The researchers did a computer-based search of the medical literature and collected all of the articles that reported on testing the effects of long-acting beta-agonists in asthmatic patients. To be included in this study, the articles had to report that patients were assigned to a group that received a long-acting beta-agonist or to a group that received placebo (an ineffective substance used in place of the active medicine). Assignment to one group or the other had to be done completely by chance. In addition, the study had to have lasted at least 3 months. After retrieving the articles, the researchers judged the quality of each study. They then analyzed the pooled results from all the patients they had been able to gather from all the studies combined and calculated the proportion of patients who had had 1 of the complications listed earlier ...
Although asthma is highly variable in presentation, regular daily treatment is often required. Tolerance to the bronchoprotective effect of both long and short acting β2 agonists has been shown.1. Walters et al examined studies that compared the effects of regular use of inhaled long acting β2 agonists with inhaled short acting β2 agonists. This important clinical question has dimensions of benefits, harms, and costs. The review addressed a clear question, had a comprehensive search strategy, clear inclusion and exclusion criteria, and used the Jadad scale for rating methodological quality. 3 studies involved children ,12 years of age, and data from these studies were combined with studies of adults for the results reported in the tables. The review provides comparisons of some outcomes for children, but each comparison is based on only 1 study, limiting the applicability of the results for children.. Sears reports that the pharmacologically predictable effects of both short and long acting ...
Cathecholamines increase heart rate and contraction force. This effect is mainly mediated by their interaction with the β-adrenergic receptor...
Quick-relief medications relax the muscles around the bronchial tubes so that air can flow freely through them. As noted earlier, these medications are called bronchodilators or beta-agonists because
If you do ok with everyday living and socializing but need the boost to read jornals, write theses or pay bills, arent there some advantages? My Dr acknowledges the reality of tolerance and the desire to use as little drugs as possible as legitimate reasons to go with the IRs…. They are unpredictable…but so is long-acting. A lot of folks like the precision and the feeling that goes on like a light switch when it starts working…whereas the long acting can often leave you feeling like you have taken nothing…. ...
Overuse of inhaled bronchodilator beta agonist medication results in a loss of effectiveness (i.e. tolerance). This has been shown for the short acting beta agonist salbutamol and the long acting beta agonist salmeterol. Tolerance to salmeterol is present within 24 hours. The onset of tolerance to salbutamol is not known ...
165 trials were reviewed and eight were included; a total of 461 patients have been studied (229 with CBA; 232 with intermittent beta-agonists). Overall, admission to hospital was reduced with CBA compared to intermittent beta-agonists (RR: 0.68; 95% CI: 0.5 to 0.9); patients with severe airway obstruction at presentation appeared to benefit most from this intervention (RR: 0.64; 95% CI: 0.5 to 0.9). Patients receiving CBA demonstrated small but statistically significant improvements in pulmonary function tests when all studies were pooled. Patients receiving CBA had greater improvements in % predicted FEV-1 (SMD: 0.3; 95% CI: 0.03 to 0.5) and PEFR (SMD: 0.33; 95% CI: 0.1 to 0.5); this effect was observed by 2-3 hours. Continuous treatment was generally well tolerated, with no clinically important differences observed in pulse rate (WMD: -2.87; 95% CI: -6.0 to 0.3) or blood pressure (WMD: -1.75; 95% CI: -5.6 to 2.1) between the treatment groups. Tremor was equally common in both groups (OR: ...
A major new study shows that, contrary to previously published reports, regular daily use of so-called beta-agonists such as albuterol for mild asthma does no harm to patients. The study, reported
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The species, which eluted at 6.75 min and produced a molecular ion of m/z 255.13 (Fig. 4E), was assigned to a mono-nitrated salbutamol derivative 3 (Fig. 1). This assignment is consistent with elemental analysis (C12H19N2O4+, exact mass 255.13397) and further supported by MS/MS spectrum obtained from this molecular ion (Fig. 4G). Formation of this nitrophenol was unexpected as it required the side chain at C3 of the aromatic ring, -CH2OH, to be eliminated. We verified that the putative phenolic precursor of 3, a salbutamol analog, in which the -CH2OH moiety was replaced with -H, (m/z 210), was not present as an impurity in salbutamol samples. This indicates that the corresponding radical (1d in Fig. 11) had to be produced in situ, during enzymatic oxidation of salbutamol itself. In the proposed mechanism (Fig. 11), the initially generated phenoxyl radical, 1a, undergoes intramolecular hydrogen atom transfer from the adjacent -CH2OH moiety to generate the aryl-methoxyl-type radical 1c. After ...
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This test is based on clenbuterol antibodies and it is recommended for the detection of the following Beta-Agonists (% of cross-reactivity): clenbute-rol (100%)
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TY - JOUR. T1 - Impaired beta-adrenergic receptor activation of adenylyl cyclase in airway smooth muscle in the basenji-greyhound dog model of airway hyperresponsiveness.. AU - Emala, C.. AU - Black, C.. AU - Curry, C.. AU - Levine, M. A.. AU - Hirshman, C. A.. PY - 1993/6. Y1 - 1993/6. N2 - Previous studies in human asthmatics have suggested a defect in the beta-adrenergic pathway leading to cyclic adenosine monophosphate (cAMP) generation. Although these studies have suggested normal or increased numbers of beta-adrenergic receptors, limitations in the quantity of tissue available have not allowed further delineation of the biochemical or molecular mechanisms of human asthma. The basenji-greyhound (BG) dog model of nonspecific airway hyperreactivity displays similarities to human asthma, and altered functional response to beta-adrenergic agonists has been previously shown in airway tissue from this model. We have now correlated this functional impairment in beta-adrenergic response with a ...
Repeated administration of the centrally acting beta adrenoceptor agonist, clenbuterol, to rats reduced the ability of isoproterenol to increase the concentration of cyclic AMP (cAMP) in slices of cerebellum. This reduced responsiveness to isoproterenol was accompanied by a marked reduction in the density of beta adrenoceptors as measured by the binding of the beta adrenoceptor antagonist [125I]iodopindolol. In addition, the agonist-binding properties of remaining cerebellar beta adrenoceptors were altered after clenbuterol treatment. The clenbuterol-induced reduction in the density of beta adrenoceptors in the cerebellum is in marked contrast to its inability to do this in cerebral cortex. Comparison of the ability of clenbuterol to that of isoproterenol to increase levels of cAMP in slices of cerebral cortex or cerebellum showed that clenbuterol is a weakly potent agonist in both brain regions. The increase in cAMP induced by isoproterenol in the cortex was significantly reduced in the ...
While the popular drug, known as a long-acting beta agonist, provides effective and satisfying relief of asthma symptoms, it doesnt attack the inflammation nearly always present in the airways of people with asthma, the study found. "Most asthma experts have concluded that long-acting beta agonists alone do not provide enough protection," said Dr. Stephen Lazarus, a pulmonologist at UCSF Medical Center and leader of the national study. "This is the first clear-cut clinical study confirming this impression." The most effective treatment is a combination of the beta agonist and an inhaled steroid or other anti-inflammatory drug.. ...
INTRODUCTION: Clenbuterol has been used to alleviate chronic obstructive pulmonary disease and elicit an anabolic response in muscles. The aim of this study was to determine the influence of muscle mass variation on physical capacities in rats.. METHODS: The left hindlimbs of Wistar rats were immobilized for 20 days in plantarflexion with a splint and then remobilized for 16 days. The effect of a non-myotoxic dose of clenbuterol during the immobilization period was evaluated. Physical capacities were coordination, free locomotion, grip strength, and bilateral deficit.. RESULTS: Immobilization induced a loss of muscle mass, coordination, and strength without any effect on free locomotion. The positive anabolic effect of clenbuterol did not prevent a loss of physical capacities resulting from immobilization.. CONCLUSIONS: Muscle mass correlated strongly with coordination and isometric strength in untreated rats. Anabolic effect, fiber phenotype modification, and perturbation in neuromuscular ...
Pirbuterol is a beta-2 adrenergic bronchodilator. In vitro studies and in vivo pharmacologic studies have demonstrated that pirbuterol has a preferential effect on beta-2 Adrenergic receptors compared with isoproterenol. While it is recognized that beta-2 adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta-2 receptors in the human heart, existing in a concentration between 10-50%. The precise function of these receptors has not been established. The pharmacologic effects of beta adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (AlP) to cyclic-3† ,5†-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells,
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Background. Sex differences in LV mechanics exist at rest and during acute physiological stress. Differences in cardiac autonomic and adrenergic control may contribute to sex differences in LV mechanics and LV hemodynamics. Accordingly, this study aimed to investigate sex differences in LV mechanics with altered adrenergic stimulation achieved through post handgrip exercise ischemia (PEI) and ß1-adrenergic receptor (AR) blockade. Methods and Results. 20 males (23±5 yr) and 20 females (22±3 yr) were specifically matched for LV length (males: 8.5±0.5 cm, females: 8.2±0.6 cm, p=0.163), and 2-dimensional speckle-tracking echocardiography was used to assess LV structure and function at baseline, during PEI and following administration of 5mg bisoprolol (ß1-AR antagonist). During PEI, LV end-diastolic volume and stroke volume were increased in both groups (p,0.001), as was end-systolic wall stress (p,0.001). LV twist and apical rotation werent altered from baseline or different between the ...
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The Boxed Warning, the most prominent warning, about asthma-related death has been removed from these drug labels Read More.... In 2011, the FDA required that drug companies that market long-acting beta agonists (LABAs) in combination with inhaled corticosteroids (ICS) conduct trials to evaluate the safety of these agents. After review of four large studies, the FDA has determined that treating asthma with ICS/LABA does not result in significantly more serious asthma-related side effects than treatment with ICS alone. Four trials also assessed efficacy of the ICS/LABA products, and demonstrated that the ICS/LABA combination reduced asthma exacerbations compared to ICS alone. Using LABAs alone without an ICS for asthma is linked with an increased risk of asthma-related death and this Boxed Warning will remain on single ingredient LABA medicine. Labels on combo inhalers such as Advair, Breo Ellipta, Dulera, AirDuo, and Symbicort will be updated.. ...
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Background. Persistent asthma is characterized by airway remodeling. Whereas we have previously shown that neither β(2)-agonists nor corticosteroids inhibit extracellular matrix (ECM) protein release from airway smooth muscle (ASM) cells, the effect
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It is now well established that any given ligand for a G-protein-couple receptor (GPCR) does not simply possess a single defined efficacy. Rather, a ligand possesses multiple efficacies, depending on the specific down-stream signal transduction pathway analyzed. This diversity may be based on ligand-specific GPCR conformations and is often referred to as "functional selectivity." It has been known for a century that stereoisomers of catecholamines differ in their potency and, in some systems, also in their efficacy. However, the molecular basis for efficacy differences of GPCR ligand stereoisomers has remained poorly defined. In an elegant study published in this issue of Molecular Pharmacology, Woo et al. (p. 158) show that stereoisomers of the β2-adrenoceptor selective agonist fenoterol differentially activates Gs- and Gi-proteins in native rat cardiomyocytes. This study is so important because it is the first report to show that even the subtle structural differences within a ligand ...
The beta-2 agonist Clenbuterol is used for treating asthma, since it is a bronchodilator, in many countries. However, it is more commonly used to burn fat
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Clen, short for Clenbuterol, is a widespread terminology that is used to refer to a well-known bronchodilator, Clenbuterol Hydrochloride. Clen - which is also coined as Ventipulmin, Spiropent, and Dilaterol in the market - is typically used by people who have chronic asthma or other breathing disorders as a decongestant. Aside from its common use,…
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