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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. Pharmacokinetic and pharmacodynamic interactions between phenprocoumon and atenolol or metoprolol

    OpenAIRE

    H. Spahn; Kirch, W; Mutschler, E; Ohnhaus, E E; Kitteringham, N R; Lögering, H. J.; Paar, D.

    1984-01-01

    Pharmacological interactions in both directions between phenprocoumon and atenolol and metoprolol were investigated using a crossover trial. Co-administration of phenprocoumon did not significantly affect Cmax, tmax, t½,22, AUC for atenolol or metoprolol. Co-administration of metoprolol, but not atenolol, increased mean plasma phenprocoumon concentrations 4 and 6 h after dosing and was caused by a decrease in the apparent volume of distribution. This increase in plasma phenprocoumon was not a...

  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. New alginic acid–atenolol microparticles for inhalatory drug targeting

    International Nuclear Information System (INIS)

    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

  5. Atenolol in the treatment of essential hypertension during pregnancy.

    Science.gov (United States)

    Rubin, P C; Butters, L; Low, R A; Reid, J L

    1982-08-01

    Atenolol has been studied prospectively in the management of ten patients with essential hypertension during pregnancy. Median supine BP fell significantly from 156/98 mmHg before treatment to 128/82 mmHg at term. Atenolol did not suppress cardiotocographic signs of foetal distress. Although there was one intrauterine death, the remaining nine babies had a median Apgar score at birth of 9 and a median weight which was 82% of the gestational mean. There were no cases of neonatal bradycardia or respiratory depression and the only case of hypoglycaemia was in a dysmature baby. These findings justify a formal study of beta-adrenoceptor blocker therapy in hypertensive diseases of pregnancy. PMID:7104179

  6. Exercise metabolism in healthy volunteers taking celiprolol, atenolol, and placebo.

    OpenAIRE

    Head, A; Maxwell, S; Kendall, M J

    1997-01-01

    OBJECTIVE: Previous studies have shown that beta 1 selective agents have fewer adverse effects on exercise metabolism than nonselective beta blockers, and this has been attributed to their reduced blockade of beta 2 receptors. This study aimed at determining whether a beta blocker with partial agonist activity at beta 1 and beta 2 receptors (celiprolol) was better than a conventional beta 1 receptor-blocker (atenolol) in prolonging exercise capabilities. METHODS: After four days of treatment ...

  7. 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...

  8. Increased platelet adhesion and aggregation in hypertensive patients: effect of atenolol.

    OpenAIRE

    Markel, A.; Brook, J. G.; LEVY, Y.; Aviram, M.; Youdim, M. B.

    1983-01-01

    Fourteen patients with established hypertension followed a double-blind crossover-styled trial to study the effects of 100 mg/day atenolol compared to placebo. Atenolol was found to be an effective antihypertensive agent, reducing both systolic and diastolic blood pressure. Hypertensive patients appear to have increased in vitro platelet adhesion and aggregation. Atenolol significantly reduced platelet adhesion, but had little effect on aggregation. This may be important in contributing towar...

  9. 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 Berend;

    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....

  10. 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...

  11. STUDIES IN DISSOLUTION ENHANCEMENT OF ATENOLOL USING HP-βCD

    OpenAIRE

    Ghule Prashant Jalindar; Das Saumya; Karle Ganesh Daulat

    2011-01-01

    Atenolol β1 cardio selective adrenoreceptor blocking agent, which is poorly soluble with only 40-50% bioavailability. In the present study attempt has been made to prepare and characterize inclusion complexes of Atenolol with HP-β-CD.The phase solubility analysis indicated the formation of 1:1 molar inclusion complex of atenolol with HP- β-CD. Apparent stability constant ( KC) was 43.195 M-1 for HP- β-CD complexes. The inclusion complexes were prepared by three different methods viz. physica...

  12. Effect of atenolol and metoprolol on the anticoagulant activity of acenocoumarin

    OpenAIRE

    Mantero, F; Procidano, M.; Vicariotto, M. A.; Girolami, A.

    1984-01-01

    In patients receiving long-term acenocoumarin treatment, the effect on anticoagulant activity of atenolol (100 mg once-daily) and metoprolol (100 mg twice daily) was compared in a randomised within-patient open trial. No significant differences were demonstrated between mean prothrombin time and Thrombotest during treatment with atenolol, metoprolol or placebo. These data do not suggest the existence of an interaction between acenocoumarin and the moderately lipophilic β-adrenoceptor blocker ...

  13. 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

  14. 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)

  15. Anterior spinal cord syndrome after initiation of treatment with atenolol.

    Science.gov (United States)

    Schneider, Gregory S

    2010-06-01

    Anterior spinal cord syndrome is a rare condition with a variety of precipitating factors. Patients typically complain of weakness or paralysis of the extremities, often accompanied by pain, but frequently without a history of trauma. A 48-year-old man presented to the emergency department complaining of neck pain and inability to move his legs in the absence of trauma. Several hours prior he had seen his private physician and was given a dose of atenolol for elevated blood pressure. He had not previously been on medications for hypertension. His neurological examination revealed bilateral paralysis of the lower extremities. In the upper extremities he had weakness and sensory loss at the level of C6. Rectal tone was decreased and without sensation. Cervical and thoracic spine magnetic resonance imaging showed spondylotic disc disease, with disc herniation at C6-7 causing severe spinal canal stenosis. Despite i.v. methylprednisolone, pressors, and a prolonged intensive care unit course, the patient was discharged 5 weeks later with continued neurological deficits. Anterior spinal cord syndrome results from compression of the anterior spinal artery and often occurs in the absence of traumatic injury. The recognition, management, and prognosis of this condition are discussed. PMID:18597977

  16. 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.

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

    International Nuclear Information System (INIS)

    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

  18. 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.

  19. 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.

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

    International Nuclear Information System (INIS)

    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

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

    Directory of Open Access Journals (Sweden)

    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.

  2. Flow-injection chemiluminescence analysis for sensitive determination of atenolol using cadmium sulfide quantum dots

    Science.gov (United States)

    Khataee, Alireza; Lotfi, Roya; Hasanzadeh, Aliyeh; Iranifam, Mortaza; Joo, Sang Woo

    2016-03-01

    A sensitive, rapid and simple flow-injection chemiluminescence (CL) system based on the light emitted from KMnO4-cadmium sulfide quantum dots (CdS QDs) reaction in the presence of cetyltrimethylammonium bromide (CTAB) in acidic medium was developed as a CL probe for the sensitive determination of atenolol. Optical and structural features of CdS QDs capped with L-cysteine, which synthesized via hydrothermal approach, were investigated using X-ray diffraction (XRD), scanning electron microscopy (SEM), photoluminescence (PL), and UV-Vis spectroscopy. The CL intensity of KMnO4-CdS QDs-CTAB was remarkably enhanced in the presence of trace level of atenolol. Under optimum experimental conditions, there is a linear relationship between the increase in CL intensity of KMnO4-CdS QDs-CTAB system and atenolol concentration in a range of 0.001 to 4.0 mg L- 1 and 4.0 to 18.0 mg L- 1, with a detection limit (3σ) of 0.0010 mg L- 1. A possible mechanism for KMnO4-CdS QDs-CTAB-atenolol CL reaction is proposed. To prove the practical application of the KMnO4-CdS QDs-CTAB CL method, the method was applied for the determination of atenolol in spiked environmental water samples and commercial pharmaceutical formulation. Furthermore, corona discharge ionization ion mobility spectrometry (CD-IMS) technique was utilized for determination of atenolol. Figure S2. Optimization of the CL reaction conditions: (a) effect of KMnO4 concentration. Conditions: the concentrations of H2SO4, CdS QDs and atenolol were 1 mol L-1, 0.35 mol L-1, and 4.0 mg L-1, respectively; (b) effect of acidic media. Conditions: the concentrations of KMnO4 was 0.04 mmol L-1, other conditions were as in (a); (c) effect of CdS QDs concentration. Conditions: H2SO4 concentration was 1.0 mol L-1, other conditions were as in (b), and (d) effect of CTAB concentration. Conditions: CdS QDs concentration was 0.35 mmol L-1, other conditions were as in (c). Figure S3. UV-Vis absorption spectra of KMnO4-CdS QDs-atenolol CL system

  3. 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...

  4. SIMULTANEOUS ESTIMATION OF ATENOLOL AND AMLODIPINE BESYLATE IN TABLETS FORMULATIONS BY VIERODT’S METHOD USING U.V.SPECTROPHOTOMETRY

    Directory of Open Access Journals (Sweden)

    Jha Girdhari

    2012-02-01

    Full Text Available A new UV- Spectrophotometric method has been developed for the simultaneous estimation of atenolol and amlodipine besylate in tablet dosage forms using 0.1N hydrochloric acid (pH 1.2. The method is based on simultaneous equation or Vieordt’s method. The λmax values for atenolol and amlodipine besylate were found to be 224.6 nm and 239.6 nm respectively. The system obey Beer’s law in the range of 4-28 µg/ml and 4-32 µg/ml with correlation coefficient of 0.9991 and 0.9932 for atenolol and amlodipine besylate respectively. Intraday and Interday precision were found to be 0.08577-1.4682, 0.1080-1.71138, 0.2525-1.6080 and 0.2599-1.3906 respectively. The developed method can be successfully employed for the assay of atenolol and amlodipine besylate in different formulations.

  5. The effects of propranolol or atenolol on the cardiovascular responses to central hypovolaemia in Europeans and Bengalees.

    OpenAIRE

    Rahman, M A; Bennett, T.

    1990-01-01

    1. The effects of single oral doses of propranolol (80 mg), or atenolol (100 mg) on resting heart rate, blood pressure, forearm blood flow and forearm vascular resistance and on responses to central hypovolaemia, were compared with those of placebo in nine healthy European and nine healthy Bengalee volunteers, in a double-blind, three-period, cross-over study. 2. Atenolol induced a significant reduction in resting systolic blood pressure (SBP) in Europeans but not in Bengalees, although the b...

  6. A clinical study of effect of oral atenolol on normal intraocular pressure and systemic blood pressure

    Directory of Open Access Journals (Sweden)

    Chauhan Jugal

    1989-01-01

    Full Text Available Atenolol is a newer betablocker, widely used as an antihypertensive drug. It cause a large and rapid fall in IOP when used orally and topically. A total of 33 patients both having normal and raised IOP were included in the study. The drug was given in a dose of 50 mg. tab. orally once a day for 7 days at 8 A.M. and IOP recorded after 24 hours, 72 hours and on 7th day. It produces significant and sustained fall in IOP in both normal and raised IOP patients besides lowering of systematic B.P. and pulse rate. The IOP on patients with systemic hypertension with Atenolol will be reduced and stoppage of therapy may cause glaucoma damage.

  7. 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...

  8. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  10. 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

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

    Directory of Open Access Journals (Sweden)

    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.

  12. Electrochemical behavior of atenolol, carvedilol and propranolol on copper-oxide nanoparticles

    International Nuclear Information System (INIS)

    Graphical abstract: General morphologies of synthesized CuO nanoflowers. A large number of CuO nanoflowers agglomerates with a uniform size of about 1–2 μm. An individual flower-like nanostructure is shown in the inset, which demonstrates that the CuO nanostructures with flower-like shapes are composed of many interconnected sheet-like crystallites with thicknesses in the range of 30 nm. Highlights: ► We prepared a new electrochemical sensor for determination of atenolol, carvedilol and propranolol. ► We exam ability of copper-oxide nanoparticles for electrocatalytical oxidation of β-blockers. ► Micromolar concentrations of above β-blockers were determined by differential pulse voltammetry method. ► The prepared modified electrode can be used as a chronoamperometric detector for β-blockers determination in a flow system. - Abstract: The electrochemical behavior of atenolol, carvedilol and propranolol was investigated on copper-oxide nanoparticle modified carbon paste electrodes. The process of oxidation and its kinetics were established by using cyclic voltammetry, chronoamperometry techniques and also steady state polarization measurements. The results revealed that copper-oxide nanoparticle promotes the rate of oxidation by increasing the peak current, so these drugs are oxidized at lower potentials. The apparent electron transfer rate constant (Ks) and transfer coefficient (a) were determined by cyclic voltammetry and were approximately 7.1 s−1 and 0.49, respectively. The modified electrodes showed excellent catalytic activity towards the oxidation of β-blockers at an unusually positive potential in buffer solution. The linear concentration range of the proposed sensor for the atenolol, carvedilol and propranolol detection were 12–96, 5–37, and 10–104 μM, respectively.

  13. 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.

  14. 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.

  15. 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

  16. 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

  17. 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

  18. Design, development and optimization of s (- Atenolol floating sustained release matrix tablets using surface response methodology

    Directory of Open Access Journals (Sweden)

    P T Gunjal

    2015-01-01

    Full Text Available The objective of this present investigation was to develop and formulate floating sustained release matrix tablets of s (- atenolol, by using different polymer combinations and filler, to optimize by using surface response methodology for different drug release variables and to evaluate the drug release pattern of the optimized product. Floating sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: Hydroxypropyl methylcellulose, sodium bicarbonate as a gas generating agent, polyvinyl pyrrolidone as a binder and lactose monohydrate as filler. The 32 full factorial design was employed to investigate the effect of formulation variables on different properties of tablets applicable to floating lag time, buoyancy time, % drug release in 1 and 6 h (D1 h,D6 h and time required to 90% drug release (t90%. Significance of result was analyzed using analysis of non variance and P<0.05 was considered statistically significant. S (- atenolol floating sustained release matrix tablets followed the Higuchi drug release kinetics that indicates the release of drug follows anomalous (non-Fickian diffusion mechanism. The developed floating sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.

  19. 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....

  20. 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.

  1. COMPARISON OF FOSINOPRIL AND ATENOLOL EFFECT ON HEART 0.1 HZ-RHYTHMS SYNCHRONIZATION AND BLOOD MICROCIRCULATION IN PATIENTS WITH ARTERIAL HYPERTENSION

    Directory of Open Access Journals (Sweden)

    A. R. Kiselev

    2016-01-01

    Full Text Available Aim. To compare the effect of fosinopril and atenolol on synchronization of heart 0.1 Hz-rhythms and blood microcirculatory.Material and methods. 63 patients at the age of 47±8 with hypertension (HT of grade 1-2 were enrolled in the study. 0.1 Hz-oscillations in heart rate variability (HRV and in filling of microcirculatory bed were registered during passive tilt test under spontaneous breathing. The duration of each stage of test was 10 min. Synchronization was estimated as a phase difference between 0.1 Hz-rhythms of heart rate and filling of microcirculatory bed. Frequency values of HRV spectrum in LF- and HF-ranges were also assessed.Results. Fosinopril and atenolol showed comparable effect on blood pressure (BP reduction. Atenolol decreased in heart rate significantly. Treatment with either fosinopril or atenolol in patients with significant vegetative dysfunction resulted in repair of functional interaction between heart 0.1 Hz-regulation and microcirculatory bed. Functional dissociation of 0.1 Hz-regulation mechanisms was observed under the treatment with fosinopril or atenolol in patients with initially sufficient interaction.Conclusions. Fosinopril and atenolol influenced similarly on heart 0.1 Hz-mechanisms and microcirculation autonomic regulation in patients with HT. Atenolol is a drug of choice in patients with sympathicotony. Both drugs should be administered in according with an individual level of 0.1-Hz rhythms synchronization assessed before start of the treatment.

  2. 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.

  3. Synthesis of the 11C-labelled β-adrenergic receptor ligands atenolol, metoprolol and propanolol

    International Nuclear Information System (INIS)

    The 11C-labelled β-adrenergic receptor ligands atenolol 1, metoprolol 2 and propranolol 3 have been synthesized by an N-alkylation reaction using [2-11C]isopropyl iodide. The labelled isopropyl iodide was prepared in a one-pot reactor system from [11C]carbon dioxide and obtained in 40% radiochemical yield within 14 min reaction time. The total reaction times for compounds 1-3, counted from the start of the isopropyl iodide synthesis and including purification were 45-55 min. The products were obtained in 5-15% radiochemical yields and with radiochemical purities higher than 98%. The specific activity ranged from 0.4 to 4 GBq/μmol. In a typical experiment starting with 4 GBq around 75 MBq of product was obtained. (author)

  4. Synthesis of the sup 11 C-labelled. beta. -adrenergic receptor ligands atenolol, metoprolol and propanolol

    Energy Technology Data Exchange (ETDEWEB)

    Antoni, G.; Ulin, J.; Laangstroem, B. (Uppsala Univ. (Sweden). Dept. of Organic Chemistry)

    1989-01-01

    The {sup 11}C-labelled {beta}-adrenergic receptor ligands atenolol 1, metoprolol 2 and propranolol 3 have been synthesized by an N-alkylation reaction using (2-{sup 11}C)isopropyl iodide. The labelled isopropyl iodide was prepared in a one-pot reactor system from ({sup 11}C)carbon dioxide and obtained in 40% radiochemical yield within 14 min reaction time. The total reaction times for compounds 1-3, counted from the start of the isopropyl iodide synthesis and including purification were 45-55 min. The products were obtained in 5-15% radiochemical yields and with radiochemical purities higher than 98%. The specific activity ranged from 0.4 to 4 GBq/{mu}mol. In a typical experiment starting with 4 GBq around 75 MBq of product was obtained. (author).

  5. Spectroscopic and DFT study of atenolol and metoprolol and their copper complexes

    Science.gov (United States)

    Cozar, O.; Szabó, L.; Cozar, I. B.; Leopold, N.; David, L.; Căinap, C.; Chiş, V.

    2011-05-01

    IR, Raman and surface-enhanced Raman scattering (SERS) spectra of atenolol (ATE) and metoprolol (MET) were recorded and assigned on the basis of density functional theory (DFT) calculations. A reliable assignment of vibrational IR and Raman bands of the two compounds was possible by a proper choice of models used in quantum chemical calculations. Both molecules are adsorbed to the silver surface mainly through the oxygen atoms and π-electrons of the phenyl ring. The coordination mode of the metal ions in Cu(II)-ATE and -MET compounds was also derived from IR and EPR spectra. EPR spectra give evidence for a square-planar arrangement around the copper (II) ion in the case of Cu-ATE complex, with a N 2O 2 chromophore. Only oxygen atoms are involved in the cooper coordination for Cu-MET complex, and two types of local symmetries with d and d as ground states for paramagnetic electron coexist.

  6. 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.

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

    International Nuclear Information System (INIS)

    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 (1O2) 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 1O2 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 1O2 and triplet state effluent organic matter, are likely to play important roles in fates of these compounds

  8. 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...

  9. Post-exercise hypotension: the effects of epanolol or atenolol on some hormonal and cardiovascular variables in hypertensive men.

    OpenAIRE

    Wilcox, R G; Bennett, T.; Macdonald, I A; Broughton Pipkin, F; Baylis, P. H.

    1987-01-01

    1 Eight men with primary hypertension were treated for 3 weeks with placebo, epanolol (200 mg or 400 mg), or atenolol 100 mg in a randomised cross-over study. Each active treatment period was preceded by a 3 week placebo treatment period and both investigators and subjects were blind to the active drug sequence. 2 At the end of each period, measurements were made of resting cardiovascular (heart rate, blood pressure, forearm blood flow) and biochemical variables (plasma renin, angiotensin II,...

  10. Effects of tedisamil, atenolol and their combination on heart andrate-dependent QT interval in healthy volunteers

    OpenAIRE

    Démolis, Jean-Louis; Martel, Christine; Funck-Brentano, Christian; Sachse, Alisia; Weimann, Hans-Joseph; Jaillon, Patrice

    1997-01-01

    Aims Tedisamil is a new blocker of K+ currents in cardiac tissues, exerts bradycardic effects and has shown clinical efficacy in angina pectoris. Theoretically, when coadministered with a &bgr;-adrenoceptor blocker the tedisamil combination could induce dangerous bradycardia and QT interval prolongation. Therefore, the aim of this study was to evaluate the effects of tedisamil and atenolol alone and in combination, on heart rate and QT interval duration at rest and during exercise tests.

  11. Indobufen interacts with the sulphonylurea, glipizide, but not with the beta-adrenergic receptor antagonists, propranolol and atenolol.

    OpenAIRE

    Elvander-Ståhl, E; Melander, A; Wåhlin-Boll, E

    1984-01-01

    This study assessed the possible interactions of the cyclooxygenase inhibitor indobufen with one sulphonylurea, glipizide, and with two beta-adrenoceptor antagonists, one of which is extensively metabolised already in the first passage through the liver (propranolol) while the other essentially escapes biotransformation (atenolol). Indobufen was first given as a single 200 mg dose and then for a 5 day period in a dosage of 200 mg twice daily, to six healthy volunteers. Glipizide (5 mg), propr...

  12. 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

  13. DEVELOPMENT AND VALIDATION OF RP- HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF ATENOLOL AND INDAPAMIDE IN PHARMACEUTICAL DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Pawar Prachi Vasant

    2011-03-01

    Full Text Available A simple, sensitive, precise and specific Reverse Phase High Performance Liquid Chromatographic method was developed and validated for the determination of Atenolol and Indapamide in bulk and tablet dosage forms. It was found that the excipient in the tablet dosage forms does not interfere in the quantification of active drug by proposed method. The HPLC separation was carried out by reverse phase chromatography by Intelligent C18 column (200×4.6mm with a mobile phase composed of Methanol: Water: Diethylamine: Glacial Acetic Acid, (70:30:0.12:0.08 in isocratic mode at a flow rate of 1.2ml/min. The detection was monitored at 240 nm. The calibration curve for Atenolol and Indapamide was linear from 20-100 µg/ml and 1-5 µg/ml respectively. The inter-day and intra-day precision was found to be within limits. The proposed method has adequate sensitivity, reproducibility and specificity for the determination of Atenolol and Indapamide in bulk and its tablet dosage forms. Accuracy (recoveries: 99.07-101.44% and reproducibility were found to satisfactory.

  14. 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.

  15. X-ray absorption and selectively excited X-ray emission spectra of atenolol and nadolol

    International Nuclear Information System (INIS)

    Full text: The biological function of a drug given by the oral route is ruled by its degree of absorption in the gastrointestinal tract. These absorption characteristics (dissolution, solubility, permeability, metabolism) of the drug are time consuming and expensive to investigate experimentally. The predictive power of traditional theoretical models is quite limited. This is especially so for solubility, where a model predicting values within one order of magnitude of the experimentally determined solubility is accepted by the research field. Aiming at a more detailed understanding of drug solubility, we are carrying out X-ray absorption and X-ray emission spectroscopy on a series of pharmaceutical model substances in solid form and in water solution. Changes in local geometry and electronic structure primarily associated with changes in the way the drug molecules are hydrogen bonded to surrounding molecules are directly reflected in the spectra. Here we present and analyze the spectra of two solid β-adrenoreceptors, atenolol and nadolol, at the carbon, nitrogen and oxygen K edges. Special attention is given to the influence on the spectra of hydrogen bonding. An increased understanding of hydrogen bonding is essential for improving solubility models

  16. 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

  17. Comparison of two long-acting preparations of metoprolol with conventional metoprolol and atenolol in healthy men during chronic dosing.

    OpenAIRE

    Freestone, S; Silas, J H; Lennard, M. S.; Ramsay, L E

    1982-01-01

    1 Eight healthy men received two long-acting formulations of metoprolol 200 mg (SA Astra, SR Geigy), conventional metoprolol 200 mg and atenolol 100 mg once daily for 1 week each in balanced, crossover fashion. There was a washout period of at least a week between each phase. 2 On the last day of each phase, post-exercise heart rate was recorded at intervals and compared to pretreatment values. Plasma metoprolol concentrations were measured. 3 The mean AUC was similar after each of the three ...

  18. The effect of atenolol on the spontaneous and reflex activity of the sympathetic nerves in the cat: influence of cardiopulmonary receptors

    OpenAIRE

    Scott, Evelyn M.

    1983-01-01

    1 Atenolol reduces sympathetic efferent discharge and attenuates the responses of the sympathetic nerves to changes in blood pressure. The present experiments were carried out to determine whether these changes were mediated by cardiopulmonary receptors whose afferents lie in the vagal nerves.

  19. 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

  20. 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.

  1. 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

  2. Effect of treatment with chlorthalidone and atenolol on response to dilator agents in the forearm resistance vessels of men with primary hypertension.

    OpenAIRE

    Robinson, B F; Dobbs, R J; Phillips, R J

    1983-01-01

    The forearm resistance vessels of men with primary hypertension respond to verapamil with a greater than normal dilatation relative to that induced by sodium nitroprusside. We have examined the effect on this functional abnormality of treatment with chlorthalidone (50 mg daily in 16 patients) and atenolol (100 mg daily in eight patients and 200 mg daily in two). The responsiveness of the forearm resistance vessels to local intra-arterial infusion of verapamil and sodium nitroprusside was asse...

  3. The effect of two beta-adrenoceptor blockers (mepindolol and atenolol) on blood lipids and platelet aggregation in normal volunteers and essential hypertensive patients.

    OpenAIRE

    Luque Otero, M; Fernandez Pinilla, C; Escriba Polo, A; Rodriguez Vazquez, M; Martell Claros, N; A Fernandez-Cruz

    1984-01-01

    beta-adrenoceptor blocking agents are widely used as treatment of essential hypertension. We studied the action of a new non cardioselective beta-adrenoceptor blocker, mepindolol, comparing its effects on blood pressure, blood lipids and platelet aggregation with those of a cardioselective beta-adrenoceptor blocker, atenolol. Blood pressure fell significantly in the patients treated with both drugs. Triglycerides rose non-significantly only in volunteers treated with mepindolol. We did not fi...

  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 < 0.001) independent of hydrochlorothiazide...

  6. 201 thallium scintiscanning during exercise in patients with coronary diseases following administration of the cardioselective beta-blocker atenolol

    International Nuclear Information System (INIS)

    Changes of regional myocardial perfusion before and after administration of Atenolol (AT) (5 mg i.v.) were investigated by 201-Tl stress-imaging in 14 patients (PAT) with >= 70% coronary obstructions. Scintigrams were performed in 4 projections; scintigraphic defects (SD) in one of the six LV segments had to be identified in at least 2 projections and to show a decrease of activity >= 25%. All PAT had at least one reversible SD. Results: After AT, stress-induced SDs were unchanged in 11 of the 14 PAT at identical work loads (131 Watt). The total number of reversible defects was 33 before and 28 after AT (n.s.). However, not only the 3 PAT with improved stress scintigrams, but also 6 of the 11 PAT with unchanged abnormal stress scintigrams were clinically improved (ECG normalized, no angina). Thus in almost half of the patients (6/14), the stress ECG was normalized without normalisation of perfusion pattern of thallium scintigrams. We conclude that in these patients subendocardial perfusion was enough improved to meet the reduced metabolic needs but not enough to normalise stress images. (orig./MG)

  7. 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

  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. 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

  10. 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.

  11. Comparative proteomics analysis of vascular smooth muscle cells incubated with S- and R-enantiomers of atenolol using iTRAQ-coupled two-dimensional LC-MS/MS.

    Science.gov (United States)

    Sui, Jianjun; Zhang, Jianhua; Tan, Tuan Lin; Ching, Chi Bun; Chen, Wei Ning

    2008-06-01

    Atenolol is a beta(1)-selective drug, which exerts greater blocking activity on beta(1)-adrenoreceptors than on beta(2)-adrenoreceptors, with the S-enantiomer being more active than R-enantiomer. The aim of this study was to investigate the proteins with differential protein expression levels in the proteome of vascular smooth muscle cells (A7r5) incubated separately with individual enantiomers of atenolol using an iTRAQ-coupled two-dimensional LC-MS/MS approach. Our results indicated that some calcium-binding proteins such as calmodulin, protein S100-A11, protein S100-A4, and annexin A6 were down-regulated and showed relatively lower protein levels in cells incubated with the S-enantiomer of atenolol than those incubated with the R-enantiomer, whereas metabolic enzymes such as aspartate aminotransferase, glutathione S-transferase P, NADH-cytochrome b(5) reductase, and alpha-N-acetylgalactosaminidase precursor were up-regulated and displayed higher protein levels in cells incubated with the S-enantiomer relative to those incubated with the R-enantiomer. The involvement of NADH-cytochrome b(5) reductase in the intracellular anabolic activity was validated by NAD+/NADH assay with a higher ratio of NAD+/NADH correlating with a higher proportion of NAD+. The down-regulation of the calcium-binding proteins was possibly involved in the lower intracellular Ca2+ concentration in A7r5 cells incubated with the S-enantiomer of atenolol. Ca2+ signals transduced by calcium-binding proteins acted on cytoskeletal proteins such as nestin and beta-tropomyosin, which can play a complex role in phenotypic modulation and regulation of the cytoskeletal modeling. Our preliminary results thus provide molecular evidence on the metabolic effect and possible link of calcium-binding proteins with treatment of hypertension associated with atenolol. PMID:18270196

  12. 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

  13. [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

  14. 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 an...... and beta blockers. Our aim, therefore, was to compare the effect on non-fatal myocardial infarction and fatal CHD of combinations of atenolol with a thiazide versus amlodipine with perindopril....

  15. 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...

  16. 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.

  17. 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...

  18. 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...

  19. 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 an...

  20. 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.

  1. 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), ...

  2. 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 ...

  3. 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, ...

  4. 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 ...

  5. 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...

  6. 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...

  7. 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....

  8. 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.

  9. Biodegradation and cometabolic modeling of selected beta blockers during ammonia oxidation.

    Science.gov (United States)

    Sathyamoorthy, Sandeep; Chandran, Kartik; Ramsburg, C Andrew

    2013-11-19

    Accurate prediction of pharmaceutical concentrations in wastewater effluents requires that the specific biochemical processes responsible for pharmaceutical biodegradation be elucidated and integrated within any modeling framework. The fate of three selected beta blockers-atenolol, metoprolol, and sotalol-was examined during nitrification using batch experiments to develop and evaluate a new cometabolic process-based (CPB) model. CPB model parameters describe biotransformation during and after ammonia oxidation for specific biomass populations and are designed to be integrated within the Activated Sludge Models framework. Metoprolol and sotalol were not biodegraded by the nitrification enrichment culture employed herein. Biodegradation of atenolol was observed and linked to the activity of ammonia-oxidizing bacteria (AOB) and heterotrophs but not nitrite-oxidizing bacteria. Results suggest that the role of AOB in atenolol degradation may be disproportionately more significant than is otherwise suggested by their lower relative abundance in typical biological treatment processes. Atenolol was observed to competitively inhibit AOB growth in our experiments, though model simulations suggest inhibition is most relevant at atenolol concentrations greater than approximately 200 ng·L(-1). CPB model parameters were found to be relatively insensitive to biokinetic parameter selection suggesting the model approach may hold utility for describing pharmaceutical biodegradation during biological wastewater treatment. PMID:24112027

  10. 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.

  11. 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.

  12. 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...

  13. 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

    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...

  14. 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...

  15. 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...

  16. 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

  17. 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

    . METHODS: Patients had either untreated hypertension or treated hypertension. For those with type II diabetes mellitus, inclusion criteria required at least two additional risk factors. Patients were randomized to amlodipine with addition of perindopril as required (amlodipine-based) or atenolol...

  18. 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

    . 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...

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

    Directory of Open Access Journals (Sweden)

    TorillBerg

    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

  20. 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

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

    DEFF Research Database (Denmark)

    Escola Casas, Monica; Torresi, Elena; Plósz, Benedek G.;

    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 efficiently removed in both reactors. However, type or concentration of carbon did not correlate to micro-pollutant...... removal rates. Second, an anoxic-batch test with spiked micropollutants was conducted. The batch test showed that acetyl-sulfadiazine, atenolol, citalopram, propranolol and trimethoprim were easily removed in both reactors. Ibuprofen, clarithromycin, iopromide, metoprolol, iohexol, iomeprol, venlafaxine...... removal of such compounds. In contrast, for moderately degraded micro-pollutants, the biofilm developed under methanol dosing presented the highest removal rate constants. This might mean that the primary metabolism of methanol improved the metabolism of these micro-pollutants. In general...

  2. 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 in...... 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...

  3. 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...

  4. 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...

  5. 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...

  6. 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...

  7. 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...

  8. 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...

  9. Cardiovascular reflexes in patients after myocardial infarction. Effect of long-term treatment with beta-adrenoceptor antagonists.

    OpenAIRE

    Bennett, T.; Wilcox, R G; Hampton, J.R.

    1980-01-01

    A double-blind study was made of men who had had a myocardial infarction at least one year previously, and who were being treated with propranolol, atenolol, or placebo. They were compared with age- and sex-matched control subjects. Under resting conditions, there were no differences between the systemic arterial blood pressures, forearm blood flows, or heart rates of the control subjects and the post-infarction patients treated with placebo. The patients, however, showed signs of reduced sym...

  10. An assessment of the partial agonist activity of Ro 31-1118, flusoxolol and pindolol in man.

    OpenAIRE

    McCaffrey, P. M.; Riddell, J G; Shanks, R.G.

    1987-01-01

    1. The effects of single oral doses of three beta-adrenoceptor partial agonists (Ro 31-1118, flusoxolol and pindolol), two beta-adrenoceptor antagonists (propranolol and atenolol), two beta-adrenoceptor agonists (salbutamol and prenalterol) and placebo on sleeping heart rate, quality of sleep, supine heart rate, exercise heart rate, blood pressure, forearm blood flow and finger tremor were studied in eight healthy male volunteers. 2. Sleeping heart rate was increased by Ro 31-1118, flusoxolol...

  11. 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 with...

  12. 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

  13. Development and validation of a reversed-phase ultra-performance liquid chromatographic method for the simultaneous determination of six drugs used for combined hypertension therapy.

    Science.gov (United States)

    Kaila, Harshad O; Ambasana, Mrunal A; Shah, Anamik K

    2013-01-01

    A simple, rapid, and reliable ultra-performance LC assay method has been developed for the simultaneous estimation of orally administered hypertension drugs (atenolol, hydrochlorothiazide, amlodipine besylate, indapamide, nifedipine, and lercanidipine hydrochloride), any of which may be administered with atenolol in combined hypertension therapy. Chromatography was carried out at 25 degrees C on a 2.1 x 50 mm id, 1.7 microm particle size Acquity BEH C18 column with the isocratic mobile phase 0.01 M, 4.0 pH aqueous phosphate buffer-acetonitrile (50 + 50, v/v) at a flow rate of 0.35 mL/min. All drugs were separated in less than 4 min with good resolution and minimal tailing, without interference by excipients. The method was validated according to International Conference on Harmonization guidelines, and the acceptance criteria for accuracy, precision, linearity, specificity, and system suitability were met in all cases. The column effluent was monitored at 230 nm. The detector response was linear in the range of 1-20 microg/mL of these drugs. LOD obtained was 0.04 microg/mL for atenolol, 0.02 microg/mL for hydrochlorothiazide, 0.03 microg/mL for amlodipine besylate, 0.03 microg/mL for indapamide, 0.02 microg.mL for nifedipine, and 0.01 microg/mL for lercanidipine hydrochloride. The suggested method has the advantage that all the drugs can be quantified alone or in combination with atenolol using a single mobile phase. PMID:23767353

  14. 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.

  15. 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...

  16. Drug efficacy in treating stable angina pectoris: a protocol for network meta-analysis of randomised controlled trials

    OpenAIRE

    Jia, Yongliang; Leung, Siu-wai

    2014-01-01

    Introduction There were 11 pairwise meta-analysis on the efficacy of β-blockers (including atenolol, propranolol, bisoprolol, metoprolol and nadolol), calcium channel blockers (including amlodipine, diltiazem, felodipine, nifedipine and verapamil), and nitrates (including isosorbide dinitrate, isosorbide mononitrate and nitroglycerin) in treating stable angina pectoris. No network meta-analytic study has been published to evaluate the efficacies of these antianginal drugs. Current clinical gu...

  17. 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...

  18. 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

  19. 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...

  20. 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...

  1. Effects of beta-adrenoceptor drug stimulation on various models of gastric ulcer in rats.

    OpenAIRE

    Esplugues, J.; Lloris, J. M.; Martí-Bonmatí, E.; Morcillo, E. J.

    1982-01-01

    1. Experiments were designed to evaluate the effect of the pharmacological activation of beta-adrenoceptors on various models of gastric ulcer in the rat. 2. Pretreatment with the beta-adrenoceptor stimulant drugs, isoprenaline or salbutamol, significantly inhibited stress-induced gastric ulcers. This anti-ulcer effect was abolished by propranolol but not by atenolol, suggesting that beta 2-adrenoceptors mediate this response. 3. In the pylorus-ligation model, salbutamol inhibited lesion form...

  2. 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.

  3. Constant optimization of oral drug absorption kinetics in the compartment absorption and transit models using particle swarm optimization algorithm

    Science.gov (United States)

    Prabowo, K.; Sumaryada, T.; Kartono, A.

    2016-01-01

    Simulation of predictive modeling oral drug namely Compartment Absorption and Transit (CAT) using Particle Swarm Optimization (PSO) algorithm has been performed. This research will be carried out optimization of kinetic constant value oral drug use PSO algorithm to obtain the best global transport constant values for CAT equation that can predict drug concentration in plasma. The value of drug absorption rate constant for drug atenolol 25 mg is k10, k12, k21, k13 and k31 with each value is 0.8562, 0.3736, 0.2191, 0.4334 and 1.000 have been obtained thus raising the value of the coefficient of determination of a model CAT. From the experimental data plasma drug concentrations used are Atenolol, the coefficient of determination (R2) obtained from simulations atenolol 25 mg (PSO) was 81.72% and 99.46%. Better correlation between the dependent variable as the drug concentration and explanatory variables such as mass medication, plasma volume, and rate of absorption of the drug has increased in CAT models using PSO algorithm. Based on the results of CAT models fit charts can predict drug concentration in plasma.

  4. 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.

  5. 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

  6. 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, pmetoprolol. The transport of clindamycin, clarithromycin and atenolol through the vadose zone seems less probable. PMID:26657382

  7. 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.

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

    International Nuclear Information System (INIS)

    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. 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

  10. 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

  11. Cost-effectiveness of losartan-based therapy in patients with hypertension and left ventricular hypertrophy: a UK-based economic evaluation of the Losartan Intervention for Endpoint reduction in hypertension (LIFE) study.

    Science.gov (United States)

    McInnes, G; Burke, T A; Carides, G

    2006-01-01

    The Losartan Intervention for Endpoint reduction in hypertension (LIFE) study demonstrated the clinical benefit of losartan-based therapy in hypertensive patients with left ventricular hypertrophy (LVH), mainly due to a highly significant 25% reduction in the relative risk of stroke compared with an atenolol-based regimen, for a similar reduction in blood pressure. The aim of this economic evaluation was to estimate the cost-effectiveness of losartan compared with atenolol from a UK national health system perspective. Quality-adjusted survival and direct medical costs were modelled beyond the trial using the within-trial incidence of stroke. Survival with stroke, study medication use and quality of life by stroke status were taken directly from the LIFE trial. The LIFE data were supplemented with UK data on lifetime direct medical costs of stroke and life expectancy in individuals without stroke. No additional stroke events or use of study treatment were assumed beyond the trial. Costs and benefits were discounted using current UK Treasury rates. In the base-case analysis, the reduction in stroke-related costs (by 968 sterling pound) offset 86% of the increase in study medication costs (1128 sterling pound) among losartan-treated patients. The incremental cost-effectiveness ratio (ICER) for losartan versus atenolol in hypertensive patients with LVH was 2130 sterling pound per quality-adjusted life year (QALY) gained (3195 Euro/QALY), and this increased to 11,352 sterling pound per QALY gained (16,450 Euro/QALY) when the costs of stroke beyond the first 5 years were excluded. Thus, the clinical benefit of losartan was achieved at a cost well within reported thresholds for cost-effectiveness. PMID:16357874

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

    Directory of Open Access Journals (Sweden)

    M. V. Soura

    2016-01-01

    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.

  13. 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

  14. Pharmaceuticals as emerging organic contaminants in Umgeni River water system, KwaZulu-Natal, South Africa.

    Science.gov (United States)

    Agunbiade, Foluso O; Moodley, Brenda

    2014-11-01

    The occurrences of pharmaceuticals and personal care products as emerging organic contaminants (EOCs) have been reported in several countries of the world except from African countries. This study was therefore conducted to investigate the occurrence of nine antibiotics, five antipyretics, atenolol, bezafibrate, and caffeine in wastewater and surface water samples from the Umgeni River. The water samples were extracted with solid-phase extraction using hydrophilic-lipophilic balance (HLB) and C-18 cartridges for the acidic and neutral drugs, respectively. The quantification was carried out with high-performance liquid chromatography-diode array detector (HPLC-DAD) using the standard addition method. The method limits of detections were in the range of 0.14-0.97 μg/L while the recoveries were between 53.8 and 108.1 %. The wastewater had 100 % occurrence of the analytes studied, with caffeine having the highest concentration at 61 ± 5 μg/L and nalidixic acid being the most observed antibiotic at 31 ± 3 μg/L. The waste treatment process reduced the influent concentrations by 43.0-94.2 % before discharge except for atenolol removal that is lower. The concentrations of the analytes were lower in the surface water with most compounds having concentrations below 10 μg/L except acetaminophen and atenolol. The estuary mouth and Blue Lagoon had the highest concentrations of some of the compounds in surface water which depict downstream load. The factors governing the fate and mobility of these compounds in this environment are not fully understood yet and will require further studies. PMID:25027777

  15. 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

  16. 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

  17. Selective stimulation of glucagon secretion by beta 2-adrenoceptors in isolated islets of Langerhans of the rat.

    OpenAIRE

    Lacey, R J; Berrow, N.S.; Scarpello, J H; Morgan, N. G.

    1991-01-01

    1. In rat isolated islets of Langerhans the selective beta 2-adrenoceptor agonist, clenbuterol (1 to 20 microM), significantly increased the level of adenosine 3':5'-cyclic monophosphate (cyclic AMP) within 2 min of incubation. 2. The cyclic AMP response to clenbuterol was inhibited in the presence of the selective beta 2 adrenoceptor antagonist, ICI 118551 (0.1 or 10 microM) but remained unchanged when the beta 1-antagonist, atenolol (0.1 microM) was administered. 3. Despite causing an eleva...

  18. 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...

  19. 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

    decreased approximately 8% following all three doses of ICI 141,292 and 14.9% after atenolol 5 mg. No changes in blood pressure were observed under resting conditions after any of the drugs. In six patients with ischaemic heart disease the intrinsic sympathomimetic activity following intravenous...... significant changes were observed in mean arterial blood pressure, stroke volume or total peripheral resistance whereas an increase in supine resting mean pulmonary arterial pressure of 3.4 mm Hg (P less than 0.05) could be demonstrated. ICI 141,292 seems to be a potent (at least five times as potent as...

  20. 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

  1. 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

    with the same gender-specific definitions for high and low hemoglobin as time-varying covariates with adjustment for treatment allocation and established risk factors and diseases, hemoglobin in the lowest decile was associated with higher rates of all-cause mortality (HR 3.03, 95% CI 1.89-4.85, P ... 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...

  2. Markers of collagen synthesis is related to blood pressure and vascular hypertrophy: a LIFE substudy

    DEFF Research Database (Denmark)

    Olsen, M H; Christensen, M K; Wachtell, K; Tuxen, Christian; Fossum, E; Bang, L E; Wiinberg, N; Devereux, R B; Kjeldsen, S E; Hildebrandt, Per; Dige-Petersen, H; Rokkedal, J; Ibsen, H

    2005-01-01

    Cardiac fibrosis and high levels of circulating collagen markers has been associated with left ventricular (LV) hypertrophy. However, the relationship to vascular hypertrophy and blood pressure (BP) load is unclear. In 204 patients with essential hypertension and electrocardiographic LV hypertrophy...... losartan- or an atenolol-based regimen. Furthermore, we measured intima-media thickness of the common carotid arteries (IMT), minimal forearm vascular resistance (MFVR) by plethysmography and ambulatory 24-h BP in around half of the patients. At baseline, PICP/ICTP was positively related to IMT (r=0.24, P...

  3. Association of pulse pressure with new-onset atrial fibrillation in patients with hypertension and left ventricular hypertrophy

    DEFF Research Database (Denmark)

    Larstorp, Anne Cecilie K; Ariansen, Inger; Gjesdal, Knut;

    2012-01-01

    Previous studies have found pulse pressure (PP), a marker of arterial stiffness, to be an independent predictor of atrial fibrillation (AF) in general and hypertensive populations. We examined whether PP predicted new-onset AF in comparison with other blood pressure components in the Losartan...... Intervention For Endpoint reduction in hypertension study, a double-blind, randomized (losartan versus atenolol), parallel-group study, including 9193 patients with hypertension and electrocardiographic left ventricular hypertrophy. In 8810 patients with neither a history of AF nor AF at baseline, Minnesota...

  4. 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.

  5. 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)

  6. 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

  7. Modification of mesoporous silica surface applied as drug delivery system

    International Nuclear Information System (INIS)

    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, N2 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)

  8. Deletion of neurturin impairs development of cholinergic nerves and heart rate control in postnatal mouse hearts.

    Science.gov (United States)

    Downs, Anthony M; Jalloh, Hawa B; Prater, Kayla J; Fregoso, Santiago P; Bond, Cherie E; Hampton, Thomas G; Hoover, Donald B

    2016-05-01

    The neurotrophic factor neurturin is required for normal cholinergic innervation of adult mouse heart and bradycardic responses to vagal stimulation. Our goals were to determine effects of neurturin deletion on development of cardiac chronotropic and dromotropic functions, vagal baroreflex response, and cholinergic nerve density in nodal regions of postnatal mice. Experiments were performed on postnatal C57BL/6 wild-type (WT) and neurturin knockout (KO) mice. Serial electrocardiograms were recorded noninvasively from conscious pups using an ECGenie apparatus. Mice were treated with atenolol to evaluate and block sympathetic effects on heart rate (HR) and phenylephrine (PE) to stimulate the baroreflex. Immunohistochemistry was used to label cholinergic nerves in paraffin sections. WT and KO mice showed similar age-dependent increases in HR and decreases in PR interval between postnatal days (P) 2.5 and 21. Treatment with atenolol reduced HR significantly in WT and KO pups at P7.5. PE caused a reflex bradycardia that was significantly smaller in KO pups. Cholinergic nerve density was significantly less in nodal regions of P7.5 KO mice. We conclude that cholinergic nerves have minimal influence on developmental changes in HR and PR, QRS, and QTc intervals in mouse pups. However, cholinergic nerves mediate reflex bradycardia by 1 week postnatally. Deletion of neurturin impairs cholinergic innervation of the heart and the vagal efferent component of the baroreflex early during postnatal development. PMID:27162260

  9. Demonstration of β1-adrenoceptor mediating relaxation of porcine coronary artery by radioligand binding and pharmacological methods

    International Nuclear Information System (INIS)

    β-adrenoceptors in the porcine coronary artery were characterized by a radioligand binding assay using (-)-[3H]dihydroalprenolol (DHA) and also by measuring the relaxant response of isolated coronary artery to norepinephrine. Specific (-)-[3H]DHA binding in the porcine coronary artery was saturable, reversible and of high affinity with a maximal number of binding sites of 63 fmol/mg protein, and it showed a pharmacological specificity as well as stereoselectivity which characterized β-adrenoceptors. The Hofstee analysis of inhibition of (-)-[3H]DHA binding by atenolol, practolol and ICI 118551 has shown that the averaged concentration of β1 and β2-adrenoceptors in this tissue was 68% and 32% respectively. The relaxant response of isolated coronary artery to norepinephrine was competitively antagonized by (-)propranolol, (+)propranolol, atenolol, practolol and ICI 118551. The pA2 values of these adrenoceptor antagonists were significantly correlated with the Ki values for β1 but not β2-adrenoceptors determined by the (-)-[3H]DHA binding assay. Thus, the present study demonstrates that the relaxant response of porcine coronary artery to norepinephrine is predominantly mediated through the stimulation of β1-adrenoceptors on vascular smooth muscles

  10. ''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.)

  11. 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.

  12. 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

  13. 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

  14. 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.

  15. 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

  16. 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.

  17. 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.

  18. 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

  19. Concentrations of prioritized pharmaceuticals in effluents from 50 large wastewater treatment plants in the US and implications for risk estimation

    International Nuclear Information System (INIS)

    We measured concentrations of 56 active pharmaceutical ingredients (APIs) in effluent samples from 50 large wastewater treatment plants across the US. Hydrochlorothiazide was found in every sample. Metoprolol, atenolol, and carbamazepine were found in over 90% of the samples. Valsartan had the highest concentration (5300 ng/L), and also had the highest average concentration (1600 ng/L) across all 50 samples. Estimates of potential risks to healthy human adults were greatest for six anti-hypertensive APIs (lisinopril, hydrochlorothiazide, valsartan, atenolol, enalaprilat, and metoprolol), but nevertheless suggest risks of exposure to individual APIs as well as their mixtures are generally very low. Estimates of potential risks to aquatic life were also low for most APIs, but suggest more detailed study of potential ecological impacts from four analytes (sertraline, propranolol, desmethylsertraline, and valsartan). -- Highlights: • Report concentrations of 56 pharmaceuticals in effluents from 50 wastewater plants. • Model and measurements agree that potential risks to healthy adult humans are low. • Model and measurements agree some uncertainties remain about risks to aquatic life. -- Measurements of pharmaceuticals in municipal effluent suggest risks of exposure to healthy human adults are low, but suggest the need for study of potential impacts on aquatic life

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

    International Nuclear Information System (INIS)

    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.)

  1. Pharmacogenomic Genome-Wide Meta-Analysis of Blood Pressure Response to β-Blockers in Hypertensive African Americans.

    Science.gov (United States)

    Gong, Yan; Wang, Zhiying; Beitelshees, Amber L; McDonough, Caitrin W; Langaee, Taimour Y; Hall, Karen; Schmidt, Siegfried O F; Curry, Robert W; Gums, John G; Bailey, Kent R; Boerwinkle, Eric; Chapman, Arlene B; Turner, Stephen T; Cooper-DeHoff, Rhonda M; Johnson, Julie A

    2016-03-01

    African Americans suffer a higher prevalence of hypertension compared with other racial/ethnic groups. In this study, we performed a pharmacogenomic genome-wide association study of blood pressure (BP) response to β-blockers in African Americans with uncomplicated hypertension. Genome-wide meta-analysis was performed in 318 African American hypertensive participants in the 2 Pharmacogenomic Evaluation of Antihypertensive Responses studies: 150 treated with atenolol monotherapy and 168 treated with metoprolol monotherapy. The analysis adjusted for age, sex, baseline BP and principal components for ancestry. Genome-wide significant variants with Pmetoprolol monotherapy, and atenolol add-on therapy: -9.3 versus -4.6, -9.6 versus -4.8, and -9.7 versus -6.4 mm Hg, respectively (3-group meta-analysis P=2.5×10(-8), β=-4.42 mm Hg per variant allele). Similarly, LRRC15 rs11313667 was validated for systolic BP response to β-blocker therapy with 3-group meta-analysis P=7.2×10(-8) and β=-3.65 mm Hg per variant allele. In this first pharmacogenomic genome-wide meta-analysis of BP response to β-blockers in African Americans, we identified novel variants that may provide valuable information for personalized antihypertensive treatment in this group. PMID:26729753

  2. Cutaneous reactions due to antihypertensive drugs

    Directory of Open Access Journals (Sweden)

    Upadhayai J

    2006-01-01

    Full Text Available Out of a total of 1147 patients on antihypertensive drugs, 23 (2.04% developed adverse cutaneous drug reactions (ACDR. The commonest antihypertensive drug group causing ACDR was beta-blockers of which atenolol was the commonest culprit. The second most common group was calcium channel blockers with amlodipine as the commonest offender. The most common patterns of ACDR observed included urticaria followed by lichenoid drug eruption (LDE. We noted 2 new patterns of reactions; (i one patient developed brownish blue pigmentation of nails while on atenolol for 3 years, which resolved in 4 months after withdrawal and (ii another patient on amlodipine for 8 years developed Schamberg′s like purpuric pigmentation, which resolved on withdrawal of drug within 3 months. These findings have not been reported in the literature earlier. This study is presented for paucity of Indian data on ACDR due to antihypertensive drugs, and remarkable advancement in area of cardiovascular and antihypertensive pharmacology and a large number of population taking antihypertensive drugs.

  3. 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

  4. 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

  5. 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

  6. 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

  7. 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...

  8. Studies on vasoconstrictor activity of Curculigo pilosa extracts and of its isolated compounds.

    Science.gov (United States)

    Cometa, M F; Palazzino, G; Galeffi, C; Palmery, M

    2001-01-01

    The Curculigo pilosa total extract, its butanolic fraction (0.5 microg-100 mg/kg) and the most active in vitro compound structurally similar to adrenaline, pilosidine (10 ng-l mg/kg), caused a reversible and dose-dependent increase in blood pressure in anaesthetized rat. This hypertensive effect is partially reversed (90%) by the prior administration of phentolamine (1 mg/kg) and abolished by pre-treatment with phentolamine (1 mg/kg) and atenolol (100 microg/kg). Neither tachiphylaxis nor any toxic effects were observed. These experimental findings suggest an interaction between C. pilosa and the peripheral adrenergic system (particularly with alpha1 and beta1 receptors); the structure of the bioactive glucosides could be important in evoking this effect. PMID:11482757

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

    DEFF Research Database (Denmark)

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

    Dosing of carbon as methanol or ethanol is a common practice in post-denitrification steps during wastewater treatment by MBBR technology. The impact of the carbon dosage on micro-pollutants removal, in terms of type (methanol or ethanol) and concentration was investigated. First, with continuous...... 53% and 30 to 100 % respectively. However, type or concentration of carbon did not lead to different micro-pollutant removal rates. Second, an anoxic-batch test with the same wastewater but containing spiked micro-pollutants (2 ng/mL) was conducted. The batch test showed that acetyl...... operation and indigenous micro-pollutants concentrations, different dosages of methanol and ethanol were used to manipulate the carbon-to-nitrate ratio in the two systems. This test revealed that atenolol, citalopram and trimethoprim were efficiently removed, with removal percentages from 56 to 98%, 17 to...

  10. Emerging organic contaminants in coastal waters: anthropogenic impact, environmental release and ecological risk.

    Science.gov (United States)

    Jiang, Jheng-Jie; Lee, Chon-Lin; Fang, Meng-Der

    2014-08-30

    This study provides a first estimate of the sources, distribution, and risk presented by emerging organic contaminants (EOCs) in coastal waters off southwestern Taiwan. Ten illicit drugs, seven nonsteroidal anti-inflammatory drugs (NSAIDs), five antibiotics, two blood lipid regulators, two antiepileptic drugs, two UV filters, caffeine, atenolol, and omeprazole were analyzed by solid-phase extraction and liquid chromatography coupled to tandem mass spectrometry (SPE-LC-MS/MS). Thirteen EOCs were detected in coastal waters, including four NSAIDs (acetaminophen, ibuprofen, ketoprofen, and codeine), three antibiotics (ampicillin, erythromycin, and cefalexin), three illicit drugs (ketamine, pseudoephedrine, and MDMA), caffeine, carbamazepine, and gemfibrozil. The median concentrations for the 13 EOCs ranged from 1.47 ng/L to 156 ng/L. Spatial variation in concentration of the 13 EOCs suggests discharge into coastal waters via ocean outfall pipes and rivers. Codeine and ampicillin have significant pollution risk quotients (RQ>1), indicating potentially high risk to aquatic organisms in coastal waters. PMID:24439316

  11. Análise de fármacos em águas por SPE-UPLC-ESI-MS/MS

    Directory of Open Access Journals (Sweden)

    Vanessa de Jesus Gaffney

    2014-01-01

    Full Text Available A method was developed for the analysis of 31 pharmaceutical compounds in Lisbon's drinking water system, using solid-phase extraction (SPE and ultra-performance liquid chromatography coupled to tandem mass spectrometry (UPLC-MS/MS. The method was validated through estimation of the linearity range, method detection and quantification limits, matrix effects, precision and accuracy. The method detection and quantification limit ranges were 0.009-10 and 0.03-33 ng/L, respectively. Analytes were quantified in water samples collected from the EPAL (Empresa Portuguesa das Águas Livres S.A. supply system. Carbamazepine, atenolol, sulfadiazine, sulfamethazine, sulfapyridine, sulfamethoxazole, acetaminophen, caffeine and erythromycin were quantified in the analysed samples.

  12. 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

  13. 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.

  14. 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.

  15. A BRIEF VIEW ON ANTIHYPERTENSIVE DRUGS DELIVERY THROUGH TRANSDERMAL PATCHES

    Directory of Open Access Journals (Sweden)

    V. Rastogi*, Pragya, P. Upadhyay

    2012-07-01

    Full Text Available Transdermal Drug Delivery System (TDDS is one of the systems lying under the category of controlled drug delivery, in which the aim is to deliver the drug through skin in a predetermined and controlled rate. Hypertension is one of the common disorder for the mankind. It is not a disease in itself, but is an important risk factor for cardiovascular mortality and morbidity. The present article delivers a brief view on the work been done to increase the bioavailability of various antihypertensive drugs by formulated and delivered as transdermal patches. The different drugs includes carvedilol, metoprolol, atenolol, propranolol, labetolol, verapamil, indapamide, losartan, bisoprolol, timolol maleate, nicardipine hydrochloride, captopril, clonidine, pinacidil, nitrendipine, nicorandil, diltiazem hydrochloride, lisinopril, nifedipine, amlodipine, valsartan, enalapril maleate.

  16. 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

  17. The left atrium, atrial fibrillation, and the risk of stroke in hypertensive patients with left ventricular hypertrophy

    DEFF Research Database (Denmark)

    Wachtell, K.; Devereux, R.B.; Lyle, P.A.;

    2008-01-01

    The Losartan Intervention For Endpoint reduction in hypertension (LIFE) study provided extensive data on predisposing factors, consequences, and prevention of atrial fibrillation (AF) in patients with hypertension and left ventricular (LV) hypertrophy. Randomized losartan-based treatment was...... superior to atenolol-based treatment for reducing new-onset AF and complications, especially stroke, associated with new-onset or pre-existing AF. Potential mechanisms of AF prevention by angiotensin receptor blockade supported by LIFE results include greater reduction in left atrial size and LV...... hypertrophy. Differential effects of antihypertensive treatment on the left atrium and left ventricle may help prevent AF and reduce risk of stroke associated with hypertensive heart disease Udgivelsesdato: 2008/12...

  18. 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

  19. 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

  20. 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

  1. 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.

  2. Die Behandlung der arteriellen Hypertonie mit Angiotensin-Rezeptorblockern

    Directory of Open Access Journals (Sweden)

    Wink K

    2007-01-01

    Full Text Available Angiotensin-II-Typ-1-Rezeptorantagonisten sind die neueste Gruppe zur Behandlung der arteriellen Hypertonie. Pharmakologisch ergeben sich bei den sieben zur Verfügung stehenden Angiotensin-Rezeptorblockern Unterschiede bezüglich der Halbwertszeit und der Rezeptorbindung. Die pharmakologischen Unterschiede bei der Behandlung der arteriellen Hypertonie sind hinsichtlich Blutdrucksenkung vernachlässigbar, hinsichtlich Mortalität und Morbidität sind aber nur Losartan und Valsartan in Vergleichsstudien mit Atenolol bzw. Amlodipin untersucht worden. Da vergleichbare Ergebnisse der Angiotensin-Rezeptorblocker mit den Vergleichssubstanzen vorliegen, kann aufgrund der in placebokontrollierten Studien nachgewiesenen mortalitäts- und morbiditätssenkenden Wirkung von Atenolol davon ausgegangen werden, daß diese Wirkungen auch bei Losartan erzielt werden und, da bei den placebokontrollierten Studien keine ausreichenden Hinweise für eine Mortalitätssenkung bestehen, der morbiditätssenkende Effekt von Amlodipin auch bei Valsartan besteht. Bei den übrigen Angiotensin-Rezeptorblockern wurden keine Mortalitäts- und Morbiditätsstudien durchgeführt, sodaß nur aufgrund des Verhaltens des Surrogatendpunktes Blutdrucksenkung auf einen günstigen Einfluß auf die Mortalität und Morbidität geschlossen werden kann. Hilfsweise kann noch hinzugezogen werden, daß bei den Angiotensin-Rezeptorblockern günstige Wirkungen auf die diabetische Nephropathie und eventuell auf die Entstehung eines Diabetes mellitus bestehen. Es gibt auch Hinweise darauf, daß Angiotensin-Rezeptorblocker bei Patienten nach zerebrovaskulären Ereignissen weiter kardio- und zerebrovaskuläre Ereignisse reduzieren.

  3. A 3-year study on occurrence of emerging contaminants in an urban stream of São Paulo State of Southeast Brazil.

    Science.gov (United States)

    Campanha, Mariele B; Awan, Almas Taj; de Sousa, Diana N R; Grosseli, Guilherme M; Mozeto, Antonio A; Fadini, Pedro S

    2015-05-01

    This manuscript reports a 3-year study on occurrence of pharmaceuticals, hormones, and triclosan in surface waters of a central urban region of São Paulo State of Southeast Brazil (the Monjolinho River in São Carlos). Water samples collected once at every 2 months were pre-concentrated by solid-phase extraction (SPE) and analyzed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS). The most frequently detected compounds in higher concentrations were caffeine, paracetamol, and atenolol (maximum concentrations 129,585, 30,421, and 8199 ng L(-1), respectively), while hormones estrone and 17-β-estradiol were the least detected, in levels up to 14.8 ng L(-1). There was an increasing trend in concentrations of most of the compounds along the river course, especially downstream of the river where there is discharge of both wastewater treatment plant effluent and raw sewage from a particular region of São Carlos city. Concentrations of contaminants were higher during dry periods as a result of decline in the water levels. Decrease in concentrations near the river mouth occurred to different extents for each compound. It was high for caffeine and atenolol, but was very low for carbamazepine and diclofenac. The present study reports the first data about the occurrence of some major emerging contaminants in the Monjolinho River. Besides its regional significance, this work may assist in composing a dataset for water contamination diagnosis focusing on emerging contaminants, both in the Brazilian as well as in the Global studies related to aquatic ecosystems. Such datasets can be helpful for making future public policies on water quality, since these compounds are not yet legally regulated. PMID:25516246

  4. 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

  5. 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.

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

    International Nuclear Information System (INIS)

    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−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 (·OH) and singlet oxygen (1ΔO2), and, the direct reaction with the triplet excited state, 3NOM⁎, also varied but collectively appeared to be the major loss factor. Bimolecular reaction rate constants of the three beta-blockers with 1ΔO2 and ·OH were measured and accounted for 0.02–0.04% and 7.2–38.9% of their loss, respectively. These data suggest that the 3NOM⁎ contributed 50.6–85.4%. Experiments with various 3NOM⁎ 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: ► Photochemical degradation of beta-blockers in the simulated natural waters. ► Reactive Oxygen Species play a minor role in the indirect photodegradation. ► The loss of beta-blockers results from direct reaction with 3DOM⁎.

  7. Two-chiral component microemulsion EKC - chiral surfactant and chiral oil. Part 2: diethyl tartrate.

    Science.gov (United States)

    Kahle, Kimberly A; Foley, Joe P

    2007-08-01

    In this second study on dual-chirality microemulsions containing a chiral surfactant and a chiral oil, a less hydrophobic and lower interfacial tension chiral oil, diethyl tartrate, is employed (Part 1, Foley, J. P. et al.., Electrophoresis, DOI: 10.1002/elps.200600551). Six stereochemical combinations of dodecoxycarbonylvaline (DDCV: R, S, or racemic, 2.00% w/v), racemic 2-hexanol (1.65% v/v), and diethyl tartrate (D, L, or racemic, 0.88% v/v) were examined as pseudostationary phases (PSPs) for the enantioseparation of six chiral pharmaceutical compounds: pseudoephedrine, ephedrine, N-methyl ephedrine, metoprolol, synephrine, and atenolol. Average efficiencies increased with the addition of a chiral oil to R-DDCV PSP formulations. Modest improvements in resolution and enantioselectivity (alpha(enant)) were achieved with two-chiral-component systems over the one-chiral-component microemulsion. Slight enantioselective synergies were confirmed using a thermodynamic model. Results obtained in this study are compared to those obtained in Part 1 as well as those obtained with chiral MEEKC using an achiral, low-interfacial-tension oil (ethyl acetate). Dual-chirality microemulsions with the more hydrophobic oil dibutyl tartrate yielded, relative to diethyl tartrate, higher efficiencies (100,000-134,000 vs. 80,800-94,300), but lower resolution (1.64-1.91 vs. 2.08-2.21) due to lower enantioselectivities (1.060-1.067 vs. 1.078-1.081). Atenolol enantiomers could not be separated with the dibutyl tartrate-based microemulsions but were partially resolved using diethyl tartrate microemulsions. A comparable single-chirality microemulsion based on the achiral oil ethyl acetate yielded, relative to diethyl tartrate, lower efficiency (78 300 vs. 91 600), higher resolution (1.99 vs. 1.83), and similar enantioselectivities. PMID:17597467

  8. 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.

  9. 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

  10. Impact of sludge stabilization processes and sludge origin (urban or hospital) on the mobility of pharmaceutical compounds following sludge landspreading in laboratory soil-column experiments.

    Science.gov (United States)

    Lachassagne, Delphine; Soubrand, Marilyne; Casellas, Magali; Gonzalez-Ospina, Adriana; Dagot, Christophe

    2015-11-01

    This study aimed to determine the effect of sludge stabilization treatments (liming and anaerobic digestion) on the mobility of different pharmaceutical compounds in soil amended by landspreading of treated sludge from different sources (urban and hospital). The sorption and desorption potential of the following pharmaceutical compounds: carbamazepine (CBZ), ciprofloxacin (CIP), sulfamethoxazole (SMX), salicylic acid (SAL), ibuprofen (IBU), paracetamol (PAR), diclofenac (DIC), ketoprofen (KTP), econazole (ECZ), atenolol (ATN), and their solid-liquid distribution during sludge treatment (from thickening to stabilization) were investigated in the course of batch testing. The different sludge samples were then landspread at laboratory scale and leached with an artificial rain simulating 1 year of precipitation adapted to the surface area of the soil column used. The quality of the resulting leachate was investigated. Results showed that ibuprofen had the highest desorption potential for limed and digested urban and hospital sludge. Ibuprofen, salicylic acid, diclofenac, and paracetamol were the only compounds found in amended soil leachates. Moreover, the leaching potential of these compounds and therefore the risk of groundwater contamination depend mainly on the origin of the sludge because ibuprofen and diclofenac were present in the leachates of soils amended with urban sludge, whereas paracetamol and salicylic acid were found only in the leachates of soils amended with hospital sludge. Although carbamazepine, ciprofloxacin, sulfamethoxazole, ketoprofen, econazole, and atenolol were detected in some sludge, they were not present in any leachate. This reflects either an accumulation and/or (bio)degradation of these compounds (CBZ, CIP, SMX, KTP, ECZ, and ATN ), thus resulting in very low mobility in soil. Ecotoxicological risk assessment, evaluated by calculating the risk quotients for each studied pharmaceutical compound, revealed no high risk due to the

  11. 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

  12. 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

  13. 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

  14. 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

  15. 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.

  16. 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

  17. The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation.

    Science.gov (United States)

    Tsume, Yasuhiro; Amidon, Gordon L

    2010-08-01

    The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaivers. The World Health Organization (WHO) has shortened the requisite dissolution time of BCS class III drugs on their Essential Medicine List (EML) from 30 to 15 min for extended biowaivers; however, the impact of the shorter dissolution time on AUC(0-inf) and C(max) is unknown. The objectives of this investigation were to assess the ability of gastrointestinal simulation software to predict the oral absorption of the BCS class I drugs propranolol and metoprolol and the BCS class III drugs cimetidine, atenolol, and amoxicillin, and to perform in silico bioequivalence studies to assess the feasibility of extending biowaivers to BCS class III drugs. The drug absorption from the gastrointestinal tract was predicted using physicochemical and pharmacokinetic properties of test drugs provided by GastroPlus (version 6.0). Virtual trials with a 200 mL dose volume at different drug release rates (T(85%) = 15 to 180 min) were performed to predict the oral absorption (C(max) and AUC(0-inf)) of the above drugs. Both BCS class I drugs satisfied bioequivalence with regard to the release rates up to 120 min. The results with BCS class III drugs demonstrated bioequivalence using the prolonged release rate, T(85%) = 45 or 60 min, indicating that the dissolution standard for bioequivalence is dependent on the intestinal membrane permeability and permeability profile throughout the gastrointestinal tract. The results of GastroPlus simulations indicate that the dissolution rate of BCS class III drugs could be prolonged to the point where dissolution, rather than permeability, would control the overall absorption. For BCS class III drugs with intestinal absorption patterns

  18. 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

  19. 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

  20. 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 }.

  1. 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

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

    Directory of Open Access Journals (Sweden)

    E. M. Manoshkina

    2016-01-01

    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

  3. 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

  4. The influence of radiation sterilisation on some β-blockers in the solid state

    International Nuclear Information System (INIS)

    Research highlights: → Six β-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. → To establish the effects of irradiation on their physico-chemical properties, the compounds were then analysed by DSC, SEM, XRD and FT-IR. → 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). → 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 β-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 (∼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 oC. 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 the FT-IR spectra and in the SEM images

  5. 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

  6. 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

  7. 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

  8. 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.

  9. beta. -Adrenoceptors in human tracheal smooth muscle: characteristics of binding and relaxation

    Energy Technology Data Exchange (ETDEWEB)

    van Koppen, C.J.; Hermanussen, M.W.; Verrijp, K.N.; Rodrigues de Miranda, J.F.; Beld, A.J.; Lammers, J.W.J.; van Ginneken, C.A.M.

    1987-06-29

    Specific binding of (/sup 125/I)-(-)-cyanopindolol to human tracheal smooth muscle membranes was saturable, stereo-selective and of high affinity (K/sub d/ = 5.3 +/- 0.9 pmol/l and R/sub T/ = 78 +/- 7 fmol/g tissue). The ..beta../sub 1/-selective antagonists atenolol and LK 203-030 inhibited specific (/sup 125/I)-(-)-cyanopindolol binding according to a one binding site model with low affinity in nearly all subjects, pointing to a homogeneous BETA/sub 2/-adrenoceptor population. In one subject using LK 203-030 a small ..beta../sub 1/-adrenoceptor subpopulation could be demonstrated. The beta-mimetics isoprenaline, fenoterol, salbutamol and terbutaline recognized high and low affinity agonist binding sites. Isoprenaline's pK/sub H/- and pK/sub L/-values for the high and low affinity sites were 8.0 +/- 0.2 and 5.9 +/- 0.3 respectively. In functional experiments isoprenaline relaxed tracheal smooth muscle strips having intrinsic tone with a pD/sub 2/-value of 6.63 +/- 0.19. 32 references, 4 figures, 2 tables.

  10. 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.

  11. 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.

  12. 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 ...

  13. Drug treatment of hypertension in pregnancy: a critical review of adult guideline recommendations.

    Science.gov (United States)

    Al Khaja, Khalid A J; Sequeira, Reginald P; Alkhaja, Alwaleed K; Damanhori, Awatif H H

    2014-03-01

    This review evaluates the guideline recommendations for the management of hypertension in pregnancy as presented by 25 national/international guidelines developed for the management of arterial hypertension in adults. There is a general consensus that oral α-methyldopa and parenteral labetalol are the drugs of choice for nonsevere and severe hypertension in pregnancy, respectively. Long-acting nifedipine is recommended by various guidelines as an alternative for first-line and second-line therapy in nonsevere and severe hypertension. The safety of β-blockers, atenolol in particular, in early and late stages of pregnancy is unresolved; their use is contraindicated according to several guidelines. Diuretic-associated harmful effects on maternal and fetal outcomes are controversial: their use is discouraged in pregnancy. It is important to develop specific guidelines for treating hypertension in special groups such as adult females of childbearing age and sexually active female adolescents to minimize the risk of adverse effects of drugs on the fetus. In several guidelines, the antihypertensive classes, recommended drug(s), intended drug formulation, and route of administration are not explicit. These omissions should be addressed in future guideline revisions in order to enhance the guidelines' utility and credibility in clinical practice. PMID:24384846

  14. Effects of chronic isoproterenol administration of β1-adrenoceptors and growth of pancreas of young and adult rats

    International Nuclear Information System (INIS)

    [3H]Dihydroalprenolol (DHA) binding of membranes of adult pancreas differed from that of pancreas of young rats, and the DHA binding in the presence of atenolol or butoxamine also was different in the two age groups. The adult pancreas had 93% β2- and 7% β1-adrenoceptors and did not exhibit an increased incorporation of [3H]thymidine into deoxyribonucleic acid (DNA) following 2 days of DL-isoproterenol (ISO) administration; in contrast, pancreas of the 20-day-old rat had 71% β2-adrenoceptors and 27% β1-adrenoceptors and exhibited a 34-fold increase over that of adult, and a 6-fold increase over that of the control 20-day-old pancreas. Acinar cell differentiation was also accelerated by a 7-day regimen of ISO administration from 13 to 20 days of age. These growth responses to ISO appear to be β1 mediated. The lack of β1-adrenoceptors in the adult may account for the failure of the adult pancreas to exhibit a growth response to ISO

  15. 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.

  16. 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.

  17. 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.

  18. 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.

  19. 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.

  20. 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

  1. Characterizing redox conditions and monitoring attenuation of selected pharmaceuticals during artificial recharge through a reactive layer.

    Science.gov (United States)

    Valhondo, Cristina; Carrera, Jesús; Ayora, Carlos; Tubau, Isabel; Martinez-Landa, Lurdes; Nödler, Karsten; Licha, Tobias

    2015-04-15

    A permeable reactive layer was installed at the floor of an infiltration basin. The reactive layer comprised 1) vegetable compost to provide a sorption surface for neutral organic compounds and to release easily degradable organic matter, thus generating a sequence of redox states, and 2) minor amounts of clay and iron oxide to increase sorption of cationic and anionic species, respectively. Field application of this design was successful in generating denitrification, and manganese-, and iron-reducing conditions beneath the basin. This, together with the increase in types of sorption sites, may explain the improved removal of three of the four selected pharmaceuticals compared with their behavior prior to installation of the layer. After installation of the reactive layer, atenolol concentrations were below the detection limits in the vadose zone. Moreover, concentrations of gemfibrozil and cetirizine were reduced to 20% and 40% of their initial concentrations, respectively, after 200 h of residence time. In contrast, prior to installation of the reactive layer, the concentrations of these three pharmaceuticals in both the vadose zone and the aquifer were more than 60% of the initial concentration. Carbamazepine exhibited recalcitrant behavior both prior to and after the reactive barrier installation. PMID:25625636

  2. 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

  3. 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

  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. 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

  6. 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.

  7. Nicotine promotes cell proliferation via α7-nicotinic acetylcholine receptor and catecholamine-synthesizing enzymes-mediated pathway in human colon adenocarcinoma HT-29 cells

    International Nuclear Information System (INIS)

    Cigarette smoking has been implicated in colon cancer. Nicotine is a major alkaloid in cigarette smoke. In the present study, we showed that nicotine stimulated HT-29 cell proliferation and adrenaline production in a dose-dependent manner. The stimulatory action of nicotine was reversed by atenolol and ICI 118,551, a β1- and β2-selective antagonist, respectively, suggesting the role of β-adrenoceptors in mediating the action. Nicotine also significantly upregulated the expression of the catecholamine-synthesizing enzymes [tyrosine hydroxylase (TH), dopamine-β-hydroxylase (DβH) and phenylethanolamine N-methyltransferase]. Inhibitor of TH, a rate-limiting enzyme in the catecholamine-biosynthesis pathway, reduced the actions of nicotine on cell proliferation and adrenaline production. Expression of α7-nicotinic acetylcholine receptor (α7-nAChR) was demonstrated in HT-29 cells. Methyllycaconitine, an α7-nAChR antagonist, reversed the stimulatory actions of nicotine on cell proliferation, TH and DβH expression as well as adrenaline production. Taken together, through the action on α7-nAChR nicotine stimulates HT-29 cell proliferation via the upregulation of the catecholamine-synthesis pathway and ultimately adrenaline production and β-adrenergic activation. These data reveal the contributory role α7-nAChR and β-adrenoceptors in the tumorigenesis of colon cancer cells and partly elucidate the carcinogenic action of cigarette smoke on colon cancer

  8. 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.

  9. 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.; Wachtell, K.; Papademetriou, V.; Nieminen, M.S.; Dahlof, B.; Devereux, R.B.

    2008-01-01

    , -15% at year 2, and -16% at year 3 follow-up, and was sustained through year 4 and year 5 follow-ups; change in PP/SVi was related to increased SVi and decreased PP during the annual follow-ups, but not to LV mass change. Restricting analyses to the first two follow-ups to ensure highest statistical...... power, age >65 and diabetes were associated with higher PP/SVi at baseline and throughout follow-ups; black participants and women had baseline PP/SVi mean values comparable with those of their counterparts, showed blunted PP/SVi reduction after 1 year, but differences became smaller 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...

  10. 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

  11. 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

  12. 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

  13. Determination of excipient based solubility increases using the CheqSol method.

    Science.gov (United States)

    Etherson, Kelly; Halbert, Gavin; Elliott, Moira

    2014-04-25

    Aqueous solubility is an essential characteristic assessed during drug development to determine a compound's drug-likeness since solubility plays an important pharmaceutical role. However, nearly half of the drug candidates discovered today display poor water solubility; therefore methods have to be applied to increase solubility. Solubility determination using the CheqSol method is a novel rapid solubility screening technique for ionisable compounds. The aim of this study is to determine if the CheqSol method can be employed to determine solubility increases of four test drugs (ibuprofen, gliclazide, atenolol and propranolol) induced by non-ionising excipients such as hydroxypropyl-β-cyclodextrin and poloxamers 407 and 188. CheqSol assays were performed for the drugs alone or in combination with varying solubiliser concentrations. The measured intrinsic solubility of all four drugs increased with all the excipients tested in an excipient concentration dependent manner providing results consistent with previous literature. The results demonstrate that it may be possible to use this method to determine the solubility increases induced by non-ionic solubilising excipients with results that are comparable to standard equilibrium based solubility techniques. Since the technique is automated and requires only small drug quantities it may serve as a useful solubility or formulation screening tool providing more detailed physicochemical information than multiwell plate or similar visual systems. PMID:24513529

  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. Evaluation of pharmaceuticals in surface water: reliability of PECs compared to MECs.

    Science.gov (United States)

    Celle-Jeanton, Hélène; Schemberg, Dimitri; Mohammed, Nabaz; Huneau, Frédéric; Bertrand, Guillaume; Lavastre, Véronique; Le Coustumer, Philippe

    2014-12-01

    Due to the current analytical processes that are not able to measure all the pharmaceutical molecules and to the high costs and the consumption of time to sample and analyze PhACs, models to calculate Predicted Environmental Concentrations (PECs) have been developed. However a comparison between MECs and PECs, taking into account the methods of calculations and peculiarly the parameters included in the calculation (consumption data, pharmacokinetic parameters, elimination rate in STPs and in the environment), is necessary to assess the validity of PECs. MEC variations of sixteen target PhACs [acetaminophen (ACE), amlodipine (AML), atenolol (ATE), caffeine (CAF), carbamazepine (CAR), doxycycline (DOX), epoxycarbamazepine (EPO), fluvoxamine (FLU), furosemide (FUR), hydrochlorothiazide (HYD), ifosfamide (IFO), losartan (LOS), pravastatin (PRA), progesterone (PROG), ramipril (RAM), trimetazidine (TRI)] have been evaluated during one hydrological cycle, from October 2011 to October 2012 and compared to PECs calculated by using an adaptation of the models proposed by Heberer and Feldmann (2005) and EMEA (2006). Comparison of PECs and MECS has been achieved for six molecules: ATE, CAR, DOX, FUR, HYD and PRA. DOX, FUR and HYD present differences between PECs and MECs on an annual basis but their temporal evolutions follow the same trends. PEC evaluation for these PhACs could then be possible but need some adjustments of consumption patterns, pharmacokinetic parameters and/or mechanisms of (bio)degradation. ATE, CAR and PRA are well modeled; PECs can then be used as reliable estimation of concentrations without any reserve. PMID:25080069

  16. 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. PMID:26282775

  17. 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.

  18. Multi-residue enantiomeric analysis of pharmaceuticals and their active metabolites in the Guadalquivir River basin (South Spain) by chiral liquid chromatography coupled with tandem mass spectrometry.

    Science.gov (United States)

    López-Serna, Rebeca; Kasprzyk-Hordern, Barbara; Petrović, Mira; Barceló, Damià

    2013-07-01

    This paper describes the development and application of a multi-residue chiral liquid chromatography coupled with tandem mass spectrometry method for simultaneous enantiomeric profiling of 18 chiral pharmaceuticals and their active metabolites (belonging to several therapeutic classes including analgesics, psychiatric drugs, antibiotics, cardiovascular drugs and β-agonists) in surface water and wastewater. To the authors' knowledge, this is the first time an enantiomeric method including such a high number of pharmaceuticals and their metabolites has been reported. Some of the pharmaceuticals have never been studied before in environmental matrices. Among them are timolol, betaxolol, carazolol and clenbuterol. A monitoring programme of the Guadalquivir River basin (South Spain), including 24 sampling sites and five wastewater treatment plants along the basin, revealed that enantiomeric composition of studied pharmaceuticals is dependent on compound and sampling site. Several compounds such as ibuprofen, atenolol, sotalol and metoprolol were frequently found as racemic mixtures. On the other hand, fluoxetine, propranolol and albuterol were found to be enriched with one enantiomer. Such an outcome might be of significant environmental relevance as two enantiomers of the same chiral compound might reveal different ecotoxicity. For example, propranolol was enriched with S(-)-enantiomer, which is known to be more toxic to Pimephales promelas than R(+)-propranolol. Fluoxetine was found to be enriched with S(+)-enantiomer, which is more toxic to P. promelas than R(-)-fluoxetine. PMID:23579471

  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. 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

  1. [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

  2. Adrenal secretion of catecholamines by inhalation of radon water in relation to an increase of the tissue perfusion rate in rabbits

    International Nuclear Information System (INIS)

    To clarify the relationship between the increase in subcutaneous tissue perfusion rate (TPR) upon inhalation of radon water and the vasoactive effects of radon, rabbits inhaled nebulized water containing 14,000-18,000 Bq/1 radon (radon group) taken from Ikeda Mineral Spring, Shimane, Japan. Control rabbits inhaled radon water from the same springs which had been kept for over 10 radon half-life periods. TPR was evaluated 15 minutes after the beginning of inhalation by mass spectrometry. After inhalation for 90 minutes, plasma and adrenal glands were removed, and levels of adrenaline and noradrenaline were analyzed by high-performance liquid chromatography (THI method). Each group was divided into 4 subgroups according to intravenously injected medication as follows: 1) no medication (without adrenergic blocker), 2) phentolamine (α-blocker), 0.05 mg/kg/min, 3) propranolol (non-selective β-blocker), 1 mg/kg/, and 4) atenolol (selective β-blocker), 6 mg/kg. In the radon group, plasma adrenaline and noradrenaline levels were significantly higher (p1-action of catecholamines contributes to the increase in tissue perfusion. (author)

  3. Towards high potential magnetic biocatalysts for on-demand elimination of pharmaceuticals.

    Science.gov (United States)

    Kumar, Vaidyanathan Vinoth; Cabana, Hubert

    2016-01-01

    The present study investigated the applicability of a laccase based bioprocess for the treatment of a mixture containing 13 selected pharmaceuticals. To do so, laccase was immobilized as cross-linked enzyme aggregates (MAC-CLEAs) on amine functionalized magnetic nanoparticles using chitosan/1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride (EDAC) as the cross-linking system. The activity recovery of laccase reached 61.4% under the optimal conditions of MAC-CLEAs formation. The latter exhibited enhanced storage stability over one year at 4°C and showed better temperature resistance compared to its soluble counterpart. The biocatalysts were properly recycled and the catalytic activity recovery was good even after a hundred and fifty batch reactions. Complete removal of pharmaceuticals like acetaminophen, diclofenac, mefenamic acid, atenolol and epoxy carbamazepine and partial removal of fenofibrate, diazepam, trimethoprim, and ketoprofen by laccase was achieved within 12h of incubation, whereas efficient removal of indometacin required the presence of mediator. PMID:26476168

  4. Solubility and pKa of select pharmaceuticals in water, ethanol, and 1-octanol

    International Nuclear Information System (INIS)

    Solubilities of six pharmaceuticals, namely nadolol, atenolol, bifonazole, nimesulide, estrone, mefenamic acid at constant pH, were measured over the range of temperature from (240 to 340) K in three important for drug solvents: water, ethanol, and 1-octanol using the dynamic method and spectroscopic UV-Vis method. Dissociation constants and corresponding pKa values of the drugs were obtained with the Bates-Schwarzenbach method using UV-Vis Perkin-Elmer Lambda 35 Spectrophotometer at temperature 298.15 K in the buffer solutions. Our experimental pKa values for nadolol, bifonazole, nimesulide, and mefenamic acid are 9.3, 5.85, 7.34, and 3.88, respectively. The basic thermal properties of pure drugs i.e. fusion and glass-transition temperatures, as well as the enthalpy of fusion and the molar heat capacity at the glass-transition (at constant pressure) have been measured using the differential scanning microcalorimetry technique (DSC). Molar volumes have been calculated with the Barton group contribution method. The experimental solubility results have been correlated by means of three commonly known GE equations: the Wilson, NRTL, and UNIQUAC with the assumption that the systems studied here are simple eutectic mixtures. The activity coefficients of pharmaceuticals in saturated solutions in each correlated binary mixture were calculated from the experimental results. Prediction of solubility in water at T = 298.15 K was made by the group contribution method.

  5. 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.

  6. 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

  7. 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

  8. 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

  9. Assessment of the Presence of Pharmaceutical Compounds in Seawater Samples from Coastal Area of Gran Canaria Island (Spain

    Directory of Open Access Journals (Sweden)

    José Juan Santana-Rodríguez

    2013-05-01

    Full Text Available This study presents the evaluation of seven pharmaceutical compounds belonging to different commonly used therapeutic classes in seawater samples from coastal areas of Gran Canaria Island. The target compounds include atenolol (antihypertensive, acetaminophen (analgesic, norfloxacin and ciprofloxacin (antibiotics, carbamazepine (antiepileptic and ketoprofen and diclofenac (anti-inflammatory. Solid phase extraction (SPE was used for the extraction and preconcentration of the samples, and liquid chromatography tandem mass spectrometry (LC-MS/MS was used for the determination of the compounds. Under optimal conditions, the recoveries obtained were in the range of 78.3% to 98.2%, and the relative standard deviations were less than 11.8%. The detection and quantification limits of the method were in the ranges of 0.1–2.8 and 0.3–9.3 ng·L−1, respectively. The developed method was applied to evaluate the presence of these pharmaceutical compounds in seawater from four outfalls in Gran Canaria Island (Spain during one year. Ciprofloxacin and norfloxacin were found in a large number of samples in a concentration range of 9.0–3551.7 ng·L−1. Low levels of diclofenac, acetaminophen and ketoprofen were found sporadically.

  10. Identification of transformation products from β-blocking agents formed in wetland microcosms using LC-Q-ToF.

    Science.gov (United States)

    Svan, Alfred; Hedeland, Mikael; Arvidsson, Torbjörn; Jasper, Justin T; Sedlak, David L; Pettersson, Curt E

    2016-03-01

    Identification of degradation products from trace organic compounds, which may retain the biological activity of the parent compound, is an important step in understanding the long-term effects of these compounds on the environment. Constructed wetlands have been successfully utilized to remove contaminants from wastewater effluent, including pharmacologically active compounds. However, relatively little is known about the transformation products formed during wetland treatment. In this study, three different wetland microcosm treatments were used to determine the biotransformation products of the β-adrenoreceptor antagonists atenolol, metoprolol and propranolol. LC/ESI-Q-ToF run in the MS(E) and MS/MS modes was used to identify and characterize the degradation products through the accurate masses of precursor and product ions. The results were compared with those of a reference standard when available. Several compounds not previously described as biotransformation products produced in wetlands were identified, including propranolol-O-sulfate, 1-naphthol and the human metabolite N-deaminated metoprolol. Transformation pathways were significantly affected by microcosm conditions and differed between compounds, despite the compounds' structural similarities. Altogether, a diverse range of transformation products in wetland microcosms were identified and elucidated using high resolving MS. This work shows that transformation products are not always easily predicted, nor formed via the same pathways even for structurally similar compounds. Copyright © 2016 John Wiley & Sons, Ltd. PMID:26956388

  11. Photocatalytic degradation kinetics and mechanism of environmental pharmaceuticals in aqueous suspension of TiO2: A case of β-blockers

    International Nuclear Information System (INIS)

    This study investigated the photocatalytic degradation of three β-blockers in TiO2 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-1 for atenolol, metoprolol and propranolol, respectively. After 240 min irradiation, the reaction intermediates were completely mineralized to CO2 and the nitrogen was predominantly as NH4+. The influence of initial pH and β-blocker concentration on the kinetics was also studied. From adsorption studies it appears that the photocatalytic degradation occurred mainly on the surface of TiO2. Further studies indicated that surface reaction with ·OH radical was principally responsible for the degradation of these three β-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 β-blockers.

  12. Comparison of Mass Transfer Models for Determination of the Intestinal Permeability

    Directory of Open Access Journals (Sweden)

    P Zakeri-Milani

    2008-09-01

    Full Text Available Background and the purpose of the study: In determination of the permeability of the intestinal wall by external perfusion techniques, several models have been proposed. In the present study three models were used for experimental results that differ in their convection and diffusion assumptions. Material and Methods: Permeability coefficients for 13 compounds (metoprolol, propranolol, naproxen, ketoprofen, furosemide, hydrochlorothiazide, cimetidine, ranitidine, atenolol, piroxicam, antipyrine, ibuprofen and carbamazepine with known human intestinal permeability values were determined in anaesthetized rats by different mass transfer models and plotted versus the observed human intestinal permeabilities. Results: The calculated dimensionless wall permeability values were in the range of 0.37 - 4.85, 0.38-6.54 and 0.41-16.59 for complete radial mixing, mixing tank and laminar flow models respectively. The results indicated that all of the models work relatively well for our data despite fundamentally different assumptions. The wall permeabilities were in the order laminar flow > mixing tank > complete radial mixing. Conclusion: Although laminar flow model provides the most direct measure of the intrinsic wall permeability, it has limitations for highly permeable drugs such as ibuprofen. The normal physiological hydrodynamics is more complex and more investigation is required to find out the real hydrodynamics.

  13. Seasonal Monitoring of Cardiovascular and Antiulcer Agents’ Concentrations in Stream Waters Encompassing a Capital City

    Directory of Open Access Journals (Sweden)

    Renáta Varga

    2013-01-01

    Full Text Available Nowadays monitoring pharmaceutical residues from surface waters is a widespread analytical task. Most of the studies are conducted from river waters or sewage treatment plants and mainly in Western Europe or North America. Such studies are seldom published from Eastern Europe, especially from stream waters, even though the prescription and consumption patterns of drugs as well as wastewater treatment procedures are very dissimilar. In Hungary the active substance of the most often prescribed drugs are cardiovascular and antiulcer agents. Hence in our study compounds belonging to these two groups were seasonally monitored in two main streams encompassing the Buda side of the Hungarian capital city and flowing into the Danube. To obtain data on the occurrence, fate, and seasonal variation of the compounds, samples were taken from altogether eleven points located near wastewater treatment plants and confluences. The results gave no identifiable pattern in the seasonal variation of concentrations but the contribution of the tributaries and wastewater treatment plants could be followed as expected. From the runoff corrected estuary concentrations the annual contribution of these streams to pharmaceutical pollution of the Danube could be estimated to be in excess of 1 kilogram for atenolol, famotidine, metoprolol, ranitidine, and sotalol.

  14. The Impact of Different Proportions of a Treated Effluent on the Biotransformation of Selected Micro-Contaminants in River Water Microcosms

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    Karsten Nödler

    2014-10-01

    Full Text Available Attenuation of micro-contaminants is a very complex field in environmental science and evidence suggests that biodegradation rates of micro-contaminants in the aqueous environment depend on the water matrix. The focus of the study presented here is the systematic comparison of biotransformation rates of caffeine, carbamazepine, metoprolol, paracetamol and valsartan in river water microcosms spiked with different proportions of treated effluent (0%, 0.1%, 1%, and 10%. Biotransformation was identified as the dominating attenuation process by the evolution of biotransformation products such as atenolol acid and valsartan acid. Significantly decreasing biotransformation rates of metoprolol were observed at treated effluent proportions ≥0.1% whereas significantly increasing biotransformation rates of caffeine and valsartan were observed in the presence of 10% treated effluent. Potential reasons for the observations are discussed and the addition of adapted microorganisms via the treated effluent was suggested as the most probable reason. The impact of additional phosphorus on the biodegradation rates was tested and the experiments revealed that phosphorus-limitation was not responsible.

  15. Aqueous chlorination of acebutolol: kinetics, transformation by-products, and mechanism.

    Science.gov (United States)

    Khalit, Wan Nor Adira Wan; Tay, Kheng Soo

    2016-02-01

    This study investigated the reaction kinetics and the transformation by-products of acebutolol during aqueous chlorination. Acebutolol is one of the commonly used β-blockers for the treatment of cardiovascular diseases. It has been frequently detected in the aquatic environment. In the kinetics study, the second-order rate constant for the reaction between acebutolol and chlorine (k app) was determined at 25 ± 0.1 °C. The degradation of acebutolol by free available chlorine was highly pH dependence. When the pH increased from 6 to 8, it was found that the k app for the reaction between acebutolol and free available chlorine was increased from 1.68 to 11.2 M(-1) min(-1). By comparing with the reported k app values, the reactivity of acebutolol toward free available chlorine was found to be higher than atenolol and metoprolol but lower than nadolol and propranolol. Characterization of the transformation by-products formed during the chlorination of acebutolol was carried out using liquid chromatography-quadrupole time-of-flight high-resolution mass spectrometry. Seven major transformation by-products were identified. These transformation by-products were mainly formed through dealkylation, hydroxylation, chlorination, and oxidation reactions. PMID:26423291

  16. 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.

  17. 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

  18. 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

  19. 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

  20. 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.

  1. 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。

  2. 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

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

    International Nuclear Information System (INIS)

    Potential applications in drug delivery from nanostructures composed of two oppositely charged polymethacrylates, eudragit® L100 (EL) and eudragit® 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-D50)–EEX, were obtained by mixing the aqueous dispersions of both polyelectrolytes at room temperature in an ultrasound bath. Dispersions of (EL-D50) 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.

  4. Carvedilol-mediated antioxidant protection against doxorubicin-induced cardiac mitochondrial toxicity

    International Nuclear Information System (INIS)

    The cardiotoxicity associated with doxorubicin (DOX) therapy limits the total cumulative dose and therapeutic success of active anticancer chemotherapy. Cardiac mitochondria are implicated as primary targets for DOX toxicity, which is believed to be mediated by the generation of highly reactive free radical species of oxygen from complex I of the mitochondrial electron transport chain. The objective of this study was to determine if the protection demonstrated by carvedilol (CV), a β-adrenergic receptor antagonist with strong antioxidant properties, against DOX-induced mitochondrial-mediated cardiomyopathy [Toxicol. Appl. Pharmacol. 185 (2002) 218] is attributable to its antioxidant properties or its β-adrenergic receptor antagonism. Our results confirm that DOX induces oxidative stress, mitochondrial dysfunction, and histopathological lesions in the cardiac tissue, all of which are inhibited by carvedilol. In contrast, atenolol (AT), a β-adrenergic receptor antagonist lacking antioxidant properties, preserved phosphate energy charge but failed to protect against any of the indexes of DOX-induced oxidative mitochondrial toxicity. We therefore conclude that the cardioprotective effects of carvedilol against DOX-induced mitochondrial cardiotoxicity are due to its inherent antioxidant activity and not to its β-adrenergic receptor antagonism

  5. 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

  6. 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

  7. 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

  8. 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

  9. 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

  10. 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

  11. Affinity and selectivity of beta-adrenoceptor antagonists in vitro

    International Nuclear Information System (INIS)

    The potency order of the catecholamines (-)-isoprenaline (Iso), (-)-noradrenaline (NA), and (-)-adrenaline (Adr) in competition for radiolabelled sites is used for their pharmacological classification. It is shown that the radioligand 3H-CGP 12177 exclusively labels beta 1-adrenoceptors in rat salivary gland membranes (Iso greater than NA greater than Adr), and beta 2-adrenoceptors in rat reticulocytes (Iso greater than Adr greater than or equal to NA). These models are then used to derive the subtype-selectivity of the classical beta-adrenoceptor antagonists (+/-)-propranolol (prop; twofold beta 2-selective) and (+/-)-atenolol (aten; 35-fold beta 1-selective), as well as of the newer antagonists (+/-)-betaxolol and (+/-)-bisoprolol (betax and biso; 35-fold and 75-fold beta 1-selective, respectively). The ligand with the highest selectivity is ICI 118,551 (ICI), with a 300-fold beta 2-subtype selectivity. For comparison with antagonistic effects in humans at given plasma concentrations, the equilibrium dissociation constants of the ligands are measured in the presence of native human plasma and yield values for the relative selectively labelled subtype in the mean (Ki-values in nmol/l): prop: 20, aten: 250, biso: 24, betax: 23, and ICI: 2.5

  12. Evaluation and performance of desorption electrospray ionization using a triple quadrupole mass spectrometer for quantitation of pharmaceuticals in plasma.

    Science.gov (United States)

    Kennedy, Joseph H; Wiseman, Justin M

    2010-02-01

    The present work describes the methodology and investigates the performance of desorption electrospray ionization (DESI) combined with a triple quadrupole mass spectrometer for the quantitation of small drug molecules in human plasma. Amoxepine, atenolol, carbamazepine, clozapine, prazosin, propranolol and verapamil were selected as target analytes while terfenadine was selected as the internal standard common to each of the analytes. Protein precipitation of human plasma using acetonitrile was utilized for all samples. Limits of detection were determined for all analytes in plasma and shown to be in the range 0.2-40 ng/mL. Quantitative analysis of amoxepine, prazosin and verapamil was performed over the range 20-7400 ng/mL and shown to be linear in all cases with R(2) >0.99. In most cases, the precision (relative standard deviation) and accuracy (relative error) of each method were less than or equal to 20%, respectively. The performance of the combined techniques made it possible to analyze each sample in 15 s illustrating DESI tandem mass spectrometry (MS/MS) as powerful tool for the quantitation of analytes in deproteinized human plasma. PMID:20049888

  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. 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.

  15. 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

  16. 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

  17. 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

  18. 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.

  19. 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

  20. 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

  1. Cromatografia líquida com fase quiral aplicada na separação enantiomérica de fármacos cardiovasculares Applied chiral phase liquid chromatography in enantiomeric separation of cardiovascular drugs

    Directory of Open Access Journals (Sweden)

    Anil Kumar Singh

    2006-12-01

    Full Text Available A maioria dos agentes terapêuticos, freqüentemente prescritos, é formulada e comercializada sob a forma racêmica, embora, para alguns deles, já tenha sido demonstrado que os efeitos farmacológicos e/ou tóxicos estejam relacionados apenas a um dos enantiômeros. Além disso, é conhecido o fato de que os enantiômeros podem apresentar perfis farmacocinéticos e farmacodinâmicos diferentes. Neste trabalho foram selecionados compostos que fazem parte de um importante grupo de fármacos muito empregados na terapêutica. São fármacos freqüentemente prescritos em doenças cardiovasculares. As separações enantioméricas diretas do atenolol, betaxolol, metoprolol e nadolol foram obtidas utilizando-se fase estacionária quiral do tipo carbamato de celulose tris-3,5-dimetilfenil, Chiralcel OD®, (250 x 4.6 mm, 10 µm. Os enantiômeros do pindolol foram separados com fase estacionária quiral derivada de dinitrobenzoil (DNB, a-Burke 2®, (250 x 4.6 mm, 10 µm. Os fármacos foram cromatografados à temperatura ambiente, com volume de injeção de 20 µL. A detecção foi efetuada em 276 nm exceto para o pindolol, que foi detectado em 220 nm. Os métodos propostos neste trabalho empregando CLAE-FEQs oferecem vantagens sobre as técnicas clássicas de separação de enantiômeros e podem ser empregados na análise quantitativa dos enantiômeros em preparações farmacêuticas e amostras biológicas.The majority of frequently prescribed therapeutic agents are formulated and commercialized in the racemic form, even though, for some of them, it has already been demonstrated that the pharmacological and/or toxicological effects are associated only with one of the enantiomers. Moreover, it is well known that these antipodes can present different pharmacokinetic and pharmacodynamic profiles. In this work we selected drugs that belong to an important group of pharmaceuticals, frequently prescribed in the treatment of cardiovascular disorders. The direct

  2. 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

  3. 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

  4. 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

  5. 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

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

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    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.

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

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    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.

  8. 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.

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

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    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.

  11. 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

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

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    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

  13. 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

  14. Activity in prelimbic cortex is required for adjusting the anxiety response level during the elevated plus-maze retest.

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    Stern, C A J; Do Monte, F H M; Gazarini, L; Carobrez, A P; Bertoglio, L J

    2010-09-29

    The prelimbic (PL) subregion of medial prefrontal cortex has been implicated in anxiety regulation. It is unknown, however, whether PL cortex also serves to fine-tuning the level of anxiety-related behavior exhibited on the next exposure to the same potentially threatening situation. To address this, we infused cobalt (1.0 mM) to temporarily inactivate the PL cortex during testing, post-testing or retesting in the elevated plus-maze (EPM). This protocol was chosen because it allowed us to concurrently investigate anxiety and the process of aversive learning and memory. PL cortex inactivation during the EPM testing increased the exploration of open-arms, substantiating its role in anxiety. PL cortex inactivation during the EPM retesting counteracted the further avoidance to open-arms exhibited by rats. Interestingly, as evidenced by min-by-min analysis, the cobalt-treated group behaved on EPM retesting as did the vehicle-treated group on EPM testing. This result may imply that activity in PL cortex is necessary for retrieving previously learned information that adjusts the anxiety response level on EPM retesting. Alternatively, a simple reduction in anxiety could explain the cobalt-induced increase in retest open-arms exploration. Neither test nor post-test PL cortex inactivation affected the further avoidance to open-arms observed on EPM retesting. To extend the investigation of PL cortex role in the regulation of open-arms avoidance, we infused other drugs prior to testing or retesting in the EPM. Antagonism of PL cortex adrenergic beta-1 receptors with atenolol (10 nmol), cholinergic muscarinic receptors with scopolamine (20 nmol) or glutamatergic N-methyl-d-aspartic acid (NMDA) receptors with AP5 (6.0 nmol) interfered with the level of open-arms exploration on testing, but not on retesting. PMID:20620194

  15. 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

  16. Pharmacological Evidence that Histamine H3 Receptors Mediate Histamine-Induced Inhibition of the Vagal Bradycardic Out-flow in Pithed Rats.

    Science.gov (United States)

    García, Mónica; García-Pedraza, José Ángel; Villalón, Carlos M; Morán, Asunción

    2016-02-01

    In vivo stimulation of cardiac vagal neurons induces bradycardia by acetylcholine (ACh) release. As vagal release of ACh may be modulated by autoreceptors (muscarinic M2 ) and heteroreceptors (including serotonin 5-HT1 ), this study has analysed the pharmacological profile of the receptors involved in histamine-induced inhibition of the vagal bradycardic out-flow in pithed rats. For this purpose, 180 male Wistar rats were pithed, artificially ventilated and pre-treated (i.v.) with 1 mg/kg atenolol, followed by i.v. administration of physiological saline (1 ml/kg), histamine (10, 50, 100 and 200 μg/kg) or the selective histamine H1 (2-pyridylethylamine), H2 (dimaprit), H3 (methimepip) and H4 (VUF 8430) receptor agonists (1, 10, 50 and 100 μg/kg each). Under these conditions, electrical stimulation (3, 6 and 9 Hz; 15 ± 3 V and 1 ms) of the vagus nerve resulted in frequency-dependent bradycardic responses, which were (i) unchanged during the infusions of saline, 2-pyridylethylamine, dimaprit or VUF 8430; and (ii) dose-dependently inhibited by histamine or methimepip. Moreover, the inhibition of the bradycardia caused by 50 μg/kg of either histamine or methimepip (which failed to inhibit the bradycardic responses to i.v. bolus injections of acetylcholine; 1-10 μg/kg) was abolished by the H3 receptor antagonist JNJ 10181457 (1 mg/kg, i.v.). In conclusion, our results suggest that histamine-induced inhibition of the vagal bradycardic out-flow in pithed rats is mainly mediated by pre-junctional activation of histamine H3 receptors, as previously demonstrated for the vasopressor sympathetic out-flow and the vasodepressor sensory CGRPergic (calcitonin gene-related peptide) out-flow. PMID:26301462

  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. Allosteric interactions between the oxytocin receptor and the β2-adrenergic receptor in the modulation of ERK1/2 activation are mediated by heterodimerization.

    Science.gov (United States)

    Wrzal, Paulina K; Devost, Dominic; Pétrin, Darlaine; Goupil, Eugénie; Iorio-Morin, Christian; Laporte, Stéphane A; Zingg, Hans H; Hébert, Terence E

    2012-01-01

    The oxytocin receptor (OTR) and the β(2)-adrenergic receptor (β(2)AR) are key regulators of uterine contraction. These two receptors are targets of tocolytic agents used to inhibit pre-term labor. Our recent study on the nature of OTR- and β(2)AR-mediated ERK1/2 activation in human hTERT-C3 myometrial cells suggested the presence of an OTR/β(2)AR hetero-oligomeric complex (see companion article). The goal of this study was to investigate potential allosteric interactions between OTR and β(2)AR and establish the nature of the interactions between these receptors in myometrial cells. We found that OTR-mediated ERK1/2 activation was attenuated significantly when cells were pretreated with the β(2)AR agonist isoproterenol or two antagonists, propranolol or timolol. In contrast, pretreatment of cells with a third β(2)AR antagonist, atenolol resulted in an increase in OTR-mediated ERK1/2 activation. Similarly, β(2)AR-mediated ERK1/2 activation was strongly attenuated by pretreatment with the OTR antagonists, atosiban and OTA. Physical interactions between OTR and β(2)AR were demonstrated using co-immunoprecipitation, bioluminescence resonance energy transfer (BRET) and protein-fragment complementation (PCA) assays in HEK 293 cells, the latter experiments indicating the interactions between the two receptors were direct. Our analyses suggest physical interactions between OTR and β(2)AR in the context of a new heterodimer pair lie at the heart of the allosteric effects. PMID:21963428

  19. Polypharmacy among older adults in Tehran

    Directory of Open Access Journals (Sweden)

    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.

  20. 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

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

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    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.

  2. 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

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

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

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    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

  5. 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.

  6. Environmental optimization of continuous flow ozonation for urban wastewater reclamation.

    Science.gov (United States)

    Rodríguez, Antonio; Muñoz, Iván; Perdigón-Melón, José A; Carbajo, José B; Martínez, María J; Fernández-Alba, Amadeo R; García-Calvo, Eloy; Rosal, Roberto

    2012-10-15

    Wastewater samples from the secondary clarifier of two treatment plants were spiked in the microgram-to-tens-of-microgram per liter range with diuron (herbicide), ibuprofen and diclofenac (anti-inflammatory drugs), sulfamethoxazole and erythromycin (antibiotics), bezafibrate and gemfibrozil (lipid regulators), atenolol (β-blocker), carbamazepine (anti-epileptic), hydrochlorothiazide (diuretic), caffeine (stimulant) and N-acetyl-4-amino-antipiryne, a metabolite of the antipyretic drug dypirone. They were subsequently ozonated in continuous flow using 1.2L lab-scale bubble columns. The concentration of all spiking compounds was monitored in the outlet stream. The effects of varying ozone input, expressed as energy per unit volume, and water flow rate, and of using single or double column were studied in relation to the efficiency of ozone usage and the ratio of pollutant depletion. The ozone dosage required to treat both wastewaters with pollutant depletion of >90% was in the 5.5-8.5 mg/L range with ozone efficiencies greater than 80% depending on the type of wastewater and the operating conditions. This represented 100-200 mol of ozone transferred per mole of pollutant removed. Direct and indirect environmental impacts of ozonation were assessed according to Life Cycle Assessment, a technique that helped identify the most effective treatments in terms of potential toxicity reduction, as well as of toxicity reduction per unit mass of greenhouse-gas emissions, which were used as an indicator of environmental efficiency. A trade-off between environmental effectiveness (toxicity reduction) and greenhouse-gas emissions was observed since maximizing toxicity removal led to higher greenhouse-gas emissions, due to the latter's relatively high ozone requirements. Also, there is an environmental trade-off between effectiveness and efficiency. Our results indicate that an efficient use of ozone was not compatible with a full pollutant removal. PMID:22922131

  7. 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.

  8. 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

  9. 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

  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. PMID:26074188

  11. Transport of hop bitter acids across intestinal Caco-2 cell monolayers.

    Science.gov (United States)

    Cattoor, Ko; Bracke, Marc; Deforce, Dieter; De Keukeleire, Denis; Heyerick, Arne

    2010-04-14

    Several health-beneficial properties of hop bitter acids have been reported (inhibition of bone resorption and anticarcinogenic and anti-inflammatory activities); however, scientific data on the bioavailability of these compounds are lacking. As a first approach to study the bioavailability, the epithelial transport of hop alpha- and beta-acids across Caco-2 monolayers was investigated. Hop acids were added either to the apical or to the basolateral chamber and, at various time points, amounts transported to the receiving compartment were determined. The monolayer integrity control was performed by using marker compounds (atenolol and propranolol), transepithelial electrical resistance (TEER) measurement, and determination of the fluorescein efflux. The TEER and fluorescein efflux confirmed the preservation of the monolayer integrity. The membrane permeability of the alpha-acids (apparent permeability coefficients for apical to basolateral transport (P(appAB)) ranged from 14 x 10(-6) to 41 x 10(-6) cm/s) was determined to be substantially higher than that of the beta-acids (P(appAB) values ranging from 0.9 x 10(-6) to 2.1 x 10(-6) cm/s). Notably, the beta-acids exhibited significantly different bidirectional P(app) values with efflux ratios around 10. The involvement of carrier-mediated transport for beta-acids (active efflux pathway by P-gp, BCRP, and/or MRP-2 type efflux pumps) could be confirmed by transport experiments with specific inhibitors (verapamil and indomethacin). It appears that alpha-acids are efficiently absorbed, whereas the permeability of beta-acids is low. Limiting factors in the absorption of beta-acids could involve P-gp and MRP-2 type efflux transporters and phase II metabolism. PMID:20329731

  12. Timeline of History of Hypertension Treatment.

    Science.gov (United States)

    Saklayen, Mohammad G; Deshpande, Neeraj V

    2016-01-01

    It is surprising that only about 50 years ago hypertension was considered an essential malady and not a treatable condition. Introduction of thiazide diuretics in late 50s made some headway in successful treatment of hypertension and ambitious multicenter VA co-operative study (phase 1 and 2) started in 1964 for diastolic hypertension ranging between 90 and 129 mmHg and completed by 1971 established for the first time that treating diastolic hypertension reduced CV events such as stroke and heart failure and improved mortality. In the following decade, these results were confirmed for the wider US and non-US population, including women and goal-oriented BP treatment to diastolic 90 became the standard therapy recommendation. But isolated systolic hypertension (accounting for two-thirds of the 70 million hypertensive population in USA alone) was not considered treatable until 1991 when SHEP study (systolic hypertension in elderly program) was completed and showed tremendous benefits of treating systolic BP over 160 mmHg using only a simple regimen using small dose chlorthalidone with addition of atenolol if needed. In the next two decades, ALLHAT and other studies examined the comparability of outcomes with use of different classes and combinations of antihypertensive drugs. Although diastolic BP goal was established as 90 in the late 70s and later confirmed by HOT study, the goal BP for systolic hypertension was not settled until very recently with completion of SPRINT study. ACCORD study showed no significant difference in outcome with sys 140 vs. 120 in diabetics. But recently completed SPRINT study with somewhat similar protocol as in ACCORD but in non-diabetic showed almost one-quarter reduction in all-cause mortality and one-third reduction of CV events with systolic BP goal 120. PMID:26942184

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

    International Nuclear Information System (INIS)

    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 3DOM*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 (3DOM*) 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

  14. 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.

  15. 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)

  16. A study on prescribing patterns of antihypertensives in geriatric patients

    Directory of Open Access Journals (Sweden)

    Arshad H Mohd

    2012-01-01

    Full Text Available Objective: Hypertension is a leading contributor to the global burden of cardiovascular morbidity and mortality. The main objective of the present study was to assess the prescribing patterns for antihypertensives in geriatric patients. Materials and Methods: A Prospective observational study was carried out for the period of six months in an out-patient department. Elderly patients who have been diagnosed with hypertension as per JNC-7 guidelines and patients receiving or prescribed with antihypertensive drugs were included. Results: A total of 100 prescriptions were analyzed during the six-month study period. 72% of the patients were in the age group of 65-67 years and this was found to be higher in men 69%. During the study period 80% of the patients were Pre-Hypertensive systolic (80-89 mmHg and Diastolic (120-139 mmHg followed by Stage-I Hypertension and Stage-II Hypertension. The most common drug classes involved in the study was Calcium Channel Blockers 37% followed by Angiotensin II receptor antagonists 21% and the most commonly prescribed drugs in the study population were Amlodipine 37%, Losartan 11% and Telmisartan 10%. The most common anti-hypertensive fixed dose combination therapy involved in the study was Telmisartan + Hydrochlorothiazide 15% and most common two drug combination therapy involved in the study was Amlodipine + Atenolol 7% followed by Metoprolol + Amlodipine 1%. Conclusion: Our study shows that the most commonly prescribed drug classes involved were Calcium Channel Blockers followed by Angiotensin II receptor antagonists and the anti-hypertensive drug combinations among hypertensive patients were considerable and this practice positively impacted on the overall blood pressure control.

  17. 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

  18. 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

  19. MODERN VIEWS ON THE VARIABILITY OF BLOOD PRESSURE

    Directory of Open Access Journals (Sweden)

    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.

  20. 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

  1. 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

  2. A simple and sensitive LC-MS/MS method for the determination of sotalol in rat plasma.

    Science.gov (United States)

    Feng, Zhiping; Yu, Siyuan; Liu, Wei; Yang, Li; Liu, Yang; Zhai, Suodi; Wang, Fang; Zhang, Xianhua

    2015-08-01

    A sensitive, rapid and robust HPLC method with tandem mass spectrometry (HPLC/MS/MS) detection has been developed and validated for the quantification of sotalol in rat plasma. Plasma samples were precipitated with acetonitrile before analysis. The chromatographic separation was performed on an Atlantis hydrophilic interaction liquid chromatography Silica column (50 × 2.1 mm, 3 µm) with a gradient mobile phase of 10 mm NH4 COOH (containing 0.2% of formic acid) as buffer A and acetonitrile as mobile phase B. Sotalol (m/z 273.2 → 255.1) and atenolol (the internal standard, IS, m/z 267.2 → 190.1) were monitored under positive ionization mode with 5500 QTRAP. Retention time of sotalol and the IS were 2.69 and 3.43 min, respectively. The linear range was 5-500 nm based on the analysis of 0.1 mL of plasma. The intrabatch precision ranged from 1.2 to 6.1%, and the inter-batch precision was from 3.3 to 6.5%. The coefficient of variation of IS-normalized matrix factor was 7.6%. Experiments for stability were performed and the analyte was sufficiently stable. A run time of 6 min for each injection made it possible to analyze a high throughput of plasma samples. The assay was successfully applied to the determination of sotalol in rat plasma after a micro-dose oral administration. PMID:25582386

  3. 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

  4. Treatment of severe neutropenia with high-dose pyridoxine in a patient with chronic graft versus host disease and squamous cell carcinoma: a case report

    Directory of Open Access Journals (Sweden)

    Rauf Mariam

    2011-08-01

    Full Text Available Abstract Introduction The differential diagnosis of neutropenia includes medications, infections, autoimmune diseases, and deficiencies of Vitamin B12 and folate. The association of Vitamin B6 deficiency with severe neutropenia is a rare finding. Case presentation A 51-year-old Caucasian woman presented with fever and profound neutropenia (48 neutrophils/uL. Her clinical history included non-Hodgkin lymphoma, in remission following treatment with allogeneic bone marrow transplantation, quiescent chronic graft-versus-host disease, and squamous cell carcinoma of the skin metastatic to cervical lymph nodes. Medications included atenolol, topical clobetasol, Ditropan (oxybutynin, prophylactic voriconazole, prophylactic valganciclovir, Soriatane (acitretin, and Carac (fluorouracil cream. The bone marrow was hypocellular without metastatic cancer or myelodysplasia. Neutropenia did not respond to stopping medications that have been associated with neutropenia (valganciclovir, voriconazole and Soriatane or treatment with antibiotics or granulocyte colony stimulating factor. Blood tests revealed absence of antineutrophil antibodies, normal folate and B12 levels, moderate zinc deficiency and severe Vitamin B6 deficiency. Replacement therapy with oral Vitamin B6 restored blood vitamin levels to the normal range and corrected the neutropenia. Her cervical adenopathy regressed clinically and became negative on scintography following Vitamin B6 therapy and normalization of the blood neutrophil count. Conclusion Severe pyridoxine deficiency can lead to neutropenia. Screening for Vitamin B6 deficiency, along with folate and Vitamin B12 levels, is recommended in patients with refractory neutropenia, especially those with possible malabsorption syndromes, or a history of chronic-graft-versus host disease. Severe neutropenia may facilitate progression of squamous cell carcinoma.

  5. 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

  6. 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.

  7. A pharmacodynamic study on clenbuterol-induced toxicity: beta1- and beta2-adrenoceptors involvement in guinea-pig tachycardia in an in vitro model.

    Science.gov (United States)

    Mazzanti, Gabriela; Di Sotto, Antonella; Daniele, Claudia; Battinelli, Lucia; Brambilla, Gianfranco; Fiori, Maurizio; Loizzo, Stefano; Loizzo, Alberto

    2007-09-01

    Beta(2)-receptor adrenergic agonists as clenbuterol and analogues are illegally used as growth promoters in cattle, in Europe, as well as in other countries. Following consumption of meat or liver, intoxication cases were described, and cardiovascular toxic effects (tachycardia, hypertension) were of clinical relevance. Therefore, we investigated whether heart rate increase induced by clenbuterol could depend upon stimulation of beta(1)- and/or beta(2)-adrenergic receptors, and in which ratio. We used in vitro guinea-pig atria, a model in which beta(1)-/beta(2)-receptors ratio is similar to that found in men. In our experiments both beta(1)- and beta(2)-receptors contributed to clenbuterol-induced heart rate increase, but with a different potency. The selective beta(2)-antagonist ICI-118,551 competitively antagonized responses to clenbuterol with high affinity (pA(2) 9.47+/-0.28, SchildSlope 0.98+/-0.20 not significantly different from unity, K(B) 0.34 nM). The selective beta(1)-antagonist atenolol antagonized clenbuterol with a relatively lower affinity (pA(2)=7.59+/-0.14), the SchildSlope=1.97+/-0.33 was significantly different from unity (Pclenbuterol stimulates guinea-pig heart rate by acting chiefly on beta(2)-adrenoceptor, although responses to clenbuterol apparently are mediated by an inter-play between both beta-adrenoceptors. Further experiments are necessary to understand which beta-adrenergic antagonists are of effectiveness to counteract cardiovascular effects in case of intoxication following clenbuterol, or other beta-adrenergic stimulants. PMID:17449161

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

    Directory of Open Access Journals (Sweden)

    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. 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

  10. 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

  11. 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.

  12. 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)

  13. 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

  14. 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

  15. 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

  16. 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

  17. 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

  18. 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

  19. 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

  20. 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

  1. 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

  2. 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

  3. 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

  4. 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

  5. Financial Burden and Impoverishment Due to Cardiovascular Medications in Low and Middle Income Countries: An Illustration from India

    Science.gov (United States)

    Pandey, Kiran Raj; Meltzer, David O.

    2016-01-01

    Background Health expenditures are a major financial burden for many persons in low and middle-income countries, where individuals often lack health insurance. We estimate the effect of purchasing cardiovascular medicines on poverty in low and middle-income populations using rural and urban India as an example. Methods We created step-up treatment regimens for prevention of ischemic heart disease for the most common cardiovascular medications in India based on their cost and relative risk reduction. Cost was measured by Government of India mandated ceiling prices in rupees (Rs. 1 = $0·016) for essential medicines plus taxes. We calculated step-wise projected incidence and intensity of impoverishment due to medicine purchase. To do this we measured the resources available to individuals as daily per-capita expenditures from the latest National Sample Survey, subtracted daily medication costs, and compared this to 2014 poverty thresholds recommended by an expert group. Findings Analysis of cost-effectiveness resulted in five primary prevention drug regimens, created by progressive addition of Aspirin 75 mg, Hydrochlorothiazide 12.5mg, Losartan 25 mg, and Atorvastatin 10 mg or 40mg. Daily cost from steps 1 to 5 increased from Rs. 0·13, Rs. 1.16, Rs. 3.81, Rs. 10.07, to Rs. 28.85. At baseline, 31% of rural and 27% percent of urban Indian population are poor at the designated poverty thresholds. The Rs. 28.85 regimen would be unaffordable to 81% and 58% of rural and urban people. A secondary prevention regimen with aspirin, hydrochlorothiazide, atenolol and atorvastatin could be unaffordable to 81% and 57% rural and urban people respectively. According to our estimates, 17% of the rural 32% of the urban adult population could benefit with these medications, and their out of pocket purchase could impoverish 17 million rural and 10 million urban people in India and increase respective poverty gaps by 2.9%. Conclusion Medication costs for cardiovascular disease have the

  6. Prevalence of Coronary Artery Intramyocardial Course in a Large Population of Clinical Patients Detected by Multislice Computed Tomography Coronary Angiography

    International Nuclear Information System (INIS)

    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

  7. 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

  8. 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.

  9. 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

  10. 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

  11. 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

  12. 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

  13. 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.

  14. 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

  15. 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.

  16. 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

  17. Temporal profile and mechanisms of the prompt sympathoexcitation following coronary ligation in Wistar rats.

    Science.gov (United States)

    Passamani, Luciana Mesquita; Abdala, Ana Paula; Moraes, Davi José de Almeida; Sampaio, Karla Nívea; Mill, José Geraldo; Paton, Julian Francis Richmond

    2014-01-01

    Our aim was to assess the timing and mechanisms of the sympathoexcitation that occurs immediately after coronary ligation. We recorded thoracic sympathetic (tSNA) and phrenic activities, heart rate (HR) and perfusion pressure in Wistar rats subjected to either ligation of the left anterior descending coronary artery (LAD) or Sham operated in the working heart-brainstem preparation. Thirty minutes after LAD ligation, tSNA had increased (basal: 2.5±0.2 µV, 30 min: 3.5±0.3 µV), being even higher at 60 min (5.2±0.5 µV, P<0.01); while no change was observed in Sham animals. HR increased significantly 45 min after LAD (P<0.01). Sixty minutes after LAD ligation, there was: (i) an augmented peripheral chemoreflex - greater sympathoexcitatory response (50, 45 and 27% of increase to 25, 50 and 75 µL injections of NaCN 0.03%, respectively, when compared to Sham, P<0.01); (ii) an elevated pressor response (32±1 versus 23±1 mmHg in Sham, P<0.01) and a reduced baroreflex sympathetic gain (1.3±0.1 versus Sham 2.0±0.1%.mmHg-1, P<0.01) to phenylephrine injection; (iii) an elevated cardiac sympathetic tone (ΔHR after atenolol: -108±8 versus -82±7 bpm in Sham, P<0.05). In contrast, no changes were observed in cardiac vagal tone and bradycardic response to both baroreflex and chemoreflex between LAD and Sham groups. The immediate sympathoexcitatory response in LAD rats was dependent on an excitatory spinal sympathetic cardiocardiac reflex, whereas at 3 h an angiotensin II type 1 receptor mechanism was essential since Losartan curbed the response by 34% relative to LAD rats administered saline (P<0.05). A spinal reflex appears key to the immediate sympathoexcitatory response after coronary ligation. Therefore, the sympathoexcitatory response seems to be maintained by an angiotensinergic mechanism and concomitant augmentation of sympathoexcitatory reflexes. PMID:25006809

  18. 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

  19. 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

  20. 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

  1. 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

  2. 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.

  3. 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.

  4. Beta-blockers and heart failure.

    Science.gov (United States)

    Cruickshank, John M

    2010-01-01

    , mainly, with beta-2 blockade and alpha-blockade. Thus non-selective (e.g. propranolol) or modestly beta-1 selective (e.g. metoprolol, atenolol) are associated with metabolic disturbance, bronchospasm, epinephrine/hypertensive interaction (with cigarette-smoking or insulin-induced hypoglycaemia), while the possession of alpha-blocking activity (e.g. carvedilol) is associated with dizziness and postural hypotension. The possession of beta-2 blockade, particularly if combined with alpha-blockade, is associated with an increased occurrence of sexual dysfunction. Lipophilic BB like propranolol and metoprolol appear in high concentrations in human brain tissue and are associated with side-effects such as insomnia, dreams and nightmares. PMID:21180298

  5. 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

  6. A tool for assessing the feasibility of comparative effectiveness research

    Directory of Open Access Journals (Sweden)

    Walker AM

    2013-01-01

    pairs were considered suitable for CER if at least half of the dispensings of each treatment-pair member fell within a preference range of 30% to 70%.Results: Among 3889 community-acquired pneumonia patients, insurance claims histories were sufficiently similar in seven drug pairs to suggest that observational CER might be effective. Relapse appears to have been less common in levofloxacin recipients than in similar patients given other products. In 6035 heart failure patients, metoprolol, carvedilol, and atenolol were employed in patients with similar claims histories, and thus might be suitable for observational CER. The long-acting succinate formulation of metoprolol had lower failure rates in head-to-head comparisons with all other beta-blockers. Both findings are candidates for further investigation. Confounding by unmeasured factors operating in the same manner as the measured covariates would not have produced the apparent superiority of levofloxacin, which was given to people in poorer respiratory health. The baseline covariate distributions of persons starting beta-blockers suggest only that carvedilol recipients were healthier than others.Conclusion: A straightforward algorithm can identify empirical equipoise, in which prescribers as a group seem evenly divided on the merits of alternative therapies. This is the setting in which CER may be most necessary and is likely to be most accurate. The imbalances identified by propensity models can identify situations in which the results of screening analyses may be biased in the direction of the observed effect.Keywords: equipoise, observational CER, methodology, community-acquired pneumonia, heart failure

  7. 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

  8. 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

  9. 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

  10. 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