vervaet C, Dreu R Tags: Eur J Pharm Sci Source Type: research

Investigation into the Effect of Ethylcellulose Viscosity Variation on the Drug Release of Metoprolol Tartrate and Acetaminophen Extended Release Multiparticulates-Part I.
Abstract Ethylcellulose is one of the most commonly used polymers to develop reservoir type extended release multiparticulate dosage forms. For multiparticulate extended release dosage forms, the drug release is typically governed by the properties of the barrier membrane coating. The ICH Pharmaceutical Development Guideline (ICH Q8) requires an understanding of the influence of critical material attributes and critical process parameters on the drug release of a pharmaceutical product. Using this understanding, it is possible to develop robust formulations with consistent drug release characteristics. Critical ma...
Source: AAPS PharmSciTech - January 7, 2016 Category: Drugs & Pharmacology Authors: Mehta R, Teckoe J, Schoener C, Workentine S, Ferrizzi D, Rajabi-Siahboomi A Tags: AAPS PharmSciTech Source Type: research

Similar but Different: The Case of Metoprolol Tartrate and Succinate Salts
Crystal Growth & DesignDOI: 10.1021/acs.cgd.5b01383 (Source: Crystal Growth and Design)
Source: Crystal Growth and Design - January 4, 2016 Category: Chemistry Authors: Paola Paoli, Patrizia Rossi, Eleonora Macedi, Andrea Ienco, Laura Chelazzi, Gian Luca Bartolucci and Bruno Bruni Source Type: research

Discharge Heart Rate and β-Blocker Dose in Patients Hospitalized With Heart Failure: Findings From the OPTIMIZE-HF Registry
Conclusions Despite treatment with β-blockers, a substantial proportion of patients hospitalized with heart failure with reduced ejection fraction have elevated heart rate at discharge. (Source: American Heart Journal)
Source: American Heart Journal - December 22, 2015 Category: Cardiology Source Type: research

Swallowing‐induced atrial tachycardia: case report
Key Clinical Message A 53‐year‐old man presented with heart palpitations while swallowing. Electrophysiologic study (EPS) and immunohistochemical results of his esophageal leiomyoma suggested that swallowing‐induced atrial tachycardia is related with neural reflex. S100‐immunopositive nerve fibers are demonstrated sympathetic nerves which possibly explain the mechanism. Metoprolol tartrate tablets are effective in our patient. A 53‐year‐old man presented with heart palpitations while swallowing. EPS and immunohistochemical results of his esophageal leiomyoma suggested that swallowing‐induced atrial tachycard...
Source: Clinical Case Reports - December 6, 2015 Category: Journals (General) Authors: Ye Xu, Kuan Cheng, Wenqing Zhu Tags: Case Report Source Type: research

Tapioca starch blended alginate mucoadhesive-floating beads for intragastric delivery of Metoprolol Tartrate.
The objective of the study was to develop tapioca starch blended alginate mucoadhesive-floating beads for the intragastric delivery of Metoprolol Tartrate (MT). The beads were prepared by ionotropic gelation method using calcium chloride as crosslinker and gas forming calcium carbonate (CaCO3) as floating inducer. The alginate gel beads having 51-58% entrapped MT showed 90% release within 45min in gastric medium (pH 1.2). Tapioca starch blending markedly improved the entrapment efficiency (88%) and sustained the release for 3-4h. A 12% w/w HPMC coating on these beads extended the release upto 9-11h. In vitro wash off and b...
Source: International Journal of Biological Macromolecules - November 16, 2015 Category: Biochemistry Authors: Biswas N, Sahoo RK Tags: Int J Biol Macromol Source Type: research

Development and validation of a hydrophilic interaction chromatography method coupled with a charged aerosol detector for quantitative analysis of nonchromophoric α–hydroxyamines, organic impurities of metoprolol
Publication date: 25 January 2016 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 118 Author(s): Qun Xu, Shane Tan, Katya Petrova The European Pharmacopeia (EP) metoprolol impurities M and N are polar, nonchromophoric α-hydroxyamines, which are poorly retained in a conventional reversed-phase chromatographic system and are invisible for UV detection. Impurities M and N are currently analyzed by TLC methods in the EP as specified impurities and in the United States Pharmacopeia–National Formulary (USP–NF) as unspecified impurities. In order to modernize the USP monographs of metoprolo...
Source: Journal of Pharmaceutical and Biomedical Analysis - November 14, 2015 Category: Drugs & Pharmacology Source Type: research

Association of Treatment with Carvedilol, Bisoprolol and Metoprolol on the Risk of Mortality and Hospital Admission Among Older Adults with Heart Failure
The objective of this study is to compare the effectiveness of ß-blockers for patients with HF in a clinical practice. (Source: Value in Health)
Source: Value in Health - October 23, 2015 Category: Global & Universal Authors: S Perreault, S de Denus, M White, B White-Guay, M Bouvier, M Dorais, M Dubé, J Rouleau, J Tardif, S Jenna, B Haibe-Kains, R Leduc, D Deblois Source Type: research

Visualizing Compound Distribution during Zebrafish Embryo Development: The Effects of Lipophilicity and DMSO
The predictability of the zebrafish embryo model is highly influenced by internal exposure of the embryo/larva. As compound uptake is likely to be influenced by factors such as lipophilicity, solvent use, and chorion presence, this article focuses on investigating their effects on compound distribution within the zebrafish embryo. To visualize compound uptake and distribution, zebrafish embryos were exposed for 96 hr, starting at 4 hr postfertilization, to water‐soluble dyes: Schiff's reagent (logP –4.63), Giemsa stain (logP –0.77), Van Gierson stain (logP 1.64), Cresyl fast violet (logP 3...
Source: Birth Defects Research Part B: Developmental and Reproductive Toxicology - October 1, 2015 Category: Perinatology & Neonatology Authors: Coco Koning, Manon Beekhuijzen, Marysia Tobor‐Kapłon, Selinda Vries‐Buitenweg, Dick Schoutsen, Nico Leeijen, Beppy Waart, Harry Emmen Tags: Research Article Source Type: research

Fatty acids for controlled release applications: a comparison between prilling and solid lipid extrusion as manufacturing techniques.
Abstract The aim of the present study was to evaluate the solid state characteristics, drug release and stability of fatty acid-based formulations after processing via prilling and solid lipid extrusion. Myristic acid (MA), stearic acid (SA) and behenic acid (BA) were used as matrix formers combined with metoprolol tartrate (MPT) as model drug. The prilling process allowed complete dissolution of MPT in the molten fatty acid phase, generating semi-crystalline MPT and the formation of hydrogen bonds between drug and fatty acids in the solid prills. In contrast, as solid lipid extrusion (SLE) induced only limited me...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 28, 2015 Category: Drugs & Pharmacology Authors: Vervaeck A, Monteyne T, Siepmann F, Boone MN, Van Hoorebeke L, De Beer T, Siepmann J, Remon JP, Vervaet C Tags: Eur J Pharm Biopharm Source Type: research

Carvedilol Compared With Metoprolol Succinate in the Treatment and Prognosis of Patients With Stable Chronic Heart Failure: Carvedilol or Metoprolol Evaluation Study [Original Articles]
Background— β-Blockers exert a prognostic benefit in the treatment of chronic heart failure. Their pharmacological properties vary. The only substantial comparative trial to date—the Carvedilol or Metoprolol European Trial—has compared carvedilol with short-acting metoprolol tartrate at different dose equivalents. We therefore addressed the relative efficacy of equal doses of carvedilol and metoprolol succinate on survival in multicenter hospital outpatients with chronic heart failure. Methods and Results— Four thousand sixteen patients with stable systolic chronic heart failure who were using...
Source: Circulation: Heart Failure - September 15, 2015 Category: Cardiology Authors: Frohlich, H., Zhao, J., Tager, T., Cebola, R., Schellberg, D., Katus, H. A., Grundtvig, M., Hole, T., Atar, D., Agewall, S., Frankenstein, L. Tags: Congestive, Cardiovascular Pharmacology Original Articles Source Type: research

Identification, synthesis, isolation and characterization of new impurity in metoprolol tartrate tablets
Publication date: 5 January 2016 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 117 Author(s): R. Buchi Reddy, Kishor R. More, Leena Gupta, Mukesh S. Jha, Laki Magar A new unknown impurity was observed in accelerated stability studies of Metoprolol tartrate tablets. This impurity has been identified, synthesized and characterized through different spectral studies and confirmed as an adduct of lactose and Metoprolol formed by Maillard reaction. Graphical abstract (Source: Journal of Pharmaceutical and Biomedical Analysis)
Source: Journal of Pharmaceutical and Biomedical Analysis - September 6, 2015 Category: Drugs & Pharmacology Source Type: research

Calendering as a direct shaping tool for the continuous production of fixed-dose combination products via co-extrusion.
In this study calendering is used as a downstream technique to shape monolithic co-extruded fixed-dose combination products in a continuous way. Co-extrudates with a metoprolol tartrate-loaded sustained-release core and a hydrochlorothiazide-loaded immediate-release coat were produced and immediately shaped into a monolithic drug delivery system via calendering, using chilled rolls with tablet-shaped cavities. In vitro metoprolol tartrate release from the ethylcellulose core of the calendered tablets was prolonged in comparison to the sustained release of a multiparticulate dosage form, prepared manually by cutting co-extr...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 29, 2015 Category: Drugs & Pharmacology Authors: Vynckier AK, Lin H, Zeitler JA, Willart JF, Bongaers E, Voorspoels J, Remon JP, Vervaet C Tags: Eur J Pharm Biopharm Source Type: research

Drug disposition and modelling before and after gastric bypass: immediate and controlled‐release metoprolol formulations
ConclusionsThe disposition of metoprolol from an immediate‐release and a controlled‐release formulation was not significantly altered after RYGB; there was a tendency to an increase, which was also predicted by PBPK modelling and simulation. (Source: British Journal of Clinical Pharmacology)
Source: British Journal of Clinical Pharmacology - July 6, 2015 Category: Drugs & Pharmacology Authors: Ina Gesquiere, Adam S. Darwich, Bart Van der Schueren, Jan Hoon, Matthias Lannoo, Christophe Matthys, Amin Rostami, Veerle Foulon, Patrick Augustijns Tags: Pharmacokinetics Source Type: research

Development of hollow/porous floating beads of metoprolol for pulsatile drug delivery
Abstract The purpose of this work was to develop hollow calcium pectinate beads for floating pulsatile release of metoprolol tartrate intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic cross-linking using low methoxy pectin, xanthan gum, sodium carboxy methyl cellulose, guar gum, locust bean, gellan gum and calcium chloride as a cros...
Source: European Journal of Drug Metabolism and Pharmacokinetics - May 10, 2015 Category: Drugs & Pharmacology Source Type: research

Preparation and evaluation of monodispersed, submicron, non‐porous silica particles functionalized with β‐CD derivatives for chiral‐pressurized capillary electrochromatography
This article is protected by copyright. All rights reserved (Source: Electrophoresis)
Source: Electrophoresis - May 1, 2015 Category: Biochemistry Authors: Lu Yangfang, Wang Hui, Xue Yun, Gu Xue, Wang Yan, Yan Chao Tags: Research Paper Source Type: research

Drug disposition and modelling before and after gastric bypass: immediate and controlled release metoprolol formulations
CONCLUSIONSThe disposition of metoprolol from an immediate release formulation and a controlled release formulation was not significantly altered after RYGB; there was a tendency to an increase, which was also predicted by PBPK modelling and simulation. This article is protected by copyright. All rights reserved. (Source: British Journal of Clinical Pharmacology)
Source: British Journal of Clinical Pharmacology - April 28, 2015 Category: Drugs & Pharmacology Authors: Ina Gesquiere, Adam S. Darwich, Bart Van der Schueren, Jan Hoon, Matthias Lannoo, Christophe Matthys, Amin Rostami, Veerle Foulon, Patrick Augustijns Tags: Pharmacokinetics Source Type: research

Successful Treatment of a Massive Metoprolol Overdose Using Intravenous Lipid Emulsion and Hyperinsulinemia/Euglycemia Therapy
We describe the case of a 59‐year‐old man who intentionally ingested ~7.5 g of metoprolol tartrate. Initial treatment of bradycardia and hypotension included glucagon, atropine, dopamine, and norepinephrine. Despite these treatment modalities, the patient developed cardiac arrest. Intravenous lipid emulsion (ILE) and hyperinsulinemia/euglycemia (HIE) therapies were initiated during advanced cardiac life support and were immediately followed by return of spontaneous circulation. Further treatment included gastric lavage, activated charcoal, continued vasopressor therapy, and a repeat bolus of ILE. The patient was w...
Source: Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy - April 22, 2015 Category: Drugs & Pharmacology Authors: Cassie A. Barton, Nathan B. Johnson, Nathan D. Mah, Gillian Beauchamp, Robert Hendrickson Tags: Case Report Source Type: research

Meta-analysis of the effects of Carvedilol vs Metoprolol on All-cause Mortality and Hospitalizations in Patients with Heart Failure
Long-term treatment with appropriate doses of carvedilol or metoprolol is currently recommended for patients with Heart Failure with reduced Ejection Fraction (HFrEF) to decrease the risk of death, hospitalizations and patients’ symptoms. It remains unclear if the b-blockers used in HFrEF patients are equal or carvedilol is superior to metoprolol types. We performed a meta-analysis of the comparative effects of carvedilol vs metoprolol tartrate and succinate on all-cause mortality or/and hospitalization. (Source: The American Journal of Cardiology)
Source: The American Journal of Cardiology - January 31, 2015 Category: Cardiology Authors: Alexandros Briasoulis, Mohan Palla, Luis Afonso Source Type: research

Meta-Analysis of the Effects of Carvedilol Versus Metoprolol on All-Cause Mortality and Hospitalizations in Patients With Heart Failure
Long-term treatment with appropriate doses of carvedilol or metoprolol is currently recommended for patients with heart failure with reduced ejection fraction (HFrEF) to decrease the risk of death, hospitalizations, and patients' symptoms. It remains unclear if the β blockers used in patients with HFrEF are equal or carvedilol is superior to metoprolol types. We performed a meta-analysis of the comparative effects of carvedilol versus metoprolol tartrate and succinate on all-cause mortality and/or hospitalization. (Source: The American Journal of Cardiology)
Source: The American Journal of Cardiology - January 31, 2015 Category: Cardiology Authors: Alexandros Briasoulis, Mohan Palla, Luis Afonso Tags: Heart Failure Source Type: research

Successful treatment of metoprolol-induced cardiac arrest with high-dose insulin, lipid emulsion and extracorporeal membrane oxygenation
Beta-adrenergic antagonist toxicity causes cardiovascular collapse often refractory to standard therapy. Alternative therapies include high-dose insulin, lipid emulsion and venoarterial extracorporeal membrane oxygenation (VA-ECMO).CaseA 47-year-old male ingested ten grams of metoprolol tartrate in a suicide attempt. Upon emergency department (ED) presentation, he was comatose, bradycardic and hypotensive. Glucagon (14mg IV) and vasopressor/inotropic support (epinephrine 0.1 mcg/kg/min, dobutamine 10 mcg/kg/min) were administered. (Source: The American Journal of Emergency Medicine)
Source: The American Journal of Emergency Medicine - January 16, 2015 Category: Emergency Medicine Authors: Jeremiah T. Escajeda, Ken D. Katz, Jon C. Rittenberger Tags: Case Report Source Type: research

Successful treatment of metoprolol-induced cardiac arrest with high-dose insulin, lipid emulsion, and extracorporeal membrane oxygenation
β-Adrenergic antagonist toxicity causes cardiovascular collapse often refractory to standard therapy. Alternative therapies include high-dose insulin, lipid emulsion, and venoarterial extracorporeal membrane oxygenation (VA-ECMO). A 47-year-old man ingested 10 g of metoprolol tartrate in a suicide attempt. Upon emergency department presentation, he was comatose, bradycardic, and hypotensive. Glucagon (14 mg IV) and vasopressor/inotropic support (epinephrine 0.1 μg/[kg min], dobutamine 10 μg/[kg min]) were administered. (Source: The American Journal of Emergency Medicine)
Source: The American Journal of Emergency Medicine - January 16, 2015 Category: Emergency Medicine Authors: Jeremiah T. Escajeda, Ken D. Katz, Jon C. Rittenberger Tags: Case Reports Source Type: research

Formulation and evaluation of new long acting metoprolol tartrate ophthalmic gels
Publication date: December 2014 Source:Saudi Pharmaceutical Journal, Volume 22, Issue 6 Author(s): Amal El Sayeh F. Abou el Ela , Mona Mohamed El Khatib The rationale of the present work is to formulate and evaluate metoprolol tartrate (MT), which is a beta-1 selective adrenergic blocking agent in a new ocular gel delivery system; this is our way and method to increase its contact to the cornea, giving a longer time of drug contact to the eye and slow possible release from the preparation. Metoprolol tartrate is chosen as a candidate for gel formulation because although it has been available for a few years as ophthalmic...
Source: Saudi Pharmaceutical Journal - December 27, 2014 Category: Drugs & Pharmacology Source Type: research

Kidney Function and Population-Based Outcomes of Initiating Oral Atenolol Versus Metoprolol Tartrate in Older Adults
Conclusions Contrary to our expectation, we found that atenolol versus metoprolol tartrate was associated with lower 90-day risk of mortality in patients regardless of eGFR, with no difference in risk of hospitalization with bradycardia or hypotension. (Source: American Journal of Kidney Diseases)
Source: American Journal of Kidney Diseases - November 20, 2014 Category: Urology & Nephrology Source Type: research

Thermoplastic polyurethanes for the manufacturing of highly dosed oral sustained release matrices via hot melt extrusion and injection molding.
This study evaluated thermoplastic polyurethanes (TPUR) as matrix excipients for the production of oral solid dosage forms via hot melt extrusion (HME) in combination with injection molding (IM). We demonstrated that TPURs enable the production of solid dispersions - crystalline API in a crystalline carrier - at an extrusion temperature below the drug melting temperature (Tm) with a drug content up to 65% (wt.%). The release of metoprolol tartrate was controlled over 24h, whereas a complete release of diprophylline was only possible in combination with a drug release modifier: polyethylene glycol 4000 (PEG 4000) or Tween 8...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 15, 2014 Category: Drugs & Pharmacology Authors: Claeys B, Vervaeck A, Hillewaere XK, Possemiers S, Hansen L, De Beer T, Remon JP, Vervaet C Tags: Eur J Pharm Biopharm Source Type: research

Autoantibodies against β1 Receptor and AT1 Receptor in Type 2 Diabetes Patients with Left Ventricular Dilatation
Objectives: To explore the relationship between the autoantibodies against the β1 and AT1 receptors and left ventricular dilatation in patients with type 2 diabetes (T2DM). Methods: The autoantibodies against the β1 and angiotensin II type 1 (AT1) receptors of T2DM patients with and without hypertension were screened by ELISA. Multiple logistic regression was used to analyze the risk factors for left ventricular dilatation. The reversing effect of left ventricular dilatation was evaluated after receptor blocker treatment. Results: The positive rates of autoantibodies against the β1 and AT1 receptors (43.0 an...
Source: Cardiology - November 6, 2014 Category: Cardiology Source Type: research