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International Journal of Molecular... Nov 2022Asthma is a common inflammatory disease of the lungs. The prevalence of asthma is increasing worldwide, and the tendency indicates that the number of asthma sufferers... (Review)
Review
Asthma is a common inflammatory disease of the lungs. The prevalence of asthma is increasing worldwide, and the tendency indicates that the number of asthma sufferers will soar in the coming years for several reasons, in particular, the lifestyles we have adopted that expose us to risk factors. Salbutamol is the first selective short-acting β-agonist (SABA) used as an alternative reliever in the treatment of asthma. Its therapeutic effect is based on its potent smooth muscle relaxant properties, which allow the inhibition of bronchial smooth muscle contraction and subsequent bronchodilation. Salbutamol can be administered orally, intravenously (IV), intramuscularly (IM), subcutaneously, or by inhalation. For this reason, the pharmacokinetic (PK) parameters-absorption, distribution, metabolism, and elimination-are highly diverse and, consequently, the efficacy and adverse effects also differ between each formulation. Here, we review the pharmacological profile of different salbutamol formulations, focusing on their efficacy and adverse effects for its original application, asthma.
Topics: Humans; Albuterol; Asthma; Bronchi; Drug-Related Side Effects and Adverse Reactions; Risk Factors
PubMed: 36430683
DOI: 10.3390/ijms232214207 -
PloS One 2021A combination of ipratropium bromide (IB) and salbutamol is commonly used to treat asthma in children and adolescents; however, there has been a lack of consistency in... (Meta-Analysis)
Meta-Analysis
BACKGROUND
A combination of ipratropium bromide (IB) and salbutamol is commonly used to treat asthma in children and adolescents; however, there has been a lack of consistency in its usage in clinical practice.
OBJECTIVE
To evaluate the efficacy and safety of IB + salbutamol in the treatment of asthma in children and adolescents.
METHODS
The MEDLINE, Embase, and Cochrane Library as well as other Chinese biomedical databases (including China Biological Medicine Database, Chinese National Knowledge Infrastructure, Chongqing VIP, and Wanfang Chinese language bibliographic database) were systematically searched from the earliest record date to September 2020 for randomized controlled trials in children and adolescents (≤18 years) with asthma who received IB + salbutamol or salbutamol alone. The primary outcomes included hospital admission and adverse events. A random effects model with a 95% confidence interval (CI) was used. Subgroup analysis was performed according to age, severity of asthma, and co-interventions with other asthma controllers. This study was registered with PROSPERO.
RESULTS
Of the 1061 studies that were identified, 55 met the inclusion criteria and involved 6396 participants. IB + salbutamol significantly reduced the risk of hospital admission compared with salbutamol alone (risk ratio [RR] 0.79; 95% CI 0.66-0.95; p = 0.01; I2 = 40%). Subgroup analysis only showed significant difference in the risk of hospital admission in participants with severe asthma exacerbation (RR 0.73; 95% CI 0.60-0.88; p = 0.0009; I2 = 4%) and moderate-to-severe exacerbation (RR 0.69; 95% CI 0.50-0.96; p = 0.03; I2 = 3%). There were no significant differences in the risk of adverse events between IB + salbutamol group and salbutamol alone group (RR 1.77; 95% CI 0.63-4.98).
CONCLUSION
IB + salbutamol may be more effective than salbutamol alone for the treatment of asthma in children and adolescents, especially in those with severe and moderate to severe asthma exacerbation. The very low to high quality of evidence indicated that future well-designed double-blind RCTs with large sample are needed for research on evaluating the effectiveness of IB + salbutamol treatment for asthma in children and adolescents.
Topics: Administration, Inhalation; Adolescent; Albuterol; Anti-Asthmatic Agents; Asthma; Bronchodilator Agents; Child; Child, Preschool; China; Disease Progression; Drug Therapy, Combination; Female; Humans; Ipratropium; Male
PubMed: 33621253
DOI: 10.1371/journal.pone.0237620 -
The Annals of Pharmacotherapy Jul 2023Critically ill patients are often prescribed both inhaled beta-agonists and intravenous vasoactive; however, the interaction of the additive beta-agonist effects of...
BACKGROUND
Critically ill patients are often prescribed both inhaled beta-agonists and intravenous vasoactive; however, the interaction of the additive beta-agonist effects of these 2 agents remains largely uncharacterized.
OBJECTIVE
The purpose of this study was to evaluate how concomitant use of albuterol and vasoactive or inotropes affected ventilator-free days (VFDs) by re-analyzing the data from the Albuterol to Treat Acute Lung Injury (ALTA) trial.
METHODS
In this study, subjects were grouped to albuterol-vasoactive (n = 84) (vs) placebo-vasoactive (n = 62). Ventilator-free days, intensive care unit (ICU)-free days, organ failure-free days, cardiovascular adverse events, and 90-day mortality were compared. The primary outcome was VFDs.
RESULTS
Patients in the albuterol-vasoactive group had significantly fewer VFDs than patients in the placebo-vasoactive group (11 vs 19, = 0.05). Patients in the albuterol-vasoactive group also had significantly fewer ICU-free days (9.5 vs 18.5, = .006). The 90-day mortality was similar between groups (36.9% vs 27.4%, = .20). Similarly, no significant difference in cardiac adverse events between the groups (14.3% vs 11.3%, = 0.59).
CONCLUSION AND RELEVANCE
This study has shown fewer VFDs for patients who received both vasoactive and albuterol. There were also fewer ICU-free days when compared to those on vasoactive only. Given the common use of both agents, a prospective evaluation of the additive adverse effects of beta-agonism is warranted.
Topics: Humans; Acute Lung Injury; Administration, Intravenous; Albuterol; Drug-Related Side Effects and Adverse Reactions; Intensive Care Units
PubMed: 36189647
DOI: 10.1177/10600280221128014 -
Cell Reports. Medicine Feb 2023While brown adipose tissue (BAT) is activated by the beta-3-adrenergic receptor (ADRB3) in rodents, in human brown adipocytes, the ADRB2 is dominantly present and... (Randomized Controlled Trial)
Randomized Controlled Trial
While brown adipose tissue (BAT) is activated by the beta-3-adrenergic receptor (ADRB3) in rodents, in human brown adipocytes, the ADRB2 is dominantly present and responsible for noradrenergic activation. Therefore, we performed a randomized double-blinded crossover trial in young lean men to compare the effects of single intravenous bolus of the ADRB2 agonist salbutamol without and with the ADRB1/2 antagonist propranolol on glucose uptake by BAT, assessed by dynamic 2-[F]fluoro-2-deoxy-D-glucose positron emission tomography-computed tomography scan (i.e., primary outcome). Salbutamol, compared with salbutamol with propranolol, increases glucose uptake by BAT, without affecting the glucose uptake by skeletal muscle and white adipose tissue. The salbutamol-induced glucose uptake by BAT positively associates with the increase in energy expenditure. Notably, participants with high salbutamol-induced glucose uptake by BAT have lower body fat mass, waist-hip ratio, and serum LDL-cholesterol concentration. In conclusion, specific ADRB2 agonism activates human BAT, which warrants investigation of ADRB2 activation in long-term studies (EudraCT: 2020-004059-34).
Topics: Male; Humans; Albuterol; Adipose Tissue, Brown; Propranolol; Glucose; Receptors, Adrenergic; Receptors, Adrenergic, beta-3
PubMed: 36812890
DOI: 10.1016/j.xcrm.2023.100942 -
Respiratory Medicine Oct 2023Bronchial thermoplasty is an effective intervention to improve respiratory symptoms and to reduce the rate of exacerbations in uncontrolled severe asthma. A reduction in...
INTRODUCTION
Bronchial thermoplasty is an effective intervention to improve respiratory symptoms and to reduce the rate of exacerbations in uncontrolled severe asthma. A reduction in airway smooth muscle is arguably the most widely discussed mechanisms accounting for these clinical benefits. Yet, this smooth muscle reduction should also translate into an impaired response to bronchodilator drugs. This study was designed to address this question.
METHODS
Eight patients with clinical indication for thermoplasty were studied. They were uncontrolled severe asthmatics despite optimal environmental control, treatment of comorbidities, and the use of high-dose inhaled corticosteroids and long-acting β-agonists. Lung function measured by spirometry and respiratory mechanics measured by oscillometry were examined pre- and post-bronchodilator (salbutamol, 400 μg), both before and at least 1 year after thermoplasty.
RESULTS
Consistent with previous studies, thermoplasty yielded no benefits in terms of baseline lung function and respiratory mechanics, despite improving symptoms based on two asthma questionnaires (ACQ-5 and ACT-5). The response to salbutamol was also not affected by thermoplasty based on spirometric readouts, including forced expiratory volume in 1 s (FEV), forced vital capacity (FVC), and FEV/FVC ratio. However, a significant interaction was observed between thermoplasty and salbutamol for two oscillometric readouts, namely reactance at 5 Hz (X) and reactance area (Ax), showing an attenuated response to salbutamol after thermoplasty.
CONCLUSIONS
Thermoplasty attenuates the response to a bronchodilator. We argue that this result is a physiological proof of therapeutic efficacy, consistent with the well-described effect of thermoplasty in reducing the amount of airway smooth muscle.
Topics: Humans; Bronchodilator Agents; Bronchial Thermoplasty; Asthma; Albuterol; Adrenal Cortex Hormones; Forced Expiratory Volume
PubMed: 37422022
DOI: 10.1016/j.rmed.2023.107340 -
The American Journal of Managed Care Jul 2004Albuterol is a selective beta2-agonist that is widely used in the prevention and treatment of reactive airway disease. It is formulated as a racemic mixture containing... (Comparative Study)
Comparative Study Review
Albuterol is a selective beta2-agonist that is widely used in the prevention and treatment of reactive airway disease. It is formulated as a racemic mixture containing equal parts of the R- and S-isomers. The therapeutic activity of albuterol is due entirely to the R-isomer, whereas the S-isomer may actually have detrimental effects. Because the slowly metabolized S-isomer tends to accumulate in the body, there has been concern that chronic use of racemic albuterol might lead to loss of effectiveness and clinical deterioration, with potentially serious health and cost consequences. Levalbuterol is a formulation containing only the R-isomer of albuterol, and clinical trials have demonstrated that it offers therapeutic advantages over racemic albuterol. The cost effectiveness of levalbuterol derives mainly from reduced need for acute medical care and hospitalization.
Topics: Albuterol; Asthma; Bronchodilator Agents; Cost-Benefit Analysis; Humans; Stereoisomerism; United States
PubMed: 15354680
DOI: No ID Found -
Journal of Medical Economics 2022For hospitalized patients with chronic obstructive pulmonary disease (COPD), albuterol and levalbuterol can both be used as relievers to alleviate bronchoconstriction....
OBJECTIVES
For hospitalized patients with chronic obstructive pulmonary disease (COPD), albuterol and levalbuterol can both be used as relievers to alleviate bronchoconstriction. This study aimed to evaluate levalbuterol and albuterol's cost-utility and budget impact in hospitalized patients with COPD.
INTERVENTIONS
A cost-utility analysis was used to evaluate the impact on the costs of nebulized levalbuterol verse albuterol in hospitalized patients with COPD. The decision tree model was employed to estimate the incremental cost per quality-adjusted life year in the admission setting. A budget impact model was used to examine the impact of budget on levalbuterol's entry into the Chinese market from the healthcare system's perspective. One-way sensitivity and probabilistic sensitivity analyses were performed to test the uncertainty of the parameters.
RESULTS
The cost-utility results showed that levalbuterol saved ¥495.7 ($105.1) per hospitalization, while the budget impact analysis revealed a potential saving of ¥22.3 ($6.8) million in 3 years. The sensitivity analysis indicated that the results were robust to the changes in input parameter values.
CONCLUSION
Levalbuterol is a cost-saving option for treating hospitalized patients with COPD in China.
Topics: Albuterol; Asthma; Bronchodilator Agents; Humans; Levalbuterol; Pulmonary Disease, Chronic Obstructive
PubMed: 35786135
DOI: 10.1080/13696998.2022.2096892 -
International Journal of Pharmaceutics Feb 2023The surface of particles is the hotspot of interaction with their environment and is therefore a major target for particle engineering. Particles with tailored coatings...
The surface of particles is the hotspot of interaction with their environment and is therefore a major target for particle engineering. Particles with tailored coatings are greatly desired for a range of different applications. Amorphous coatings applied via film coating or microencapsulation have frequently been described in the pharmaceutical context and usually result in homogeneous surfaces. In the present study we have been exploring the feasibility of coating core particles with crystalline substances, a matter that has rarely been investigated. The expansion of the range of possible coating materials to include small organic molecules enables completely new product properties to be achieved. We present an approach based on temperature cycles performed in a tubular crystallizer to result in engineered crystalline coatings on excipient core particles. By manipulating the process settings and by the choice of coating substance we are able to tailor surface roughness, topography as well as surface chemistry. Benefits of our approach are demonstrated by using resulting particles as carriers in dry-powder-inhaler formulations. Depending on the resulting surface chemistry and surface roughness, coated carrier particles show varying fitness for delivering the model API salbutamol sulphate to the lung.
Topics: Drug Carriers; Temperature; Particle Size; Powders; Administration, Inhalation; Albuterol; Dry Powder Inhalers; Excipients; Surface Properties
PubMed: 36596318
DOI: 10.1016/j.ijpharm.2022.122577 -
The European Respiratory Journal Mar 1994The extended duration of bronchodilation due to formoterol and salmeterol greatly exceeds that of short acting beta 2-adrenoceptor agonists, such as salbutamol or... (Review)
Review
The extended duration of bronchodilation due to formoterol and salmeterol greatly exceeds that of short acting beta 2-adrenoceptor agonists, such as salbutamol or terbutaline. This extended duration and their capacity to "reassert" airway smooth muscle relaxation in vitro despite repeated washing has prompted considerable debate on the underlying mechanism(s). The comparative pharmacology, and molecular modelling of these drugs and of the beta 2-adrenoceptor and its ligand binding core have cast doubt on the exosite/exoceptor model previously proposed to explain the behaviour of salmeterol. We present evidence supporting a unifying hypothesis that the duration of action both of formoterol and salmeterol is determined principally by their physicochemical interactions with membrane lipid bilayers (plasmalemma diffusion microkinetic model), rather than putative distinct exosite/exoceptor binding sites in or near the beta 2-adrenoceptor. This model provides a clearer understanding of the pharmacological profile of these drugs (rate of onset, duration, "reassertion", interaction with hydrophilic and hydrophobic beta 2-adrenoceptor antagonists), and explains why in human airway smooth muscle in vitro a true relaxation-concentration response may not exist for salmeterol.
Topics: Adrenergic beta-Agonists; Albuterol; Bronchodilator Agents; Ethanolamines; Formoterol Fumarate; Humans; Salmeterol Xinafoate
PubMed: 7912202
DOI: 10.1183/09031936.94.07030569 -
The Journal of Asthma : Official... Apr 2021Albuterol can trigger supraventricular tachycardia (SVT). The clinical characteristics, incidence, and risk factors of SVT after inhaled SABA treatment in children are...
INTRODUCTION
Albuterol can trigger supraventricular tachycardia (SVT). The clinical characteristics, incidence, and risk factors of SVT after inhaled SABA treatment in children are currently unknown. Through review of regional care delivery, we will describe cases of SVT during asthma treatment in hospital-based settings, define the incidence of SVT in our population, and evaluate risk factors of SABA-induced SVT.
METHODS
We identified hospital-based care episodes of children 0-18 years old between 2006 and 2015 recorded in the Intermountain Healthcare EDW with either 1) diagnosis codes for both asthma and SVT or 2) both SABA and adenosine listed as billed medications. Controls were matched with cases by age and sex to determine risk factors for SVT after SABA using conditional logistic regression.
RESULTS
Of 93 care episodes meeting criteria, we found 7 cases of SVT after SABA treatment in 6 patients over 10 years. In our population, the incidence of SVT is 3.9 per 10,000 episodes of SABA treatment, and 5.1 per 10,000 children with asthma receiving hospital-based asthma care. Two episodes of SVT followed treatment with only levalbuterol, three after only albuterol, and two after both albuterol and levalbuterol treatment. Five cases of SVT were converted to sinus rhythm with adenosine, one converted with synchronized electrical cardioversion, and one resolved spontaneously. No cases of SVT led to death. No examined variables were associated with SABA-induced SVT.
CONCLUSIONS
SVT is rare during hospital-based treatment for acute asthma using inhaled SABAs and has low morbidity and mortality.
Topics: Adrenergic beta-2 Receptor Agonists; Albuterol; Asthma; Body Mass Index; Child; Child, Preschool; Female; Humans; Incidence; Infant; Levalbuterol; Male; Racial Groups; Risk Factors; Tachycardia, Supraventricular
PubMed: 31902263
DOI: 10.1080/02770903.2019.1709867