Search results for "Ethanolamines"
showing 10 items of 65 documents
Adjustable maintenance dosing with budesonide/formoterol in a single inhaler provides effective asthma symptom control at a lower dose than fixed mai…
2004
Asthma guidelines suggest a stepwise approach to maintenance pharmacological treatment of persistent asthma until control is attained, and a 3 month review of the fixed maintenance dosing for step-up or step-down adjustment. This 12-week study compared the efficacy and safety of budesonide/formoterol in a single inhaler (Symbicort Turbuhaler 160/4.5 or 80/4.5 microg) given as adjustable maintenance or fixed maintenance dosing. Patients (n = 2358) were randomised to budesonide/formoterol fixed maintenance dosing (two inhalations bid) or adjustable maintenance dosing (two inhalation bid; stepping up to four inhalations bid if asthma worsened for a maximum of 14 days; stepping down to two inha…
Effects of Inhaled Fenoterol on the Circadian Rhythm of Expiratory Flow in Allergic Bronchial Asthma
1983
Metered-dose aerosol treatment with fenoterol for three consecutive days, in eight patients suffering from allergic asthma, caused the disappearance of FEV1 and MEF50 circadian rhythm. We attribute such behavior to the suppression of the bronchomotor tone induced by fenoterol. The administration on different days of a single dose of fenoterol aerosol in another group of eight patients pointed out the variability of the effects of the drug at different hours of the day. We believe the results obtained are important for a better dosage and time distribution of the therapy with beta2 agonists.
Effects of nebivolol and atenolol on central aortic pressure in hypertensive patients: a multicenter, randomized, double-blind study.
2013
The main objective was to compare the mean change in augmentation index of hypertensive patients treated with nebivolol or atenolol.Multicenter, double-blind randomized study conducted in six Spanish centers. We enrolled outpatients between the ages of 40 and 65 years with mild or moderate essential hypertension (systolic blood pressure, SBP ≥ 140 mmHg to ≤ 179 mmHg and diastolic blood pressure, DBP ≥ 90 mmHg to ≤ 109 mmHg after a 2-week run-in placebo period). Patients received nebivolol 5 mg or atenolol 50 mg once daily. At week 3, atenolol could be titrated up to 100 mg qd for non-responders. Additionally, patients not achieving normal blood pressure after 6 weeks could be treated with 2…
Relaxation by β3-adrenoceptor agonists of the isolated human internal anal sphincter
2009
In this study, responses of beta(3)-adrenoceptor agonists were examined on human isolated internal anal sphincter (IAS) in order to explore their relaxant effects on hypertonicity of IAS.The relaxant efficacy (E(max)) and potency (-logIC(50)) of BRL37344 and SR58611A, beta(3)-adrenoceptor agonists, were examined in contracted IAS muscle strips. The presence of beta(3)-adrenoceptors, and changes in intracellular calcium and cyclic nucleotide levels in IAS muscle were tested by Western blotting, epifluorescence microscopy and enzyme immunoassay, respectively.BRL37344 and SR58611A relaxed contracted IAS muscle (E(max)=27+/-3% and 35+/-3%; -logIC(50)=6.26+/-0.24 and 4.87+/-0.13; respectively). …
Effects of Nebivolol versus Carvedilol on Left Ventricular Function in Patients with Chronic Heart Failure and Reduced Left Ventricular Systolic Func…
2006
Beta-adrenoceptor antagonist (beta-blocker) therapy results in a significant improvement in left ventricular (LV) systolic function and prognosis in patients with chronic heart failure. Both carvedilol and nebivolol produce hemodynamic and clinical benefits in chronic heart failure, but it is unknown whether their peculiar pharmacologic properties produce different effects on LV function.To assess the effects on LV function of nebivolol compared with carvedilol in patients with chronic heart failure and reduced LV systolic function.Seventy patients with a LV ejection fractionor=40% and in New York Heart Association (NYHA) functional class II or III were randomly assigned to receive carvedil…
Biochemical interaction between effects of beclomethasone dipropionate and salbutamol or formoterol in sputum cells from mild to moderate asthmatics.
2005
Background: Several in vitro studies demonstrate that corticosteroids and long-acting β2 agonists may have a complementary and synergistic mode of action on the inflammatory processes in asthma. Methods: Sputum was induced in 20 mild to moderate asthmatic patients and the induced sputum cells (ISC) were cultured with beclomethasone dipropionate (BDP) 10−7 M, salbutamol 10−8 M and formoterol 10−8 M either alone or in combination, BDP plus salbutamol and BDP plus formoterol, for 24 h. We measured the levels of growth macrophages-colony stimulating factor (GM-CSF), released on activation normal T cells expressed and activated (RANTES) and interleukin-8 (IL-8), in the supernatant of stimulate…
Plasma and fibroblasts of Tangier disease patients are disturbed in transferring phospholipids onto apolipoprotein A-I
1998
Plasmas of patients with Tangier disease (TD) lack lipid-rich α-HDL which, in normal plasma, constitutes the majority of high density lipoprotein (HDL). Residual amounts of apolipoprotein (apo)A-I in TD plasma occur as lipid-poor or even lipid-free preβ-HDL. By contrast to normal plasma, TD plasma does not convert preβ-HDL into α-HDL. Moreover, fibroblasts of TD patients were found to be defective in secreting cholesterol or phospholipids in the presence of lipid-free apoA-I. We have therefore hypothesized that both defective conversion of preβ-HDL into α-HDL and defective lipid efflux from TD cells onto lipid-free apoA-I result from a disturbance in phospholipid transfer occurring in both …
Sympathetic nervous activity and the pressor effect of noradrenaline under chronic?-?-adrenoceptor blockade with labetalol in hypertension
1983
In 14 patients with essential hypertension, the influence of the alpha- and beta-adrenoceptor blocking drug labetalol on blood pressure, heart rate, plasma renin, plasma noradrenaline and pressor effect of exogenous noradrenaline was investigated during long-term treatment. During the initial four weeks of treatment, labetalol at a dose of 400 mg/day showed a slight effect only on supine blood pressure, whereas upright blood pressure was already lowered effectively after the second week of treatment (p less than 0.01). An increase in the mean dose to 850 mg/day had an additional blood pressure-lowering effect (p less than 0.001), whereby a preferential decrease of the orthostatic blood pres…
Design, Synthesis, and Biological Evaluation of Novel Fluorinated Ethanolamines
2011
The preparation of novel fluorinated allylamines and their use as key fragments for the stereoselective synthesis of hydroxyethyl secondary amine (HEA)-type peptidomimetics is described. Our strategy employs chiral sulfinyl imines as synthesis intermediates, by treatment of hemiaminal precursors with two equivalents of vinylmagnesium bromide. The subsequent oxidation of the allylic amines to the corresponding epoxides was achieved by treatment with methyl(trifluoromethyl)dioxirane. Finally, epoxide ring opening with a range of nitrogen nucleophiles provided a library of HEA-derived peptidomimetics with a phenyldifluoromethylene moiety. The biological evaluation of these derivatives revealed…
Development and validation of a liquid chromatography tandem mass spectrometry method for the analysis of beta-agonists in animal feed and drinking w…
2010
A reproducible, sensitive and selective multiresidue analytical method for seven beta-agonists: clenbuterol (CBT), clenpenterol (CPT), ractopamine (RTP), brombuterol (BBT), mabuterol (MBT), mapenterol (MPT), and hydroxymethylclenbuterol (HMCBT) was developed and validated by using liquid chromatography tandem mass spectrometry (LC-MS/MS) in feed and drinking water samples. The validation was achieved according to the criteria laid down in the Commission Decision 2002/657/EC, however it was necessary to use minimum required performance limits (MRPLs) proposed by the Community Reference Laboratories (CRLs) due to the lack of maximum residue limits (MRLs) for beta-agonists. By setting up these…