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Sample records for atenolol

  1. Adsorption of Atenolol on Kaolinite

    Directory of Open Access Journals (Sweden)

    Yingmo Hu

    2015-01-01

    Full Text Available In this study the adsorption of atenolol (AT, a β-blocker, on kaolinite, a clay mineral of low surface charge, was investigated under varying initial AT concentration, equilibrium time, solution pH, ionic strength, and temperature conditions. The results showed that the amounts of AT uptake by kaolinite were close to its cation exchange capacity value and the AT adsorption was almost instantaneous, suggesting a surface adsorption. The adsorption was exothermic and the free energy of adsorption was small negative, indicating physical adsorption. The increase in ionic strength of the solution drastically reduced AT uptake on kaolinite. A significant reduction in AT uptake was found at solution pH below 5 or above 10. The FTIR results showed band shifting and disappearance for NH bending vibration and benzene ring skeletal vibration at 3360 and 1515 cm−1 and band splitting at 1412 and 1240 cm−1 attributed to C–N valence vibration coupled with NH bending vibrations and alkyl aryl ether linkage, suggesting the participation of NH, –O–, and benzene ring for AT adsorption on kaolinite.

  2. Flurbiprofen interaction with single doses of atenolol and propranolol.

    Science.gov (United States)

    Webster, J; Petrie, J C; McLean, I; Hawksworth, G M

    1984-01-01

    In patients with mild hypertension, flurbiprofen in a dose of 100 mg daily for 7 days attenuated the hypotensive effect of a single dose of propranolol 80 mg but not of atenolol 100 mg. The attenuation was not due to an effect on the pharmacokinetic profile of either propranolol or atenolol. An alternative explanation is required. PMID:6529525

  3. New alginic acid–atenolol microparticles for inhalatory drug targeting

    Energy Technology Data Exchange (ETDEWEB)

    Ceschan, Nazareth Eliana; Bucalá, Verónica [Planta Piloto de Ingeniería Química (PLAPIQUI), CONICET, Universidad Nacional del Sur (UNS), Camino La Carrindanga Km 7, 8000 Bahía Blanca (Argentina); Departamento de Ingeniería Química, UNS, Avenida Alem 1253, 8000 Bahía Blanca (Argentina); Ramírez-Rigo, María Verónica, E-mail: vrrigo@plapiqui.edu.ar [Planta Piloto de Ingeniería Química (PLAPIQUI), CONICET, Universidad Nacional del Sur (UNS), Camino La Carrindanga Km 7, 8000 Bahía Blanca (Argentina); Departamento de Biología, Bioquímica y Farmacia, UNS, San Juan 670, 8000 Bahía Blanca (Argentina)

    2014-08-01

    The inhalatory route allows drug delivery for local or systemic treatments in a noninvasively way. The current tendency of inhalable systems is oriented to dry powder inhalers due to their advantages in terms of stability and efficiency. In this work, microparticles of atenolol (AT, basic antihypertensive drug) and alginic acid (AA, acid biocompatible polyelectrolyte) were obtained by spray drying. Several formulations, varying the relative composition AT/AA and the total solid content of the atomized dispersions, were tested. The powders were characterized by: Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry and Powder X-ray Diffraction, while also the following properties were measured: drug load efficiency, flow properties, particles size and density, moisture content, hygroscopicity and morphology. The ionic interaction between AA and AT was demonstrated, then the new chemical entity could improve the drug targeting to the respiratory membrane and increase its time residence due to the mucoadhesive properties of the AA polymeric chains. Powders exhibited high load efficiencies, low moisture contents, adequate mean aerodynamic diameters and high cumulative fraction of respirable particles (lower than 10 μm). - Highlights: • Novel particulate material to target atenolol to the respiratory membrane was developed. • Crumbled microparticles were obtained by spray drying of alginic–atenolol dispersions. • Ionic interaction between alginic acid and atenolol was demonstrated in the product. • Amorphous solids with low moisture content and high load efficiency were produced. • Relationships between the feed formulation and the product characteristics were found.

  4. FORMULATION AND EVALUATION OF GASTRO RETENTIVE FLOATING DRUG DELIVERY SYSTEM OF ATENOLOL

    OpenAIRE

    BRAHMAIAH BONTHAGARALA; G.V.PAVAN KUMAR; P. Venkateswara Rao; N.MANOHAR BABU

    2014-01-01

    Objective: Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastro retentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Atenolol is an antihypertensive drug, which has low elimination half life: 3–4 hrs. The floating tablets of Atenolol were prepared to increase the gastric retention and to improve the bioavailability of the drug. Atenolol was chosen as a model drug because it is be...

  5. Losartan versus atenolol-based antihypertensive treatment reduces cardiovascular events especially well in elderly patients

    DEFF Research Database (Denmark)

    Ruwald, Anne Christine H; Westergaard, Bo; Sehestedt, Thomas;

    2012-01-01

    The Losartan Intervention For Endpoint reduction in hypertension (LIFE) study has previously demonstrated a beneficial effect of losartan compared to atenolol-based antihypertensive treatment in patients with essential hypertension and left-ventricular hypertrophy (LVH). However, patient age often...... influences the choice of antihypertensive drugs. Therefore, we investigated the influence of age on the effects of losartan versus atenolol-based antihypertensive treatment....

  6. Atenolol Pharmacokinetics and Excretion in Breast Milk during the first 6–8 Months Postpartum

    OpenAIRE

    Eyal, Sara; Kim, Joong D.; Gail D Anderson; Buchanan, Megan L.; Brateng, Debra A.; Carr, Darcy; Woodrum, David E.; Easterling, Thomas R.; Hebert, Mary F.

    2010-01-01

    Our objectives were to evaluate the time course for atenolol pharmacokinetics in lactating women postpartum and to quantify atenolol plasma concentrations in their 3–4 months old nursing infants. Data were collected over one dosing interval from lactating women treated with atenolol for therapeutic reasons, at 2–4 weeks (n=32), 3–4 months (n=22), and 6–8 months (n=17) postpartum. A single blood sample was collected from 15 nursing infants (3–4 months of age) of the mothers participating in th...

  7. Synergism of atenolol and nitrendipine on hemody-namic amelioration and organ protection in hypertensive rats

    Institute of Scientific and Technical Information of China (English)

    He-huiXIE; Chao-yuMIAO; Yuan-yingJIANG; Ding-fengSU

    2004-01-01

    AIM: This study was designed to investigate the possible synergism of atenolol and nitrendipine on blood pressure (BP) and blood pressure variability (BPV) reductions, baroreflex sensitivity (BRS) amelioration, and organ protection in hypertensive rats. METHODS:The dose is 20 mg/kg for atenolol, 10 mg/kg for nitrendipine and the combination of these two drugs. In acute study, a single dose was given via a catheter previously inserted

  8. Aspirin and atenolol enhance metformin activity against breast cancer by targeting both neoplastic and microenvironment cells.

    Science.gov (United States)

    Talarico, Giovanna; Orecchioni, Stefania; Dallaglio, Katiuscia; Reggiani, Francesca; Mancuso, Patrizia; Calleri, Angelica; Gregato, Giuliana; Labanca, Valentina; Rossi, Teresa; Noonan, Douglas M; Albini, Adriana; Bertolini, Francesco

    2016-01-01

    Metformin can induce breast cancer (BC) cell apoptosis and reduce BC local and metastatic growth in preclinical models. Since Metformin is frequently used along with Aspirin or beta-blockers, we investigated the effect of Metformin, Aspirin and the beta-blocker Atenolol in several BC models. In vitro, Aspirin synergized with Metformin in inducing apoptosis of triple negative and endocrine-sensitive BC cells, and in activating AMPK in BC and in white adipose tissue (WAT) progenitors known to cooperate to BC progression. Both Aspirin and Atenolol added to the inhibitory effect of Metformin against complex I of the respiratory chain. In both immune-deficient and immune-competent preclinical models, Atenolol increased Metformin activity against angiogenesis, local and metastatic growth of HER2+ and triple negative BC. Aspirin increased the activity of Metformin only in immune-competent HER2+ BC models. Both Aspirin and Atenolol, when added to Metformin, significantly reduced the endothelial cell component of tumor vessels, whereas pericytes were reduced by the addition of Atenolol but not by the addition of Aspirin. Our data indicate that the addition of Aspirin or of Atenolol to Metformin might be beneficial for BC control, and that this activity is likely due to effects on both BC and microenvironment cells. PMID:26728433

  9. Labeling of atenolol with radioactive iodine-125 using N-bromosuccinimide and hydrogen peroxide as oxidizing agents

    International Nuclear Information System (INIS)

    An adopted method for the preparation of high radiochemical purity 125I-atenolol was investigated. Direct radioiodination of atenolol was carried out using N-bromosuccinamide or hydrogen peroxide as an oxidizing agent. The reaction proceeds well within 30 min at room temperature (25 ± 1 deg C) and afforded a radiochemical yield up to 97% as pure as 125I-atenolol. Different chromatographic techniques (electrophoresis, TLC and HPLC) were used to determine the radiochemical yield and purity of the labeled product. Biodistribution studies were carried out in normal Albino Swiss mice and the results indicate that 125I-atenolol can be used safely as myocardial imaging agent. (author)

  10. FORMULATION AND EVALUATION OF GASTRO RETENTIVE FLOATING DRUG DELIVERY SYSTEM OF ATENOLOL

    Directory of Open Access Journals (Sweden)

    BRAHMAIAH BONTHAGARALA

    2014-08-01

    Full Text Available Objective: Drugs that have narrow absorption window in the gastrointestinal tract (GIT will have poor absorption. For these drugs, gastro retentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Atenolol is an antihypertensive drug, which has low elimination half life: 3–4 hrs. The floating tablets of Atenolol were prepared to increase the gastric retention and to improve the bioavailability of the drug. Atenolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. Methods: The floating tablets were formulated using HPMC K4M and HPMC K100M as the release retardant polymers, and sodium bicarbonate as the gas generating agent to reduce the floating lag time. The tablets were prepared by direct compression. Results: The formulated tablets were evaluated for weight variation, hardness, friability, swelling index floating lag time, total floating time and dissolution rate in pH 1.2. The floating tablets extended the drug release up to 8 hrs. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR. The FTIR study indicated the lack of drug-polymer interaction. Conclusion: Eight Formulations of Floating tablets of Atenolol were developed by direct compression technique. The F8 Formulation was found to be best of all the trails showing that the drug release matches with brand product.

  11. Photodegradation kinetics and transformation products of ketoprofen, diclofenac and atenolol in pure water and treated wastewater

    Energy Technology Data Exchange (ETDEWEB)

    Salgado, R. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); ESTS-IPS, Escola Superior de Tecnologia de Setúbal do Instituto Politécnico de Setúbal, Rua Vale de Chaves, Campus do IPS, Estefanilha, 2910-761 Setúbal (Portugal); Pereira, V.J. [Instituto de Biologia Experimental e Tecnológica (IBET), Av. da República (EAN), 2784-505 Oeiras (Portugal); Instituto de Tecnologia Química e Biológica (ITQB) – Universidade Nova de Lisboa (UNL), Av. da República, Estação Agronómica Nacional, 2780-157 Oeiras, 5 Portugal (Portugal); Carvalho, G., E-mail: gs.carvalho@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Instituto de Biologia Experimental e Tecnológica (IBET), Av. da República (EAN), 2784-505 Oeiras (Portugal); Soeiro, R. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Gaffney, V.; Almeida, C. [Institute for Medicines and Pharmaceutical Sciences (iMed.UL), Faculdade de Farmácia da Universidade de Lisboa (FFUL), Av. Prof. Gama Pinto, 1600-049 Lisboa (Portugal); Cardoso, V. Vale; Ferreira, E.; Benoliel, M.J. [Empresa Portuguesa das Águas Livres, S.A., Direcção de Controlo de Qualidade da Água, Laboratório Central, Avenida de Berlim, 15, 1800-031 Lisboa (Portugal); and others

    2013-01-15

    Highlights: ► Direct UV photolysis of 3 pharmaceuticals in pure and waste water was investigated. ► Ketoprofen has higher photodegradion kinetics, followed by diclofenac and atenolol. ► MP/UV photodegradation products were identified for the 3 compounds. ► Photodegradation pathways were proposed to explain the obtained products. ► The persistent photoproducts were identified for each compound. -- Abstract: Pharmaceutical compounds such as ketoprofen, diclofenac and atenolol are frequently detected at relatively high concentrations in secondary effluents from wastewater treatment plants. Therefore, it is important to assess their transformation kinetics and intermediates in subsequent disinfection processes, such as direct ultraviolet (UV) irradiation. The photodegradation kinetics of these compounds using a medium pressure (MP) lamp was assessed in pure water, as well as in filtered and unfiltered treated wastewater. Ketoprofen had the highest time- and fluence-based rate constants in all experiments, whereas atenolol had the lowest values, which is consistent with the corresponding decadic molar absorption coefficient and quantum yield. The fluence-based rate constants of all compounds were evaluated in filtered and unfiltered wastewater matrices as well as in pure water. Furthermore, transformation products of ketoprofen, diclofenac and atenolol were identified and monitored throughout the irradiation experiments, and photodegradation pathways were proposed for each compound. This enabled the identification of persistent transformation products, which are potentially discharged from WWTP disinfection works employing UV photolysis.

  12. Ecotoxicity of ketoprofen, diclofenac, atenolol and their photolysis byproducts in zebrafish (Danio rerio)

    Energy Technology Data Exchange (ETDEWEB)

    Diniz, M.S., E-mail: mesd@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Salgado, R., E-mail: r.salgado@campus.fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); ESTS-IPS, Escola Superior de Tecnologia de Setúbal do Instituto Politécnico de Setúbal, Rua Vale de Chaves, Campus do IPS, Estefanilha, 2910-761 Setúbal (Portugal); Pereira, V.J., E-mail: vanessap@itqb.unl.pt [Instituto de Biologia Experimental e Tecnológica (IBET), Av. da República (EAN), 2784-505 Oeiras (Portugal); Instituto de Tecnologia Química e Biológica (ITQB)—Universidade Nova de Lisboa (UNL), Estação Agronómica Nacional, Av. da República, 2780-157 Oeiras (Portugal); Carvalho, G., E-mail: gs.carvalho@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Instituto de Biologia Experimental e Tecnológica (IBET), Av. da República (EAN), 2784-505 Oeiras (Portugal); Oehmen, A., E-mail: a.oehmen@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Reis, M.A.M., E-mail: amr@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Noronha, J.P., E-mail: jpnoronha@fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal)

    2015-02-01

    The occurrence of pharmaceutical compounds in wastewater treatment plants and surface waters has been detected worldwide, constituting a potential risk for aquatic ecosystems. Adult zebrafish, of both sexes, were exposed to three common pharmaceutical compounds (atenolol, ketoprofen and diclofenac) and their UV photolysis by-products over seven days. The results show that diclofenac was removed to concentrations < LOD after 5 min of UV irradiation. The oxidative stress response of zebrafish to pharmaceuticals and their photolysis by-products was evaluated through oxidative stress enzymes (glutathione-S-transferase, catalase, superoxide dismutase) and lipid peroxidation. Results suggest that the photolysis by-products of diclofenac were more toxic than those from the other compounds tested, showing an increase in GST and CAT levels, which are also supported by higher MDA levels. Overall, the toxicity of waters containing atenolol and ketoprofen was reduced after the parent compounds were transformed by photolysis, whereas the toxicity increased significantly from the by-products generated through diclofenac photolysis. Therefore, diclofenac photolysis would possibly necessitate higher irradiation time to ensure that the associated by-products are completely degraded to harmless form(s). - Highlights: • Toxicity evaluated for 3 common pharmaceuticals (atenolol, ketoprofen and diclofenac). • Toxicity assessed for the pharmaceuticals and UV photolysis by-products in zebrafish. • Diclofenac photolysis by-products are more toxic than the parent compound. • Ketoprofen and atenolol show stronger oxidative stress response than by-products. • UV photolysis should ensure full removal of diclofenac metabolites to avoid toxicity.

  13. Distinct effects of losartan and atenolol on vascular stiffness in Marfan syndrome.

    Science.gov (United States)

    Bhatt, Ami B; Buck, J Stewart; Zuflacht, Jonah P; Milian, Jessica; Kadivar, Samoneh; Gauvreau, Kimberlee; Singh, Michael N; Creager, Mark A

    2015-08-01

    We conducted a randomized, double-blind trial of losartan (100 mg QD) versus atenolol (50 mg QD) for 6 months in adults with Marfan syndrome. Carotid-femoral pulse wave velocity (PWV), central augmentation index (AIx), aortic diameter and left ventricular (LV) function were assessed with arterial tonometry and echocardiography. Thirty-four subjects (18 female; median age 35 years, IQR 27, 45) were randomized. Central systolic and diastolic blood pressure decreased comparably with atenolol and losartan (p = 0.64 and 0.31, respectively); heart rate decreased with atenolol (p = 0.02), but not with losartan. PWV decreased in patients treated with atenolol (-1.15 ± 1.68 m/s; p = 0.01), but not in those treated with losartan (-0.22 ± 0.59 m/s; p = 0.15; between-group difference p = 0.04). In contrast, AIx decreased in the losartan group (-9.6 ± 8.6%; p losartan reduces the AIx. By improving vascular stiffness via distinct mechanisms of action, there is physiologic value to considering the use of both medications in individuals with Marfan syndrome.

  14. A molecular inclusion complex of atenolol with 2-hydroxypropyl-b-cyclodextrin; the production and characterization thereof

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    VESNA NIKOLIC

    2007-08-01

    Full Text Available The molecular inclusion complex of atenolol with 2-hydroxypropyl-b-cy­clodextrin was synthesized using the coprecipitation method. The complex obtained was characterized by FT-IR, 1H‑NMR, 13C-NMR spectroscopy, as well as by DSC and X-ray diffraction analysis. The DSC analysis confirmed the existence of the com­plex with the endothermic atenolol melting peak at about 155 ºC disappearing. The X-ray diffraction patterns of the complex and 2-hydroxypropyl-b-cyclodextrin were very similar, thus confirming the complete inclusion of the atenolol molecule within the cavity of the 2-hydroxypropyl-b-cyclodextrin. The peaks originating from ate­nolol were completely absent in the diffractogram of the complex. 1H-NMR and 13C-NMR spectra showed certain changes in the chemical shifts of protons and C atoms from atenolol and 2-hydroxypropyl-b-cyclodextrin, indicating that a complex had been formed and also which protons participated in the hydrogen bonds which formed the complex. The atenolol solubility in water was improved (254 mg com­plex cm-3, i.e., 37.5 mg atenolol cm-3, and in pH 3 HCl solution (251 mg com­plex cm-3, i.e., 37 mg atenolol cm-3 when compared to pure atenolol, and even when compared to the atenolol complex with b-cyclodextrin. The increased solubility en­sures greater bioavailability of the active component and, due to the low solubility, significantly corrects for the lack of the basic active substance and, simultaneously, increases its overall therapeutic effect, combined with reduced side effects.

  15. Long-term treatment with losartan versus atenolol improves insulin sensitivity in hypertension: ICARUS, a LIFE substudy

    DEFF Research Database (Denmark)

    Olsen, Michael H; Fossum, Eigil; Høieggen, Aud;

    2005-01-01

    Hypertension and insulin resistance might be associated through peripheral vascular hypertrophy/rarefaction which compromises skeletal muscle blood flow and decreases glucose uptake, inducing insulin resistance. We hypothesized that treatment with losartan as compared to atenolol would improve...

  16. Pharmacokinetics and safety of olmesartan medoxomil in combination with either amlodipine or atenolol compared to respective monotherapies in healthy subjects.

    Science.gov (United States)

    Bolbrinker, Juliane; Huber, Matthias; Scholze, Jürgen; Kreutz, Reinhold

    2009-12-01

    The aim of this study was to investigate any influence on olmesartan plasma pharmacokinetics from amlodipine or atenolol. We analysed pharmacokinetics and safety of olmesartan medoxomil in combination with either amlodipine or atenolol compared to respective monotherapies in two separate studies. In one study, 18 subjects received once daily treatment for 7 days with olmesartan medoxomil 20 mg alone or with amlodipine 5 mg or amlodipine 5 mg alone. In the other study, atenolol 50 mg once daily replaced amlodipine. Concentration vs. time profiles for olmesartan monotherapy were similar to combination therapy. Mean olmesartan AUC(ss,tau) for olmesartan alone and with amlodipine were 2439 and 2388 ng h/mL and for olmesartan alone and with atenolol were 2340 and 2247 ng h/mL. Corresponding olmesartan C(ss,max) values were 465.7 and 439.5 ng/mL for amlodipine, and 447.4 and 423.8 ng/mL for atenolol. Median t(max) values for olmesartan were 1.5 h for each group in each study. Bioequivalence was established for all pharmacokinetic parameters. Lack of significant pharmacokinetic interactions between olmesartan and amlodipine or atenolol provides a basis for combination therapy.

  17. Formulation and evaluation of atenolol floating bioadhesive system using optimized polymer blends

    OpenAIRE

    Siddam, Haritha; Kotla, Niranjan G.; Maddiboyina, Balaji; Singh, Sima; Sunnapu, Omprakash; Kumar, Anil; Sharma, Dinesh

    2016-01-01

    Introduction: Oral sustained release gastro retentive dosage forms offer several advantages for drugs having absorption from the upper gastrointestinal tract to improve the bioavailability of medications which have narrow absorption window. The aim of the study was to develop a floating bioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong the residence in the stomach using atenolol as a model drug. Methods: Prior to compression, polymeric b...

  18. Lack of a pharmacokinetic interaction between nifedipine and the beta-adrenoceptor blockers metoprolol and atenolol.

    OpenAIRE

    Kendall, M. J.; Jack, D B; Laugher, S J; Lobo, J.; Rolf Smith, S

    1984-01-01

    Nifedipine, metoprolol and atenolol were administered orally to young, healthy volunteers. Each drug was given alone and nifedipine was also given with both beta-adrenoceptor blockers. Each drug was given for 3 days immediately before the study days. Plasma and urine drug concentrations were measured and the relevant pharmacokinetic parameters calculated. No pharmacokinetic interaction between nifedipine and the beta-adrenoceptor blockers was revealed.

  19. COMPARATIVE RESEARCH OF ENALAPRIL AND ATENOLOL ANTIHYPERTENSIVE EFFICACY IN HIGH RISK PATIENTS

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    O. M. Moiseeva

    2006-01-01

    Full Text Available Aim. To evaluate the effecacy of enalapril (Enam, Dr.Reddy’s, India and atenolol (Tenormin, AstraZeneca, UK and their influence on processes of cardiovascular system remodeling in comparative research in patients with arterial hypertension. Material and methods. 38 patients with arterial hypertension stage II were examined. 21 patients were treated with enalapril (10-40 mg\\d and 17 – with atenolol (50-100 mg\\d. Duration of therapy was 24 weeks.  A daily monitoring of blood pressure and echocardiography were made before and after the treatment. Spontaneous erythrocyte aggregation and deformability, spontaneous platelet aggregation and adhesive property of neutrophils were also estimated. A number of leucocytes carrying activation markers and expressing adhesive molecules was calculated. The plasma concentration of adhesive molecules (ICAM-1 and von Willebrand protein as well as serum concentration of N-terminal peptide of procollagen type III was also estimated. Results. Enalapril versus atenolol improved blood rheology, reduced functional leucocytes activity, plasma concentration of von Willebrand protein and intercellular adhesive molecules. The reduction in collagen III synthesis activity in enalapril therapy was proved. A significant regress of left ventricle hypertrophy due to enalapril treatment was related with favorable non-hemodynamic effects. Conclusion. The research revealed that the blockage of tissue rennin-angiotensin system is very important in prevention of cardiovascular complications especially in high risk patients.

  20. Permeation studies of atenolol and metoprolol tartrate from three different polymer matrices for transdermal delivery

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    Agrawal S

    2007-01-01

    Full Text Available Since oral bioavailability of atenolol and metoprolol tartrate is poor, different matrix -type transdermal patches incorporating atenolol and metoprolol tartrate were formulated with an objective to study the effect of polymers on transdermal release of the drugs. The polymers selected were polyvinylpyrrolidone, cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate and ethyl cellulose. The patches were formulated using combination of polymers and propylene glycol and 1,8-cineole as plasticizer and penetration enhancer, respectively. The physico-chemical evaluation of the polymer matrices was performed for suitability. The interaction among various components of the matrices was studied by performing Differential Scanning Calorimetry and Scanning Electron Micrography of the formulated patches. In vitro permeation studies were performed using rat abdominal skin as the permeating membrane in Keshary-Chien cell. The results indicated that maximum release was obtained at 48 h (85% and 44% of atenolol and metoprolol tartrate, respectively. The drug permeation studies across cadaver skin showed about 27% of reduction in the amount of drug release as that compared to rat abdominal skin was used.

  1. Comparison of nifedipine gastrointestinal therapeutic system and atenolol on antianginal efficacies and exercise hemodynamic responses in stable angina pectoris.

    Science.gov (United States)

    Wallace, W A; Wellington, K L; Chess, M A; Liang, C S

    1994-01-01

    A gastrointestinal therapeutic system (GITS) of nifedipine has been developed to provide a once-daily dosing, and predictable, relatively constant plasma concentrations. This study compared the antianginal efficacy of nifedipine GITS with a once-a-day beta-receptor blocker, atenolol. Seventeen patients with documented coronary artery disease and stable stress-induced angina pectoris were studied during a 2-week, single-blind, placebo baseline phase and a 12-week randomized, double-blind, active drug crossover efficacy phase, using the bicycle exercise test and ambulatory electrocardiographic recordings. Patients exercised significantly longer with nifedipine GITS (883 +/- 47 seconds) and atenolol (908 +/- 44 seconds) than with placebo (794 +/- 41 seconds). Nifedipine GITS reduced systolic blood pressure at all stages of exercise compared with placebo but, because heart rate tended to increase more during nifedipine therapy, there was no difference in rate-pressure products between the placebo and nifedipine GITS periods. In contrast, atenolol reduced heart rate, systolic blood pressure and rate-pressure product during exercise compared with placebo. Whereas left ventricular ejection fractions (by radionuclide angiocardiography) increased with exercise, the maximal increase was smaller with atenolol than with placebo and nifedipine. The net increase in left ventricular ejection fraction at the end of exercise was greater with nifedipine than with placebo or atenolol. Ambulatory electrocardiograms showed only a small number of ischemic events. Neither nifedipine GITS nor atenolol reduced the number of ischemic events or total duration of ST-segment deviations significantly. It is concluded that nifedipine GITS is as effective an antianginal agent as atenolol, but the hemodynamic effects of the 2 agents differ.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:8279372

  2. DEVELOPMENT AND VALIDATION OF RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF ATENOLOL AND CHLORTHALIDONE FROM PHARMACEUTICAL FORMULATION

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    G. S Kumar

    2012-10-01

    Full Text Available A reverse phase high performance liquid chromatography (RP HPLC method was developed and validated for the simultaneous estimation of atenolol and chlorthalidone in marketed formulation. The determination was carried out on an Xterra RP8 (150 x 4.6 mm, 5 µm column using a mobile phase of potassium dihydrogen phosphate buffer solution: methanol (50:50v/v, pH 3.6 with flow rate 0.5ml/min (UVdetection at 240 nm. The retention time for atenolol was 3.2 min and for chlorthalidone 5.0 min. Atenolol and chlorthalidone showed a linear response in the concentration range of 50-150 µg/ml. The correlation co-efficient (' r ' value for atenolol and chlorthalidone was 0.9996. The developed method was validated with regard to linearity, accuracy, precision, selectivity and robustness and the method was found to be precise, accurate, linear and specific. The method was validated as per ICH guidelines. The RSD for intra-day and inter-day precision were found to be less than 2 %. The percentage recoveries obtained for atenolol and chlorthalidone ranges from 100.54-103.32% and 98.03-102.77% respectively which was in good agreement with the labeled amount in the pharmaceutical formulations.

  3. Study of polymorphism of Atenolol and Captopril antihypertensives using x-ray powder diffraction and Rietveld refinement

    Science.gov (United States)

    Sato, Juliana; Ferreira, Fabio

    2013-03-01

    Characterization of bulk drugs has become increasingly important in the pharmaceutical industry. X-ray powder diffractometry is an effective technique for the identification of crystalline solid-phase drugs. The technique is unique, since it combines specificity with a high degree of accuracy for the characterization of pharmaceuticals in solid state and is an especially useful method to describe the possible polymorphic behavior of drugs substances. In this work X-ray diffraction data have been obtained for two well-known antihypertensive drugs currently being administered in tablet form. They include atenolol and captopril. Atenolol and captopril were purchased from drugstore. The characterizations of the atenolol and captopril samples were carried out by FTIR spectroscopy and X-ray powder diffraction (XRPD). We would like to thank the Brazilian agencies CNPq and FAPESP for their financial support.

  4. INFLUENCE OF ENALAPRIL, DIGOXIN, ATENOLOL AND DILTIAZEM ON LIPID PEROXIDATION IN EXPERIMENTAL MODEL OF COMPLEX METABOLIC DISORDERS

    Directory of Open Access Journals (Sweden)

    A. A. Usanova

    2016-01-01

    Full Text Available Aim. To study influence of enalapril, digoxin, atenolol and diltiazem on lipid peroxidation and antioxidative protection in experimental disorders of glucose and lipid metabolism.Material and methods. White nonlinear mice were used for modeling of the complex metabolic disorders by alloxan and cholesterol infusion. Evaluation of acute drug toxicity and indicators of lipid peroxidation and antioxidant protection was performed. Superoxide dismutase and catalase activity, malondialdehyde concentration were evaluated.Results. Toxicity of digoxin, diltiazem, atenolol in complex metabolic disorders was increased, and toxicity of enalapril was unchanged. Enalapril had antioxidant effect. Atenolol had prooxidative effect in myocardium and kidneys, and diltiazem - in kidneys.Conclusion. Enalapril showed antioxidant effect and decreased concentration of secondary products of lipid peroxidation in renal tissue. It may be considered as the first line drug in complex metabolic disorders.

  5. Synergistic effects of atenolol and amlodipine for lowering and stabilizing blood pressure in 2K1Crenovascular hypertensive rats

    Institute of Scientific and Technical Information of China (English)

    Fu-ming SHEN; He-hui XIE; Gang LING; Li-ping XU; Ding-feng SU

    2005-01-01

    Aim: To test the synergistic effects of atenolol and amlodipine on lowering blood pressure (BP) and reducing blood pressure variability (BPV) in 2-kidney, one-clip(2K1C) renovascular hypertensive rats. Methods: Forty-eight 2K1C renovascular hypertensive rats were randomly divided into 6 groups. They were respectively given 0.8% carboxymethylcellulose sodium (control), atenolol (10.0 mg/kg),amlodipine (1.0 mg/kg), and combined atenolol and amlodipine (low dose: 5.0+0.5mg/kg; intermediate dose: 10.0+ 1.0 mg/kg; high dose: 20.0+2.0 mg/kg). The drugs were given via a catheter in a gastric fistula. BP was recorded for 25 h from 1 h before drug administration to 24 h after administration. Results: Compared with BP before medication, all 3 doses of combined atenolol and amlodipine significantly decreased the BP at 24 h after administration, except for the low dose on diastolic BP. Compared with the control group, all 3 doses of combined atenolol and amlodipine significantly reduced the average BP levels for the 24 h period after administration; furthermore, the high and intermediate doses also significantly decreased the BPV levels for the same period. The q values calculated by probability sum analysis for systolic and diastolic BP for the 24 h period after administration were 2.29 and 1.45, respectively, and for systolic and diastolic BPV for the same period they were 1.41 and 1.60, respectively. Conclusion: There is significant synergism between atenolol and amlodipine in lowering and stabilizing BP in 2K1C renovascular hypertensive rats.

  6. Transdermal Iontophoretic Delivery of Atenolol in Combination with Penetration Enhancers: Optimization and Evaluation on Solution and Gels

    Directory of Open Access Journals (Sweden)

    Nandy B. C.

    2009-07-01

    Full Text Available In the present investigation, we prepared Atenolol (1.5 % w/w solution and various polymer formulations by incorporating the tween-20 or L-menthol, as a penetration enhancers and its effect on permeation of the drug through the excised abdominal rat skin were used to examined by using the vertical Franz-type diffusion cell. The physicochemical interactions between Atenolol and various polymers were investigated by performing the assay, ultra violet absorption maxima, Fourier transform infrared spectroscopy and it was further confirmed by thin layer chromatography studies, from which drug did not show any evidence of interaction with the polymers. We found that, L-menthol was superior than tween-20 to iontophoresis [current density applied 0.5 mA/cm2 and 90:10 (on: off ratio], in enhancing the transdermal permeation of Atenolol; it enhanced the flux of Atenolol by more than 2-folds, comparison to the preparations without penetration enhancer via passive diffusion, and 3 folds increased using iontophoresis alone with a shorter lag time. Atenolol also showed good stability in gel formulations. The basic parameters like % loading dose released at the end of the study, permeation coefficient and steady state flux (Jss were calculated and showed statistically significant difference (p<0.05. The results indicated that suitable iontophoretic delivery with desired permeability could be appeared and the cumulative amount-time curves were suitable to fit by a zero order equations which indicated a steady state permeation rate or sustained effect could be achieved from hydrogel; when it is combined with penetration enhancer, L-menthol. The results demonstrate that the semisolid gel formulations are more applicable than solution as a transdermal iontophoretic delivery system to administer clinically. Electrically assisted transdermal delivery of Atenolol significantly increased transport compared to passive delivery. Also, rapid and modulated delivery was

  7. Photochemical degradation of atenolol, carbamazepine, meprobamate, phenytoin and primidone in wastewater effluents.

    Science.gov (United States)

    Dong, Mei Mei; Trenholm, Rebecca; Rosario-Ortiz, Fernando L

    2015-01-23

    The photochemical degradation of five pharmaceuticals was examined in two secondary wastewater effluents. The compounds, which included atenolol, carbamazepine, meprobamate, phenytoin and primidone, were evaluated for both direct and sensitized photolysis. In the two wastewaters, direct photolysis did not lead to significant compound degradation; however, sensitized photolysis was an important removal pathway for the five pharmaceuticals. Upon solar irradiation, hydroxyl radical (HO) was quantified using the hydroxylation of benzene and singlet oxygen ((1)O2) formation was monitored following the degradation of furfuryl alcohol. Degradation via sensitized photolysis was observed following five-day exposures for atenolol (69-91%), carbamazepine (67-98%), meprobamate (16-52%), phenytoin (44-85%), and primidone (34-88%). Varying removal is likely a result of the differences in reactivity with transient oxidants. Averaged steady state HO concentrations ranged from 1.2 to 4.0×10(-16)M, whereas the concentrations of (1)O2 were 6.0-7.6×10(-14)M. Partial removal due to presence of HO indicates it was not the major sink for most compounds examined. Other transient oxidants, such as (1)O2 and triplet state effluent organic matter, are likely to play important roles in fates of these compounds. PMID:24798495

  8. Simultaneous enantioseparation and purity determination of chiral switches of amlodipine and atenolol by liquid chromatography.

    Science.gov (United States)

    Kannappan, Valliappan; Mannemala, Sai Sandeep

    2016-02-20

    A novel, selective and robust enantiospecific HPLC method was developed for simultaneous determination of amlodipine and atenolol enantiomers. Box-Behnken design was employed to identify the effect of factors (% ethanol, % diethylamine and flow rate) and their interactions on enantioresolution and analysis time. Chromatography was performed using mobile phase comprising acetonitrile, ethanol and DEA (92:8:0.2% v/v/v) delivered at a flow rate of 1.2mLmin(-1) on a Lux Cellulose-4 column. The enantiomers were monitored at a wavelength of 240nm and separation was achieved within 8min. The method was validated in terms of specificity, linearity, accuracy, precision, limit of detection and quantification. The method was found to be linear (R(2)≥0.991), accurate (99.8-101.4%) and precise (%RSD≤3%). Additionally, fractional factorial design was used to evaluate the robustness of the method and non-significant intervals for mixture related factors were established using contour profiling. Furthermore, the pertinence of this validated method was established by analyzing three different commercially available formulations. The obtained results confirmed that the proposed method can be extended for routine enantiopurity assay of amlodipine and atenolol in pharmaceutical formulations. PMID:26760239

  9. Kinetic, mechanistic and spectral investigation of ruthenium (III)-catalysed oxidation of atenolol by alkaline permanganate (stopped-flow technique)

    Indian Academy of Sciences (India)

    Rahamatalla M Mulla; Gurubasavaraj C Hiremath; Sharanappa T Nandibewoor

    2005-01-01

    Kinetics of ruthenium (III) catalyzed oxidation of atenolol by permanganate in alkaline medium at constant ionic strength of 0.30 mol dm3 has been studied spectrophotometrically using a rapid kinetic accessory. Reaction between permanganate and atenolol in alkaline medium exhibits 1 : 8 stoichiometry (atenolol : KMnO4). The reaction shows first-order dependence on [permanganate] and [ruthenium (III)] and apparently less than unit order on both atenolol and alkali concentrations. Reaction rate decreases with increase in ionic strength and increases with decreasing dielectric constant of the medium. Initial addition of reaction products does not affect the rate significantly. A mechanism involving the formation of a complex between catalyst and substrate has been proposed. The active species of ruthenium (III) is understood as [Ru(H2O)5OH]2+. The reaction constants involved in the different steps of mechanism are calculated. Activation parameters with respect to the slow step of the mechanism are computed and discussed and thermodynamic quantities are also calculated.

  10. DIFFERENTIAL-EFFECTS OF ENALAPRIL AND ATENOLOL ON PROTEINURIA AND RENAL HEMODYNAMICS IN NONDIABETIC RENAL-DISEASE

    NARCIS (Netherlands)

    APPERLOO, AJ; DEZEEUW, D; SLUITER, HE; DEJONG, PE

    1991-01-01

    Objective - To compare the antihypertensive, renal haemodynamic and antiproteinuric effect of enalapril and atenolol in patients with proteinuria of non-diabetic origin. Design - Prospective, double blind, randomised 16 week study after a pretreatment period of at least three weeks. Setting - Outpat

  11. Long-term treatment with losartan versus atenolol improves insulin sensitivity in hypertension: ICARUS, a LIFE substudy

    DEFF Research Database (Denmark)

    Olsen, Michael H; Fossum, Eigil; Høieggen, Aud;

    2005-01-01

    Hypertension and insulin resistance might be associated through peripheral vascular hypertrophy/rarefaction which compromises skeletal muscle blood flow and decreases glucose uptake, inducing insulin resistance. We hypothesized that treatment with losartan as compared to atenolol would improve...... insulin sensitivity through regression of peripheral vascular hypertrophy/rarefaction....

  12. Titrimetric, spectrophotometric and kinetic methods for the assay of atenolol using bromate–bromide and methyl orange

    Directory of Open Access Journals (Sweden)

    KANAKAPURA BASAVAIAH

    2006-05-01

    Full Text Available Three new methods have been developed for the determination of atenolol in bulk drug and in tablet formulation. The methods are based on the oxidation–bromination reaction of the drug by bromine, generated in situ by the action of acid on a bromate–bromide mixture. In the titrimetric method, the drug is treated with a known excess of bromate–bromide mixture in hydrochloric acid medium, followed by the determination of the unreacted bromine iodometrically. The spectrophotometric method involves the addition of a measured excess of bromate–bromide reagent in hydrochloric acid medium to atenolol, and after ensuring the reaction had gone to completion, the unreacted bromine is treated with a fixed amount of methyl orange, and absorbance measured at 520 nm. The absorbance was found to increase linearly with increasing concentration of atenolol. The kinetic method depends on the existence of a linear relationship between the concentration of the drug and the time of the oxidation–bromination reaction, as indicated by the bleaching of methyl orange acid colour. The working conditions were optimized. The titrimetric method is based on a 1:1 reaction stoichiometry (atenolol:bromate and is applicable over the 3–20 mg range. The spectrophotometric method permits micro determination of the drug (0.5–4.0 mg ml-1with an apparentmolar absorptivity of 4.13x104 lmol-1 cm-1 and detection limit of 0.07 mg ml-1. The kinetic method is applicable in the concentration range 5–25 mg ml-1 with a detection limit of 3.72 mg ml-1. The proposed methods were successfully applied to the determination of atenolol in tablet preparations with mean recoveries of 97.63 to 101.78 %. The reliability of the assay was established by parallel determination by the reference method and by recovery studies using the standard addition technique.

  13. Photochemical degradation of atenolol, carbamazepine, meprobamate, phenytoin and primidone in wastewater effluents

    Energy Technology Data Exchange (ETDEWEB)

    Dong, Mei Mei [Civil, Environmental and Architectural Engineering, 428 UCB, University of Colorado, Boulder, CO 80309 (United States); Southern Nevada Water Authority (SNWA), P.O. Box 99954, Las Vegas, NV 89193-9954 (United States); Trenholm, Rebecca [Southern Nevada Water Authority (SNWA), P.O. Box 99954, Las Vegas, NV 89193-9954 (United States); Rosario-Ortiz, Fernando L., E-mail: Fernando.rosario@colorado.edu [Civil, Environmental and Architectural Engineering, 428 UCB, University of Colorado, Boulder, CO 80309 (United States)

    2015-01-23

    Highlights: • The photochemical degradation of 5 compounds was evaluated in wastewater effluents. • Attenuation by sensitized photolysis was the most important degradation pathway. • Hydroxyl radical accounted for most of the degradation for aliphatic compounds. • Other transient oxidants could also significantly impact the degradation of the compounds. - Abstract: The photochemical degradation of five pharmaceuticals was examined in two secondary wastewater effluents. The compounds, which included atenolol, carbamazepine, meprobamate, phenytoin and primidone, were evaluated for both direct and sensitized photolysis. In the two wastewaters, direct photolysis did not lead to significant compound degradation; however, sensitized photolysis was an important removal pathway for the five pharmaceuticals. Upon solar irradiation, hydroxyl radical (HO·) was quantified using the hydroxylation of benzene and singlet oxygen ({sup 1}O{sub 2}) formation was monitored following the degradation of furfuryl alcohol. Degradation via sensitized photolysis was observed following five-day exposures for atenolol (69–91%), carbamazepine (67–98%), meprobamate (16–52%), phenytoin (44–85%), and primidone (34–88%). Varying removal is likely a result of the differences in reactivity with transient oxidants. Averaged steady state HO· concentrations ranged from 1.2 to 4.0 × 10{sup −16} M, whereas the concentrations of {sup 1}O{sub 2} were 6.0–7.6 × 10{sup −14} M. Partial removal due to presence of HO· indicates it was not the major sink for most compounds examined. Other transient oxidants, such as {sup 1}O{sub 2} and triplet state effluent organic matter, are likely to play important roles in fates of these compounds.

  14. Contribution of beta 1- and beta 2-adrenoceptors of human atrium and ventricle to the effects of noradrenaline and adrenaline as assessed with (-)-atenolol.

    OpenAIRE

    Lemoine, H.; Schönell, H.; Kaumann, A. J.

    1988-01-01

    1. (-)-Atenolol was used as a tool to assess the function of beta 1- and beta 2-adrenoceptors in human heart. Right atrial and left ventricular preparations from patients undergoing open heart surgery were set up to contract isometrically. Membrane particles were prepared for beta-adrenoceptor labelling with [3H]-(-)-bupranolol and adenylate cyclase assays. 2. The positive inotropic effects of (-)-noradrenaline were antagonized to a similar extent by (-)-atenolol in atrial and ventricular pre...

  15. DEVELOPMENT AND VALIDATION OF A UV SPECTROPHOTOMETRIC METHOD FOR THE SIMULTANEOUS DETERMINATION OF NIFEDIPINE AND ATENOLOL IN COMBINED DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Shelke O. S.

    2012-04-01

    Full Text Available Simultaneous estimation and validation of developed method of Nifedipine (NIF and Atenolol (ATN in combined dosage form as well as in laboratory mixture is studied under this paper. Nifedipine and Atenolol are used in combined dosage form for Cardiovascular System Diseases.The compound was identified by taking the IR spectra. The method is applied for laboratory mixture and marketed tablet. The developed method was validated as per ICH guidelines using the parameter such as accuracy, linearity and range, ruggedness, limit of detection & quantification, robustness, and precisión. Precisión was analysed by taking Reading interday and Intraday. Ruggedness was analysed by differant analyst and robustness by changing the solvent composition.

  16. Competitive sorption of atenolol, trimetoprim, carbamazepine and sulfamethoxazole in three soil types

    Science.gov (United States)

    Kočárek, Martin; Kodešová, Radka; Klement, Aleš; Golovko, Oksana; Fér, Miroslav; Nikodem, Antonín; Vondráčková, Lenka; Jakšík, Ondřej; Grabic, Roman

    2016-04-01

    Transport of human and veterinary pharmaceuticals in soils and consequent ground-water contamination are influenced by many factors, including compound sorption on soil particles and dissipation. Batch sorption experiment for 9 soils (3 soil types with 3 (Greyic Phaeozem on loess), 4 (Haplic Luvisol on loess) and 2 (Haplic Cambisol on gneiss) horizons) and mixture of 4 pharmaceuticals (atenolol, trimetoprim, carbamazepine and sulfamethoxazole) was performed to study competitive sorption of compounds in each soil sample. Sorption affinities and dissipation half-lives of all compounds in topsoils were previously studied by Kodešová et al. (2015 and 2016). Ten grams of dry soil was placed directly into the plastic centrifuge tubes and 20 ml of solution of a known pharmaceutical concentration was added. The same concentrations (0.5, 1, 2.5, 5 and 10 mg/l) were used for all compounds. Three replicates of each concentration were applied for each soil. Tube was shaken for 24 h using the shaking apparatus at 20 C. After shaking, the analyzed soil suspension was centrifuged for 10 min at 6,000 rotations per minute. The actual initial and final equilibrium pharmaceutical concentrations were measured using two-dimensional liquid chromatography-tandem mass spectrometry LC/LC-MS/MS using isotope dilution and internal standard methods. The pharmaceutical concentration adsorbed on soil particles was calculated using the initial and final (i.e. after incubation) pharmaceutical concentrations. The Freundlich equations were used to fit data points of the measured adsorption isotherms. In the case of carbamazepine (neutral form) and sulfamethoxazole (partly negatively charged) sorption affinity of compounds decrease with soil depth. On the other hand in the case of atenolol and trimethoprim (both positively charged) compound sorption affinity was not depth dependent. Data obtained for top soils were compared with sorption affinities for single compounds published by (Kodešová et

  17. Formulation development and evaluation of controlled porosity osmotic pump delivery system for oral delivery of atenolol

    Directory of Open Access Journals (Sweden)

    Garvendra S Rathore

    2012-01-01

    Full Text Available In the present study, we developed and evaluated the controlled porosity osmotic pump (CPOP based drug delivery system of sparingly water soluble drug atenolol (ATL. We selected target release profile and optimized different variables to help us achieve this. Formulation variables, such as, the levels of solubility enhancer (0-15% w/w of drug, ratio of the drug to the osmogents, coat thickness of the semipermeable membrane (SPM and level of pore former (0-20% w/w of polymer were found to effect the drug release from the developed formulations. Cellulose acetate (CA 398-10 was used as the semipermeable membrane containing polyethylene glycol 400 as the Cplasticizer. ATL release was directly proportional to the level of the solubility enhancer, osmotic pressure generated by osmotic agent and level of pore former; however, was inversely proportional to the coat thickness of SPM. Drug release from developed formulations was independent of the pH and agitation intensities of release media. Burst strength of the exhausted shells decreased with increase in the level of pore former. The optimized formulations were subjected to stability studies as per International Conference on Harmonisation (ICH guidelines, and formulations were found to be stable after 3 months study. Steady-state plasma levels of drug were predicted by the method of superposition.

  18. Formulation and evaluation of atenolol floating bioadhesive system using optimized polymer blends

    Science.gov (United States)

    Siddam, Haritha; Kotla, Niranjan G.; Maddiboyina, Balaji; Singh, Sima; Sunnapu, Omprakash; Kumar, Anil; Sharma, Dinesh

    2016-01-01

    Introduction: Oral sustained release gastro retentive dosage forms offer several advantages for drugs having absorption from the upper gastrointestinal tract to improve the bioavailability of medications which have narrow absorption window. The aim of the study was to develop a floating bioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong the residence in the stomach using atenolol as a model drug. Methods: Prior to compression, polymeric blend(s) were evaluated for flow properties. The tablets were prepared by direct compression method using bioadhesive polymer like Carbopol 934P and hydrophilic polymers like HPMC K4M, HPMC K15M, and HPMC K100M. The prepared tablets were evaluated for physical characteristics, bioadhesive strength, buoyancy lag time, swelling index and in vitro drug release studies. Results: The mean bioadhesive strength was found to be in the range of 16.2 to 52.1 gm. The optimized blend (F11) showed 92.3% drug releases after 24 hrs. Whilst, increase in concentration of carbopol 934P, bioadhesive strength and swelling index was increased with slow release. The n values of optimized formulations were found in the range of 0.631-0.719 indicating non-fickian anomalous type transport mechanism. Conclusion: The study aided in developing an ideal once-a-day gastro retentive floating drug delivery system with improved floating, swelling and bioadhesive characteristics with better bioavailability. PMID:27051631

  19. Degradation of atenolol by UV/peroxymonosulfate: kinetics, effect of operational parameters and mechanism.

    Science.gov (United States)

    Liu, Xiaowei; Zhang, Tuqiao; Zhou, Yongchao; Fang, Lei; Shao, Yu

    2013-11-01

    Photoactivation of peroxymonosulfate (PMS) with UV (254nm) irradiation was used to generate the SO4(-)-based advanced oxidation process, which was adopted to degrade atenolol (ATL) in water. The second-order reaction rate constants of ATL with HO and SO4(-) were determined, and the effects of operational parameters (dose of PMS, solution pH, HCO3(-), humic acids (HA), and N2 bubbling) were evaluated as well. Finally the main transformation intermediates were identified and possible degradation pathways were proposed. The results showed that there was a linear positive correlation between the degradation rate of ATL and specific dose of PMS (1-16M PMS/M ATL). Increasing solution pH from 3 to 9 promoted elimination of ATL due to the pH-dependent effect of PMS photodecomposition, while further pH increase from 9 to 11 caused slowing down of degradation because of apparent conversion of HO to SO4(-). 1-8mM HCO3(-) exerted no more than 5.3% inhibition effect on ATL destruction, suggesting HCO3(-) was a weak inhibitor. Absorption (or complexation) and photosensitized oxidation induced by HA improved ATL degradation during the first minute of degradation process, whereas photon competition and radical scavenging effects became the leading role afterward. Bubbling with nitrogen enhanced the degradation rate due to the stripping of dissolved oxygen. Hydroxylation of aromatic ring, cleavage of ether bond, oxidation of primary and secondary amine moieties, and dimerization were involved in the degradation mechanism of ATL by UV/PMS.

  20. Characterization of a new degradation product of nifedipine formed on catalysis by atenolol: A typical case of alteration of degradation pathway of one drug by another.

    Science.gov (United States)

    Handa, Tarun; Singh, Saranjit; Singh, Inder Pal

    2014-02-01

    An increasing interest is being shown throughout the world on the use of fixed-dose combinations of drugs in the therapy of select diseases, like cardiovascular diseases, due to their multiple advantages. Though the main criterion for combining drugs in a single dosage form is the rationale, but consideration like stability of formulation is equally important, due to an added aspect of drug-drug interaction. The objective of this study was to evaluate interaction among the drugs in an antihypertensive combination of nifedipine and atenolol. Nifedipine is a known light sensitive drug, which degrades via intra-molecular mechanisms to nitro- and nitroso-pyridine analogs, along with a few minor secondary products that are formed through inter-molecular interactions amongst primary degradation products and their intermediates. Atenolol is reasonably stable weakly basic drug that is mainly hydrolyzed at acetamide terminal amide moiety to its corresponding carboxylic acid. To the best of our knowledge, there is no known information on chemical compatibility among the two drugs. The present study involved subjecting of nifedipine, atenolol and their combination to a variety of accelerated and stress conditions. HPLC studies revealed formation of a new product in the mixture of two drugs (∼2%), which was also generated from nifedipine alone, but at trace levels (<0.1%). The product was isolated by preparative chromatography and subjected to indepth studies for its characterization. Ultra-violet, FT-IR, mass spectrometric and nuclear magnetic resonance spectroscopic studies highlighted that the principal photo-degradation pathway of nifedipine was modified and diverted in the presence of atenolol. To verify the same, a study was conducted employing two other β-blockers with similar structures to atenolol, and the same product was formed in relatively higher quantity therein also. The new product is postulated to be produced as a result of rearrangement of hydroxylamine

  1. Effects of combination therapy with atenolol and amlodipine on blood pressure control and stroke prevention in stroke-prone spontaneously hypertensive rats

    Institute of Scientific and Technical Information of China (English)

    Gang LING; Ai-jun LIU; Fu-ming SHEN; Guo-jun CAI; Jian-guo LIU; Ding-feng SU

    2007-01-01

    Aim:To test the effects of atenolol and amlodipine,either alone or in combination,on blood pressure,blood pressure variability (BPV),baroreflex sensitivity (BRS),and the prevalence of stroke in stroke-prone spontaneously hypertensive rats (SHR-SP). Methods:In the first set of the study,24 8-month-old,female SHR-SP rats were randomly divided into 3 groups. Blood pressure,heart period,and BRS were determined before and after the intragastric administration of atenolol (10 mg/kg) and amlodipine (1.0 mg/kg),either alone or in combination. In the second set of the study,40 male and 40 female rats were randomly assigned to 1 of the and both (10 male and 10 female in each group). The stroke incident and survival time were recorded. Results:Atenolol and amlodipine,either alone or in combination,significantly decreased blood pressure,with the exception of the amlodipine-induced effect on diastolic blood pressure. Meanwhile,only the combination treatment significantly decreased the BPV levels for the same period.The q-values calculated by the probability sum analysis were 1.17 and 2.67 for systolic and diastolic blood pressure,respectively,and were 2.48 and 2.10 for systolic and diastolic BPV,respectively,following administration. Neither drug exhibited any significant effect on BRS. Atenolol and amlodipine,either alone or in combination,significantly increased the lifespan of SHR-SP,with the best effeet elicited by the combination therapy. Conclusion:A significant synergism exists between atenolol and amlodipine in lowering and stabilizing blood pressure in SHR-SP. Combination therapy may be an optimal strategy for the prevention of stroke in hypertension.

  2. Avaliação do teor de Atenolol em comprimidos divididos com faca caseira e aparelho cortador Evaluación de la proporción de Atenolol en comprimidos divididos con cuchillo casero y con cortador Evaluation of the content of Atenolol tablets divided with a knife and homemade machine cutter

    Directory of Open Access Journals (Sweden)

    Mariangela Tirico Auricchio

    2011-01-01

    Full Text Available OBJETIVO: Avaliar se o teor de Atenolol em fragmentos de comprimidos nas dosagens de 100 mg, 50 mg e 25 mg partidos em duas e quatro partes com auxílio de faca caseira e de aparelho cortador de comprimidos é diferente em função do modo como a divisão é realizada. MÉTODOS: Os comprimidos íntegros foram divididos com faca caseira e com aparelho cortador de comprimidos, e os teores de Atenolol foram determinados em todos os fragmentos. RESULTADOS: Não houve diferença significativa entre os teores obtidos, após divisão dos comprimidos com faca caseira ou com aparelho cortador, apesar da divisão levar a acentuada dispersão dos teores entre os fragmentos, na divisão em metade, a dispersão dos resultados deu-se entre 7,8% e 12,1%, e quando divididos em quatro partes, foi entre 9,2% e 21,1%, indicando a possibilidade de comprometer a eficácia do tratamento dos pacientes independente de como a divisão foi feita. CONCLUSÃO: Os resultados indicaram a ocorrência de dispersão maior do que a estabelecida para garantir uniformidade da dose recebida a cada administração do medicamento independente da forma de realizar a divisão, seja por meio de faca caseira ou com aparelho cortador de comprimidos.OBJETIVO: Evaluar si la proporción de Atenolol en fragmentos de comprimidos en las dosis de 100 mg, 50 mg y 25 mg partidos en dos y cuatro partes con la ayuda de un cuchillo casero y de un cortador de comprimidos es diferente en función al modo cómo se realiza la división. MÉTODOS: Los comprimidos enteros fueron divididos con un cuchillo casero y con un cortador de comprimidos, siendo determinadas las proporciones de Atenolol en todos los fragmentos. RESULTADOS: No hubo diferencia significativa entre las proporciones obtenidas, después de la división de los comprimidos tanto con cuchillo casero como con el cortador. A pesar de que la división lleve una acentuada dispersión de las proporciones entre los fragmentos, en la división por

  3. Excimer formation in inclusion complexes of β-cyclodextrin with salbutamol, sotalol and atenolol: Spectral and molecular modeling studies

    Science.gov (United States)

    Antony Muthu Prabhu, A.; Subramanian, V. K.; Rajendiran, N.

    2012-10-01

    The inclusion complexation behavior of salbutamol, sotalol and atenolol drugs with β-cyclodextrin (β-CD) were investigated by UV-visible, fluorometry, time resolved fluorescence, FT-IR, 1H NMR, SEM and PM3 methods. The above drugs gave a single emission maximum in water where as dual emission in β-CD. In β-CD solutions the shorter wavelength fluorescence intensity was regularly decreased and longer wavelength fluorescence intensity increased. Addition of β-CD to aqueous solutions of drugs resulted into excimer emission. The excimer emission is concluded to be due to a 1:2 inclusion complex between β-CD and drug. Nanosecond time-resolved studies indicated that all drugs exhibited biexponential decay in solvents and triexponential decay in CD. Investigations of thermodynamic and electronic properties confirmed the stability of the inclusion complex.

  4. Potentiometric study of atenolol as hypertension drug with Co(II, Ni(II, Cu(II and Zn(II transition metal ions in aqueous solution

    Directory of Open Access Journals (Sweden)

    Abdulbaset A. Zaid

    2015-01-01

    Full Text Available Binary and ternary complexes of Co(II, Ni(II, Cu(II and Zn(II with atenolol as hypertension drug and glycine have been determined pH metrically at room temperature and 0.01 M ionic strength (NaClO4 in aqueous solution. The formation of various possible species has been evaluated by computer program and discussed in terms of various relative stability parameters.

  5. Effects of losartan compared with atenolol on lipids in patients with hypertension and left ventricular hypertrophy: the Losartan Intervention For Endpoint reduction in hypertension study

    DEFF Research Database (Denmark)

    Olsen, Michael Hecht; Wachtell, Kristian; Beevers, Gareth;

    2009-01-01

    OBJECTIVE: Beta-blockers and angiotensin II receptor blockers have different effects on lipids. METHODS: We examined lipid levels in the Losartan Intervention For Endpoint reduction in hypertension study and their impact on the primary composite endpoint of cardiovascular death, myocardial...... infarction, or stroke. We measured total and high-density lipoprotein cholesterol at baseline and annually during 4.8 years of losartan-based compared with atenolol-based treatment in 8611 patients with hypertension and left ventricular hypertrophy. RESULTS: Patients randomized to losartan-based or atenolol...... decreased less during the first 2 years in patients randomized to losartan compared with atenolol (-0.13 +/- 0.24 vs. -0.19 +/- 0.25 mmol/l) and remained higher each year (1.38, 1.37, 1.42, 1.47, and 1.48 mmol/l vs. 1.32, 1.30, 1.36, 1.40, and 1.42 mmol/l, all P

  6. Comparison of UV/PDS and UV/H2O2 processes for the degradation of atenolol in water

    Institute of Scientific and Technical Information of China (English)

    Xiaowei Liu; Lei Fang; Yongchao Zhou; Tuqiao Zhang; Yu Shao

    2013-01-01

    UV/H2O2 and UV/peroxodisulfate (PDS) processes were adopted to degrade a typical β-blocker atenolol (ATL).The degradation efficiencies under various operational parameters (oxidant dosage,pH,HCO3-,humic acid (HA),NO3-,and Cl-) were compared.Principal factor analysis was also performed with a statistical method for the two processes.It was found that increasing the specific dosage of the two peroxides ([peroxide]0/[ATL]0) ranging from 1∶1 to 8∶1 led to a faster degradation rate but also higher peroxide residual.Within the pH range 3-11,the optimum pH was 7 for the UV/PDS process and elevating pH benefitted the UV/H2O2 process.The presence of HCO3-,HA,and Cl-adversely affected ATL oxidation in both processes.The NO3-concentration 1-3 mmol/L accelerated the destruction of ATL by the UV/PDS process,but further increase of NO3-concentration retarded the degradation process,contrary to the case in the UV/H2O2 process.The rank orders of effects caused by the six operational parameters were pH ≈ specific dosage > [HA]0 > [NO3-]0 > [HCO3-]0 > [Cl-]0 for the UV/H2O2 process and specific dosage > pH > [HA]0 > [NO3-]0 > [HCO3-]0 >[Cl-]0 for the UV/PDS process.The UV/PDS process was more sensitive to changes in operational parameters than the UV/H2O2 process but more efficient in ATL removal under the same conditions.

  7. Sensitive Spectrophotometric Determination of Atenolol in Pharmaceutical Formulations Using Bromate-Bromide Mixture as an Eco-Friendly Brominating Agent

    Directory of Open Access Journals (Sweden)

    Kudige N. Prashanth

    2012-01-01

    Full Text Available Three simple and sensitive spectrophotometric methods are proposed for the determination of atenolol (ATN in bulk drug and tablets. The methods are based on the bromination of ATN by the bromine generated in situ by the action of the acid on the bromate–bromide mixture followed by the determination of unreacted bromine by reacting with a fixed amount of either meta-cresol purple (MCP and measuring the absorbance at 540 nm (method A and 445 nm (method B or erioglaucine (EGC and measuring the absorbance at 630 nm (method C. Beer's law is valid within the concentration ranges of 1.0–20.0, 2.0–40.0 and 1.0–8.0 μg/mL for method A, method B and method C, respectively. The calculated molar absorptivities were found to be 1.20×104, 4.51×103 and 3.46×104  L/mol⋅cm for method A, method B and method C, respectively. Sandell’s sensitivity values, correlation coefficients, limits of detection and quantification are also reported. Recovery results were statistically compared with those of a reference method by applying Student’s t- and F-test. The novelty of the present study is the measurement of two different colors using MCP, that is, red-pink color of MCP in acid medium at 540 nm and yellowish-orange color of brominated MCP at 445 nm.

  8. Atenolol Reduces Leishmania major-Induced Hyperalgesia and TNF-α Without Affecting IL-1β or Keratinocyte Derived Chemokines (KC)

    Science.gov (United States)

    Karam, Marc C.; Merckbawi, Rana; Salman, Sara; Mobasheri, Ali

    2016-01-01

    Infection with a high dose of the intracellular parasitic protozoan Leishmania major induces a sustained hyperalgesia in susceptible BALB/c mice accompanied by up-regulation of the pro-inflammatory cytokines IL-1β and IL-6. Interleukin-13 (IL-13) has been shown to reduce this hyperalgesia (despite increased levels of IL-6) and the levels of IL-1β during and after the treatment period. These findings favor the cytokine cascade leading to the production of sympathetic amines (involving TNF-α and KC) over prostaglandins (involving IL-lβ and IL-6) as the final mediators of hyperalgesia. The aim of this study was to investigate the effect of daily treatment with the β-blockers atenolol on L. major-induced inflammation in mice with respect to hyperalgesia as well as the levels of TNF-α and KC (the analog of IL-8 in mice). Our data demonstrates that atenolol is able to reduce the L. major induced sustained peripheral hyperalgesia, which does not seem to involve a direct role for neither IL-lβ nor KC. Moreover, our results show that TNF-α may play a pivotal and direct role in sensitizing the peripheral nerve endings (nociceptors) since its level was reduced during the period of atenolol treatment, which correlates well with the reduction of the observed peripheral, but not central, hyperalgesia. These findings contribute to a better understanding of the cytokine cascade leading to hyperalgesia and may lead to the development of new and more efficient medications for many types of pain. PMID:26913003

  9. Determination of atenolol in human plasma using ionic-liquid-based ultrasound-assisted in situ solvent formation microextraction followed by high-performance liquid chromatography.

    Science.gov (United States)

    Zeeb, Mohsen; Farahani, Hadi; Papan, Mohammad Kazem

    2016-06-01

    An efficient analytical method called ionic-liquid-based ultrasound-assisted in situ solvent formation microextraction followed by high-performance liquid chromatography was developed for the determination of atenolol in human plasma. A hydrophobic ionic liquid (1-butyl-3-methylimidazolium hexafluorophosphate) was formed by the addition of a hydrophilic ionic liquid (1-butyl-3-methylimidazolium tetrafluoroborate) to a sample solution containing an ion-pairing agent during microextraction. The analyte was extracted into the ionic liquid phase while the microextraction solvent was dispersed throughout the sample by utilizing ultrasound. The sample was then centrifuged, and the extracting phase retracted into the microsyringe and injected to liquid chromatography. After optimization, the calibration curve showed linearity in the range of 2-750 ng/mL with the regression coefficient corresponding to 0.998. The limits of detection (S/N = 3) and quantification (S/N = 10) were 0.5 and 2 ng/mL, respectively. A reasonable relative recovery range of 90-96.7% and satisfactory intra-assay (4.8-5.1%, n = 6) and interassay (5.0-5.6%, n = 9) precision along with a substantial sample clean-up demonstrated good performance of the procedure. It was applied for the determination of atenolol in human plasma after oral administration and some pharmacokinetic data were obtained.

  10. Stability of Atenolol, Clonazepam, Dexamethasone, Diclofenac Sodium, Diltiazem, Enalapril Maleate, Ketoprofen, Lamotrigine, Penicillamine-D, and Thiamine in SyrSpend SF PH4 Oral Suspensions.

    Science.gov (United States)

    Polonini, Hudson C; Loures, Sharlene; Lima, Luis Claudio; Ferreira, Anderson O; Brandão, Marcos Antônio F

    2016-01-01

    The objective of this study was to evaluate the stability of 10 commonly used active pharmaceutical ingredients compounded in oral suspensions using SyrSpend SF PH4 (atenolol 1.0 and 5.0 mg/mL, clonazepam 0.2 mg/mL, dexamethasone 1.0 mg/mL, diclofenac sodium 5.0 mg/mL, diltiazem 12.0 mg/mL, enalapril maleate 1.0 mg/mL, ketoprofen 20.0 mg/mL, lamotrigine 1.0 mg/mL, penicillamine-D 50.0 mg/mL, thiamine 100 mg/m) and stored both at controlled refrigerated (2°C to 8°C) and room temperature (20°C to 25°C). Stability was assessed by means of measuring percent recovery at varying time points throughout a 90-day period. The quantification of the active pharmaceutical ingredients was performed by a stability-indicating, high-performance liquid chromatographic method. The beyond-use date of the products was found to be at least 90 days for all suspensions (except atenolol 1 mg/mL, which was stable up to 60 days), both for controlled refrigerated temperature and room temperature. This confirms that SyrSpend SF PH4 is a stable suspending vehicle for compounding with a broad range of different active pharmaceutical ingredients. PMID:27323429

  11. Effects of Long-term Use of Polyphenols on the Absorption and Tissue Distribution of Orally Administered Metformin and Atenolol in Rats

    Directory of Open Access Journals (Sweden)

    Saad Abdulrahman Hussain

    2013-06-01

    Full Text Available Aim: To evaluate the effect of long-term use of silibinin, epigallocatechin (ECGC, quercetin and rutin on the absorption and tissue distribution of metformin and atenolol. Materials and Methods: Thirty male rats were used, allocated into 5 groups and treated as follow: 1st group treated with olive oil and served as control; the other 4 groups were treated with either silibinin, EPGC, quercetin or rutin, administered orally as oily solutions for 30 days. At day 30, a 300mg/kg metformin and 50mg/kg atenolol were administered orally; 3.0 hrs later, the animals were sacrificed and blood samples, tissues of brain, kidney and liver were obtained for evaluation of the drugs level. Results: The polyphenols increased both serum and tissue levels of metformin compared with controls. This effect was relatively varied according to the structural differences among flavonoids. Conclusion: Long-term use of supraphysiological doses of flavonoids increase absorption of Zn, Cu and Fe and their tissue availability in brain, kidney and liver; this effect seems to be different with variations in structural features. [J Intercult Ethnopharmacol 2013; 2(3.000: 147-154

  12. An economic assessment of losartan-based versus atenolol-based therapy in patients with hypertension and left-ventricular hypertrophy : Results from the Losartan Intervention For Endpoint reduction (LIFE) study adapted to The Netherlands

    NARCIS (Netherlands)

    Boersma, Cornelis; Carides, George W.; Atthobari, Jarir; Voors, Adriaan A.; Postma, Maarten J.

    2007-01-01

    Background: The Losartan Intervention For Endpoint reduction (LIFE) study was a randomized, doubleblind trial that compared the effects of losartan-based treatment with those of atenolol-based treatment on cardiovascular disease (CVD)-related morbidity and mortality in 9193 patients with hypertensio

  13. Comparative evaluation of atenolol and clonidine premedication on cardiovascular response to nasal speculum insertion during trans-sphenoid surgery for resection of pituitary adenoma: A prospective, randomised, double-blind, controlled study

    Directory of Open Access Journals (Sweden)

    Devendra Gupta

    2011-01-01

    Full Text Available Severe cardiovascular responses in the form of tachycardia and hypertension following nasal speculum insertion occur during sublabial rhinoseptal trans-sphenoid approach for resection of small pituitary tumours. We compare the effects of preoperative administration of clonidine (α-2 agonist and atenolol (α-blocker over haemodynamic response, caused by speculum insertion during trans-sphenoid pituitary resection. We enrolled 66 patients in age range 18-65 years, of ASA I-II, and of either sex undergoing elective sublabial rhinoseptal trans-sphenoidal hypophysectomy. Group I (control received placebo, group II (clonidine received tablet clonidine 5 μg/kg, and group III (atenolol received tablet atenolol 0.5 mg/kg. The heart rate increased on speculum insertion and 5 and 10 minutes following speculum insertion as compared to the pre-speculum values in the control group, while no change in the heart rate was observed in other groups (P<0.05. There was a rise in the mean arterial pressure during and 5, 10, and 15 minutes after nasal speculum insertion in the control group, whereas it was not seen in other groups (P<0.05. We therefore suggest that oral clonidine and oral atenolol (given 2 hours prior to surgery is an equally effective and safe method of attenuating haemodynamic response caused by nasal speculum insertion during trans-sphenoid pituitary resection.

  14. Efeitos da associação da estimulação atrial dinâmica em duplo sítio atrial com atenolol na prevenção da fibrilação atrial recorrente Effects of the association of dual-site dynamic atrial overdrive and atenolol in preventing recurrent atrial fibrillation

    Directory of Open Access Journals (Sweden)

    Antonio da Silva Menezes Júnior

    2007-01-01

    Full Text Available OBJETIVO: Avaliar os efeitos da estimulação atrial otimizada (EAO (estimulação duplo-sítio atrial, freqüência acima da intrínseca e algoritmo funcional específico e uso de atenolol, na prevenção da fibrilação atrial (FA recorrente. Desfecho primário: quantificar a taxa de episódios de FA. Desfechos secundários: qualidade de vida, avaliação de sintomas específicos cardiovasculares, taxa de internações hospitalares, taxa de cardioversões elétricas e farmacológicas e eventos cardíacos adversos. MÉTODOS: Vinte e sete pacientes com FA paroxística recorrente e doença do nó sinusal foram submetidos ao implante de marcapasso duplo-sítio atrial e ventricular e iniciaram com atenolol 100 mg/dia, a seguir foram randomizados em dois grupos, grupo I (3 meses iniciais com EAO e algoritmo especifico ligado e mais 3 com o mesmo desligado e grupo II (seqüência inversa do grupo I. O modo de estimulação foi DDDR e após 3 meses, foram submetidos à avaliação clínica e eletrônica do sistema de estimulação - mudança automática de modo (AMS, Holter de 24 horas, ecocardiograma e questionário SF-36. Em seguida, foram cruzados e após 6 meses, nova avaliação. RESULTADOS: Pacientes com EAO, quando comparados ao grupo com algoritmo desligado, apresentaram menores taxas de: FA/semana (pOBJECTIVE: Evaluate the effects of optimized atrial stimulation - OAS (dual-site atrial pacing, heart rate above the intrinsic rate, and specific functional algorithm, and the use of atenolol in preventing recurrent atrial fibrillation (AF. Primary endpoint: to quantify the rate of AF episodes. Secondary endpoints: assessment of quality of life, specific cardiovascular symptoms, rate of hospital admissions, rate of electrical and pharmacological cardioversions, and adverse cardiac events. METHODS: Twenty-five patients with recurrent episodes of paroxysmal AF and sinus node disease had dual-site atrial and ventricular pacemakers implanted, and were

  15. [Gallopamil and chlorthalidone versus atenolol and chlorthalidone in the treatment of obstructive hypertrophic cardiomyopathy in patients with arterial hypertension: polycardiographic evaluation of the systolic and diastolic function of the left ventricle].

    Science.gov (United States)

    Chieppa, S; Lobascio, C; Brandini, V; Iarussi, D; Giuliani, F; Langella, S; De Simone, R

    1989-08-01

    In 13 patients, affected by hypertrophic obstructive cardiomyopathy (HOCM) and essential hypertension, antihypertensive-efficacy and effects of a new calcium-channel blocker (gallopamil) associated with a diuretic agent (chlorthalidone) on left ventricular systolic and diastolic performance assessed by phonocardiographic methods. The results were compared to those obtained, in the same group of patients, with a selective beta-blocker (atenolol) associated with the same diuretic agent (chlorthalidone). With both therapeutic regimens a statistically significant reduction of systolic and diastolic arterial pressure was observed; both agents were able to reduce hemodynamic gradient in systole which characterize HOCM; however, the treatment with gallopamil plus chlorthalidone determined greater effects on left ventricular diastolic function as compared to the treatment with atenolol plus chlorthalidone; both treatments determined bradycardia. PMID:2605580

  16. Different effects of calcium antagonist and beta-blocker therapy on left-ventricular diastolic function in ischemic heart disease. A direct comparison of the impact of mibefradil and atenolol

    DEFF Research Database (Denmark)

    Hassager, C; Thygesen, K; Grande, P;

    2001-01-01

    OBJECTIVE: To compare the effect of a calcium antagonist and a beta-blocker on left-ventricular diastolic function in patients with ischemic heart disease. METHODS: 138 patients with chronic stable angina pectoris were randomized in a multicenter, double-blind trial to treatment with either...... mibefradil or atenolol for 6 weeks (50 mg once daily for 2 weeks followed by 100 mg once daily for 4 weeks). The ratio between early (E) and late (A) diastolic mitral flow velocities (E/A), the E wave deceleration time (DT) and the left ventricular isovolumetric relaxation time (IRT) were measured by Doppler...... echocardiography as parameters of left-ventricular diastolic function initially, after 4 and after 6 weeks of treatment. RESULTS: Mibefradil did not change the E/A ratio significantly (+4%, NS), while atenolol treatment resulted in a significant increase in the E/A ratio (+20%, p treatment...

  17. Influence of Losartan and Atenolol on Cardiovascular and Cerebrovascular Events: An Evidence-Based Analysis%氯沙坦与阿替洛尔对心脑血管事件影响的循证分析

    Institute of Scientific and Technical Information of China (English)

    杨莉萍; 刘瑶; 谢婧; 胡欣

    2013-01-01

    目的 为《中国基本药物目录》遴选血管紧张素Ⅱ受体阻断剂(ARB)类降压药物提供循证研究数据.方法 以losartan、atenolol、clinical trial、氯沙坦、阿替洛尔、临床试验为检索词,计算机检索EMbase、PubMed、Cochrane图书馆、Clinicaltrials.gov、CNKI、VIP和CBM,纳入氯沙坦与阿替洛尔治疗高血压相关的临床试验,语种限中、英文.结果 共纳入52篇文献,多数来源于氯沙坦减少高血压患者终点事件(LIFE)研究.其主要结果显示:①在降压效果相当的情况下,氯沙坦比阿替洛尔的耐受性更好、降低高血压患者的左室肥厚作用更好;②氯沙坦防治心脑血管事件的发生,特别是预防脑卒中首次发作的效果也更好;③氯沙坦对伴/不伴有糖尿病、伴/不伴有房颤、有低血红蛋白或高血尿酸,以及合用阿司匹林或氢氯噻嗪患者的治疗效果均优于阿替洛尔;④无论用氯沙坦还是阿替洛尔,强化降压治疗会增加有QRS间期延长的高血压患者发生心源性猝死的风险;⑤对吸烟、少量或大量饮酒的高血压患者,氯沙坦的作用均优于阿替洛尔;⑥氯沙坦和阿替洛尔在非洲裔、不同性别、血管紧张素转化酶基因突变的高血压患者中的作用无显著差别.结论 氯沙坦与阿替洛尔的降压效果相当,但氯沙坦比阿替洛尔能更有效地降低高血压患者的左室肥厚,且氯沙坦带给高血压患者降压以外的益处远比阿替洛尔多,如降低尿蛋白和尿酸,不降低高密度脂蛋白等方面的作用.%Objective To provide the China Essential Drugs List with evidence-based data for selecting the antihy-pertensive drugs in ARBs category. Methods With following search terms such as losartan, atenolol and clinical trial, the relevant clinical trials on losartan and atenolol for treating hypertension in both Chinese and English languages were collected from the EMbase, PubMed, The Cochrane Library

  18. Validación de métodos por Espectrofotometría Utravioleta y HPLC para la determinación cuantitativa del Atenolol en preparaciones farmacéuticas

    OpenAIRE

    Weich, Anelise; Carvalho de Oliveira, Daniele; Melo, Janine de; Goebel, Karin; Rolim Clarice M. B.

    2007-01-01

    Se ha desarrollado y validado un método de cromatografía líquida y espectrofotometría ultravioleta para la determinación de comprimidos de atenolol. La fase móvil empleada fue buffer acetato de amonio 10 mM (pH 7.0) y acetonitrilo (80:20 v/v). Las muestras se inyectaron en una columna Purospher RP-18 (250 mm x 4,6 mm, 5 mm), con una velocidad de flujo de 0,8 ml.min–1 Las muestras . se detectaron a 275 nm. El ensayo resultó lineal en el rango de concentración de 125 a 375 μg.ml̵...

  19. 伊伐布雷定和阿替洛尔保护大鼠心肌梗死后冠脉储备的比较研究%Comparative Study on Coronary Reserve between Ivabradine Therapy and Atenolol Therapy after Rat Myocardial Infarction

    Institute of Scientific and Technical Information of China (English)

    张荣林; Robert J.Tomanek

    2011-01-01

    OBJECTIVE We compared the ivabradine and atenolol in preserving coronary reserve of infarcted rats. METHODS 12-month-old male Sprague-Dawley rats were randomly divided into 4 groups: sham group, MI group, MI +Iva group and MI +Ate group. Medical treatment was immediately begun following infarction and continued until the 28th day. Infarction area, heart rate and coronary reserve were compared among groups. RESULTS There were no statistical differences among the 3 infarcted groups with infarction size and baseline heart rate. Heart rates 28 d later were significantly lower in both MI + Ate group and MI + Iva group compared to MI group. However, there was no statistical difference between the two medicine treated groups. Compared with the sham group, the coronary reserve of both the free wall and the ventricular septum in the MI group were significantly lower, and the coronary reserve of the ventricular septum in the MI + Ate group was also significantly lower. The coronary reserve of both the free wall and the septum in the MI + Iva group were higher, compared with both the MI group and the MI + Ate group. CONCLUSION Iva preserves the coronary reserve of infarcted rats better than Ate treatment.%目的 比较伊伐布雷定(Iva)和阿替洛尔(Ate)治疗对大鼠心梗后冠脉储备的保护作用有无差异.方法 受试大鼠分为假手术(sham)组、心肌梗死(MI)组、MI+Iva组和MI+Ate组,药物治疗在诱导心肌梗死后开始,疗程28d.比较大鼠的心梗面积,以及治疗前后的心率、冠脉储备等情况.结果 三组心梗大鼠之间基础心率、梗死面积占心室面积的比例均无统计学差异;与MI组相比,术后第28天MI+Iva组和MI+Ate组的心率明显减慢;而MI+Iva组和Ml+Ate组相比,术后第28天的心率减慢程度没有统计学差异.与sham组相比,MI组无论游离壁还是室间隔的冠脉储备都显著降低,MI+Ate组室间隔的冠脉储备也显著降低.MI+Iva组无论游离壁还是室间隔的冠脉

  20. Efficacy of atenolol and captopril in reducing risk of macrovascular and microvascular complications in type 2 diabetes: UKPDS 39

    OpenAIRE

    1998-01-01

    Objective: To determine whether tight control of blood pressure with either a β blocker or an angiotensin converting enzyme inhibitor has a specific advantage or disadvantage in preventing the macrovascular and microvascular complications of type 2 diabetes.

  1. Value of the addition of Amlodipine to atenolol in patients with angina pectoris despite adequate beta blockade

    NARCIS (Netherlands)

    Dunselman, PHJM; Bouwens, LHM; Herweijer, AH; Bernink, PJLM

    1998-01-01

    Anginal patients who remain symptomatic despite optimally dosed beta blockade may also be given dihydropyridine calcium antagonists. This treatment regimen was examined in a double-blind parallel, randomized, controlled study in 147 patients with angina and positive bicycle exercise tests despite op

  2. Prevention of cardiovascular events with an antihypertensive regimen of amlodipine adding perindopril as required versus atenolol adding bendroflumethiazide as required, in the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA): a multicentre randomised controlled

    DEFF Research Database (Denmark)

    Dahlöf, Björn; Sever, Peter S; Poulter, Neil R;

    2005-01-01

    The apparent shortfall in prevention of coronary heart disease (CHD) noted in early hypertension trials has been attributed to disadvantages of the diuretics and beta blockers used. For a given reduction in blood pressure, some suggested that newer agents would confer advantages over diuretics...

  3. Does calcium channel blockade and beta-adrenergic blockade affect platelet function and fibrinolysis to a varying degree?

    DEFF Research Database (Denmark)

    Fornitz, Gitte Gleerup; Mehlsen, J; Winther, K

    1995-01-01

    The effects of isradipine and atenolol on platelet function and fibrinolytic activity were studied in 10 male patients with mild untreated hypertension. After a 2-week placebo run-in period, the volunteers were randomized to either isradipine 2.5 mg twice daily or atenolol 100 mg daily for a 6-mo...

  4. Prevention of cardiovascular events with an antihypertensive regimen of amlodipine adding perindopril as required versus atenolol adding bendroflumethiazide as required, in the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA): a multicentre randomised controlled trial

    DEFF Research Database (Denmark)

    Dahlöf, Björn; Sever, Peter S; Poulter, Neil R;

    2005-01-01

    The apparent shortfall in prevention of coronary heart disease (CHD) noted in early hypertension trials has been attributed to disadvantages of the diuretics and beta blockers used. For a given reduction in blood pressure, some suggested that newer agents would confer advantages over diuretics...

  5. Nebivolol

    Science.gov (United States)

    ... Nebivolol is in a class of medications called beta blockers. It works by relaxing blood vessels and slowing ... mention any of the following: amiodarone (Cordarone, Pacerone); beta blockers such as acebutolol (Sectral), atenolol (Tenormin, in Tenoretic), ...

  6. Atrial Fibrillation Medications

    Science.gov (United States)

    ... won't go away Heart Rate Controlling Medications Beta blockers . These are drugs used to slow the heart ... their heart rate is controlled. Read more about beta blockers . Some examples may include: Atenolol Bisoprolol Carvedilol Metoprolol ...

  7. Dorzolamide and Timolol Ophthalmic

    Science.gov (United States)

    ... is in a class of medications called topical beta blockers. Dorzolamide and timolol lowers pressure in the eye ... Be sure to mention any of the following: beta blockers such as atenolol (Tenormin), labetalol (Normodyne), metoprolol (Lopressor, ...

  8. Potassium Test

    Science.gov (United States)

    ... non-steroidal anti-inflammatory drugs (NSAIDs) , ACE inhibitors, beta blockers (such as propanolol and atenolol), angiotensin-converting enzyme ... be due to certain drugs such as NSAIDs, beta blockers, and lithium or due to the adrenal glands ...

  9. Design and Development of Osmotic Drug Delivery System for Anti-Hypertensive Agent

    Directory of Open Access Journals (Sweden)

    Shah N

    2013-04-01

    Full Text Available Controlled porosity osmotic tablet of Atenolol prepared and evaluated in this study. Atenolol is v lowsoluble drug. So it is difficult to formulate osmotic tablet of Atenolol which gives drug release up to 24hr at zero order. To get desired dissolution profile various formulation parameters like osmogenconcentration, level of weight gain and level of pore former concentration were studied. Polysorbate 80was added as solubilizer to increase its dissolution rate and get drug release up to 24 hr at zero order. Asconcentration of solubilizer increases, dissolution rate increases. Final optimized formulation wasstudied for effect of pH of dissolution media, agitation intensity and osmotic pressure of dissolutionmedia. There is no effect of pH of dissolution media and agitation intensity on dissolution. There issignificant effect of osmotic pressure on dissolution confirms that prepared Atenolol tablet gives drugrelease in osmotically control manner.

  10. Effect of ACE insertion/deletion and 12 other polymorphisms on clinical outcomes and response to treatment in the life study

    DEFF Research Database (Denmark)

    2010-01-01

    OBJECTIVE: This pharmacogenetics substudy from the Losartan Intervention for Endpoint reduction in Hypertension study in patients with hypertension and left ventricular hypertrophy (LVH) treated with the angiotensin receptor blocker losartan versus the beta-blocker atenolol for 4.8 years tested....... These polymorphisms were chosen because they could affect blood pressure control or the pharmacological action of losartan or atenolol. METHODS: We genotyped 3503 patients, 1774 on losartan and 1729 on atenolol. RESULTS: ACE and the 12 other genotypes did not affect the reduction in systolic blood pressure, diastolic...... blood pressure, pulse pressure, mean arterial pressure, or heart rate, or treatment differences between losartan and atenolol on these endpoints, as assessed by general linear models. Also, ACE and the 12 other genotypes did not affect risk of the primary composite endpoint or its components stroke...

  11. Hypertension--er det lige meget, hvordan vi saenker blodtrykket?

    DEFF Research Database (Denmark)

    Mehlsen, Jesper

    2008-01-01

    ASCOT compared the effect of atenolol combined with a thiazide versus amlodipine with perindopril in hypertensive patients. It also studied the effect of atorvastatin in those with normal cholesterol. ASCOT concluded that reductions in cardiovascular events with atorvastatin were significant...

  12. Beneficial effect of isradipine on the development of left ventricular hypertrophy in mild hypertension

    DEFF Research Database (Denmark)

    Mehlsen, J; Fornitz, Gitte Gleerup; Haedersdal, C;

    1993-01-01

    The objective of this study was to analyze the long-term hemodynamic effects of the calcium antagonist isradipine in mild hypertension compared with those of the beta 1-selective adrenoceptor antagonist atenolol, focusing in particular on the development of cardiac hypertrophy. Ten male patients...... isradipine (254 +/- 55 g). The results indicate that antihypertensive treatment with isradipine as monotherapy may prevent the development of left ventricular hypertrophy whereas treatment with atenolol as monotherapy does not appear to offer this possibility....

  13. 雷诺嗪与阿替洛尔、氨氯地平或地尔硫(艹卓)联合用药对重度慢性心绞痛患者运动耐量和心绞痛发作频率的影响随机对照试验%Effects of Ranolazine With Atenolol,Amlodipine,or Diltiazem on Exercise Tolerance and Angina Frequency in Patients With Severe Chronic Angina A randomized controlled trial

    Institute of Scientific and Technical Information of China (English)

    Bernard R.Chaitman; Carl J.Pepine; John O.Parker; MUDr Jaroslav Skopal; Galina Chumakova; Jerzy Kuch; Whedy Wang; Sandra L.Skettino; Andrew A.Wolff

    2004-01-01

    背景:许多慢性心绞痛患者尽管接受了血运重建和抗心绞痛药物治疗,但仍有心绞痛反复发作.以往一项研究表明,单独应用雷诺嗪(能够部分抑制脂肪酸氧化)能增加患者平板运动耐量.然而,雷诺嗪与β-受体阻断剂或钙通道拮抗剂联合治疗的远期疗效和安全性尚缺乏在重度慢性心绞痛患者人群进行的大规模研究.

  14. Beneficial effect of isradipine on the development of left ventricular hypertrophy in mild hypertension

    DEFF Research Database (Denmark)

    Mehlsen, J; Fornitz, Gitte Gleerup; Haedersdal, C;

    1993-01-01

    with mild essential hypertension were entered into a double-blind crossover study. Examinations were carried out after 2 weeks of placebo run-in, and after 6 and 12 months of active treatment. Mean resting blood pressure was reduced from 115 +/- 12 mm Hg to 106 +/- 12 mm Hg with atenolol, and to 107 +/- 8...... mm Hg with isradipine. The increase in the product of heart rate times blood pressure was significantly greater during isradipine treatment, as was the maximum exercise capacity. Left ventricular mass was increased from 228 +/- 36 g to 305 +/- 68 g with atenolol whereas it remained unchanged......The objective of this study was to analyze the long-term hemodynamic effects of the calcium antagonist isradipine in mild hypertension compared with those of the beta 1-selective adrenoceptor antagonist atenolol, focusing in particular on the development of cardiac hypertrophy. Ten male patients...

  15. Hypersomnolence with beta-adrenergic blockers.

    Science.gov (United States)

    Thachil, J; Zeller, J R; Kochar, M S

    1987-11-01

    An elderly, mildly demented, hypertensive male patient developed hypersomnolence on administration of propranolol for treatment of hypertension; no other cause for hypersomnolence was detected. Upon replacement of propranolol with atenolol, he felt better but continued to be quite somnolent. When atenolol was discontinued, he reported to have lack of sleep. On readministration of subtherapeutic doses of the same beta-adrenergic blocking agents, he once again experienced excessive sleepiness. By discontinuing beta-blocking agents and introducing captopril, he felt much better, became pleasant and talkative, and blood pressure was well controlled. Beta antagonists are important drugs in the management of many cardiovascular problems. Propranolol, a lipophilic beta-blocking agent, and atenolol, a hydrophilic beta-blocking agent, are two of the major agents currently used clinically in the United States. Numerous neuropsychiatric side-effects of the beta-adrenergic blocking drugs have been reported, but hypersomnolence is not readily recognized as one of them. PMID:3665616

  16. Prognostic importance of hemoglobin in hypertensive patients with electrocardiographic left ventricular hypertrophy: the Losartan Intervention For End point reduction in hypertension (LIFE) study

    DEFF Research Database (Denmark)

    Olsen, Michael Hecht; Wachtell, Kristian; Beevers, Gareth;

    2008-01-01

    baseline hemoglobin measurements were randomized to losartan- or atenolol-based treatment and followed for 4.8 years for end points of all-cause mortality and composite of cardiovascular death, nonfatal stroke, or nonfatal myocardial infarction. RESULTS: U-shaped relations were observed between deciles.......53, 95% CI 1.27-1.85, both P or =15.0/16.2 g/dL) was not. The decrease in hemoglobin was higher (P losartan- (14.3-13.8 g/dL) versus atenolol-based treatment (14.3-14.0 g/dL). In Cox models...

  17. Clopidogrel: A possible exacerbating factor for psoriasis

    Directory of Open Access Journals (Sweden)

    Vikram K Mahajan

    2014-01-01

    Full Text Available A 64-year-old man developed palmoplantar pustulosis eventuating into palmoplantar pustular psoriasis following treatment with diltiazem, atenolol, aspirin and atorvastatin for suspected coronary artery disease (CAD. Treatment for psoriasis, stopping atenolol and substituting aspirin with clopidogrel did not benefit. Subsequently, he stopped all his drugs and did not develop psoriasis or symptoms/signs of CAD. Re-challenge with oral clopidogrel precipitated his skin lesions. This case has implications for patients having psoriasis and cardiovascular comorbidity where clopidogrel/ticlopidine or aspirin may not be a useful alternative.

  18. Pulse pressure, left ventricular function and cardiovascular events during antihypertensive treatment (the LIFE study)

    DEFF Research Database (Denmark)

    Gerdts, Eva; Franklin, Stanley; Rieck, Ashild;

    2009-01-01

    systolic function and cardiovascular events was assessed in 883 patients with electrocardiographic LV hypertrophy during 4.8 years of randomized losartan- or atenolol-based treatment within the echocardiographic substudy of the Losartan Intervention For Endpoint reduction in hypertension (LIFE) study...

  19. Trends in drug usage among elderly with cardiovascular diseases

    Directory of Open Access Journals (Sweden)

    Rajeshwari Shastry

    2014-08-01

    Conclusion: Among the antihypertensive groups CCBs were the most commonly used followed by BB, ARBs and ACEIs. Among these antihypertensive agents amlodipine, losartan, atenolol and enalapril were most commonly used. Commonly used antidiabetic agents were metformin and glimepiride. [Int J Basic Clin Pharmacol 2014; 3(4.000: 723-725

  20. Omkostningseffektivitet ved hypertensionsbehandling med Losartan i Danmark

    DEFF Research Database (Denmark)

    Keiding, Hans; Hildebrandt, Per; Burke, Thomas;

    2006-01-01

    Formålet med denne analyse var set såvel fra samfundets som fra det danske sundhedsvæsens perspektiv at evaluere omkostningseffektiviteten af losartan sammenlignet med atenolol ved behandling af hypertension, baseret på Losartan Intervention For Endpoint (LIFE)-undersøgelsens data Udgivelsesdato...

  1. Effect of ACE insertion/deletion and 12 other polymorphisms on clinical outcomes and response to treatment in the life study

    DEFF Research Database (Denmark)

    Nordestgaard, Børge G; Kontula, Kimmo; Benn, Marianne;

    2010-01-01

    OBJECTIVE: This pharmacogenetics substudy from the Losartan Intervention for Endpoint reduction in Hypertension study in patients with hypertension and left ventricular hypertrophy (LVH) treated with the angiotensin receptor blocker losartan versus the beta-blocker atenolol for 4.8 years tested...

  2. Effects of Nebivolol on Endothelial Gene Expression during Oxidative Stress in Human Umbilical Vein Endothelial Cells

    Directory of Open Access Journals (Sweden)

    Ulisse Garbin

    2008-01-01

    Full Text Available The endothelium plays a key role in the development of atherogenesis and its inflammatory and proliferative status influences the progression of atherosclerosis. The aim of this study is to compare the effects of two beta blockers such as nebivolol and atenolol on gene expression in human umbilical vein endothelial cells (HUVECs following an oxidant stimulus. HUVECs were incubated with nebivolol or atenolol (10 micromol/L for 24 hours and oxidative stress was induced by the addition of oxidized (ox-LDL. Ox-LDL upregulated adhesion molecules (ICAM-1, ICAM-2, ICAM-3, E-selectin, and P-selectin; proteins linked to inflammation (IL-6 and TNFalpha, thrombotic state (tissue factor, PAI-1 and uPA, hypertension such as endothelin-1 (ET-1, and vascular remodeling such as metalloproteinases (MMP-2, MMP-9 and protease inhibitor (TIMP-1. The exposure of HUVECs to nebivolol, but not to atenolol, reduced these genes upregulated by oxidative stress both in terms of protein and RNA expression. The known antioxidant properties of the third generation beta blocker nebivolol seem to account to the observed differences seen when compared to atenolol and support the specific potential protective role of this beta blocker on the expression of a number of genes involved in the initiation and progression of atherosclerosis.

  3. β1-blockers lower norepinephrine release by inhibiting presynaptic, facilitating β1-adrenoceptors in normotensive and hypertensive rats

    Directory of Open Access Journals (Sweden)

    Torill eBerg

    2014-04-01

    Full Text Available Peripheral norepinephrine release is facilitated by presynaptic β-adrenoceptors (AR, believed to involve the β2-subtype exclusively. However, β1-selective blockers are the most commonly used β-blockers in hypertension. Here I tested the hypothesis that β1AR may function as presynaptic, release-facilitating auto-receptors. Since β1AR-blockers are injected during myocardial infarction, their influence on the cardiovascular response to acute norepinephrine release was also studied. By a newly established method, using tyramine-stimulated release through the norepinephrine transporter (NET, presynaptic control of catecholamine release was studied in normotensive and spontaneously hypertensive rats. β1AR-selective antagonists (CGP20712A, atenolol, metoprolol reduced norepinephrine overflow to plasma equally efficient as β2AR-selective (ICI-118551 and β1+2AR (nadolol antagonists in both strains. Neither antagonist lowered epinephrine secretion. Atenolol, which does not cross the blood-brain barrier, reduced norepinephrine overflow after adrenalectomy, adrenalectomy+ganglion blockade, losartan or nephrectomy. Atenolol and metoprolol reduced resting cardiac work load. During tyramine-stimulated norepinephrine release, they had little effect on work load, and increased the transient rise in total peripheral vascular resistance, particularly atenolol when combined with losartan. In conclusion, β1AR, like β2AR, stimulated norepinephrine but not epinephrine release, independent of adrenal catecholamines, ganglion transmission, or renal renin release/angiotensin AT1-receptor activation. β1AR therefore functioned as a peripheral, presynaptic, facilitating auto-receptor. Like tyramine, hypoxia may induce NET-mediated release. Augmented tyramine-induced vasoconstriction, as observed after injection of β1AR-blocker, particularly atenolol combined with losartan, may hamper organ perfusion, and may have clinical relevance in hypoxic conditions such as

  4. TR146 cells grown on filters as a model of human buccal epithelium

    DEFF Research Database (Denmark)

    Nielsen, H M; Rassing, M R; Nielsen, Hanne Mørck

    2000-01-01

    The objective of the present study was to evaluate the TR146 cell culture model as an in vitro model of human buccal epithelium. For this purpose, the permeability of water, mannitol and testosterone across the TR146 cell culture model was compared to the permeability across human, monkey and...... determined. The mannitol and testosterone permeability across the TR146 cell culture model could be related to the permeability across porcine and human buccal mucosa. The permeability of the beta-adrenoceptor antagonists across the TR146 cell culture model varied between 2.2 x 10(-6) cm/s (atenolol) and 165...... increased the permeability only for the hydrophilic atenolol, which may help explain the mechanism for GC-induced enhancement. The present results indicate that the TR146 cell culture model can be used as an in vitro model for permeability studies and mechanistic studies of human buccal drug delivery of...

  5. Left Ventricular Wall Stress-Mass-Heart Rate Product and Cardiovascular Events in Treated Hypertensive Patients

    DEFF Research Database (Denmark)

    Devereux, Richard B; Bang, Casper N; Roman, Mary J;

    2015-01-01

    In the Losartan Intervention for End Point Reduction in Hypertension (LIFE) study, 4.8 years' losartan- versus atenolol-based antihypertensive treatment reduced left ventricular hypertrophy and cardiovascular end points, including cardiovascular death and stroke. However, there was no difference...... randomized treatment, the triple product was reduced more by atenolol, with prevalences of elevated triple product of 39% versus 51% on losartan (both P≤0.001). In Cox regression analyses adjusting for age, smoking, diabetes mellitus, and prior stroke, MI, and heart failure, 1 SD lower triple product...... was associated with 23% (95% confidence interval 13%-32%) fewer composite end points, 31% (18%-41%) less cardiovascular mortality, 30% (15%-41%) lower MI, and 22% (11%-33%) lower all-cause mortality (all P≤0.001), without association with stroke (P=0.34). Although losartan-based therapy reduced ventricular mass...

  6. Relaxation and filling of the left ventricle assessed by Doppler echocardiography

    International Nuclear Information System (INIS)

    In patients with coronary disease the Doppler method described in the present work was capable of detecting a delayed left ventricular (LV) relaxation and a shift of LV filling from early towards late diastole. This might reflect changes in LV diastolic function due to myocardial ischemia. Furthermore, the method allowed monitoring of changes during treatment with atenolol and verapamil. These changes indicated that atenolol and verapamil were able to partially correct the relaxation abnormailty and increase the relative contribution of early diastolic filling. Although all the numerous variables that influence LV transmitral filling could be controlled in this noninvasive clinical study, the results suggest that antianginal drugs may have beneficial effect on diastolic function in coronary disease. 62 refs., 3 figs., 4 tabs

  7. Effects of preoperative β-blocker on blood loss and blood transfusion during spinal surgeries with sodium nitroprusside-controlled hypotension

    Directory of Open Access Journals (Sweden)

    Yasser Mohamed Amr

    2012-01-01

    Full Text Available Background: The present study sought to determine whether premedication with oral β-blocker before hypotensive anesthesia with sodium nitroprusside could improve the quality of surgical field, decrease the blood loss, and decrease the need for homologous blood transfusion and duration of surgery. Methods: Eighty patients scheduled for spinal fixation surgery were included in a prospective, randomized, double-blinded study. Patients were classified into two groups: Group I received oral atenolol 50 mg twice one day before surgery; and Group II received placebo tablets identical in appearance to atenolol tablets for the same period and interval. All patients in both the groups received intraoperative sodium nitroprusside (SNP as a hypotensive agent. Hemodynamic variables, amount of sodium nitroprusside used, quality of surgical field, and the amount of homologous blood transfusion and blood loss were compared between groups. Results: Heart rate and amount of SNP used were significantly less (P<0.0001 in the atenolol group, but no significant difference was found in intraoperative mean arterial blood pressure (MABP between the two groups. The time of surgeries was significantly shorter in Group I than in Group II (185±15.21 vs 225±12.61 min, P<0.0001. The quality of surgical field was better in Group I than in Group II in all times of measurements, P<0.0001. The amount of blood loss and the amount of packed red blood cells transfused were significantly less in Group I than in Group II, P<0.0001. No clinically significant complications were observed in either group. Conclusion: Premedication with oral atenolol 50 mg twice/day for one day before hypotensive anesthesia with SNP during spinal surgeries seems to be clinically safe and effective to reduce heart rate, amount of SNP used, amount of blood loss, and amount of blood transfused with better quality of surgical field.

  8. Effects of anti-hypertensive drugs on esophageal body contraction

    Institute of Scientific and Technical Information of China (English)

    Koichi; Yoshida; Kenji; Furuta; Kyoichi; Adachi; Shunji; Ohara; Terumi; Morita; Takashi; Tanimura; Shuji; Nakata; Masaharu; Miki; Kenji; Koshino; Yoshikazu; Kinoshita

    2010-01-01

    AIM:To clarify the effects of anti-hypertensive drugs on esophageal contraction and determine their possi-ble relationship with gastro-esophageal reflux disease.METHODS:Thirteen healthy male volunteers were enrolled. Esophageal body peristaltic contractions and lower esophageal sphincter (LES) pressure were measured using high resolution manometry. All subjects were randomly examined on four separate occasions following administrations of nifedipine,losartan,and atenolol,as well as without any drug administ...

  9. Exposure of the Main Italian River Basin to Pharmaceuticals

    OpenAIRE

    Federico Ferrari; Agata Gallipoli; Matteo Balderacchi; Maria M. Ulaszewska; Ettore Capri; Marco Trevisan

    2011-01-01

    This study give a preliminary survey of pharmaceutical contamination and accumulation in surface waters and sediments along the river Po basin (74,000 km2, the largest in Italy), a strategic region for the Italian economy: it collects sewage from a vast industrialized area of Italy (Autorità di Baciono del fiume Po, 2006, 2009). 10 pharmaceuticals (atenolol, propanolol, metoprolol, nimesulide, furosemide, carbamazepine, ranitidine, metronidazole, paracetamol, and atorvastatin) from several th...

  10. High performance liquid chromatographic separation of thirteen drugs collected in Chinese Pharmacopoeia 2010(Ch.P2010) on cellulose ramification chiral stationary phase

    Institute of Scientific and Technical Information of China (English)

    2012-01-01

    The enantiomers separation of thirteen drugs collected in Ch.P2010 was performed on chiral stationary phase of cellulose ramification (chiralpak OD and chiralpak OJ) by high performance liquid chromatographic (HPLC) methods, which included ibuprofen (C1), ketoprofen (C2), nitrendipine (C3), nimodipine (C4), felodipine (C5), omeprazole (C6), praziquantel (C7), propranolol hydrochloride (C8), atenolol (C9), sulpiride (C10), clenbuterol hydrochloride (C11), verapamil hydrochloride (C12), and chlorphenamine mal...

  11. Beta-Blockers in the Management of Hypertension and/or Chronic Kidney Disease

    OpenAIRE

    Hirofumi Tomiyama; Akira Yamashina

    2014-01-01

    This minireview provides current summaries of beta-blocker use in the management of hypertension and/or chronic kidney disease. Accumulated evidence suggests that atenolol is not sufficiently effective as a primary tool to treat hypertension. The less-than-adequate effect of beta-blockers in lowering the blood pressure and on vascular protection, and the unfavorable effects of these drugs, as compared to other antihypertensive agents, on the metabolic profile have been pointed out. On the oth...

  12. Left Ventricular Wall Stress-Mass-Heart Rate Product and Cardiovascular Events in Treated Hypertensive Patients: LIFE Study.

    Science.gov (United States)

    Devereux, Richard B; Bang, Casper N; Roman, Mary J; Palmieri, Vittorio; Boman, Kurt; Gerdts, Eva; Nieminen, Markku S; Papademetriou, Vasilios; Wachtell, Kristian; Hille, Darcy A; Dahlöf, Björn

    2015-11-01

    In the Losartan Intervention for End Point Reduction in Hypertension (LIFE) study, 4.8 years' losartan- versus atenolol-based antihypertensive treatment reduced left ventricular hypertrophy and cardiovascular end points, including cardiovascular death and stroke. However, there was no difference in myocardial infarction (MI), possibly related to greater reduction in myocardial oxygen demand by atenolol-based treatment. Myocardial oxygen demand was assessed indirectly by the left ventricular mass×wall stress×heart rate (triple product) in 905 LIFE participants. The triple product was included as time-varying covariate in Cox models assessing predictors of the LIFE primary composite end point (cardiovascular death, MI, or stroke), its individual components, and all-cause mortality. At baseline, the triple product in both treatment groups was, compared with normal adults, elevated in 70% of patients. During randomized treatment, the triple product was reduced more by atenolol, with prevalences of elevated triple product of 39% versus 51% on losartan (both P≤0.001). In Cox regression analyses adjusting for age, smoking, diabetes mellitus, and prior stroke, MI, and heart failure, 1 SD lower triple product was associated with 23% (95% confidence interval 13%-32%) fewer composite end points, 31% (18%-41%) less cardiovascular mortality, 30% (15%-41%) lower MI, and 22% (11%-33%) lower all-cause mortality (all P≤0.001), without association with stroke (P=0.34). Although losartan-based therapy reduced ventricular mass more, greater heart rate reduction with atenolol resulted in larger reduction of the triple product. Lower triple product during antihypertensive treatment was strongly, independently associated with lower rates of the LIFE primary composite end point, cardiovascular death, and MI, but not stroke.

  13. Drug effects on aldosterone/plasma renin activity ratio in primary aldosteronism.

    Science.gov (United States)

    Mulatero, Paolo; Rabbia, Franco; Milan, Alberto; Paglieri, Cristina; Morello, Fulvio; Chiandussi, Livio; Veglio, Franco

    2002-12-01

    Primary aldosteronism is a specifically treatable and potentially curable form of secondary hypertension. The aldosterone/plasma renin activity ratio (ARR) is routinely used as a screening test. Antihypertensive therapy can interfere with the interpretation of this parameter, but a correct washout period can be potentially harmful. We have investigated the effects of therapy with atenolol, amlodipine, doxazosin, fosinopril, and irbesartan on the ARR in a group of 230 patients with suspected primary aldosteronism. The percent change from control of ARR in patients taking amlodipine was -17%+/-32; atenolol, 62%+/-82; doxazosin, -5%+/-26; fosinopril, -30%+/-24; and irbesartan, -43%+/-27. The ARR change induced by atenolol was significantly higher compared with that induced by all other drugs (P<0.0001), and the ARR change induced by irbesartan was significantly lower than that induced by doxazosin (P<0.0001). One of 55 patients from the group taking amlodipine (1.8%) and 4/17 of the patients taking irbesartan (23.5%) gave a false-negative ARR (<50). None of the patients of the groups taking fosinopril, doxazosin, and atenolol displayed a false-negative ARR. Doxazosin and fosinopril can be used in hypertensive patients who need to undergo aldosterone and PRA measurement for the diagnosis of primary aldosteronism; amlodipine gave a very small percentage of false-negative diagnoses. beta-Blockers also do not interfere with the diagnosis of primary aldosteronism, but they can be responsible for an increased rate of false-positive ARRs. The high rate of false-negative diagnoses in patients undergoing irbesartan treatment requires confirmation in a higher number of patients. PMID:12468576

  14. Impact of carbon-dosing on micro-pollutants removal in MBBR post-denitrification systems

    OpenAIRE

    Escola Casas, Monica; Torresi, Elena; Plósz, Benedek G.; Bester, Kai; Christensen, M.

    2015-01-01

    Dosing of methanol or ethanol is a common practice in post-denitrification steps during wastewater treatment by MBBR technology. The carbon-dosage impact on micro- pollutants removal, in terms of type (methanol or ethanol) and concentration was investigated. First, with continuous operation and indigenous micro-pollutants concentrations, different methanol and ethanol dosages were used to manipulate the carbon-to-nitrate ratio in two MBBRs. Atenolol, citalopram and trimethoprim were efficient...

  15. Modulation of reflexly evoked vagal bradycardias by central 5-HT1A receptors in anaesthetized rabbits

    OpenAIRE

    Skinner, Matthew R; Ramage, Andrew G; Jordan, David

    2002-01-01

    The role of central 5-HT1A receptors in the control of the bradycardia and changes in central respiratory drive, renal nerve activity and blood pressure evoked by stimulating cardiopulmonary afferents with phenylbiguanide, baroreceptors by electrical stimulation of the aortic nerve and chemoreceptors by injections of sodium cyanide (NaCN) in atenolol-pretreated anaesthetized rabbits were studied.Buspirone (100 μg kg−1; i.c.) potentiated the bradycardia (increase in R-R interval) and the chang...

  16. [Medicamentous kidney protection in type 2 diabetic patients--is cheaper also more economical? A model calculation for Swiss health care].

    Science.gov (United States)

    Faller, J; Hess, B

    2002-05-01

    Impaired renal function occurs in about 50% of patients suffering from type 2 diabetes, and diabetic nephropathy has become the leading cause of endstage renal disease. Reduction of blood pressure to levels around 120/80 mmHg is one of the most effective way to slow progression of diabetic nephropathy. Recent meta-analyses, however, have emphasized on the fact that ACE inhibitors (ACEI) and non-dihydropyridine calcium channel blockers (NDHP-CCB) exert nephro-protective effects which go beyond the effect of blood pressure reduction. This has lately been confirmed by a prospective trial in comparison to the betablocker atenolol. Based on these data, demographics of the Swiss population, literature data on mortality rates of type 2 diabetics with impaired renal function and studies on true costs of antihypertensives, we calculated the costs of a longterm intervention (20 years) with antihypertensives in 3536 middle-aged Swiss patients with type 2 diabetes and macro-albuminuria whose antihypertensive regimen was based either on the ACEI lisinopril, or the ND-HP-CCB verapamil, or the betablocker atenolol. Under atenolol, acquisition costs were lowest, whereas faster loss of renal function over time increased mortality rate and thus reduced the number of patients to be treated. Nevertheless, due to the fact that patients reached uremia and had to be dialyzed, 20 years of atenolol-based regimen with costs of 316 millions of Swiss francs turned out to be much more expensive than the lisinopril- or the verapamil-based regimen with 121 and 38 millions of Swiss francs, respectively. Thus, low acquisition cost is not necessarily the only important determinant of overall costs of drug therapy.

  17. Digoxin use and risk of mortality in hypertensive patients with atrial fibrillation

    DEFF Research Database (Denmark)

    Okin, Peter M; Hille, Darcy A; Wachtell, Kristian;

    2015-01-01

    follow-up (n = 803), randomly assigned to losartan or atenolol-based treatment, in post-hoc analysis of a substudy of the Losartan Intervention For Endpoint Reduction in hypertension (LIFE) trial. During 4.7 ± 1.1 years of mean follow-up, 167 patients died (17.8%) and 372 (39.7%) were treated...

  18. Changes in electrocardiographic left ventricular hypertrophy and risk of major cardiovascular events in isolated systolic hypertension: the LIFE study

    DEFF Research Database (Denmark)

    Larstorp, A C K; Okin, P M; Devereux, R B;

    2011-01-01

    The predictive value of changes in the severity of electrocardiographic left ventricular hypertrophy (ECG-LVH) during antihypertensive therapy remains unclear in isolated systolic hypertension (ISH). In a Losartan Intervention For Endpoint reduction in hypertension substudy, we included 1320...... patients aged 54–83 years with systolic blood pressure (BP) of 160–200¿mm¿Hg, diastolic BP losartan- or atenolol-based treatment with a mean follow-up of 4.8 years. The composite end point...

  19. Role of blood pressure and other variables in the differential cardiovascular event rates noted in the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA)

    DEFF Research Database (Denmark)

    Poulter, Neil R; Wedel, Hans; Dahlöf, Björn;

    2005-01-01

    Results of the Anglo-Scandinavian Cardiac Outcomes Trial-Blood Pressure Lowering Arm (ASCOT-BPLA) show significantly lower rates of coronary and stroke events in individuals allocated an amlodipine-based combination drug regimen than in those allocated an atenolol-based combination drug regimen (HR...... 0.86 and 0.77, respectively). Our aim was to assess to what extent these differences were due to significant differences in blood pressures and in other variables noted after randomisation....

  20. A comparison of Chinese traditional and Western medical approaches for the treatment of mild hypertension.

    OpenAIRE

    Wong, N. D.; Ming, S.; Zhou, H.Y.; Black, H. R.

    1991-01-01

    We compared the efficacy of Chinese traditional treatment for mild hypertension with that of a standard Western medical regimen in a group of 50 well-matched patients (24 allocated to Western medicine and 26 to Chinese traditional medicine) with mild hypertension (diastolic blood pressure 90-104 mmHg). Those receiving Western therapy were treated in a stepped-care fashion with dihydrochlorothiazide and atenolol. Those in the Chinese traditional therapy group received one of two mixtures of ni...

  1. The pressor effect of angiotensin-(1-7 in the rat rostral ventrolateral medulla involves multiple peripheral mechanisms

    Directory of Open Access Journals (Sweden)

    Rita C. Oliveira

    2013-01-01

    Full Text Available OBJECTIVE: In the present study, the peripheral mechanism that mediates the pressor effect of angiotensin-(1-7 in the rostral ventrolateral medulla was investigated. METHOD: Angiotensin-(1-7 (25 pmol was bilaterally microinjected in the rostral ventrolateral medulla near the ventral surface in urethane-anesthetized male Wistar rats that were untreated or treated (intravenously with effective doses of selective autonomic receptor antagonists (atenolol, prazosin, methyl-atropine, and hexamethonium or a vasopressin V1 receptor antagonist [d(CH25 -Tyr(Me-AVP] given alone or in combination. RESULTS: Unexpectedly, the pressor response produced by angiotensin-(1-7 (16 ± 2 mmHg, n = 12, which was not associated with significant changes in heart rate, was not significantly altered by peripheral treatment with prazosin, the vasopressin V1 receptor antagonist, hexamethonium or methyl-atropine. Similar results were obtained in experiments that tested the association of prazosin and atenolol; methyl-atropine and the vasopressin V1 antagonist or methyl-atropine and prazosin. Peripheral treatment with the combination of prazosin, atenolol and the vasopressin V1 antagonist abolished the pressor effect of glutamate; however, this treatment produced only a small decrease in the pressor effect of angiotensin-(1-7 at the rostral ventrolateral medulla. The combination of hexamethonium with the vasopressin V1 receptor antagonist or the combination of prazosin, atenolol, the vasopressin V1 receptor antagonist and methyl-atropine was effective in blocking the effect of angiotensin-(1-7 at the rostral ventrolateral medulla. CONCLUSION: These results indicate that angiotensin-(1-7 triggers a complex pressor response at the rostral ventrolateral medulla that involves an increase in sympathetic tonus, release of vasopressin and possibly the inhibition of a vasodilatory mechanism.

  2. Liver cirrhosis and fatty liver

    Institute of Scientific and Technical Information of China (English)

    1993-01-01

    930137 Effects of selective and non-selectiveβ-adrenoreceptor blockers on portal hemody-namics in patients with liver cirrhosis.HUANGTianwei(黄天卫),et al.1st Affili Hosp,DalianMed Coll.Chin J Digest 1992;12(3):145-147.Effects of selective(atenolol)and non-selec-tive(propranolol)β-adrenoreceptor blockerson portal hemodynamics in patients with livercirrhosis were measured by pulsed Doppler du-

  3. Effect of different beta blockers on penile vascular velocities in hypertensive males

    OpenAIRE

    Samer Malak Botros; Ahmed Mohamed Hussein; Ahmed Shawky Elserafy

    2015-01-01

    Background: Beta blockers are very commonly used as antihypertensive medications in young active individuals. This class has been accused of erectile dysfunction in patients taking them. Problems with erectile function can raise a concern in the treatment of hypertension and may influence the choice of treatment regimens and decisions to discontinue drugs. Aim: The aim was to assess the effect of different beta blockers: nebivolol, atenolol, bisoprolol, and carvedilol on the penile arteria...

  4. ISOCRATIC SEPARATION OF FOUR BETA BLOCKERS WITH AMLODIPINE BY C18 RP-HPLC: APPLICATION TO AMLODIPINE DETERMINATION IN PHARMACEUTICAL DOSAGE FORMS

    OpenAIRE

    Panchumarthy Ravisankar; Garikapati Devala Rao

    2013-01-01

    This method described for the successful separation of a beta blockers with amlodipine by RP-HPLC on a C18 column with UV detection. One of the key goals of High Performance Liquid Chromatography technique is to achieve a consistent and reproducible separation. A simple, precise, selective and sensitive HPLC method was developed and validated for determination of five anti-hypertensive agents, atenolol hydrochloride, metoprolol succinate, propranolol hydrochloride, amlodipine besylate and neb...

  5. Adrenalectomy abolishes antagonism of alpha-adrenoceptor-mediated hypotension by a beta-blocker in conscious rats.

    OpenAIRE

    Tabrizchi, R.; Pang, C. C.

    1990-01-01

    1. The effects of a single bolus injection of propranolol, atenolol or ICI 118,551, non-selective beta-, selective beta 1- and selective beta 2-adrenoceptor antagonists, respectively, on mean arterial pressure (MAP) and plasma catecholamine concentrations were examined in seven groups of conscious and unrestrained adrenalectomized rats receiving a continuous infusion of the alpha-adrenoceptor antagonist phentolamine. In all rats adrenaline was undetectable in the plasma four days after adrena...

  6. Ambulatory pressure monitoring in the assessment of antihypertensive therapy.

    Science.gov (United States)

    Coats, A J; Conway, J; Somers, V K; Isea, J E; Sleight, P

    1989-06-01

    A low-cost, ambulatory blood-pressure monitor has been calibrated and validated against a random zero sphygmomanometer. The repeatability of ambulatory pressure recordings after a placebo month in 44 mild to moderate untreated hypertensives was assessed. Systolic blood pressure showed a mean difference over 1 month of 2.0 mmHg, with a standard deviation of differences of 9.3 mmHg. The diastolic blood pressure mean difference was 0.1 mmHg (SD = 6.3 mmHg). This variability was much less than for clinic readings (SD = 17.3 mmHg) or for single home pressure readings (SD = 19.7 mmHg). Using ambulatory monitoring to detect a drop in pressure of 8/5 mmHg with a power of 0.9, the number of subjects needed in a parallel group trial is reduced from 360 to 68, and in a crossover study from 88 to 16 subjects. The usefulness of ambulatory pressure monitoring is demonstrated in a placebo-controlled comparison of atenolol, nifedipine retard, or their combination in random order. Eleven subjects, 21-60 years, with initial average blood pressures of 166.5/104.7 mmHg, showed a reduction in pressure with atenolol 50 mg a day of 15.1/10.0 mmHg, with nifedipine retard 20 mg b.i.d. of 21.0/11.6 mmHg, and with atenolol 50 mg and nifedipine retard 20 mg once a day of 26.2/16.8 mmHg. Ambulatory monitoring of pressure improved the accuracy of the trial and demonstrated a reduction in the alerting response with atenolol. PMID:2487802

  7. Effects of nine antihypertensive drugs on blood pressure variability in sinoaortic-denervated rats

    Institute of Scientific and Technical Information of China (English)

    Jin Wang; Fu-ming SHEN; Min-wei WANG; Ding-feng SU

    2006-01-01

    Aim: The present work was designed to investigate the effects of nine commonly used antihypertensive drugs on blood pressure (BP) and blood pressure variability (BPV) in conscious sinoaortic-denervated (SAD) rats. Methods: Seventy-two SAD rats were randomly divided into nine groups. They were respectively given nifedipine 3 mg/kg, nitrendipine 5 mg/kg, amlodipine 1 mg/kg, clonidine 10 μg/kg, prazosin 0.5 mg/kg, atenolol 20 mg/kg, telmisartan 20 mg/kg, hydrochlorothiazide 40 mg/kg or captopril 50 mg/kg. The drugs were given via a catheter previously implanted into the stomach. BP was recorded for 5 h from 1 h before drug administration to 4 h after drug administration in conscious, freely moving rats. Results: It was found that all these nine drugs significantly decreased BP in SAD rats. Six of these drugs (nifedipine, nitrendipine, amlodipine, clonidine, prazosin and atenolol) significantly decreased BPV in SAD rats, but the remaining three drugs did not. Clonidine and atenolol increased the heart period and the others did not. No drugs affected the heart period variability. Conclusion: Among nine antihypertensive drugs from different classes, calcium antagonists and sympathetic inhibitors decreased BPV in SAD rats.

  8. Effect of redox conditions on pharmaceutical loss during biological wastewater treatment using sequencing batch reactors

    Energy Technology Data Exchange (ETDEWEB)

    Stadler, Lauren B., E-mail: lstadler@umich.edu [Department of Civil and Environmental Engineering, University of Michigan, 1351 Beal Avenue, EWRE, Ann Arbor, MI 48109 (United States); Su, Lijuan, E-mail: lijuansu@buffalo.edu [Department of Chemistry, University at Buffalo, State University of New York, Buffalo, NY 14260 (United States); Moline, Christopher J., E-mail: christopher.moline@hdrinc.com [Department of Civil and Environmental Engineering, University of Michigan, 1351 Beal Avenue, EWRE, Ann Arbor, MI 48109 (United States); Ernstoff, Alexi S., E-mail: alexer@dtu.dk [Department of Civil and Environmental Engineering, University of Michigan, 1351 Beal Avenue, EWRE, Ann Arbor, MI 48109 (United States); Aga, Diana S., E-mail: dianaaga@buffalo.edu [Department of Chemistry, University at Buffalo, State University of New York, Buffalo, NY 14260 (United States); Love, Nancy G., E-mail: nglove@umich.edu [Department of Civil and Environmental Engineering, University of Michigan, 1351 Beal Avenue, EWRE, Ann Arbor, MI 48109 (United States)

    2015-01-23

    Highlights: • Pharmaceutical fate was studied in SBRs operated at different redox conditions. • Stable carbon oxidation and nitrification occurred under microaerobic conditions. • Losses of atenolol and trimethoprim were highest under fully aerobic conditions. • Loss of sulfamethoxazole was highest under microaerobic conditions. • Deconjugation occurred during treatment to form sulfamethoxazole and desvenlafaxine. - Abstract: We lack a clear understanding of how wastewater treatment plant (WWTP) process parameters, such as redox environment, impact pharmaceutical fate. WWTPs increasingly install more advanced aeration control systems to save energy and achieve better nutrient removal performance. The impact of redox condition, and specifically the use of microaerobic (low dissolved oxygen) treatment, is poorly understood. In this study, the fate of a mixture of pharmaceuticals and several of their transformation products present in the primary effluent of a local WWTP was assessed in sequencing batch reactors operated under different redox conditions: fully aerobic, anoxic/aerobic, and microaerobic (DO concentration ≈0.3 mg/L). Among the pharmaceuticals that were tracked during this study (atenolol, trimethoprim, sulfamethoxazole, desvenlafaxine, venlafaxine, and phenytoin), overall loss varied between them and between redox environments. Losses of atenolol and trimethoprim were highest in the aerobic reactor; sulfamethoxazole loss was highest in the microaerobic reactors; and phenytoin was recalcitrant in all reactors. Transformation products of sulfamethoxazole and desvenlafaxine resulted in the reformation of their parent compounds during treatment. The results suggest that transformation products must be accounted for when assessing removal efficiencies and that redox environment influences the degree of pharmaceutical loss.

  9. Single nucleotide polymorphisms in the apolipoprotein B and low density lipoprotein receptor genes affect response to antihypertensive treatment

    Directory of Open Access Journals (Sweden)

    Kahan Thomas

    2004-09-01

    Full Text Available Abstract Background Dyslipidemia has been associated with hypertension. The present study explored if polymorphisms in genes encoding proteins in lipid metabolism could be used as predictors for the individual response to antihypertensive treatment. Methods Ten single nucleotide polymorphisms (SNP in genes related to lipid metabolism were analysed by a microarray based minisequencing system in DNA samples from ninety-seven hypertensive subjects randomised to treatment with either 150 mg of the angiotensin II type 1 receptor blocker irbesartan or 50 mg of the β1-adrenergic receptor blocker atenolol for twelve weeks. Results The reduction in blood pressure was similar in both treatment groups. The SNP C711T in the apolipoprotein B gene was associated with the blood pressure response to irbesartan with an average reduction of 19 mmHg in the individuals carrying the C-allele, but not to atenolol. The C16730T polymorphism in the low density lipoprotein receptor gene predicted the change in systolic blood pressure in the atenolol group with an average reduction of 14 mmHg in the individuals carrying the C-allele. Conclusions Polymorphisms in genes encoding proteins in the lipid metabolism are associated with the response to antihypertensive treatment in a drug specific pattern. These results highlight the potential use of pharmacogenetics as a guide for individualised antihypertensive treatment, and also the role of lipids in blood pressure control.

  10. Occurrence and fate of select psychoactive pharmaceuticals and antihypertensives in two wastewater treatment plants in New York State, USA.

    Science.gov (United States)

    Subedi, Bikram; Kannan, Kurunthachalam

    2015-05-01

    The fates of psychoactive pharmaceuticals, including two antischizophrenics, six sedative-hypnotic-anxiolytics, four antidepressants, four antihypertensives, and their select metabolites, were determined in two wastewater treatment plants (WWTPs) in the Albany area of New York. All target psychoactive pharmaceuticals and their metabolites were found at a mean concentration that ranged from 0.98 (quetiapine) to 1220 ng/L (atenolol) in wastewater and from 0.26 (lorazepam) to 1490 ng/g dry weight (sertraline) in sludge. In this study, the fraction of psychoactive pharmaceuticals that was sorbed to suspended particulate matter (SPM) was calculated for the first time. Over 50% of the total mass of aripiprazole, norquetiapine, norsertraline, citalopram, desmethyl citalopram, propranolol, verapamil, and norverapamil was found sorbed to SPM in the influent. The mass loadings, i.e., influx, of target psychoactive pharmaceuticals in WWTPs ranged from 0.91 (diazepam) to 347 mg/d/1000 inhabitants (atenolol), whereas the environmental emissions ranged from 0.01 (dehydro-aripiprazole) to 316 mg/d/1000 inhabitants (atenolol). The highest calculated removal efficiencies were found for antischizophrenics (quetiapine=88%; aripiprazole=71%). However, the removal of some psychoactive pharmaceuticals through adsorption onto sludge was minimal (<1% of the initial mass load), which suggests that bio-degradation and/or chemical-transformation are the dominant mechanisms of removal of these pharmaceuticals in WWTPs. PMID:25666287

  11. The Influence of Molecular Structure Modifications on Vibrational Properties of Some Beta Blockers: A Combined Raman and DFT Study

    Directory of Open Access Journals (Sweden)

    A. Farcaș

    2016-01-01

    Full Text Available We report results of a systematic Raman, SERS, and DFT study on four beta blocking molecules: Atenolol, Metoprolol, Propranolol, and, for the first time reported in the literature, Bisoprolol. The choice of these molecules was motivated by the structural similarities between Atenolol, Bisoprolol, and Metoprolol on one hand and by their differences relative to Propranolol. The density functional theory (DFT approach, using the B3LYP method at the 6-311+G(d,p level of theory, has been employed for geometry optimization and vibration bands assignments. The obtained results highlight the major role played by the central aromatic ring whose vibrations dominate the Raman spectra in all compounds. While the phenyl group vibrations dominate the Raman spectrum in the case of Atenolol, Bisoprolol, and Metoprolol, the spectrum of Propranolol presents high intensity vibrations of the naphthyl group. SERS performed on gold and silver colloids, at various pH conditions, revealed a higher sensitivity for Propranolol detection. The pH dependence of the spectrum indicates that the studied beta blockers attach themselves to the metal nanoparticles in a protonated form. The molecular adsorption geometry on metal nanoparticles surface has been evaluated by using the experimental SER spectra and the quantum chemical calculations.

  12. Tratamento farmacológico da hiperalgesia experimentalmente induzida pelo núcleo pulposo Pharmacologic treatment of hyperalgesia experimentally induced by nucleus pulposus

    Directory of Open Access Journals (Sweden)

    André Luiz de Souza Grava

    2010-01-01

    Full Text Available OBJETIVO: Avaliar o efeito de drogas anti-inflamatórias (dexametasona, indometacina, atenolol, indometacina e atenolol e analgésica (morfina sobre a hiperalgesia experimentalmente induzida pelo núcleo pulposo em contato com o gânglio da raiz dorsal de L5. MÉTODOS: Trinta ratos Wistar machos com peso de 220 a 250g foram utilizados no estudo. A indução da hiperalgesia foi realizada por meio do contato de fragmento de núcleo pulposo retirado da região sacrococcígea e colocado sobre o gânglio da raiz dorsal de L5. Os 30 animais foram divididos em grupos experimentais de acordo com a droga utilizada. As drogas foram administradas durante duas semanas a partir da realização do procedimento cirúrgico para a indução da hiperalgesia. A hiperalgesia mecânica e térmica foram avaliadas por meio do teste da pressão constante da pata, von Frey eletrônico e Hargraves por um período de sete semanas. RESULTADOS: A maior redução da hiperalgesia foi observada no grupo de animais tratados pela morfina, seguido pela dexametasona, indometacina e atenolol. A redução da hiperalgesia foi observada após a interrupção da administração das drogas, com exceção do grupo de animais tratados com morfina, nos quais ocorreu aumento da hiperalgesia após a interrupção do tratamento. CONCLUSÕES: A hiperalgesia induzida pelo contato do núcleo pulposo com o gânglio da raiz dorsal pode ser reduzida com a administração de anti-inflamatórios e analgésicos, tendo sido observado a maior redução da hiperalgesia com a administração da morfina e dexametasona.OBJECTIVE: To evaluate the effect of antiinflammatory (dexamethasone, indomethacin, atenolol, indomethacin and atenolol and analgesic drugs (morphine on hyperalgesia experimentally induced by nucleus pulposus (NP contact with the L5- dorsal root ganglion (DRG. METHODS: Thirty male Wistar rats with weights ranging from 220 to 250 g were used in the study. The hyperalgesia was induced by

  13. Impact of soil properties on selected pharmaceuticals adsorption in soils

    Science.gov (United States)

    Kodesova, Radka; Kocarek, Martin; Klement, Ales; Fer, Miroslav; Golovko, Oksana; Grabic, Roman; Jaksik, Ondrej

    2014-05-01

    The presence of human and veterinary pharmaceuticals in the environment has been recognized as a potential threat. Pharmaceuticals may contaminate soils and consequently surface and groundwater. Study was therefore focused on the evaluation of selected pharmaceuticals adsorption in soils, as one of the parameters, which are necessary to know when assessing contaminant transport in soils. The goals of this study were: (1) to select representative soils of the Czech Republic and to measure soil physical and chemical properties; (2) to measure adsorption isotherms of selected pharmaceuticals; (3) to evaluate impact of soil properties on pharmaceutical adsorptions and to propose pedotransfer rules for estimating adsorption coefficients from the measured soil properties. Batch sorption tests were performed for 6 selected pharmaceuticals (beta blockers Atenolol and Metoprolol, anticonvulsant Carbamazepin, and antibiotics Clarithromycin, Trimetoprim and Sulfamethoxazol) and 13 representative soils (soil samples from surface horizons of 11 different soil types and 2 substrates). The Freundlich equations were used to describe adsorption isotherms. The simple correlations between measured physical and chemical soil properties (soil particle density, soil texture, oxidable organic carbon content, CaCO3 content, pH_H2O, pH_KCl, exchangeable acidity, cation exchange capacity, hydrolytic acidity, basic cation saturation, sorption complex saturation, salinity), and the Freundlich adsorption coefficients were assessed using Pearson correlation coefficient. Then multiple-linear regressions were applied to predict the Freundlich adsorption coefficients from measured soil properties. The largest adsorption was measured for Clarithromycin (average value of 227.1) and decreased as follows: Trimetoprim (22.5), Metoprolol (9.0), Atenolol (6.6), Carbamazepin (2.7), Sulfamethoxazol (1.9). Absorption coefficients for Atenolol and Metoprolol closely correlated (R=0.85), and both were also

  14. Use of carvedilol in hypertension: an update

    Directory of Open Access Journals (Sweden)

    Leonetti G

    2012-05-01

    Full Text Available Gastone Leonetti,1 Colin G Egan21Istituto Auxologico Italiano, Ospedale San Luca, Milan, Italy; 2Primula Multimedia SRL, Pisa, ItalyAbstract: β-blockers are effective antihypertensive agents and, together with diuretics, have been the cornerstone of pioneering studies showing their benefits on cardiovascular morbidity and mortality as a consequence of blood pressure reduction in patients with hypertension. However, evidence from recent meta-analyses have demonstrated no benefit afforded by atenolol compared with placebo in risk of mortality, myocardial infarction, or stroke, and a higher risk of mortality and stroke with atenolol/propranolol compared with other antihypertensive drug classes. Thus, the effect of these agents on cardiovascular morbidity and mortality in hypertensive patients, especially their use in uncomplicated hypertension, has remained largely controversial. However, it is recognized that the clinical studies used in these meta-analyses were mainly based on the older second-generation β-blockers, such as atenolol and metoprolol. Actually, considerable heterogeneity in, eg, pharmacokinetic, pharmacological, and physicochemical properties exists across the different classes of β-blockers, particularly between the second-generation and newer third-generation agents. Carvedilol is a vasodilating noncardioselective third-generation β-blocker, without the negative hemodynamic and metabolic effects of traditional β-blockers, which can be used as a cardioprotective agent. Compared with conventional β-blockers, carvedilol maintains cardiac output, has a reduced prolonged effect on heart rate, and reduces blood pressure by decreasing vascular resistance. Studies have also shown that carvedilol exhibits favorable effects on metabolic parameters, eg, glycemic control, insulin sensitivity, and lipid metabolism, suggesting that it could be considered in the treatment of patients with metabolic syndrome or diabetes. The present report

  15. Enantiomeric selectivity in adsorption of chiral β-blockers on sludge.

    Science.gov (United States)

    Sanganyado, Edmond; Fu, Qiuguo; Gan, Jay

    2016-07-01

    Adsorption of weakly basic compounds by sludge is poorly understood, although it has important implications on the distribution and fate of such micropollutants in wastewater effluent and sludge. Additionally, many of these compounds are chiral, and it is likely that their interactions with sludge is stereoselective and that the process may be further modified by surfactants that coexist in these systems. Adsorption of (R) and (S)-enantiomers of five commonly used β-blockers, i.e., acebutolol, atenolol, metoprolol, pindolol and propranolol, on sludge was characterized through batch experiments. Stereoselectivity in adsorption increased with decreases in hydrophobicity of the β-blockers. The enantiomeric fraction (EF) of the amount of acebutolol, atenolol and metoprolol sorbed on sludge were 0.27, 0.55 and 0.32, respectively. Thus, Kd values of the (S)-enantiomers of acebutolol and metoprolol were approximately twice that of the (R)-enantiomer, that is, 109 ± 11 and 57 ± 8 L/kg compared to 52 ± 13 and 22 ± 8 L/kg, respectively. There was no statistically significant difference in Kd values of the enantiomers of pindolol and propranolol, suggesting stereoselectivity in adsorption was likely driven by specific polar interactions rather than hydrophobic interactions. The EF value of atenolol decreased from 0.55 ± 0.03 to 0.44 ± 0.04 after modifying the sludge with Triton X 100. These results suggested that surfactants altered adsorption of β-blockers to sludge, likely by forming ion pair complexes that promote hydrophobic interactions with the solid surfaces. PMID:27155096

  16. CLINICAL AND ECONOMICAL ASSESSMENTS OF METOPROLOL TARTRATE/SUCCINATE USAGE IN PATIENTS WITH ISCHEMIC HEART DISEASE

    Directory of Open Access Journals (Sweden)

    M. V. Soura

    2008-01-01

    Full Text Available Clinical and clinicoeconomical studies review is presented as well as results of author’s comparative cost analysis on metoprolol tartrate (Betaloc and metoprolol succinate (Betaloc ZOK usage in patients with ischemic heart disease. Efficacy of metoprolol therapy is proven in randomized clinical studies in patients with angina and myocardial infarction (MI. In angina patients metoprolol prevents cardiac attacks, MI, reduces nitroglycerine consumption, increases exercise tolerability, prolongs the exercise time before ST segment depression (succinate better than tartrate, decrease of angina intensity. In MI patients metoprolol therapy reduces mortality, sudden death, recurring MI and the rate of early post MI angina attacks. Nowadays metoprolol is the only β-blocker having indication on secondary MI prevention. Besides for the present metoprolol succinate is the only β-blocker with proven direct antisclerosis effect. According to Swedish clinicoeconomical study in patients after MI secondary prevention with metoprolol therapy saves the costs in comparison with placebo. American clinicoeconomical model of metoprolol and atenolol usage in all patients with MI could result in significant reduction in mortality and recurring MI rate, prolong the life and improve its quality, save financial resources. The cost of monthly treatment of angina patient with metoprolol tartrate (Betaloc and metoprolol succinate (Betaloc ZOK is 135 and 354 rubles, respectively. The price range of comparative β-blockers in ascending order is the following: atenolol (Atenolol Nicomed → metoprolol tartrate (Betaloc → metoprolol succinate (Betaloc ZOK → bisoprolol (Concor → nebivolol (Nebilet. In conclusion, metoprolol therapy is the one of mostly economically reasonable approach.

  17. Occurrence and fate of the angiotensin II receptor antagonist transformation product valsartan acid in the water cycle--a comparative study with selected β-blockers and the persistent anthropogenic wastewater indicators carbamazepine and acesulfame.

    Science.gov (United States)

    Nödler, Karsten; Hillebrand, Olav; Idzik, Krzysztof; Strathmann, Martin; Schiperski, Ferry; Zirlewagen, Johannes; Licha, Tobias

    2013-11-01

    The substantial transformation of the angiotensin II receptor antagonist valsartan to the transformation product 2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-carboxylic acid (referred to as valsartan acid) during the activated sludge process was demonstrated in the literature and confirmed in the here presented study. However, there was a severe lack of knowledge regarding the occurrence and fate of this compound in surface water and its behavior during drinking water treatment. In this work a comparative study on the occurrence and persistency of valsartan acid, three frequently used β-blockers (metoprolol, atenolol, and sotalol), atenolol acid (one significant transformation product of atenolol and metoprolol), and the two widely distributed persistent anthropogenic wastewater indicators carbamazepine and acesulfame in raw sewage, treated wastewater, surface water, groundwater, and tap water is presented. Median concentrations of valsartan acid in the analyzed matrices were 101, 1,310, 69, treatment plants were confirmed as significant source. Regarding concentration levels of pharmaceutical residues in surface waters valsartan acid was found just as relevant as the analyzed β-blockers and the anticonvulsant carbamazepine. Regarding its persistency in surface waters it was comparable to carbamazepine and acesulfame. Furthermore, removal of valsartan acid during bank filtration was poor, which demonstrated the relevance of this compound for drinking water suppliers. Regarding drinking water treatment (Muelheim Process) the compound was resistant to ozonation but effectively eliminated (≥90%) by subsequent activated carbon filtration. However, without applying activated carbon filtration the compound may enter the drinking water distribution system as it was demonstrated for Berlin tap water.

  18. Role of primary substrate composition and concentration on attenuation of trace organic chemicals in managed aquifer recharge systems

    KAUST Repository

    Alidina, Mazahirali

    2014-11-01

    This study was undertaken to investigate the role of primary substrate composition and concentration on the attenuation of biodegradable emerging trace organic chemicals (TOrCs) in simulated managed aquifer recharge (MAR) systems. Four sets of soil columns were established in the laboratory, each receiving synthetic feed solutions comprising different ratios and concentrations of peptone-yeast and humic acid as the primary substrate to investigate the effect on removal of six TOrCs (atenolol, caffeine, diclofenac, gemfibrozil, primidone, and trimethoprim). Based on abiotic control experiments, adsorption was not identified as a significant attenuation mechanism for primidone, gemfibrozil and diclofenac. Caffeine, atenolol and trimethoprim displayed initial adsorptive losses, however, adsorption coefficients derived from batch tests confirmed that adsorption was limited and in the long-term experiment, biodegradation was the dominant attenuation process. Within a travel time of 16h, caffeine - an easily degradable compound exhibited removal exceeding 75% regardless of composition or concentration of the primary substrate. Primidone - a poorly degradable compound, showed no removal in any column regardless of the nature of the primary substrate. The composition and concentration of the primary substrate, however, had an effect on attenuation of moderately degradable TOrCs, such as atenolol, gemfibrozil and diclofenac, with the primary substrate composition seeming to have a larger impact on TOrC attenuation than its concentration. When the primary substrate consisted mainly of refractory substrate (humic acid), higher removal of the moderately degradable TOrCs was observed. The microbial communities in the columns receiving more refractory carbon, were noted to be more diverse and hence likely able to express a wider range of enzymes, which were more suitable for TOrC transformation. The effect of the primary substrate on microbial community composition, diversity

  19. An analysis of the dissipation of pharmaceuticals under thirteen different soil conditions.

    Science.gov (United States)

    Kodešová, Radka; Kočárek, Martin; Klement, Aleš; Golovko, Oksana; Koba, Olga; Fér, Miroslav; Nikodem, Antonín; Vondráčková, Lenka; Jakšík, Ondřej; Grabic, Roman

    2016-02-15

    The presence of human and veterinary pharmaceuticals in the environment is recognized as a potential threat. Pharmaceuticals have the potential to contaminate soils and consequently surface and groundwater. Knowledge of contaminant behavior (e.g., sorption onto soil particles and degradation) is essential when assessing contaminant migration in the soil and groundwater environment. We evaluated the dissipation half-lives of 7 pharmaceuticals in 13 soils. The data were evaluated relative to the soil properties and the Freundlich sorption coefficients reported in our previous study. Of the tested pharmaceuticals, carbamazepine had the greatest persistence (which was mostly stable), followed by clarithromycin, trimethoprim, metoprolol, clindamycin, sulfamethoxazole and atenolol. Pharmaceutical persistence in soils was mostly dependent on the soil-type conditions. In general, lower average dissipation half-lives and variability (i.e., trimethoprim, sulfamethoxazole, clindamycin, metoprolol and atenolol) were found in soils of better quality (well-developed structure, high nutrition content etc.), and thus, probably better microbial conditions (i.e., Chernozems), than in lower quality soil (Cambisols). The impact of the compound sorption affinity onto soil particles on their dissipation rate was mostly negligible. Although there was a positive correlation between compound dissipation half-life and Freundlich sorption coefficient for clindamycin (R=0.604, psoil-type conditions. Based on the calculated dissipation and sorption data, carbamazepine would be expected to have the greatest potential to migrate in the soil water environment, followed by sulfamethoxazole, trimethoprim and metoprolol. The transport of clindamycin, clarithromycin and atenolol through the vadose zone seems less probable.

  20. Impact of alcohol habits and smoking on the risk of new-onset atrial fibrillation in hypertensive patients with ECG left ventricular hypertrophy: The LIFE Study

    DEFF Research Database (Denmark)

    Ariansen, Inger; Reims, Henrik M; Gjesdal, Knut;

    2012-01-01

    . Methods. In the Losartan Intervention For Endpoint reduction in Hypertension (LIFE) study, a double-blinded, randomized, parallel-group study, 9193 hypertensive patients with electrocardiogram (ECG)-documented left ventricular hypertrophy (LVH), randomized to once-daily losartan- or atenolol......-based antihypertensive therapy were followed for a mean of 4.8 years. At baseline, 8831 patients (54% women, mean age 67 years, mean blood pressure 174/98 mmHg after placebo run-in) had neither a history of AF nor AF on ECG, and they were thus at risk of developing this condition during the study. Results. New-onset AF...

  1. Cardiac sympathetic-parasympathetic balance in rats with experimentally-induced acute chagasic myocarditis O balanço autonômico cardíaco nas ratas com miocardite chagásica aguda experimental

    Directory of Open Access Journals (Sweden)

    Diego F. Davila

    1995-04-01

    Full Text Available To clarify the mechanism responsible for the transient sinus tachycardia in rats with acute chagasic myocarditis, we have examined the cardiac sympathetic-parasympathetic balance of 29 rats inoculated with 200,000 parasites (Trypanosoma cruzi. Sixteen infected animals and 8 controls were studied between days 18 and 21 after inoculation (acute stage. The remaining 13 infected animals and 9 controls were studied between days 60 and 70 after inoculation (sub-acute stage. Under anesthesia (urethane 1.25 g/kg, all animals received intravenous atenolol (5 mg/kg and atropine (10 mg/kg. Acute stage: The baseline heart rate of the infected animals was significantly higher than that of the controls (P Com a finalidade de pesquisar o mecanismo responsável pela taquicardia sinusal transitória que ocorre nas ratas com miocardite chagásica aguda, foi estudado o balanço autonômico cardíaco em 16 ratas inoculadas com Trypanosoma cruzi por via intraperitoneal. Oito animais foram estudados aos 18 e 21 dias após-inoculação (Estádio agudo; os oito animais restantes foram estudados entre os dias 60 a 70 após inoculação (Estádio sub-agudo. Todos os animais em estudo bem como os controles receberam atenolol e atropina. No estádio agudo, a frequência cardíaca basal dos animais infectados foi significativamente maior que a dos controles. A resposta cronotrópica negativa pela administração de atenolol foi quatro vezes maior nos animais infectados. No estádio sub-agudo, a frequência cardíaca basal e a resposta cronotrópica ao atenolol e atropina foi similar nos dois grupos do estudo. Os nossos resultados sugerem que no estádio agudo da miocardite chagásica experimental, a atividade simpática encontra-se periodicamente aumentada.

  2. Temporal variations and trends in loads of commonly used pharmaceuticals to large wastewater treatment plants in Sweden, a case study (Ryaverket)

    DEFF Research Database (Denmark)

    Paxeus, Nicklas; Bester, Kai; El-taliawy, Haitham

    pharmaceuticals. Lower daily loads of pharmaceuticals to WWTP observed for periods of high hydraulic loads were ascribed to the WWTP operation set-up resulting in a partial treatment of the total inflow to the sewer. Trend analysis in loads of individual pharmaceuticals over years indicated an increase...... for diclofenac, no significant changes for ibuprofen and metoprolol and a decrease for the other pharmaceuticals. The declining trend in daily loads per connected person for atenolol, propanolol, citalopram, sulfamethoxazole and trimethoprim was ascribed to their decreased prescription and use. The increase...

  3. Modification of mesoporous silica surface applied as drug delivery system; Modificacao de silica mesoporosa aplicada como sistema de liberacao de droga

    Energy Technology Data Exchange (ETDEWEB)

    Andrade, G.F.; Sousa, A.; Sousa, E.M.B., E-mail: graciellefandrade@yahoo.com.b [Centro de Desenvolvimento da Tecnologia Nuclear (CDTN/CNEN-MG), Belo Horizonte, MG (Brazil)

    2010-07-01

    A mesoporous silica with ordered cubic structure, SBA16, was chemically modified with different alcoxisilanos using solvents with different solubility parameters (methanol and toluene), to evaluate its effectiveness as a matrix for the controlled delivery of atenolol. The structural characteristics of the material were evaluated by small angle XRD, N{sub 2} adsorption and scanning electron microscopy. The degree of functionalization of the matrix was evaluated using techniques of FTIR, thermal analysis and elemental analysis CHN. It was found that the type of solvent influences the degree of functionalization and this significantly affects the release process. (author)

  4. Polar organic chemical integrative sampler (POCIS): application for monitoring organic micropollutants in wastewater effluent and surface water.

    Science.gov (United States)

    Miège, Cécile; Budzinski, Hélène; Jacquet, Romain; Soulier, Coralie; Pelte, Thomas; Coquery, Marina

    2012-02-01

    In this paper, we discuss the advantages and drawbacks of POCIS (Polar Organic Chemical Integrative Sampler) for the evaluation of river water quality downstream of wastewater treatment plants. POCIS proved well adapted to sampling alkylphenols and several pharmaceuticals. Concentration factors and the decrease in limits of quantification, compared to grab water sample analyses, were significant except for hormones, β-blockers and bronchodilators. Promising preliminary results obtained in situ on deuterated atenolol used as a performance reference compound need to be confirmed in-lab. This work confirms that POCIS is a valuable tool for monitoring hydrophilic organic molecules in river and wastewaters. PMID:22193508

  5. Sympathovagal balance analysis in idiopathic postural orthostatic tachycardia syndrome.

    Science.gov (United States)

    Russo, Vincenzo; De Crescenzo, Ilaria; Ammendola, Ernesto; Santangelo, Lucio; Calabrò, Raffaele

    2007-08-01

    The idiopathic postural tachycardia syndrome (POTS) is a complex disorder characterized by chronic orthostatic symptoms and an increase in heart rate within 10 minutes of standing on upright posture, without significant orthostatic hypotension. We describe a case of a 36 year-old patient with POTS, diagnosed by head-up tilt testing. Power spectral analysis of heart rate variability (HRV), performed during the tilt test, revealed the ratio of low and high frequency powers (LF/HF) that increased with the onset of orthostatic intolerance. The increase in LF/HF power ratio may represent sympathetic beta-receptors hyperactivity. Atenolol alleviated his clinical symptoms.

  6. Four-group classification of left ventricular hypertrophy based on ventricular concentricity and dilatation identifies a low-risk subset of eccentric hypertrophy in hypertensive patients

    DEFF Research Database (Denmark)

    Bang, Casper N; Gerdts, Eva; Aurigemma, Gerard P;

    2014-01-01

    -diastolic volume [EDV] index) and concentricity (mass/end-diastolic volume [M/EDV](2/3)) in hypertensive patients. METHODS AND RESULTS: In the Losartan Intervention for Endpoint Reduction (LIFE) echocardiography substudy, 939 hypertensive patients with measurable LVM at baseline were randomized to a mean of 4.......8 years of losartan- or atenolol-based treatment. Patients with LVH (LVM/body surface area ≥116 and ≥96 g/m(2) in men and woman, respectively) were divided into 4 groups-concentric nondilated (increased M/EDV, normal EDV), eccentric dilated (increased EDV, normal M/EDV), concentric dilated (increased M...

  7. A Potential Link between the C5a Receptor 1 and the β1-Adrenoreceptor in the Mouse Heart.

    Directory of Open Access Journals (Sweden)

    Kuan Hua Khor

    Full Text Available Inflammation may contribute to the pathogenesis of specific cardiovascular diseases, but it is uncertain if mediators released during the inflammatory process will affect the continued efficacy of drugs used to treat clinical signs of the cardiac disease. We investigated the role of the complement 5a receptor 1 (C5aR1/CD88 in the cardiac response to inflammation or atenolol, and the effect of C5aR1 deletion in control of baseline heart rate in an anesthetized mouse model.An initial study showed that PMX53, an antagonist of C5aR1 in normal C57BL6/J (wild type, WT mice reduced heart rate (HR and appeared to have a protective effect on the heart following induced sepsis. C5aR1 knockout (CD88-/- mice had a lower HR than wild type mice, even during sham surgery. A model to assess heart rate variability (HRV in anesthetized mice was developed to assess the effects of inhibiting the β1-adrenoreceptor (β1-AR in a randomized crossover study design.HR and LF Norm were constitutively lower and SDNN and HF Norm constitutively higher in the CD88-/- compared with WT mice (P 0.05, except for the reduced LF/HF (Lower frequency/High frequency ratio (P< 0.05 at 60 min post-atenolol, suggesting increased parasympathetic tone of the heart due to the effect of atenolol administration. The HR of the WT mice were lower post atenolol compared to the CD88-/- mice (P = 0.001 but the HRV of CD88-/- mice were significantly increased (P< 0.05, compared with WT mice.Knockout of the C5aR1 attenuated the effect of β1-AR in the heart, suggesting an association between the β1-AR and C5aR1, although further investigation is required to determine if this is a direct or causal association.

  8. Acyanotic tetralogy of Fallot in a Persian cat.

    Science.gov (United States)

    Choi, Won-Jin; Suh, Sang-Il; Choi, Ran; Hyun, Changbaig

    2016-06-01

    An 8-year-old, intact male Persian cat was presented with a prominent heart murmur, exercise intolerance, anorexia, and periodontitis. There was no cyanosis and no laboratory evidence for systemic hypoxemia. Echocardiography showed a dextropositioned aorta, moderate pulmonic stenosis (maximal velocity 4.06 m/s), ventricular septal defect, and right ventricular hypertrophy. The shunt direction was predominantly left-to-right in systole and minimally right-to-left in diastole. The cat was diagnosed with acyanotic (pink) tetralogy of Fallot and was managed medically with atenolol. PMID:27247457

  9. Monozygotic twins with Marfan's syndrome and ascending aortic aneurysm.

    Science.gov (United States)

    Redruello, Héctor Jorge; Cianciulli, Tomas Francisco; Rostello, Eduardo Fernandez; Recalde, Barbara; Lax, Jorge Alberto; Picone, Victorio Próspero; Belforte, Sandro Mario; Prezioso, Horacio Alberto

    2007-08-01

    Marfan's syndrome is a hereditary connective tissue disease, in which cardiovascular abnormalities (especially aortic root dilatation) are the most important cause of morbidity and mortality. In this report, we describe two 24-year-old twins, with a history of surgery for lens subluxation and severe cardiovascular manifestations secondary to Marfan's syndrome. One of the twins suffered a type A aortic dissection, which required replacement of the ascending aorta, and the other twin had an aneurysmal dilatation of the ascending aorta (46mm) and was prescribed medical treatment with atenolol and periodic controls to detect the presence of a critical diameter (50mm) that would indicate the need for prophylactic surgery.

  10. Impact of carbon dosing on micro-pollutants removal in MBBR post-denitrification systems

    DEFF Research Database (Denmark)

    Escola, Monica; Torresi, Elena; Gy Plósz, Benedek;

    -sulfadiazine, atenolol, citalopram, propranolol and trimethoprim were easily removed, with removal rate constants ranging from 10.1 to 17.9 L gTSS -1d-1. Other spiked compounds were moderately well removed (namely ibuprofen, clarithromycin, iopromide, metoprolol, iohexol, iomeprol, venlafaxine, erythromycin, sotalol...... layer determined de removal of such compounds. In contrast, the biofilm developed under methanol dosing presented the highest removal rate constants for moderately degraded micro-pollutants, meaning that methanol primary-metabolism favored the co-metabolism of these micro-pollutants. Both, continuous...

  11. ''In-house'' pharmacological management for computed tomography coronary angiography: heart rate reduction, timing and safety of different drugs used during patient preparation

    Energy Technology Data Exchange (ETDEWEB)

    Maffei, Erica; Tedeschi, Carlo; Seitun, Sara; Ruffini, Livia; Aldrovandi, Annachiara [Azienda Ospedaliero - Universitaria di Parma, Department of Radiology and Cardiology, Parma (Italy); Palumbo, Alessandro A.; Martini, Chiara [Azienda Ospedaliero - Universitaria di Parma, Department of Radiology and Cardiology, Parma (Italy); Erasmus Medical Center, Department of Radiology and Cardiology, Rotterdam (Netherlands); Tarantini, Giuseppe [Azienda Ospedaliero - Universitaria di Parma, Department of Radiology and Cardiology, Parma (Italy); University of Padua, Department of Cardiology, Padua (Italy); Weustink, Annick C.; Meijboom, Willem B.; Mollet, Nico R.; Krestin, Gabriel P.; Feyter, Pim J. de [Erasmus Medical Center, Department of Radiology and Cardiology, Rotterdam (Netherlands); Cademartiri, Filippo [Azienda Ospedaliero - Universitaria di Parma, Department of Radiology and Cardiology, Parma (Italy); Erasmus Medical Center, Department of Radiology and Cardiology, Rotterdam (Netherlands); Azienda Ospedaliero-Universitaria - Parma, Department of Radiology c/o Piastra Tecnica - Piano 0, Parma (Italy)

    2009-12-15

    We retrospectively evaluated the effect, timing and safety of different pharmacological strategies during 64-slice CT coronary angiography (CT-CA). From the institutional database of CT-CA we enrolled 560 consecutive patients with suspected coronary artery disease. The type of drug preparation (group 1 = no treatment; group 2 = oral metoprolol; group 3 = other; group 4 = intravenous (IV) atenolol; group 5 = IV atenolol + nitrates; NR = non-responders), timing, and adverse effects were recorded. Heart rate (HR) during different preparation phases was recorded. Four adverse effects were recorded, none of which was attributable to pharmacological treatment. In all groups, except group 1, the HR on arrival was significantly reduced by the pharmacological treatment (p < 0.01). Group 4 showed the best (-16 {+-} 8 bpm) HR reduction. There was no significant effect on HR due to nitrates (p = 0.49), while a slight increase due to contrast material was noted (p < 0.05). Average time required for preparation was 44 {+-} 25 min. Groups 4 and 5 showed the most effective timing (8 {+-} 9 min and 8 {+-} 8 min, respectively; p < 0.01). Pharmacological preparation in patients undergoing CT-CA is safe and effective. Best results in terms of HR reduction and fast preparation are obtained with IV administration of beta-blockers. (orig.)

  12. Caracterización del consumo de betabloqueadores en una farmacia de un área urbana / Characterization of beta blocker consumption in a pharmacy of an urban area

    Directory of Open Access Journals (Sweden)

    Anayda Alfonso Hidalgo

    2015-08-01

    Full Text Available Introducción: La hipertensión arterial presenta una alta prevalencia como motivo de consulta frecuente. Esta enfermedad es el principal factor de riesgo de enfermedad cerebrovascular y los betabloqueadores constituyen uno de los pilares de su trata-miento. Objetivo: Caracterizar el uso de estos fármacos en la población hipertensa de una farmacia de un área urbana. Método: Se realizó una investigación descriptiva de corte transversal, en la Farmacia 6.76 de Santa Clara en Villa Clara, Cuba, durante los meses de octubre a diciembre de 2013. Resultados: Los principales resultados mostraron un predominio del consumo de be-tabloqueadores en las mujeres (53,4 %, en las edades entre 50-64 años (48,9 %, y el fármaco más utilizado fue el atenolol (93,2 %. Su dosis predominante fue de 1 table-ta diaria (68,3 %, de propranolol, 2 (50,0 %; y los fármacos más asociados fueron los diuréticos e inhibidores de la enzima conversora de angiotensina. Conclusiones: El atenolol fue el BB más utilizado en esta investigación y se asoció fre-cuentemente a diuréticos e IECA. Predominaron los pacientes del sexo femenino, con edades entre 50-64 años y HTA grado 2.

  13. Comparative enantiomer affinity pattern of β-blockers in aqueous and nonaqueous CE using single-component anionic cyclodextrins.

    Science.gov (United States)

    Feng, Ying; Wang, Tingting; Jiang, Zhengjin; Chankvetadze, Bezhan; Crommen, Jacques

    2015-06-01

    A series of eight chiral β-blocker drugs, acebutolol, atenolol, carazolol, carteolol, carvedilol, propranolol, sotalol, and talinolol, have been enantioseparated using two single-component anionic β-CD derivatives, namely heptakis (2,3-di-O-methyl-6-sulfo)-β-CD (HDMS-β-CD) and heptakis (2,3-di-O-acetyl-6-sulfo)-β-CD (HDAS-β-CD), in aqueous CE and NACE. The influence of the nature of substituents (methyl or acetyl) in positions 2 and 3 on the CD derivatives and of the electrophoretic medium (water or methanol) on the enantioselectivity and enantiomer affinity pattern (EAP) of these structurally related compounds was systematically studied. All eight β-blockers could be enantioseparated at least partially in the four CE systems, except sotalol with HDMS-β-CD in NACE. In general, lower affinity and enantioselectivity were obtained in the presence of HDMS-β-CD compared to HDAS-β-CD. Reversals of EAPs were observed for all compounds. EAPs toward these two CDs were found to be opposite to each other in NACE for all compounds except carvedilol and in aqueous CE for atenolol, carteolol, talinolol, and sotalol. It is particularly noteworthy that opposite EAPs were also observed using the same CD derivative when the aqueous BGE was replaced with the methanolic one: for carazolol, carvedilol, and propranolol in the presence of HDMS-β-CD and for acebutolol and carvedilol with HDAS-β-CD.

  14. Pharmaceutical Residues Affecting the UNESCO Biosphere Reserve Kristianstads Vattenrike Wetlands: Sources and Sinks.

    Science.gov (United States)

    Björklund, Erland; Svahn, Ola; Bak, Søren; Bekoe, Samuel Oppong; Hansen, Martin

    2016-10-01

    This study is the first to investigate the pharmaceutical burden from point sources affecting the UNESCO Biosphere Reserve Kristianstads Vattenrike, Sweden. The investigated Biosphere Reserve is a >1000 km(2) wetland system with inflows from lakes, rivers, leachate from landfill, and wastewater-treatment plants (WWTPs). We analysed influent and treated wastewater, leachate water, lake, river, and wetland water alongside sediment for six model pharmaceuticals. The two WWTPs investigated released pharmaceutical residues at levels close to those previously observed in Swedish monitoring exercises. Compound-dependent WWTP removal efficiencies ranging from 12 to 100 % for bendroflumethiazide, oxazepam, atenolol, carbamazepine, and diclofenac were observed. Surface-water concentrations in the most affected lake were ≥100 ng/L for the various pharmaceuticals with atenolol showing the highest levels (>300 ng/L). A small risk assessment showed that adverse single-substance toxicity on aquatic organisms within the UNESCO Biosphere Reserve is unlikely. However, the effects of combinations of a large number of known and unknown pharmaceuticals, metals, and nutrients are still unknown.

  15. Pharmaceuticals and endocrine disrupting compounds in U.S. drinking water.

    Science.gov (United States)

    Benotti, Mark J; Trenholm, Rebecca A; Vanderford, Brett J; Holady, Janie C; Stanford, Benjamin D; Snyder, Shane A

    2009-02-01

    The drinking water for more than 28 million people was screened for a diverse group of pharmaceuticals, potential endocrine disrupting compounds (EDCs), and other unregulated organic contaminants. Source water, finished drinking water, and distribution system (tap) water from 19 U.S. water utilities was analyzed for 51 compounds between 2006 and 2007. The 11 most frequently detected compounds were atenolol, atrazine, carbamazepine, estrone, gemfibrozil, meprobamate, naproxen, phenytoin, sulfamethoxazole, TCEP, and trimethoprim. Median concentrations of these compounds were less than 10 ng/L, except for sulfamethoxazole in source water (12 ng/L), TCEP in source water (120 ng/L), and atrazine in source, finished, and distribution system water (32, 49, and 49 ng/L). Atrazine was detected in source waters far removed from agricultural application where wastewater was the only known source of organic contaminants. The occurrence of compounds in finished drinking water was controlled by the type of chemical oxidation (ozone or chlorine) used at each plant. At one drinking water treatment plant, summed monthly concentrations of the detected analytes in source and finished water are reported. Atenolol, atrazine, DEET, estrone, meprobamate, and trimethoprim can serve as indicator compounds representing potential contamination from other pharmaceuticals and EDCs and can gauge the efficacy of treatment processes. PMID:19244989

  16. Investigating the removal of some pharmaceutical compounds in hospital wastewater treatment plants operating in Saudi Arabia.

    Science.gov (United States)

    Al Qarni, Hamed; Collier, Philip; O'Keeffe, Juliette; Akunna, Joseph

    2016-07-01

    The concentrations of 12 pharmaceutical compounds (atenolol, erythromycin, cyclophosphamide, paracetamol, bezafibrate, carbamazepine, ciprofloxacin, caffeine, clarithromycin, lidocaine, sulfamethoxazole and N-acetylsulfamethoxazol (NACS)) were investigated in the influents and effluents of two hospital wastewater treatment plants (HWWTPs) in Saudi Arabia. The majority of the target analytes were detected in the influent samples apart from bezafibrate, cyclophosphamide, and erythromycin. Caffeine and paracetamol were detected in the influent at particularly high concentrations up to 75 and 12 ug/L, respectively. High removal efficiencies of the pharmaceutical compounds were observed in both HWWTPs, with greater than 90 % removal on average. Paracetamol, sulfamethoxazole, NACS, ciprofloxacin, and caffeine were eliminated by between >95 and >99 % on average. Atenolol, carbamazepine, and clarithromycin were eliminated by >86 % on average. Of particular interest were the high removal efficiencies of carbamazepine and antibiotics that were achieved by the HWWTPs; these compounds have been reported to be relatively recalcitrant to biological treatment and are generally only partially removed. Elevated temperatures and high levels of sunlight were considered to be the main factors that enhanced the removal of these compounds. PMID:26996911

  17. Ultrasound-assisted extraction method for the simultaneous determination of emerging contaminants in freshwater sediments.

    Science.gov (United States)

    de Sousa, Diana Nara Ribeiro; Grosseli, Guilherme Martins; Mozeto, Antonio Aparecido; Carneiro, Renato Lajarim; Fadini, Pedro Sergio

    2015-10-01

    Sediments are the fate of several emerging organic contaminants, such as pharmaceuticals, personal care products and hormones, and therefore an important subject in environmental monitoring studies. In the present work, a simple and sensitive method was developed, validated and applied for the simultaneous extraction of atenolol, caffeine, carbamazepine, diclofenac, ibuprofen, naproxen, propranolol, triclosan, estrone, 17-β-estradiol and 17-α-ethinylestradiol using ultrasound-assisted extraction from freshwater sediment samples followed by solid-phase extraction clean-up and liquid chromatography with tandem mass spectrometry detection. The solvent type and extraction pH were evaluated to obtain the highest recoveries of the compounds. The best method shows absolute recoveries between 54.0 and 94.4% at 50 ng/g concentration. The method exhibits good precision with relative standard deviation ranging from 1.0-16%. The detection and quantification limits ranged from 0.006-0.067 and 0.016-0.336 ng/g, respectively. The developed method was successfully applied to freshwater sediment samples collected from different sites in Jundiaí River basin of São Paulo State, Brazil. The compounds atenolol, caffeine, propranolol and triclosan were detected in all the sampling sites with concentrations of 13.8, 41.0, 28.5 and 176 ng/g, respectively. PMID:26257164

  18. Microcosm experiments to control anaerobic redox conditions when studying the fate of organic micropollutants in aquifer material

    Science.gov (United States)

    Barbieri, Manuela; Carrera, Jesús; Sanchez-Vila, Xavier; Ayora, Carlos; Cama, Jordi; Köck-Schulmeyer, Marianne; López de Alda, Miren; Barceló, Damià; Tobella Brunet, Joana; Hernández García, Marta

    2011-11-01

    The natural processes occurring in subsurface environments have proven to effectively remove a number of organic pollutants from water. The predominant redox conditions revealed to be one of the controlling factors. However, in the case of organic micropollutants the knowledge on this potential redox-dependent behavior is still limited. Motivated by managed aquifer recharge practices microcosm experiments involving aquifer material, settings potentially feasible in field applications, and organic micropollutants at environmental concentrations were carried out. Different anaerobic redox conditions were promoted and sustained in each set of microcosms by adding adequate quantities of electron donors and acceptors. Whereas denitrification and sulfate-reducing conditions are easily achieved and maintained, Fe- and Mn-reduction are strongly constrained by the slower dissolution of the solid phases commonly present in aquifers. The thorough description and numerical modeling of the evolution of the experiments, including major and trace solutes and dissolution/precipitation of solid phases, have been proven necessary to the understanding of the processes and closing the mass balance. As an example of micropollutant results, the ubiquitous beta-blocker atenolol is completely removed in the experiments, the removal occurring faster under more advanced redox conditions. This suggests that aquifers constitute a potentially efficient alternative water treatment for atenolol, especially if adequate redox conditions are promoted during recharge and long enough residence times are ensured.

  19. Beneficial effects of switching from β-blockers to nebivolol on the erectile function of hypertensive patients

    Institute of Scientific and Technical Information of China (English)

    Michael Doumas; Alexandros Tsakiris; Stella Douma; Alkiviadis Grigorakis; Angelos Papadopoulos; Athina Hounta; Sotirios Tsiodras; Dimitrios Dimitriou; Helen Giamarellou

    2006-01-01

    Aim: To investigate the effect of substituting β-blockers with nebivolol on the erectile function of patients suffering from essential hypertension. Methods: Forty-four young and middle-aged men (31-65 years) with essential hypertension visited our outpatient clinic and took β-blocker treatment (atenolol, metoprolol or bisoprolol) for more than 6months. All the patients completed a questionnaire regarding erectile function (International Index for Erectile Function).Patients were then switched to an equipotent dose of nebivolol for 3 months and, at the end of this time period, filled out the same questionnaire. Results: Twenty-nine out of the 44 (65.9%) patients who took β-blockers (atenolol,metoprolol or bisoprolol) had exhibited erectile dysfunction (ED). Their systolic and diastolic blood pressure did not change significantly with the treatment switch. In 20 out of these 29 (69%) patients, a significant improvement in the erectile function score was exhibited after 3 months of nebivolol administration, and in 11 of these 20 patients, erectile function was normalized. Conclusion: Nebivolol seems to have a beneficial effect on ED (possibly due to increased nitric oxide availability); however, further prospective, randomized, placebo-controlled studies are needed to confirm the beneficial effects of nebivolol.

  20. Oral ‘hydrogen water' induces neuroprotective ghrelin secretion in mice

    Science.gov (United States)

    Matsumoto, Akio; Yamafuji, Megumi; Tachibana, Tomoko; Nakabeppu, Yusaku; Noda, Mami; Nakaya, Haruaki

    2013-01-01

    The therapeutic potential of molecular hydrogen (H2) is emerging in a number of human diseases and in their animal models, including in particular Parkinson's disease (PD). H2 supplementation of drinking water has been shown to exert disease-modifying effects in PD patients and neuroprotective effects in experimental PD model mice. However, H2 supplementation does not result in detectable changes in striatal H2 levels, indicating an indirect effect. Here we show that H2 supplementation increases gastric expression of mRNA encoding ghrelin, a growth hormone secretagogue, and ghrelin secretion, which are antagonized by the β1-adrenoceptor blocker, atenolol. Strikingly, the neuroprotective effect of H2 water was abolished by either administration of the ghrelin receptor-antagonist, D-Lys3 GHRP-6, or atenolol. Thus, the neuroprotective effect of H2 in PD is mediated by enhanced production of ghrelin. Our findings point to potential, novel strategies for ameliorating pathophysiology in which a protective effect of H2 supplementation has been demonstrated. PMID:24253616

  1. Anti-hypertensive drugs have different effects on ventricular hypertrophy regression

    Directory of Open Access Journals (Sweden)

    Celso Ferreira Filho

    2010-01-01

    Full Text Available OBJECTIVES: There is a direct relationship between the regression of left ventricular hypertrophy (LVH and a decreased risk of mortality. This investigation aimed to describe the effects of anti-hypertensive drugs on cardiac hypertrophy through a meta-analysis of the literature. METHODS: The Medline (via PubMed, Lilacs and Scielo databases were searched using the subject keywords cardiac hypertrophy, antihypertensive and mortality. We aimed to analyze the effect of anti-hypertensive drugs on ventricle hypertrophy. RESULTS: The main drugs we described were enalapril, verapamil, nifedipine, indapamina, losartan, angiotensin-converting enzyme inhibitors and atenolol. These drugs are usually used in follow up programs, however, the studies we investigated used different protocols. Enalapril (angiotensin-converting enzyme inhibitor and verapamil (Ca++ channel blocker caused hypertrophy to regress in LVH rats. The effects of enalapril and nifedipine (Ca++ channel blocker were similar. Indapamina (diuretic had a stronger effect than enalapril, and losartan (angiotensin II receptor type 1 (AT1 receptor antagonist produced better results than atenolol (selective β1 receptor antagonist with respect to LVH regression. CONCLUSION: The anti-hypertensive drugs induced various degrees of hypertrophic regression.

  2. Postmeningitis headache: case report Cefaléia pós-meningite: relato de caso

    Directory of Open Access Journals (Sweden)

    André Palma da Cunha Matta

    2007-06-01

    Full Text Available We report a case of a 18-year-old female patient that developed a migraine-like headache following an acute meningococcal meningitis. She had no previous history of recurrent headaches. The pain was intense, pulsatile and throbbing, typically unilateral, without aura. Its frequency increased during the following weeks and a prophylactic treatment with amitriptyline and atenolol was initiated. There was remission of the attacks.Relatamos o caso de uma paciente de 18 anos, previamente hígida, sem história pregressa de cefaléia, que apresentou um quadro agudo caracterizado por febre, cefaléia holocraniana, sonolência, vômitos e sinais de irritação meníngea. Teve investigação laboratorial compatível com meningite meningocócica. Recebeu o tratamento adequado, evoluindo com regressão do quadro infeccioso. Desenvolveu, entretanto, episódios recorrentes de cefaléia pulsátil, sem aura, unilateral, de forte intensidade e acompanhada por náusea e fotofobia. A freqüência dos episódios aumentou progressivamente até que se instituiu tratamento profilático com atenolol e amitriptilina, havendo remissão da dor.

  3. Transport of beta-blockers and calcium antagonists by diffusion in cat myocardium

    DEFF Research Database (Denmark)

    Haunsø, Stig; Sejrsen, Per; Svendsen, Jesper Hastrup

    1991-01-01

    of the concentration profile of 3H-metoprolol and 3H-atenolol into the tissue during 20 min was calculated to be 0.36 and 0.31 mm, respectively. The protein binding of 14C-verapamil and 3H-propranolol caused a significant fall in the progression to 0.24 mm for both drugs. These results indicate that, by diffusion......Beta-blockers and calcium antagonists have been claimed to possess cardioprotective properties. This study addresses the question of whether a significant amount of these drugs will reach the cardiac myocytes during no-flow ischemia, where solute transport depends solely on diffusion....... In anesthetized cats the hearts were excised. Apparent diffusion coefficients in cat myocardium at 37 degrees C (D'37) for 14C-verapamil (protein bound), 3H-metoprolol (lipophilic), 3H-atenolol (hydrophilic), and 3H-propranolol (lipophilic and protein bound) were determined by means of a "true transient diffusion...

  4. Corrigendum to “Sorption/desorption of non-hydrophobic and ionisable pharmaceutical and personal care products from reclaimed water onto/from a natural sediment” Sci Total Environ 472 (2014) 273–281

    International Nuclear Information System (INIS)

    In the present work, the sorption of pharmaceutical and personal care products (PPCPs) (acetaminophen, atenolol, carbamazepine, caffeine, naproxen and sulphamethoxazole) onto the natural organic matter (NOM) and the inorganic surfaces of a natural sandy loam sediment was quantified separately. The quantification was based on the PPCP charge, their degree of ionisation, their octanol-water partitioning coefficient (KOW) and the sediment organic carbon fraction (ƒOC). PPCP desorption from the sediment was examined under conditions of infiltrating water containing a high concentration of inorganic ions (mimicking infiltrating reclaimed water), and a low concentration (and smaller diversity) of inorganic ions (mimicking rainwater infiltration). Batch tests were performed using a sediment/water ratio of 1:4 and a PPCP initial concentration ranging from 1 to 100 μg L−1. The results showed the type and degree of PPCP ionisation to strongly influence the sorption of these compounds onto the sediment. The sorption of cationic species onto the sediment was higher than that of anionic species and mostly reversible; the sorption of neutral species was negligible with the exception of caffeine. The anionic species sorbed less onto the sediment, but also desorbed less easily. Most of the compounds showed a sorption that was highly influenced by interaction with mineral surfaces. The presence of inorganic ions had no impact on the desorption of the PPCPs from the sediment. According to the calculated percentages of removal, the mobility followed the order: carbamazepine > acetaminophen > naproxen > atenolol > sulphamethoxazole > caffeine

  5. Development and evaluation of degradable hydroxyapatite/sodium silicate composite for low-dose drug delivery systems

    Indian Academy of Sciences (India)

    R MORSY

    2016-09-01

    This study was designed to develop innovative degradable hydroxyapatite (HAp)-based systems working as potential carriers for low-dose drugs. The HAp-based systems combine three components: HAp, sodium silicate and citric acid (HSC), which together could exhibit optimal characteristics as drug carriers. Both synthetic HAp (s-HAp) and extracted biological HAp (b-HAp) were used as sources of HAp due to their optimal biological properties and adsorption capacity. The s-HAp powder was prepared by co-precipitation method, while the b-HAp powder was extracted from bovine bone. Aqueous drug solutions of the atenolol, antihypertensive drug, were used as a model drug to investigate the drug release behaviour from HSC composites. The properties of s-HAP, b-HAp powders and HSC composite tablets were characterized by conventional methods. The results revealed that both s-HAp and b-HAp are pure powders and exhibited agglomerated microstructures with grain sizes less than 100 $\\mu$m. The HSC composite tablets exhibited a dense structure, excellent compressive strength and excellent in-vitro release behaviour of atenolol. The results indicated that HAp powders and their composite tablets can be promised as economic raw materials and carriers for low-dose drugs.

  6. Hypertension and insulin resistance are not directly related in obese dogs.

    Science.gov (United States)

    Rocchini, Albert P; Yang, John Q; Gokee, Amy

    2004-05-01

    In dogs fed a high-fat diet, we determined whether there was a direct relation between obesity-induced insulin resistance and obesity-induced hypertension. Thirty-six adult mongrel dogs were chronically instrumented and assigned to receive either a high-fat diet alone (n=7) or a high-fat diet combined with a low-sodium diet plus furosemide (n=6), prazosin plus atenolol (n=7), clonidine (n=10), or aspirin (n=6). Blood pressure, heart rate, and body weight were measured daily. Insulin resistance was assessed with a single-dose euglycemic hyperinsulinemic clamp (2 mU x kg(-1) x min(-1)) before and after 1, 3, and 6 weeks of the high-fat diet. The low-salt diet plus furosemide, prazosin plus atenolol, and clonidine treatments prevented the hypertension associated with feeding the dogs a high-fat diet. Only clonidine treatment totally prevented the development of insulin resistance, and high-dose aspirin, known to prevent insulin resistance by inhibition of the activity of IkappaB kinase-beta, decreased the degree of insulin resistance by almost 70%. However, aspirin had no effect on the development of hypertension. We conclude that obesity-induced hypertension and obesity-induced insulin resistance are not directly related. In addition, there is a suggestion that insulin resistance in this experimental model is mediated through the central and or peripheral alpha2-adrenoceptors, whereas hypertension is mediated through the alpha1- and or beta-adrenoceptors.

  7. Los betabloqueadores como primera opción del tratamiento en la hipertensión no complicada ¿posible o no?

    Directory of Open Access Journals (Sweden)

    Alberto Morales Salinas

    2011-02-01

    Full Text Available Hasta la publicación de la guía del National Institute for Health and Clinical Excellence del 2006, existía consenso en las principales directrices de hipertensión arterial, en cuanto a que los beta-bloqueadores podían utilizarse como tratamiento de primera línea en la hipertensión arterial no complicada. Los cambios sugeridos consistían en considerar a los beta-bloqueadores como antihipertensivos de cuarta línea. Estas modificaciones estuvieron sustentadas fundamentalmente en los resultados de dos grandes ensayos aleatorizados; sin embargo, la guía del 2007 de las Sociedades Europea de Hipertensión y Cardiología, así como su actualización del 2009, mantuvieron a los beta-bloqueadores como droga de primera línea. En el presente artículo se realiza un análisis crítico de las principales evidencias disponibles en contra de los beta-bloqueadores. Se concluye que las limitaciones del atenolol no deben ser extendidas a los nuevos beta-bloqueadores, además de que estas limitaciones pudiesen estar influidas por una dosificación subóptima del atenolol.

  8. Use of beta adrenoceptor blockade during and after acute myocardial infarction.

    Science.gov (United States)

    Sleight, P

    1986-01-01

    In the last year, two large randomized controlled trials of metoprolol (MIAMI, almost 6,000 patients) and atenolol (ISIS 1, over 16,000 patients) given intravenously within 12 hours of the onset of acute myocardial infarction reduced mortality by about 15% in low-risk subjects. The reduction was significant for atenolol (2P = 0.04) but not for metoprolol, probably because of the smaller size of that trial. The reduction in mortality in both trials was nearly all in the first 36 hours, a finding that reduced the fears that the treatment might produce irreversible failure, shock, or heart block. Tolerance in these relatively low-risk subjects (control mortality about 5%) was good. Inotropes were used in 1-2% more subjects in the beta-blocked group but were effective in reversing the side effects without increasing mortality. No clear subgroups (age, sex, site, time from onset, initial blood pressure or heart rate) were found in which treatment was more beneficial. In the ISIS study, patients with higher heart rates were more likely to need inotropes after beta blockade and patients with long PR intervals at entry were more likely to develop block. Neither of these complications resulted in excess mortality in the blocked group, which suggests that these adverse effects were largely reversible. PMID:2871805

  9. Corrigendum to “Sorption/desorption of non-hydrophobic and ionisable pharmaceutical and personal care products from reclaimed water onto/from a natural sediment” Sci Total Environ 472 (2014) 273–281

    Energy Technology Data Exchange (ETDEWEB)

    Martínez-Hernández, Virtudes, E-mail: virtudes.martinez@imdea.org [IMDEA Agua, Madrid Institute for Advanced Studies in Water, Parque Científico Tecnológico de la Universidad de Alcalá, 28805 Alcalá de Henares, Madrid (Spain); Meffe, Raffaella; Herrera, Sonia [IMDEA Agua, Madrid Institute for Advanced Studies in Water, Parque Científico Tecnológico de la Universidad de Alcalá, 28805 Alcalá de Henares, Madrid (Spain); Arranz, Elena [University of Alcalá, Geography and Geology Department, 28871 Alcalá de Henares, Madrid (Spain); Bustamante, Irene de [IMDEA Agua, Madrid Institute for Advanced Studies in Water, Parque Científico Tecnológico de la Universidad de Alcalá, 28805 Alcalá de Henares, Madrid (Spain); University of Alcalá, Geography and Geology Department, 28871 Alcalá de Henares, Madrid (Spain)

    2015-02-01

    In the present work, the sorption of pharmaceutical and personal care products (PPCPs) (acetaminophen, atenolol, carbamazepine, caffeine, naproxen and sulphamethoxazole) onto the natural organic matter (NOM) and the inorganic surfaces of a natural sandy loam sediment was quantified separately. The quantification was based on the PPCP charge, their degree of ionisation, their octanol-water partitioning coefficient (K{sub OW}) and the sediment organic carbon fraction (ƒ{sub OC}). PPCP desorption from the sediment was examined under conditions of infiltrating water containing a high concentration of inorganic ions (mimicking infiltrating reclaimed water), and a low concentration (and smaller diversity) of inorganic ions (mimicking rainwater infiltration). Batch tests were performed using a sediment/water ratio of 1:4 and a PPCP initial concentration ranging from 1 to 100 μg L{sup −1}. The results showed the type and degree of PPCP ionisation to strongly influence the sorption of these compounds onto the sediment. The sorption of cationic species onto the sediment was higher than that of anionic species and mostly reversible; the sorption of neutral species was negligible with the exception of caffeine. The anionic species sorbed less onto the sediment, but also desorbed less easily. Most of the compounds showed a sorption that was highly influenced by interaction with mineral surfaces. The presence of inorganic ions had no impact on the desorption of the PPCPs from the sediment. According to the calculated percentages of removal, the mobility followed the order: carbamazepine > acetaminophen > naproxen > atenolol > sulphamethoxazole > caffeine.

  10. Synchronized separation of seven medications representing most commonly prescribed antihypertensive classes by using reversed-phase liquid chromatography: Application for analysis in their combined formulations.

    Science.gov (United States)

    Ebeid, Walid M; Elkady, Ehab F; El-Zaher, Asmaa A; El-Bagary, Ramzia I; Patonay, Gabor

    2014-04-01

    A reversed-phase high-performance liquid chromatography method was developed for the simultaneous determination of the diuretic, hydrochlorothiazide, along with six drugs representing the most commonly prescribed antihypertensive pharmacological classes such as atenolol, a selective β1 blocker, amlodipine besylate, a calcium channel blocker, moexipril hydrochloride, an angiotensin-converting-enzyme inhibitor, valsartan and candesartan cilexetil, which are angiotensin II receptor blockers, and aliskiren hemifumarate, a renin inhibitor, using irbesartan as an internal standard. The chromatographic separation was achieved using acetonitrile/sodium phosphate dibasic buffer (0.02 M, pH 5.5) at a flow rate of 1 mL/min in gradient elution mode at ambient temperature on a stationary phase composed of an Eclipse XDB-C18 (4.6 × 150 mm, 5 μm) column. UV detection was carried out at 220 nm. The method was validated according to ICH guidelines. Linearity, accuracy, and precision were satisfactory over the concentration ranges of 2-40 μg/mL for hydrochlorothiazide and candesartan cilexetil, 20-120, 10-160, 5-40, 20-250, and 5-50 μg/mL for atenolol, valsartan, moexipril hydrochloride, aliskiren hemifumarate, and amlodipine besylate, respectively. The method was successfully applied for the determination of each of the studied drugs in their combined formulations with hydrochlorothiazide. The developed method is suitable for the quality control and routine analysis of the cited drugs in their pharmaceutical dosage forms. PMID:24482404

  11. Assessment of blood brain barrier penetration of drugs using a rat steady-state brain distribution model%大鼠稳态脑分布模型评价药物的血脑屏障通透性

    Institute of Scientific and Technical Information of China (English)

    原梅; 阳海鹰; 钟玉环; 庄笑梅; 李桦

    2015-01-01

    目的 建立大鼠稳态脑分布模型用于评价安替比林、阿替洛尔和ZZB 系列新药候选化合物的稳态脑分布和血脑屏障通透性.方法 大鼠静脉推注负荷剂量的药物后恒量输注使血药浓度达到稳态,取血和脑组织样品,LC-MS/MS 定量测定血浆和脑组织药物浓度,计算稳态脑血比值(Kp值).在Caco-2 单层细胞体外模型上评价受试药物的双向跨膜通透性,计算表观通透系数(Papp).结果 安替比林和阿替洛尔分别为已知的血脑屏障易通透和难通透药物.安替比林的平均稳态脑分布浓度为(2561±125)ng/g,Kp值为0.93±0.04.阿替洛尔则分别为(20.1±0.8)ng/g 和0.015±0.002.安替比林的Kp值约为阿替洛尔的60 倍.ZZB 系列化合物的结构相似,但Kp值的差异较大,从0.044 到6.41,并与Caco-2 细胞模型的Papp值不相关.结论 建立的大鼠稳态脑分布模型可快速形成稳态血浆浓度,适用于药物血脑屏障通透程度的评价,方法简单、可靠且经济.%Objective To develop a steady-state brain distribution model in rats and to assess the blood brain barrier(BBB) penetration of antipyrine, atenolol and a group of ZZB candidate compounds. Methods Antipyrine, atenolol and ZZB compounds were administered to rats by an initial iv bolus dose (loading dose) followed by iv infusion at a constant rate for 30-40 min to reach steady-state plasma kinetics. The blood and brain tissue samples were then collected. The steady-state concentrations of the samples were measured by LC-MS/MS. The steady-state ratio of brain to plasma concentration (Kp) was calculated. The drugs and candidate compounds were also tested with Caco-2 cell model and the apparent bidirectional transport permeability coefficient (Papp) was obtained. Results Antipyrine and atenolol were known as drugs with high and low BBB penetration properties respectively. The mean brain concentrations of antipyrine and atenolol at steady-state were(2561 ± 125) and(20.1

  12. Transport of four pharmaceuticals in different horizons of three soil types

    Science.gov (United States)

    Kodesova, Radka; Svatkova, Paula; Klement, Ales; Jaksik, Ondrej; Golovko, Oksana; Fer, Miroslav; Kocarek, Martin; Nikodem, Antonin; Grabic, Roman

    2015-04-01

    Soil structure, which varies in different soil types and the horizons of these soil types, has a significant impact on water flow and contaminant transport in soils. Transport of many contaminants is in addition strongly influenced by their sorption on soil particles. Transport of four pharmaceuticals (sulfamethoxazole, trimethoprim, atenolol and carbamazepine) was studied in soil columns (a diameter of 10.5 cm and a height of 13 cm) taken from all diagnostic horizons of three different soil types (Haplic Luvisol, Greyic Phaeozem and Haplic Cambisol). The irrigation by water contaminated by a mixture of all four compounds followed by ponding infiltration of distilled water was simulated and water outflow and solute concentrations from the bottom of the soil sample was monitored in time. The highest infiltration rates were observed for soil samples from the Bt horizons of the Greyic Phaeozem that exhibited prismatic structure, followed by rates observed in the Ap horizons of the Haplic Luvisol, Greyic Phaeozem and Haplic Cambisol (due to their granular soil structure and presence of root channels). The lowest infiltration rate was measured for the Bw horizon of the Haplic Cambisol, which had a poorly developed soil structure and a low fraction of macropores. Compound discharge was however also highly affected by their sorption on solids. The highest mobility was observed for sulfamethoxazole followed by carbamazepine atenolol and trimethoprim, which corresponds to measured sorption isotherms. Mobility of ionizable compounds in different soil samples was influenced by pH (i.e. degree and form of their ionization) and sites available for absorption. Mobility of sulfamethoxazole decreased with decreasing pH (i.e. the largest sorption measured in horizons of the Haplic Cambisol). While mobility of atenolol and trimethoprim decreased with increasing base cation saturation, and with increasing organic matter content for carbamazepine. As result of both affects (i.e. soil

  13. EUM: antihipertensivos en la seguridad social y análisis comparativo entre centros de atención médica ambulatoria

    Directory of Open Access Journals (Sweden)

    Desirée Sáenz-Campos

    2001-03-01

    Full Text Available Justificación: La Hipertensión Arterial es una enfennedad crónica y asintómatica, ocupa la primera causa de consulta médica ambulatorio, contribuye directamente con la primera causa de mortalidad en el país, y casi siempre es fácil de tratar con una intervención integral que incluye la terapia farmacológica. Objetivo: Identificar los fármacos con mayor consumo institucional, valorar si el perfil resultante es compatible con los principios del uso racional de antihipertensivos y comparar la utilización de estos agentes entre clínicas similares de atención médica ambulatorio, durante un periodo anual. Métodos: Estudio observacional de tipo farmacoepidemiológico, se obtuvo el registro del consumo institucional de cada antihipertensivo y reporte local de consumo mensual de seis centros de atención médica ambulatorio,durante 1999. Se calculó dosis diaria definida (DDD y estimación de pacientes tratados y se hizo un análisis estadístico descriptivo. Resultados: Los fármacos más prescritos fueron atenolol (25%, enalapril (21% e hidroclorotiacida (19%; según DDD, el consumo global de atenolol fue 39%, enalapril 25% e hidroclorotiacida 23%, con lo que se benefició el 87% de los pacientes tratados. Con los antihipertensivos se dio tratamiento a unos 185,639 pacientes. Al nivel local, los perfiles de consumo tienden a simular la distribución institucional al predominar el uso de atenolol pero se alterna el diurético con enalapril; se registraron variaciones en el consumo mensual durante el periodo y en la cobertura de pacientes hipertensos de la zona. Conclusiones: Todos los fármacos antihipertensivos disponibles son utilizados aunque su consumo muestra un perfil heterogéneo. Los fármacos más prescritos al nivel local replican el perfil de consumo institucional, pero hay notables variaciones locales. Los hábitos de prescripción se ajustan al uso racional de los antibipertensivos en el ámbito ambulatorio. Las estimaciones

  14. Behavior of selected pharmaceuticals in topsoil of Greyic Phaeozem

    Science.gov (United States)

    Kodesova, Radka; Klement, Ales; Kocarek, Martin; Fer, Miroslav; Golovko, Oksana; Grabic, Roman; Jaksik, Ondrej

    2014-05-01

    It has been documented in several studies that soil may be contaminated by human or veterinary pharmaceuticals. Some of pharmaceutical ingredient may be retained in soils. The rest can be transported to the surface and groundwater through surface runoff and infiltration. Mobility of contaminants in soils is dependent on many soil and pharmaceutical properties (e.g. pharmaceutical adsorption on soil particles and pharmaceutical degradation). The goals of this study were: (1) to measure adsorption isotherms of selected pharmaceuticals in one soil; (2) to evaluate degradation of selected pharmaceuticals in this soil, and (3) to evaluate impact of applied pharmaceuticals on biological activity in soil, which influences pharmaceutical decomposition. Batch sorption tests were performed for 7 selected pharmaceuticals (beta blockers Atenolol and Metoprolol, anticonvulsant Carbamazepin, and antibiotics Clarithromycin, Clindamycin, Trimetoprim and Sulfamethoxazol) and one soil (topsoil of Greyic Phaeozem from Čáslav). The same concentrations (0.5, 1, 2.5, 5 and 10 mg/l) were used for almost all pharmaceuticals except Clarithromycin (0.033, 0.08, 0.165, 0.25, 0.33 mg/l). The Freundlich equations were used to describe adsorption isotherms. Degradation of all 7 pharmaceuticals was also studied. Solutes of different pharmaceuticals (concentration of 8.3 mg/l) were added into the plastic bottles (one pharmaceutical per bottle) with soil. Concentrations of pharmaceuticals remaining in soil 1, 2, 5, 12, 23, 40 and 61 days after the pharmaceutical application were analyzed. Colony forming unites were evaluated to describe microbial activity in time affected by different pharmaceuticals. Adsorption of studied pharmaceuticals on soil particles decreasing as follows: Clarithromycin, Trimetoprim, Metoprolol, Clindamycin, Atenolol, Carbamazepin, Sulfamethoxazol. Degradation rates in some degree reflected adsorption of studied pharmaceuticals on soil particles and increased with

  15. Effect of beta-adrenoceptor blockers on human ether-a-go-go-related gene (HERG) potassium channels

    DEFF Research Database (Denmark)

    Dupuis, Delphine S; Klaerke, Dan A; Olesen, Søren-Peter

    2005-01-01

    Patients with congenital long QT syndrome may develop arrhythmias under conditions of increased sympathetic tone. We have addressed whether some of the beta-adrenoceptor blockers commonly used to prevent the development of these arrhythmias could per se block the cardiac HERG (Human Ether....... These data showed that HERG blockade by beta-adrenoceptor blockers occurred only at high micromolar concentrations, which are significantly above the recently established safe margin of 100 (Redfern et al., 2003).......-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride) blocked the HERG channel with similar affinity, whereas the beta1-receptor antagonists metoprolol and atenolol showed weak effects. Further, the four compounds blocked HERG channels expressed in a mammalian HEK293 cell line...

  16. Fibrilación auricular en una paciente con megaorejuela auricular izquierda

    Directory of Open Access Journals (Sweden)

    Alejandro Villamil

    2007-01-01

    Full Text Available La FA constituye una de las arritmias sostenidas más frecuentes que motivan la consulta. El sustrato comprende diferentes mecanismos, entre los que se encuentra el agrandamiento auricular izquierdo. Presentamos el caso de una mujer de 33 años con antecedentes depalpitaciones, que ingresó en la guardia por FA de alta respuesta ventricular. En la radiografía de tórax se observó una deformación del borde izquierdo de la silueta cardíaca. Posteriormente,el ecocardiograma transesofágico y la resonancia magnética nuclear evidenciaron una megaorejuela aneurismática debida, probablemente, a un defecto pericárdico. La conducta fue anticoagulación oral y tratamiento con atenolol, con evolución favorable.

  17. Attenuation of contaminants of emerging concern during surface-spreading aquifer recharge.

    Science.gov (United States)

    Laws, Bonnie V; Dickenson, Eric R V; Johnson, Theodore A; Snyder, Shane A; Drewes, Jörg E

    2011-02-15

    The attenuation of a diverse suite of contaminants of emerging concern (CECs) and bulk water quality changes was evaluated at a surface-spreading aquifer recharge operation across a detailed subsurface profile (9 locations), representing both short- and long-travel times (10 h to 60 days). Seventeen CECs were detected in the recharge basin and the concentrations of all were reduced during soil aquifer treatment (SAT), with 11 of the target compounds attenuated by >80% after 60 days of travel time. Select CECs (atenolol, gemfibrozil, N,N-diethly-3-methylbenzamide, meprobamate, tris(2-chloroethyl)phosphate, and primidone) and bulk water organic-carbon measurements (total organic carbon, biodegradable organic carbon, size-exclusion chromatography and fluorescence excitation-emission matrices) were identified as monitoring parameters that can be used to assess SAT performance at surface-spreading operations. PMID:21211820

  18. Gender differences in left ventricular structure and function during antihypertensive treatment: the Losartan Intervention for Endpoint Reduction in Hypertension Study

    DEFF Research Database (Denmark)

    Gerdts, E.; Okin, P.M.; Simone, G. de;

    2008-01-01

    In hypertensive patients with left ventricular hypertrophy, antihypertensive treatment induces changes in left ventricular structure and function. However, less is known about gender differences in this response. Baseline and annual echocardiograms until the end of study or a primary end point...... occurred were assessed in 863 hypertensive patients with electrocardiographic left ventricular hypertrophy aged 55 to 80 years (mean: 66 years) during 4.8 years of randomized losartan- or atenolol-based treatment in the Losartan Intervention for Endpoint Reduction in Hypertension Echocardiography substudy...... (47% versus 32%; Ptreatment reduction in mean blood pressure. In logistic regression, left ventricular hypertrophy at study end was more common in women (odds ratio: 1.61; 95% CI: 1.16 to 2.26; P

  19. Study on clarithromycin lactobionate based dual selector systems for the enantioseparation of basic drugs in capillary electrophoresis.

    Science.gov (United States)

    Yu, Tao; Du, Yingxiang; Chen, Jiaquan; Xu, Guangfu; Yang, Ke; Zhang, Qi; Zhang, Jinjing; Du, Shuaijing; Feng, Zijie; Zhang, Yanjie

    2015-08-01

    In this paper, the use of clarithromycin lactobionate, a kind of antibiotic chiral selector, in combination with four neutral cyclodextrin derivatives (glucose-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, methyl-β-cyclodextrin and hydroxypropyl-β-cyclodextrin) was reported for the first time. As a result, these dual systems gave much better resolution of nefopam (the Rs increased to 3.58, 2.72, 1.49 and 1.42, respectively) compared to the single systems. The effects of buffer pH and selector concentration on the separation of nefopam were also investigated. Additionally, some other basic drugs including metoprolol, atenolol, propranolol, bisoprolol, esmolol and ritodrine were tested for the investigation and evaluation of the enantiorecognition capability of the four dual systems. As expected, the synergistic effect was observed in four systems. Different results of these dual systems were also summarized. PMID:26097042

  20. Immediate haemodynamic effects of a novel partial agonist, beta 1-adrenoceptor blocking drug ICI 141,292 after intravenous administration to healthy young volunteers and patients with ischaemic heart disease

    DEFF Research Database (Denmark)

    Bonde, J; Svendsen, T L; Lyngborg, K;

    1987-01-01

    administration of four sequential doses (0.5, 0.5, 1.0 and 2.0 mg) of ICI 141,292 was examined. HR decreased 7% (P less than 0.05) following ICI 141,292 1 mg with no further decrease following the succeeding doses. Cardiac output decreased 5.2% (P less than 0.05) following a cumulative dose of 4 mg...... were administered intravenously. The attenuation in exercise induced tachycardia varied between 16.0 and 21.2% (P less than 0.01). A significant reduction in blood pressure could be demonstrated following all three doses of ICI 141,292 and atenolol during exercise. At rest in the sitting position HR...

  1. Polar organic micropollutants in the coastal environment of different marine systems.

    Science.gov (United States)

    Nödler, Karsten; Voutsa, Dimitra; Licha, Tobias

    2014-08-15

    Polar anthropogenic organic micropollutants are frequently detected in freshwater and discharged on large scale into marine systems. In this work the results of 153 samples collected from the shorelines of the Baltic Sea (Germany), Northern Adriatic Sea (Italy), Aegean Sea and Dardanelles (Greece & Turkey), San Francisco Bay (USA), Pacific Ocean (USA), Mediterranean Sea (Israel), and Balearic Sea (Spain) are presented. The samples were analyzed for various classes of micropollutants such as pharmaceuticals, corrosion inhibitors, biocides, and stimulants. Caffeine, paraxanthine, theobromine, tolyltriazole, 1H-benzotriazole, and atrazine were detected in>50% of all samples. The detection frequencies of carbamazepine, iopamidol, diuron, sulfamethoxazole, paracetamol, theophylline, and atenolol were between 20% and 32%. As caffeine is linked to untreated wastewater, the widespread occurrence of raw sewage in marine environments and thus potentially elevated nutrient concentrations and risk for the presence of wastewater-related pathogens is remarkable. PMID:25015017

  2. HEART FAILURE, DIABETES, BETA-BLOCKERS AND RISK OF HYPOGLYCEMIA

    Directory of Open Access Journals (Sweden)

    A. A. Aleksandrov

    2008-01-01

    Full Text Available Aim. To evaluate an influence of carvedilol on risk of hypoglycemia in patients with diabetes type 2 (D2 and chronic heart failure (CHF treated with angiotensin converting enzyme (ACE inhibitors.Material and methods. 13 patients (10 men, 3 women; aged 59,8±6,7 y.o. with D2 and CHF caused by ischemic heart disease were included in the study. Before inclusion all patients were treated with ACE inhibitors and various beta-blockers (atenolol, metoprolol, bisoprolol. These beta-blockers were changed for carvedilol. Heart ultrasonography, blood pressure control, glycemia monitoring, HbA1c level determination were performed before, during and after carvedilol therapy.Results. Carvedilol reduces frequency and duration of hypoglycaemia episodes. There were not episodes of severe hypoglycaemia during carvedilol therapy.Conclusion. Carvedilol reduces risk of hypoglycemia when it is used in combination with ACE inhiditors in diabetic patients with CHF.

  3. Drug points Severe myalgia from an interaction between treatments with pantoprazole and methotrexate%用药点滴由潘托拉唑和氨甲蝶呤药物相互作用导致的严重肌痛

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    @@ 一位59岁的男子因皮肤型滤泡趋向性T细胞淋巴瘤接受2a-干扰素治疗.由于肿瘤复发致治疗中断后,患者开始使用小剂量的氨甲蝶呤(15 mg 肌注,每周1次).同时,因其患有Barrett食管和高血压,分别服用潘托拉唑(pantoprazole)(每日20 mg,口服)和阿替洛尔(atenolol).在首次注射氨甲蝶呤后,患者出现严重广泛的肌痛和骨痛.

  4. Dorsomedial hypothalamic GABA regulates anxiety in the social interaction test.

    Science.gov (United States)

    Shekhar, A; Katner, J S

    1995-02-01

    Blockade of GABAA function in the region of the dorsomedial hypothalamus (DMH) of rats is known to elicit a constellation of physiologic responses including increases in heart rate (HR), mean arterial blood pressure (BP), respiratory rate, and plasma catecholamine levels, as well as behavioral responses such as increases in locomotor activity and anxiogenic-like effects as measured in a conflict test and the elevated plus-maze test. The aim of the present study was to test the effects of microinjecting GABAA antagonists bicuculline methiodide (BMI) and picrotoxin, as well as the GABAA agonist muscimol, into the DMH of rats placed in the social interaction (SI) test. Muscimol decreased HR and BP but increased SI, whereas the GABA antagonists increased HR and BP but decreased SI time. Blocking the HR changes elicited by GABAergic drugs injected into the DMH with systemic injections of atenolol and atropine methylbromide did not block their effects on SI.

  5. Investigation of thin ZnO layers in view of laser desorption-ionization

    Science.gov (United States)

    Grechnikov, A. A.; Georgieva, V. B.; Alimpiev, S. S.; Borodkov, A. S.; Nikiforov, S. M.; Simanovsky, Ya O.; Dimova-Malinovska, D.; Angelov, O. I.

    2010-04-01

    Thin zinc oxide films (ZnO) were developed as a matrix-free platform for surface assisted laser desorption-ionization (SALDI) time-of-flight mass spectrometry. The ZnO films were deposited by RF magnetron sputtering of ZnO ceramic targets in Ar atmospheres on monocrystalline silicon. The generation under UV (355 nm) laser irradiation of positive ions of atenolol, reserpine and gramicidin S from the ZnO layers deposited was studied. All analytes tested were detected as protonated molecules with no or very structure-specific fragmentation. The mass spectra obtained showed low levels of chemical background noise. All ZnO films studied exhibited high stability and good reproducibility. The detection limits for test analytes are in the 10 femtomol range.

  6. Change in pulse pressure/stroke index in response to sustained blood pressure reduction and its impact on left ventricular mass and geometry changes: the life study

    DEFF Research Database (Denmark)

    Palmieri, V.; Bella, J.N.; Gerdts, E.;

    2008-01-01

    BACKGROUND: In cross-sectional data in hypertensive subjects, brachial pulse pressure (PP)/Doppler stroke index (SVi), (PP/SVi) correlates weakly but significantly with left ventricular (LV) mass and relative wall thickness (RWT). METHODS: In the Losartan Intervention For End-point reduction...... in hypertension (LIFE) study, we evaluated the impact of antihypertensive treatment on change of PP/SVi as raw indicator of systemic arterial stiffness, and further explored the impact of the change in PP/SVi on the change in LV mass and RWT. RESULTS: Compared to baseline, mean PP/SVi reduction was -13% at year 1...... and not statistically significant at year 2 follow-up. Losartan- or atenolol-based treatments were associated with comparable reduction of PP/SVi. At year 2 follow-up, reduced PP/SVi was associated with greater reductions in mean blood pressure (BP) and heart rate and greater increase in SVi, but not with lower LV mass...

  7. The Anglo-Scandinavian Cardiac Outcomes Trial: blood pressure-lowering limb: effects in patients with type II diabetes

    DEFF Research Database (Denmark)

    Ostergren, Jan; Poulter, Neil R; Sever, Peter S;

    2008-01-01

    OBJECTIVE: To compare the effects of two antihypertensive treatment strategies for the prevention of coronary heart disease and other cardiovascular events in the large subpopulation (n=5137) with diabetes mellitus in the blood pressure-lowering arm of the Anglo-Scandinavian Cardiac Outcomes Trial...... by 48% (P=0.004) and noncoronary revascularization procedures by 57% (Pdeaths and nonfatal myocardial infarctions (the primary endpoint), which were reduced...... nonsignificantly by 8% (hazard ratio 0.92, confidence interval 0.74-1.15). CONCLUSION: In the large diabetic subgroup in the blood pressure-lowering arm of the Anglo-Scandinavian Cardiac Outcomes Trial, the benefits of amlodipine-based treatment, compared with atenolol-based treatment, on the incidence of total...

  8. Sorption and degradation of selected pharmaceuticals in representative soils of the Czech Republic

    Science.gov (United States)

    Kodesova, Radka; Kocarek, Martin; Klement, Ales; Golovko, Oksana; Grabic, Roman; Fer, Miroslav; Nikodem, Antonin; Jaksik, Ondrej

    2015-04-01

    Knowledge of contaminant behavior (e.g. its sorption onto soil particle, degradation etc.) is essential when assessing contaminant migration in soil and groundwater environment. This study was focused on evaluating sorption isotherms and half-lives for 7 pharmaceuticals (clarithromycin, trimethoprim, metoprolol, atenolol, clindamycin, carbamazepine, sulfamethoxazole) on 13 soils of different soil properties. Sorption of ionizable compounds was highly affected by soil pH. The sorption coefficient of sulfamethoxazole was negatively correlated to soil pH and thus positively related to hydrolytic acidity and exchangeable acidity. Sorption coefficients for clindamycin and clarithromycin were positively related to soil pH and thus negatively related to hydrolytic acidity and exchangeable acidity and positively related to base cation saturation. Sorption coefficients for the remaining pharmaceuticals (trimethoprim, metoprolol, atenolol, and carbamazepine) were also positively correlated with the base cation saturation and cation exchange capacity. Degradation rates in some degree reflected sorption of studied pharmaceuticals on soil particles and increased with decreasing sorption. The highest mobility in studied soils was observed for sulfamethoxazole, but this pharmaceutical was relatively quickly degraded. The second highest mobility was found for carbamazepine, which mostly did not noticeably degrade during our experiments. Thus this pharmaceutical has the highest potential to migrate in water environment. The lowest mobility was observed for clarithromycin. However, this pharmaceutical due to its stability may be retained in an environment for a long time. Acknowledgement: The authors acknowledge the financial support of the Czech Science Foundation (Project No. 13-12477S, Transport of pharmaceuticals in soils). References: Kodesova, R., Grabic, R., Kocarek, M., Klement, A., Golovko, O., Fer, M., Nikodem, A., Jaksik, O., Pharmaceuticals' sorptions relative to

  9. Effects of β2-Adrenergic Antagonist on Cytosolic Ca2+ in Ventricular Myocytes from Infarcted Rat Heart

    Institute of Scientific and Technical Information of China (English)

    Yang Hui; Wu Wei; Zeng Chong; Deng Chunyu; Fang Chang; Chen Shanming

    2006-01-01

    Objectives To investigate the effects of β2-adrenergic antagonist on cytosolic Ca2 +([Ca2+]i) in ventricular myocytes from infarcted rat heart. Methods A ligature was placed around left anterior descending coronary artery of rat hearts. Rats in the control group were sham-operated.Cardiomyocytes were dissociated at two, four, eight weeks after myocardial infarction (MI) and [Ca2+]i was measured via fura-2 fluorescence. The response of cardiomyocytes to isoproterenol in presence or absenceof beta1-adrenergic antagonist atenolol, beta2-adrenergic antagonist ICI118, 551 or non-selective β1,2- adrenergic antagonists propranolol was examined.Results The followings were found that ICI11 8, 551 had no significant effects on the rise of [Ca2+]i induced by isoproterenol in normal ventricular myocytes (P >0.05), ICI118, 551 only significantly attenuated the rise of [Ca2+]i induced by isoproterenol at four weeks and eight weeks after MI (24.5% ±5.7% vs 57.8% ±13.2%, P< 0.01; 12.2%±7.9% vs 44.6%±11.3%, P<0.01). Atenolol had suppressive effects only in the control group and the post-MI group of two weeks (P<0.05), and propranolol had suppressive effects in the control and all the three post-MI groups (P<0.01).Conclusions Beta2-adrenergic antagonist ICI118,551 may exert negative effects on Ca2+ overload initiated by sympathetic stimulation after MI.

  10. Development of SPME-LC-MS method for screening of eight beta-blockers and bronchodilators in plasma and urine samples.

    Science.gov (United States)

    Goryński, Krzysztof; Kiedrowicz, Alicja; Bojko, Barbara

    2016-08-01

    The current work describes the development and validation of a simple, efficient, and fast method using solid phase microextraction coupled to liquid chromatography-tandem mass spectrometry (SPME-LC-MS/MS) for the concomitant measurement of eight beta-blockers and bronchodilators in plasma and urine. The presented assay enables quantitative determination of acebutolol, atenolol, fenoterol, nadolol, pindolol, procaterol, sotalol, and timolol. In this work, samples were prepared on a high-throughput platform using the 96-well plate format of the thin film solid phase microextraction (TFME) system, and a biocompatible extraction phase made of hydrophilic-lipophilic balance particles. Analytes were separated on a pentafluorophenyl column (100mm×2.1mm, 3μm) by gradient elution using an UPLC Nexera coupled with an LCMS-8060 mass spectrometer. The mobile phase consisted of water-acetonitrile (0.1% formic acid) at a flow rate of 0.4mLmin(-1). The linearity of the method was checked within therapeutic blood-plasma concentrations, and shown to adequately reflect typically expected concentrations of future study samples. Post-extraction addition experiments showed that the matrix effect ranged in plasma from 98% for procaterol to 115% for nadolol, and in urine, from 85% for nadolol and pindolol to 119% for atenolol. The method was successfully validated using Food and Drug Administration (FDA) guidelines, and met all acceptance criteria for bioanalytical assays at five concentration levels for all selected drugs. The final protocol can be successfully applied for monitoring concentrations of the selected drugs in both plasma and urine matrices obtained from patients or athletes. PMID:26971030

  11. Uptake and effects of a mixture of widely used therapeutic drugs in Eruca sativa L. and Zea mays L. plants.

    Science.gov (United States)

    Marsoni, Milena; De Mattia, Fabrizio; Labra, Massimo; Bruno, Antonia; Bruno, Antonella; Bracale, Marcella; Vannini, Candida

    2014-10-01

    Pharmaceutically active compounds (PACs) are continuously dispersed into the environment due to human and veterinary use, giving rise to their potential accumulation in edible plants. In this study, Eruca sativa L. and Zea mays L. were selected to determine the potential uptake and accumulation of eight different PACs (Salbutamol, Atenolol, Lincomycin, Cyclophosphamide, Carbamazepine, Bezafibrate, Ofloxacin and Ranitidine) designed for human use. To mimic environmental conditions, the plants were grown in pots and irrigated with water spiked with a mixture of PACs at concentrations found in Italian wastewaters and rivers. Moreover, 10× and 100× concentrations of these pharmaceuticals were also tested. The presence of the pharmaceuticals was tested in the edible parts of the plants, namely leaves for E. sativa and grains for Z. mays. Quantification was performed by liquid chromatography mass spectroscopy (LC/MS/MS). In the grains of 100× treated Z. mays, only atenolol, lincomycin and carbamazepine were above the limit of detection (LOD). At the same concentration in E. sativa plants the uptake of all PACs was >LOD. Lincomycin and oflaxacin were above the limit of quantitation in all conditions tested in E. sativa. The results suggest that uptake of some pharmaceuticals from the soil may indeed be a potential transport route to plants and that these environmental pollutants can reach different edible parts of the selected crops. Measurements of the concentrations of these pharmaceuticals in plant materials were used to model potential adult human exposure to these compounds. The results indicate that under the current experimental conditions, crops exposed to the selected pharmaceutical mixture would not have any negative effects on human health. Moreover, no significant differences in the growth of E. sativa or Z. mays plants irrigated with PAC-spiked vs. non-spiked water were observed. PMID:25042244

  12. MÉTODO DE ESCOLHA DE MEDICAMENTOS ANTI-HIPERTENSIVOS POR GESTORES DA ÁREA DE SAÚDE

    Directory of Open Access Journals (Sweden)

    Rondinelli de Carvalho LADEIRA

    2016-06-01

    Full Text Available Um problema enfrentado pelos gestores de saúde é a aquisição de medicamentos que, para o abastecimento do SUS, deve-se levar em consideração a efetividade, os custos e a segurança dos mesmos. A análise farmacoeconômica pode ser vista como a descrição e a análise dos custos da terapia farmacêutica para os sistemas de assistência à saúde e para a sociedade. O presente trabalho faz a análise de custo-efetividade de cinco betabloqueadores adrenérgicos usados no tratamento de hipertensão arterial (atenolol, carvedilol, metoprolol, propranolol e sotalol através de auxílio multicritério à decisão. Tendo em vista gestores de saúde como agentes da decisão, foram testados os métodos de Borda para definição dos pesos dos critérios por especialistas e AHP para escolha do medicamento através do software IPE 1.0. Questionários foram aplicados a sete profissionais médicos especialistas em cardiologia para a comparação dos critérios (efetividade, custo, experiência com o fármaco e segurança, sub-critérios (agravamento da insuficiência cardíaca congestiva, agravamento da doença arterial periférica, broncoespasmo, bradicardia e alterações metabólicas, relativos ao critério segurança e alternativas à luz dos critérios estudados. O betabloqueador que se apresentou como melhor escolha foi o atenolol (32,38%.

  13. Evaluation of clinical bradycardiac effect and respiratory adverse effect of β-blocking agents in coronary computed tomography angiography based on theoretical analysis.

    Science.gov (United States)

    Fujito, Kaori; Takayanagi, Risa; Kimura, Koji; Yokoyama, Haruko; Yamada, Yasuhiko

    2016-04-01

    β-blocking agents are used for patients with tachycardia to improve the image quality of coronary computed tomography angiography (CCTA). In this study, we analyzed the clinical bradycardiac effects and the adverse respiratory effects of five β-blocking agents (landiolol, esmolol, propranolol, metoprolol and atenolol) used for CCTA. The changes of the occupancy binding to β1 or β2 receptor of these drugs were calculated based on the receptor occupancy theory. Thereafter, we predicted both the rate of heart rate decline (▲HR) as a clinical effect and the rate of decrease in forced expiratory volume in 1 s (▲FEV1) as an adverse effect, by using the ternary complex model. The results showed that the drugs with ▲HR greater than 10 %, necessary for CCTA, were as follows: landiolol at 13.5 %, propranolol at 11.0 %, and atenolol at 22.6 %. The ▲HR values at the end of CCTA for those three drugs were 0.3, 6.7, and 22.9 %, respectively. It is desirable for the bradycardiac effect to disappear at the end of CCTA. Therefore, landiolol is thought to be a preferable drug. On the other hand, ▲FEV1 at start and end of CCTA for those three drugs was 0.04-2.5, 34.9-40.3, and 6.0-6.1 %, respectively. Our results suggested that landiolol has the most appropriate effect and safety for patients with tachycardia who are undergoing a CCTA procedure. PMID:25510848

  14. Pharmaceuticals and organic pollution mitigation in reclamation osmosis brines by UV/H2O2 and ozone.

    Science.gov (United States)

    Justo, A; González, O; Aceña, J; Pérez, S; Barceló, D; Sans, C; Esplugas, S

    2013-12-15

    One significant disadvantage of using reverse osmosis (RO) for reclamation purposes is the need to dispose of the RO retentates. These retentates contain a high concentration of micropollutants, effluent organic matter (EfOM) and other inorganic constituents, which are recalcitrant to biological treatment and may impact the environment. The occurrence of 11 pharmaceuticals (concentrations ranging from 0.2 to 1.6 μg L(-1)) and their mitigation in RO retentates by a UV/H2O2 process and ozonation was studied using a wide range of oxidant dosages. Eleven pharmaceuticals were identified at. Initial observed kinetic constants (kobs) were calculated for the different pharmaceuticals. Other typical wastewater parameters were also monitored during the UV/H2O2 and ozonation reactions. The range for kobs was found to be 0.8-12.8L mmol O3(-1) and 9.7-29.9 L mmol H2O2(-1) for the ozonation and UV/H2O2 process, respectively. For ozonation, Atenolol, Carbamazepine, Codeine, Trimethoprim and Diclofenac showed the lowest initial kobs (in the order mentioned). Atenolol and Carbamazepine appeared as the most ozone resistant pharmaceuticals, exhibiting the lowest percentage of elimination at low ozone doses. On the other hand, despite the non-selectivity of HO, differences in the initial kobs were also observed during the UV/H2O2 process. Trimethoprim, Paroxetine and Sulfamethoxazole exhibited the lowest initial kobs values (in the order mentioned). Trimethoprim and Paroxetine also exhibited the lowest percentage removal when low H2O2 doses were assayed. The compounds that were identified as problematic during ozonation were more efficiently removed by the UV/H2O2 process. UV/H2O2 generally appeared to be a more efficient technology for removing pharmaceuticals from RO brines compared to ozonation. PMID:23768786

  15. Uptake and effects of a mixture of widely used therapeutic drugs in Eruca sativa L. and Zea mays L. plants.

    Science.gov (United States)

    Marsoni, Milena; De Mattia, Fabrizio; Labra, Massimo; Bruno, Antonia; Bruno, Antonella; Bracale, Marcella; Vannini, Candida

    2014-10-01

    Pharmaceutically active compounds (PACs) are continuously dispersed into the environment due to human and veterinary use, giving rise to their potential accumulation in edible plants. In this study, Eruca sativa L. and Zea mays L. were selected to determine the potential uptake and accumulation of eight different PACs (Salbutamol, Atenolol, Lincomycin, Cyclophosphamide, Carbamazepine, Bezafibrate, Ofloxacin and Ranitidine) designed for human use. To mimic environmental conditions, the plants were grown in pots and irrigated with water spiked with a mixture of PACs at concentrations found in Italian wastewaters and rivers. Moreover, 10× and 100× concentrations of these pharmaceuticals were also tested. The presence of the pharmaceuticals was tested in the edible parts of the plants, namely leaves for E. sativa and grains for Z. mays. Quantification was performed by liquid chromatography mass spectroscopy (LC/MS/MS). In the grains of 100× treated Z. mays, only atenolol, lincomycin and carbamazepine were above the limit of detection (LOD). At the same concentration in E. sativa plants the uptake of all PACs was >LOD. Lincomycin and oflaxacin were above the limit of quantitation in all conditions tested in E. sativa. The results suggest that uptake of some pharmaceuticals from the soil may indeed be a potential transport route to plants and that these environmental pollutants can reach different edible parts of the selected crops. Measurements of the concentrations of these pharmaceuticals in plant materials were used to model potential adult human exposure to these compounds. The results indicate that under the current experimental conditions, crops exposed to the selected pharmaceutical mixture would not have any negative effects on human health. Moreover, no significant differences in the growth of E. sativa or Z. mays plants irrigated with PAC-spiked vs. non-spiked water were observed.

  16. The Effect of Sympathetic Antagonists on the Antidepressant Action of Alprazolam

    Directory of Open Access Journals (Sweden)

    Gorash ZM

    2008-01-01

    Full Text Available Alprazolam is an anti-anxiety drug shown to be effective in the treatment of depression. In this study, the effect of sympathetic receptor antagonists on alprazolam–induced antidepressant action was studied using a mouse model of forced swimming behavioral despair. The interaction of three sympathetic receptor antagonists with benzodiazepines, which may impact the clinical use of alprazolam, was also studied. Behavioral despair was examined in six groups of albino mice. Drugs were administered intraperitoneally. The control group received only a single dose of 1% Tween 80. The second group received a single dose of alprazolam, and the third group received an antagonist followed by alprazolam. The fourth group was treated with imipramine, and the fifth group received an antagonist followed by imipramine. The sixth group was treated with a single dose of an antagonist alone (atenolol, a β1-selective adrenoceptor antagonist; propranolol, a non selective β-adrenoceptor antagonist; and prazocin, an α1-adrenoceptor antagonist. Results confirmed the antidepressant action of alprazolam and imipramine. Prazocin treatment alone produced depression, but it significantly potentiated the antidepressant actions of imipramine and alprazolam. Atenolol alone produced an antidepressant effect and potentiated the antidepressant action of alprazolam. Propranolol treatment alone produced depression, and antagonized the effects of alprazolam and imipramine, even producing depression in combined treatments. In conclusion, our results reveal that alprazolam may produce antidepressant effects through the release of noradrenaline, which stimulates β2 receptors to produce an antidepressant action. Imipramine may act by activating β2 receptors by blocking or down-regulating β1 receptors.

  17. Analysis of some pharmaceuticals in municipal wastewater of Almadinah Almunawarah

    KAUST Repository

    Shraim, Amjad

    2012-11-29

    The chemical pollution of water resources is a major challenge facing the humanity in this century. Pharmaceuticals and personal care products (PPCPs) are a group of emerging environmental chemical pollutants distinguished by their bioactivity and high solubility. They may also cause health complications to humans and living organisms. Pharmaceuticals enter the environment, mainly via wastewater and can eventually reach the surface and ground water. Despite this, PPCPs received less attention as environmental pollutants than other chemical pollutants (e.g. heavy metals and pesticides). The purpose of this work was to investigate the presence of some of the most frequently dispensed drugs for the residents of Almadinah Almunawarah, Saudi Arabia in the municipal wastewater before and after treatment. For this purpose, wastewater samples were collected biweekly from the city’s sewage treatment plant for a period of 4 months and analyzed the targeted drugs using tandem LC–MS. Out of the 19 investigated drugs, 5 pharmaceuticals have been found in concentrations greater than the limit of detection in both the influents and effluents of the sewage treatment plant. As expected, the concentrations of investigated pharmaceuticals in the wastewater were found to be low. These drugs and their average concentrations (in ng mL−1) in the influents were: acetaminophen (38.9), metformin (15.2), norfluoxetine (7.07), atenolol (2.04), and cephalexin (1.88). Meanwhile, the effluents contained slightly lower levels (in ng mL−1) than those of influents: acetaminophen (31.2), metformin (3.19), norfluoxetine (7.25), atenolol (0.545), and cephalexin (1.53). The results of this study supported by many other investigations indicate the inefficiency of current conventional wastewater treatment protocols in eliminating such a group of active and potentially hazardous pollutants from the wastewater.

  18. EUM: antihipertensivos en la seguridad social y análisis comparativo entre centros de atención médica ambulatoria

    Directory of Open Access Journals (Sweden)

    Desirée Sáenz-Campos

    2001-03-01

    Full Text Available Justificación: La Hipertensión Arterial es una enfennedad crónica y asintómatica, ocupa la primera causa de consulta médica ambulatorio, contribuye directamente con la primera causa de mortalidad en el país, y casi siempre es fácil de tratar con una intervención integral que incluye la terapia farmacológica. Objetivo: Identificar los fármacos con mayor consumo institucional, valorar si el perfil resultante es compatible con los principios del uso racional de antihipertensivos y comparar la utilización de estos agentes entre clínicas similares de atención médica ambulatorio, durante un periodo anual. Métodos: Estudio observacional de tipo farmacoepidemiológico, se obtuvo el registro del consumo institucional de cada antihipertensivo y reporte local de consumo mensual de seis centros de atención médica ambulatorio,durante 1999. Se calculó dosis diaria definida (DDD y estimación de pacientes tratados y se hizo un análisis estadístico descriptivo. Resultados: Los fármacos más prescritos fueron atenolol (25%, enalapril (21% e hidroclorotiacida (19%; según DDD, el consumo global de atenolol fue 39%, enalapril 25% e hidroclorotiacida 23%, con lo que se benefició el 87% de los pacientes tratados. Con los antihipertensivos se dio tratamiento a unos 185,639 pacientes. Al nivel local, los perfiles de consumo tienden a simular la distribución institucional al predominar el uso de atenolol pero se alterna el diurético con enalapril; se registraron variaciones en el consumo mensual durante el periodo y en la cobertura de pacientes hipertensos de la zona. Conclusiones: Todos los fármacos antihipertensivos disponibles son utilizados aunque su consumo muestra un perfil heterogéneo. Los fármacos más prescritos al nivel local replican el perfil de consumo institucional, pero hay notables variaciones locales. Los hábitos de prescripción se ajustan al uso racional de los antibipertensivos en el ámbito ambulatorio. Las estimaciones

  19. THE EFFECT OF NEBIVOLOL ON BONE MINERAL DENSITY IN POSTMENOPAUSAL WOMEN WITH MILD HYPERTENSION

    Directory of Open Access Journals (Sweden)

    I. L. Tepoyan

    2015-09-01

    Full Text Available Aim. To study the effects of nebivolol on bone mineral density (BMD in postmenopausal women with mild hypertension (HT and osteopenia.Material and methods. Postmenopausal women (n=56 aged 50-65 years with mild HT фтв osteopenia were included into the randomized controlled study and divided in two groups (28 patients in each. During 12 months patients of the main group received treatment with nebivolol (5-7.5 mg/day and patients of the control group received treatment with atenolol (12.5-25 mg/day. Clinical and anthropometric examinations, blood pressure measurements, ECG registrations were performed in all patients initially and after 12 months of treatment. Quantitative estimation of BMD was performed by dual energy X-ray absorptiometry with osteodensitometry DELPHI W manufactured by HOLOGIC company (USA in the lumbar spine (L1-L4, femoral neck and proximal femur in the anterior-posterior projection. In addition, calcium and bone metabolism indices were determined: ionized calcium, total alkaline phosphatase, C-telopeptide of type I collagen (CTX.Results. Therapy of mild HT with nebivolol during 12 months showed increase in BMD in the spine according to the T-test from -1.7±0.4 SD to -1.4±0.53 SD (p<0.001, while in atenolol group this index decreased from -1.5±0.7 SD to -1.6±0.64 SD (p<0.001. When evaluating T-test of the femoral neck the index changed in the main group from - 1.4±0.44 SD to -1.27±0.5 SD (p=0.015, in the control group - from -1.3±0.64 SD to -1.5±0.65 SD (p=0.0005. In the study group T-test of proximal femur changed from -0.58±0.4 SD to -0.49±0.4 SD (p=0.003, and in the control group - from -0.8±0.84 SD to -0.83±0.93 SD (p=0.3. The dynamics of the BMD due to 12 month therapy in all investigated bone segments distinguished significantly between study and control groups. Nebivolol therapy group showed reduction in CTX level from 0.367±0.16 to 0.294±0.12 ng/ml (p<0.001, whereas the control group showed increase in

  20. Combinação de anlodipino e enalaprila em pacientes hipertensos com doença coronariana Combinación de amlodipino y enalapril en pacientes hipertensos con enfermedad coronaria Combination of amlodipine and enalapril in hypertensive patients with coronary disease

    Directory of Open Access Journals (Sweden)

    Marcos Rienzo

    2009-03-01

    Full Text Available FUNDAMENTO: Pacientes (pts com doença coronariana (DAC estável podem se beneficiar de menor pressão arterial (PA, conforme estudos recentes. OBJETIVO: Avaliar a eficácia e a tolerabilidade da combinação fixa anlodipino + enalaprila, comparada a anlodipino na normalização da PA diastólica (PAD ( 90 e 110 mmHg durante o wash-out de quatro semanas, em uso só de atenolol. Após wash-out randomizamos para combinação (A ou anlodipino (B e seguimos de quatro em quatro semanas até 98 dias. As doses (mg iniciais foram, respectivamente: A- 2,5/10 e B- 2,5, sendo incrementadas se PAD> 85mmHg, nas visitas. Estatística com χ2, Fischer e análise de variância, para pFUNDAMENTO: Pacientes (pts con enfermedad coronaria (EAC estable pueden beneficiarse con una menor presión arterial (PA, de acuerdo con estudios recientes. OBJETIVO: Evaluar la eficacia y la tolerancia de la combinación fija amlodipino + enalapril, comparada a el amlodipino en la normalización de la PA diastólica (PAD (90 y 110 mmHg durante el wash-out de cuatro semanas, en uso sólo de atenolol. Después del wash-out randomizamos para combinación (A o amlopidino (B y seguimos de cuatro en cuatro semanas hasta 98 días. Las dosis (mg iniciales fueron, respectivamente: A- 2,5/10 y B- 2,5, siendo incrementadas si PAD> 85mmHg, en las visitas. Estadística con χ2, Fischer y análisis de varianza, para pBACKGROUND: Patients (pts with stable coronary artery disease (CAD can benefit from a decrease in the blood pressure (BP, according to recent studies. OBJECTIVE: To evaluate the efficacy and tolerability of the fixed combination: amlodipine + enalapril, when compared to amlodipine in the normalization of the diastolic arterial pressure (DAP (90 and 110 mmHg during the four-week wash-out with atenolol treatment alone, were excluded. After the wash-out, pts were randomly distributed for the use of the combination (A or amlodipine (B and were followed every four weeks up to 98 days

  1. Evaluation of tablets splitting in NAH treatment for hypertensive patients in primary clinic unit%基层高血压NAH治疗方案片剂分剂量评价

    Institute of Scientific and Technical Information of China (English)

    刘元江; 缪经纬; 詹金陶; 刘其东

    2012-01-01

    AIM To evaluate accuracy and rationality of tablets splitting in nifedipine, atenolol, hydro-chlorothiazide and captopril ( NAH) treatment for hypertensive patients in primary clinical unit. METHODS Tablet cutter was utilized to split these pills into quarter or one eighth, and then European Pharmacopoeia (EP) and other standards was adopted to evaluate the accuracy of tablets spittin, expected weight (EW) and real wegtht (RW), mean weight loss percentage, and friability. RESULTS When these tablets split into quarter, they could not meet the accuracy subdivision of EP standards. There was significant difference when compared EW1/4 with RW1/4, such as nifedipine tablets produced by Xiangxue Pharmaceutical Company, atenolol tablets produced by Zhongyang Pharmaceutical Company or Wanraa Pharmaceutical Company, and hydrochlorothiazide tablets produced by Yunpeng Pharmaceutical Company. All tablets met the mean weight loss percentage ≤3%, however part of tablets could not meet the requirement of friability. When these tablets split into one eighth, they could not meet the accuracy subdivision of EP standards. There was significant difference when compared EW1/8 with RW^, such as nifedipine tablets produced by Xiangxue Pharmaceutical Company and atenolol tablets produced by Wanma Pharmaceutical Company. Meanwhile, mean weight loss percentage and friability could not meet the related regulation. CONCLUSION In the NAH treatment for hypertensive patients in primary clinical unit, the accuracy of tablets spitting and other indicators can not meet the requirements. It should be solved urgently to improve rational drug use.%目的 评价基层高血压硝苯地平、阿替洛尔、氢氯噻嗪和卡托普利(NAH)治疗方案片剂分剂量的准确性、合理性.方法 采用药片切割器对4种片剂四等分和(或)八等分,参照《欧洲药典》及相关参考文献评价分剂量准确性、期望重量(EW)与实际重量(RW)的比较、平均损失百分

  2. The influence of radiation sterilisation on some {beta}-blockers in the solid state

    Energy Technology Data Exchange (ETDEWEB)

    Marciniec, B. [Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, 6 Gruwaldzka Str., 60-780 Poznan (Poland); Ogrodowczyk, M., E-mail: mogrodo@ump.edu.pl [Department of Pharmaceutical Chemistry, Poznan University of Medical Sciences, 6 Gruwaldzka Str., 60-780 Poznan (Poland); Czajka, B.; Hofman, M. [Department of Cooridinational Chemistry, A. Mickiewicz University, Grunwaldzka 6, 60-780 Poznan (Poland)

    2011-02-20

    Research highlights: {yields} Six {beta}-blockers (acebutolol, alprenolol, atenolol, metoprolol, pindolol, propranolol) in solid phase were exposed to the ionising radiation by e-beam in doses from 25 to 400 kGy. {yields} To establish the effects of irradiation on their physico-chemical properties, the compounds were then analysed by DSC, SEM, XRD and FT-IR. {yields} For alprenolol, propranolol and metoprolol linear relations were found between the irradiation dose and the decrease in the melting point (r = 0.9446-0.9864). {yields} No changes were observed in the FT-IR spectra and in the SEM images of the compounds studied. - Abstract: Six derivatives of aryloxyalkylaminopropanol of known {beta}-adrenolytic activity (acebutolol, alprenolol, atenolol, metoprolol, pindolol, propranolol) in solid phase were exposed to the ionising radiation generated by e-beam of high-energy electrons from an accelerator ({approx}10 MeV) in doses from 25 to 400 kGy. To establish the effects of irradiation on their physico-chemical properties, the compounds were then analysed by differential scanning calorimetry (DSC), scanning electron microscope (SEM), X-ray diffraction (XRD) and FT-IR spectrometry. The standard sterilisation dose (25 kGy) was found to cause no changes in only one derivative - acebutolol, whereas in the other derivatives the irradiation caused colour changes, differences in X-ray diffraction patterns and in the character of DSC curves, including a decrease in the melting point. For each derivative one clear peak corresponding to the process of melting was observed and its position shifted towards lower temperatures with increasing dose of irradiation. For all compounds studied the value of the shift was between 0.1 and 1.0 {sup o}C. For alprenolol, propranolol and metoprolol linear relations were found between the irradiation dose and the decrease in the melting point, described by the correlation coefficient (between 0.9446 and 0.9864). No changes were observed in

  3. Xerostomia: prevalence and pharmacotherapy. With special reference to beta-adrenoceptor antagonists.

    Science.gov (United States)

    Nederfors, T

    1996-01-01

    The main objective of this thesis was to estimate the prevalence of subjectively perceived dry mouth, xerostomia, in a representative general adult population, and the possible co-morbidity between xerostomia and on-going pharmacotherapy. Further, to evaluate the effects of beta-adrenoceptor antagonists on saliva flow rate and composition. The prevalence of xerostomia was evaluated by means of a questionnaire mailed to a random sample of 4.200 adult subjects living in the southern part of the province of Halland, Sweden. Three hundred men and equally many women aged 20, 30, 40, 50, 60, 70 and 80 years were selected from the national census register. From 3311 (81%) evaluable questionnaires was concluded that, in the studied population, 21.3% of the men and 27.3% of the women reported xerostomia. The difference between the sexes was statistically significant, women reporting higher prevalence of dry mouth than men. It was also found that xerostomia was significantly age-related. Further, it was demonstrated that there was a strong co-morbidity between reported prevalence of dry mouth and on-going pharmacotherapy. Generally, no specific drug or drug-group proved to be especially xerogenic, rather, polypharmacy was strongly correlated to reported symptoms of dry mouth, and it was also a significant correlation between increasing xerostomia and the number of medications taken. The effects of beta-adrenoceptor antagonists on saliva flow rate and composition were evaluated both in healthy volunteers and in hypertensive patients. The effects of one week of treatment with the non-selective (propranolol) and the beta 1-selective (atenolol) adrenoceptor antagonists were compared with that of placebo in three different clinical trials, including 38, 11 and 19 healthy volunteers, respectively. Two of these studies were focused on the effects on whole saliva secretion rate and composition and the third study on the secretions from the parotid and the submandibular

  4. Relative Importance of Aortic Stiffness and Volume as Predictors of Treatment-Induced Improvement in Left Ventricular Mass Index in Dialysis.

    Directory of Open Access Journals (Sweden)

    Panagiotis I Georgianos

    Full Text Available This study aimed to explore the relative contribution of aortic stiffness and volume in treatment-induced change of left ventricular mass in dialysis. Hypertension in Hemodialysis Patients Treated with Atenolol or Lisinopril trial compared the effect of lisinopril versus atenolol in reducing left ventricular mass index; 179 patients with echo measurements of aortic pulse wave velocity and left ventricular mass at baseline were included. In unadjusted analysis, overall reductions of 26.24 g/m2 (95% CI: -49.20, -3.29 and 35.67 g/m2 (95% CI: -63.70, -7.64 in left ventricular mass index were noted from baseline to 6 and 12 months respectively. Volume control emerged as an important determinant of regression of left ventricular mass index due to the following reasons: (i additional control for change in ambulatory systolic blood pressure mitigated the reduction in left ventricular mass index in the statistical model above [6-month visit: -18.6 g/m2 (95% CI: -43.7, 6.5; 12-month visit: -22.1 g/m2 (95% CI: -52.2, 8.0] (ii regression of left ventricular hypertrophy was primarily due to reduction in left ventricular chamber and not wall thickness and (iii adjustment for inferior vena cava diameter (as a proxy for volume removed the effect of time on left ventricular mass index reduction [6-month visit: -6.6 g/m2 (95% CI: (-41.6, 28.4; 12-month visit: 0.6 g/m2 (95% CI: -39.5, 40.7]. In contrast, aortic pulse wave velocity was neither a determinant of baseline left ventricular mass index nor predictor of its reduction. Among dialysis patients, ambulatory systolic pressure, a proxy for volume expansion, but not aortic stiffness is more important predictor of reduction in left ventricular mass index. Improving blood pressure control via adequate volume management appears as an effective strategy to improve left ventricular hypertrophy in dialysis.

  5. INFLUENCE OF ANTIHYPERTENSIVE THERAPY ON PSYCHOLOGICAL STATUS OF CHERNOBYL NUCLEAR POWER PLANT ACCIDENT CONSEQUENCES LIQUIDATORS

    Directory of Open Access Journals (Sweden)

    E. M. Manoshkina

    2006-01-01

    Full Text Available Aim. To study psychological status and influence of antihypertensive therapy (AHT on it in Chernobyl nuclear power plant (NPP accident consequences liquidators, who suffer arterial hyper-tension (AH, with controlled treatment compared to the standard treatment in out-patient clinic. Material and methods. 81 liquidators with AH (all men were included into open compara-tive randomized study. Study duration was 12 months. Patients were randomized into main group (MG and control group (CG. Patients of MG received strictly regulated stepped AHT based on ACE inhibitor spirapril 6 mg daily (Quadropril®, Pliva-AVD, hypothiazide was added if necessary (12.5-25 mg daily and afterwards – atenolol (12.5-100 mg daily. In CG AHT and its correction was set by physician in polyclinic. Brief multifactor questionnaire for personality analysis was used to study psychological status. Results. 57 patients completed the study, 28 in MG and 29 in CG. In MG target blood pres-sure (BP levels were reached in 22 (78.6% patients, in CG – in 11 (38% patients (p<0.01. The main feature of psychological status of liquidators with AH was hypochondriac, depressive and anxious disorders. Controlled AHT made it possible to reach improvement in psychological status, i.e. growth of optimism and activity of patients, more often, than standard treatment in out-patient clinics. Increase in number of patients with pronounced anxious changes was observed in CG. Effi-ciency of AHT in liquidators with AH is connected with severity of depressive disturbances: in subgroups with inefficient treatment patients had the highest level of depression. In liquidators with AH, possessing neurotic disturbances, spirapril was efficient both as monotherapy, and in combina-tion with diuretic hydrochlorothiazide and beta-blocker atenolol. Conclusion. Controlled AHT in liquidators with AH has advantages over standard treatment in out-patient clinic and results in more frequent target BP level

  6. Mesoporous silica based MCM-41 as solid-phase extraction sorbent combined with micro-liquid chromatography-quadrupole-mass spectrometry for the analysis of pharmaceuticals in waters.

    Science.gov (United States)

    Dahane, S; Martínez Galera, M; Marchionni, M E; Socías Viciana, M M; Derdour, A; Gil García, M D

    2016-05-15

    This paper reports the first application of the silica based mesoporous material MCM-41 as a sorbent in solid phase extraction, to pre-concentrate pharmaceuticals of very different polarity (atenolol, nadolol, pindolol, timolol, bisoprolol, metoprolol, betaxolol, ketoprofen, naproxen, ibuprofen, diclofenac, tolfenamic acid, flufenamic acid and meclofenamic acid) in surface waters. The analytes were extracted from 100mL water samples at pH 2.0 (containing 10(-3)mol/L of sodium chloride) by passing the solution through a cartridge filled with 100mg of MCM-41. Following elution, the pharmaceuticals were determined by micro-liquid chromatography and triple quadrupole-mass spectrometry. Two selected reaction monitoring transitions were monitored per compound, the most intense one being used for quantification and the second one for confirmation. Matrix effect was found in real waters for most analytes and was overcome using the standard addition method, which compared favorably with the matrix matched calibration method. The detection limits in solvent (acetonitrile:water 10:90, v/v) ranged from 0.01 to 1.48μg/L and in real water extracts from 0.10 to 3.85μg/L (0.001-0.0385μg/L in the water samples). The quantitation limits in solvent were in the range 0.02-4.93μg/L, whereas in real water extracts were between 0.45 and 10.00μg/L (0.0045 and 0.1000μg/L in the water samples). When ultrapure water samples were spiked at two concentration levels of each pharmaceutical (0.1 and 0.2μg/L) and quantified using solvent based calibration graphs, recoveries were near 100%. However, recoveries for most pharmaceuticals were comparable or better than de described above, when river water samples (spiked at the same concentration levels) were quantified by the standard addition method and slightly worse using the matrix matched calibration method. Five real samples (two rivers, one dam and two fountain water samples) were analyzed by the developed method, atenolol, timolol

  7. Photochemical fate of beta-blockers in NOM enriched waters

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Ling; Xu, Haomin; Cooper, William J. [Urban Water Research Center, Department of Civil and Environmental Engineering, University of California, Irvine, Irvine, CA 92697-2175 (United States); Song, Weihua, E-mail: wsong@fudan.edu.cn [Department of Environmental Science and Engineering, Fudan University, Shanghai 200433 (China)

    2012-06-01

    Beta-blockers, prescribed for the treatment of high blood pressure and for long-term use after a heart attack, have been detected in surface and ground waters. This study examines the photochemical fate of three beta-blockers, atenolol, metoprolol, and nadolol. Hydrolysis accounted for minor losses of these beta-blockers in the pH range 4-10. The rate of direct photolysis at pH 7 in a solar simulator varied from 6.1 to 8.9 h{sup -1} at pH 7. However, the addition of a natural organic matter (NOM) isolate enhanced the photochemical loss of all three compounds. Indirect photochemical fate, generally described by reactions with hydroxyl radical ({center_dot}OH) and singlet oxygen ({sup 1}{Delta}O{sub 2}), and, the direct reaction with the triplet excited state, {sup 3}NOM{sup Low-Asterisk }, also varied but collectively appeared to be the major loss factor. Bimolecular reaction rate constants of the three beta-blockers with {sup 1}{Delta}O{sub 2} and {center_dot}OH were measured and accounted for 0.02-0.04% and 7.2-38.9% of their loss, respectively. These data suggest that the {sup 3}NOM{sup Low-Asterisk} contributed 50.6-85.4%. Experiments with various {sup 3}NOM{sup Low-Asterisk} quenchers supported the hypothesis that it was singly the most important reaction. Atenolol was chosen for more detailed investigation, with the photoproducts identified by LC-MS analysis. The results suggested that electron-transfer could be an important mechanism in photochemical fate of beta-blockers in the presence of NOM. - Highlights: Black-Right-Pointing-Pointer Photochemical degradation of beta-blockers in the simulated natural waters. Black-Right-Pointing-Pointer Reactive Oxygen Species play a minor role in the indirect photodegradation. Black-Right-Pointing-Pointer The loss of beta-blockers results from direct reaction with {sup 3}DOM{sup Low-Asterisk }.

  8. Wastewater micropollutants as tracers of sewage contamination: analysis of combined sewer overflow and stream sediments.

    Science.gov (United States)

    Hajj-Mohamad, M; Aboulfadl, K; Darwano, H; Madoux-Humery, A-S; Guérineau, H; Sauvé, S; Prévost, M; Dorner, S

    2014-01-01

    A sensitive method was developed to measure the sediment concentration of 10 wastewater micropollutants selected as potential sanitary tracers of sewage contamination and include: nonsteroidal anti-inflammatory drugs (acetaminophen - ACE and diclofenac - DIC), an anti-epileptic drug (carbamazepine - CBZ), a β-blocker (atenolol - ATL), a stimulant (caffeine - CAF), a bronchodilator (theophylline - THEO), steroid hormones (progesterone - PRO and medroxyprogesterone - MedP), an artificial sweetener (aspartame - APM) and personal care products (N,N-diethyl-3-methylbenzamide - DEET). Natural sediments (combined sewer overflow and stream sediments) were extracted by ultrasonic-assisted extraction followed by solid-phase extraction. Analyses were performed using ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) using atmospheric pressure chemical ionisation in positive mode (APCI+) with a total analysis time of 4.5 min. Method detection limits were in the range of 0.01 to 15 ng g(-1) dry weight (dw) for the compounds of interest, with recoveries ranging from 75% to 156%. Matrix effects were observed for some compounds, never exceeding |±18%|. All results displayed a good degree of reproducibility and repeatability, with relative standard deviations (RSD) of less than 23% for all compounds. The method was applied to an investigation of stream and combined sewer overflow sediment samples that differed in organic carbon contents and particle size distributions. Acetaminophen, caffeine and theophylline (as confounded with paraxanthine) were ubiquitously detected at 0.13-22 ng g(-1) dw in stream bed sediment samples and 98-427 ng g(-1) dw in combined sewer overflow sediment samples. Atenolol (80.5 ng g(-1) dw) and carbamazepine (54 ng g(-1) dw) were quantified only in combined sewer overflow sediment samples. The highest concentrations were recorded for DEET (14 ng g(-1) dw) and progesterone (11.5 ng g(-1) dw) in stream bed and combined

  9. Soil Aquifer Treatment (SAT) and Constructed Wetlands (CW) Applications for Nutrients and Organic Micropollutants (OMPs) Attenuation Using Primary and Secondary Wastewater Effluents

    KAUST Repository

    Hamadeh, Ahmed F.

    2014-06-01

    Constructed wetlands (CW) and soil aquifer treatment (SAT) represent natural wastewater treatment systems (NWTSs). The high costs of conventional wastewater treatment techniques encourage more studies to investigate lower cost treatment methods which make these appropriate for developing and also in developed countries. The main objective of this research was to investigate the removals of nutrients and organic micropollutants (OMPs) through SAT, CW and the CW-SAT hybrid system. CWs are an efficient technology to purify and remove different nutrients as well as OMPs from wastewater. They removed most of the dissolved organic matter (DOC), total nitrogen (TN), ammonium and phosphate. Furthermore, CWs aeration could be used as one of the alternatives to reduce CWs footprint by around 10%. The vegetation in CWs plays an essential role in the treatment especially for nitrogen and phosphate removals, it is responsible for the removal of 15%, 55%, 38%, and 22% for TN, dissolved organic nitrogen (DON), nitrate and phosphate, respectively. CWs achieved a very high removal for some OMPs; they attenuated acetaminophen, caffeine, fluoxetine and trimethoprim (>90%) under different redox conditions. Moreover, it was found that increasing temperature (up to 36 C) could enhance the removals of atenolol, caffeine, DEET and trimethoprim by 17%, 14%, 28% and 45%, respectively. On the other hand, some OMPs, were found to be removed by vegetation such as: acetaminophen, caffeine, fluoxetine, sulfamethoxazole, and trimethoprim. Moreover, atenolol, caffeine, fluoxetine and trimethoprim, showed high removal (>80%) through SAT system. It was also found that, temperature increasing and using primary instead of secondary effluent could enhance the removal of some OMPs. The CWs performance study showed that these systems are adapted to the prevailing extreme arid conditions and the average percent removals are about, 88%, 96%, 98%, 98% and 92%, for COD, BOD and TSS, ammonium and phosphate

  10. Organically functionalized mesoporous SBA-15 as sorbents for removal of selected pharmaceuticals from water

    Energy Technology Data Exchange (ETDEWEB)

    Bui, Tung Xuan [School of Environmental Science and Engineering, Gwangju Institute of Science and Technology (GIST), 261 Cheomdan-gwagiro, Buk-gu, Gwangju 500-712 (Korea, Republic of); Kang, Seo-Young [International Environmental Research Center (IERC), Gwangju Institute of Science and Technology (GIST), 261 Cheomdan-gwagiro, Buk-gu, Gwangju 500-712 (Korea, Republic of); Lee, Sang-Hyup [Water Environment Center, Korea Institute of Science and Technology, Cheongryang, Seoul 130-650 (Korea, Republic of); Choi, Heechul, E-mail: hcchoi@gist.ac.kr [School of Environmental Science and Engineering, Gwangju Institute of Science and Technology (GIST), 261 Cheomdan-gwagiro, Buk-gu, Gwangju 500-712 (Korea, Republic of)

    2011-10-15

    Highlights: {yields} SBA-15 grafted with aminopropyl, hydroxymethyl, and trimethylsilyl groups as sorbents. {yields} Sorbents for removal of a mixture of 12 pharmaceuticals from water. {yields} Hydroxymethyl-SBA-15 shows similar adsorption efficiency like SBA-15. {yields} Aminopropyl-SBA-15 makes increase for clofibric acid, diclofenac, decrease for atenolol, estrone, trimethoprim. {yields} Trimethylsilyl-SBA-15 makes increase for 9 compounds; 7 compounds from 70.6% to 98.9%. - Abstract: Mesoporous silica SBA-15 and its postfunctionalized counterparts with hydroxymethyl (HM-SBA-15), aminopropyl (AP-SBA-15), and trimethylsilyl (TMS-SBA-15) were prepared and characterized by powder X-ray diffraction, N{sub 2} adsorption-desorption measurement, Fourier-transform infrared spectroscopy, and elemental analysis. The removal of a mixture of 12 selected pharmaceuticals was investigated by batch adsorption experiments onto SBA-15 and the grafted materials. SBA-15 showed to have moderate adsorption affinity with amino-containing (atenolol, trimethoprim) and hydrophobic pharmaceuticals, but it displayed minimal adsorption affinity toward hydrophilic compounds. HM-SBA-15 was analogous with SBA-15 in terms of the adsorption efficiency toward all pharmaceuticals. AP-SBA-15 exhibited an increase in the adsorption of two acidic compounds (clofibric acid, diclofenac) but a decrease in the adsorption of estrone and the two amino-containing compounds. Among the grafted materials, TMS-SBA-15 had the highest adsorption affinity toward most pharmaceuticals. Moreover, the adsorption of nine pharmaceuticals to TMS-SBA-15 was significantly higher than that to SBA-15; seven of which showed the removal percentages from 70.6% to 98.9% onto TMS-SBA-15. The number of pharmaceuticals showing high adsorption efficiency onto TMS-SBA-15 did not alter significantly as the pH changed in the range of 5.5-7.6. The results suggest that TMS-SBA-15 is a promising material for the removal of pharmaceuticals

  11. Factores de riesgo para infarto agudo de miocardio y prescripción de medicamentos para prevención secundaria

    Directory of Open Access Journals (Sweden)

    Desirée Sáenz-Campos

    2005-01-01

    Full Text Available Objetivo: tipificar algunos factores de riesgo coronario presentes en los pacientes que sobreviven a un primer infarto agudo de miocardio (IAM y describir el tratamiento farmacológico prescrito para profilaxis secundaria al egreso hospitalario. Métodos: estudio observacional, transversal y descriptivo, con información extraída del expediente clínico de 50 pacientes atendidos en 3 hospitales nacionales. Resultados: 42 varones y 8 mujeres, edad 63 ± 15 años, peso 67 ± 12 kg, Índice de Masa Corporal= 26.1 ± 2.1 kg/m², 38% hipertensos, 22% diabéticos (n= 8 pacientes con diabetes + hipertensión y 34% fumadores. Colesterol total 191 ± 45.7 mg/dL, colesterol-LDL 112 ± 33.8 mg/dL y colesterol-HDL 39.4 ± 8.26 mg/dL. Todos egresaron con medicamentos: 92% con antitrombóticos (predominó aspirina, 92% con estatinas, 78% con betabloqueador (atenolol o carvedilol, 70% con enalapril o losartán y 48% con nitratos. Conclusiones: este estudio piloto mostró que la enfermedad coronaria tiende a manifestarse desde la etapa de adulto joven, persiste en su mayor afectación a los varones y parecen prevalecer los factores de riesgo coronario modificables. Los antitrombóticos, beta- bloqueadores y las estatinas más frecuentemente prescritos.Objective: To describe some factors of coronary risk present in patients who survive a first acute myocardial infartion and the pharmacological treatment prescribed for secondary prevention. Methods: Observational, cross sectional and descriptive pilot study, information was obtained from the charts of 50 patients seen at 3 national hospitals. Results: 42 males and 8 women, age 63 ± 15 years, weight 67 ± 12 kg, Body Mass Index = 26.1 ± 2.1 kg/m², 38% hypertensive, 22% diabetic (n = 8 smokers patients with diabetes+hypertension and 34% smokers. Total cholesterol levels: 191 ± 45.7 mg/dL, cholesterol-LDL= 112 ± 33.8 mg/dL and cholesterol-HDL: 39.4 ± 8.26 mg/dL. The patients were prescribed: 92

  12. A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache.

    Directory of Open Access Journals (Sweden)

    Jeffrey L Jackson

    Full Text Available To compare the effectiveness and side effects of migraine prophylactic medications.We performed a network meta-analysis. Data were extracted independently in duplicate and quality was assessed using both the JADAD and Cochrane Risk of Bias instruments. Data were pooled and network meta-analysis performed using random effects models.PUBMED, EMBASE, Cochrane Trial Registry, bibliography of retrieved articles through 18 May 2014.We included randomized controlled trials of adults with migraine headaches of at least 4 weeks in duration.Placebo controlled trials included alpha blockers (n = 9, angiotensin converting enzyme inhibitors (n = 3, angiotensin receptor blockers (n = 3, anticonvulsants (n = 32, beta-blockers (n = 39, calcium channel blockers (n = 12, flunarizine (n = 7, serotonin reuptake inhibitors (n = 6, serotonin norepinephrine reuptake inhibitors (n = 1 serotonin agonists (n = 9 and tricyclic antidepressants (n = 11. In addition there were 53 trials comparing different drugs. Drugs with at least 3 trials that were more effective than placebo for episodic migraines included amitriptyline (SMD: -1.2, 95% CI: -1.7 to -0.82, -flunarizine (-1.1 headaches/month (ha/month, 95% CI: -1.6 to -0.67, fluoxetine (SMD: -0.57, 95% CI: -0.97 to -0.17, metoprolol (-0.94 ha/month, 95% CI: -1.4 to -0.46, pizotifen (-0.43 ha/month, 95% CI: -0.6 to -0.21, propranolol (-1.3 ha/month, 95% CI: -2.0 to -0.62, topiramate (-1.1 ha/month, 95% CI: -1.9 to -0.73 and valproate (-1.5 ha/month, 95% CI: -2.1 to -0.8. Several effective drugs with less than 3 trials included: 3 ace inhibitors (enalapril, lisinopril, captopril, two angiotensin receptor blockers (candesartan, telmisartan, two anticonvulsants (lamotrigine, levetiracetam, and several beta-blockers (atenolol, bisoprolol, timolol. Network meta-analysis found amitriptyline to be better than several other medications including candesartan, fluoxetine, propranolol, topiramate and valproate and no different than

  13. ISOCRATIC SEPARATION OF FOUR BETA BLOCKERS WITH AMLODIPINE BY C18 RP-HPLC: APPLICATION TO AMLODIPINE DETERMINATION IN PHARMACEUTICAL DOSAGE FORMS

    Directory of Open Access Journals (Sweden)

    Panchumarthy Ravisankar

    2013-06-01

    Full Text Available This method described for the successful separation of a beta blockers with amlodipine by RP-HPLC on a C18 column with UV detection. One of the key goals of High Performance Liquid Chromatography technique is to achieve a consistent and reproducible separation. A simple, precise, selective and sensitive HPLC method was developed and validated for determination of five anti-hypertensive agents, atenolol hydrochloride, metoprolol succinate, propranolol hydrochloride, amlodipine besylate and nebivolol hydrochloride with application to estimation of amlodipine besylate. RP-HPLC method was developed by using Welchrom C18 column (4.6 mm i.d. X 250mm, 5µm, Shimadzu LC-20AT ProminenceLiquid Chromatograph. The mobile phase composed of 10mM Phosphate buffer (pH3.0, adjusted with triethylamine: acetonitrile (50:50, v/v. The flow rate was set to 1.0ml/min with the responses measured at 235nm using Shimadzu SPD-20A Prominence UV-Visible detector. This method provides effective and reproducible separation of five anti-hypertensive agents less than 6 minutes. The retention times of atenolol hydrochloride, metoprolol succinate, propranolol hydrochloride, amlodipine besylate and nebivolol hydrochloride were found to be 2.310 min, 2.830 min, 3.473 min, 4.260 min and 4.960 min respectively. The statistical validation of the developed method was carried out according to ICH guidelines. Amlodipine besylate was found to give linear response in the concentration range of 2-10µg/ml. Recovery studies were performed to ascertain the accuracy by standard addition method and average recovery was found to be 99.83-100.40%. The LOD and LOQ were found to be 0.2251µg/ml and 0.6823µg/ml respectively. The developed method can be used for routine quality control analysis of amlodipine besylate in pharmaceutical tablet dosage form. It can also be extended for the determination of other above mentioned most commonly prescribed anti-hypertensive agents. The analysis yields a

  14. Ordered mesoporous silica carrier system applied in nanobiothecnology

    Directory of Open Access Journals (Sweden)

    Andreza de Sousa

    2005-10-01

    Full Text Available Ordered mesoporous materials like SBA15 possess a network of channels and pores of well-defined size in the nanoscale range (2-50 nm. This particular pore architecture makes them suitable candidates for hosting and delivery under appropriate conditions of a variety of molecules of pharmaceutical interest, including radiopharmaceuticals. The characteristics of SBA-15 prepared in different temperatures and the behavior of this system regarding microencapsulation of a model drug were investigated. The calcined samples were formed in 0.2 g disks and were soaked in a solution of atenolol used as a model drug. The modification of the aging temperature provoked changes in the structure of the pores, indicating the presence of microporosity and connections between mesopores. Aging the materials at a higher temperature resulted in no microporosity and this fact influenced the control of the release of the model drug.Recentes estudos conduziram à descoberta da sílica mesoporosa com estrutura hexagonal, que apresenta elevada área superficial (700 a 1000 m²/g, tamanho de poros grande (5 a 9 nm e espessura fina de parede do poro (3,5 a 5,3 nm, chamado SBA-15. Essas características fazem destes materiais matrizes adequadas para a incorporação e liberação controlada, sob condições apropriadas, de uma série de biomoléculas, principalmente radiofármacos. As características do SBA-15 preparado em diferentes temperaturas de envelhecimento e o comportamento desse sistema com relação ao micreoencapsulamento de uma droga modelo foi investigado. As amostras calcinadas foram conformadas em discos e imersas em uma solução saturada de atenolol, usado como droga modelo. A variação na temperatura de tratamento provoca algumas mudanças na estrutura dos poros, indicando a presença de microporosidade e interconectividade entre os mesoporos em condições específicas. Foi observado que materiais envelhecidos a elevadas temperaturas não apresentam

  15. Preparation of a novel positively charged nanofiltration composite membrane incorporated with silver nanoparticles for pharmaceuticals and personal care product rejection and antibacterial properties.

    Science.gov (United States)

    Huang, Zhong-Hua; Yin, Yan-Na; Aikebaier, Gu-li-mi-la; Zhang, Yan

    2016-01-01

    A novel positively charged N-[(2-hydroxy-3-trimethylammonium)propyl] chloride chitosan (HTCC)-Ag/polyethersulfone (PES) composite nanofiltration membrane was easily prepared by coating the active layer, HTCC, onto PES as the support through epichlorohydrin as the cross-linking reagent and nano-Ag particles as the introduced inorganic components. Scanning election microscopy, X-ray photoelectron spectroscopy, atomic force microscopy, and X-ray diffraction were employed to characterize the morphology of the resultant membranes, of which the molecular weight cut-off was about 941 Da. At 25 °C, the pure water permeability is 16.27 L/h·m(2)·MPa. Our results showed that the rejection of pharmaceuticals and personal care products (PPCPs) followed the sequence: atenolol > carbamazepine > ibuprofen, confirming that the membranes were positively charged. The antibacterial properties of the membranes were compared to elucidate the existence of Ag nanoparticles which help to improve antibacterial activity against Gram-negative Escherichia coli (DH5α, Rosetta) and Gram-positive Bacillus subtilis. The inhibition zone diameters of HTCC-Ag/PES membranes towards E. coli DH5α, E. coli Rosetta and Bacillus subtilis were 17.77, 16.18, and 15.44 mm, respectively. It was found that HTCC-Ag/PES membrane has a better antibacterial activity against E. coli than against Bacillus subtilis, especially for E. coli DH5α. PMID:27120646

  16. Occurrence of pharmaceuticals in river water and their elimination in a pilot-scale drinking water treatment plant.

    Science.gov (United States)

    Vieno, Niina M; Härkki, Heli; Tuhkanen, Tuula; Kronberg, Leif

    2007-07-15

    The occurrence of four beta blockers, one antiepileptic drug, one lipid regulator, four anti-inflammatories, and three fluoroquinolones was studied in a river receiving sewage effluents. All compounds but two of the fluoroquinolones were observed in the water above their limit of quantification concentrations. The highest concentrations (up to 107 ng L(-1)) of the compounds were measured during the winter months. The river water was passed to a pilot-scale drinking water treatment plant, and the elimination of the pharmaceuticals was followed during the treatment. The processes applied by the plant consisted of ferric salt coagulation, rapid sand filtration, ozonation, two-stage granular activated carbon filtration (GAC), and UV disinfection. Following the coagulation, sedimentation, and rapid sand filtration, the studied pharmaceuticals were found to be eliminated only by an average of 13%. An efficient elimination was found to take place during ozonation at an ozone dose of about 1 mg L(-1) (i.e., 0.2-0.4 mg of O3/ mg of TOC). Following this treatment, the concentrations of the pharmaceuticals dropped to below the quantification limits with the exception of ciprofloxacin. Atenolol, sotalol, and ciprofloxacin, the most hydrophilic of the studied pharmaceuticals, were not fully eliminated during the GAC filtrations. All in all, the treatment train was found to very effectively eliminate the pharmaceuticals from the rawwater. The only compound that was found to pass almost unaffected through all the treatment steps was ciprofloxacin.

  17. Development of surrogate correlation models to predict trace organic contaminant oxidation and microbial inactivation during ozonation.

    Science.gov (United States)

    Gerrity, Daniel; Gamage, Sujanie; Jones, Darryl; Korshin, Gregory V; Lee, Yunho; Pisarenko, Aleksey; Trenholm, Rebecca A; von Gunten, Urs; Wert, Eric C; Snyder, Shane A

    2012-12-01

    The performance of ozonation in wastewater depends on water quality and the ability to form hydroxyl radicals (·OH) to meet disinfection or contaminant transformation objectives. Since there are no on-line methods to assess ozone and ·OH exposure in wastewater, many agencies are now embracing indicator frameworks and surrogate monitoring for regulatory compliance. Two of the most promising surrogate parameters for ozone-based treatment of secondary and tertiary wastewater effluents are differential UV(254) absorbance (ΔUV(254)) and total fluorescence (ΔTF). In the current study, empirical correlations for ΔUV(254) and ΔTF were developed for the oxidation of 18 trace organic contaminants (TOrCs), including 1,4-dioxane, atenolol, atrazine, bisphenol A, carbamazepine, diclofenac, gemfibrozil, ibuprofen, meprobamate, naproxen, N,N-diethyl-meta-toluamide (DEET), para-chlorobenzoic acid (pCBA), phenytoin, primidone, sulfamethoxazole, triclosan, trimethoprim, and tris-(2-chloroethyl)-phosphate (TCEP) (R(2) = 0.50-0.83) and the inactivation of three microbial surrogates, including Escherichia coli, MS2, and Bacillus subtilis spores (R(2) = 0.46-0.78). Nine wastewaters were tested in laboratory systems, and eight wastewaters were evaluated at pilot- and full-scale. A predictive model for OH exposure based on ΔUV(254) or ΔTF was also proposed.

  18. Temporal variability of pharmaceuticals and illicit drugs in wastewater and the effects of a major sporting event.

    Science.gov (United States)

    Gerrity, Daniel; Trenholm, Rebecca A; Snyder, Shane A

    2011-11-01

    Diurnal variations in wastewater flows are common phenomena related to peak water use periods. However, few studies have examined high-resolution temporal variability in trace organic contaminant (TOrC) concentrations and loadings. Even fewer have assessed the impacts of a special event or holiday. This study characterizes the temporal variability associated with a major sporting event using flow data and corresponding mass loadings of a suite of prescription pharmaceuticals, potential endocrine disrupting compounds (EDCs), and illicit drugs. Wastewater influent and finished effluent samples were collected during the National Football League's Super Bowl, which is a significant weekend for tourism in the study area. Data from a baseline weekend is also provided to illustrate flows and TOrC loadings during "normal" operational conditions. Some compounds exhibited interesting temporal variations (e.g., atenolol), and several compounds demonstrated different loading profiles during the Super Bowl and baseline weekends (e.g., the primary cocaine metabolite benzoylecgonine). Interestingly, the influent mass loadings of prescription pharmaceuticals were generally similar in magnitude to those of the illicit drugs and their metabolites. However, conventional wastewater treatment was more effective in removing the illicit drugs and their metabolites. Total influent and effluent mass loadings are also provided to summarize treatment efficacy and environmental discharges.

  19. Comparison of the Usefulness of SPE Cartridges for the Determination of β-Blockers and β-Agonists (Basic Drugs in Environmental Aqueous Samples

    Directory of Open Access Journals (Sweden)

    Magda Caban

    2015-01-01

    Full Text Available Even though the methodology used for the determination of β-blockers and β-agonists in environmental samples is based mainly on solid-phase extraction (SPE and gas chromatography or liquid chromatography with mass spectrometric detection, the available literature data on the applied SPE procedures is rather sparse. In this paper such comparison is presented. Moreover, the usefulness of the eight SPE cartridges for the determination of five β-blockers (acebutolol, atenolol, metoprolol, nadolol, and propranolol and two β-agonists (salbutamol and terbutaline in environmental aqueous samples using GC techniques is tested. Among them, three (the trifunction sorbent Strata Screen C, the copolymers LiChrolut EN, and the functionalized copolymer Isolute ENV+ were used for the first time for this purpose. It was confirmed that polystyrene-divinylbenzene-N-vinylpyrrolidone copolymers (PS-DVB-VP, Strata-X, and Oasis HLB cartridges have a better potential than a cation-exchange sorbent for the extraction of the target drugs from environmental water samples. However, it should be stressed out that the direct application of the tested SPE conditions for the analysis of real environmental water samples is not possible, and such parameters, like volume of loading sample, appropriate solvents for washing and elution steps, and so forth, must be optimized again in order to achieve satisfactory recovery values for the target compounds.

  20. A rational approach to selecting and ranking some pharmaceuticals of concern for the aquatic environment and their relative importance compared with other chemicals.

    Science.gov (United States)

    Donnachie, Rachel L; Johnson, Andrew C; Sumpter, John P

    2016-04-01

    Aquatic organisms can be exposed to thousands of chemicals discharged by the human population. Many of these chemicals are considered disruptive to aquatic wildlife, and the literature on the impacts of these chemicals grows daily. However, because time and resources are not infinite, research must focus on the chemicals that represent the greatest threat. One group of chemicals of increasing concern is pharmaceuticals, for which the primary challenge is to identify which represent the greatest threat. In the present study, a list of 12 pharmaceuticals was compiled based on scoring the prevalence of different compounds from previous prioritization reviews. These included rankings based on prescription data, environmental concentrations, predicted environmental concentration/predicted no-effect concentration (PEC/PNEC) ratios, persistency/bioaccumulation/(eco)toxicity (PBT), and fish plasma model approaches. The most frequently cited were diclofenac, paracetamol, ibuprofen, carbamazepine, naproxen, atenolol, ethinyl estradiol, aspirin, fluoxetine, propranolol, metoprolol, and sulfamethoxazole. For each pharmaceutical, literature on effect concentrations was compiled and compared with river concentrations in the United Kingdom. The pharmaceuticals were ranked by degree of difference between the median effect and median river concentrations. Ethinyl estradiol was ranked as the highest concern, followed by fluoxetine, propranolol, and paracetamol. The relative risk of these pharmaceuticals was compared with those of metals and some persistent organic pollutants. Pharmaceuticals appear to be less of a threat to aquatic organisms than some metals (Cu, Al, Zn) and triclosan, using this ranking approach.

  1. Sorption behavior of 20 wastewater originated micropollutants in groundwater — Column experiments with pharmaceutical residues and industrial agents

    Science.gov (United States)

    Burke, Victoria; Treumann, Svantje; Duennbier, Uwe; Greskowiak, Janek; Massmann, Gudrun

    2013-11-01

    Since sorption is an essential process with regard to attenuation of organic pollutants during subsurface flow, information on the sorption properties of each pollutant are essential for assessing their environmental fate and transport behavior. In the present study, the sorption behavior of 20 wastewater originated organic micropollutants was assessed by means of sediment column experiments, since experimentally determined data for these compounds are not or sparsely represented in the literature. Compounds investigated include various psychoactive drugs, phenazone-type pharmaceuticals and β-blockers, as well as phenacetine, N-methylphenacetine, tolyltriazole and para-toluenesulfonamide. While for most of the compounds no or only a low sorption affinity was observed, an elevated tendency to sorb onto aquifer sand was obtained for the β-blockers atenolol, propranolol and metoprolol. A comparison between experimental data and data estimated based on the octanol/water partition coefficient following the QSAR approach demonstrated the limitations of the latter to predict the adsorption behavior in natural systems for the studied compounds.

  2. Simultaneous monitoring of photocatalysis of three pharmaceuticals by immobilized TiO2 nanoparticles: Chemometric assessment, intermediates identification and ecotoxicological evaluation

    Science.gov (United States)

    Khataee, A. R.; Fathinia, M.; Joo, S. W.

    2013-08-01

    In this study, the photocatalytic degradation of a mixture of three pharmaceuticals, Metronidazole (MET), Atenolol (ATL) and Chlorpromazine (CPR), was quantified simultaneously during the UV/TiO2 process. The investigated TiO2 was Millennium PC-500 immobilized on ceramic plates by sol-gel based method. The partial least squares modeling was successfully applied for the multivariate calibration of the spectrophotometric data. The central composite design was applied to model and optimize the UV/TiO2 process. Predicted values of removal efficiency were found to be in good agreement with experimental values for MET, ATL and CPR (R2 = 0.947 and Adj-R2 = 0.906, R2 = 0.977 and Adj-R2 = 0.960 and R2 = 0.982 and Adj-R2 = 0.969, respectively). The optimum initial concentration of pharmaceuticals, reaction time and UV light intensity was found to be 10 mg L-1, 150 min and 38.45 W m-2, respectively. The main degradation intermediates of pharmaceuticals produced in this process were identified by GC-MS technique. The chronic ecotoxicity of pharmaceuticals was evaluated using aquatic species Spirodela polyrrhiza prior to and after photocatalysis. The TOC results (90% removal after 16 h) and ecotoxicological experiments revealed that the photocatalysis process could effectively mineralize and reduce the ecotoxicity of the pharmaceuticals from their aqueous solutions.

  3. Distribuce léčiv v čistírnách odpadních vod

    OpenAIRE

    Šilhánková, Lenka

    2016-01-01

    Předložená bakalářská práce se zabývá aktuálním tématem – distribucí léčiv v odpadních vodách, u nichž byla prokázána toxicita na necílové organismy. Konkrétně řeší výskyt farmak ze skupiny beta-blokátorů, která se hojně podávají při léčbě hypertenze a dalších kardiovaskulárních onemocněních. Jako zástupci byly vybrány acebutolol, atenolol a bisoprolol, jejichž schopnost eliminace byla pozorována u tří čistíren odpadních vod (ČOV) s různou technologií čištění a rozdílným počet ekvivalentních ...

  4. Is it time to replace propranolol with carvedilol for portalhypertension?

    Institute of Scientific and Technical Information of China (English)

    2015-01-01

    Beta-adrenergic receptor antagonists (β-blockers) havebeen well established for use in portal hypertensionfor more than three decades. Different Non-selectiveβ-blockers like propranolol, nadolol, timolol, atenolol,metoprolol and carvedilol have been in clinical practicein patients with cirrhosis. Carvedilol has proven 2-4times more potent than propranolol as a beta-receptorblocker in trials conducted testing its efficacy forheart failure. Whether the same effect extends to itspotency in the reduction of portal venous pressuresis a topic of on-going debate. The aim of this reviewis to compare the hemodynamic and clinical effectsof carvedilol with propranolol, and attempt assesswhether carvedilol can be used instead of propranolol inpatients with cirrhosis. Carvedilol is a promising agentamong the beta blockers of recent time that has shownsignificant effects in portal hypertension hemodynamics.It has also demonstrated an effective profile in itsclinical application specifically for the prevention ofvariceal bleeding. Carvedilol has more potent desiredphysiological effects when compared to Propranolol.However, it is uncertain at the present juncture whetherthe improvement in hemodynamics also translates into adecreased rate of disease progression and complicationswhen compared to propranolol. Currently Carvedilolshows promise as a therapy for portal hypertension butmore clinical trials need to be carried out before we canconsider it as a superior option and a replacement forpropranolol.

  5. Photocatalytic degradation kinetics and mechanism of environmental pharmaceuticals in aqueous suspension of TiO{sub 2}: A case of {beta}-blockers

    Energy Technology Data Exchange (ETDEWEB)

    Yang Hai [State Key Laboratory of Organic Geochemistry and Guangdong Key Laboratory of Environmental Resources Utilization and Protection, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Kehua Street, Tianhe District, Guangzhou 510640 (China); Graduate School of Chinese Academy of Sciences, Beijing 100049 (China); An Taicheng, E-mail: antc99@gig.ac.cn [State Key Laboratory of Organic Geochemistry and Guangdong Key Laboratory of Environmental Resources Utilization and Protection, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Kehua Street, Tianhe District, Guangzhou 510640 (China); Li Guiying [State Key Laboratory of Organic Geochemistry and Guangdong Key Laboratory of Environmental Resources Utilization and Protection, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Kehua Street, Tianhe District, Guangzhou 510640 (China); Song Weihua; Cooper, William J. [Urban Water Research Center, Department of Civil and Environmental Engineering, University of California, Irvine, CA 92697-2175 (United States); Luo Haiying [State Key Laboratory of Organic Geochemistry and Guangdong Key Laboratory of Environmental Resources Utilization and Protection, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Kehua Street, Tianhe District, Guangzhou 510640 (China); Graduate School of Chinese Academy of Sciences, Beijing 100049 (China); Guangzhou Product Quality Supervision and Testing Institute, National Centre for Quality Supervision and Testing of Processed Food (Guangzhou), Guangzhou 510110 (China); Guo Xindong [Guangzhou Product Quality Supervision and Testing Institute, National Centre for Quality Supervision and Testing of Processed Food (Guangzhou), Guangzhou 510110 (China)

    2010-07-15

    This study investigated the photocatalytic degradation of three {beta}-blockers in TiO{sub 2} suspensions. The disappearance of the compounds followed pseudo-first-order kinetics according to the Langmuir-Hinshelwood model and the rate constants were 0.075, 0.072 and 0.182 min{sup -1} for atenolol, metoprolol and propranolol, respectively. After 240 min irradiation, the reaction intermediates were completely mineralized to CO{sub 2} and the nitrogen was predominantly as NH{sub 4}{sup +}. The influence of initial pH and {beta}-blocker concentration on the kinetics was also studied. From adsorption studies it appears that the photocatalytic degradation occurred mainly on the surface of TiO{sub 2}. Further studies indicated that surface reaction with {center_dot}OH radical was principally responsible for the degradation of these three {beta}-blockers. The major degradation intermediates were identified by HPLC/MS analysis. Cleavage of the side chain and the addition of the hydroxyl group to the parent compounds were found to be the two main degradation pathways for all three {beta}-blockers.

  6. Cardiac electrophysiological effects of selective adrenoceptor stimulation and their possible roles in arrhythmias.

    Science.gov (United States)

    Vaughan Williams, E M

    1985-01-01

    The selective alpha 1- and alpha 2-adrenoceptor agonists St 587 and BHT 933, respectively, and the antagonists prazosin (alpha 1) and WY 25309 (alpha 2) have been used in combination with the selective beta 2-adrenoceptor agonist pirbuterol, and the antagonists atenolol (beta 1) and ICI 118551 (beta 2), to analyse the effects of individual types of adrenoceptor stimulation in various parts of the rabbit heart. In the sinus node, beta 1-, but not beta 2-adrenoceptor stimulation increased the fast phase of depolarisation. Both beta 1- and beta 2-adrenoceptor stimulation increased the slope of the slow diastolic depolarisation, accelerated repolarisation, and increased maximum diastolic potential. Beta 1- and beta 2-adrenoceptor stimulation also accelerated repolarisation in Purkinje cells and papillary muscle. After blockade of both beta 1- and beta 2-adrenoceptors, alpha 1-adrenoceptor stimulation caused bradycardia, owing exclusively to delayed repolarisation. Alpha 2-adrenoceptor stimulation had no effect. Beta 1-, but not beta 2-adrenoceptor stimulation augmented peak contractions three- to fivefold, and reduced the time-to-peak tension. In contrast, alpha 1-adrenoceptor stimulation only moderately (up to 47%) increased peak tension, but increased time-to-peak and duration of contractions. The results would be consistent with beta 1-adrenoceptor stimulation increasing inward calcium current, and with stimulation of alpha 1-adrenoceptors delaying the decline of [Ca]i rather than increasing its magnitude. Both beta 1- and beta 2-stimulation increased repolarising current, but alpha 1-stimulation decreased it.

  7. Temporal variations and trends in loads of commonly used pharmaceuticals to large wastewater treatment plants in Sweden, a case study (Ryaverket).

    Science.gov (United States)

    Paxéus, N; Bester, K; El-taliawy, Haitham

    2016-01-01

    Loads of individual commonly used analgesics (ibuprofen, diclofenac), antibiotics (sulfamethoxazole, trimethoprim), β-blockers (atenolol, metoprolol, sotalol, propranolol) and neuroleptics (carbamazepine, citalopram) to a large-scale operating wastewater treatment plant (WWTP) in Sweden (Ryaverket) were studied by monitoring concentrations and flows during a 9-year period (2006-2015). Variations in loads due to sampling and possible errors in chemical analyses were estimated to be below 40%. The variations in loads were analyzed and discussed in terms of the design of collecting wastewater system as an integrated part of the water treatment at the WWTP as well as the prescription and use of individual pharmaceuticals. Trend analysis in daily loads of individual pharmaceuticals indicated an increase for diclofenac, no significant changes for ibuprofen and metoprolol and a decrease for the other pharmaceuticals. The latter was ascribed to a decrease in their prescription and use. The increase in loads of diclofenac was ascribed to its growing topical use not requiring prescription. In view of future regulations by the EU, growing loads of diclofenac to WWTPs and its low removal rates in WWTPs may require an upgrade of WWTPs to achieve quality standards for diclofenac in receiving waters.

  8. Self-organized nanoparticles based on drug-interpolyelectrolyte complexes as drug carriers

    Energy Technology Data Exchange (ETDEWEB)

    Palena, M. C.; Manzo, R. H.; Jimenez-Kairuz, A. F., E-mail: alvaro@fcq.unc.edu.ar [Universidad Nacional de Cordoba, UNITEFA-CONICET, Departamento de Farmacia, Facultad de Ciencias Quimicas (Argentina)

    2012-06-15

    Potential applications in drug delivery from nanostructures composed of two oppositely charged polymethacrylates, eudragit{sup Registered-Sign} L100 (EL) and eudragit{sup Registered-Sign} EPO (EE), loaded with three model basic drugs (D), atenolol, propranolol, and metroclopramide were evaluated. The self-organized nanoparticles based on drug-interpolyelectrolyte complexes (DIPEC), (EL-D{sub 50})-EE{sub X}, were obtained by mixing the aqueous dispersions of both polyelectrolytes at room temperature in an ultrasound bath. Dispersions of (EL-D{sub 50}) neutralized with increasing proportions of EE exhibited a rise of turbidity, particle sizes in the range of 150-400 nm, and high negative zeta potential. The sign of zeta potential was shifted from negative to positive by changes in composition of DIPEC. Freeze dried DIPEC were easily redispersed in water yielding nearly the same parameters of fresh dispersions. In vitro release experiments using Franz cells showed that DIPEC systems behave as a drug reservoir that slowly releases the drug as water is placed in the receptor compartment. The release rate was raised by ionic exchange with counterions present in simulated physiological fluids placed in the receptor media. Delivery of D from DIPEC exhibited a remarkable robustness toward simulated physiological media of different pH. The DIPEC systems exhibit interesting properties to design nanoparticulate drug delivery systems for oral and/or topical routes.

  9. How Do Antihypertensive Drugs Work? Insights from Studies of the Renal Regulation of Arterial Blood Pressure.

    Science.gov (United States)

    Digne-Malcolm, Holly; Frise, Matthew C; Dorrington, Keith L

    2016-01-01

    Though antihypertensive drugs have been in use for many decades, the mechanisms by which they act chronically to reduce blood pressure remain unclear. Over long periods, mean arterial blood pressure must match the perfusion pressure necessary for the kidney to achieve its role in eliminating the daily intake of salt and water. It follows that the kidney is the most likely target for the action of most effective antihypertensive agents used chronically in clinical practice today. Here we review the long-term renal actions of antihypertensive agents in human studies and find three different mechanisms of action for the drugs investigated. (i) Selective vasodilatation of the renal afferent arteriole (prazosin, indoramin, clonidine, moxonidine, α-methyldopa, some Ca(++)-channel blockers, angiotensin-receptor blockers, atenolol, metoprolol, bisoprolol, labetolol, hydrochlorothiazide, and furosemide). (ii) Inhibition of tubular solute reabsorption (propranolol, nadolol, oxprenolol, and indapamide). (iii) A combination of these first two mechanisms (amlodipine, nifedipine and ACE-inhibitors). These findings provide insights into the actions of antihypertensive drugs, and challenge misconceptions about the mechanisms underlying the therapeutic efficacy of many of the agents. PMID:27524972

  10. Preparation and characterization of mesoporous silicas modified with chiral selectors as stationary phase for high-performance liquid chromatography.

    Science.gov (United States)

    Pérez-Quintanilla, Damián; Morante-Zarcero, Sonia; Sierra, Isabel

    2014-01-15

    New hybrid materials were prepared as novel chiral stationary phases (CSPs) for high-performance liquid chromatography (HPLC). Pure mesoporous silica (SM) and ethylene-bridged periodic mesostructured organosilica (PMO) were functionalized, by a post-synthesis method, with derivates of erythromycin and vancomycin. N2 adsorption-desorption measurements, XRD, FT-IR, MAS NMR, SEM, TEM and elemental analysis were used to characterize the physico-chemical properties of these mesostructured materials, before and after the modification process. The synthesized particles had non-symmetrical 3-D wormhole-like mesostructure, spherical morphology, and a mean pore diameter between 53 and 59 Å. CSPs prepared were tested for the separation of four chiral β-blockers (atenolol, metoprolol, pindolol and propranolol) in normal phase (NP) and polar organic phase (PO) elution modes. Much stronger chiral interaction was observed in vancomycin-modified silicas. Results obtained in these preliminary studies will permit in future works to improve the synthesis route in order to design mesoporous materials with better performance as a chiral stationary phase for HPLC. PMID:24231079

  11. A Dual-Functional [SBA-15/Fe3O4/P(N-iPAAm] Hybrid System as a Potential Nanoplatform for Biomedical Application

    Directory of Open Access Journals (Sweden)

    Andreza de Sousa

    2014-01-01

    Full Text Available The synthesis strategy of a multifunctional system of [SBA-15/Fe3O4/P(N-iPAAm] hybrids of interest for bioapplications was explored. Magnetite nanoparticles coated by mesoporous silica were prepared by an alternative chemical route using neutral surfactant and without the application of any functionalization method. Monomer adsorption followed by in situ polymerization initiated by a radical was the adopted procedure to incorporate the hydrogel into the pore channels of silica nanocomposite. Characterization of the materials was carried out by using X-ray diffraction (XRD, Fourier-transform infrared spectroscopy (FTIR, N2 adsorption, transmission electron microscopy (TEM, and Temperature programmed reduction studies (TPR. Their application as drug delivery system using atenolol as a model drug to assess the influence of the application of low frequency alternating magnetic fields on drug release was evaluated. The structural characteristics of the magnetic hybrid nanocomposite, including the effect of the swelling behavior on heating by the application of an alternating magnetic field, are presented and discussed.

  12. Analysis by liquid chromatography-electrospray ionization tandem mass spectrometry and acute toxicity evaluation for beta-blockers and lipid-regulating agents in wastewater samples.

    Science.gov (United States)

    Hernando, M D; Petrovic, M; Fernández-Alba, A R; Barceló, D

    2004-08-13

    This paper describes a multiresidue method for the extraction and determination of two therapeutic groups of pharmaceuticals, lipid-regulating agents (clofibric acid, bezafibrate, gemfibrocil, fenofibrate) and beta-blockers (atenolol, sotalol, metoprolol, betaxolol) in waters by solid-phase extraction followed by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS-MS). Recoveries obtained from spiked HPLC water, as well as, from spiked real samples (sewage treatment plants influent and effluents, river and tap water) were all above 60%, with the exception of betaxolol with a 52% recovery. The quantitative MS analysis was performed using a multiple reaction monitoring. The LC-MS-MS method gave detection limits ranging from 0.017 to 1.25 microg/l in spiked effluent. Precision of the method, calculated as relative standard deviation, ranged from 3.7 to 18.5%. Individual and combined effects on Daphnia magna were evaluated for both therapeutic groups. Individual effects in culture medium showed these compounds as not harmful and not toxic, an exception is fenofibrate that was found to be harmful, but at high, in the environment unrealistic concentrations (EC50 of 50 mg/l). Combined effect in wastewater showed synergistic toxic effects at low concentration level (2 microg/l). PMID:15387181

  13. Metabolism of pharmaceutical and personal care products by carrot cell cultures.

    Science.gov (United States)

    Wu, Xiaoqin; Fu, Qiuguo; Gan, Jay

    2016-04-01

    With the increasing use of treated wastewater and biosolids in agriculture, residues of pharmaceutical and personal care products (PPCPs) in these reused resources may contaminate food produce via plant uptake, constituting a route for human exposure. Although various PPCPs have been reported to be taken up by plants in laboratories or under field conditions, at present little information is available on their metabolism in plants. In this study, we applied carrot cell cultures to investigate the plant metabolism of PPCPs. Five phase I metabolites of carbamazepine were identified and the potential metabolism pathways of carbamazepine were proposed. We also used the carrot cell cultures as a rapid screening tool to initially assess the metabolism potentials of 18 PPCPs. Eleven PPCPs, including acetaminophen, caffeine, meprobamate, primidone, atenolol, trimethoprim, DEET, carbamazepine, dilantin, diazepam, and triclocarban, were found to be recalcitrant to metabolism. The other 7 PPCPs, including triclosan, naproxen, diclofenac, ibuprofen, gemfibrozil, sulfamethoxazole, and atorvastatin, displayed rapid metabolism, with 0.4-47.3% remaining in the culture at the end of the experiment. Further investigation using glycosidase hydrolysis showed that 1.3-20.6% of initially spiked naproxen, diclofenac, ibuprofen, and gemfibrozil were transformed into glycoside conjugates. Results from this study showed that plant cell cultures may be a useful tool for initially exploring the potential metabolites of PPCPs in plants as well as for rapidly screening the metabolism potentials of a variety of PPCPs or other emerging contaminants, and therefore may be used for prioritizing compounds for further comprehensive evaluations. PMID:26745399

  14. Leaching of pharmaceuticals and personal care products in turfgrass soils during recycled water irrigation.

    Science.gov (United States)

    Bondarenko, S; Gan, J; Ernst, F; Green, R; Baird, J; McCullough, M

    2012-01-01

    An important beneficial reuse of treated wastewater (recycled water) in arid and semiarid regions is landscape irrigation. However, the environmental fate, especially groundwater contamination potential, of trace contaminants such as pharmaceuticals and personal care products (PPCPs) is a significant concern that can hinder the acceptance and adoption of such reuses. In this study, we irrigated mature turfgrass plots with nonspiked tertiary treated wastewater for over 6 mo at 100 or 130% of the reference evapotranspiration rate (ETo) and collected leachate water at the 90-cm depth on a weekly basis. In the recycled water, all 14 target PPCPs were consistently found, and the mean levels of atenolol, gemfibrozil, meprobamate, carbamazepine, and sulfamethoxazole were above 100 ng L. However, only five compounds were detected in the leachate at trace levels. Trimethoprim and primidone were frequently found, whereas the detection of sulfamethoxazole, meprobamate and carbamazepine was less frequent (meprobamate. The majority of the target PPCPs were completely removed. Given that the irrigation rates were higher than normal, this study clearly demonstrated the efficacy of turfgrass systems in attenuating PPCPs during recycled water irrigation. However, it is also apparent that some PPCPs are more susceptible to leaching than others, and these PPCPs thus merit further research attention. PMID:22751071

  15. Biotransformation of trace organic compounds by activated sludge from a biological nutrient removal treatment system.

    Science.gov (United States)

    Inyang, Mandu; Flowers, Riley; McAvoy, Drew; Dickenson, Eric

    2016-09-01

    The removal of trace organic compounds (TOrCs) and their biotransformation rates, kb (LgSS(-)(1)h(-)(1)) was investigated across different redox zones in a biological nutrient removal (BNR) system using an OECD batch test. Biodegradation kinetics of fourteen TOrCs with initial concentration of 1-36μgL(-)(1) in activated sludge were monitored over the course of 24h. Degradation kinetic behavior for the TOrCs fell into four groupings: Group 1 (atenolol) was biotransformed (0.018-0.22LgSS(-)(1)h(-)(1)) under anaerobic, anoxic, and aerobic conditions. Group 2 (meprobamate and trimethoprim) biotransformed (0.01-0.21LgSS(-)(1)h(-)(1)) under anoxic and aerobic conditions, Group 3 (DEET, gemfibrozil and triclosan) only biotransformed (0.034-0.26LgSS(-)(1)h(-)(1)) under aerobic conditions, and Group 4 (carbamazepine, primidone, sucralose and TCEP) exhibited little to no biotransformation (<0.001LgSS(-)(1)h(-)(1)) under any redox conditions. BNR treatment did not provide a barrier against Group 4 compounds. PMID:27309772

  16. Using ultraviolet absorbance and color to assess pharmaceutical oxidation during ozonation of wastewater.

    Science.gov (United States)

    Wert, Eric C; Rosario-Ortiz, Fernando L; Snyder, Shane A

    2009-07-01

    The reduction of ultraviolet (UV) absorbance at 254 nm (UV254) and true color were identified as appropriate surrogates to assess the oxidation of six pharmaceuticals (i.e., carbamazepine, meprobamate, dilantin, primidone, atenolol, and iopromide) during ozonation of wastewater. Three tertiary-treated wastewaters were evaluated during oxidation with ozone (O3) and O3 coupled with hydrogen peroxide (O3/H2O2). The correlation between pharmaceutical oxidation and removal of UV254 was dependent upon the reactivity of each specific compound toward ozone, as measured by the second-order rate constant (k'(O3)). Oxidation of compounds with k'(O3) > 10(3) M(-1) s(-1) correlated well (R2 > 0.73) with UV254 reduction between 0-50%. Oxidation of compounds with apparent k'(O3) 0.80) with the UV254 reduction of 15-85%. The removal of true color also correlated well (R2 > 0.85) with the oxidation of pharmaceuticals during the ozonation of two wastewaters. These correlations demonstrate that UV254 reduction and true color removal may be used as surrogates to evaluate pharmaceutical oxidation in the presence or absence of dissolved ozone residual during advanced wastewater treatment with O3 or O3/H2O2. The use of online UV254 measurements would allow wastewater utilities to optimize the ozone dose required to meet their specific treatment objectives. PMID:19673276

  17. Evaluation of UV/H(2)O(2) treatment for the oxidation of pharmaceuticals in wastewater.

    Science.gov (United States)

    Rosario-Ortiz, Fernando L; Wert, Eric C; Snyder, Shane A

    2010-03-01

    Advanced oxidation treatment using low pressure UV light coupled with hydrogen peroxide (UV/H(2)O(2)) was evaluated for the oxidation of six pharmaceuticals in three wastewater effluents. The removal of these six pharmaceuticals (meprobamate, carbamazepine, dilantin, atenolol, primidone and trimethoprim) varied between no observed removal and >90%. The role of the water quality (i.e., alkalinity, nitrite, and specifically effluent organic matter (EfOM)) on hydroxyl radical (OH) exposure was evaluated and used to explain the differences in pharmaceutical removal between the three wastewaters. Results indicated that the efficacy of UV/H(2)O(2) treatment for the removal of pharmaceuticals from wastewater was a function of not only the concentration of EfOM but also its inherent reactivity towards OH. The removal of pharmaceuticals also correlated with reductions in ultraviolet absorbance at 254nm (UV(254)), which offers utilities a surrogate to assess pharmaceutical removal efficiency during UV/H(2)O(2) treatment. PMID:19931113

  18. Removal of pharmaceuticals and personal care products in a membrane bioreactor wastewater treatment plant.

    Science.gov (United States)

    Kim, M; Guerra, P; Shah, A; Parsa, M; Alaee, M; Smyth, S A

    2014-01-01

    Ninety-nine pharmaceuticals and personal care products (PPCPs) were analyzed in influent, final effluent, and biosolids samples from a wastewater treatment plant employing a membrane bioreactor (MBR). High concentrations in influent were found for acetaminophen, caffeine, metformin, 2-hydroxy-ibuprofen, paraxanthine, ibuprofen, and naproxen (10(4)-10(5) ng/L). Final effluents contained clarithromycin, metformin, atenolol, carbamazepine, and trimethoprim (>500 ng/L) at the highest concentrations, while triclosan, ciprofloxacin, norfloxacin, triclocarban, metformin, caffeine, ofloxacin, and paraxanthine were found at high concentrations in biosolids (>10(3) ng/g dry weight). PPCP removals varied from -34% to >99% and 23 PPCPs had ≥90% removal. Of the studied PPCPs, 26 compounds have been rarely or never studied in previous membrane bioreactor (MBR) investigations. The removal pathway showed that acetaminophen, 2-hydroxy-ibuprofen, naproxen, ibuprofen, codeine, metformin, enalapril, atorvastatin, caffeine, paraxanthine, and cotinine exhibited high degradation/transformation. PPCPs showing strong sorption to solids included triclocarban, triclosan, miconazole, tetracycline, 4-epitetracycline, norfloxacin, ciprofloxacin, doxycycline, paroxetine, and ofloxacin. Trimethoprim, oxycodone, clarithromycin, thiabendazole, hydrochlorothiazide, erythromycin-H2O, carbamazepine, meprobamate, and propranolol were not removed during treatment, and clarithromycin was even formed during treatment. This investigation extended our understanding of the occurrence and fate of PPCPs in an MBR process through the analysis of the largest number of compounds in an MBR study to date. PMID:24901615

  19. Development of surrogate correlation models to predict trace organic contaminant oxidation and microbial inactivation during ozonation.

    Science.gov (United States)

    Gerrity, Daniel; Gamage, Sujanie; Jones, Darryl; Korshin, Gregory V; Lee, Yunho; Pisarenko, Aleksey; Trenholm, Rebecca A; von Gunten, Urs; Wert, Eric C; Snyder, Shane A

    2012-12-01

    The performance of ozonation in wastewater depends on water quality and the ability to form hydroxyl radicals (·OH) to meet disinfection or contaminant transformation objectives. Since there are no on-line methods to assess ozone and ·OH exposure in wastewater, many agencies are now embracing indicator frameworks and surrogate monitoring for regulatory compliance. Two of the most promising surrogate parameters for ozone-based treatment of secondary and tertiary wastewater effluents are differential UV(254) absorbance (ΔUV(254)) and total fluorescence (ΔTF). In the current study, empirical correlations for ΔUV(254) and ΔTF were developed for the oxidation of 18 trace organic contaminants (TOrCs), including 1,4-dioxane, atenolol, atrazine, bisphenol A, carbamazepine, diclofenac, gemfibrozil, ibuprofen, meprobamate, naproxen, N,N-diethyl-meta-toluamide (DEET), para-chlorobenzoic acid (pCBA), phenytoin, primidone, sulfamethoxazole, triclosan, trimethoprim, and tris-(2-chloroethyl)-phosphate (TCEP) (R(2) = 0.50-0.83) and the inactivation of three microbial surrogates, including Escherichia coli, MS2, and Bacillus subtilis spores (R(2) = 0.46-0.78). Nine wastewaters were tested in laboratory systems, and eight wastewaters were evaluated at pilot- and full-scale. A predictive model for OH exposure based on ΔUV(254) or ΔTF was also proposed. PMID:23062789

  20. Short-limb dwarfism and hypertrophic cardiomyopathy in a patient with paternal isodisomy 14: 45,XYidic(14)(p11)

    Energy Technology Data Exchange (ETDEWEB)

    Walter, C.A.; Moore, C.M.; Kaye, C.I. [Univ. of Texas Health Science Center, San Antonio, TX (United States)] [and others

    1996-11-11

    Uniparental disomy (UPD) has been shown to result in specific disorders either due to imprinting and/or homozygosity of mutant alleles. Here we present the findings in a child with paternal UPD14. Ultrasound evaluation was performed at 30 weeks of gestation because of abnormally large uterine size. Pertinent ultrasound findings included polyhydramnios, short limbs, abnormal position of hands, small thorax, and nonvisualization of the fetal stomach. Postnatally the infant was found to have a low birth weight, short birth length, contractures, short limbs, and a small thorax with upslanting ribs. Assisted ventilation and gastrostomy were required. At age 6 months, the infant required hospitalization for hypertrophic cardiomyopathy which responded to Atenolol{reg_sign}. Initial cytogenetic studies demonstrated an apparently balanced de novo Robertsonian translocation involving chromosomes 14 and a karyotype designation of 45,XY,t(14q14q). No indication of mosaicism for trisomy 14 was observed in metaphase spreads prepared from peripheral blood lymphocytes or skin-derived fibroblasts. C-band and fluorescence in situ hybridization results demonstrated that the chromosome was dicentric. DNA analyses showed paternal uniparental isodisomy for chromosome 14. Based on the cytogenetic and DNA results a final karyotype designation of 45,XY,idic(14)(p11) was assigned to this infant with paternal isodisomy of chromosome 14. 41 refs., 5 figs., 2 tabs.

  1. A Sensitive Medium-Throughput Method to Predict Intestinal Absorption in Humans Using Rat Intestinal Tissue Segments.

    Science.gov (United States)

    Da Silva, Laís Cristina; Da Silva, Taynara Lourenço; Antunes, Alisson Henrique; Rezende, Kênnia Rocha

    2015-09-01

    A range of in vitro, ex vivo, and in vivo approaches are currently used for drug development. Highly predictive human intestinal absorption models remain lagging behind the times because of numerous variables concerning permeability through gastrointestinal tract in humans. However, there is a clear need for a drug permeability model early in the drug development process that can balance the requirements for high throughput and effective predictive potential. The present study developed a medium throughput screening Snapwell (MTS-Snapwell) ex vivo model to provide an alternative method to classify drug permeability. Rat small intestine tissue segments were mounted in commercial Snapwell™ inserts. Unidirectional drug transport (A-B) was measured by collecting samples at different time points. Viability of intestinal tissue segments was measured by examining transepithelial electric resistance (TEER) and phenol red and caffeine transport. As a result, the apparent permeability (Papp; ×10(-6) cm/s) was determined for atenolol (10.7 ± 1.2), caffeine (17.6 ± 3.1), cimetidine (6.9 ± 0.1), metoprolol (12.6 ± 0.7), theophylline (15.3 ± 1.6) and, ranitidine (3.8 ± 0.4). All drugs were classified in high/low permeability according to Biopharmaceutics Classification System showing high correlation with human data (r = 0.89). These findings showed a high correlation with human data (r = 0.89), suggesting that this model has potential predictive capacity for paracellular and transcellular passively absorbed molecules.

  2. Effect of Sesame Oil on Diuretics or ß-blockers in the Modulation of Blood Pressure, Anthropometry, Lipid Profile, and Redox Status

    Science.gov (United States)

    Sankar, D.; Rao, M. Ramakrishna; Sambandam, G.; Pugalendi, K.V.

    2007-01-01

    The study was undertaken to investigate the effect of sesame oil in hypertensive patients who were on antihypertensive therapy either with diuretics (hydrochlorothiazide) or ß-blockers (atenolol). Thirty-two male and 18 female patients aged 35 to 60 years old were supplied sesame oil (Idhayam gingelly oil) and instructed to use it as the only edible oil for 45 days. Blood pressure, anthropometry, lipid profile, lipid peroxidation, and enzymic and non-enzymic antioxidants were measured at baseline and after 45 days of sesame oil substitution. Substitution of sesame oil brought down systolic and diastolic blood pressure to normal. The same patients were asked to withdraw sesame oil consumption for another 45 days, and the measurements were repeated at the end of withdrawal period. Withdrawal of sesame oil substitution brought back the initial blood pressure values. A significant reduction was noted in body weight and body mass index (BMI) upon sesame oil substitution. No significant alterations were observed in lipid profile except triglycerides. Plasma levels of sodium reduced while potassium elevated upon the substitution of sesame oil. Lipid peroxidation (thiobarbituric acid reactive substances [TBARS]) decreased while the activities of superoxide dismutase (SOD), catalase (CAT), and the levels of vitamin C, vitamin E, ß-carotene, and reduced glutathione (GSH) were increased. The results suggested that sesame oil as edible oil lowered blood pressure, decreased lipid peroxidation, and increased antioxidant status in hypertensive patients. PMID:17876372

  3. Dietary Supplementation of Ginger and Turmeric Rhizomes Modulates Platelets Ectonucleotidase and Adenosine Deaminase Activities in Normotensive and Hypertensive Rats.

    Science.gov (United States)

    Akinyemi, Ayodele Jacob; Thomé, Gustavo Roberto; Morsch, Vera Maria; Bottari, Nathieli B; Baldissarelli, Jucimara; de Oliveira, Lizielle Souza; Goularte, Jeferson Ferraz; Belló-Klein, Adriane; Oboh, Ganiyu; Schetinger, Maria Rosa Chitolina

    2016-07-01

    Hypertension is associated with platelet alterations that could contribute to the development of cardiovascular complications. Several studies have reported antiplatelet aggregation properties of ginger (Zingiber officinale) and turmeric (Curcuma longa) with limited scientific basis. Hence, this study assessed the effect of dietary supplementation of these rhizomes on platelet ectonucleotidase and adenosine deaminase (ADA) activities in Nω-nitro-l-arginine methyl ester hydrochloride (l-NAME) induced hypertensive rats. Animals were divided into seven groups (n = 10): normotensive control rats; induced (l-NAME hypertensive) rats; hypertensive rats treated with atenolol (10 mg/kg/day); normotensive and hypertensive rats treated with 4% supplementation of turmeric or ginger, respectively. After 14 days of pre-treatment, the animals were induced with hypertension by oral administration of l-NAME (40 mg/kg/day). The results revealed a significant (p < 0.05) increase in platelet ADA activity and ATP hydrolysis with a concomitant decrease in ADP and AMP hydrolysis of l-NAME hypertensive rats when compared with the control. However, dietary supplementation with turmeric or ginger efficiently prevented these alterations by modulating the hydrolysis of ATP, ADP and AMP with a concomitant decrease in ADA activity. Thus, these activities could suggest some possible mechanism of the rhizomes against hypertension-derived complications associated to platelet hyperactivity. Copyright © 2016 John Wiley & Sons, Ltd. PMID:27151061

  4. How to Give TCM Differential Treatment for Senile Severe Hypertension?

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    @@ Senile severe hypertension refers to the condition in patients over 60 years old who have a diastolic pressure ≥ 14.7 kPa (110 mmHg) and a systolic pressure ≥ 26.7 kPa (200mmHg). Usually, the course of illness is long, and accompanied with various degrees of visceral lesions of the heart, brain and kidney. It has been proved by clinical experience that the blood pressure can't be made to decrease too fast nor decrease too slow so as to prevent the severe complications which may happen after a long-term high blood pressure. In addition to small dosage of such western drugs as Nifepine (10mg), Captopril (12.5mg) and Atenolol (12.5mg), Chinese herbal drugs can be prescribed based on TCM differentiation of the syndromes for lowering the blood pressure, improving the blood supply of the heart and brain, and relieving the clinical symptoms. The TCM differential treatment can be given for the following 3 patterns of syndromes.

  5. EVALUATION OF THE RELATIVE INCIDENCE OF ADVERSE EFFECTS LEADING TO TREATMENT DISCONTINUATION OF RECOMMENDED ANTIHYPERTENSIVE DRUGS

    Directory of Open Access Journals (Sweden)

    Yakubu Sani Ibn

    2013-06-01

    Full Text Available This study aimed at evaluating the incidence of adverse effects leading to treatment discontinuation of antihypertensive drugs within the same therapeutic class. Individual medical records were searched to identify those hypertensive patients who had been commenced on antihypertensive therapy during a 24-month period and who had subsequently for a reason(s discontinued the therapy. The results showed variation in discontinuation rates for drugs within same class, and that might be related to the relative frequency of specific adverse effects. Cough was the reason cited for discontinuation of angiotensin converting enzyme inhibitors, with linosopril appearing to be better tolerated than captopril (39% vs 48% ; peripheral oedema with calcium channel blockers, with amlodipine appearing to be better tolerated than nifedipine (29% vs 38% and bradycardia with beta adrenergic receptor blockers, with propranolol better tolerated than atenolol (0% vs 48%. Diuretics showed the lowest discontinuation rate (3.3% mainly due to hypokalemia, with thiazide better tolerated than frusemide (11% vs 43%. Prescribers should verify their use of antihypertensive drugs to ensure that they prescribe drugs with lower adverse effect rates, in order that patients with hypertension continue using the medication in the long term, thereby reducing the risk of developing cardiovascular complications associated with uncontrolled blood pressure.

  6. [General awareness and use of generic medication among citizens of Tubarão, state of Santa Catarina, Brazil].

    Science.gov (United States)

    Blatt, Carine Raquel; Trauthman, Silvana Cristina; Schmidt, Edegar Henrique; Marchesan, Samuel; da Silva, Luana May; Martins, João Luiz

    2012-01-01

    Although generic medication has been introduced in the country to offer an accessible alternative to brand-name medication, it represents only 14% of sales in number of units within the pharmaceutical market. The aim of this work was to research the level of awareness and the use of generic products among residents of the municipality of Tubarão, State of Santa Catarina, Brazil. A transversal study was carried out with a sample of 234 interviewees, distributed among municipal areas. With regard to use, the majority of those interviewed had used generic medication, and half of them had at least one such product in their home. To verify awareness of different types of medication, pictures with the generic, brand name and similar packaging for paracetamol and atenolol were shown and 91% were able to identify all products correctly. To be of higher economic standing, already having used generic products, believing that the generic medication has the same effect as the brand name medication, finding generic products in drugstores easily and being accustomed to buy generic products, were factors that were positively associated with the correct identification. PMID:22218542

  7. sup 86 Rb(K) influx and ( sup 3 H)ouabain binding by human platelets: Evidence for beta-adrenergic stimulation of Na-K ATPase activity

    Energy Technology Data Exchange (ETDEWEB)

    Turaihi, K.; Khokher, M.A.; Barradas, M.A.; Mikhailidis, D.P.; Dandona, P. (Royal Free Hospital and School of Medicine, London (England))

    1989-08-01

    Although active transport of potassium into human platelets has been demonstrated previously, there is hitherto no evidence that human platelets have an ouabain-inhibitable Na-K ATPase in their membrane. The present study demonstrates active rubidium (used as an index of potassium influx), {sup 86}Rb(K), influx into platelets, inhibitable by ouabain, and also demonstrates the presence of specific ({sup 3}H)ouabain binding by the human platelet. This {sup 86}Rb(K) influx was stimulated by adrenaline, isoprenaline, and salbutamol, but noradrenaline caused a mild inhibition. Active {sup 86}Rb(K) influx by platelets was inhibited markedly by timolol, mildly by atenolol, but not by phentolamine. Therefore, active {sup 86}Rb(K) influx in human platelets is enhanced by stimulation of beta adrenoceptors of the beta 2 subtype. The platelet may therefore replace the leukocyte in future studies of Na-K ATPase activity. This would be a considerable advantage in view of the ease and rapidity of preparation of platelets.

  8. Sorption behavior of 20 wastewater originated micropollutants in groundwater--column experiments with pharmaceutical residues and industrial agents.

    Science.gov (United States)

    Burke, Victoria; Treumann, Svantje; Duennbier, Uwe; Greskowiak, Janek; Massmann, Gudrun

    2013-11-01

    Since sorption is an essential process with regard to attenuation of organic pollutants during subsurface flow, information on the sorption properties of each pollutant are essential for assessing their environmental fate and transport behavior. In the present study, the sorption behavior of 20 wastewater originated organic micropollutants was assessed by means of sediment column experiments, since experimentally determined data for these compounds are not or sparsely represented in the literature. Compounds investigated include various psychoactive drugs, phenazone-type pharmaceuticals and β-blockers, as well as phenacetine, N-methylphenacetine, tolyltriazole and para-toluenesulfonamide. While for most of the compounds no or only a low sorption affinity was observed, an elevated tendency to sorb onto aquifer sand was obtained for the β-blockers atenolol, propranolol and metoprolol. A comparison between experimental data and data estimated based on the octanol/water partition coefficient following the QSAR approach demonstrated the limitations of the latter to predict the adsorption behavior in natural systems for the studied compounds. PMID:24077094

  9. Role of wetland organic matters as photosensitizer for degradation of micropollutants and metabolites.

    Science.gov (United States)

    Lee, Eunkyung; Shon, Ho Kyong; Cho, Jaeweon

    2014-07-15

    Overall photodegradation of pharmaceuticals, personal care products (PPCPs) and pharmaceutical metabolites were investigated in order to evaluate their photochemical fate in aquatic environments in various natural organic matter (NOM) enriched solutions. Tested PPCPs exhibited different rates of loss during direct and indirect photolysis. Here, only ultraviolet (UV) light source was used for direct photolysis and UV together with (3)DOM(*)for indirect photolysis. Diclofenac and sulfamethoxazole were susceptible to photodegradation, whereas carbamazepine, caffeine, paraxanthine and tri(2-chloroethyl) phosphate (TCEP) showed low levels of photodegradation rate, reflecting their conservative photoreactivity. During indirect photodegradation, in contrast to the hydrophilic autochthonous NOM, allochthonous NOM with relatively high molecular weight (MW), specific ultraviolet absorbance (SUVA) and hydrophobicity (e.g., Suwannee River humic acid (SRHA)) revealed to significantly inhibit the photolysis of target micropollutants. The presence of Typha wetland NOM enhanced the indirect photolysis of well-known conservative micopollutants (carbamazepine and paraxanthine). And atenolol, carbamazepine, glimepiride, and N-acetyl-sulfamethoxazole were found to be sensitive to the triplet excited state of dissolved organic matter ((3)DOM(*)) with Typha wetland NOM under deoxygenated condition. This suggests that photolysis in constructed wetlands connected to the wastewater treatment plant can enhance the degradation of some anthropogenic micropollutants by the interaction with (3)DOM(*) in wetlands. PMID:24862465

  10. Optimal use of β-blockers in high-risk hypertension: A guide to dosing equivalence

    Directory of Open Access Journals (Sweden)

    Janet B McGill

    2010-05-01

    Full Text Available Janet B McGillDepartment of Medicine, Washington University School of Medicine, St. Louis, Missouri, USAAbstract: Hypertension is the number one diagnosis made by primary care physicians, placing them in a unique position to prescribe the antihypertensive agent best suited to the individual patient. In individuals with diabetes mellitus, blood pressure (BP levels > 130/80 mmHg confer an even higher risk for cardiovascular and renal disease, and these patients will benefit from aggressive antihypertensive treatment using a combination of agents. β‑blockers are playing an increasingly important role in the management of hypertension in high-risk patients. β‑blockers are a heterogeneous class of agents, and this review presents the differences between β‑blockers and provides evidence-based protocols to assist in understanding dose equivalence in the selection of an optimal regimen in patients with complex needs. The clinical benefits provided by β‑blockers are only effective if patients adhere to medication treatment long term. β‑blockers with proven efficacy, once-daily dosing, and lower side effect profiles may become instrumental in the treatment of hypertensive diabetic and nondiabetic patients.Keywords: antihypertensive, blood pressure, atenolol, carvedilol, labetalol, metoprolol, nebivolol

  11. Perindopril/indapamide combination in the first-line treatment of hypertension and end-organ protection.

    Science.gov (United States)

    Gosse, Philippe

    2006-05-01

    This article examines evidence-based findings in the literature on the efficacy of perindopril 2 mg/indapamide 0.625 mg, a first-line, low-dose antihypertensive drug combination. In regulatory Phase II and III trials, perindopril/indapamide significantly lowered blood pressure compared with other first-line therapies (atenolol, losartan and irbesartan). This was also the case in STRAtegies of Treatment in Hypertension: Evaluation, a postregistration study versus current monotherapies and stepped-care therapy with different classes of antihypertensive agents. The efficacy/safety ratio (both clinical and with regard to laboratory parameters) of perindopril/indapamide was good. Perindopril/indapamide provides additional antihypertensive efficacy compared with each component used alone and with current monotherapies, with major efficacy on systolic blood pressure, an important predictor of cardiovascular risk. It also reduces pulse pressure, an independent cardiovascular risk factor, large-vessel arterial stiffness and microcirculatory alterations. The fixed dosage of a once-daily tablet, ensures optimal ease of use and enhances patient compliance. Perindopril/indapamide also reduces target organ damage in patients at high cardiovascular risk, such as patients with cardiac hypertrophy and Type 2 diabetics with albuminuria. These benefits, together with the good efficacy/tolerability ratio, fulfill the requirements of the European Society of Hypertension and of the Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure guidelines for low-dose, first-line combination therapy in hypertension. PMID:16716093

  12. Fruit juice, organic anion transporting polypeptides, and drug interactions in psychiatry.

    Science.gov (United States)

    Andrade, Chittaranjan

    2014-11-01

    Organic anion transporting polypeptides (OATPs) are a group of membrane transport proteins that facilitate the influx of endogenous and exogenous substances across biological membranes. OATPs are found in enterocytes and hepatocytes and in brain, kidney, and other tissues. In enterocytes, OATPs facilitate the gastrointestinal absorption of certain orally administered drugs. Fruit juices such as grapefruit juice, orange juice, and apple juice contain substances that are OATP inhibitors. These fruit juices diminish the gastrointestinal absorption of certain antiallergen, antibiotic, antihypertensive, and β-blocker drugs. While there is no evidence, so far, that OATP inhibition affects the absorption of psychotropic medications, there is no room for complacency because the field is still nascent and because the necessary studies have not been conducted. Patients should therefore err on the side of caution, taking their medications at least 4 hours distant from fruit juice intake. Doing so is especially desirable with grapefruit juice, orange juice, and apple juice; with commercial fruit juices in which OATP-inhibiting substances are likely to be present in higher concentrations; with calcium-fortified fruit juices; and with medications such as atenolol and fexofenadine, the absorption of which is substantially diminished by concurrent fruit juice intake. PMID:25470100

  13. Screening determination of pharmaceutical pollutants in different water matrices using dual-channel capillary electrophoresis coupled with contactless conductivity detection.

    Science.gov (United States)

    Le, Minh Duc; Duong, Hong Anh; Nguyen, Manh Huy; Sáiz, Jorge; Pham, Hung Viet; Mai, Thanh Duc

    2016-11-01

    In this study, the employment of purpose-made dual-channel compact capillary electrophoresis (CE) instrument with capacitively coupled contactless conductivity detection (C(4)D) as a simple and inexpensive solution for screening determination of various pharmaceutical pollutants frequently occurring in surface water and hospital wastewater in Hanoi, Vietnam is reported. Five negatively charged pharmaceutically active compounds, namely ibuprofen, diclofenac, bezafibrate, ketoprofen and mefenamic acid were determined using the first channel whereas three positively charged ones, namely diphenhydramine, metoprolol and atenolol were determined with the second channel of the CE-C(4)D instrument. Two different background electrolytes (BGEs) were used in these two CE channels independently. The best detection limits achieved were in the range of 0.2-0.8mg/L without sample pre-concentration. Enrichment factors up to 200 were obtainable with the inclusion of a solid phase extraction step. Good agreement between results obtained from CE-C(4)D and those with the standard confirmation method (HPLC-DAD) was achieved, with correlation coefficients higher than 0.98. PMID:27591645

  14. Factores de riesgo para infarto agudo de miocardio y prescripción de medicamentos para prevención secundaria

    Directory of Open Access Journals (Sweden)

    Desirée Sáenz-Campos

    2005-01-01

    Full Text Available Objetivo: tipificar algunos factores de riesgo coronario presentes en los pacientes que sobreviven a un primer infarto agudo de miocardio (IAM y describir el tratamiento farmacológico prescrito para profilaxis secundaria al egreso hospitalario. Métodos: estudio observacional, transversal y descriptivo, con información extraída del expediente clínico de 50 pacientes atendidos en 3 hospitales nacionales. Resultados: 42 varones y 8 mujeres, edad 63 ± 15 años, peso 67 ± 12 kg, Índice de Masa Corporal= 26.1 ± 2.1 kg/m², 38% hipertensos, 22% diabéticos (n= 8 pacientes con diabetes + hipertensión y 34% fumadores. Colesterol total 191 ± 45.7 mg/dL, colesterol-LDL 112 ± 33.8 mg/dL y colesterol-HDL 39.4 ± 8.26 mg/dL. Todos egresaron con medicamentos: 92% con antitrombóticos (predominó aspirina, 92% con estatinas, 78% con betabloqueador (atenolol o carvedilol, 70% con enalapril o losartán y 48% con nitratos. Conclusiones: este estudio piloto mostró que la enfermedad coronaria tiende a manifestarse desde la etapa de adulto joven, persiste en su mayor afectación a los varones y parecen prevalecer los factores de riesgo coronario modificables. Los antitrombóticos, beta- bloqueadores y las estatinas más frecuentemente prescritos.

  15. ASCOT发现新降压药优于老药

    Institute of Scientific and Technical Information of China (English)

    徐欣(摘)

    2006-01-01

    ASCOT降低血压组的研究资料显示,与老的联合用药方案即β-阻滞剂和利尿剂(atenolol and bendroflumethiazide,阿替洛尔和苄氟噻嗪)相比,钙通道阻滞剂和ACE抑制剂(amlodipine and perindopril,氨氯地平和培哚普利)这种新的组合在其降压治疗中,能够预防更多心血管事件的发生,并引发更少的糖尿病。这项研究的全部数据发表在2005年9月于斯得哥尔摩召开的欧洲心脏病学会会议上,并刊登在2005年9月10日的《柳叶刀》杂志上。

  16. eNOS-dependent antisenscence effect of a calcium channel blocker in human endothelial cells.

    Directory of Open Access Journals (Sweden)

    Toshio Hayashi

    Full Text Available Senescence of vascular endothelial cells is an important contributor to the pathogenesis of age-associated vascular disorders such as atherosclerosis. We investigated the effects of antihypertensive agents on high glucose-induced cellular senescence in human umbilical venous endothelial cells (HUVECs. Exposure of HUVECs to high glucose (22 mM for 3 days increased senescence-associated- β-galactosidase (SA-β-gal activity, a senescence marker, and decreased telomerase activity, a replicative senescence marker. The calcium channel blocker nifedipine, but not the β1-adrenergic blocking agent atenolol or the angiotensin-converting enzyme inhibitor perindopril, reduced SA-β-gal positive cells and prevented a decrease in telomerase activity in a high-glucose environment. This beneficial effect of nifedipine was associated with reduced reactive oxygen species (ROS and increased endothelial nitric oxide synthase (eNOS activity. Thus, nifedipine prevented high glucose-induced ROS generation and increased basal eNOS phosphorylation level at Ser-1177. Treatment with N (G-nitro-L-arginine (L-NAME and transfection of small interfering RNA (siRNA targeting eNOS eliminated the anti-senscence effect of nifedipine. These results demonstrate that nifedipine can prevent endothelial cell senescence in an eNOS-dependent manner. The anti-senescence action of nifedipine may represent a novel mechanism by which it protects against atherosclerosis.

  17. Effect of adrenergic receptor ligands on metaiodobenzylguanidine uptake and storage in neuroblastoma cells

    Energy Technology Data Exchange (ETDEWEB)

    Babich, J.W. [Division of Nuclear Medicine, Department of Radiology, Massachusetts General Hospital, Boston, Massachusetts (United States)]|[Department of Radiology, Harvard Medical School, Boston, Massachusetts (United States); Graham, W. [Division of Nuclear Medicine, Department of Radiology, Massachusetts General Hospital, Boston, Massachusetts (United States); Fischman, A.J. [Division of Nuclear Medicine, Department of Radiology, Massachusetts General Hospital, Boston, Massachusetts (United States)]|[Department of Radiology, Harvard Medical School, Boston, Massachusetts (United States)

    1997-05-01

    The effects of adrenergic receptor ligands on uptake and storage of the radiopharmaceutical [{sup 125}I]metaiodobenzylguanidine (MIBG) were studied in the human neuroblastoma cell line SK-N-SH. For uptake studies, cells were with varying concentrations of {alpha}-agonist (clonidine, methoxamine, and xylazine), {alpha}-antagonist (phentolamine, tolazoline, phenoxybenzamine, yohimbine, and prazosin), {beta}-antagonist (propranolol, atenolol), {beta}-agonist (isoprenaline and salbutamol), mixed {alpha}/{beta} antagonist (labetalol), or the neuronal blocking agent guanethidine, prior to the addition of [{sup 125}I]MIBG (0.1 {mu}M). The incubation was continued for 2 h and specific cell-associated radioactivity was measured. For the storage studies, cells were incubated with [{sup 125}I]MIBG for 2 h, followed by replacement with fresh medium with or without drug (MIBG, clonidine, or yohimbine). Cell-associated radioactivity was measured at various times over the next 20 h. Propanolol reduced [{sup 125}I]MIBG uptake by approximately 30% (P<0.01) at all concentrations tested, most likely due to nonspecific membrane changes. In conclusion, the results of this study establish that selected adrenergic ligands can significantly influence the pattern of uptake and storage of MIBG in cultured neuroblastoma cells, most likely through inhibition of uptake or through noncompetitive inhibition. The potential inplications of these findings justify further study. (orig./VHE). With 4 figs., 1 tab.

  18. Impacts of compound properties and sediment characteristics on the sorption behaviour of pharmaceuticals in aquatic systems.

    Science.gov (United States)

    Al-Khazrajy, Omar S A; Boxall, Alistair B A

    2016-11-01

    Sorption is a key factor in determining the persistence, attenuation and bioavailability of sediment-associated contaminants. However, our understanding of the sorption behaviour of pharmaceuticals in sediments is poor. In this study, we investigated the sorption behaviour of a diverse set of pharmaceuticals in a range sediment types. Sorption affinity of pharmaceuticals for all sediments was found to increase in the order mefenamic acidlinear regression analysis was therefore used to develop new models for estimating sorption of individual pharmaceuticals based on sediment properties. The analyses indicated that sorption is related to properties such as Log Dow of a compound in the sediment (lipophilicity corrected for the sediment pH), cation exchange capacity, clay%, organic carbon content and exchangeable Ca(2+), although, with the exception of atenolol, robust relationships between sediment properties and sorption were not obtained. Overall, the results demonstrate how complex the processes are that drive the sorption of pharmaceuticals in sediments and highlight the need for generation of further experimental data and further model development work. PMID:27270139

  19. Calibration and field evaluation of polar organic chemical integrative sampler (POCIS) for monitoring pharmaceuticals in hospital wastewater

    International Nuclear Information System (INIS)

    The Polar Organic Chemical Integrative Sampler (POCIS) is a new tool for the sampling of organic pollutants in water. We tested this device for the monitoring of pharmaceuticals in hospital wastewater. After calibration, a field application was carried out in a French hospital for six pharmaceutical compounds (Atenolol, Prednisolone, Methylprednisolone, Sulfamethoxazole, Ofloxacin, Ketoprofen). POCIS were calibrated in tap water and wastewater in laboratory conditions close to relevant environmental conditions (temperature, flow velocity). Sampling rates (Rs) were determined and we observed a significant increase with flow velocity and temperature. Whatever the compound, the Rs value was lower in wastewater and the linear phase of uptake was shorter. POCIS were deployed in a hospital sewage pipe during four days and the estimated water concentrations were close to those obtained with twenty-four hour composite samples. -- Highlights: ► Calibration of POCIS for the monitoring of pharmaceuticals in hospital wastewater. ► Uptake profile presents a shorter linear phase in wastewater than in tap water. ► Influence of Rs values by temperature, flow velocity and bio-fouling. ► Correlation between concentrations estimated from POCIS or measured in TWA samples. ► Deployment period should be no longer than five days. -- After calibration in tap water and hospital wastewater, POCIS were used to monitor pharmaceuticals in hospital sewage and were compared to TWA sampling

  20. Charge-transfer complexes of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone with amino molecules in polar solvents

    Science.gov (United States)

    Berto, Silvia; Chiavazza, Enrico; Ribotta, Valentina; Daniele, Pier Giuseppe; Barolo, Claudia; Giacomino, Agnese; Vione, Davide; Malandrino, Mery

    2015-10-01

    The charge-transfer complexes have scientific relevance because this type of molecular interaction is at the basis of the activity of pharmacological compounds and because the absorption bands of the complexes can be used for the quantification of electron donor molecules. This work aims to assess the stability of the charge-transfer complexes between the electron acceptor 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and two drugs, procaine and atenolol, in acetonitrile and ethanol. The stability of DDQ in solution and the time required to obtain the maximum complex formation were evaluated. The stoichiometry and the stability of the complexes were determined, respectively, by Job's plot method and by the elaboration of UV-vis titrations data. The latter task was carried out by using the non-linear global analysis approach to determine the equilibrium constants. This approach to data elaboration allowed us to overcome the disadvantages of the classical linear-regression method, to obtain reliable values of the association constants and to calculate the entire spectra of the complexes. NMR spectra were recorded to identify the portion of the donor molecule that was involved in the interaction. The data support the participation of the aliphatic amino groups in complex formation and exclude the involvement of the aromatic amine present in the procaine molecule.

  1. Removal of beta-blockers from aqueous media by adsorption onto graphene oxide.

    Science.gov (United States)

    Kyzas, George Z; Koltsakidou, Anastasia; Nanaki, Stavroula G; Bikiaris, Dimitrios N; Lambropoulou, Dimitra A

    2015-12-15

    The aim of the present study is the evaluation of graphene oxide (GhO) as adsorbent material for the removal of beta-blockers (pharmaceutical compounds) in aqueous solutions. The composition and morphology of prepared materials were characterized by scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FT-IR). Atenolol (ATL) and propranolol (PRO) were used as model drug molecules and their behavior were investigated in terms of GhO dosage, contact time, temperature and pH. Adsorption mechanisms were proposed and the pH-effect curves after adsorption were discussed. The kinetic behavior of GhO-drugs system was analyzed after fitting to pseudo-first and -second order equations. The adsorption equilibrium data were fitted to Langmuir, Freundlich and Langmuir-Freundlich model calculating the maximum adsorption capacity (67 and 116 mg/g for PRO and ATL (25 °C), respectively). The temperature effect on adsorption was tested carrying out the equilibrium adsorption experiments at three different temperatures (25, 45, 65 °C). Then, the thermodynamic parameters of enthalpy, free energy and entropy were calculated. Finally, the desorption of drugs from GhO was evaluated by using both aqueous eluants (pH2-10) and organic solvents.

  2. Electrical conductivity and emerging contaminant as markers of surface freshwater contamination by wastewater.

    Science.gov (United States)

    de Sousa, Diana Nara Ribeiro; Mozeto, Antonio Aparecido; Carneiro, Renato Lajarim; Fadini, Pedro Sergio

    2014-06-15

    The use of chemical markers of undoubted anthropogenic sources for surface freshwater contamination by wastewaters was evaluated employing correlations observed between measured physico-chemical parameters as the electrical conductivity and the concentration of different emerging organic compounds. During the period from April/2011 to April/2012 spatial-temporal variations and contamination patterns of two rivers (Piraí and Jundiaí rivers), São Paulo state, Brazil were evaluated. Seven physico-chemical parameters and concentrations of different classes of emerging contaminants were determined in samples collected in seven field campaigns. The high linear correlation coefficients obtained for the compounds diclofenac (r=0.9085), propanolol (r=0.8994), ibuprofen (r=0.8720) and atenolol (r=0.7811) with electrical conductivity, also corroborated by principal component analysis (PCA), point to the potential use of these compounds as markers of investigated surface water contamination by wastewaters. Due to specific inputs, these environmental markers showed very good effectiveness for the identification and differentiation of water body contamination by discharges of treated and untreated urban sewage.

  3. Contaminants of emerging concern in municipal wastewater effluents and marine receiving water.

    Science.gov (United States)

    Vidal-Dorsch, Doris E; Bay, Steven M; Maruya, Keith; Snyder, Shane A; Trenholm, Rebecca A; Vanderford, Brett J

    2012-12-01

    The occurrence and concentrations of contaminants of emerging concern (CECs) were investigated in municipal effluents and in marine receiving water. Final effluent from four large publicly owned treatment works (POTWs) and seawater collected near the respective POTW outfall discharges and a reference station were collected quarterly over one year and analyzed for 56 CECs. Several CECs were detected in effluents; naproxen, gemfibrozil, atenolol, and tris(1-chloro-2-propyl)phosphate were the compounds most frequently found and with the highest concentrations (>1 µg/L). Gemfibrozil and naproxen had the highest seawater concentrations (0.0009 and 0.0007 µg/L) and also were among the most frequently detected compounds. Effluent dilution factors ranged from >400 to approximately 1,000. Fewer CECs were detected and at lower concentrations in seawater collected from the reference station than at the outfall sites. Effluent concentrations for some CECs (e.g., pharmaceuticals) were inversely related to the degree of wastewater treatment. This trend was not found in seawater samples. Few temporal differences were observed in effluent or seawater samples. Effluent CEC concentrations were lower than those currently known for chronic toxicity thresholds. Nevertheless, the evaluation of potential chronic effects for CECs is uncertain because aquatic life toxicity thresholds have been developed for only a few CECs, and the effluent and seawater samples had compounds, such as nonylphenol, known to bioaccumulate in local fish. Additional data are needed to better understand the significance of CEC presence and concentrations in marine environments. PMID:22987561

  4. Solar photocatalytic ozonation of a mixture of pharmaceutical compounds in water.

    Science.gov (United States)

    Márquez, Gracia; Rodríguez, Eva M; Beltrán, Fernando J; Álvarez, Pedro M

    2014-10-01

    Aqueous solutions of mixtures of four pharmaceutical compounds (atenolol, hydrochlorothiazide, ofloxacin and trimethoprim) both in Milli-Q ultrapure water and in a secondary effluent from a municipal wastewater treatment plant have been treated at pH 7 by different oxidation methods, such as conventional ozonation, photolytic ozonation, TiO2 catalytic ozonation, TiO2 photocatalytic oxidation and TiO2 photocatalytic ozonation. Experiments were carried out using a solar compound parabolic concentrator. The performance results have been compared in terms of removal of emerging contaminants (ECs), generation rate of phenolic intermediates, organic matter mineralization, ecotoxicity removal and enhancement of biodegradability. Also, the consumption of ozone to achieve certain treatment goals (95% removal of ECs and 40% mineralization) is discussed. Results reveal that solar photocatalytic ozonation is a promising oxidation method as it led to the best results in terms of EC mineralization (∼85%), toxicity removal (∼90%) and efficient use of ozone (∼2mgO3mgEC(-1) to achieve complete EC removal and ∼18mgO3mgTOC(-1) to achieve 40% EC mineralization, respectively). PMID:25065792

  5. Human and simulated intestinal fluids as solvent systems to explore food effects on intestinal solubility and permeability.

    Science.gov (United States)

    Stappaerts, Jef; Wuyts, Benjamin; Tack, Jan; Annaert, Pieter; Augustijns, Patrick

    2014-10-15

    The mixed micelles and vesicles present in the intraluminal environment of the postprandial state exhibit suitable solubilizing capacities for lipophilic drugs. This increase in solubility, however, is accompanied by a decrease in the free fraction caused by micellar entrapment of these lipophilic compounds. In this study, both simulated and aspirated human intestinal fluids of fasted and fed state conditions were used to evaluate the influence of food on the intestinal disposition of a series of structurally related β-blockers, with varying logP values. Using the in situ intestinal perfusion technique with mesenteric blood sampling in rats, it was demonstrated that fed state conditions significantly decreased the absorptive flux of the more lipophilic compounds metoprolol, propranolol and carvedilol, whereas the influence on the flux of the hydrophilic β-blocker atenolol was limited. The solubility of BCS class II compound carvedilol was found to increase significantly in simulated and aspirated media of the fed state. Intestinal perfusions using intestinal media saturated with carvedilol, revealed a higher flux in the fasted state compared to the fed state, despite the higher solubility in the fed state. This study underscores the importance of addressing the complex nature of the behavior of compounds in the intraluminal environment in fasted and fed state conditions. Moreover, our data point out the value of studying the effect of food on both solubility and permeability using biorelevant experimental conditions.

  6. Fatal Renal Failure in a Spinal Cord Injury Patient with Vesicoureteric Reflux Who Underwent Repeated Ureteric Reimplantations Unsuccessfully: Treatment Should Focus on Abolition of High Intravesical Pressures rather than Surgical Correction of Reflux

    Directory of Open Access Journals (Sweden)

    Subramanian Vaidyanathan

    2012-01-01

    Full Text Available A 29-year-old man developed paraplegia at T-10 level due to road traffic accident in 1972. Both kidneys were normal and showed good function on intravenous urography. Division of external urethral sphincter was performed in 1973. In 1974, cystogram showed retrograde filling of left renal tract, which was hydronephrotic. Left ureteric reimplantation was performed. Following surgery, cystogram revealed marked retrograde filling of left renal tract as before. Penile sheath drainage was continued. In 1981, intravenous urography revealed bilateral severe hydronephrosis. Left ureteric reimplantation was performed again in 1983. Blood pressure was 220/140 mm Hg; this patient was prescribed atenolol. Cystogram showed gross left vesicoureteral reflux. Intermittent catheterisation was commenced in 2001. In 2007, proteinuria was 860 mg/day. This patient developed progressive renal failure and expired in 2012. In a spinal cord injury patient with vesicoureteral reflux, the treatment should focus on abolition of high intravesical pressures rather than surgical correction of vesicoureteric reflux. Detrusor hyperactivity and high intravesical pressures are the basic causes for vesicoureteral reflux in spinal cord injury patients. Therefore, it is important to manage spinal cord injury patients with neuropathic bladder by intermittent catheterisations along with antimuscarinic drug therapy in order to abolish high detrusor pressures and prevent vesicoureteral reflux. Angiotensin-converting enzyme inhibitors or angiotensin-receptor-blocking agents should be prescribed even in the absence of hypertension when a spinal cord injury patient develops vesicoureteral reflux and proteinuria.

  7. Sucrose esters increase drug penetration, but do not inhibit p-glycoprotein in caco-2 intestinal epithelial cells.

    Science.gov (United States)

    Kiss, Lóránd; Hellinger, Éva; Pilbat, Ana-Maria; Kittel, Ágnes; Török, Zsolt; Füredi, András; Szakács, Gergely; Veszelka, Szilvia; Sipos, Péter; Ózsvári, Béla; Puskás, László G; Vastag, Monika; Szabó-Révész, Piroska; Deli, Mária A

    2014-10-01

    Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference absorption enhancers, Tween 80 and Cremophor RH40, were tested on Caco-2 cells. Caco-2 monolayers formed a good barrier as reflected by high transepithelial resistance and positive immunostaining for junctional proteins claudin-1, ZO-1, and β-catenin. Sucrose esters in nontoxic concentrations significantly reduced resistance and impedance, and increased permeability for atenolol, fluorescein, vinblastine, and rhodamine 123 in Caco-2 monolayers. No visible opening of the tight junctions was induced by sucrose esters assessed by immunohistochemistry and electron microscopy, but some alterations were seen in the structure of filamentous actin microfilaments. Sucrose esters fluidized the plasma membrane and enhanced the accumulation of efflux transporter ligands rhodamine 123 and calcein AM in epithelial cells, but did not inhibit the P-glycoprotein (P-gp)-mediated calcein AM accumulation in MES-SA/Dx5 cell line. These data indicate that in addition to their dissolution-increasing properties sucrose esters can enhance drug permeability through both the transcellular and paracellular routes without inhibiting P-gp.

  8. Occurrence of pharmaceuticals and UV filters in swimming pools and spas.

    Science.gov (United States)

    Ekowati, Yuli; Buttiglieri, Gianluigi; Ferrero, Giuliana; Valle-Sistac, Jennifer; Diaz-Cruz, M Silvía; Barceló, Damià; Petrovic, Mira; Villagrasa, Marta; Kennedy, Maria D; Rodríguez-Roda, Ignasi

    2016-07-01

    The occurrence of 32 pharmaceuticals and 14 UV filters in swimming pools and spas was studied. Fifty-one water samples were collected from 17 pools located in sport centres and hotels in Catalonia, Spain. The samples were analysed by liquid chromatography-tandem mass spectrometry. The pharmaceuticals atenolol, carbamazepine, hydrochlorothiazide, metronidazole, ofloxacin, sulfamethoxazole, acetaminophen, ibuprofen, ketoprofen and phenazone were measured in water samples at concentrations higher than their limit of quantification (LOQ). The highest concentration of any individual pharmaceutical was measured for the diuretic hydrochlorothiazide (904 ng/L). The most frequently detected pharmaceutical was carbamazepine, as it was observed in more than half of all the water samples measured (53 %, 27/51). The UV filters at concentrations higher than LOQ in water samples were BP1, BP2, BP3, BP8, THB, 4DHB, 4MBC, OD-PABA, 1HBT, MeBT and DMeBT. The highest concentration of UV filter observed was 4MBC (69.3 ng/L) while the most frequent UV filters in the samples were 1HBT (59 %, 30/51). The results also showed that pharmaceuticals and UV filters were most frequently found in spas. Finally, from a water treatment technology perspective, the lowest occurrence of pharmaceuticals was in the pools applying sand filters followed by disinfection by sodium hypochlorite, while the lowest occurrence of UV filters was in the pools applying coagulation, sand filtration, UV and salt electrolysis. PMID:27068900

  9. Myocardial infarction induced by oral terazosin in a patient with predisposing structural cardiomyopathy: case report

    Directory of Open Access Journals (Sweden)

    Alejandro Vidal Margenat

    2016-06-01

    Full Text Available Describimos el caso de un hombre de 71 años de edad, que presentó un infarto agudo de miocardio debido a la obstrucción dinámica del tracto de salida del ventrículo izquierdo inducida por la terazosina. Luego de recibir dicha medicación el paciente presentó un síncope y posteriormente angina de pecho. El electrocardiograma evidenció ondas Q y sobreelevación del segmento ST en las derivaciones precordiales e inferiores. La angiografía coronaria evidenció una oclusión crónica de la arteria descendente anterior y el ecocardiograma Doppler reveló aquinesia apical, segmentos basales hiperdinámicos, movimiento anterior sistólico de la válvula mitraI y obstrucción dinámica del tracto de salida del ventrículo izquierdo. La administración intravenosa de suero fisiológico y atenolol determinó una clara mejoría clínica. Un infarto agudo de miocardio hemodinámico fue el resultado de la caída de la presión de perfusión coronaria en un paciente con disminución crónica de la reserva coronaria.

  10. Comparison of in vitro cell models in predicting in vivo brain entry of drugs.

    Science.gov (United States)

    Hakkarainen, Jenni J; Jalkanen, Aaro J; Kääriäinen, Tiina M; Keski-Rahkonen, Pekka; Venäläinen, Tetta; Hokkanen, Juho; Mönkkönen, Jukka; Suhonen, Marjukka; Forsberg, Markus M

    2010-12-15

    Although several in vitro models have been reported to predict the ability of drug candidates to cross the blood-brain barrier, their real in vivo relevance has rarely been evaluated. The present study demonstrates the in vivo relevance of simple unidirectional permeability coefficient (P(app)) determined in three in vitro cell models (BBMEC, Caco-2 and MDCKII-MDR1) for nine model drugs (alprenolol, atenolol, metoprolol, pindolol, entacapone, tolcapone, baclofen, midazolam and ondansetron) by using dual probe microdialysis in the rat brain and blood as an in vivo measure. There was a clear correlation between the P(app) and the unbound brain/blood ratios determined by in vivo microdialysis (BBMEC r=0.99, Caco-2 r=0.91 and MDCKII-MDR1 r=0.85). Despite of the substantial differences in the absolute in vitro P(app) values and regardless of the method used (side-by-side vs. filter insert system), the capability of the in vitro models to rank order drugs was similar. By this approach, thus, the additional value offered by the true endothelial cell model (BBMEC) remains obscure. The present results also highlight the need of both in vitro as well as in vivo methods in characterization of blood-brain barrier passage of new drug candidates.

  11. Influence of a compost layer on the attenuation of 28 selected organic micropollutants under realistic soil aquifer treatment conditions: insights from a large scale column experiment.

    Science.gov (United States)

    Schaffer, Mario; Kröger, Kerrin Franziska; Nödler, Karsten; Ayora, Carlos; Carrera, Jesús; Hernández, Marta; Licha, Tobias

    2015-05-01

    Soil aquifer treatment is widely applied to improve the quality of treated wastewater in its reuse as alternative source of water. To gain a deeper understanding of the fate of thereby introduced organic micropollutants, the attenuation of 28 compounds was investigated in column experiments using two large scale column systems in duplicate. The influence of increasing proportions of solid organic matter (0.04% vs. 0.17%) and decreasing redox potentials (denitrification vs. iron reduction) was studied by introducing a layer of compost. Secondary effluent from a wastewater treatment plant was used as water matrix for simulating soil aquifer treatment. For neutral and anionic compounds, sorption generally increases with the compound hydrophobicity and the solid organic matter in the column system. Organic cations showed the highest attenuation. Among them, breakthroughs were only registered for the cationic beta-blockers atenolol and metoprolol. An enhanced degradation in the columns with organic infiltration layer was observed for the majority of the compounds, suggesting an improved degradation for higher levels of biodegradable dissolved organic carbon. Solely the degradation of sulfamethoxazole could clearly be attributed to redox effects (when reaching iron reducing conditions). The study provides valuable insights into the attenuation potential for a wide spectrum of organic micropollutants under realistic soil aquifer treatment conditions. Furthermore, the introduction of the compost layer generally showed positive effects on the removal of compounds preferentially degraded under reducing conditions and also increases the residence times in the soil aquifer treatment system via sorption. PMID:25723339

  12. Double-wavelength overlapping resonance Rayleigh scattering technique for the simultaneous quantitative analysis of three β-adrenergic blockade

    Science.gov (United States)

    Tan, Xuanping; Yang, Jidong; Li, Qin; Yang, Qiong; Shen, Yizhong

    2016-05-01

    Four simple and accurate spectrophotometric methods were proposed for the simultaneous determination of three β-adrenergic blockade, e.g. atenolol, metoprolol and propranolol. The methods were based on the reaction of the three drugs with erythrosine B (EB) in a Britton-Robinson buffer solution at pH 4.6. EB could combine with the drugs to form three ion-association complexes, which resulted in the resonance Rayleigh scattering (RRS) intensity that is enhanced significantly with new RRS peaks that appeared at 337 nm and 370 nm, respectively. In addition, the fluorescence intensity of EB was also quenched. The enhanced scattering intensities of the two peaks and the fluorescence quenched intensity of EB were proportional to the concentrations of the drugs, respectively. What is more, the RRS intensity overlapped with the double-wavelength of 337 nm and 370 nm (so short for DW-RRS) was also proportional to the drugs concentrations. So, a new method with highly sensitive for simultaneous determination of three bisoprolol drugs was established. Finally, the optimum reaction conditions, influencing factors and spectral enhanced mechanism were investigated. The new DW-RRS method has been applied to simultaneously detect the three β-blockers in fresh serum with satisfactory results.

  13. Comprehensive evaluation of pharmaceuticals and personal care products (PPCPs) in typical highly urbanized regions across China

    International Nuclear Information System (INIS)

    This study evaluated the occurrence of 36 PPCPs in urban river water samples collected from Beijing, Changzhou and Shenzhen. Twenty-eight compounds were detected. Compounds found with highest median concentrations included: sulfadimethoxine (164 ng/L), sulpiride (77.3 ng/L), atenolol (52.9 ng/L), and indomethacin (50.9 ng/L). Antibiotic was the predominant class detected and contributed about half of the overall PPCPs contamination level. Effluents from wastewater treatment plants (WWTPs) were demonstrated to be the predominant pathways through which PPCPs entering into aquatic environment in all investigated areas. The ratio of persistent PPCPs like sulpiride and carbamazepine was identified to be feasible in tracing their contamination sources in rivers. Concentrations of most detected PPCPs showed significant positive correlations with total nitrogen and total phosphorus. Two groups of representative PPCPs were selected as the chemical indicators for predicting the overall PPCPs contamination, based on the significant correlations between PPCPs. - Highlights: • PPCPs were detected at high detection frequencies and average concentrations. • Antibiotics contributed about half of the overall PPCPs contamination level. • Wastewater treatment plant effluent was the dominant contributor to PPCPs residue. • Ratio of two persistent compounds was used in tracing contamination sources. • Two groups of representative PPCPs were selected as surrogate of overall PPCPs. - The occurrence, spatial distribution, sources, and surrogate of Pharmaceuticals and personal care products in aquatic environment of three typical cities across China were demonstrated

  14. Gateways to clinical trials.

    Science.gov (United States)

    Bayes, M; Rabasseda, X; Prous, J R

    2002-01-01

    Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses, which has been retrieved from the Clinical Studies knowledge area of Prous Science Integrity, the world's first drug discovery and development portal, providing information on study design, treatments, conclusions and references. This issue focuses on the following selection of drugs: Abacavir sulfate; abciximab; abetimus sodium; adalimumab; aldesleukin; almotriptan; alteplase; amisulpride; amitriptyline hydrochloride; amoxicillin trihydrate; atenolol; atorvastatin calcium; atrasentan; Beclometasone dipropionate; bosentan; Captopril; ceftriaxone sodium; cerivastatin sodium; cetirizine hydrochloride; cisplatin; citalopram hydrobromide; Dalteparin sodium; darusentan; desirudin; digoxin; Efalizumab; enoxaparin sodium; ertapenem sodium; esomeprazole magnesium; estradiol; ezetimibe; Famotidine; farglitazar; fluorouracil; fluticasone propionate; fosamprenavir sodium; Glibenclamide; glucosamine sulfate; Heparin sodium; HSPPC-96; hydrochlorothiazide; Imatinib mesilate; implitapide; Lamivudine; lansoprazole; lisinopril; losartan potassium; l-Propionylcarnitine; Melagatran; metformin hydrochloride; methotrexate; methylsulfinylwarfarin; Nateglinide; norethisterone; Olmesartan medoxomil; omalizumab; omapatrilat; omeprazole; oseltamivir phosphate; oxatomide; Pantoprazole; piperacillin sodium; pravastatin sodium; Quetiapine hydrochloride; Rabeprazole sodium; raloxifene hydrochloride; ramosetron hydrochloride; ranolazine; rasburicase; reboxetine mesilate; recombinant somatropin; repaglinide; reteplase; rosiglitazone; rosiglitazone maleate; rosuvastatin calcium; Sertraline; simvastatin; sumatriptan succinate; Tazobactam sodium; tenecteplase; tibolone; tinidazole; tolterodine tartrate; troglitazone; Uniprost; Warfarin sodium; Ximelagatran. PMID:11980386

  15. Removal and seasonal variability of selected analgesics/anti-inflammatory, anti-hypertensive/cardiovascular pharmaceuticals and UV filters in wastewater treatment plant.

    Science.gov (United States)

    Golovko, Oksana; Kumar, Vimal; Fedorova, Ganna; Randak, Tomas; Grabic, Roman

    2014-06-01

    Seasonal removal efficiency of 16 pharmaceuticals and personal care products was monitored in a wastewater treatment plant in České Budějovice, Czech Republic, over a period of 1 year (total amount of samples, n = 272). The studied compounds included four UV filters, three analgesics/anti-inflammatory drugs and nine anti-hypertensive/cardiovascular drugs. In most cases, elimination of the substances was incomplete, and overall removal rates varied strongly from -38 to 100%. Therefore, it was difficult to establish a general trend for each therapeutic group. Based on the removal efficiencies (REs) over the year, three groups of target compounds were observed. A few compounds (benzophenon-1, valsartan, isradipine and furosemide) were not fully removed, but their REs were greater than 50%. The second group of analytes, consisting of 2-phenylbenzimidazole-5-sulfonic acid, tramadol, sotalol, metoprolol, atenolol and diclofenac, showed a very low RE (lower than 50%). The third group of compounds showed extremely variable RE (benzophenon-3 and benzophenon-4, codeine, verapamil, diltiazem and bisoprolol). There were significant seasonal trends in the observed REs, with reduced efficiencies in colder months.

  16. Simple determination of terbutaline in dog plasma by column-switching liquid chromatography.

    Science.gov (United States)

    Zhang, Y; Zhang, Z R

    2004-06-15

    Terbutaline is a beta-adrenergic receptor antagonist that acts as a bronchodilator in the treatment of asthma and chronic bronchitis. In the present work, a column-switching high-performance liquid chromatographic method was developed to monitor terbutaline sulphate in dog plasma. The system consists of a C2 pre-column (PC) and a C18 analytical column connected in series via a switching valve. Atenolol was used as the internal standard. Good linearity was achieved in the range of 5-800 ng/ml plasma. The mean intra- and inter-assay variation coefficients for this analysis were 2.3 and 4.7%, respectively. The average recovery for terbutaline was 87.4% from plasma. The mean concentration after three freeze-thaw cycles was 99.4% of the normal value. The analytical sensitivity and accuracy of this assay is adequate for characterisation of the pharmacokinetics of oral administration of terbutaline to dogs and has been successfully used to provide pharmacokinetic data using pulsatile and immediate-release tablets. PMID:15135092

  17. A validated stability-indicating RP-LC method for the simultaneous determination of amlodipine and perindopril in tablet dosage form and their stress degradation behavior under ICH-recommended stress conditions.

    Science.gov (United States)

    Gumustas, Mehmet; Ozkan, Sibel A

    2013-01-01

    A stability-indicating RP-LC assay method was developed for the simultaneous determination of the cardiovascular drugs amlodipine and perindopril in the presence of degradation products generated from forced decomposition studies. The developed method is applicable for the determination of related substances in bulk drugs and simultaneous assay in a tablet pharmaceutical dosage form. Separation of the drugs and their degradation products was obtained using an RP Waters Spherisorb ODS1 column (250 x 4.6 mm id, 5 pm particle size) with the mobile phase acetonitrile-water (30 + 70, v/v) containing 15 mM phosphoric acid. The pH of the mobile phase was adjusted to 5.0. A flow rate of 1.2 mL/min was used for the separations, with detection at 215 nm. The chromatographic separation was performed at a column temperature of 45 degrees C. Atenolol was chosen as the internal standard. Amlodipine and perindopril were exposed to thermal, photolytic, hydrolytic, and oxidative stress conditions, and the stressed samples were analyzed by the proposed method. Degradation studies showed that both compounds were degraded under these stress conditions. The method was found to be stability-indicating and can be used for the routine analysis of amlodipine and perindopril in the studied combined tablet dosage form. PMID:24000747

  18. [Drug-induced exacerbation of hypoaldosteronism in autoimmune polyglandular syndrome type 2].

    Science.gov (United States)

    Krysiak, Robert; Okopień, Bogusław

    2012-01-01

    Hypoaldosteronism is a clinical condition resulting from inadequate stimulation of aIdosterone secretion (hyporeninemic hypoaIdosteronism), defects in adrenal synthesis of aldosterone (hyperreninemic hypoaldosteronism), or resistance to the peripheral action of this hormone (pseudohypoaldosteronism). The disease is characterized by a wide spectrum of clinical manifestations, ranging from asymptomatic hyperkalemia to life-threatening volume depletion, and, if unrecognized and untreated, it increases morbidity and mortality rates. In this paper, we report a case of a woman diagnosed with autoimmune polyglandular syndrome type 2. As a consequence of adrenal cortex destruction, the patient developed subclinical hypoaldosteronism which was effectively treated with small doses of fludrocortisone. Two and fours years later, she required ibuprofen and atenolol treatment and each of these treatments was accompanied by a transient deterioration in mineralocorticoid activity which resolved after drug withdrawal. This case shows for the first time that drugs reducing plasma renin activity may unmask subclinical hypoaldosteronism in subjects with autoimmune polyglandular syndromes, and that they should be avoided in patients with even small disturbances in the hormonal function of the zona glomerulosa.

  19. Liddle′s syndrome: A case report

    Directory of Open Access Journals (Sweden)

    Pranav Patel

    2015-01-01

    Full Text Available Liddle′s syndrome or pseudoaldosteronism is a rare autosomal dominant disease mimicking primary hyperaldosteronism, characterized by early-onset hypertension, hypokalemia and hypoaldosteronism, caused by excessive salt and water reabsorption in the distal nephron. As of 2008, there are <30 pedigrees or isolated cases that have been reported worldwide. We present an isolated case of a Liddle′s syndrome in a 48-year-old female. A 48-year-old female presented to the clinic with palpitation and a three to four-year history of low potassium level and hypertension. She was initially treated with a high potassium diet and potassium supplements. Her cardiac work-up including echocardiography, stress test and Holter monitoring were all negative. After a few months, she was admitted to the hospital with an acute hypertensive episode and hypokalemia. On evaluation, she was found to have low renin and aldosterone levels. Liddle′s syndrome was considered with the clinical picture of hypokalemia, hypertension and low renin/ aldosterone level. The patient was successfully treated with a high potassium diet, triamterene and atenolol. Liddle′s syndrome should be considered as the differential diagnosis in patients presenting with the clinical picture of hypokalemia, hypertension and low renin/aldosterone level.

  20. Toxicity of β-adrenergic receptor blockers to Daphnia (Daphnia magna)%β-受体阻断药物对大型蚤的毒性研究

    Institute of Scientific and Technical Information of China (English)

    施嘉琛; 尚楠; 张晶; 邵兵

    2011-01-01

    Objective To investigate the toxicity of 5 p-adrenergic receptor blockerg (bisoprolol, propranolol, sotalol, atenolol and metoprolol) to crustacean Daphnia magna. Methods The ECM of five f3-adrenergic receptor blockerg were evaluated on the 48 h toxicity experiments according to the standard protocol established by OECD. The two strongest toxic blockers were chosen to study the 21 day toxicity to physiological change of daphnia. Results The ECM of five p-adrenergic receptor blockers were 6-169 mg/L. The toxicities (48 h ECW value, mg/L) in decreasing order were propranolol, bisoprolol, sotalol, atenolol and metoprolol. The 21 day toxicity study showed both propranolol and bisoprolol owning toxic effects to daphnia. The physiological change include the delay of first pregnancy and first brood, decrease of the number of broods per female and shorten of body length. Conclusion Since the p-adrenergic receptor blockers were toxicity to Daphnia magna which was a commonly used test animal in aquatic toxicology, the management of these medicines should be concern on the ecotoxicology.%目的 研究五种常用β-受体阻断药物(比索洛尔、普萘洛尔、索他洛尔、阿替洛尔和美托洛尔)对大型蚤(Daphnia magna)的毒理学效应.方法 根据OECD操作规程,开展5种目标药物对大型蚤的48 h毒性实验,获得各药物的半数抑制浓度EC50.再对48 h毒性效应较强的两种药物开展21d毒性实验,考察相关生理学指标的变化.结果5种药物的48 h半数抑制浓度EC50为6~169 mg/L.其毒性顺序为普萘洛尔>比索洛尔>索他洛尔>阿替洛尔>美托洛尔.普萘洛尔和比索洛尔的21d毒性试验结果表明两种药物对大型蚤的生理指标均存在毒理学效应,包括怀卵和产蚤时间延迟、产蚤数减少及体长缩短等.结论 β-受体阻断药物对大型蚤(Daphnia magna)存在毒理学效应,加强该类药物的使用和管理具有现实的生态毒理学意义.

  1. Effect of Phenylephrine on Alveolar Fluid Clearance in Ventilator-induced Lung Injury

    Institute of Scientific and Technical Information of China (English)

    Nai-jing Li; Xiu Gu; Wei Li; Yan Li; Sheng-qi Li; Ping He

    2013-01-01

    Objective To investigate the effect of phenylephrine (an α-adrenergic agonist) on alveolar fluid clearance (AFC) in ventilator-induced lung injury and the possible mechanism involved. Methods A total of 170 male Wistar rats were randomly allocated into 17 groups (n=10) using ran-dom number tables. Short-term (40 minutes) mechanical ventilation with high tidal volume (HVT) was per-formed to induce lung injury,impair active Na+ transport and lung liquid clearance in the rats. Unventilated rats served as controls. To demonstrate the effect of phenylephrine on AFC,phenylephrine at different con-centrations (1×10-5,1×10-6,1×10-7,1×10-8,and 1×10-9 mol/L) was injected into the alveolar space of the HVT ventilated rats. To identify the influence of adrenergic antagonists,Na+ channel,and microtubular sys-tem on the effect of phenylephrine,phenylephrine at 1×10-5 mol/L combined with prazosin (an α1-adrener-gic antagonist,1×10-4 mol/L),yohimbine (an α2-adrenergic antagonist,1×10-4 mol/L),atenolol (a β1-adrenergic antagonist,1×10-5 mol/L),ICI-118551 (an β2-adrenergic antagonist,1×10-5 mol/L),amiloride (a Na+ channel blocker,5×10-4 mol/L),ouabain (a Na+/K+-ATPase blocker,5×10-4 mol/L),colchicine (a mi-crotubular disrupting agent,0.25 mg/100 g body weight),or β-lumicolchicine (an isomer of colchicine,0.25 mg/100 g body weight) were perfused into the alveolar space of the rats ventilated with HVT for 40 minutes. AFC and total lung water content were measured. Results Basal AFC in control rats was (17.47±2.56)%/hour,which decreased to (9.64± 1.32)%/hour in HVT ventilated rats (P=0.003). The perfusion of phenylephrine at 1×10-8,1×10-7,1×10-6,and 1×10-5 mol/L significantly increased the AFC in HVT ventilated rats (all P<0.05). This effect of phenylephrine on AFC was suppressed by prazosin,atenolol,and ICI-118551 in HVT ventilated rats by 53%,31%,and 37%,respectively (all P<0.05). The AFC-stimulating effect of phenylephrine was lowered by 33% and 42% with

  2. O tratamento farmacológico da fobia social Pharmacologic treatment of social phobia

    Directory of Open Access Journals (Sweden)

    Antonio Egidio Nardi

    1999-12-01

    Full Text Available A fobia social é o medo acentuado e persistente de comer, beber, tremer, enrubescer, falar, escrever, enfim, de agir de forma ridícula ou inadequada na presença de outras pessoas. A fobia social apresenta-se em dois tipos básicos: a circunscrita, restrita a apenas um tipo de situação social, e a generalizada, caracterizada pelo temor a todas ou quase todas situações sociais. As características clínicas da fobia social são a ansiedade antecipatória, os sintomas físicos, a esquiva e a baixa auto-estima. Conforme o rigor diagnóstico, estima-se que 5% a 13% da população geral apresentem sintomas fóbicos sociais que resultem em diferentes graus de incapacitação e limitações sociais e ocupacionais. O tratamento médico de escolha é o uso de medicamentos associados à psicoterapia cognitivo-comportamental. Beta-bloqueadores (atenolol, propranolol, antidepressivos inibidores da monoamino oxidase (IMAO (fenelzine, tanilcipromina, inibidores reversíveis da monoamino oxidase tipo-A (RIMA (moclobemida, brofaromina, benzodiazepínicos (clonazepam, bromazepam, alprazolam e antidepressivos inibidores seletivos de serotonina (ISRS (paroxetina, sertralina, fluoxetina e fluvoxamina e alguns outros (venlafaxina, nefazodone, gabapentina, clonidina têm demonstrado eficácia em inúmeros estudos com diferentes metodologias. Os antidepressivos tricíclicos (imipramina, clomipramina, o ácido valproico e a buspirona têm apresentado resultados negativos. A paroxetina é o medicamento mais estudado com metodologia duplo-cega, com melhores resultados e com boa tolerância. Atualmente, os indivíduos que têm sua vida prejudicada pela fobia social podem, com o tratamento eficaz, adquirir uma postura mais segura em situações sociais.Social phobia is a marked and persistent fear of eating, drinking, trembling, blushing, speaking, writing or doing almost everything in front of people due to concerns about embarrassment or being scrutinized by others

  3. Conhecimento popular e utilização dos medicamentos genéricos na população do município de Tubarão, SC General awareness and use of generic medication among citizens of Tubarão, state of Santa Catarina, Brazil

    Directory of Open Access Journals (Sweden)

    Carine Raquel Blatt

    2012-01-01

    Full Text Available Embora os genéricos tenham sido introduzidos no país para oferecer alternativa mais acessível aos medicamentos de referência, representam apenas 14% das vendas em unidades no conjunto do mercado farmacêutico. O objetivo deste trabalho foi pesquisar o nível de conhecimento e o grau de utilização de genéricos em residentes do município de Tubarão, SC. Para isso, realizou-se um estudo transversal com uma amostra de 234 entrevistados, estratificada por bairro. Quanto ao grau de utilização, a maioria dos entrevistados já havia utilizado genéricos, e metade possuía pelo menos um exemplar dessa opção em casa. Para verificar o conhecimento sobre os diferentes tipos de medicamentos, realizou-se um teste de identificação de figuras de embalagens representativas das versões genérico, de referência e similar do paracetamol e do atenolol, 91,0% dos sujeitos identificaram corretamente todas as figuras. Ser de classe econômica mais elevada, já ter utilizado medicamento genérico, acreditar que o genérico tem o mesmo efeito que o medicamento de referência, encontrar medicamentos genéricos nas farmácias com facilidade e costumar comprar o genérico foram fatores associados positivamente com a identificação correta.Although generic medication has been introduced in the country to offer an accessible alternative to brand-name medication, it represents only 14% of sales in number of units within the pharmaceutical market. The aim of this work was to research the level of awareness and the use of generic products among residents of the municipality of Tubarão, State of Santa Catarina, Brazil. A transversal study was carried out with a sample of 234 interviewees, distributed among municipal areas. With regard to use, the majority of those interviewed had used generic medication, and half of them had at least one such product in their home. To verify awareness of different types of medication, pictures with the generic, brand name and

  4. Assessment of prescribing information for generic drugs manufactured in the Middle East and marketed in Saudi Arabia

    International Nuclear Information System (INIS)

    Little research has assessed the quality of manufacturer provided prescribing information or documented difference in key aspects of drug information among different marketed generic products of the same drug particularly in Middle East and Arabian Gulf. We assessed the quality of written prescribing information for selected generic drugs marketed in Saudi Arabia and manufactured in various countries of Middle East. We assessed the correctness and completeness of information pertaining to indications, dosage cautions/contraindications, side effects and drug interactions in 37 packages inserts for generic products registered in Saudi Arabia and manufactured in the Middle East, including atenolol (6 inserts), fluoxetine (4 inserts), ciprofloxacin (11 inserts), melformin (7 inserts) and omeprazole (9 inserts). We also described deficiencies in quality and quantity of manufacturers provided information that could be misleading to patients and prescribes. We found substantial disagreement in information between generic packages inserts versus the British National Formulary and the package insert of the brand product marketed in Saudi Arabia. A cumulative average of 63.16% of drug information indicators were in agreement with these standard references. Section headings with the least conformity with study references were those related to dosage (57, 28%) and side effects (54+-30%). Our results indicate that national authorities should implement appropriate measures aimed at removing misleading and incorrect information in generic package inserts and incorporating crucial prescribing information that is missing. National authorities in the Middle East and Arabian Gulf should strengthen collaboration and information interchange among each other and with international agencies to maintain common quality standards for delivering information through package inserts. (author)

  5. Heterozygous disruption of activin receptor-like kinase 1 is associated with increased arterial pressure in mice

    Directory of Open Access Journals (Sweden)

    María González-Núñez

    2015-11-01

    Full Text Available The activin receptor-like kinase 1 (ALK-1 is a type I cell-surface receptor for the transforming growth factor-β (TGF-β family of proteins. Hypertension is related to TGF-β1, because increased TGF-β1 expression is correlated with an elevation in arterial pressure (AP and TGF-β expression is upregulated by the renin-angiotensin-aldosterone system. The purpose of this study was to assess the role of ALK-1 in regulation of AP using Alk1 haploinsufficient mice (Alk1+/−. We observed that systolic and diastolic AP were significantly higher in Alk1+/− than in Alk1+/+ mice, and all functional and structural cardiac parameters (echocardiography and electrocardiography were similar in both groups. Alk1+/− mice showed alterations in the circadian rhythm of AP, with higher AP than Alk1+/+ mice during most of the light period. Higher AP in Alk1+/− mice is not a result of a reduction in the NO-dependent vasodilator response or of overactivation of the peripheral renin-angiotensin system. However, intracerebroventricular administration of losartan had a hypotensive effect in Alk1+/− and not in Alk1+/+ mice. Alk1+/− mice showed a greater hypotensive response to the β-adrenergic antagonist atenolol and higher concentrations of epinephrine and norepinephrine in plasma than Alk1+/+ mice. The number of brain cholinergic neurons in the anterior basal forebrain was reduced in Alk1+/− mice. Thus, we concluded that the ALK-1 receptor is involved in the control of AP, and the high AP of Alk1+/− mice is explained mainly by the sympathetic overactivation shown by these animals, which is probably related to the decreased number of cholinergic neurons.

  6. Electrical stimulation of the aortic depressor nerve in conscious rats overcomes the attenuation of the baroreflex in chronic heart failure.

    Science.gov (United States)

    Pinto, Tomás O C Teixeira; Lataro, Renata M; Castania, Jaci A; Durand, Marina T; Silva, Carlos A A; Patel, Kaushik P; Fazan, Rubens; Salgado, Helio C

    2016-04-01

    Chronic heart failure (CHF) is characterized by autonomic dysfunction combined with baroreflex attenuation. The hypotensive and bradycardic responses produced by electrical stimulation of the aortic depressor nerve (ADN) were examined in conscious CHF and control male Wistar rats (12-13 wk old). Furthermore, the role of parasympathetic and sympathetic nervous system in mediating the cardiovascular responses to baroreflex activation was evaluated by selective β1-adrenergic and muscarinic receptor antagonists. CHF was induced by myocardial infarction. After 6 wk, the subjects were implanted with electrodes for ADN stimulation. Twenty-four hours later, electrical stimulation of the ADN was applied for 20 s using five different frequencies (5, 15, 30, 60, and 90 Hz), while the arterial pressure was recorded by a catheter implanted into the femoral artery. Electrical stimulation of the ADN elicited progressive and similar hypotensive and bradycardic responses in control (n= 12) and CHF (n= 11) rats, while the hypotensive response was not affected by methylatropine. Nevertheless, the reflex bradycardia was attenuated by methylatropine in control, but not in CHF rats. Atenolol did not affect the hypotensive or bradycardic response in either group. The ADN function was examined under anesthesia through electroneurographic recordings. The arterial pressure-ADN activity relationship was attenuated in CHF rats. In conclusion, despite the attenuation of baroreceptor function in CHF rats, the electrical stimulation of the ADN elicited a stimulus-dependent hypotension and bradycardia of similar magnitude as observed in control rats. Therefore, electrical activation of the aortic baroreflex overcomes both the attenuation of parasympathetic function and the sympathetic overdrive. PMID:26843582

  7. The role of the anaesthetised guinea-pig in the preclinical cardiac safety evaluation of drug candidate compounds

    International Nuclear Information System (INIS)

    Despite rigorous preclinical and clinical safety evaluation, adverse cardiac effects remain a leading cause of drug attrition and post-approval drug withdrawal. A number of cardiovascular screens exist within preclinical development. These screens do not, however, provide a thorough cardiac liability profile and, in many cases, are not preventing the progression of high risk compounds. We evaluated the suitability of the anaesthetised guinea-pig for the assessment of drug-induced changes in cardiovascular parameters. Sodium pentobarbitone anaesthetised male guinea-pigs received three 15 minute intravenous infusions of ascending doses of amoxicillin, atenolol, clonidine, dobutamine, dofetilide, flecainide, isoprenaline, levosimendan, milrinone, moxifloxacin, nifedipine, paracetamol, verapamil or vehicle, followed by a 30 minute washout. Dose levels were targeted to cover clinical exposure and above, with plasma samples obtained to evaluate effect/exposure relationships. Arterial blood pressure, heart rate, contractility function (left ventricular dP/dtmax and QA interval) and lead II electrocardiogram were recorded throughout. In general, the expected reference compound induced effects on haemodynamic, contractility and electrocardiographic parameters were detected confirming that all three endpoints can be measured accurately and simultaneously in one small animal. Plasma exposures obtained were within, or close to the expected clinical range of therapeutic plasma levels. Concentration–effect curves were produced which allowed a more complete understanding of the margins for effects at different plasma exposures. This single in vivo screen provides a significant amount of information pertaining to the cardiovascular risk of drug candidates, ultimately strengthening strategies addressing cardiovascular-mediated compound attrition and drug withdrawal. -- Highlights: ► Evaluation of the anaesthetised guinea-pig to determine cardiac liability. ► Haemodynamic

  8. Comparison of contaminants of emerging concern removal, discharge, and water quality hazards among centralized and on-site wastewater treatment system effluents receiving common wastewater influent.

    Science.gov (United States)

    Du, Bowen; Price, Amy E; Scott, W Casan; Kristofco, Lauren A; Ramirez, Alejandro J; Chambliss, C Kevin; Yelderman, Joe C; Brooks, Bryan W

    2014-01-01

    A comparative understanding of effluent quality of decentralized on-site wastewater treatment systems, particularly for contaminants of emerging concern (CECs), remains less understood than effluent quality from centralized municipal wastewater treatment plants. Using a novel experimental facility with common influent wastewater, effluent water quality from a decentralized advanced aerobic treatment system (ATS) and a typical septic treatment system (STS) coupled to a subsurface flow constructed wetland (WET) were compared to effluent from a centralized municipal treatment plant (MTP). The STS did not include soil treatment, which may represent a system not functioning properly. Occurrence and discharge of a range of CECs were examined using isotope dilution liquid chromatography-tandem mass spectrometry during fall and winter seasons. Conventional parameters, including total suspended solids, carbonaceous biochemical oxygen demand and nutrients were also evaluated from each treatment system. Water quality of these effluents was further examined using a therapeutic hazard modeling approach. Of 19 CECs targeted for study, the benzodiazepine pharmaceutical diazepam was the only CEC not detected in all wastewater influent and effluent samples over two sampling seasons. Diphenhydramine, codeine, diltiazem, atenolol, and diclofenac exhibited significant (ptreatment systems was generally not influenced by season. However, significant differences (pwater quality indicators were observed among the various treatment technologies. For example, removal of most CECs by ATS was generally comparable to MTP. Lowest removal of most CECs was observed for STS; however, removal was improved when coupling the STS to a WET. Across the treatment systems examined, the majority of pharmaceuticals observed in on-site and municipal effluent discharges were predicted to potentially present therapeutic hazards to fish.

  9. Does low-frequency variability of heart period reflect a specific parasympathetic mechanism?

    Science.gov (United States)

    Grasso, R; Schena, F; Gulli, G; Cevese, A

    1997-03-19

    Low frequency (LF, approximately 0.1 Hz) spontaneous oscillations of heart period in humans have been attributed to and correlated with the sympathetic efferent control of the heart. However, this interpretation is controversial, because sympathetic blockade does not suppress these oscillations, while parasympathetic blockade strongly affects them. The sympathetic origin of LF of arterial pressure, on the contrary, has been convincingly demonstrated. Four 10 min cycle-by-cycle time series of R-R interval (RR), and systolic (SAP) and diastolic (DAP) arterial pressure were produced by automatic analysis of data obtained with non-invasive methods in 10 healthy humans during supine rest and while standing, both before and after beta 1-selective blockade (atenolol). Time series were analysed by autoregressive transfer function analysis. beta-blockade failed to induce systematic changes on the power of the LF peak of RR, in any condition. The coherence between RR and SAP in the same region remained high (0.77 +/- 0.03) and a constantly negative phase (approximately 50-60 degrees, corresponding to a delay of 1-2 heart beats of RR on SAP) was always seen. beta-blockade decreased the power of the LF peak of SAP, increased the transfer function gain between SAP and RR at LF, and the HF power of RR. We conclude that LF oscillations of RR are not directly generated by the sympathetic drive to the heart but reflect mainly the parasympathetic activity. The results suggest that the LF oscillations of the vagal outflow, and of RR, are generated by the baroreceptor reflex, driven by sympathetically-induced blood pressure LF waves. PMID:9089536

  10. Electrical stimulation of the aortic depressor nerve in conscious rats overcomes the attenuation of the baroreflex in chronic heart failure.

    Science.gov (United States)

    Pinto, Tomás O C Teixeira; Lataro, Renata M; Castania, Jaci A; Durand, Marina T; Silva, Carlos A A; Patel, Kaushik P; Fazan, Rubens; Salgado, Helio C

    2016-04-01

    Chronic heart failure (CHF) is characterized by autonomic dysfunction combined with baroreflex attenuation. The hypotensive and bradycardic responses produced by electrical stimulation of the aortic depressor nerve (ADN) were examined in conscious CHF and control male Wistar rats (12-13 wk old). Furthermore, the role of parasympathetic and sympathetic nervous system in mediating the cardiovascular responses to baroreflex activation was evaluated by selective β1-adrenergic and muscarinic receptor antagonists. CHF was induced by myocardial infarction. After 6 wk, the subjects were implanted with electrodes for ADN stimulation. Twenty-four hours later, electrical stimulation of the ADN was applied for 20 s using five different frequencies (5, 15, 30, 60, and 90 Hz), while the arterial pressure was recorded by a catheter implanted into the femoral artery. Electrical stimulation of the ADN elicited progressive and similar hypotensive and bradycardic responses in control (n = 12) and CHF (n = 11) rats, while the hypotensive response was not affected by methylatropine. Nevertheless, the reflex bradycardia was attenuated by methylatropine in control, but not in CHF rats. Atenolol did not affect the hypotensive or bradycardic response in either group. The ADN function was examined under anesthesia through electroneurographic recordings. The arterial pressure-ADN activity relationship was attenuated in CHF rats. In conclusion, despite the attenuation of baroreceptor function in CHF rats, the electrical stimulation of the ADN elicited a stimulus-dependent hypotension and bradycardia of similar magnitude as observed in control rats. Therefore, electrical activation of the aortic baroreflex overcomes both the attenuation of parasympathetic function and the sympathetic overdrive.

  11. ANTIHYPERTENSIVE MEDICATION PRESCRIBING PATTERNS IN A UNIVERSITY TEACHING HOSPITAL IN SOUTH DELHI

    Directory of Open Access Journals (Sweden)

    Fowad Khurshid et al.

    2012-07-01

    Full Text Available Study objective: To investigate the use of antihypertensive drugs in hypertensive patients and to identify whether such pattern of prescription is appropriate in accordance with international guidelines for management of hypertension. Methods: This was a prospective analysis. A prescription based survey among patients with established hypertension was conducted at the Medicine Out-Patient Department of University Teaching Hospital in South Delhi, India. Data were collected from patients’ medical records as well as patients’ interviews.Results: A total of 192 hypertensive patients fulfilled the criteria for inclusion in the study analysis. Combination therapy was used more commonly than monotherapy (54.6% vs 45.4. Among the monotherapy category, the various classes of drugs used were as follows: beta- blockers (28.8%, diuretics (24.1%, calcium channel blockers (21.8%, ACE inhibitors (18.4%, angiotensin II receptor blockers (5.7% and α 1- blocker (1.1%. With respect to overall utilization pattern, diuretics (42.2% were the most frequently prescribed class, beta- blockers (41.2% ranked second followed by calcium channel blockers (39.1%, ACE inhibitors (26.0%, angiotensin II receptor blockers (23.4% and α 1- blocker (9.4%. As for individual medicines, amlodipine (35.4% was the most commonly prescribed antihypertensive drug followed by atenolol (17.8%, ramipril (17.2 % and furosemide (13.0 %. Among the combination therapies, 2- drug treatment was preferred for 75% of the hypertensive patients with CCB and β-blocker being the most frequent drug combination (22.4%.Conclusion: The general pattern of antihypertensive utilization seems to be in accordance with the international guidelines for management of hypertension.

  12. Association of variants in NEDD4L with blood pressure response and adverse cardiovascular outcomes in hypertensive patients treated with thiazide diuretics

    Science.gov (United States)

    McDonough, Caitrin W.; Burbage, Sarah E.; Duarte, Julio D.; Gong, Yan; Langaee, Taimour Y.; Turner, Stephen T.; Gums, John G.; Chapman, Arlene B.; Bailey, Kent R.; Beitelshees, Amber L.; Boerwinkle, Eric; Pepine, Carl J.; Cooper-DeHoff, Rhonda M.; Johnson, Julie A.

    2013-01-01

    Objective Single-nucleotide polymorphisms (SNPs) in NEDD4L may influence the ability of the NEDD4L protein to reduce epithelial sodium channel expression. A variant in NEDD4L, rs4149601, was associated with antihypertensive response and cardiovascular outcomes during treatment with thiazide diuretics and β-blockers in a Swedish population. We sought to further evaluate associations between NEDD4L polymorphisms, blood pressure response and cardiovascular outcomes with thiazide diuretics and β-blockers. Methods Four SNPs, rs4149601, rs292449, rs1008899 and rs75982813, were genotyped in 767 patients from the Pharmacogenomic Evaluation of Antihypertensive Responses (PEAR) clinical trial and association was assessed with blood pressure response to hydrochlorothiazide and atenolol. One SNP, rs4149601, was also genotyped in 1345 patients from the International Verapmil SR Trandolapril Study (INVEST), and association was examined with adverse cardiovascular outcomes relative to hydrochlorothiazide treatment. Results Significant associations or trends were found between rs4149601, rs292449, rs75982813 and rs1008899 and decreases in blood pressure in whites on hydrochlorothiazide, and a significant association was observed with increasing copies of the GC rs4149601-rs292449 haplotype and greater blood pressure response to hydrochlorothiazide in whites (P = 0.0006 and 0.006, SBP and DBP, respectively). Significant associations were also seen with rs4149601 and an increased risk for adverse cardiovascular outcomes in whites not treated with hydrochlorothiazide [P = 0.022, odds ratio (95% confidence interval) = 10.65 (1.18–96.25)]. Conclusion NEDD4L rs4149601, rs292449 and rs75982813 may be predictors for blood pressure response to hydrochlorothiazide in whites, and NEDD4L rs4149601 may be a predictor for adverse cardiovascular outcomes in whites not treated with hydrochlorothiazide. PMID:23353631

  13. Effect of Ginger and Turmeric Rhizomes on Inflammatory Cytokines Levels and Enzyme Activities of Cholinergic and Purinergic Systems in Hypertensive Rats.

    Science.gov (United States)

    Akinyemi, Ayodele Jacob; Thomé, Gustavo Roberto; Morsch, Vera Maria; Bottari, Nathieli B; Baldissarelli, Jucimara; de Oliveira, Lizielle Souza; Goularte, Jeferson Ferraz; Belló-Klein, Adriane; Duarte, Thiago; Duarte, Marta; Boligon, Aline Augusti; Athayde, Margareth Linde; Akindahunsi, Akintunde Afolabi; Oboh, Ganiyu; Schetinger, Maria Rosa Chitolina

    2016-05-01

    Inflammation exerts a crucial pathogenic role in the development of hypertension. Hence, the aim of the present study was to investigate the effects of ginger (Zingiber officinale) and turmeric (Curcuma longa) on enzyme activities of purinergic and cholinergic systems as well as inflammatory cytokine levels in Nω-nitro-L-arginine methyl ester hydrochloride-induced hypertensive rats. The rats were divided into seven groups (n = 10); groups 1-3 included normotensive control rats, hypertensive (Nω-nitro-L-arginine methyl ester hydrochloride) rats, and hypertensive control rats treated with atenolol (an antihypertensive drug), while groups 4 and 5 included normotensive and hypertensive (Nω-nitro-L-arginine methyl ester hydrochloride) rats treated with 4 % supplementation of turmeric, respectively, and groups 6 and 7 included normotensive and hypertensive rats treated with 4 % supplementation of ginger, respectively. The animals were induced with hypertension by oral administration of Nω-nitro-L-arginine methyl ester hydrochloride, 40 mg/kg body weight. The results revealed a significant increase in ATP and ADP hydrolysis, adenosine deaminase, and acetylcholinesterase activities in lymphocytes from Nω-nitro-L-arginine methyl ester hydrochloride hypertensive rats when compared with the control rats. In addition, an increase in serum butyrylcholinesterase activity and proinflammatory cytokines (interleukin-1 and - 6, interferon-γ, and tumor necrosis factor-α) with a concomitant decrease in anti-inflammatory cytokines (interleukin-10) was observed in Nω-nitro-L-arginine methyl ester hydrochloride hypertensive rats. However, dietary supplementation of both rhizomes was efficient in preventing these alterations in hypertensive rats by decreasing ATP hydrolysis, acetylcholinesterase, and butyrylcholinesterase activities and proinflammatory cytokines in hypertensive rats. Thus, these activities could suggest a possible insight about the protective

  14. Variation in Antiarrhythmic Management of Infants Hospitalized with Supraventricular Tachycardia: A Multi-Institutional Analysis.

    Science.gov (United States)

    Guerrier, Karine; Shamszad, Pirouz; Czosek, Richard J; Spar, David S; Knilans, Timothy K; Anderson, Jeffrey B

    2016-06-01

    Supraventricular tachycardia (SVT) is the most frequent form of symptomatic tachyarrhythmia in infants. The purposes of this study were to describe practice patterns of the management of infants hospitalized with SVT and factors associated with 30-day hospital readmission. This was a multi-institutional, retrospective review of the pediatric health information system database of SVT hospitalizations from 2003 to 2013. High-volume centers (HVC) were defined as those at the upper quartile of admissions. Infants with an ICD-9 code of paroxysmal SVT were included. Antiarrhythmics investigated included amiodarone, atenolol, digoxin, esmolol, flecainide, procainamide, propafenone, propranolol, and sotalol. Frequency of antiarrhythmic use based on center volume was the primary end point. Rate of 30-day SVT readmission was the secondary end point. Analysis of factors associated with readmission was assessed by Chi-square analysis and expressed as odds ratio and 95 % confidence interval. A total of 851 patients (60 % male, 44 % neonates) were hospitalized at 43 hospitals. Propranolol, digoxin, and amiodarone were the most frequently utilized antiarrhythmics. HVCs represented 12 hospitals comprising 494 (58 %) patients. Although HVCs were more likely to utilize propranolol (OR 2.5, CI 1.5-4.1), there was no significant difference in the 30-day readmission rate between patients treated at HVCs versus non-HVCs (p = 0.9). The majority of infants with SVT are treated with a small number of antiarrhythmic medications during index hospitalization. Although hospital-to-hospital variation in antiarrhythmic choice exists, there appears to be no difference in readmission. The remaining practice variation may be related to intrinsic patient characteristics. PMID:27033244

  15. Managing hypertension in diabetic patients – focus on trandolapril/verapamil combination

    Directory of Open Access Journals (Sweden)

    Sanjib Kumar Sharma

    2007-09-01

    Full Text Available Sanjib Kumar Sharma1,3, Piero Ruggenenti1,2, Giuseppe Remuzzi1,2, 1Clinical Research Centre for Rare Diseases “Aldo e Cele Daccò”, Mario Negri Institute for Pharmacological Research, Villa Camozzi, Ranica, Italy; 2Unit of Nephrology, Azienda Ospedaliera, Ospedali Riuniti, Bergamo, Italy; 3Department of Medicine, BP Koirala Institute of Health Sciences, Dharan, NepalAbstract: Hypertensive diabetes individuals are at higher risk for cardiovascular events and progression to end stage renal disease. Several well conducted clinical trials indicate that aggressive treatment of hypertension in individual with diabetes reduces these complications. Combinations of two or more antihypertensive drugs are frequently required to reach the target blood pressure and to improve the cardiovascular and renal outcomes in these patients. There are physiological and clinical rationales for renin-angiotensin system blockade in hypertensive diabetics. Trandolapril/verapamil sustained released (SR is a fixed-dose combination of trandolapril and a sustained release formulation of verapamil and indicated in treatment of hypertension in patients who require more than one drug to reach target blood pressure. The antihypertensive efficacy of trandolapril/verapamil SR has been evaluated extensively in large trials. In the INVEST trial, a verapamil SR-based treatment strategy that included trandolapril in most patients was effective in reducing the primary outcome in hypertensive patients with coronary artery disease. The new onset of diabetes was also significantly lower in the verapamil SR/trandolapril treatment group in comparison with those on the atenolol/hydroclorothiazide treatment group. The BErgamo NEphrologic DIabetes Complications Trial (BENEDICT documented that in hypertensive diabetes and normoalbuminuria, trandolapril plus verapamil or trandolapril alone delayed the onset of microalbuminuria independent of their blood pressurereducing effect. Thus

  16. Uncovering the Molecular Mechanism of Actions between Pharmaceuticals and Proteins on the AD Network.

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    Shujuan Cao

    Full Text Available This study begins with constructing the mini metabolic networks (MMNs of beta amyloid (Aβ and acetylcholine (ACh which stimulate the Alzheimer's Disease (AD. Then we generate the AD network by incorporating MMNs of Aβ and ACh, and other MMNs of stimuli of AD. The panel of proteins contains 49 enzymes/receptors on the AD network which have the 3D-structure in PDB. The panel of drugs is formed by 5 AD drugs and 5 AD nutraceutical drugs, and 20 non-AD drugs. All of these complexes formed by these 30 drugs and 49 proteins are transformed into dyadic arrays. Utilizing the prior knowledge learned from the drug panel, we propose a statistical classification (dry-lab. According to the wet-lab for the complex of amiloride and insulin degrading enzyme, and the complex of amiloride and neutral endopeptidase, we are confident that this dry-lab is reliable. As the consequences of the dry-lab, we discover many interesting implications. Especially, we show that possible causes of Tacrine, donepezil, galantamine and huperzine A cannot improve the level of ACh which is against to their original design purpose but they still prevent AD to be worse as Aβ deposition appeared. On the other hand, we recommend Miglitol and Atenolol as the safe and potent drugs to improve the level of ACh before Aβ deposition appearing. Moreover, some nutrients such as NADH and Vitamin E should be controlled because they may harm health if being used in wrong way and wrong time. Anyway, the insights shown in this study are valuable to be developed further.

  17. Photocatalytic degradation of pharmaceutical wastes by alginate supported TiO2 nanoparticles in packed bed photo reactor (PBPR).

    Science.gov (United States)

    Sarkar, Santanu; Chakraborty, Sudip; Bhattacharjee, Chiranjib

    2015-11-01

    In recent years deposal of pharmaceutical wastes has become a major problem globally. Therefore, it is necessary to removes pharmaceutical waste from the municipal as well as industrial effluents before its discharge. The convectional wastewater and biological treatments are generally failed to separate different drugs from wastewater streams. Thus, heterogeneous photocatalysis process becomes lucrative method for reduction of detrimental effects of pharmaceutical compounds. The main disadvantage of the process is the reuse or recycle of photocatalysis is a tedious job. In this work, the degradation of aqueous solution of chlorhexidine digluconate (CHD), an antibiotic drug, by heterogeneous photocatalysis was study using supported TiO2 nanoparticle. The major concern of this study is to bring down the limitations of suspension mode heterogeneous photocatalysis by implementation of immobilized TiO2 with help of calcium alginate beads. The alginate supported catalyst beads was characterized by scanning electron microscopy coupled with energy dispersive X-ray spectroscopy (SEM/EDAX) as well as the characteristic crystalline forms of TiO2 nanoparticle was confirmed by XRD. The degradation efficiency of TiO2 impregnated alginate beads (TIAB) was compared with the performance of free TiO2 suspension. Although, the degradation efficiency was reduced considerably using TIAB but the recycle and reuse of catalyst was increased quite appreciably. The kinetic parameters related to this work have also been measure. Moreover, to study the susceptibility of the present system photocatalysis of other three drugs ibuprofen (IBP), atenolol (ATL) and carbamazepine (CBZ) has been carried out using immobilized TiO2. The continuous mode operation in PBPR has ensured the applicability of alginate beads along with TiO2 in wastewater treatment. The variation of residence time has significant impact on the performance of PBPR. PMID:25743764

  18. Oxidative stress, energy storage, and swimming performance of Limnodynastes peronii tadpoles exposed to a sub-lethal pharmaceutical mixture throughout development.

    Science.gov (United States)

    Melvin, Steven D

    2016-05-01

    Pharmaceutical contaminants represent emerging threats to aquatic animals and ecosystem health, and research exploring toxicological outcomes associated with these compounds in non-target wildlife has been flagged for prioritization. Amphibians represent particularly vulnerable organisms and many populations around the world are currently at risk of extinction. However, to date, relatively few studies have explored the consequences of exposures to common non-steroidal pharmaceuticals during sensitive amphibian life-stages. To address existing knowledge gaps, tadpoles of the Australian striped-marsh frog (Limnodynastes peronii) were exposed to control water and a mixture of the common pharmaceutical contaminants diclofenac, naproxen, atenolol and gemfibrozil at 0.1, 1, 10, 100 and 1000 μg/L throughout the developmental period. Effects on detoxification pathways, energy storage, growth and development, and swimming performance were assessed following exposure. Developmental rates and liver-somatic index (LSI) were significantly reduced in the highest exposure concentration, and condition factor (K) was increased at concentrations as low as 10 μg/L. Morphological endpoints were associated with significantly altered levels of hepatic triglycerides, which in turn were correlated with increased peroxidase activity in animals exposed to the highest concentration (1000 μg/L). The mixture had no significant effect on swimming performance, but a trend of decreased swimming velocity (average and maximum) was observed with increasing concentration, and this was correlated with effects on LSI. Results demonstrate that mixtures of common non-steroidal pharmaceuticals can elicit a range of physiological, metabolic and morphological responses in larval amphibians, and more research is therefore warranted to explore possible relationships between endpoints at different levels of organization. PMID:26391467

  19. On-line sensor monitoring for chemical contaminant attenuation during UV/H2O2 advanced oxidation process.

    Science.gov (United States)

    Yu, Hye-Weon; Anumol, Tarun; Park, Minkyu; Pepper, Ian; Scheideler, Jens; Snyder, Shane A

    2015-09-15

    A combination of surrogate parameters and indicator compounds were measured to predict the removal efficiency of trace organic compounds (TOrCs) using low pressure (LP)-UV/H2O2 advanced oxidation process (AOP), engaged with online sensor-based monitoring system. Thirty-nine TOrCs were evaluated in two distinct secondary wastewater effluents in terms of estimated photochemical reactivity, as a function of the rate constants of UV direct photolysis (kUV) and hydroxyl radical (OH) oxidation (kOH). The selected eighteen TOrCs were classified into three groups that served as indicator compounds: Group 1 for photo-susceptible TOrCs but with minor degradation by OH oxidation (diclofenac, fluoxetine, iohexol, iopamidol, iopromide, simazine and sulfamethoxazole); Group 2 for TOrCs susceptible to both direct photolysis and OH oxidation (benzotriazole, diphenhydramine, ibuprofen, naproxen and sucralose); and Group 3 for photo-resistant TOrCs showing dominant degradation by OH oxidation (atenolol, carbamazepine, DEET, gemfibrozil, primidone and trimethoprim). The results indicate that TOC (optical-based measurement), UVA254 or UVT254 (UV absorbance or transmittance at 254 nm), and total fluorescence can all be used as suitable on-line organic surrogate parameters to predict the attenuation of TOrCs. Furthermore, the automated real-time monitoring via on-line surrogate sensors and equipped with the developed degradation profiles between sensor response and a group of TOrCs removal can provide a diagnostic tool for process control during advanced treatment of reclaimed waters. PMID:26074188

  20. Photocatalytic degradation of pharmaceutical wastes by alginate supported TiO2 nanoparticles in packed bed photo reactor (PBPR).

    Science.gov (United States)

    Sarkar, Santanu; Chakraborty, Sudip; Bhattacharjee, Chiranjib

    2015-11-01

    In recent years deposal of pharmaceutical wastes has become a major problem globally. Therefore, it is necessary to removes pharmaceutical waste from the municipal as well as industrial effluents before its discharge. The convectional wastewater and biological treatments are generally failed to separate different drugs from wastewater streams. Thus, heterogeneous photocatalysis process becomes lucrative method for reduction of detrimental effects of pharmaceutical compounds. The main disadvantage of the process is the reuse or recycle of photocatalysis is a tedious job. In this work, the degradation of aqueous solution of chlorhexidine digluconate (CHD), an antibiotic drug, by heterogeneous photocatalysis was study using supported TiO2 nanoparticle. The major concern of this study is to bring down the limitations of suspension mode heterogeneous photocatalysis by implementation of immobilized TiO2 with help of calcium alginate beads. The alginate supported catalyst beads was characterized by scanning electron microscopy coupled with energy dispersive X-ray spectroscopy (SEM/EDAX) as well as the characteristic crystalline forms of TiO2 nanoparticle was confirmed by XRD. The degradation efficiency of TiO2 impregnated alginate beads (TIAB) was compared with the performance of free TiO2 suspension. Although, the degradation efficiency was reduced considerably using TIAB but the recycle and reuse of catalyst was increased quite appreciably. The kinetic parameters related to this work have also been measure. Moreover, to study the susceptibility of the present system photocatalysis of other three drugs ibuprofen (IBP), atenolol (ATL) and carbamazepine (CBZ) has been carried out using immobilized TiO2. The continuous mode operation in PBPR has ensured the applicability of alginate beads along with TiO2 in wastewater treatment. The variation of residence time has significant impact on the performance of PBPR.

  1. The role of the anaesthetised guinea-pig in the preclinical cardiac safety evaluation of drug candidate compounds

    Energy Technology Data Exchange (ETDEWEB)

    Marks, Louise, E-mail: louise.marks@astrazeneca.com [Safety Assessment UK, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG (United Kingdom); Borland, Samantha; Philp, Karen; Ewart, Lorna; Lainée, Pierre; Skinner, Matthew [Safety Assessment UK, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG (United Kingdom); Kirk, Sarah [Innovative Medicines, Discovery Sciences, AstraZeneca, Alderley Park, Macclesfield, Cheshire, SK10 4TG (United Kingdom); Valentin, Jean-Pierre [Safety Assessment UK, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, SK10 4TG (United Kingdom)

    2012-09-01

    Despite rigorous preclinical and clinical safety evaluation, adverse cardiac effects remain a leading cause of drug attrition and post-approval drug withdrawal. A number of cardiovascular screens exist within preclinical development. These screens do not, however, provide a thorough cardiac liability profile and, in many cases, are not preventing the progression of high risk compounds. We evaluated the suitability of the anaesthetised guinea-pig for the assessment of drug-induced changes in cardiovascular parameters. Sodium pentobarbitone anaesthetised male guinea-pigs received three 15 minute intravenous infusions of ascending doses of amoxicillin, atenolol, clonidine, dobutamine, dofetilide, flecainide, isoprenaline, levosimendan, milrinone, moxifloxacin, nifedipine, paracetamol, verapamil or vehicle, followed by a 30 minute washout. Dose levels were targeted to cover clinical exposure and above, with plasma samples obtained to evaluate effect/exposure relationships. Arterial blood pressure, heart rate, contractility function (left ventricular dP/dt{sub max} and QA interval) and lead II electrocardiogram were recorded throughout. In general, the expected reference compound induced effects on haemodynamic, contractility and electrocardiographic parameters were detected confirming that all three endpoints can be measured accurately and simultaneously in one small animal. Plasma exposures obtained were within, or close to the expected clinical range of therapeutic plasma levels. Concentration–effect curves were produced which allowed a more complete understanding of the margins for effects at different plasma exposures. This single in vivo screen provides a significant amount of information pertaining to the cardiovascular risk of drug candidates, ultimately strengthening strategies addressing cardiovascular-mediated compound attrition and drug withdrawal. -- Highlights: ► Evaluation of the anaesthetised guinea-pig to determine cardiac liability.

  2. New standards in hypertension and cardiovascular risk management: focus on telmisartan

    Directory of Open Access Journals (Sweden)

    Domenico Galzerano

    2010-03-01

    Full Text Available Domenico Galzerano1, Cristina Capogrosso4, Sara Di Michele2, Antonio Galzerano1, Paola Paparello1, Diana Lama3, Carlo Gaudio21Department of Cardiology, San Gennaro Hospital, Naples, Italy; 2Department of Heart and Great Vessels, A. Reale, La Sapienza University, Rome, Italy; 3V Division of Internal Medicine, II University, Naples, Italy; 4Cardiology Division, San Giovanni Bosco Hospital, Naples, ItalyAbstract: Blockade of the renin–angiotensin system is an important approach in managing high blood pressure, and has increasingly been shown to affect cardiovascular disease processes mediated by angiotensin II throughout the cardiovascular and renal continua. Telmisartan is an angiotensin II receptor blocker (ARB displaying unique pharmacologic properties, including a longer half life than any other ARB, that result in large and sustained reductions of blood pressure. In patients with mild-to-moderate hypertension, telmisartan has proved superior to other antihypertensive agents (valsartan, losartan, ramipril, perindopril, and atenolol in controlling blood pressure particularly towards the end of the dosing interval. There is also clinical evidence that telmisartan reduces left ventricular hypertrophy, reduces arterial stiffness and the recurrence of atrial fibrillation, and confers renoprotection. The ONgoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial (ONTARGET® study has demonstrated that telmisartan has similar cardiovascular protective effects to ramipril in a large, high-risk patient population but was better tolerated. The powerful and sustained blood pressure control apparent in clinical trials, together with cardiovascular protection and tolerability demonstrated in ONTARGET® means that telmisartan may be a preferred option for patients with hypertension.Keywords: angiotensin II receptor blocker, cardiovascular disease, hypertension, renin–angiotensin system, telmisartan

  3. Olmesartan medoxomil combined with hydrochlorothiazide for the treatment of hypertension

    Directory of Open Access Journals (Sweden)

    Mark Greathouse

    2006-12-01

    Full Text Available Mark GreathouseSouth Hills Cardiology Associates of Pittsburgh, Pittsburgh, PA, USAAbstract: In most patients with hypertension, especially Stage 2 hypertension, adequate control of blood pressure (BP is only achieved with combination drug therapy. When using combination therapy, antihypertensive agents with complementary mechanisms of action are recommended, for example, an angiotensin receptor blocker (ARB in combination with hydrochlorothiazide (HCTZ, a β-blocker + HCTZ, an ACE inhibitor + HCTZ, or a calcium channel blocker + an ACE inhibitor. One such combination is olmesartan medoxomil + HCTZ, which is available as fixed-dose, single-tablet combinations for once-daily administration. In clinical trials, olmesartan medoxomil/HCTZ reduced systolic BP (SBP and diastolic BP (DBP to a greater extent than either component as monotherapy. A clinical study in patients with Stage 1 or 2 hypertension showed that olmesartan medoxomil/HCTZ achieved a similar mean reduction in DBP, but a significantly greater mean reduction in SBP and higher rate of BP control (<140/90 mmHg than observed with losartan/HCTZ, at US/European-approved starting doses. In a non-inferiority trial, the antihypertensive efficacy of olmesartan medoxomil/HCTZ was comparable to that of atenolol/HCTZ. Furthermore, indirect comparisons have shown that olmesartan medoxomil/HCTZ compares favorably with other antihypertensive combination therapies, including other ARB/HCTZ combinations and amlodipine besylate/benazepril. Olmesartan medoxomil/HCTZ is generally well tolerated. In conclusion, olmesartan medoxomil/HCTZ is an effective and well-tolerated combination antihypertensive therapy that results in significant BP reductions and BP control in many patients. Keywords: olmesartan medoxomil, hydrochlorothiazide, angiotensin II receptor blocker, hypertension

  4. Fruit juice inhibition of uptake transport: a new type of food–drug interaction

    Science.gov (United States)

    Bailey, David G

    2010-01-01

    A new type of interaction in which fruit juices diminish oral drug bioavailability through inhibition of uptake transport is the focus of this review. The discovery was based on an opposite to anticipated finding when assessing the possibility of grapefruit juice increasing oral fexofenadine bioavailability in humans through inhibition of intestinal MDR1-mediated efflux transport. In follow-up investigations, grapefruit or orange juice at low concentrations potentially and selectively inhibited in vitro OATP1A2-mediated uptake compared with MDR1-caused efflux substrate transport. These juices at high volume dramatically depressed oral fexofenadine bioavailability. Grapefruit was the representative juice to characterize the interaction subsequently. A volume–effect relationship study using a normal juice amount halved average fexofenadine absorption. Individual variability and reproducibility data indicated the clinical interaction involved direct inhibition of intestinal OATP1A2. Naringin was a major causal component suggesting that other flavonoids in fruits and vegetables might also produce the effect. Duration of juice clinical inhibition of fexofenadine absorption lasted more than 2 h but less than 4 h indicating the interaction was avoidable with appropriate interval of time between juice and drug consumption. Grapefruit juice lowered the oral bioavailability of several medications transported by OATP1A2 (acebutolol, celiprolol, fexofenadine, talinolol, L-thyroxine) while orange juice did the same for others (atenolol, celiprolol, ciprofloxacin, fexofenadine). Juice clinical inhibition of OATP2B1 was unresolved while that of OATP1B1 seemed unlikely. The interaction between grapefruit juice and etoposide also seemed relevant. Knowledge of both affected uptake transporter and drug hydrophilicity assisted prediction of the clinical interaction with grapefruit or orange juice. PMID:21039758

  5. Heterozygous disruption of activin receptor-like kinase 1 is associated with increased arterial pressure in mice

    Science.gov (United States)

    González-Núñez, María; Riolobos, Adela S.; Castellano, Orlando; Fuentes-Calvo, Isabel; de los Ángeles Sevilla, María; Oujo, Bárbara; Pericacho, Miguel; Cruz-Gonzalez, Ignacio; Pérez-Barriocanal, Fernando; ten Dijke, Peter; López-Novoa, Jose M.

    2015-01-01

    ABSTRACT The activin receptor-like kinase 1 (ALK-1) is a type I cell-surface receptor for the transforming growth factor-β (TGF-β) family of proteins. Hypertension is related to TGF-β1, because increased TGF-β1 expression is correlated with an elevation in arterial pressure (AP) and TGF-β expression is upregulated by the renin-angiotensin-aldosterone system. The purpose of this study was to assess the role of ALK-1 in regulation of AP using Alk1 haploinsufficient mice (Alk1+/−). We observed that systolic and diastolic AP were significantly higher in Alk1+/− than in Alk1+/+ mice, and all functional and structural cardiac parameters (echocardiography and electrocardiography) were similar in both groups. Alk1+/− mice showed alterations in the circadian rhythm of AP, with higher AP than Alk1+/+ mice during most of the light period. Higher AP in Alk1+/− mice is not a result of a reduction in the NO-dependent vasodilator response or of overactivation of the peripheral renin-angiotensin system. However, intracerebroventricular administration of losartan had a hypotensive effect in Alk1+/− and not in Alk1+/+ mice. Alk1+/− mice showed a greater hypotensive response to the β-adrenergic antagonist atenolol and higher concentrations of epinephrine and norepinephrine in plasma than Alk1+/+ mice. The number of brain cholinergic neurons in the anterior basal forebrain was reduced in Alk1+/− mice. Thus, we concluded that the ALK-1 receptor is involved in the control of AP, and the high AP of Alk1+/− mice is explained mainly by the sympathetic overactivation shown by these animals, which is probably related to the decreased number of cholinergic neurons. PMID:26398936

  6. Application in the STRATHE trial of a score system to compare the efficacy and the tolerability of different therapeutic strategies in the management of hypertension

    Directory of Open Access Journals (Sweden)

    Bernard Waeber

    2008-02-01

    Full Text Available Bernard Waeber1, Jean-Jacques Mourad21Division de Physiopathologie Clinique, Centre Hospitalier Universitaire Vaudois et Université de Lausanne, Lausanne, Switzerland; 2Hôpital Avicienne, Bobigny, FranceAbstract: A score system integrating the evolution of efficacy and tolerability over time was applied to a subpopulation of the STRATHE trial, a trial performed according to a parallel group design, with a double-blind, random allocation to either a fixed-dose combination strategy (perindopril/indapamide 2 mg/0.625 mg, with the possibility to increase the dose to 3 mg/0.935 mg, and 4 mg/1.250 mg if needed, n = 118, a sequential monotherapy approach (atenolol 50 mg, followed by losartan 50 mg and amlodipine 5 mg if needed, n = 108, or a stepped-care strategy (valsartan 40 mg, followed by valsartan 80 mg and valsartan 80 mg+ hydrochlorothiazide 12.5 mg if needed, n = 103. The aim was to lower blood pressure below 140/90 mmHg within a 9-month period. The treatment could be adjusted after 3 and 6 months. Only patients in whom the study protocol was strictly applied were included in this analysis. At completion of the trial the total score averaged 13.1 ± 70.5 (mean ± SD using the fixed-dose combination strategy, compared with –7.2 ± 81.0 using the sequential monotherapy approach and –17.5 ± 76.4 using the stepped-care strategy. In conclusion, the use of a score system allows the comparison of antihypertensive therapeutic strategies, taking into account at the same time efficacy and tolerability. In the STRATHE trial the best results were observed with the fixed-dose combination containing low doses of an angiotensin enzyme converting inhibitor (perindopril and a diuretic (indapamide.Keywords: antihypertensive therapy, tolerability, antihypertensive efficacy, fixed-dose combination, sequential monotherapy, stepped-care treatment

  7. MODERN VIEWS ON THE VARIABILITY OF BLOOD PRESSURE

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    V. M. Gorbunov

    2012-01-01

    Full Text Available Nowadays conception of blood pressure (BP variability (BPV includes a number of indicators related to various physiological factors. All the indexes are calculated with the standard deviation (SD or more complex formulas, including SD. BPV main varieties are considered a 24-hour BPV (measured by ambulatory BP monitoring – ABPM, midterm BPV (BP self-control or home BP – HBP, and long-term, visit-to-visit, BPV (traditional BP measurement or office BP – OBP. The 24-hour BPV was the main subject of study for many years. Recently significant attention has been paid to the visit-to-visit BPV assessment. Retrospective meta-analysis showed that in a cohort of patients after stroke or transient ischemic attack, this index was a strong and independent (from the average BP level predictor of stroke. In ASCOT-BPLA study visit-to-visit systolic BPV also was a strong predictor of stroke and coronary events. Long-term BPV in patients of amlodipine/perindopril treatment group was significantly lower than this in patients of atenolol/diuretic group during the follow-up that was associated with a lower risk of cardiovascular complications. However , the concept of visit-to-visit BPV use for risk stratification and monitoring of antihypertensive therapy efficacy is associated with significant limitations (basic data is obtained in the post hoc analysis, difficulties in objective evaluation of prognostic significance of indicators, their dependence on medication adherence, etc.. The HBP self-control is a promising approach to the BPV analysis; it may be the "happy medium" between ABPM and OPB. New-designed prospective comparative studies are needed to evaluate the clinical significance of the various BPV parameters.

  8. Verapamil-associated cardiogenic shock in a 71-year-old man with myasthenia gravis: a case report

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    Drolet Benoit

    2009-06-01

    Full Text Available Abstract Introduction Myasthenia gravis is a rare neuromuscular disorder associated with a reduction in the availability of acetylcholine receptors at the post-synaptic membranes of skeletal muscles. This is caused by the production of anti-acetylcholine receptor antibodies at the neuromuscular junction due to an autoimmune insult, leading to a compromised neuromuscular transmission. Verapamil can influence, in a dose-dependent fashion, the neuromuscular transmission in myasthenia gravis. Case presentation We report a 71-year-old Caucasian man with myasthenia gravis suffering from a cardiogenic shock following a single dose of verapamil. The patient had uncontrolled atrial fibrillation with a heart rate of 120 beats/min. Atenolol 100 mg was started. The next day, verapamil SR 240 mg was started. Two hours after the first dose of verapamil, the patient complained of weakness and dyspnea with signs of shock; his blood pressure was 70/50 mm Hg and heart rate at 101 beats/min. An echocardiogram showed diffuse hypokinesis of both ventricles with an ejection fraction of 20%. Cardiac catheterization was performed and coronary arteries appeared without significant stenosis, but there was a diffuse hypokinesis. Verapamil was stopped and the patient received intravenous glucagon and calcium chloride. Both the anti-acetylcholine receptor and anti-striated muscle antibodies tested positive. A few hours later, another echocardiogram showed an improvement in the ventricular function, which returned to normal five days later. Conclusion Caution is needed when administering verapamil to patients with myasthenia gravis, especially when the anti-acetylcholine receptor and anti-striated muscle antibodies titres are positive.

  9. Polypharmacy among older adults in Tehran

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    B. Ahmadi

    2006-08-01

    Full Text Available Background: Multiple drug use is frequently considered to be hazardous for the elderly because of their greater vulnerability to the complications. The purpose of this study was to determine the prevalence of polypharmacy in Tehran and to assess the relative demographic characteristics of patients. Methods: In a cross-sectional study 400 persons aging 55 years and older were interviewed in order to determine the presence of polypharmacy (daily intake of three or more drugs. The cases were randomly selected and asked to answer a questionnaire through interview at home. The questionnaire contained questions about all taking drugs, pattern of using each drug and also patients' personal, social and medical history. Chi-square and fisher exact tests and determination of odds ratios were used in order to data analysis. Results: Medium number of drugs used was 3.4 ± 1.9 in studied cases and %39.6 of cases were exposed to polypharmacy. The prevalence of physician prescribed drug usage was observed to be increased by increasing number of total used drugs in each case (P<0.002. The most commonly used drugs were A.S.A, Atenolol and propranolol and these drugs were prescribed by physician in over than %90 of cases. There was a positive correlations between polypharmacy with referring to multiple physicians (OR=1.96, CI 95%, 1.28-2.98 (P<0.002 and adverse drug reactions (OR=2.44, CI 95%, 1.47-4.05 (P<0.001. Polypharmacy was more prevalent in the age group of 65-75 years (P<0.04 and lower levels of education (P<0.004 and less prevalent in the group with moderate income (P<0.001. Conclusion: Polypharmacy is common among adults aging 55 years and more in Tehran and is affected by age, education level and economic status.

  10. Acquisition of Pavlovian fear conditioning using β-adrenoceptor activation of the dorsal premammillary nucleus as an unconditioned stimulus to mimic live predator-threat exposure.

    Science.gov (United States)

    Pavesi, Eloisa; Canteras, Newton S; Carobrez, Antônio P

    2011-04-01

    In the present work, we sought to mimic the internal state changes in response to a predator threat by pharmacologically stimulating the brain circuit involved in mediating predator fear responses, and explored whether this stimulation would be a valuable unconditioned stimulus (US) in an olfactory fear conditioning paradigm (OFC). The dorsal premammillary nucleus (PMd) is a key brain structure in the neural processing of anti-predatory defensive behavior and has also been shown to mediate the acquisition and expression of anti-predatory contextual conditioning fear responses. Rats were conditioned by pairing the US, which was an intra-PMd microinjection of isoproterenol (ISO; β-adrenoceptor agonist), with amyl acetate odor-the conditioned stimulus (CS). ISO (10 and 40 nmol) induced the acquisition of the OFC and the second-order association by activation of β-1 receptors in the PMd. Furthermore, similar to what had been found for contextual conditioning to a predator threat, atenolol (β-1 receptor antagonist) in the PMd also impaired the acquisition and expression of OFC promoted by ISO. Considering the strong glutamatergic projections from the PMd to the dorsal periaqueductal gray (dPAG), we tested how the glutamatergic blockade of the dPAG would interfere with the OFC induced by ISO. Accordingly, microinjections of NMDA receptor antagonist (AP5, 6 nmol) into the dPAG were able to block both the acquisition, and partially, the expression of the OFC. In conclusion, we have found that PMd β-1 adrenergic stimulation is a good model to mimic predatory threat-induced internal state changes, and works as a US able to mobilize the same systems involved in the acquisition and expression of predator-related contextual conditioning.

  11. Arterial stiffness, hypertension, and rational use of nebivolol

    Directory of Open Access Journals (Sweden)

    Enrico Agabiti-Rosei

    2009-05-01

    Full Text Available Enrico Agabiti-Rosei, Enzo Porteri, Damiano RizzoniClinica Medica, Department of Medical and Surgical Sciences, University of Brescia, ItalyAbstract: Arterial stiffness plays a key role in the pathophysiology of the cardiovascular system. Some indices of arterial stiffness (pulse wave velocity, augmentation index, characteristics of central blood pressure waveform may be presently calculated and evaluated in the clinical setting. Age and blood pressure are the two major clinical determinants of increased arterial stiffness, while molecular determinants of arterial stiffness are related to fibrotic components of the extracellular matrix, mainly elastin, collagen and fibronectin. Increased arterial stiffness has been consistently observed in conditions such as hypertension, dyslipidemia and diabetes. Arterial stiffness evaluated by means of carotid-femoral pulse wave velocity yielded prognostic significance beyond and above traditional risk factors. A more favorable effect of calcium channel blockers, diuretics and ACE inhibitors compared with β-blockers on indices of arterial stiffness was observed in several studies. It is conceivable that newer β-blockers with additional vasodilating properties, such as nebivolol, which has favorable effects on carbohydrate and lipid metabolism, as well as on endothelial function and on oxidative stress, may have favorable effects on arterial stiffness, compared with atenolol. In fact, in recent studies, nebivolol was demonstrated to improve artery stiffness to a greater extent than older β-blockers. Because endothelial dysfunction and increased arterial stiffness play an important role in the early atherosclerotic processes and are associated with poor outcomes and increased mortality, independently of blood pressure, the ability of nebivolol to enhance release of endothelium-derived nitric oxide, and consequently improve endothelial function and arterial stiffness, may have significant clinical

  12. Evaluation of microwave oven heating for prediction of drug-excipient compatibilities and accelerated stability studies.

    Science.gov (United States)

    Schou-Pedersen, Anne Marie V; Østergaard, Jesper; Cornett, Claus; Hansen, Steen Honoré

    2015-05-15

    Microwave ovens have been used extensively in organic synthesis in order to accelerate reaction rates. Here, a set up comprising a microwave oven combined with silicon carbide (SiC) plates for the controlled microwave heating of model formulations has been applied in order to investigate, if a microwave oven is applicable for accelerated drug stability testing. Chemical interactions were investigated in three selected model formulations of drug and excipients regarding the formation of ester and amide reaction products. In the accelerated stability studies, a design of experiments (DoE) approach was applied in order to be able to rank excipients regarding reactivity: Study A: cetirizine with PEG 400, sorbitol, glycerol and propylene glycol. Study B: 6-aminocaproic acid with citrate, acetate, tartrate and gluconate. Study C: atenolol with citric, tartaric, malic, glutaric, and sorbic acid. The model formulations were representative for oral solutions (co-solvents), parenteral solutions (buffer species) and solid dosage forms (organic acids applicable for solubility enhancement). The DoE studies showed overall that the same impurities were generated by microwave oven heating leading to temperatures between 150°C and 180°C as compared to accelerated stability studies performed at 40°C and 80°C using a conventional oven. Ranking of the reactivity of the excipients could be made in the DoE studies performed at 150-180°C, which was representative for the ranking obtained after storage at 40°C and 80°C. It was possible to reduce the time needed for drug-excipient compatibility testing of the three model formulations from weeks to less than an hour in the three case studies. The microwave oven is therefore considered to be an interesting alternative to conventional thermal techniques for the investigation of drug-excipient interactions during preformulation.

  13. Tracing the limits of organic micropollutant removal in biological wastewater treatment.

    Science.gov (United States)

    Falås, Per; Wick, Arne; Castronovo, Sandro; Habermacher, Jonathan; Ternes, Thomas A; Joss, Adriano

    2016-05-15

    Removal of organic micropollutants was investigated in 15 diverse biological reactors through short and long-term experiments. Short-term batch experiments were performed with activated sludge from three parallel sequencing batch reactors (25, 40, and 80 d solid retention time, SRT) fed with synthetic wastewater without micropollutants for one year. Despite the minimal micropollutant exposure, the synthetic wastewater sludges were able to degrade several micropollutants present in municipal wastewater. The degradation occurred immediately after spiking (1-5 μg/L), showed no strong or systematic correlation to the sludge age, and proceeded at rates comparable to those of municipal wastewater sludges. Thus, the results from the batch experiments indicate that degradation of organic micropollutants in biological wastewater treatment is quite insensitive to SRT increases from 25 to 80 days, and not necessarily induced by exposure to micropollutants. Long-term experiments with municipal wastewater were performed to assess the potential for extended biological micropollutant removal under different redox conditions and substrate concentrations (carbon and nitrogen). A total of 31 organic micropollutants were monitored through influent-effluent sampling of twelve municipal wastewater reactors. In accordance with the results from the sludges grown on synthetic wastewater, several compounds such as bezafibrate, atenolol and acyclovir were significantly removed in the activated sludge processes fed with municipal wastewater. Complementary removal of two compounds, diuron and diclofenac, was achieved in an oxic biofilm treatment. A few aerobically persistent micropollutants such as venlafaxine, diatrizoate and tramadol were removed under anaerobic conditions, but a large number of micropollutants persisted in all biological treatments. Collectively, these results indicate that certain improvements in biological micropollutant removal can be achieved by combining different

  14. β-Adrenergic receptor antagonists inhibit vasculogenesis of embryonic stem cells by downregulation of nitric oxide generation and interference with VEGF signalling.

    Science.gov (United States)

    Sharifpanah, Fatemeh; Saliu, Fatjon; Bekhite, Mohamed M; Wartenberg, Maria; Sauer, Heinrich

    2014-11-01

    The β-adrenoceptor antagonist Propranolol has been successfully used to treat infantile hemangioma. However, its mechanism of action is so far unknown. The hypothesis of this research was that β-adrenoceptor antagonists may interfere with endothelial cell differentiation of stem cells. Specifically, the effects of the non-specific β-adrenergic receptor (β-adrenoceptor) antagonist Propranolol, the β1-adrenoceptor-specific antagonist Atenolol and the β2-adrenoceptor-specific antagonist ICI118,551 on vasculogenesis of mouse embryonic stem (ES) cells were investigated. All three β-blockers dose-dependently downregulated formation of capillary structures in ES cell-derived embryoid bodies and decreased the expression of the vascular cell markers CD31 and VE-cadherin. Furthermore, β-blockers downregulated the expression of fibroblast growth factor-2 (FGF-2), hypoxia inducible factor-1α (HIF-1α), vascular endothelial growth factor 165 (VEGF165), VEGF receptor 2 (VEGF-R2) and phospho VEGF-R2, as well as neuropilin 1 (NRP1) and plexin-B1 which are essential modulators of embryonic angiogenesis with additional roles in vessel remodelling and arteriogenesis. Under conditions of β-adrenoceptor inhibition, the endogenous generation of nitric oxide (NO) as well as the phosphorylation of endothelial nitric oxide synthase (eNOS) was decreased in embryoid bodies, whereas an increase in NO generation was observed with the NO donor S-nitroso-N-acetyl-D,L-penicillamine (SNAP). Consequently, vasculogenesis of ES cells was restored upon treatment of differentiating ES cells with β-adrenoceptor antagonists in the presence of NO donor. In summary, our data suggest that β-blockers impair vasculogenesis of ES cells by interfering with NO generation which could be the explanation for their anti-angiogenic effects in infantile hemangioma.

  15. Seasonal occurrence, removal, mass loading and environmental risk assessment of 55 pharmaceuticals and personal care products in a municipal wastewater treatment plant in Central Greece.

    Science.gov (United States)

    Papageorgiou, Myrsini; Kosma, Christina; Lambropoulou, Dimitra

    2016-02-01

    A comprehensive study, which contains the seasonal occurrence, removal, mass loading and environmental risk assessment of 55 multi-class pharmaceuticals and personal care products (PPCPs), took place in the wastewater treatment plant (WWTP) of Volos, Greece. A one year monitoring study was performed and the samples were collected from the influent and the effluent of the WWTP. Solid phase extraction was used for the pre-concentration of the samples followed by an LC-DAD-ESI/MS analysis. Positive samples were further confirmed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS). The maximum concentrations of the PPCPs varied between 21 ng/L and 15,320 ng/L in the influents and between 18 ng/L and 9965 ng/L in the effluents. The most commonly detected PPCPs were the diuretic furosemide, the beta-blockers atenolol and metoprolol, the analgesics paracetamol, nimesulide, salicylic acid and diclofenac and the psychomotor stimulant caffeine. The removal efficiencies ranged between negative and high removal rates, demonstrating that the WWTP is not able to efficiently remove the complex mixture of PPCPs. The estimated mass loads ranged between 5.1 and 3513 mg/day/1000 inhabitants for WWTP influent and between 4.1 to 2141 mg/day/1000 inhabitants for WWTP effluent. Finally, environmental risk assessment has been regarded a necessary part of the general research. According to the results produced from the calculation of the risk quotient on three trophic levels, the anti-inflammatory drug diclofenac and the antibiotics, trimethoprim and ciprofloxacin, identified to be of high potential environmental risk for acute toxicity, while diclofenac also for chronic toxicity. PMID:26613513

  16. Interaction of hyperthermia and heart rate on stroke volume during prolonged exercise.

    Science.gov (United States)

    Trinity, Joel D; Pahnke, Matthew D; Lee, Joshua F; Coyle, Edward F

    2010-09-01

    People who become hyperthermic during exercise display large increases in heart rate (HR) and reductions in stroke volume (SV). It is not clear if the reduction in SV is due primarily to hyperthermia or if it is a secondary effect of an elevation in HR reducing ventricular filling. In the present study, the upward drift of HR during prolonged exercise was prevented by a very small dose of the β1-adrenoreceptor blocker (atenolol; βB), thus allowing SV to be compared at a given HR during normothermia and hyperthermia. Eleven men cycled for 60 min at 57% of peak O2 uptake after receiving placebo control (PL) or a low dose (0.2 mg/kg) of βB. Hyperthermia was induced by reducing heat dissipation during exercise. Four experimental conditions were studied: normothermia-PL, normothermia-βB, hyperthermia-PL, and hyperthermia-βB. Hyperthermia increased skin and core temperature by 4.3 degrees C and 0.8 degrees C (P<0.01), respectively. βB prevented HR elevation with hyperthermia: HR values were similar at minute 60 during normothermia-PL and hyperthermia-βB (155±11 and 154±13 beats/min, respectively, P=0.82). However, SV was increased by 7% during the final 20 min of exercise during hyperthermia-βB compared with normothermia-PL (treatment×time interaction, P=0.03). In conclusion, when matched for HR, mild hyperthermia increased SV during exercise. Furthermore, the reduction in SV throughout prolonged exercise under normothermic and mildly hyperthermic conditions appears to be due to the increase in HR. PMID:20595543

  17. Anti-hypertensive treatment in pheochromocytoma and paraganglioma: current management and therapeutic features.

    Science.gov (United States)

    Mazza, Alberto; Armigliato, Michela; Marzola, Maria Cristina; Schiavon, Laura; Montemurro, Domenico; Vescovo, Giorgio; Zuin, Marco; Chondrogiannis, Sotirios; Ravenni, Roberta; Opocher, Giuseppe; Colletti, Patrick M; Rubello, Domenico

    2014-04-01

    Pheochromocytoma (PH) and paraganglioma (PG) are neuroendocrine neoplasms arising from chromaffin cells of the adrenal medulla and the sympathetic ganglia, respectively. Although are unusual cause of hypertension (HT) accounting for at most 0.1-0.2 % of cases, they may lead to severe and potentially lethal hypertensive crisis due to the effects of the released catecholamines. However, both PH and PG may be asymptomatic as ~30 % of subjects are normotensive or have orthostatic hypotension and in these cases the 24 h ambulatory blood pressure (BP) monitoring is an important toll to diagnose and treat HT. HT treatment may be difficult when PH or PG occurs in pregnancy or in the elderly subjects and in these cases a multidisciplinary team is required. When surgical excision is mandatory the perioperative management requires the administration of selective α1-adrenergic blocking agents (i.e., doxazosin, prazosin or terazosin) followed by a β-adrenergic blockade (i.e., propranolol, atenolol). This latter should never be started first because blockade of vasodilatory peripheral β-adrenergic receptors with unopposed α-adrenergic receptor stimulation can lead to a further elevation of BP. Although labetalol is traditionally considered the ideal agent due to its α- and β-adrenergic antagonism, experimental studies do not support its use in this clinical setting. As second regimen, the administration of vasodilators as calcium channel blockers (i.e., nicardipine, nifedipine) may be required to control BP. Oral and sublingual short-acting nifedipine are potentially dangerous in patients with hypertensive emergencies and are not recommend. The latest evidences into the diagnosis and treatment of hypertensive crisis due to PH and PG are reviewed here. PMID:23817839

  18. [Gerstmann-Sträussler-Scheinker syndrome with a Pro102Leu mutation in the prion protein gene and atypical MRI findings, hyperthermia, tachycardia, and hyperhidrosis].

    Science.gov (United States)

    Imaiso, Y; Mitsuo, K

    1998-01-01

    A 64-year-old Japanese woman with Gerstmann-Sträussler-Scheinker syndrome (GSS) is reported. She was admitted to our hospital for progressive amnesia, twitching of the right upper limb, and difficulty in speaking and walking for 5 months. Physical examination revealed a fever, tachycardia, and hyperhidrosis without any evidence of inflammation or infection. Neurological examinations demonstrated dementia, frontal lobe signs, and spontaneous myoclonus. She developed akinetic mutism 4 months later. The levels of neuron-specific enolase and 14-3-3 protein were elevated in the cerebrospinal fluid, and serial EEG showed periodic synchronous discharges. DNA analysis of the prion protein gene revealed a Pro102Leu mutation and therefore she was diagnosed as GSS102. Head MRI showed abnormal high signal intensity by T2 weighted image in bilateral caudate nuclei, putamen, frontal lobes, and white matter around the posterior horn of lateral ventricles at admission, and extension to global cerebral cortex and diffuse deep white matter with marked atrophy of bilateral frontal and cerebellar cortices 4 months later. In 123I-IMP SPECT study, uptake of RI decreased slightly only in left frontal region at admission, but decreased markedly in bilateral frontal region 4 months later. Analysis of autonomic function (analysis of noradrenarine in plasma and urine, coefficient of variation of R-R intervals before and after giving atenolol, Aschner's eyeball pressure test, intracutaneous atropine and adrenaline injection test) revealed sympathetic hyperactivity but normal parasympathetic activity. This is a very rare case of GSS102 with atypical MRI findings and clinical features like Creutzfeldt-Jakob disease rather than GSS102, presenting hyperthermia, tachycardia, and hyperhidrosis caused presumably by sympathetic hyperactivity as well as fatal familial insomnia. Therefore it is suggested that some factors besides the codon mutation in the prion protein gene may influence clinical

  19. Biological removal of pharmaceutical compounds using white-rot fungi with concomitant FAME production of the residual biomass.

    Science.gov (United States)

    Vasiliadou, I A; Sánchez-Vázquez, R; Molina, R; Martínez, F; Melero, J A; Bautista, L F; Iglesias, J; Morales, G

    2016-09-15

    The efficiency of two white-rot fungi (WRF), Trametes versicolor and Ganoderma lucidum, to eliminate thirteen pharmaceutical pollutants with concomitant biodiesel production from the accumulating lipid content after treatment, was examined. The removal efficiency was studied using both individual and combined strains. The results of individual and combined strains showed a total removal (100%) of diclofenac (DCF), gemfibrozil (GFZ), ibuprofen (IBP), progesterone (PGT) and ranitidine (RNT). Lower removals were achieved for 4-acetamidoantipyrin (AAA), clofibric acid (ACF), atenolol (ATN), caffeine (CFN), carbamazepine (CZP), hydrochlorothiazide (HCT), sulfamethoxazole (SMX) and sulpiride (SPD), although the combination of both strains enhanced the system's efficiency, with removals ranging from 15 to 41%. This increase of the removal efficiency when combining both strains was attributed to the interactions developed between them (i.e., competition). Results from enzymatic and cytochrome P450 examination suggested that both extracellular (laccase, MnP, LiP) and intracellular oxidation mechanisms participate in the biological removal of pharmaceuticals. On the other hand, the "green" potential of the fungal sludge generated during the biological removal process was assessed for biodiesel production by means of one-step direct (in-situ) transformation. This process consists of the simultaneous extraction and conversion of lipids contained in the sludge by catalytic esterification/transesterification using a robust acid heterogeneous Zr-SBA-15 catalyst. This catalytic system provided conversions close to 80% of the saponifiable fraction (including free fatty acids and glycerides) in the presence of high amount of impurities. The overall weight FAME yield, based on the initial dried mass, was close to 30% for both strains. PMID:27233048

  20. Cardiovascular response to beta-adrenergic blockade or activation in 23 inbred mouse strains.

    Directory of Open Access Journals (Sweden)

    Corinne Berthonneche

    Full Text Available We report the characterisation of 27 cardiovascular-related traits in 23 inbred mouse strains. Mice were phenotyped either in response to chronic administration of a single dose of the beta-adrenergic receptor blocker atenolol or under a low and a high dose of the beta-agonist isoproterenol and compared to baseline condition. The robustness of our data is supported by high trait heritabilities (typically H(2>0.7 and significant correlations of trait values measured in baseline condition with independent multistrain datasets of the Mouse Phenome Database. We then focused on the drug-, dose-, and strain-specific responses to beta-stimulation and beta-blockade of a selection of traits including heart rate, systolic blood pressure, cardiac weight indices, ECG parameters and body weight. Because of the wealth of data accumulated, we applied integrative analyses such as comprehensive bi-clustering to investigate the structure of the response across the different phenotypes, strains and experimental conditions. Information extracted from these analyses is discussed in terms of novelty and biological implications. For example, we observe that traits related to ventricular weight in most strains respond only to the high dose of isoproterenol, while heart rate and atrial weight are already affected by the low dose. Finally, we observe little concordance between strain similarity based on the phenotypes and genotypic relatedness computed from genomic SNP profiles. This indicates that cardiovascular phenotypes are unlikely to segregate according to global phylogeny, but rather be governed by smaller, local differences in the genetic architecture of the various strains.

  1. The corporate bias and the molding of prescription practices: the case of hypertension

    Directory of Open Access Journals (Sweden)

    F.D. Fuchs

    2009-03-01

    Full Text Available Drug management of hypertension has been a noticeable example of the influence of the pharmaceutical industry on prescription practices. The worldwide leading brands of blood pressure-lowering agents are angiotensin receptor-blocking agents, although they are considered to be simply substitutes of angiotensin-converting enzyme (ACE inhibitors. Commercial strategies have been based on the results of clinical trials sponsored by drug companies. Most of them presented distortions in their planning, presentation or interpretation that favored the drugs from the sponsor, i.e., corporate bias. Atenolol, an ineffective blood pressure agent in elderly individuals, was the comparator drug in several trials. In a re-analysis of the INSIGHT trial, deaths appeared to have been counted twice. The LIFE trial appears in the title of more than 120 reproductions of the main and flawed trial, as a massive strategy of scientific marketing. Most guidelines have incorporated the corporate bias from the original studies, and the evidence from better designed studies, such as the ALLHAT trial, have been largely ignored. In trials published recently corporate influences have touched on ethical limits. In the ADVANCE trial, elderly patients with type 2 diabetes and cardiovascular disease or risk factors, allocated to placebo, were not allowed to use diuretic and full doses of an ACE inhibitor, despite the sound evidence of benefit demonstrated in previous trials. As a consequence, they had a 14% higher mortality rate than the participants allocated to the active treatment arm. This reality should be modified immediately, and a greater independence of the academy from the pharmaceutical industry is necessary.

  2. Mapping genetic variants associated with beta-adrenergic responses in inbred mice.

    Directory of Open Access Journals (Sweden)

    Micha Hersch

    Full Text Available β-blockers and β-agonists are primarily used to treat cardiovascular diseases. Inter-individual variability in response to both drug classes is well recognized, yet the identity and relative contribution of the genetic players involved are poorly understood. This work is the first genome-wide association study (GWAS addressing the values and susceptibility of cardiovascular-related traits to a selective β(1-blocker, Atenolol (ate, and a β-agonist, Isoproterenol (iso. The phenotypic dataset consisted of 27 highly heritable traits, each measured across 22 inbred mouse strains and four pharmacological conditions. The genotypic panel comprised 79922 informative SNPs of the mouse HapMap resource. Associations were mapped by Efficient Mixed Model Association (EMMA, a method that corrects for the population structure and genetic relatedness of the various strains. A total of 205 separate genome-wide scans were analyzed. The most significant hits include three candidate loci related to cardiac and body weight, three loci for electrocardiographic (ECG values, two loci for the susceptibility of atrial weight index to iso, four loci for the susceptibility of systolic blood pressure (SBP to perturbations of the β-adrenergic system, and one locus for the responsiveness of QTc (p<10(-8. An additional 60 loci were suggestive for one or the other of the 27 traits, while 46 others were suggestive for one or the other drug effects (p<10(-6. Most hits tagged unexpected regions, yet at least two loci for the susceptibility of SBP to β-adrenergic drugs pointed at members of the hypothalamic-pituitary-thyroid axis. Loci for cardiac-related traits were preferentially enriched in genes expressed in the heart, while 23% of the testable loci were replicated with datasets of the Mouse Phenome Database (MPD. Altogether these data and validation tests indicate that the mapped loci are relevant to the traits and responses studied.

  3. Effects of triclocarban, N,N-diethyl-meta-toluamide, and a mixture of pharmaceuticals and personal care products on fathead minnows (Pimephales promelas).

    Science.gov (United States)

    Zenobio, Jenny E; Sanchez, Brian C; Archuleta, Laura C; Sepulveda, Maria S

    2014-04-01

    Pharmaceuticals and personal care products (PPCPs) have been detected widely in aquatic ecosystems, but little is known about their mechanisms of toxicity. We exposed adult fathead minnows (Pimephales promelas) for 48 h to triclocarban (1.4 µg/L), N,N-diethyl-meta-toluamide (DEET; 0.6 µg/L), or a mixture of PPCPs consisting of atenolol (1.5 µg/L), caffeine (0.25 µg/L), diphenhydramine (0.1 µg/L), gemfibrozil (1.5 µg/L), ibuprofen (0.4 µg/L), naproxen (1.6 µg/L), triclosan (2.3 µg/L), progesterone (0.2 µg/L), triclocarban (1.4 µg/L), and DEET (0.6 µg/L). Quantitative real-time polymerase chain reaction revealed an upregulation in vitellogenin (vtg) in livers of females and males exposed to triclocarban. Also, an upregulation of hepatic lipoprotein lipase (lpl) and a downregulation of androgen receptor (ar) and steroidogenic acute regulatory protein (star) were observed in testes. The group treated with DEET only showed a significant decrease in ar in females. In contrast, the PPCP mixture downregulated vtg in females and males and expression of estrogen receptor alpha (erα), star, and thyroid hormone receptor alpha 1 (thra1) in testes. The authors' results show that the molecular estrogenic effects of triclocarban are eliminated (males) or reversed (females) when dosed in conjunction with several other PPCP, once again demonstrating that results from single exposures could be vastly different from those observed with mixtures. Environ Toxicol Chem 2014;33:910-919. © 2013 SETAC. PMID:24375658

  4. Propranolol sensitizes thyroid cancer cells to cytotoxic effect of vemurafenib.

    Science.gov (United States)

    Wei, Wei-Jun; Shen, Chen-Tian; Song, Hong-Jun; Qiu, Zhong-Ling; Luo, Quan-Yong

    2016-09-01

    Treatment options for advanced metastatic or progressive thyroid cancers are limited. Although targeted therapy specifically inhibiting intracellular kinase signaling pathways has markedly changed the therapeutic landscape, side-effects and resistance of single agent targeted therapy often leads to termination of the treatment. The objective of the present study was to identify the antitumor property of the non-selective β-adrenergic receptor antagonist propranolol for thyroid cancers. Human thyroid cancer cell lines 8505C, K1, BCPAP and BHP27 were used in the present study. Broad β-blocker propranolol and β2-specific antagonist ICI118551, but not β1-specific antagonist atenolol, inhibited the growth of 8505C and K1 cells. Propranolol treatment inhibited growth and induced apoptosis of 8505C cells in vitro and in vivo, which are closely associated with decreased expressions of cyclin D1 and anti-apoptotic Bcl-2. Expression of hexokinase 2 (HK2) and glucose transporter 1 (GLUT1) also decreased following propranolol intervention. 18F-FDG PET/CT imaging of the 8505C xenografts validated shrinkage of the tumors in the propranolol-treated group when compared to the phosphate‑buffered saline treated group. Finally, we found that propranolol can amplify the cytotoxicity of vemurafenib and sensitize thyroid cancer cells to cytotoxic effect of vemurafenib. Our present results suggest that propranolol has potential activity against thyroid cancers and investigation of the combination with targeted molecular therapy for progressive thyroid cancers could be beneficial. PMID:27432558

  5. Occurrence and persistence of organic emerging contaminants and priority pollutants in five sewage treatment plants of Spain: Two years pilot survey monitoring

    International Nuclear Information System (INIS)

    This work summarized all results obtained during almost two-years of a monitoring programme carried out in five municipal sewage treatment plants (STPs) located in the north, centre and south-east of Spain. The study evaluated the occurrence and persistence of a group of 100 organic compounds belonging to several chemical groups (pharmaceuticals, personal care products, pesticides and metabolites). The average removal efficiencies of the STPs studied varied from 20% (erythromycin) to 99% (acetaminophen). In analysed samples, we identified a large number of compounds at mean range concentrations between 7–59,495 ng/L and 5–32,720 ng/L for influent and effluent samples, respectively. This study also identified 20 of the mostly detected and persistent compounds in wastewater effluent, of which hydrochlorothiazide, atenolol, gemfibrozil, galaxolide and three metabolites (fenofibric acid, 4-AAA and 4-FAA), presented the highest average contribution percentages, in relation to the total load of contaminants for the different STPs effluent studied. Highlights: ► The results summarize two-years of a monitoring programme. ► 100 organic compounds (priority substances and emerging contaminants) were analysed. ► The removal efficiency of 5 STPs of Spain was evaluated. ► The presence of target compounds in treated wastewater was also checked. ► The most frequently drugs detected were: antibiotics< anti-inflammatories<β-blockers. - Antibiotics and analgesics/anti-inflammatories were the most frequently drugs detected, following by some β-blockers, synthetic fragrances, lipid regulators and diuretics.

  6. Leptin acts in the forebrain to differentially influence baroreflex control of lumbar, renal, and splanchnic sympathetic nerve activity and heart rate.

    Science.gov (United States)

    Li, Baoxin; Shi, Zhigang; Cassaglia, Priscila A; Brooks, Virginia L

    2013-04-01

    Although leptin is known to increase sympathetic nerve activity (SNA), we tested the hypothesis that leptin also enhances baroreflex control of SNA and heart rate (HR). Using α-chloralose anesthetized male rats, mean arterial pressure (MAP), HR, lumbar SNA (LSNA), splanchnic SNA (SSNA), and renal SNA (RSNA) were recorded before and for 2 hours after lateral cerebroventricular leptin or artificial cerebrospinal fluid administration. Baroreflex function was assessed using a 4-parameter sigmoidal fit of HR and SNA responses to slow ramp (3-5 minutes) changes in MAP, induced by intravenous infusion of nitroprusside and phenylephrine. Leptin (3 μg) increased (P<0.05) basal LSNA, SSNA, RSNA, HR, and MAP, and the LSNA, SSNA, RSNA, and HR baroreflex maxima. Leptin also increased gain of baroreflex control of LSNA and RSNA, but not of SSNA or HR. The elevations in HR were eliminated by pretreatment with methscopalamine, to block parasympathetic nerve activity; however, after cardiac sympathetic blockade with atenolol, leptin still increased basal HR and MAP and the HR baroreflex maximum and minimum. Leptin (1.5 μg) also increased LSNA and enhanced LSNA baroreflex gain and maximum, but did not alter MAP, HR, or the HR baroreflex. Lateral cerebroventricular artificial cerebrospinal fluid had no effects. Finally, to test whether leptin acts in the brain stem, leptin (3 μg) was infused into the 4th ventricle; however, no significant changes were observed. In conclusion, leptin acts in the forebrain to differentially influence baroreflex control of LSNA, RSNA, SSNA, and HR, with the latter action mediated via suppression of parasympathetic nerve activity. PMID:23424232

  7. Perindopril: the evidence of its therapeutic impact in hypertension

    Directory of Open Access Journals (Sweden)

    Andrew Thomson

    2007-03-01

    Full Text Available Andrew Thomson, Mary GreenacreCore Medical Publishing, Knutsford, UKIntroduction: Effective antihypertensive therapy reduces the risk of cardiovascular and cerebrovascular disease and death. Perindopril, a long-acting angiotensin-converting enzyme (ACE inhibitor, is an established antihypertensive agent administered as a once-daily tablet.Aims: To review recent evidence for the use of perindopril in the treatment of hypertension.Evidence review: Evidence shows that perindopril alone or in combination with other antihypertensive agents can achieve clinically significant reductions in blood pressure after 12 weeks of treatment. There is strong evidence from large randomized studies that perindopril-based therapy reduces the risk of cardiovascular outcomes, including mortality, in patients with coronary artery disease and those who have had a prior stroke or transient ischemic attack. There is also some evidence that these effects are greater than those achieved by blood pressure reduction alone, suggesting other drug-related effects including improvements in endothelial function. Recent results have also shown that an amlodipine ± perindopril regimen prevented more major cardiovascular events than an atenolol-based regimen in patients with hypertension, as a result of better control of blood pressure. Economic evidence from one major study shows that, for most patients, the incremental cost per quality-adjusted life-year gained with perindopril 8 mg was lower than the threshold value of €20 000 (73–92% of patients in Europe or £20 000 (94% of patients in the UK.Clinical value: There is strong evidence supporting the use of perindopril-based therapy for the treatment of hypertension and reduction in the risk of cardiovascular disease, stroke, and death in a wide range of patients with stable coronary artery disease or hypertension.Key words: coronary artery disease, evidence-based review, hypertension, perindopril

  8. Anti-hypertensive treatment in pheochromocytoma and paraganglioma: current management and therapeutic features.

    Science.gov (United States)

    Mazza, Alberto; Armigliato, Michela; Marzola, Maria Cristina; Schiavon, Laura; Montemurro, Domenico; Vescovo, Giorgio; Zuin, Marco; Chondrogiannis, Sotirios; Ravenni, Roberta; Opocher, Giuseppe; Colletti, Patrick M; Rubello, Domenico

    2014-04-01

    Pheochromocytoma (PH) and paraganglioma (PG) are neuroendocrine neoplasms arising from chromaffin cells of the adrenal medulla and the sympathetic ganglia, respectively. Although are unusual cause of hypertension (HT) accounting for at most 0.1-0.2 % of cases, they may lead to severe and potentially lethal hypertensive crisis due to the effects of the released catecholamines. However, both PH and PG may be asymptomatic as ~30 % of subjects are normotensive or have orthostatic hypotension and in these cases the 24 h ambulatory blood pressure (BP) monitoring is an important toll to diagnose and treat HT. HT treatment may be difficult when PH or PG occurs in pregnancy or in the elderly subjects and in these cases a multidisciplinary team is required. When surgical excision is mandatory the perioperative management requires the administration of selective α1-adrenergic blocking agents (i.e., doxazosin, prazosin or terazosin) followed by a β-adrenergic blockade (i.e., propranolol, atenolol). This latter should never be started first because blockade of vasodilatory peripheral β-adrenergic receptors with unopposed α-adrenergic receptor stimulation can lead to a further elevation of BP. Although labetalol is traditionally considered the ideal agent due to its α- and β-adrenergic antagonism, experimental studies do not support its use in this clinical setting. As second regimen, the administration of vasodilators as calcium channel blockers (i.e., nicardipine, nifedipine) may be required to control BP. Oral and sublingual short-acting nifedipine are potentially dangerous in patients with hypertensive emergencies and are not recommend. The latest evidences into the diagnosis and treatment of hypertensive crisis due to PH and PG are reviewed here.

  9. Role of wetland organic matters as photosensitizer for degradation of micropollutants and metabolites

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Eunkyung [Department of Civil and Environmental Engineering, Yonsei University, Yonsei-ro 50, Seodaemun-gu, Seoul 120-749 (Korea, Republic of); Shon, Ho Kyong [School of Civil and Environmental Engineering, University of Technology, Sydney (UTS), PO Box 123, Broadway, Sydney 2007, NSW (Australia); Cho, Jaeweon, E-mail: chojw@yonsei.ac.kr [Department of Civil and Environmental Engineering, Yonsei University, Yonsei-ro 50, Seodaemun-gu, Seoul 120-749 (Korea, Republic of)

    2014-07-15

    Highlights: • Photodegradation of PPCPs was investigated in various NOM enriched solutions. • Direct and indirect photolysis experiments were conducted upon UV irradiation. • PPCPs showed different levels of photodegradation rates depending on their photoreactivity. • Allochthonous NOM inhibited the photolysis of target PPCPs. • Wetland NOM enhanced photodegradation of some conservative PPCPs. - Abstract: Overall photodegradation of pharmaceuticals, personal care products (PPCPs) and pharmaceutical metabolites were investigated in order to evaluate their photochemical fate in aquatic environments in various natural organic matter (NOM) enriched solutions. Tested PPCPs exhibited different rates of loss during direct and indirect photolysis. Here, only ultraviolet (UV) light source was used for direct photolysis and UV together with {sup 3}DOM{sup *}for indirect photolysis. Diclofenac and sulfamethoxazole were susceptible to photodegradation, whereas carbamazepine, caffeine, paraxanthine and tri(2-chloroethyl) phosphate (TCEP) showed low levels of photodegradation rate, reflecting their conservative photoreactivity. During indirect photodegradation, in contrast to the hydrophilic autochthonous NOM, allochthonous NOM with relatively high molecular weight (MW), specific ultraviolet absorbance (SUVA) and hydrophobicity (e.g., Suwannee River humic acid (SRHA)) revealed to significantly inhibit the photolysis of target micropollutants. The presence of Typha wetland NOM enhanced the indirect photolysis of well-known conservative micopollutants (carbamazepine and paraxanthine). And atenolol, carbamazepine, glimepiride, and N-acetyl-sulfamethoxazole were found to be sensitive to the triplet excited state of dissolved organic matter ({sup 3}DOM{sup *}) with Typha wetland NOM under deoxygenated condition. This suggests that photolysis in constructed wetlands connected to the wastewater treatment plant can enhance the degradation of some anthropogenic micropollutants

  10. On-line sensor monitoring for chemical contaminant attenuation during UV/H2O2 advanced oxidation process.

    Science.gov (United States)

    Yu, Hye-Weon; Anumol, Tarun; Park, Minkyu; Pepper, Ian; Scheideler, Jens; Snyder, Shane A

    2015-09-15

    A combination of surrogate parameters and indicator compounds were measured to predict the removal efficiency of trace organic compounds (TOrCs) using low pressure (LP)-UV/H2O2 advanced oxidation process (AOP), engaged with online sensor-based monitoring system. Thirty-nine TOrCs were evaluated in two distinct secondary wastewater effluents in terms of estimated photochemical reactivity, as a function of the rate constants of UV direct photolysis (kUV) and hydroxyl radical (OH) oxidation (kOH). The selected eighteen TOrCs were classified into three groups that served as indicator compounds: Group 1 for photo-susceptible TOrCs but with minor degradation by OH oxidation (diclofenac, fluoxetine, iohexol, iopamidol, iopromide, simazine and sulfamethoxazole); Group 2 for TOrCs susceptible to both direct photolysis and OH oxidation (benzotriazole, diphenhydramine, ibuprofen, naproxen and sucralose); and Group 3 for photo-resistant TOrCs showing dominant degradation by OH oxidation (atenolol, carbamazepine, DEET, gemfibrozil, primidone and trimethoprim). The results indicate that TOC (optical-based measurement), UVA254 or UVT254 (UV absorbance or transmittance at 254 nm), and total fluorescence can all be used as suitable on-line organic surrogate parameters to predict the attenuation of TOrCs. Furthermore, the automated real-time monitoring via on-line surrogate sensors and equipped with the developed degradation profiles between sensor response and a group of TOrCs removal can provide a diagnostic tool for process control during advanced treatment of reclaimed waters.

  11. Molecular Modeling Study of Chiral Separation and Recognition Mechanism of β-Adrenergic Antagonists by Capillary Electrophoresis

    Directory of Open Access Journals (Sweden)

    Yifeng Chai

    2012-01-01

    Full Text Available Chiral separations of five β-adrenergic antagonists (propranolol, esmolol, atenolol, metoprolol, and bisoprolol were studied by capillary electrophoresis using six cyclodextrins (CDs as the chiral selectors. Carboxymethylated-β-cyclodextrin (CM-β-CD exhibited a higher enantioselectivity power compared to the other tested CDs. The influences of the concentration of CM-β-CD, buffer pH, buffer concentration, temperature, and applied voltage were investigated. The good chiral separation of five β-adrenergic antagonists was achieved using 50 mM Tris buffer at pH 4.0 containing 8 mM CM-β-CD with an applied voltage of 24 kV at 20 °C. In order to understand possible chiral recognition mechanisms of these racemates with CM-β-CD, host-guest binding procedures of CM-β-CD and these racemates were studied using the molecular docking software Autodock. The binding free energy was calculated using the Autodock semi-empirical binding free energy function. The results showed that the phenyl or naphthyl ring inserted in the hydrophobic cavity of CM-β-CD and the side chain was found to point out of the cyclodextrin rim. Hydrogen bonding between CM-β-CD and these racemates played an important role in the process of enantionseparation and a model of the hydrogen bonding interaction positions was constructed. The difference in hydrogen bonding formed with the –OH next to the chiral center of the analytes may help to increase chiral discrimination and gave rise to a bigger separation factor. In addition, the longer side chain in the hydrophobic phenyl ring of the enantiomer was not beneficial for enantioseparation and the chiral selectivity factor was found to correspond to the difference in binding free energy.

  12. An economic evaluation of antihypertensive therapies based on clinical trials

    Directory of Open Access Journals (Sweden)

    Rosana Lima Garcia Tsuji

    2012-01-01

    Full Text Available OBJECTIVE: Hypertension is a major issue in public health, and the financial costs associated with hypertension continue to increase. Cost-effectiveness studies focusing on antihypertensive drug combinations, however, have been scarce. The cost-effectiveness ratios of the traditional treatment (hydrochlorothiazide and atenolol and the current treatment (losartan and amlodipine were evaluated in patients with grade 1 or 2 hypertension (HT1-2. For patients with grade 3 hypertension (HT3, a third drug was added to the treatment combinations: enalapril was added to the traditional treatment, and hydrochlorothiazide was added to the current treatment. METHODS: Hypertension treatment costs were estimated on the basis of the purchase prices of the antihypertensive medications, and effectiveness was measured as the reduction in systolic blood pressure and diastolic blood pressure (in mm Hg at the end of a 12-month study period. RESULTS: When the purchase price of the brand-name medication was used to calculate the cost, the traditional treatment presented a lower cost-effectiveness ratio [US$/mm Hg] than the current treatment in the HT1-2 group. In the HT3 group, however, there was no difference in cost-effectiveness ratio between the traditional treatment and the current treatment. The cost-effectiveness ratio differences between the treatment regimens maintained the same pattern when the purchase price of the lower-cost medication was used. CONCLUSIONS: We conclude that the traditional treatment is more cost-effective (US$/mm Hg than the current treatment in the HT1-2 group. There was no difference in cost-effectiveness between the traditional treatment and the current treatment for the HT3 group.

  13. Proliferative glomerulonephritis and primary antiphospholipid syndrome

    International Nuclear Information System (INIS)

    Little is known regarding the association of primary antiphospholipid syndrome (APLS) and proliferative glomerulonephiritis (GN). We describe a biopsy-documented case with primary APLS and proliferative (GN) with no evidence of thrombotic microangiopathy (TMA), and in the absence of other manifestations of systematic lupus erythematosus (SLE). She presented initially with left popliteal deep venous thrombosis and nephrotic syndrome. Her first pregnancy at the age of 26 years resulted in the intra-uterine fetal death at term. Two subsequent pregnancies ended up with miscarriages at 3 and 4 months of gestation. Urinalysis revealed glomerular red blood cells of 1.0000.000/ml and granular cast; proteinuria of 13.4grams/24 hours, which was non-selective; hemoglobin 12 gm/dl, normal white blood cell and platelets; serum albumin 2.6gm/dl; anti-nuclear antibody (ANA) and anti DNA were negative and complement levels normal. Lupus anticoagulant was positive leading to a diagnosis of primary APLS. The biopsy findings were consistent with membranoproliferative GN. She continued to have steroid-resistant proteinuria, but stable renal function after a 12-year follow up period. She had 2 pregnancies during this period and was delivered at term using caesarian section. She received heparin during the pregnancies. Later she developed hypertension easily controlled by atenolol. This case provides evidence that primary APLS can be associated with proliferative GN due to immune deposits and not only TMA as previously reported, and in the complete absence of SLE. Performing more renal biopsies in this group of patients may disclose a greater prevalence of proleferative GN and may help in devising a rationale for treatment. (author)

  14. Ivabradine: the evidence of its therapeutic impact in angina

    Directory of Open Access Journals (Sweden)

    Guillaume Marquis-Gravel

    2008-12-01

    Full Text Available Guillaume Marquis-Gravel, Jean-Claude TardifMontreal Heart Institute, Université de Montréal, Montreal, Quebec, CanadaIntroduction: Stable angina pectoris (SAP is a widely prevalent disease affecting 30 000 to 40 000 per million people in Europe and the US. SAP is associated with reductions in quality of life and ability to work, and increased use of healthcare resources. Ivabradine is a drug with a unique therapeutic target, the If current of the sinus node, developed for the treatment of cardiovascular diseases including SAP. It has an exclusive heart rate reducing effect, without any negative effect on left ventricular function or coronary vasodilatation.Aims: The aim of this paper is to review the evidence concerning the use of ivabradine in the treatment of SAP.Evidence review: Ivabradine is an effective antianginal and antiischemic drug, not inferior to the beta blocker atenolol and the calcium channel antagonist (CCA amlodipine. It decreases the frequency of angina attacks and increases the time to anginal symptoms during exercise. Because of its exclusive chronotropic effect, ivabradine is not associated with the typical adverse reactions associated with beta blockers or other antianginal drugs.Clinical value: Clinical evidence shows that ivabradine is a very good antiischemic and antianginal agent, being as effective as beta blockade and CCA therapy in controlling myocardial ischemia and symptoms of stable angina. Ongoing studies will determine the potential of ivabradine to improve morbidity and mortality in coronary artery disease and heart failure.Key words: evidence, If current, ivabradine, outcomes, stable angina pectoris, treatment

  15. Exploring the occurrence and distribution of contaminants of emerging concern through unmanned sampling from ships of opportunity in the North Sea

    Science.gov (United States)

    Brumovský, Miroslav; Bečanová, Jitka; Kohoutek, Jiří; Thomas, Henrike; Petersen, Wilhelm; Sørensen, Kai; Sáňka, Ondřej; Nizzetto, Luca

    2016-10-01

    Chemical pollution is of concern for the marine environment. New European regulation demands exposure and impact assessment to be conducted in coastal environments in order to define and ensure fulfillment of environmental quality standards. A cost-effective approach for monitoring the over 100,000 km of European coasts is necessary. This proof-of-concept study focuses on the use of unmanned water sampling from a commercial ship of opportunity to implement monitoring of marine contaminants of emerging concern. Marine areas that are not directly affected by river plumes or other direct sources were covered in order to provide information on background pollution. 14 currently used pesticides, 11 pharmaceuticals and personal care products and 3 food additives were detected in water samples through targeted analysis at sub-ng to tenths of ng/L levels in both coastal and offshore areas of the North Sea. Among contaminants, 6 pesticides (dimethoate, fenpropimorph, pendimethalin, propiconazole, tebuconazole and temephos), 3 pharmaceuticals (acetaminophen, naproxen and ketoprofen) and 2 food additives (acesulfame and saccharine) have never been detected before in offshore areas. 4 pesticides (diuron, isoproturon, metazachlor and terbuthylazine), 4 pharmaceuticals (carbamazepine, atenolol, ibuprofen and ketoprofen) and 2 food additives (sucralose and acesulfame) were detected in over 90% of the samples. The antibiotic sulfamethoxazole was detected in 50% of the samples at tenths of pg/L levels, including some offshore areas. Our study highlights that the use of ships of opportunity can provide a key support for the development and cost-effective implementation of marine monitoring of chemical pollutants in Europe and elsewhere.

  16. Reactivity of β-blockers/agonists with aqueous permanganate. Kinetics and transformation products of salbutamol.

    Science.gov (United States)

    Rodríguez-Álvarez, Tania; Rodil, Rosario; Quintana, José Benito; Cela, Rafael

    2015-08-01

    The possible oxidation of two β-blockers, atenolol and propranolol, and one β-agonist, salbutamol, with aqueous potassium permanganate (KMnO4) was investigated by liquid chromatography-quadrupole-time-of-flight-mass spectrometry (LC-QTOF-MS). Under strong oxidation conditions (2 mg L(-1) KMnO4, 24 h), only salbutamol did significantly react. In this way, the oxidation kinetics of salbutamol was further investigated at different concentrations of KMnO4, chloride, phosphate and sample pH by means of a full factorial experimental design. Depending on these factors, half-lives were in the range 1-144 min for drug and it was observed that KMnO4 concentration was the most significant factor, resulting in increased reaction rate as it is increased. Moreover, the reaction of salbutamol is also enhanced at basic pH and to a minor extent by the presence of phosphates, being both factors more relevant at low KMnO4 concentrations. The use of an accurate-mass LC-QTOF-MS system permitted the identification of a total of seven transformation products (TPs). The transformation path of the drug begins by the attack of KMnO4 on two double bonds of the aromatic ring of salbutamol via 3 + 2 and 2 + 2 addition reactions, which resulted in the ring opening and that continues with oxidative reactions to finally produce smaller size TPs, ending with tert-butyl-formamide, as the smallest TP identified. Reaction in real samples showed a slower and partial oxidation of the pharmaceutical, due to other competing water organic constituents, but still exceeding 60%. Moreover, the software predicted toxicity of TPs indicates that they are expected not to be more toxic than salbutamol, in contrast to the results obtained for the predicted toxicity of chlorination TPs, excepting predicted developmental toxicity. PMID:25965887

  17. Availability, price and affordability of cardiovascular medicines: A comparison across 36 countries using WHO/HAI data

    Directory of Open Access Journals (Sweden)

    Cameron Alexandra

    2010-06-01

    Full Text Available Abstract Background The global burden of cardiovascular disease (CVD continues to rise. Successful treatment of CVD requires adequate pharmaceutical management. The aim was to examine the availability, pricing and affordability of cardiovascular medicines in developing countries using the standardized data collected according to the World Health Organization/Health Action International methodology. Methods The following medicines were included: atenolol, captopril, hydrochlorothiazide, losartan and nifedipine. Data from 36 countries were analyzed. Outcome measures were percentage availability, price ratios to international reference prices and number of day's wages needed by the lowest-paid unskilled government worker to purchase one month of chronic treatment. Patient prices were adjusted for inflation and purchasing power, procurement prices only for inflation. Data were analyzed for both generic and originator brand products and the public and private sector and summarized by World Bank Income Groups. Results For all measures, there was great variability across surveys. The overall availability of cardiovascular medicines was poor (mean 26.3% in public sector, 57.3% private sector. Procurement prices were very competitive in some countries, whereas others consistently paid high prices. Patient prices were generally substantially higher than international references prices; some countries, however, performed well. Chronic treatment with anti-hypertensive medication cost more than one day's wages in many cases. In particular when monotherapy is insufficient, treatment became unaffordable. Conclusions The results of this study emphasize the need of focusing attention and financing on making chronic disease medicines accessible, in particular in the public sector. Several policy options are suggested to reach this goal.

  18. Electrically enhanced microextraction for highly selective transport of three β-blocker drugs.

    Science.gov (United States)

    Seidi, Shahram; Yamini, Yadollah; Rezazadeh, Maryam

    2011-12-15

    Facilitated transport of three β-blocker drugs including atenolol (ATE), betaxolol (BET) and propranolol (PRO) was investigated under electrical field across a supported liquid membrane (SLM) using phosphoric acid derivatives as selective ion carriers, dissolved in 2-nitro phenyl octyl ether (NPOE). In the presence of di-(2-ethylhexyl) phosphate (DEHP) and tris-(2-ethylhexyl) phosphate (TEHP) in the membrane phase, the three β-blockers showed completely different transport behaviors which enabled highly selective separation of the drugs. Each β-blocker migrated from 3 mL of sample solutions, through a thin layer of specific organic solvent immobilized in the pores of a porous hollow fiber, and into a 15 μL acidic aqueous acceptor solution present inside the lumen of the fiber. The influences of fundamental parameters affecting the transport of target drugs including type of ion carrier for selective separation of each drug and its concentration in the membrane phase, extraction voltage, time of transport, pH of donor and acceptor phases, stirring speed of donor phase and salt effect were studied and optimized. After microextraction process, the extracts were analyzed by high-performance liquid chromatography with ultraviolet detection. Under optimal conditions, ATE was selectively extracted from different saliva samples with recovery of 37%, which corresponded to preconcentration factor of 74. A good linearity was achieved for calibration curve with a coefficient of determination higher than 0.997. Limits of detection and intra-day precision (n=3) were less than 2 μg L(-1) and 8.8%, respectively. PMID:21856103

  19. A rational approach to selecting and ranking some pharmaceuticals of concern for the aquatic environment and their relative importance compared with other chemicals.

    Science.gov (United States)

    Donnachie, Rachel L; Johnson, Andrew C; Sumpter, John P

    2016-04-01

    Aquatic organisms can be exposed to thousands of chemicals discharged by the human population. Many of these chemicals are considered disruptive to aquatic wildlife, and the literature on the impacts of these chemicals grows daily. However, because time and resources are not infinite, research must focus on the chemicals that represent the greatest threat. One group of chemicals of increasing concern is pharmaceuticals, for which the primary challenge is to identify which represent the greatest threat. In the present study, a list of 12 pharmaceuticals was compiled based on scoring the prevalence of different compounds from previous prioritization reviews. These included rankings based on prescription data, environmental concentrations, predicted environmental concentration/predicted no-effect concentration (PEC/PNEC) ratios, persistency/bioaccumulation/(eco)toxicity (PBT), and fish plasma model approaches. The most frequently cited were diclofenac, paracetamol, ibuprofen, carbamazepine, naproxen, atenolol, ethinyl estradiol, aspirin, fluoxetine, propranolol, metoprolol, and sulfamethoxazole. For each pharmaceutical, literature on effect concentrations was compiled and compared with river concentrations in the United Kingdom. The pharmaceuticals were ranked by degree of difference between the median effect and median river concentrations. Ethinyl estradiol was ranked as the highest concern, followed by fluoxetine, propranolol, and paracetamol. The relative risk of these pharmaceuticals was compared with those of metals and some persistent organic pollutants. Pharmaceuticals appear to be less of a threat to aquatic organisms than some metals (Cu, Al, Zn) and triclosan, using this ranking approach. Environ Toxicol Chem 2016;35:1021-1027. © 2015 The Authors. Environmental Toxicology and Chemistry Published by Wiley Periodicals, Inc. on behalf of SETAC. PMID:26184376

  20. Micropollutant degradation via extracted native enzymes from activated sludge.

    Science.gov (United States)

    Krah, Daniel; Ghattas, Ann-Kathrin; Wick, Arne; Bröder, Kathrin; Ternes, Thomas A

    2016-05-15

    A procedure was developed to assess the biodegradation of micropollutants in cell-free lysates produced from activated sludge of a municipal wastewater treatment plant (WWTP). This proof-of-principle provides the basis for further investigations of micropollutant biodegradation via native enzymes in a solution of reduced complexity, facilitating downstream protein analysis. Differently produced lysates, containing a variety of native enzymes, showed significant enzymatic activities of acid phosphatase, β-galactosidase and β-glucuronidase in conventional colorimetric enzyme assays, whereas heat-deactivated controls did not. To determine the enzymatic activity towards micropollutants, 20 compounds were spiked to the cell-free lysates under aerobic conditions and were monitored via LC-ESI-MS/MS. The micropollutants were selected to span a wide range of different biodegradabilities in conventional activated sludge treatment via distinct primary degradation reactions. Of the 20 spiked micropollutants, 18 could be degraded by intact sludge under assay conditions, while six showed reproducible degradation in the lysates compared to the heat-deactivated negative controls: acetaminophen, N-acetyl-sulfamethoxazole (acetyl-SMX), atenolol, bezafibrate, erythromycin and 10,11-dihydro-10-hydroxycarbamazepine (10-OH-CBZ). The primary biotransformation of the first four compounds can be attributed to amide hydrolysis. However, the observed biotransformations in the lysates were differently influenced by experimental parameters such as sludge pre-treatment and the addition of ammonium sulfate or peptidase inhibitors, suggesting that different hydrolase enzymes were involved in the primary degradation, among them possibly peptidases. Furthermore, the transformation of 10-OH-CBZ to 9-CA-ADIN was caused by a biologically-mediated oxidation, which indicates that in addition to hydrolases further enzyme classes (probably oxidoreductases) are present in the native lysates. Although the

  1. Effect of selective β-adrenoceptor blockade and surgical resection of the celiac-superior mesenteric ganglion complex on delayed liquid gastric emptying induced by dipyrone, 4-aminoantipyrine, and antipyrine in rats.

    Science.gov (United States)

    Vinagre, A M; Collares, E F

    2016-03-01

    There is evidence for participation of peripheral β-adrenoceptors in delayed liquid gastric emptying (GE) induced in rats by dipyrone (Dp), 4-aminoantipyrine (AA), and antipyrine (At). The present study aimed to determine whether β-adrenoceptors are involved in delayed GE induced by phenylpyrazole derivatives and the role of the prevertebral sympathetic nervous system in this condition. Male Wistar rats weighing 220-280 g were used in the study. In the first experiment rats were intravenously pretreated with vehicle (V), atenolol 30 mg/kg (ATE, β1-adrenergic antagonist), or butoxamine 25 mg/kg (BUT, β2-adrenergic antagonist). In the second experiment, rats were pretreated with V or SR59230A 2 mg/kg (SRA, β3-adrenergic antagonist). In the third experiment, rats were subjected to surgical resection of the celiac-superior mesenteric ganglion complex or to sham surgery. The groups were intravenously treated with saline (S), 240 µmol/kg Dp, AA, or At, 15 min after pretreatment with the antagonists or V and nine days after surgery. GE was determined 10 min later by measuring the percentage of gastric retention (%GR) of saline labeled with phenol red 10 min after gavage. The %GR (means±SE, n=6) values indicated that BUT abolished the effect of Dp (BUT+Dp vs V+Dp: 35.0%±5.1% vs 56.4%±2.7%) and At (BUT+At vs V+At: 33.5%±4.7% vs 52.9%±2.6%) on GE, and significantly reduced (P<0.05) the effect of AA (BUT+AA vs V+AA: 48.0%±5.0% vs 65.2%±3.8%). ATE, SRA, and sympathectomy did not modify the effects of treatments. These results suggest that β2-adrenoceptor activation occurred in delayed liquid gastric emptying induced by the phenylpyrazole derivatives dipyrone, 4-aminoantipyrine, and antipyrine. Additionally, the released neurotransmitter did not originate in the celiac-superior mesenteric ganglion complex. PMID:26840714

  2. A pilot study on the assessment of trace organic contaminants including pharmaceuticals and personal care products from on-site wastewater treatment systems along Skaneateles Lake in New York State, USA.

    Science.gov (United States)

    Subedi, Bikram; Codru, Neculai; Dziewulski, David M; Wilson, Lloyd R; Xue, Jingchuan; Yun, Sehun; Braun-Howland, Ellen; Minihane, Christine; Kannan, Kurunthachalam

    2015-04-01

    (caffeine) whereas that for PFASs ranged from 7.0 (perfluorobutanesulfonate) to 833 μg/m(2)/day (perfluorooctanoic acid). Based on the ratio of measured concentrations and method detection limit, triclocarban, perfluorooctanoic acid, and perfluorooctanesulfonate have the potential to be used as chemical tracers of septic water contamination in Skaneateles Lake. The median concentrations of atenolol, a beta-blocker drug, in septic water were significantly (ρ = 0.86, p = 0.01) correlated with enterococci counts.

  3. Modulation of the vagal bradycardia evoked by stimulation of upper airway receptors by central 5-HT1 receptors in anaesthetized rabbits

    Science.gov (United States)

    Dando, Simon B; Skinner, Matthew R; Jordan, David; Ramage, Andrew G

    1998-01-01

    The effects of central application of 5-HT1A and 5-HT1B/1D receptor ligands on the reflex bradycardia, apnoea, renal sympathoexcitation and pressor response evoked by stimulating upper airway receptors with smoke in atenolol-pretreated anaesthetized rabbits were studied.Intracisternal administration of the 5-HT1A receptor antagonists WAY-100635 (100 μg kg−1) and (−)pindolol (100 μg kg−1) significantly reduced the smoke-induced bradycardia, attenuated the pressor response and in the case of (−)pindolol, sympathetic nerve activity. The same dose of WAY-100635 i.v. was without effect.Buspirone (200 μg kg−1, i.c.) potentiated the reflex bradycardia. This action was prevented if the animals were pretreated with WAY-100635 (100 μg kg−1, i.v.)(+)8-OH-DPAT (25 μg kg−1, i.c.) attenuated the evoked bradycardia, pressor response, apnoea and renal sympathoexcitation. The attenuation of the apnoea and renal sympathoexcitation, but not the bradycardia or pressor response was prevented in animals pretreated with WAY-100635 (100 μg kg−1, i.v.). The attenuation of the reflex bradycardia and the reduction in the renal sympathoexcitation were reduced by pretreatment with the 5-HT1B/1D receptor antagonist GR127935 (100 μg kg−1, i.v.).In WAY-100635 (100 μg kg−1, i.v.) pretreated animals, sumatriptan (a 5-HT1B/1D receptor agonist) reduced the reflex bradycardia and the pressor response. The 5-HT1B/1D receptor antagonist GR127935 (20 μg kg−1, i.c. or 100 μg kg−1, i.v.) had no effect on the reflex responses.In conclusion, the present data are consistent with the hypothesis that activation of central 5-HT1A receptors potentiate whilst activation of 5-HT1B/1D receptors attenuate the reflex activation of cardiac preganglionic vagal motoneurones evoked by stimulation of upper airway receptors with smoke in rabbits. PMID:9786516

  4. Removal of Organic Micropollutants by Aerobic Activated Sludge

    KAUST Repository

    Wang, Nan

    2013-06-01

    The study examined the removal mechanism of non-acclimated and acclimated aerobic activated sludge for 29 target organic micropollutants (OMPs) at low concentration. The selection of the target OMPs represents a wide range of physical-chemical properties such as hydrophobicity, charge state as well as a diverse range of classes, including pharmaceuticals, personal care products and household chemicals. The removal mechanisms of OMPs include adsorption, biodegradation, hydrolysis, and vaporization. Adsorption and biodegradation were found to be the main routes for OMPs removal for all target OMPs. Target OMPs responded to the two dominant removal routes in different ways: (1) complete adsorption, (2) strong biodegradation and weak adsorption, (3) medium biodegradation and adsorption, and (4) weak sorption and weak biodegradatio. Kinetic study showed that adsorption of atenolol, mathylparaben and propylparaben well followed first-order model (R2: 0.939 to 0.999) with the rate constants ranging from 0.519-7.092 h-1. For biodegradation kinetics, it was found that benzafibrate, bisphenol A, diclofenac, gemfibrozil, ibuprofen, caffeine and DEET followed zero-order model (K0:1.15E-4 to 0.0142 μg/Lh-1, R2: 0.991 to 0.999), while TCEP, naproxen, dipehydramine, oxybenzone and sulfamethoxazole followed first-order model (K1:1.96E-4 to 0.101 h-1, R2: 0.912 to 0.996). 4 Inhibition by sodium azide (NaN3)and high temperature sterilization was compared, and it was found that high temperature sterilization will damage cells and change the sludge charge state. For the OMPs adaptation removal study, it was found that some of OMPs effluent concentration decreased, which may be due to the slow adaptation of the sludge or the increase of certain bacteria culture; some increased due to chromic toxicity of the chemicals; most of the OMPs had stable effluent concentration trend, it was explained that some of the OMPs were too difficutl to remove while other showed strong quick adaptation

  5. Development and validation of methodology SPE-LC-MS/MS for pharmaceuticals and illicit drug determination in the waters of Guarapiranga Dam, Sao Paulo, SP, Brazil

    International Nuclear Information System (INIS)

    This study presents the development of the methodology of solid phase extraction and liquid chromatography - tandem mass spectrometry, SPE-LC-MS/MS, for the determination of 21 (twenty one) pharmaceuticals belonging to different therapeutic groups, 1 (one) illicit drug and its major metabolite, in surface water samples. The chromatographic separation was optimized by studying the performance of different stationary and mobile phases. Quantitation of selected compounds was performed by electrospray ionization (ESI) and the mass spectrometer operating in a multiple reaction monitoring (MRM) mode. The validation of the proposed methodology was performed using the parameters of selectivity, matrix effect, dynamic range, linearity, limit of detection (LOD), limit of quantification (LOQ), precision, accuracy, recovery and robustness. The validation of methodology allowed to apply the methodology in the evaluation of the distribution of the 23 (twenty one) selected compounds, in Guarapiranga Dam waters, an of the major producer system of drinking water of the Metropolitan Region of Sao Paulo (MRSP). The presence of these pollutants in aquatic environments is from the direct release of urban sewage from the homes of your surroundings, as a result of poor sanitation system. The waters of Guarapiranga dam were evaluated in 14 (fourteen) locations strategically chosen and sampled in 3 (three) campaigns of sample collection (August 2011, September 2012 and April 2013). In these samples were quantified acetaminophen (9.6 - 254 ng L-1), atenolol (8.5 - 177 ng L-1), benzoylecgonine (7.9 - 139 ng L-1), caffeine (27 - 27386 ng L-1) carbamazepine (12 - 358 ng L-1), chlorthalidone (9.4 - 35 ng L-1), cocaine (12.8 - 2560 ng L-1), diclofenac (8 - 36 ng L-1), enalapril (20 ng L-1), losartan (6.7 - 114 ng L-1) and valsartan (9.7 - 47 ng L-1). The sample siting GU103-12 (23°41'88.5”S 46°44'67.3”W) was the region with the highest values in the level of concentration of the

  6. Altered β1-3-adrenoceptor influence on α2-adrenoceptor-mediated control of catecholamine release and vascular tension in hypertensive rats

    Directory of Open Access Journals (Sweden)

    Torill eBerg

    2015-04-01

    Full Text Available α2- and β-adrenoceptors (AR reciprocally control catecholamine release and vascular tension. Disorders in these functions are present in spontaneously hypertensive rats (SHR. The present study tested if α2AR dysfunctions resulted from altered α2AR/βAR interaction. Blood pressure was recorded through a femoral artery catheter and cardiac output by an ascending aorta flow probe. Total peripheral vascular resistance (TPR was calculated. Norepinephrine release was stimulated by a 15-min tyramine-infusion, which allows presynaptic release-control to be reflected as differences in overflow to plasma. Surgical stress activated some secretion of epinephrine. L-659,066 (α2AR-antagonist enhanced norepinephrine overflow in normotensive controls (WKY but not SHR. Nadolol (β1+2 and ICI-118551 (β2, but not atenolol (β1 or SR59230A (β(3/1L prevented this increase. All βAR antagonists allowed L-659,066 to augment tyramine-induced norepinephrine overflow in SHR and epinephrine secretion in both strains. Inhibition of cAMP-degradation with milrinone and β3AR agonist (BRL37344 enhanced the effect of L-659,066 on release of both catecholamines in SHR and epinephrine in WKY. β1/2AR antagonists and BRL37344 opposed the L-659,066-dependent elimination of the TPR-response to tyramine in WKY. α2AR/βAR antagonists had little influence on the TPR-response in SHR. Milrinone potentiated the L-659,066-dependent reduction of the TPR-response to tyramine. Conclusions: β2AR activity was a required substrate for α2AR auto inhibition of norepinephrine release in WKY. β1+2AR opposed α2AR inhibition of norepinephrine release in SHR and epinephrine secretion in both strains. βAR-α2AR reciprocal control of vascular tension was absent in SHR. Selective agonist provoked β3AR-Gi signaling and influenced the tyramine-induced TPR-response in WKY and catecholamine release in SHR.

  7. Attenuation of trace organic compounds (TOrCs) inbioelectrochemical systems

    KAUST Repository

    Werner, Craig M.

    2015-04-01

    Microbial fuel cells (MFCs) and microbial electrolysis cells (MECs) are two types of microbial bioelectrochemical systems (BESs) that use microorganisms to convert chemical energy in wastewaters into useful energy products such as (bio)electricity (MFC) or hydrogen gas (MEC). These two systems were evaluated for their capacity to attenuate trace organic compounds (TOrCs), commonly found in municipal wastewater, under closed circuit (current generation) and open circuit (no current generation) conditions, using acetate as the carbon source. A biocide was used to evaluate attenuation in terms of biotransformation versus sorption. The difference in attenuation observed before and after addition of the biocide represented biotransformation, while attenuation after addition of a biocide primarily indicated sorption. Attenuation of TOrCs was similar in MFCs and MECs for eight different TOrCs, except for caffeine and trimethoprim where slightly higher attenuation was observed in MECs. Electric current generation did not enhance attenuation of the TOrCs except for caffeine, which showed slightly higher attenuation under closed circuit conditions in both MFCs and MECs. Substantial sorption of the TOrCs occurred to the biofilm-covered electrodes, but no consistent trend could be identified regarding the physico-chemical properties of the TOrCs tested and the extent of sorption. The octanol-water distribution coefficient at pH 7.4 (log DpH 7.4) appeared to be a reasonable predictor for sorption of some of the compounds (carbamazepine, atrazine, tris(2-chloroethyl) phosphate and diphenhydramine) but not for others (N,N-Diethyl-meta-toluamide). Atenolol also showed high levels of sorption despite being the most hydrophilic in the suite of compounds studied (log DpH 7.4=-1.99). Though BESs do not show any inherent advantages over conventional wastewater treatment, with respect to TOrC removal, overall removals in BESs are similar to that reported for conventional wastewater

  8. Do all β-blockers attenuate the excess hematopoietic progenitor cell mobilization from the bone marrow following trauma/hemorrhagic shock?

    Science.gov (United States)

    Pasupuleti, Latha V.; Cook, Kristin M.; Sifri, Ziad C.; Alzate, Walter D.; Livingston, David H.; Mohr, Alicia M.

    2016-01-01

    BACKGROUND Severe injury results in increased mobilization of hematopoietic progenitor cells (HPC) from the bone marrow (BM) to sites of injury, which may contribute to persistent BM dysfunction after trauma. Norepinephrine is a known inducer of HPC mobilization, and nonselective β-blockade with propranolol has been shown to decrease mobilization after trauma and hemorrhagic shock (HS). This study will determine the role of selective β-adrenergic receptor blockade in HPC mobilization in a combined model of lung contusion (LC) and HS. METHODS Male Sprague-Dawley rats were subjected to LC, followed by 45 minutes of HS. Animals were then randomized to receive atenolol (LCHS + β1B), butoxamine (LCHS + β2B), or SR59230A (LCHS + β3B) immediately after resuscitation and daily for 6 days. Control groups were composed of naive animals. BM cellularity, %HPCs in peripheral blood, and plasma granulocyte-colony stimulating factor levels were assessed at 3 hours and 7 days. Systemic plasma-mediated effects were evaluated in vitro by assessment of BM HPC growth. Injured lung tissue was graded histologically by a blinded reader. RESULTS The use of β2B or β3B following LCHS restored BM cellularity and significantly decreased HPC mobilization. In contrast, β1B had no effect on HPC mobilization. Only β3B significantly reduced plasma G-CSF levels. When evaluating the plasma systemic effects, both β2B and β3B significantly improved BM HPC growth as compared with LCHS alone. The use of β2 and β3 blockade did not affect lung injury scores. CONCLUSION Both β2 and β3 blockade can prevent excess HPC mobilization and BM dysfunction when given after trauma and HS, and the effects seem to be mediated systemically, without adverse effects on subsequent healing. Only treatment with β3 blockade reduced plasma G-CSF levels, suggesting different mechanisms for adrenergic-induced G-CSF release and mobilization of HPCs. This study adds to the evidence that therapeutic strategies that

  9. Characterize Behaviour of Emerging Pollutants in Artificial Recharge: Column Experiments - Experiment Design and Results of Preliminary Tests

    Science.gov (United States)

    Wang, H.; Carrera, J.; Ayora, C.; Licha, T.

    2012-04-01

    Emerging pollutants (EPs) have been detected in water resources as a result of human activities in recent years. They include pharmaceuticals, personal care products, dioxins, flame retardants, etc. They are a source of concern because many of them are resistant to conventional water treatment, and they are harmful to human health, even in low concentrations. Generally, this study aims to characterize the behaviour of emerging pollutants in reclaimed water in column experiments which simulates artificial recharge. One column set includes three parts: influent, reactive layer column (RLC) and aquifer column (AC). The main influent is decided to be Secondary Effluent (SE) of El Prat Wastewater Treatment Plant, Barcelona. The flow rate of the column experiment is 0.9-1.5 mL/min. the residence time of RLC is designed to be about 1 day and 30-40 days for AC. Both columns are made of stainless steel. Reactive layer column (DI 10cm * L55cm) is named after the filling material which is a mixture of organic substrate, clay and goethite. One purpose of the application of the mixture is to increase dissolve organic carbon (DOC). Leaching test in batchs and columns has been done to select proper organic substrate. As a result, compost was selected due to its long lasting of releasing organic matter (OM). The other purpose of the application of the mixture is to enhance adsorption of EPs. Partition coefficients (Kow) of EPs indicate the ability of adsorption to OM. EPs with logKow>2 could be adsorbed to OM, like Ibuprofen, Bezafibrate and Diclofenac. Moreover, some of EPs are charged in the solution with pH=7, according to its acid dissociation constant (Ka). Positively charged EPs, for example Atenolol, could adsorb to clay. In the opposite, negatively charged EPs, for example Gemfibrozil, could adsorb to goethite. Aquifer column (DI 35cm * L1.5m) is to simulate the processes taking place in aquifer in artificial recharge. The filling of AC has two parts: silica sand and

  10. Micropollutant degradation via extracted native enzymes from activated sludge.

    Science.gov (United States)

    Krah, Daniel; Ghattas, Ann-Kathrin; Wick, Arne; Bröder, Kathrin; Ternes, Thomas A

    2016-05-15

    A procedure was developed to assess the biodegradation of micropollutants in cell-free lysates produced from activated sludge of a municipal wastewater treatment plant (WWTP). This proof-of-principle provides the basis for further investigations of micropollutant biodegradation via native enzymes in a solution of reduced complexity, facilitating downstream protein analysis. Differently produced lysates, containing a variety of native enzymes, showed significant enzymatic activities of acid phosphatase, β-galactosidase and β-glucuronidase in conventional colorimetric enzyme assays, whereas heat-deactivated controls did not. To determine the enzymatic activity towards micropollutants, 20 compounds were spiked to the cell-free lysates under aerobic conditions and were monitored via LC-ESI-MS/MS. The micropollutants were selected to span a wide range of different biodegradabilities in conventional activated sludge treatment via distinct primary degradation reactions. Of the 20 spiked micropollutants, 18 could be degraded by intact sludge under assay conditions, while six showed reproducible degradation in the lysates compared to the heat-deactivated negative controls: acetaminophen, N-acetyl-sulfamethoxazole (acetyl-SMX), atenolol, bezafibrate, erythromycin and 10,11-dihydro-10-hydroxycarbamazepine (10-OH-CBZ). The primary biotransformation of the first four compounds can be attributed to amide hydrolysis. However, the observed biotransformations in the lysates were differently influenced by experimental parameters such as sludge pre-treatment and the addition of ammonium sulfate or peptidase inhibitors, suggesting that different hydrolase enzymes were involved in the primary degradation, among them possibly peptidases. Furthermore, the transformation of 10-OH-CBZ to 9-CA-ADIN was caused by a biologically-mediated oxidation, which indicates that in addition to hydrolases further enzyme classes (probably oxidoreductases) are present in the native lysates. Although the

  11. Combination of UV absorbance and electron donating capacity to assess degradation of micropollutants and formation of bromate during ozonation of wastewater effluents.

    Science.gov (United States)

    Chon, Kangmin; Salhi, Elisabeth; von Gunten, Urs

    2015-09-15

    In this study, the changes in UV absorbance at 254 nm (UVA254) and electron donating capacity (EDC) were investigated as surrogate indicators for assessing removal of micropollutants and bromate formation during ozonation of wastewater effluents. To measure the EDC, a novel method based on size exclusion chromatography followed by a post-column reaction was developed and calibrated against an existing electrochemical method. Low specific ozone doses led to a more efficient abatement of EDC than of UVA254. This was attributed to the abatement of phenolic moieties in the dissolved organic matter (DOM), which lose their EDC upon oxidation, but are partially transformed into quinones, which still absorb in the measured UV range. For higher specific ozone doses, the relative EDC abatement was lower than the relative UVA abatement, which can be explained by the oxidation of UV absorbing moieties (e.g. non-activated aromatic compounds), which contribute less to EDC. The abatement of the selected micropollutants (i.e., 17α-ethinylestradiol (EE2), carbamazepine (CBZ), atenolol (ATE), bezafibrate (BZF), ibuprofen (IBU), and p-chlorobenzoic acid (pCBA)) varied significantly depending on their reactivity with ozone in the examined specific ozone dose range of 0-1.45 mgO3/mgDOC. The decrease of EE2 and CBZ with high ozone reactivity was linearly proportional to the reduction of the relative residuals of UVA254 and EDC. The abatement of ATE, BZF, IBU, and pCBA with intermediate to low ozone reactivities was not significant in a first phase (UVA254/UVA254,0 = 1.00-0.70; EDC/EDC0 = 1.00-0.56) while their abatement was more efficient than the degradation of the relative residual UVA254 and much more noticeable than the degradation of the relative residual EDC in a second phase (UVA254/UVA254,0 = 0.70-0.25; EDC/EDC0 = 0.56-0.25) because the partially destroyed UV absorbing and electron donating DOM moieties become recalcitrant to ozone attack. Bromate formation was

  12. A simple HPLC-fluorescence method for the measurement of R,S-sotalol in the plasma of patients with life-threatening cardiac arrhythmias

    Directory of Open Access Journals (Sweden)

    S.R. Santos

    2000-02-01

    Full Text Available R,S-sotalol, a ß-blocker drug with class III antiarrhythmic properties, is prescribed to patients with ventricular, atrial and supraventricular arrhythmias. A simple and sensitive method based on HPLC-fluorescence is described for the quantification of R,S-sotalol racemate in 500 µl of plasma. R,S-sotalol and its internal standard (atenolol were eluted after 5.9 and 8.5 min, respectively, from a 4-micron C18 reverse-phase column using a mobile phase consisting of 80 mM KH2PO4, pH 4.6, and acetonitrile (95:5, v/v at a flow rate of 0.5 ml/min with detection at lex = 235 nm and lem = 310 nm, respectively. This method, validated on the basis of R,S-sotalol measurements in spiked blank plasma, presented 20 ng/ml sensitivity, 20-10,000 ng/ml linearity, and 2.9 and 4.8% intra- and interassay precision, respectively. Plasma sotalol concentrations were determined by applying this method to investigate five high-risk patients with atrial fibrillation admitted to the Emergency Service of the Medical School Hospital, who received sotalol, 160 mg po, as loading dose. Blood samples were collected from a peripheral vein at zero, 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12.0 and 24.0 h after drug administration. A two-compartment open model was applied. Data obtained, expressed as mean, were: CMAX = 1230 ng/ml, TMAX = 1.8 h, AUCT = 10645 ng h-1 ml-1, Kab = 1.23 h-1, a = 0.95 h-1, ß = 0.09 h-1, t(1/2ß = 7.8 h, ClT/F = 3.94 ml min-1 kg-1, and Vd/F = 2.53 l/kg. A good systemic availability and a fast absorption were obtained. Drug distribution was reduced to the same extent in terms of total body clearance when patients and healthy volunteers were compared, and consequently elimination half-life remained unchanged. Thus, the method described in the present study is useful for therapeutic drug monitoring purposes, pharmacokinetic investigation and pharmacokinetic-pharmacodynamic sotalol studies in patients with tachyarrhythmias.

  13. Utility of a transdermal delivery system for antihypertensive therapy. Part 1.

    Science.gov (United States)

    Sclar, D A; Skaer, T L; Chin, A; Okamoto, M P; Gill, M A

    1991-07-18

    A retrospective evaluation of patient-level Medicaid claims data from two states was undertaken to discern the fiscal utility of transdermally delivered clonidine versus both the oral formulation of clonidine and oral formulations of eight other antihypertensive agents. In the first phase of our two-part study, we compared paid claims data (n = 1,135) from Florida for transdermal and oral clonidine. Multivariate regression analysis was used to evaluate the incremental impact of six variables on health-care expenditures in the first year after patients were given a diagnosis of hypertension. These variables were: age, gender, prior utilization of medical services, regimen complexity, and dosage formulation. Patients prescribed transdermal clonidine experienced a significant (p less than or equal to 0.001) increase in prescription expenditures and significant reductions in the use of physician (p less than or equal to 0.05), laboratory (p less than or equal to 0.10), and hospital (p less than or equal to 0.05) services. Moreover, savings were maximized (p less than or equal to 0.001) where multi-drug regimens incorporated the transdermal delivery system. In the second phase of our study we compared paid claims data (n = 8,894) from South Carolina for transdermal clonidine and for nine oral antihypertensive agents: atenolol, captopril, clonidine, diltiazem, enalapril, metoprolol, prazosin, terazosin, and verapamil-SR. Once again, regression analysis was used, this time to evaluate the incremental impact of five variables on health-care expenditures in the first year post diagnosis: age, gender, prior utilization of medical services, regimen complexity, and Medication Possession Ratio (MPR), an index of compliance. The data from part 2 of our study revealed that patients assigned a b.i.d. oral antihypertensive agent experienced a significant reduction (p less than or equal to 0.05) in MPR and a significant (p less than 0.05) increase in health-care expenditures when

  14. Development and validation of methodology SPE-LC-MS/MS for pharmaceuticals and illicit drug determination in the waters of Guarapiranga Dam, Sao Paulo, SP, Brazil; Desenvolvimento e validacao de metodologia SPE-LC-MS/MS para a determinacao de farmacos e droga de abuso nas aguas da represa Guarapiranga, Sao Paulo, SP, Brazil

    Energy Technology Data Exchange (ETDEWEB)

    Shihomatsu, Helena Miho

    2015-07-01

    This study presents the development of the methodology of solid phase extraction and liquid chromatography - tandem mass spectrometry, SPE-LC-MS/MS, for the determination of 21 (twenty one) pharmaceuticals belonging to different therapeutic groups, 1 (one) illicit drug and its major metabolite, in surface water samples. The chromatographic separation was optimized by studying the performance of different stationary and mobile phases. Quantitation of selected compounds was performed by electrospray ionization (ESI) and the mass spectrometer operating in a multiple reaction monitoring (MRM) mode. The validation of the proposed methodology was performed using the parameters of selectivity, matrix effect, dynamic range, linearity, limit of detection (LOD), limit of quantification (LOQ), precision, accuracy, recovery and robustness. The validation of methodology allowed to apply the methodology in the evaluation of the distribution of the 23 (twenty one) selected compounds, in Guarapiranga Dam waters, an of the major producer system of drinking water of the Metropolitan Region of Sao Paulo (MRSP). The presence of these pollutants in aquatic environments is from the direct release of urban sewage from the homes of your surroundings, as a result of poor sanitation system. The waters of Guarapiranga dam were evaluated in 14 (fourteen) locations strategically chosen and sampled in 3 (three) campaigns of sample collection (August 2011, September 2012 and April 2013). In these samples were quantified acetaminophen (9.6 - 254 ng L{sup -1}), atenolol (8.5 - 177 ng L{sup -1}), benzoylecgonine (7.9 - 139 ng L{sup -1}), caffeine (27 - 27386 ng L{sup -1}) carbamazepine (12 - 358 ng L{sup -1}), chlorthalidone (9.4 - 35 ng L{sup -1}), cocaine (12.8 - 2560 ng L{sup -1}), diclofenac (8 - 36 ng L{sup -1}), enalapril (20 ng L{sup -1}), losartan (6.7 - 114 ng L{sup -1}) and valsartan (9.7 - 47 ng L{sup -1}). The sample siting GU103-12 (23°41'88.5”S 46°44'67.3”W) was the

  15. Perindopril: first-line treatment for hypertension.

    Science.gov (United States)

    Zanchetti, A; Desche, P

    1989-01-01

    The antihypertensive efficacy and acceptability of perindopril (P) were compared to those of captopril (C), atenolol (A) and a diuretic, hydrochlorothiazide + amiloride (D), in 3 double-blind parallel multicenter studies involving 165, 173, and 165 patients, respectively. Patients with essential hypertension and a supine DBP between 95 and 125 mmHg (mean 103.9, 106.2, and 105.2 mmHg, respectively) after a 1-month placebo period were randomized to P 4 mg once daily (o.d.) and either C 25 mg twice daily, or A 50 mg o.d. or D (hydrochlorothiazide 50 mg + amiloride 5 mg o.d.) and treated for 3 months, with visits at monthly intervals. If necessary, treatment was adjusted at each visit to control BP (supine DBP less than or equal to 90 mm Hg): firstly by doubling the dose and secondly, one month later, by the addition of a second drug, a diuretic in the studies versus C or A, a beta-blocker in the study versus D. At 3 months, BP control on monotherapy in the three studies was achieved in the following proportion of patients: 49% with P vs 49% with C; 55% with P vs 48% with A; 72% with P vs 72% with D. Most of the patients controlled by P received 4 mg, about 15% were controlled with 8 mg. A further percentage of patients was controlled with combination therapy, the combination with a diuretic being more effective with P than with C (26 vs 8%) or A (23 vs 10%) and the combination with a beta-blocker being less effective with P than with D (5 vs 13%). The total percentage of patients controlled was greater with P than with C (75 vs 57%, p = 0.016) or A (78 vs 58%, p = 0.006) and there was no significant difference between P and D (78 vs 84%). The drop-out rate due to side-effects was up to 6% with P, similar to that observed with C (4%), A (5%) and D (5%). Most of the complaints reported with P were minor and non-specific, their incidence being similar to that observed with the other drugs. Cough was reported with both P (1%) and C (2%) as well as with A (1%) and D (1

  16. EVALUATION OF THE EFFECT OF “WAKOUBA '' ON THE LIPID PROFILE, SYSTOLIC BLOOD PRESSURE (SBP DIASTOLIC (DBP AND BLOOD GLUCOSE IN HYPERTENSIVE RABBITS

    Directory of Open Access Journals (Sweden)

    Tiekpa Wawa J

    2014-11-01

    blood in the kidney and cardiomyopathy. Conclusion: Wakouba at dose (950 mg / kg bw as well as tenordate decreases and normalizes systolic blood pressure (SBP , diastolic blood pressure (DBP and heart rate (HR in hypertension induced rabbit . Furthermore Wakouba (950 mg / kg BW and tenordate (20mg/kg BW increases HDL cholesterol and decrease LDL cholesterol. Wakouba would have the same mechanism of action as tenordate (ATENOLOL + NIFEDIPINE a reference anti hypertensive product, thus anti hypertensive and cardioprotective properties, which justifies it uses in traditional medicine in Cote d’Ivoire as an anti hypertensive.

  17. Analytical strategy based on the use of liquid chromatography and gas chromatography with triple-quadrupole and time-of-flight MS analyzers for investigating organic contaminants in wastewater.

    Science.gov (United States)

    Pitarch, E; Portolés, T; Marín, J M; Ibáñez, M; Albarrán, F; Hernández, F

    2010-08-01

    pollutants that did not form a part of the previous list of target contaminants were identified in the samples, because of the high sensitivity of TOF MS in full-spectrum acquisition mode and the valuable accurate-mass information provided by these instruments. The insecticide diazinon, the fungicide diphenylamide, the UV filter benzophenone, N-butylbenzenesulfonamide (N-BBSA), the insect repellent diethyltoluamide, caffeine, and the pharmaceuticals erythromycin, benzenesulfonanilide, ibuprofen, atenolol, and paracetamol were some of the compounds identified in the water samples analyzed. PMID:20428853

  18. Pharmaceutically active compounds in sludge stabilization treatments: anaerobic and aerobic digestion, wastewater stabilization ponds and composting.

    Science.gov (United States)

    Martín, Julia; Santos, Juan Luis; Aparicio, Irene; Alonso, Esteban

    2015-01-15

    Sewage sludge disposal onto lands has been stabilized previously but still many pollutants are not efficiently removed. Special interest has been focused on pharmaceutical compounds due to their potential ecotoxicological effects. Nowadays, there is scarce information about their occurrence in different sludge stabilization treatments. In this work, the occurrence of twenty-two pharmaceutically active compounds has been studied in sludge from four sludge stabilization treatments: anaerobic digestion, aerobic digestion, composting and lagooning. The types of sludge evaluated were primary, secondary, anaerobically-digested and dehydrated, composted, mixed, aerobically-digested and dehydrated and lagoon sludge. Nineteen of the twenty-two pharmaceutically active compounds monitored were detected in sewage sludge. The most contaminated samples were primary sludge, secondary sludge and mixed sludge (the average concentrations of studied compounds in these sludges were 179, 310 and 142 μg/kg dm, respectively) while the mean concentrations found in the other types of sewage sludge were 70 μg/kg dm (aerobically-digested sludge), 63 μg/kg dm (lagoon sludge), 12 μg/kg dm (composted sludge) and 8 μg/kg dm (anaerobically-digested sludge). The antibiotics ciprofloxacin and norfloxacin were found at the highest concentration levels in most of the analyzed sludge samples (up to 2660 and 4328 μg/kg dm, respectively). Anaerobic-digestion treatment reduced more considerably the concentration of most of the studied compounds than aerobic-digestion (especially in the case of bezafibrate and fluoroquinolones) and more than anaerobic stabilization ponds (in the case of acetaminophen, atenolol, bezafibrate, carbamazepine, 17α-ethinylestradiol, naproxen and salicylic acid). Ecotoxicological risk assessment, of sludge application onto soils, has also been evaluated. Risk quotients, expressed as the ratio between the predicted environmental concentration and the predicted non

  19. Estudio de las fracciones lipídicas de colesterol y triglicéridos en pacientes de dos consultorios médicos de la familia

    Directory of Open Access Journals (Sweden)

    José Luis Cusidó Carralero

    2014-11-01

    Full Text Available La segunda causa de muerte en la provincia de Las Tunas son las enfermedades del corazón, estas se asocian a múltiples factores de riesgo, como, por ejemplo, los niveles elevados de colesterol y triglicéridos. La alta frecuencia de valores patológicos de colesterol y triglicéridos en pacientes de los Consultorios Médicos de la Familia (CMF 19-01 y 20-01 en el Policlínico Docente “Manuel Fajardo Rivero” motivó a la realización de este trabajo, que tiene como objetivo evaluar el comportamiento de las fracciones lipídicas de colesterol y triglicéridos en pacientes de estos CMF, durante el período comprendido entre enero y junio de 2014. Las variables analizadas fueron: rango de valores de colesterol y triglicéridos, edad, sexo, antecedentes patológicos personales, diagnóstico clínico y tratamiento médico. Se incluyeron los pacientes mayores de 20 años de ambos consultorios, los diabéticos, hipertensos, cardiópatas; se excluyeron de la investigación las gestantes, enfermos hospitalizados o con ingreso domiciliario. Se obtuvo como resultado que casi la mitad de los pacientes presentó valores elevados en las fracciones lipídicas de colesterol y triglicéridos, las edades más afectadas fueron los adultos de 41 a 60 años, con predominio del sexo masculino. En la revisión de historias clínicas se tabularon como principales antecedentes patológicos personales que más de la mitad de los pacientes con alteraciones lipídicas son fumadores y un cuarto de ellos consumen alcohol. En el diagnóstico clínico y tratamiento médico registrado en la historia clínica de los pacientes afectados se constató que dos tercios de ellos son hipertensos y utilizan el captopril, enalapril y atenolol y casi un tercio son diabéticos, que se medican con los hipoglucemiantes, insulina y glibenclamida

  20. The Importance of G Protein-Coupled Receptor Kinase 4 (GRK4 in Pathogenesis of Salt Sensitivity, Salt Sensitive Hypertension and Response to Antihypertensive Treatment

    Directory of Open Access Journals (Sweden)

    Brian Rayner

    2015-03-01

    two major hypertension studies, the 65Leu/142Val heterozygote predicted a significantly decreased response to atenolol treatment, and the 65Leu/142Val heterozygote and 486Val homozygote were associated in an additive fashion with adverse cardiovascular outcomes, independent of BP. In conclusion, there is considerable evidence that GRK4 variants are linked to impaired Na excretion, hypertension in animal models and humans, therapeutic response to dietary Na restriction and response to antihypertensive drugs. It may also underlie the difference in hypertension between different geographically derived population groups, and form a basis for pharmacogenomic approaches to treatment of hypertension.

  1. Prevalence of Coronary Artery Intramyocardial Course in a Large Population of Clinical Patients Detected by Multislice Computed Tomography Coronary Angiography

    Energy Technology Data Exchange (ETDEWEB)

    De Rosa, R.; Sacco, M.; Tedeschi, C.; Pepe, R.; Capogrosso, P.; Montemarano, E.; Rotondo, A.; Runza, G.; Midiri, M.; Cademartiri, F. (UO di Radiologia, Ospedale San Gennaro, Napoli (Italy))

    2008-10-15

    Background: Intramyocardial course, an inborn coronary anomaly, is defined as a segment of a major epicardial coronary artery that runs intramurally through the myocardium; in particular, we distinguish myocardial bridging, in which the vessel returns to an epicardial position after the muscle bridge, and intramyocardial course, which is described as a vessel running and ending in the myocardium. Purpose: To evaluate the prevalence of myocardial bridging and intramyocardial course of coronary arteries as defined by multidetector computed tomography (MDCT) angiography. Material and Methods: The study population consisted of 242 consecutive patients (211 men, 31 women; mean age 59+-6 years) with atypical chest pain admitted to our hospital between December 2004 and September 2006. All MDCT examinations were performed using a 16-detector-row scanner (Aquilion 16 CFX; Toshiba Medical System, Tokyo, Japan). Patients with heart rate above 65 bpm received 50 mg atenolol orally for 3 days prior to the MDCT scan, or they increased their usual therapy with beta-blockers, in order to obtain a prescan heart rate <60 bpm. Curved multiplanar and 3D volume reconstructions were performed to explore coronary anatomy. Results: In 235 patients, the CT scan was successful and images were appropriate for evaluation. The prevalence of myocardial bridging and intramyocardial course of coronary arteries was 18.7% (47 cases) in our patient population. In 30 segments (63.8%), the vessels ran and ended in the myocardium. In the remaining 17 segments (36.2%), the vessels returned to an epicardial position after the muscle bridge. We found no difference in the prevalence of this inborn coronary anomaly when comparing different clinical characteristics of the study population (sex, age, body-mass index [BMI], etc.). The mean length of the subepicardial artery was 7 mm (range 5-12 mm), and the mean depth in the diastolic phase was 1.9 mm (range 1.2-2.3 mm). There was no significant difference of

  2. Identification of significant transport processes for organic micropollutant classes during soil aquifer treatment (SAT) - a controlled field experiment

    Science.gov (United States)

    Nödler, Karsten; Licha, Tobias; Sauter, Martin

    2010-05-01

    Supplementing existing water resources with alternative sources of water is a challenge in semi-arid areas, as deterioration of water quality must be avoided. Soil aquifer treatment (SAT) can greatly improve the quality of the injected water by attenuation of organic pollutants via sorption and degradation processes. However, only little is known about the specific transport processes of organic micropollutants under artificial recharge conditions. Organic micropollutants such as pharmaceuticals and their metabolites exhibit a wide range of chemical properties and may undergo very different environmental processes resulting in specific reactions within specified environments. In the presented study fate and transport processes of 25 organic micropollutants (iodinated contrast media, antihypertensive agents, antibiotics, anticonvulsants, lipid regulators, anti-inflammatories, antihistamines and analgesics) were investigated under SAT conditions in a controlled field experiment. Secondary treated effluent (STE) containing the compounds of interest was introduced into the aquifer by an infiltration pond and shallow wells in the vicinity were used for water quality monitoring. By means of strategic sampling procedure and a specialized multi-residue analytical method based on high-performance liquid chromatography / tandem mass spectrometry (LC/MS-MS) 3 main transport processes were identified: 1. Transport of non-polar compounds according to their respective octanol-water distribution coefficient (Kow) 2. Cation exchange 3. Colloidal transport Identification of transport processes 2 & 3 was not expected to act as a transport controlling process. Results of the positively charged beta-blockers sotalol, atenolol and metoprolol gave clear evidence for cation exchange processes of the compounds with the aquifer material. Correlation of turbidity and concentrations of macrolide antibiotics (clarithromycin, erythromycin and roxithromycin) demonstrated the colloidal transport

  3. Source discrimination of drug residues in wastewater: The case of salbutamol.

    Science.gov (United States)

    Depaolini, Andrea Re; Fattore, Elena; Cappelli, Francesca; Pellegrino, Raffaele; Castiglioni, Sara; Zuccato, Ettore; Fanelli, Roberto; Davoli, Enrico

    2016-06-15

    Analytical methods used for pharmaceuticals and drugs of abuse in sewage play a fundamental role in wastewater-based epidemiology (WBE) studies. Here quantitative analysis of drug metabolites in raw wastewaters is used to determine consumption from general population. Its great advantage in public health studies is that it gives objective, real-time data about community use of chemicals, highlighting the relationship between environmental and human health. Within a WBE study on salbutamol use in a large population, we developed a procedure to distinguish human metabolic excretion from external source of contamination, possibly industrial, in wastewaters. Salbutamol is mainly excreted as the sulphate metabolite, which is rapidly hydrolyzed to the parent compound in the environment, so this is currently not detected. When a molecule is either excreted un-metabolized or its metabolites are unstable in the environment, studies can be completed by monitoring the parent compound. In this case it is mandatory to assess whether the drug in wastewater is present because of population use or because of a specific source of contamination, such as industrial manufacturing waste. Because commercial salbutamol mainly occurs as a racemic mixture and is stereoselective in the human metabolism, the enantiomeric relative fraction (EFrel) in wastewater samples should reflect excretion, being unbalanced towards one of two enantiomers, if the drug is of metabolic origin. The procedure described involves chiral analysis of the salbutamol enantiomers by liquid chromatography-tandem mass spectrometry (LC-MS-MS) and calculation of EFrel, to detect samples where external contamination occurs. Samples were collected daily between October and December 2013 from the Milano Nosedo wastewater treatment plant. Carbamazepine and atenolol were measured in the sewage collector, as "control" drugs. Salbutamol EFrel was highly consistent in all samples during this three-month period, but a limited

  4. Uso de medicamentos en hipertensión arterial en el primer nivel de atención pública argentina. La experiencia del Programa Remediar

    Directory of Open Access Journals (Sweden)

    Ricardo G. Bernztein

    2009-01-01

    Full Text Available La hipertensión arterial (HTA es un motivo frecuente de prescripción. La Argentina fueafectada a fines de 2001 por una severa crisis socioeconómica que disminuyó el acceso de lapoblación a los medicamentos, con los consiguientes riesgos sanitarios. Como respuesta desdeel Estado, se implementó el Programa Remediar para proveer en forma gratuita medicamentosa la población de escasos recursos y sin cobertura social.ObjetivosAnalizar el uso de medicamentos antihipertensivos en la población atendida en el primernivel de atención (PNA pública de la Argentina y estimar en forma proyectada su efectividaden términos de cobertura de la población esperada con HTA.Material y métodosEl presente es un estudio ecológico con cruce de diagnósticos, prescripciones y beneficiariospor provincia de las recetas del Programa Remediar. Población objetivo: pacientes con diagnósticode HTA atendidos en 6 mil centros de salud de la Argentina desde marzo de 2005hasta febrero de 2006.ResultadosEn 15 millones de recetas, la frecuencia referida de HTA fue del 10,4%: 126.097 recetasmensuales. Este porcentaje no fue homogéneo, ya que resultó 3 a 4 veces mayor en la ciudadde Buenos Aires y la provincia de La Pampa que en las provincias de Jujuy o Salta. Lafrecuencia de prescripción fue: enalapril 77,0%, atenolol 22,1%, hidroclorotiazida 12,5% yaspirina 7,1%. Sobre la base de estadísticas poblacionales previas y la prevalencia esperadade HTA, se pudo estimar que el Programa Remediar alcanzó a cubrir porcentajes variablesde la población con cobertura pública exclusiva: 57,3% en todo el país, con grandes variaciones.El 74,9% de los beneficiarios hipertensos recibió tratamientos suficientes para 4 o menosmeses por año.ConclusiónLa utilización de tiazidas y de aspirina fue menor que la esperada de acuerdo con las guíasde práctica clínica basada en evidencias. Es posible que el impacto sanitario positivo de laprovisión de medicamentos se haya visto

  5. Removal of micro pollutants using activated biochars and powdered activated carbon in water

    Science.gov (United States)

    Kim, E.; Jung, C.; Han, J.; Son, A.; Yoon, Y.

    2015-12-01

    Recent studies have suggested that emerging micropollutants containing endocrine disrupting compounds (EDCs); bisphenol A, 17 α-ethinylestradiol, 17 β-estradiol and pharmaceuticals and personal care products (PPCPs); sulfamethoxazole, carbamazepine, ibuprofen, atenolol, benzophenone, benzotriazole, caffeine, gemfibrozil, primidone, triclocarban in water have been linked to ecological impacts, even at trace concentrations (sub ug/L). Adsorption with adsorbent such as activated carbon having a high-binding affinity has been widely used to eliminate various contaminants in the aqueous phase. Recently, an efficient treatment strategy for EDCs and PPCPs has been considered by using cost effective adsorption particularly with biochar in aqueous environmentIn this study, the objective of this study is to determine the removal of 13 target EDCs/PPCPs having different physicochemical properties by a biochar at various water quality conditions (pH (3.5, 7, and 10.5), background ions (NaCl, CaCl2, Na₂SO₄), ionic strength, natural organic matter (NOM)). The activated biochar produced in a laboratory was also characterized by using conventional analytical methods as well as advanced solid-state nuclear magnetic resonance (NMR) techniques, which answer how these properties determine the competitive adsorption characteristics and mechanisms of EDCs and PPCPs.The primary findings suggest that micropollutants can be removed more effectively by the biochar than the commercially available powdered activated carbon. At pH values below the pKa of each compound, the adsorption affinity toward adsorbents increased significantly with the pH, whereas the adsorption affinity decreased significantly at the pH above the pKa values. Na+ did not significantly impact adsorption, while increasing the concentration of Ca2+lead to increase in the adsorption of these micropollutants. NOM adsorption with humic acids on these adsorbents disturbed adsorption capacity of the target compounds as

  6. Mechanism considerations for photocatalytic oxidation, ozonation and photocatalytic ozonation of some pharmaceutical compounds in water.

    Science.gov (United States)

    Rodríguez, Eva M; Márquez, Gracia; León, Elena A; Álvarez, Pedro M; Amat, Ana M; Beltrán, Fernando J

    2013-09-30

    Aqueous solutions of four pharmaceutical compounds, belonging to the group of emergent contaminants of water: atenolol (ATL), hydrochlorothiazide (HCT), ofloxacin (OFX) and trimethoprim (TMP), have been treated with different oxidation systems, mainly, photocatalytic oxidation, ozonation and photocatalytic ozonation. TiO2 has been used as semiconductor for photocatalytic reactions both in the presence of air, oxygen or ozone-oxygen gas mixtures. Black light lamps mainly emitting at 365 nm were the source of radiation. In all cases, the influence of some variables (concentrations of semiconductor, ozone gas and pharmaceuticals and pH) on the removal of pharmaceuticals, total polyphenol content (TPC) and total organic carbon (TOC) was investigated. A discussion on the possible routes of pharmaceutical and intermediates (as TPC and TOC) elimination has been developed. Thus, OFX TiO2/UVA degradation mechanism seems to develop through the participation of non-hydroxyl free radical species. Furthermore, the presence of OFX inhibits the formation of hydroxyl radicals in the photocatalytic process. The most effective processes were those involving ozone that lead to complete disappearance of parent compounds in less than 30 min for initial pharmaceutical concentrations lower than 2.5 mg L(-1). In the ozonation systems, regardless of the pH and the presence of TiO2, pharmaceuticals are degraded through their direct reaction with ozone. Photocatalytic ozonation was the most efficient process for TPC and TOC removals (≥ 80% and ≥60% elimination after 2 h of treatment, respectively) as well as in terms of the ozone consumption efficiency (1, 5.5 and 4 mol of ozone consumed per mol of TOC mineralized, at pH 4, 7 and 9, respectively). Weakly acid conditions (pH 4) resulted to be the most convenient ones for TPC and TOC removal by photocatalytic ozonation. This was likely due to formation of hydroxyl radicals through the ozonide generated at these conditions. PMID

  7. A pilot study on the assessment of trace organic contaminants including pharmaceuticals and personal care products from on-site wastewater treatment systems along Skaneateles Lake in New York State, USA.

    Science.gov (United States)

    Subedi, Bikram; Codru, Neculai; Dziewulski, David M; Wilson, Lloyd R; Xue, Jingchuan; Yun, Sehun; Braun-Howland, Ellen; Minihane, Christine; Kannan, Kurunthachalam

    2015-04-01

    (caffeine) whereas that for PFASs ranged from 7.0 (perfluorobutanesulfonate) to 833 μg/m(2)/day (perfluorooctanoic acid). Based on the ratio of measured concentrations and method detection limit, triclocarban, perfluorooctanoic acid, and perfluorooctanesulfonate have the potential to be used as chemical tracers of septic water contamination in Skaneateles Lake. The median concentrations of atenolol, a beta-blocker drug, in septic water were significantly (ρ = 0.86, p = 0.01) correlated with enterococci counts. PMID:25466637

  8. Metoprolol-induced visual hallucinations: a case series

    Directory of Open Access Journals (Sweden)

    Goldner Jonathan A

    2012-02-01

    Full Text Available Abstract Introduction Metoprolol is a widely used beta-adrenergic blocker that is commonly prescribed for a variety of cardiovascular syndromes and conditions. While central nervous system adverse effects have been well-described with most beta-blockers (especially lipophilic agents such as propranolol, visual hallucinations have been only rarely described with metoprolol. Case presentations Case 1 was an 84-year-old Caucasian woman with a history of hypertension and osteoarthritis, who suffered from visual hallucinations which she described as people in her bedroom at night. They would be standing in front of the bed or sitting on chairs watching her when she slept. Numerous medications were stopped before her physician realized the metoprolol was the causative agent. The hallucinations resolved only after discontinuation of this medication. Case 2 was a 62-year-old Caucasian man with an inferior wall myocardial infarction complicated by cardiac arrest, who was successfully resuscitated and discharged from the hospital on metoprolol. About 18 months after discharge, he related to his physician that he had been seeing dead people at night. He related his belief that since he 'had died and was brought back to life', he was now seeing people from the after-life. Upon discontinuation of the metoprolol the visual disturbances resolved within several days. Case 3 was a 68 year-old Caucasian woman with a history of severe hypertension and depression, who reported visual hallucinations at night for years while taking metoprolol. These included awakening during the night with people in her bedroom and seeing objects in her room turn into animals. After a new physician switched her from metoprolol to atenolol, the visual hallucinations ceased within four days. Conclusion We suspect that metoprolol-induced visual hallucinations may be under-recognized and under-reported. Patients may frequently fail to acknowledge this adverse effect believing that they

  9. Removal of organic micropollutants in an artificial recharge system

    Science.gov (United States)

    Valhondo, C.; Nödler, K.; Köck-Schulmeyer, M.; Hernandez, M.; Licha, T.; Ayora, C.; Carrera, J.

    2012-04-01

    . Water from the Infiltration pond, the unsaturated zone and groundwater have been sampled and analyzed in order to elucidate the effect of the reactive layer. First results of micropollutants under natural conditions show significant removal rates of atenolol and Ibuprofen as well as the recalcitrant behaviour of carbamazepine. Once the layer was installed, carbamazepine concentration in groundwater samples was lower than the concentration in the infiltration water. These preliminary results are promising but, however, they need to be confirmed by further analysis, which will be conducted during the next weeks.

  10. Sorption of structurally different ionized pharmaceutical and illicit drugs to a mixed-mode coated microsampler.

    Science.gov (United States)

    Peltenburg, Hester; Timmer, Niels; Bosman, Ingrid J; Hermens, Joop L M; Droge, Steven T J

    2016-05-20

    The mixed-mode (C18/strong cation exchange-SCX) solid-phase microextraction (SPME) fiber has recently been shown to have increased sensitivity for ionic compounds compared to more conventional sampler coatings such as polyacrylate and polydimethylsiloxane (PDMS). However, data for structurally diverse compounds to this (prototype) sampler coating are too limited to define its structural limitations. We determined C18/SCX fiber partitioning coefficients of nineteen cationic structures without hydrogen bonding capacity besides the charged group, stretching over a wide hydrophobicity range (including amphetamine, amitriptyline, promazine, chlorpromazine, triflupromazine, difenzoquat), and eight basic pharmaceutical and illicit drugs (pKa>8.86) with additional hydrogen bonding moieties (MDMA, atenolol, alprenolol, metoprolol, morphine, nicotine, tramadol, verapamil). In addition, sorption data for three neutral benzodiazepines (diazepam, temazepam, and oxazepam) and the anionic NSAID diclofenac were collected to determine the efficiency to sample non-basic drugs. All tested compounds showed nonlinear isotherms above 1mmol/L coating, and linear isotherms below 1mmol/L. The affinity for C18/SCX-SPME for tested organic cations without Hbond capacities increased with longer alkyl chains, ranging from logarithmic fiber-water distribution coefficients (log Dfw) of 1.8 (benzylamine) to 5.8 (triflupromazine). Amines smaller than benzylamine may thus have limited detection levels, while cationic surfactants with alkyl chain lengths >12 carbon atoms may sorb too strong to the C18/SCX sampler which hampers calibration of the fiber-water relationship in the linear range. The log Dfw for these simple cation structures closely correlates with the octanol-water partition coefficient of the neutral form (Kow,N), and decreases with increased branching and presence of multiple aromatic rings. Oxygen moieties in organic cations decreased the affinity for C18/SCX-SPME. Log Dfw values of

  11. Anestesia para salpingectomia parcial bilateral em paciente com miocardiopatia hipertrófica idiopática: relato de um caso e revisão da literatura Anestesia para salpingectomía parcial bilateral en paciente con miocardiopatía hipertrófica idiopática: relato de un caso y revisión del literatura Anesthesia for partial bilateral salpingectomy in a patient with idiopathic hypertrophic cardiomyopathy: case report and review of the literature

    Directory of Open Access Journals (Sweden)

    Ana Sofia Del Castillo Sardi

    2010-02-01

    Full Text Available JUSTIFICATIVA E OBJETIVOS: A miocardiopatia hipertrófica é uma doença cardíaca rara, com transmissão autossômica dominante e que se caracteriza pela hipertrofia do septo ventricular e pelas anormalidades da valva mitral. RELATO DO CASO: Paciente secundípara, de 25 anos, com diagnóstico de miocardiopatia hipertrófica há quatro anos e antecedente de asma leve intermitente controlada com inalações esporádicas de corticosteroides. Apresentava sopro holossistólico IV/VI plurifocal e importante escoliose, com os espaços intervertebrais palpáveis. Acusou palpitações esporádicas durante toda a gravidez e recebia medicação de 100 mg de atenolol por dia. Apresentava hemograma, creatinina e eletrólitos dentro dos limites normais, ecocardiograma com miocardiopatia hipertrófica de predomínio septal, com fração de ejeção sistólica de 0,76%. A paciente entrou em trabalho de parto de rápida evolução e nasceu criança viva, do sexo feminino, com APGAR 9/9 sem complicações maternas nem fetais. Foi realizada a programação para a realização de salpingectomia parcial bilateral. Em consulta, a paciente negou-se a receber anestesia para o procedimento. A técnica anestésica de eleição foi a regional combinada. O procedimento cirúrgico durou 20 minutos e as mudanças de pressão arterial junto com a frequência cardíaca foram 10% menores que as dos valores iniciais, sem complicações hemodinâmicas nem cirúrgicas imediatas. CONCLUSÕES: A mortalidade absoluta materna com miocardiopatia hipertrófica (MH é muito baixa e costuma aparecer em mulheres com fatores de alto risco. Não há evidências de que a anestesia regional aumente o risco em mulheres com MH quando é utilizada para o parto vaginal. Tanto a anestesia geral como a regional foram utilizadas com sucesso e sem complicações em cesarianas de parturientes com MH.JUSTIFICATIVA Y OBJETIVOS: La cardiomiopatía hipertrófica es enfermedad cardíaca rara, con transmisi

  12. Anestesia para cesariana em paciente portadora de cardiomiopatia hipertrófica familiar: relato de caso Anestesia para cesária en paciente portadora de cardiomiopatía hipertrófica familiar: relato de caso Anesthesia for cesarean section in a patient with familiar hypertrophic cardiomyopathy: case report

    Directory of Open Access Journals (Sweden)

    Renato Mestriner Stocche

    2007-12-01

    Full Text Available JUSTIFICATIVA E OBJETIVOS: A cardiomiopatia hipertrófica familiar (CHF é uma doença cardíaca rara, com transmissão hereditária, caracterizada por hipertrofia do septo ventricular e grau variável de estenose aórtica subvalvar. Nessa doença, o aumento da contratilidade do miocárdio e a diminuição da resistência vascular periférica podem agravar a obstrução da via de saída do VE, produzindo disritmia e isquemia cardíaca. Este relato objetivou discutir o manuseio anestésico para cesariana em paciente com CHF. RELATO DO CASO: Paciente com 33 semanas de gestação e diagnóstico prévio de CHF apresentou no holter de 24 horas 22 episódios de taquicardia ventricular não-sustentada (TVNS e dois episódios de taquicardia ventricular sustentada (TVS. Referia episódios de palpitação, dispnéia e dor precordial de curta duração. A paciente foi medicada com atenolol e apresentou controle dos sintomas e das disritmias cardíacas. Com 38 semanas e 5 dias de gestação a paciente foi submetida à cesariana eletiva. Além do habitual a monitorização contou com análise de segmento ST e pressão arterial invasiva. Utilizou-se anestesia raquiperidural com injeção de 5 µg de sunfentanil na raqui seguida de administração de bupivacaína a 0,375% em doses de incremento até atingir altura de T6 (total de 16 mL. Utilizou-se metaraminol como vasopressor. Não houve hipotensão arterial materna ou outras complicações no perioperatório. CONCLUSÕES: A anestesia geral é freqüentemente utilizada para cesarianas de pacientes com CHF. A anestesia raquiperidural com instalação lenta do bloqueio foi uma alternativa segura. Nessas pacientes, o aumento da contratilidade miocárdica deve ser evitado, devendo-se, se necessário, utilizar-se um a-agonista para correção de hipotensão arterial materna.JUSTIFICATIVA Y OBJETIVOS: La cardiomiopatía hipertrófica familiar (CHF es una enfermedad cardiaca rara con transmisión hereditaria

  13. Effect of fosinopril on progression of the asymptomatic carotid atherosclerosis and left ventricular hypertrophy in hypertensive patients

    Directory of Open Access Journals (Sweden)

    Tasić Ivan

    2006-01-01

    Full Text Available INTRODUCTION The cardiovascular changes (vascular structure changes, hypertrophy of the left ventricle contribute to both the increased cardiovascular morbidity and the mortality of essential hypertension. Therefore, modern treatment strategies should not only target blood pressure (BP reduction but also normalize cardiovascular structure and function. OBJECTIVE Aim of the study was to determine the effect of the ACE inhibitor Fosinopril on the Intima-media thickness of the common carotid artery and on the left ventricle mass after 9-month treatment of hypertensive patients. METHOD The study included 40 patients with the arterial hypertension and the left ventricle hypertrophy verified by echocardiography. The patients were randomized on A ACE-inhibitor - Fosinopril and 6 without ACE inhibitor - atenolol, and they were followed up 9 months. The groups were not different by age, sex, and metabolic status. Color Duplex ultrasonography of the carotid arteries was performed by Acuson Sequia C236 with high-frequency linear probe of 8 MHz. The Intima-media thickness of the common carotids on the left and the right was measured in diastole at 1.5. cm from the highest point of bifurcation under maximal magnification. Using the same device, the left ventricle mass and other parameters of the left ventricle were determined in M-mode and by means of 2D image. RESULTS After 9 months, BP In both groups Was reduced In similar range (group A: systolic BP from 158 to 137 mmHg, and diastolic BP from 94 to 85 mmHg, and group B; systolic BP from 164 to 137 mmHg, and diastolic BP from 87 to 84 mmHg. The thickness of the intimomedial complex in patients using Fosinopril was decreased by 0.0278 ± 0.03 mm, while in the group of patients that did not use the ACE-inhibitor, it was increased by 0.078 ±0.13 mm. The left ventricle mass in patients using Fosinopril was decreased by 5 grams (312 ± 72 g vs. 307 ± 77 g, while in group B patients, it was increased by 15

  14. Occurrence and fate of pharmaceutically active compounds in the environment, a case study: Hoeje River in Sweden

    International Nuclear Information System (INIS)

    (B) were used as natural inert tracers to estimate the relative extent of dilution of PhACs measured in the effluent of the STP on concentrations measured further downstream. Based on spatial trends of concentrations (recalculated to reflect a hypothetical scenario with no dilution), ibuprofen, ketoprofen, naproxen and dicofenac were shown to be subject to significant abiotic or biotic transformations or physical sequestration in the river. The β-blockers atenolol, metoprolol and propanolol, the antibiotics trimetoprim and sulfametoxazole, and carbamazepine demonstrated a high degree of persistence. Fluctuations in the concentration of carbamazepine and gemfibrozil were observed along the series of reservoirs and within the river and are hypothesized to be due to release of parent compound from glucuronides. Several of the investigated substances (metaprolol, propanolol and carbamazepin) that exhibit low excretion rates as parent compounds demonstrate a surprising persistence in the aquatic environment. It is concluded that pharmaceutical substances with a high metabolic rate in humans (low excretion rate) do not necessarily induce a short lifetime in aquatic environments. Results from this study emphasize the need for a broader view on the concept of persistence that accounts for loading rates, in addition to removal mechanisms (e.g., transformation, volatility and physical sequestration by solids), under a variety of spatial and temporal scales

  15. Removal of a wide range of emerging pollutants from wastewater treatment plant discharges by micro-grain activated carbon in fluidized bed as tertiary treatment at large pilot scale.

    Science.gov (United States)

    Mailler, R; Gasperi, J; Coquet, Y; Buleté, A; Vulliet, E; Deshayes, S; Zedek, S; Mirande-Bret, C; Eudes, V; Bressy, A; Caupos, E; Moilleron, R; Chebbo, G; Rocher, V

    2016-01-15

    Among the solutions to reduce micropollutant discharges into the aquatic environment, activated carbon adsorption is a promising technique and a large scale pilot has been tested at the Seine Centre (240,000 m(3)/d - Paris, France) wastewater treatment plant (WWTP). While most of available works studied fixed bed or contact reactors with a separated separation step, this study assesses a new type of tertiary treatment based on a fluidized bed containing a high mass of activated carbon, continuously renewed. For the first time in the literature, micro-grain activated carbon (μGAC) was studied. The aims were (1) to determine the performances of fluidized bed operating with μCAG on both emerging micropollutants and conventional wastewater quality parameters, and (2) to compare its efficiency and applicability to wastewater to former results obtained with PAC. Thus, conventional wastewater quality parameters (n=11), pharmaceuticals and hormones (PPHs; n=62) and other emerging pollutants (n=57) have been monitored in μGAC configuration during 13 campaigns. A significant correlation has been established between dissolved organic carbon (DOC), PPHs and UV absorbance at 254 nm (UV-254) removals. This confirms that UV-254 could be used as a tertiary treatment performance indicator to monitor the process. This parameter allowed identifying that the removals of UV-254 and DOC reach a plateau from a μGAC retention time (SRT) of 90-100 days. The μGAC configuration substantially improves the overall quality of the WWTP discharges by reducing biological (38-45%) and chemical oxygen demands (21-48%), DOC (13-44%) and UV-254 (22-48%). In addition, total suspended solids (TSS) are retained by the μGAC bed and a biological activity (nitratation) leads to a total elimination of NO2(-). For micropollutants, PPHs have a good affinity for μGAC and high (>60%) or very high (>80%) removals are observed for most of the quantified compounds (n=22/32), i.e. atenolol (92

  16. 超高效液相色谱-串联质谱法同时检测地表水中18种药物与个人护理品的残留量%Simultaneous determination of 18 pharmaceuticals and personal care products in surface water by ultra-high performance liquid chromatography-tandem mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    朱赛嫦; 王静; 邵卫伟; 陈红

    2013-01-01

    An analytical method has been developed and validated for the simultaneous determination of 18 Pharmaceuticals and personal care products (PPCPs) , including antibiotics (tri-methoprim, erythromycin · 2H2O, norfloxacin, ofloxacin, pencilline G, penicillin V potassium salt, cephalexin and sulfamethoxazole) , β-bloker (atenolol), anophelifuge (N, N-diethyl-3-methylbenzoylamide, DEET) , antiepileptics ( carbamazepine) , central nervous system stimulant (caffeine) , lipid modifying agent ( clofibric acid) , non-steroidal anti-inflammatory drugs (ibuprofen, naproxen and diclofenac sodium salt) and antimicrobial agents (triclosan and tri-clocarban). The detection and qualification of the target compounds were performed by ultra-high performance liquid chromatography-tandem mass spectrometry. The optimized mobile phases were methanol as organic phase, 0. 3% (v/v) formic acid-5 mmol/L ammonium acetate for positive electrospray ionization (ESI+ ) and 5 mmol/L ammonium acetate for ESI- as inorganic phase. Water samples were concentrated by solid phase extraction at 2 mL/min, and all the target PPCPs were efficiently extracted at pH 7. The extracted PPCPs were eluted by the mixture of methanol and acetonitrile (1:1, v/v). The average recoveries of the target compounds in the spiked pure water samples ranged from 53. 9% - 112%. The average recoveries of the target compounds ranged from 45. 1% - 156. 6% with the relative standard deviations ranged from 2. 4% - 15. 7%, in the surface water samples spiked at 100 ng/L. The surface water samples collected from Yu Hangtang River in Hangzhou were detected. The results showed that nine PPCPs were detected including caffeine that reached a maximum concentration of 550. 7 ng/L. It proved that this analytical method is reliable and acceptable.%采用固相萃取对水样进行预处理,建立了同时检测地表水中包括抗生素、β-阻滞剂、驱蚊剂、抗癫痫药、中枢神经兴奋剂、血脂调节剂、非甾体抗炎

  17. Removal of a wide range of emerging pollutants from wastewater treatment plant discharges by micro-grain activated carbon in fluidized bed as tertiary treatment at large pilot scale.

    Science.gov (United States)

    Mailler, R; Gasperi, J; Coquet, Y; Buleté, A; Vulliet, E; Deshayes, S; Zedek, S; Mirande-Bret, C; Eudes, V; Bressy, A; Caupos, E; Moilleron, R; Chebbo, G; Rocher, V

    2016-01-15

    Among the solutions to reduce micropollutant discharges into the aquatic environment, activated carbon adsorption is a promising technique and a large scale pilot has been tested at the Seine Centre (240,000 m(3)/d - Paris, France) wastewater treatment plant (WWTP). While most of available works studied fixed bed or contact reactors with a separated separation step, this study assesses a new type of tertiary treatment based on a fluidized bed containing a high mass of activated carbon, continuously renewed. For the first time in the literature, micro-grain activated carbon (μGAC) was studied. The aims were (1) to determine the performances of fluidized bed operating with μCAG on both emerging micropollutants and conventional wastewater quality parameters, and (2) to compare its efficiency and applicability to wastewater to former results obtained with PAC. Thus, conventional wastewater quality parameters (n=11), pharmaceuticals and hormones (PPHs; n=62) and other emerging pollutants (n=57) have been monitored in μGAC configuration during 13 campaigns. A significant correlation has been established between dissolved organic carbon (DOC), PPHs and UV absorbance at 254 nm (UV-254) removals. This confirms that UV-254 could be used as a tertiary treatment performance indicator to monitor the process. This parameter allowed identifying that the removals of UV-254 and DOC reach a plateau from a μGAC retention time (SRT) of 90-100 days. The μGAC configuration substantially improves the overall quality of the WWTP discharges by reducing biological (38-45%) and chemical oxygen demands (21-48%), DOC (13-44%) and UV-254 (22-48%). In addition, total suspended solids (TSS) are retained by the μGAC bed and a biological activity (nitratation) leads to a total elimination of NO2(-). For micropollutants, PPHs have a good affinity for μGAC and high (>60%) or very high (>80%) removals are observed for most of the quantified compounds (n=22/32), i.e. atenolol (92

  18. Fate and Transport of Pharmaceutical Compounds Applied to Turf-Covered Soil

    Science.gov (United States)

    Young, M.; Green, R. L.; Devitt, D.; McCullough, M.; Wright, L.; Vanderford, B. J.; Snyder, S. A.

    2012-12-01

    In arid and semi-arid regions, the use of treated wastewater for landscape irrigation is becoming common practice and a significant asset to conserve potable water supplies. Public interest and lack of field-scale data are leading to a concern that compounds found in reuse water could persist in the environment and contaminate groundwater. As part of a larger study, 2-yr experiments were conducted in CA and NV, where reuse water was the primary source of non-ambient water input. A total of 13 compounds were studied, all originating in irrigation water applied to soil covered in turf or left bare. The target compounds included atenolol, atorvastatin, carbamazepine, diazepam, diclofenac, fluoxetine, gemfibrozil, ibuprofen, meprobamate, naproxen, primidone, sulfamethoxazole, triclosan, and trimethoprim. Analytical protocols for all compounds (detection at ng/L range) were established before the study commenced. The goals of the research were to increase available data on the fate and transport of these target compounds in turfgrass/soil systems, and to use these data to assess long-term risk from using water containing these compounds. Experiments conducted at two scales are discussed here: lysimeter-scale and field-scale. At the lysimeter-scale, 24 drainage lysimeters (120 cm thick) were exposed to treated wastewater as an irrigation source. Lysimeters varied by soil type (two types), soil cover (bare- versus turf-covered) and leaching fraction (5% and 25%). Upper and lower boundary conditions were monitored throughout the study. Water samples were collected periodically after water breakthrough. After the study, soil samples were analyzed for compound mass, allowing compound mass balance and removal to be assessed. At the field-scale, passive drain gages (Decagon Devices) were installed in triplicate in fairways at four operational golf courses, one in NV and three in CA, all with histories of using treated wastewater. The gages measure water fluxes through the 60

  19. Occurrence and fate of pharmaceutically active compounds in the environment, a case study: Hoeje River in Sweden

    Energy Technology Data Exchange (ETDEWEB)

    Bendz, David [Swedish Geotechnical Institute, Department of Environmental Technology, Hospitalsgatan 16A, S-211 33 Malmoe (Sweden)]. E-mail: David.Bendz@swedgeo.se; Paxeus, Nicklas A. [Gryaab, Karl IX:s vaeg, S-418 34 Gothenburg (Sweden); Ginn, Timothy R. [University of California, Department of Civil and Environmental Engineering, 1 Shields Avenue, 2001 Engineering III, Davis, CA 95616 (United States); Loge, Frank J. [University of California, Department of Civil and Environmental Engineering, 1 Shields Avenue, 2001 Engineering III, Davis, CA 95616 (United States)

    2005-07-15

    {sup -}) and boron (B) were used as natural inert tracers to estimate the relative extent of dilution of PhACs measured in the effluent of the STP on concentrations measured further downstream. Based on spatial trends of concentrations (recalculated to reflect a hypothetical scenario with no dilution), ibuprofen, ketoprofen, naproxen and dicofenac were shown to be subject to significant abiotic or biotic transformations or physical sequestration in the river. The {beta}-blockers atenolol, metoprolol and propanolol, the antibiotics trimetoprim and sulfametoxazole, and carbamazepine demonstrated a high degree of persistence. Fluctuations in the concentration of carbamazepine and gemfibrozil were observed along the series of reservoirs and within the river and are hypothesized to be due to release of parent compound from glucuronides. Several of the investigated substances (metaprolol, propanolol and carbamazepin) that exhibit low excretion rates as parent compounds demonstrate a surprising persistence in the aquatic environment. It is concluded that pharmaceutical substances with a high metabolic rate in humans (low excretion rate) do not necessarily induce a short lifetime in aquatic environments. Results from this study emphasize the need for a broader view on the concept of persistence that accounts for loading rates, in addition to removal mechanisms (e.g., transformation, volatility and physical sequestration by solids), under a variety of spatial and temporal scales.

  20. 小剂量药物联合治疗高血压的可行性研究%Feasibility Study of Small Doses of Combined Drug Therapy in Treating Hypertension

    Institute of Scientific and Technical Information of China (English)

    丁绍祥

    2011-01-01

    Objective To analyze the present situation of individual treatment plan in treating hypertension with small doses of combined drugs including nifedipine ( N ), atenolol ( A ), hydrochlorothiazide ( H ) and captopril ( C ) after four years of its spread in grass roots, Xining. To evaluate the feasibility of the plan and the existing problems. Methods Select all the medical records of hypertension patients treated by NAHC individual treatment therapy in Xining from January 1, 2006 to December 31, 2009 to summarize and analyze this method from the aspects of its technical training, drugs selection, joins procedure, method of taking drugs, treatment costs and blood pressure of the patients before treatment, the blood pressure after treatment, the situation of continual medicine - taking, the reason of withdrawal from the therapeutic schedule and so on. Results A total of 801 patients were included with average age ( 57. 3 ± 10. 3 ), 340 males and 433 females. Before treatment, the average systolic blood pressure ( SBP ): ( 147. 9 ± 19. 4 ) mm Hg, the average diastolic blood pressure ( DBP ): ( 91. 4 ± 14. 1 ) mm Hg; After treatment, 368 subjects have records of blood pressure, the male are 160 cases and female 280 cases. The average SBP: ( 128. 5 ± 12. 4 ) mm Hg, the average DBP: ( 80. 05 ±8. 7 ) mm Hg. 351 patients' hypertension were recovered; the total effective rate was 95. 4% ; 85 cases had kept on taking medicine for 2 years or more, accounting for 10. 6% . Because the medical records are not complete, the numbers of no sex record, no contact phone number, no blood pressure record before treatment, no age record, no previous highest blood pressure record or family history were respectively 28, 29, 33, 34, 365 and 392. The average expense of daily use on drugs was 0. 09 yuan, and annual cost was 33 yuan. Conclusion The cost of NAHC indi-viduation therapeutic schedule is inexpensive with sound therapeutic effects and is fit to be popularized in the grass roots