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Carvedilol

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https://www.readbyqxmd.com/read/28814664/pulmonary-arterial-hypertension-treatment-with-carvedilol-for-heart-failure-a-randomized-controlled-trial
#1
Samar Farha, Didem Saygin, Margaret M Park, Hoi I Cheong, Kewal Asosingh, Suzy Aa Comhair, Olivia R Stephens, Emir C Roach, Jacqueline Sharp, Kristin B Highland, Frank P DiFilippo, Donald R Neumann, W H Wilson Tang, Serpil C Erzurum
BACKGROUND: Right-sided heart failure is the leading cause of death in pulmonary arterial hypertension (PAH). Similar to left heart failure, sympathetic overactivation and β-adrenoreceptor (βAR) abnormalities are found in PAH. Based on successful therapy of left heart failure with β-blockade, the safety and benefits of the nonselective β-blocker/vasodilator carvedilol were evaluated in PAH. METHODS: PAH Treatment with Carvedilol for Heart Failure (PAHTCH) is a single-center, double-blind, randomized, controlled trial...
August 17, 2017: JCI Insight
https://www.readbyqxmd.com/read/28811301/topically-applied-carvedilol-attenuates-solar-ultraviolet-radiation-induced-skin-carcinogenesis
#2
Kevin M Huang, Sherry Liang, Steven Yeung, Etuajie Oiyemhonlan, Kristan H Cleveland, Cyrus Parsa, Robert Orlando, Frank L Meyskens, Bradley Andresen, Ying Huang
In previous studies, the β-blocker carvedilol inhibited EGF-induced epidermal cell transformation and chemical carcinogen-induced mouse skin hyperplasia. As exposure to ultraviolet (UV) radiation leads to skin cancer, the present study examined whether carvedilol can prevent UV-induced carcinogenesis. Carvedilol absorbs UV like a sunscreen; thus, to separate pharmacological from sunscreen effects, 4-hydroxycarbazole (4-OHC), which absorbs UV to the same degree as carvedilol, served as control. JB6 P+ cells, an established epidermal model for studying tumor promotion, were used for evaluating the effect of carvedilol on UV-induced neoplastic transformation...
August 15, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28811130/comparative-study-on-stabilizing-ability-of-food-protein-non-ionic-surfactant-and-anionic-surfactant-on-bcs-type-ii-drug-carvedilol-loaded-nanosuspension-physicochemical-and-pharmacokinetic-investigation
#3
Tianjiao Geng, Parikshit Banerjee, Zhangdi Lu, Abdelmoumin Zoghbi, Tiantian Li, Bo Wang
Carvedilol (CAR) in its pure state has low aqueous solubility and extremely poor bioavailability which largely limit its clinical application. The aim of the study is to improve the dissolution rate and the bioavailability of CAR via preparing nanosuspensions with different stabilizers. Antisolvent precipitation-ultrasonication technique was used here. Attempts have been made to use food protein- Whey protein isolate (WPI) as a stabilizer in CAR loaded nanosuspension and also to compare its stabilizing potential with conventional nanosuspension stabilizers such as non-ionic linear copolymer-poloxamer 188 (PLX188) and anionic surfactant-sodium dodecyl sulfate (SDS)...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28803116/efficient-molecularly-imprinted-polymer-as-a-pipette-tip-solid-phase-sorbent-for-determination-of-carvedilol-enantiomers-in-human-urine
#4
Anny Talita Maria da Silva, Hanna Leijoto de Oliveira, Camilla Fonseca Silva, Matheus Cecílio Fonseca, Thales Fernando Dias Pereira, Clebio Soares Nascimento, Eduardo Costa de Figueiredo, Keyller Bastos Borges
In this work, an efficient pipette tip based on molecularly imprinted polymers solid-phase extraction (PT-MIP-SPE) method was developed for carvedilol (CAR) analysis. This compound is available in clinical practice as a racemic mixture, in which (-)-(S)-CAR is a β- and α1-adrenergic antagonist, while (+)-(R)-CAR only acts as an α1-adrenergic antagonist. Enantioseparation of CAR presented satisfactory retention times (5.85 and 14.84min), acceptable theoretical plates (N=2048 and 2018) and good resolution (Rs=9...
August 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28760606/synthesis-analytical-characterization-and-capillary-electrophoretic-use-of-the-single-isomer-heptakis-6-o-sulfobutyl-beta-cyclodextrin
#5
Milo Malanga, Ida Fejős, Erzsébet Varga, Gábor Benkovics, András Darcsi, Julianna Szemán, Szabolcs Béni
This contribution reports the synthesis, characterization and capillary electrophoretic application of heptakis-(6-O-sulfobutyl-ether)-β-cyclodextrin sodium salt, (6-(SB)7-β-CD). The compound was obtained through a five-steps synthesis and it represents the first example of single-isomer sulfobutylated cyclodextrin that carries the negatively charged functions exclusively on its primary side and it is unmodified on the lower rim. The purity of each intermediate was determined by appropriate liquid chromatographic methods, while the isomeric purity of the final product was established by an ad-hoc developed HPLC method based on a CD-Screen-IEC column...
July 21, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28749696/the-influence-of-physiological-gastrointestinal-surfactant-ratio-on-the-equilibrium-solubility-of-bcs-class-ii-drugs-investigated-using-a-four-component-mixture-design
#6
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
The absorption of poorly water-soluble drugs is influenced by the luminal gastrointestinal fluid content and composition which controls solubility. Simulated intestinal fluids have been introduced into dissolution testing including endogenous amphiphiles and digested lipids at physiological levels; however, in vivo individual variation exists in the concentrations of these components, which will alter drug absorption through an effect on solubility. The use of a factorial design of experiment and varying media by introducing different levels of bile, lecithin and digested lipids has been previously reported, but here we investigate the solubility variation of poorly-soluble drugs through more complex biorelevant amphiphile interactions...
July 27, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28748731/long-term-management-of-distinct-facial-flushing-and-persistent-erythema-of-rosacea-by-treatment-with-carvedilol
#7
Katharina Pietschke, Martin Schaller
BACKGROUND: The treatment of persistent erythema and flushing episodes in patients with rosacea remains a clinical challenge. A possible therapeutic option could be given be the use of antihypertensive drugs. OBJECTIVES: We therefore evaluated the effect of the non-selective β-blocker carvedilol in five caucasian patients. METHODS: In a monocentric, retrospective case study the patients were treated with carvedilol titrated up to 12.5 mg twice a day over at least six months...
July 27, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/28733066/effective-use-of-levosimendan-in-anthracycline-induced-cardiomyopathy-a-case-report
#8
Nikolaos Miaris, Stefanos Zezas, Joseph Sgouros, Dimitra-Christina Zirou, Stefania Gkoura, George Stamoulis, Helen Angelopoulou, George Avgeropoulos, Epaminondas Samantas
BACKGROUND: Anthracycline-induced cardiomyopathy is a serious side effect that ranges from mild left ventricular systolic impairment to congestive heart failure and cardiogenic shock. Currently, there is no evidence indicating the effective use of levosimendan in these cases. OBJECTIVE: We aim to present a case of life-threatening doxorubicin-induced cardiomyopathy that was successfully managed with levosimendan. CASE: A 48-year-old female with formerly normal heart function, who had been treated with doxorubicin-based regimens for dedifferentiated chondrosarcoma, presented with cardiomyopathy with low left ventricular ejection fraction eight months after the last infusion...
July 18, 2017: Heart & Lung: the Journal of Critical Care
https://www.readbyqxmd.com/read/28732927/ultrasound-promoted-dispersive-micro-solid-phase-extraction-of-trace-anti-hypertensive-drugs-from-biological-matrices-using-a-sonochemically-synthesized-conductive-polymer-nanocomposite
#9
Maryam Hemmati, Maryam Rajabi, Alireza Asghari
In this work, a rapid and efficient procedure named ultrasound meliorated dispersive micro solid-phase extraction followed by high performance liquid chromatography-ultra violet detection (US-D-μSPE-HPLC-UV) was developed for the pre-concentration of the main trace anti-hypertensive drugs in complex matrices. The basis of this procedure was a polypyrrole-sodium dodecylbenzenesulfonate/zinc oxide (PPy-DBSNa/ZnO) nanocomposite. It was readily synthesized by the impressive way of in situ sonochemical oxidative polymerization in the presence of some additives such as FeCl3 and DBSNa, ultimately leading to the effective coating of PPy on the ZnO nanoparticle cores...
November 2017: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/28732286/development-of-liquid-chromatographic-methods-for-enantioseparation-and-sensitive-detection-of-%C3%AE-adrenolytics-%C3%AE-2-agonists-in-human-plasma-using-a-single-enantiomer-reagent
#10
Poonam Malik, Ravi Bhushan
Enantioseparation of four commonly used β-adrenolytics (bisoprolol, salbutamol, and carvedilol, marketed as racemic mixtures) has been achieved by both TLC and RPHPLC via an indirect approach. A new chiral reagent, (S)-naproxen benzotriazole ester, was synthesized and it was characterized by UV, IR, (1)HNMR, elemental analysis and polarimetry. It was used to synthesize diastereomeric derivatives of the three β-adrenolytics under microwave irradiation. TLC separation of diastereomeric derivatives was achieved which were then isolated by preparative approach; these were characterized and were used as standard reference for determining absolute configuration of diastereomeric derivatives and for establishing validated HPLC method for enantioseparation and sensitive detection of the three β-adrenolytics in human plasma...
July 14, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28729042/effects-of-%C3%AE-blockers-on-house-dust-mite-driven-murine-models-pre-and-post-development-of-an-asthma-phenotype
#11
Radhika Joshi, Daniel Valdez, Hosu Kim, Douglas C Eikenburg, Brian J Knoll, Richard A Bond
BACKGROUND: Our previous studies suggested certain β-adrenoceptor blockers (β-blockers) attenuate the asthma phenotype in ovalbumin driven murine models of asthma. However, the ovalbumin model has been criticized for lack of clinical relevance. METHODS: We tested the non-selective β-blockers, carvedilol and nadolol, in house dust mite (HDM) driven murine asthma models where drugs were administered both pre- and post-development of the asthma phenotype. We measured inflammation, mucous metaplasia, and airway hyper-responsiveness (AHR)...
July 17, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28726655/influence-of-beta-blockers-and-ivabradine-on-long-term-prognosis-of-patients-with-stable-angina
#12
T Ilashchuk, O Glubochenko, B Senyuk, N Bachuk-Ponich, I Lukashevich
The purpose of the study was to evaluate the influence of beta-blockers and ivabradine on long-term prognosis of patients with stable angina. 90 patients with stable angina that have been involved in present study along with nitrates, antiplatelet agents and statins received bisoprolol (Group I), carvedilol (Group II) and ivabradine (Group III). We analyzed the following indicators: patient adherence to treatment, cases of myocardial infarction and circulatory decompensation, which resulted in necessity of patient's hospitalization during the year of observation, calculating the probability of achieving a key prognostic endpoint by patient using the concept of the odds ratio and determination of important components in the progression of the disease...
June 2017: Georgian Medical News
https://www.readbyqxmd.com/read/28726654/the-safety-and-efficacy-of-amiodarone-and-carvedilol-combination-in-treatment-of-patients-with-severe-cardiac-rhythm-disorders
#13
E Tsetskhladze, I Khintibidze
Different arrhythmias are cause of sudden death in many patients with heart failure. Amiodarone is usually used for prevent this arrhythmias, but it is not drug of choice for treatment the patients with heart failure. We retrospectively analyzed 142 patients with moderate and severe heart failure and history of myocardial infarction. These patients have received amiodarone, carvedilol or combination of these two medications together with standard therapy. In our retrospective analysis, the combination therapy with Amiodarone and Carvedilol had highly significant decrease arrhythmic death compare with carvedilol and amiodarone groups...
June 2017: Georgian Medical News
https://www.readbyqxmd.com/read/28720509/the-neuropeptide-galanin-promotes-an-anti-thrombotic-phenotype-on-endocardial-endothelial-cells-from-heart-failure-patients
#14
Christina Tyrrell, Amanda Toyooka, Faiza Khan, Kent L Thornburg, James O Mudd, Wohaib Hasan
Thromboembolic complications are a significant cause of mortality and re-hospitalization in heart failure (HF) patients. One source of thrombi is the ventricular endocardial surface that becomes increasingly pro-thrombotic as HF progresses. Anticoagulation comes with bleeding risks so identifying therapeutic agents for improving cardiac endothelial health are of critical clinical importance. Endocardial endothelial cells are closely apposed to cardiac sympathetic nerves. In HF, cardiac sympathetic nerves are dysregulated and promote disease progression...
September 2017: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/28718228/early-initiation-of-beta-blockers-following-primary-endoscopic-therapy-for-bleeding-oesophageal-varices-in-cirrhotics
#15
Adnan Salim, Kashif Malik, Muhammad Omer Farooq, Umair Butt, Arshad Kamal Butt, Altaf Alam
BACKGROUND AND AIMS: Beta-blockers provide secondary prophylaxis following endoscopic therapy for variceal bleeding. Guidelines recommend starting beta-blockers 6 days after endoscopy to prevent masking hemodynamic signs of re-bleeding. We aimed to see safety of earlier initiation of betablockers. METHODS: Cirrhotic patients with upper GI bleed were given intravenous vasoactive agents until undergoing endoscopy. Patients with only oesophageal varices as source of bleed were recruited...
April 2017: Journal of Ayub Medical College, Abbottabad: JAMC
https://www.readbyqxmd.com/read/28711030/carvedilol-can-attenuate-histamine-induced-paw-edema-and-formaldehyde-induced-arthritis-in-rats-without-risk-of-gastric-irritation
#16
Afaf Sayed Osman, Dina Ahmed Labib, Mahmoud M Kamel
BACKGROUND AND AIM: Rheumatoid arthritis treatment aims to control joint damage and any associated complications such as cardiovascular disease. Most anti-inflammatory drugs have a high tendency to cause gastro-intestinal irritation. The present study is designed to investigate the anti-inflammatory effect of carvedilol and to study its effect on gastric mucosa. EXPERIMENTAL APPROACH: Lornoxicam (1.3mg/kg) or carvedilol (10mg/kg) was administrated orally 1h before histamine injection into animals of a histamine-induced paw edema model and orally daily for 11days into animals of a formaldehyde-induced arthritis model...
July 12, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28698881/assessment-of-haemodynamic-response-to-nonselective-beta-blockers-in-portal-hypertension-by-phase-contrast-magnetic-resonance-angiography
#17
Natasha McDonald, David M L Lilburn, Neil J Lachlan, Gillian Macnaught, Dilip Patel, Arjun N A Jayaswal, Peter C Hayes, Scott I Semple, Jonathan A Fallowfield
A significant unmet need exists for accurate, reproducible, noninvasive diagnostic tools to assess and monitor portal hypertension (PHT). We report the first use of quantitative MRI markers for the haemodynamic assessment of nonselective beta-blockers (NSBB) in PHT. In a randomized parallel feasibility study in 22 adult patients with PHT and a clinical indication for NSBB, we acquired haemodynamic data at baseline and after 4 weeks of NSBB (propranolol or carvedilol) using phase-contrast MR angiography (PC-MRA) in selected intra-abdominal vessels...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28692870/air-assisted-liquid-liquid-microextraction-using-floating-organic-droplet-solidification-for-simultaneous-extraction-and-spectrophotometric-determination-of-some-drugs-in-biological-samples-through-chemometrics-methods
#18
Farnaz Farahmand, Bahar Ghasemzadeh, Abdolhossein Naseri
An air assisted liquid-liquid microextraction by applying the solidification of a floating organic droplet method (AALLME-SFOD) coupled with a multivariate calibration method, namely partial least squares (PLS), was introduced for the fast and easy determination of Atenolol (ATE), Propanolol (PRO) and Carvedilol (CAR) in biological samples via a spectrophotometric approach. The analytes would be extracted from neutral aqueous solution into 1-dodecanol as an organic solvent, using AALLME. In this approach a low-density solvent with a melting point close to room temperature was applied as the extraction solvent...
July 3, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28687594/reduced-threshold-for-store-overload-induced-ca-2-release-is-a-common-defect-of-ryr1-mutations-associated-with-malignant-hyperthermia-and-central-core-disease
#19
COMPARATIVE STUDY
Wenqian Chen, Andrea Koop, Yingjie Liu, Wenting Guo, Jinhong Wei, Ruiwu Wang, David H MacLennan, Robert T Dirksen, Sui Rong Wayne Chen
Mutations in the skeletal muscle ryanodine receptor (RyR1) cause malignant hyperthermia (MH) and central core disease (CCD), whereas mutations in the cardiac ryanodine receptor (RyR2) lead to catecholaminergic polymorphic ventricular tachycardia (CPVT). Most disease-associated RyR1 and RyR2 mutations are located in the N-terminal, central, and C-terminal regions of the corresponding ryanodine receptor (RyR) isoform. An increasing body of evidence demonstrates that CPVT-associated RyR2 mutations enhance the propensity for spontaneous Ca(2+) release during store Ca(2+) overload, a process known as store overload-induced Ca(2+) release (SOICR)...
August 7, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28660548/chemotherapy-induced-cardiomyopathy-caused-by-pemetrexed
#20
Takuya Oyakawa, Kei Iida, Masatoshi Kusuhara, Hirotsugu Kenmotsu, Takashi Sugino
Chemotherapy-related cardiac toxicity is a rare but serious adverse event in patients with cancer. Thus far, no case of serious cardiac toxicity of pemetrexed has been reported. We describe the case of a patient with advanced lung cancer and cardiomyopathy due to pemetrexed. A 59-year-old woman visited our hospital, and we found abnormal findings on a chest radiograph. She was diagnosed as having stage IV lung adenocarcinoma. Chemotherapy with cisplatin and pemetrexed every 3 weeks was initiated. After four cycles of chemotherapy, maintenance chemotherapy with pemetrexed was administered every 3 weeks...
June 28, 2017: Investigational New Drugs
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