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https://www.readbyqxmd.com/read/28920690/regional-intestinal-permeability-in-rats-a-comparison-of-methods
#1
Carl Roos, David Dahlgren, E Sjögren, Christer Tannergren, Bertil Abrahamsson, H Lennernas
Currently, the screening of new drug candidates for intestinal permeation is typically based on in vitro models which give no information regarding regional differences along the gut. When evaluation of intestinal permeability by region is undertaken, two preclinical rat models are commonly used, the Ussing chamber method and single-pass intestinal perfusion (SPIP). To investigate the robustness of in vivo predictions of human intestinal permeability, a set of four model compounds was systematically investigated in both these models, using tissue specimens and segments from the jejunum, ileum, and colon of rats from the same genetic strain...
September 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28917751/structural-characterization-of-electrochemically-and-in-vivo-generated-potential-metabolites-of-selected-cardiovascular-drugs-by-ec-uhplc-esi-ms-using-an-experimental-design-approach
#2
Małgorzata Szultka-Młyńska, Sylwia Bajkacz, Irena Baranowska, Bogusław Buszewski
In the last few years, a number of studies were conducted which aimed at understanding the mechanisms of cardiovascular drug, metabolism, and there is still the need to determine the metabolites of cardiac drugs for the purpose of metabolism control. In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol)...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28911302/what-is-the-real-efficacy-of-beta-blockers-for-the-treatment-of-essential-hypertension
#3
Christian Höcht, Facundo M Bertera, Julieta S Del Mauro, Yanina Santander Plantamura, Carlos A Taira, Ariel H Polizio
OBJECTIVE: This review covers the pharmacokinetics and pharmacodynamic of β-blockers, the rationale for their use, some recent controversies in its use for managing hypertension, as well as, the beneficial properties of the third-generation β-blockers beyond hypertension. BACKGROUND: The efficacy and safety of -blockers in the treatment of hypertension and other cardiovascular diseases have been established during more than 50 years of clinical experience. Recent updates of clinical guidelines have downgraded the use of -blockers for the treatment of uncomplicated hypertension to second and third line therapy...
June 7, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28905405/bioassay-determination-and-separation-of-enantiomers-of-atenolol-by-direct-and-indirect-approaches-using-liquid-chromatography-a-review
#4
REVIEW
Sonika Batra, Ravi Bhushan
Atenolol, a β-adrenergic receptor antagonist, is a chiral compound used for the treatment of cardiovascular diseases and to treat hypertension, coronary heart disease, arrhythmias, sinus tachycardia and myocardial infarction, where it acts preferentially upon the β-adrenergic receptors in the heart. It is marketed as a racemate, but only (S)-enantiomer of (RS)-atenolol is responsible for the β-adrenoceptor blocking activity. Different chromatographic methods have been applied for separation and determination of enantiomers...
September 14, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28893583/facile-formation-of-co-amorphous-atenolol-and-hydrochlorothiazide-mixtures-via-cryogenic-milling-enhanced-physical-stability-dissolution-and-pharmacokinetic-profile
#5
Sakib M Moinuddin, Sida Ruan, Yuting Huang, Qin Gao, Qin Shi, Baochang Cai, Ting Cai
The development of poorly water-soluble drugs faces the risk of low bioavailability and therapeutic efficacy. The co-amorphous drug delivery system has recently gained considerable interest because it offers an alternative approach to modify properties of poorly water-soluble drugs. Herein, we developed a co-amorphous system of atenolol (ATE) and poorly water-soluble hydrochlorothiazide (HCT) by means of cryogenic milling. The co-administration of ATE and HCT has been reported to show therapeutic advantages for patients with uncomplicated hypertension...
September 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28857292/ion-suppression-effect-in-desi-mass-spectrometry-and-esi-mass-spectrometry
#6
Zheng Wang, Haijing Zhu, Guangming Huang
RATIONALE: Although desorption electrospray ionization (DESI) is claimed to have less ion suppression effect than electrospray ionization (ESI), related investigation with quantification measurement of ion suppression effect is absent. Herein, comparative analysis of ion suppression effect between DESI and ESI was conducted, aiming to quantitatively study the ion suppression effect. METHODS: CTVA mixtures, constant concentration of tioconazole with varied concentrations of atenolol, were detected for ESI and DESI...
August 31, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28836972/access-to-medicines-and-diagnostic-tests-integral-in-the-management-of-diabetes-mellitus-and-cardiovascular-diseases-in-uganda-insights-from-the-accodad-study
#7
Davis Kibirige, David Atuhe, Leaticia Kampiire, Daniel Ssekikubo Kiggundu, Pamela Donggo, Juliet Nabbaale, Raymond Mbayo Mwebaze, Robert Kalyesubula, William Lumu
BACKGROUND: Despite the burgeoning burden of diabetes mellitus (DM) and cardiovascular diseases (CVD) in low and middle income countries (LMIC), access to affordable essential medicines and diagnostic tests for DM and CVD still remain a challenge in clinical practice. The Access to Cardiovascular diseases, Chronic Obstructive pulmonary disease, Diabetes mellitus and Asthma Drugs and diagnostics (ACCODAD) study aimed at providing contemporary information about the availability, cost and affordability of medicines and diagnostic tests integral in the management of DM and CVD in Uganda...
August 24, 2017: International Journal for Equity in Health
https://www.readbyqxmd.com/read/28816547/drug-utilization-among-hypertensive-patients-in-the-outpatient-department-of-medicine-in-a-tertiary-care-hospital-a-cross-sectional-study
#8
Sarika G Paradkar, Shyamal R Sinha
BACKGROUND: Hypertension is one of the leading risk factors for cardiovascular, cerebrovascular, and renal disease. Its increasing prevalence and treatment costs influence the prescribing pattern among physicians. Drug utilization studies provide insights into the current prescribing practices and help us facilitate the rational use of drugs. We carried out the present study to assess the pattern of drug utilization in hypertensive patients. METHOD: Adults seeking treatment for hypertension were recruited...
August 17, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28814785/comparison-between-spectral-analysis-and-symbolic-dynamics-for-heart-rate-variability-analysis-in-the-rat
#9
Luiz Eduardo Virgilio Silva, Victor Rezende Geraldini, Bianca Potratz de Oliveira, Carlos Alberto Aguiar Silva, Alberto Porta, Rubens Fazan
Spectral analysis of heart rate (HR) has been widely used to assess the autonomic cardiovascular control. A nonlinear approach, known as symbolic analysis, has been reported to be very useful to assess the autonomic control of cardiovascular system in humans, but very few studies reported on the differences between these two approaches on experimental models. Two distinct approaches were used to elicit autonomic changes in conscious Wistar rats: (1) pharmacological blockade of cardiac autonomic receptors with atenolol (ATE, N = 9) or methylatropine (ATR, N = 9) and (2) mild changes in arterial pressure (AP) induced by phenylephrine (PHE, N = 9) or sodium nitroprusside (NPS, N = 9)...
August 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28776459/extraction-of-clarithromycin-and-atenolol-by-cuttlefish-bone-powder
#10
Hassen Khazri, Ibtissem Ghorbel-Abid, Rafik Kalfat, Malika Trabelsi-Ayadi
Pharmaceutical products including analgesics, antibiotics, and antiepileptics are often present in wastewater treatment effluents, lakes, and rivers and have been found in waterways of many countries. The adsorption of two common pharmaceuticals present in surface waters, clarithromycin (CLR) and atenolol (ATN), onto cuttlefish bone powder treated with HCl has been investigated. Adsorption experiments were carried out at different pH conditions and the experimental equilibrium data were fitted to the Langmuir and Freundlich...
August 16, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28760606/synthesis-analytical-characterization-and-capillary-electrophoretic-use-of-the-single-isomer-heptakis-6-o-sulfobutyl-beta-cyclodextrin
#11
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/28760594/s-oxiracetam-protect-against-ischemic-stroke-via-alleviating-blood-brain-barrier-dysfunction-in-rats
#12
Liangliang Huang, Erxin Shang, Wenxiang Fan, Xiang Li, Binbin Li, Shucheng He, Yuxin Fu, Yizhi Zhang, Yunman Li, Weirong Fang
The blood brain barrier (BBB) maintains the basic stability of the brain tissue under physiological conditions, while destroys and exaggerates brain edema and inflammatory response after ischemic stroke. In this study, we researched S-oxiracetam (S-ORC), a nootropic drug, alleviates BBB dysfunction and protects against ischemic stroke in rats. Middle cerebral artery occlusion(MCAO)/reperfusion in rats is applied to mimic ischemic stroke. One hour after reperfusion, rats are administered intravenously with different dose (0...
July 29, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28760243/comparative-efficacy-of-%C3%AE-blockers-on-mortality-and-cardiovascular-outcomes-in-patients-with-hypertension-a-systematic-review-and-network-meta-analysis
#13
Yuqing Zhang, Ningling Sun, Xueli Jiang, Yang Xi
The differential efficacy of lipophilic and hydrophilic β-blockers on clinical outcomes has not been investigated. We sought to compare the effects of lipophilic and hydrophilic β-blockers on mortality and cardiovascular outcomes by conducting a comprehensive systematic review and network meta-analysis. MEDLINE/PubMed, EMBASE, and the Cochrane Database were searched for all dates to January 5, 2015, for randomized trials with comparisons between all β-blockers or between β-blockers and other antihypertensive agents...
July 2017: Journal of the American Society of Hypertension: JASH
https://www.readbyqxmd.com/read/28757554/multifunctional-cinnamic-acid-derivatives
#14
Aikaterini Peperidou, Eleni Pontiki, Dimitra Hadjipavlou-Litina, Efstathia Voulgari, Konstantinos Avgoustakis
Our research to discover potential new multitarget agents led to the synthesis of 10 novel derivatives of cinnamic acids and propranolol, atenolol, 1-adamantanol, naphth-1-ol, and (benzylamino) ethan-1-ol. The synthesized molecules were evaluated as trypsin, lipoxygenase and lipid peroxidation inhibitors and for their cytotoxicity. Compound 2b derived from phenoxyphenyl cinnamic acid and propranolol showed the highest lipoxygenase (LOX) inhibition (IC50 = 6 μΜ) and antiproteolytic activity (IC50 = 0.425 μΜ)...
July 25, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28743866/mass-spectrometry-imaging-proves-differential-absorption-profiles-of-well-characterised-permeability-markers-along-the-crypt-villus-axis
#15
Anna Nilsson, Alexandra Peric, Marie Strimfors, Richard J A Goodwin, Martin A Hayes, Per E Andrén, Constanze Hilgendorf
Knowledge about the region-specific absorption profiles from the gastrointestinal tract of orally administered drugs is a critical factor guiding dosage form selection in drug development. We have used a novel approach to study three well-characterized permeability and absorption marker drugs in the intestine. Propranolol and metoprolol (highly permeable compounds) and atenolol (low-moderate permeability compound) were orally co-administered to rats. The site of drug absorption was revealed by high spatial resolution matrix-assisted laser desorption ionization mass spectrometry imaging (MALDI-MSI) and complemented by quantitative measurement of drug concentration in tissue homogenates...
July 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28743285/%C3%AE-adrenergic-receptor-camp-pka-signaling-contributes-to-the-intracellular-ca-2-release-by-tentacle-extract-from-the-jellyfish-cyanea-capillata
#16
Qianqian Wang, Hui Zhang, Bo Wang, Chao Wang, Liang Xiao, Liming Zhang
BACKGROUND: Intracellular Ca(2+) overload induced by extracellular Ca(2+) entry has previously been confirmed to be an important mechanism for the cardiotoxicity as well as the acute heart dysfunction induced by jellyfish venom, while the underlying mechanism remains to be elucidated. METHODS: Under extracellular Ca(2+)-free or Ca(2+)-containing conditions, the Ca(2+) fluorescence in isolated adult mouse cardiomyocytes pre-incubated with tentacle extract (TE) from the jellyfish Cyanea capillata and β blockers was scanned by laser scanning confocal microscope...
July 25, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28728322/perioperative-hypertension-management-during-facelift-under-local-anesthesia-with-intravenous-hypnotics
#17
Ki Ho Chung, Myeong Soo Cho, Hoon Jin
Perioperative hypertension is a phenomenon in which a surgical patient's blood pressure temporarily increases throughout the preoperative and postoperative periods and remains high until the patient's condition stabilizes. This phenomenon requires immediate treatment not only because it is observed in a majority of patients who are not diagnosed with high blood pressure, but also because occurs in patients with underlying essential hypertension who show a sharp increase in their blood pressure. The most common complication following facelift surgery is hematoma, and the most critical risk factor that causes hematoma is elevated systolic blood pressure...
July 2017: Archives of Plastic Surgery
https://www.readbyqxmd.com/read/28722356/hansen-solubility-parameters-for-assay-method-optimization-of-simvastatin-ramipril-atenolol-hydrochlorothiazide-and-aspirin-in-human-plasma-using-liquid-chromatography-with-tandem-mass-spectrometry
#18
Murali Mohan Reddy Devalapalli, Hanumanth Srikanth Cheruvu, Thejaswi Yertha, Vijaya Bhaskar Veeravalli, Sunitha Sampathi, Savithri Shivakumar
A simple, specific, sensitive validated method was developed using liquid chromatography with tandem mass spectrometry with electrospray ionization of human plasma for the simultaneous estimation of drugs (simvastatin, ramipril, atenolol, hydrochlorothiazide and aspirin) of Polycap(TM) capsule used in cardiovascular therapy. The interaction of these actives including internal standards between the stationary and mobile phase were investigated using Hansen solubility parameters. Chromatographic separation was performed on Phenomenex Synergi Polar-RP (30 × 2 mm, 4 μm) column with a gradient mobile phase composition of acetonitrile and 5 mM ammonium formate for positive mode and 0...
July 19, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28719875/novel-magnetic-carboxyl-modified-hypercrosslinked-resins-for-effective-removal-of-typical-ppcps
#19
Jing Jin, Tianyu Feng, Yan Ma, Wei Wang, Yunshu Wang, Qing Zhou, Aimin Li
A series of novel magnetic carboxyl modified hypercrosslinked resins were successfully prepared via a sequence of suspension polymerization, hydrolysis and post-crosslinking reactions. The serial resins possessed both high cation exchange capacity and high specific surface area with MA-10 having the supreme specific surface area of 1238.65 m(2)/g and MA-70 having the largest exchange capacity of 6.45 mmol/g. The serial resins exhibited excellent adsorption capacity of typical PPCPs including chloramphenicol, atenolol, ibuprofen and tetracycline, which were neutral, cationic, anionic and zwitterionic respectively in natural water...
October 2017: Chemosphere
https://www.readbyqxmd.com/read/28713440/investigating-the-physical-stability-of-repackaged-medicines-stored-into-commercially-available-multicompartment-compliance-aids-mcas
#20
Bahijja Tolulope Raimi-Abraham, Alba Garcia Del Valle, Carlota Varon Galcera, Susan Anne Barker, Mine Orlu
BACKGROUND: Compliance aids are devices which have been developed and are currently used to assist individuals in their medicines management. The use of compliance aids involves the transfer of medicines from the manufacturers' original packaging and repackaged into an multicompartment compliance aid (MCA). MCAs do not guarantee the same level of protection compared to manufacturer's original packaging. OBJECTIVE: The aim of this study was to investigate the stability profile of atenolol, aspirin and lansoprazole dosage forms repackaged together in two different commercially available MCAs...
June 2017: Journal of Pharmaceutical Health Services Research
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