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Current Allergy and Asthma Reports Sep 2009Albuterol has been used for more than 40 years to treat acute asthma exacerbations as a racemic mixture of isomers: the active form, (R)-albuterol, or levalbuterol, and... (Comparative Study)
Comparative Study
Albuterol has been used for more than 40 years to treat acute asthma exacerbations as a racemic mixture of isomers: the active form, (R)-albuterol, or levalbuterol, and (S)-albuterol, classically considered inert. The single-isomer formulation, levalbuterol, has been synthesized recently and used therapeutically when the racemate is deemed less desirable. Basic investigations indicate that racemic albuterol and levalbuterol can produce effects that favor asthma remediation, including corticosteroid amplification and reduction of inflammatory mediators; in contrast, (S)-albuterol produces opposite effects. With inhalation of racemic albuterol, circulating (S)-albuterol persists 12 times longer than levalbuterol, suggesting potential for paradoxical effects observed clinically. Although mainly consistent with basic findings, clinical studies suggest no overwhelming superiority of levalbuterol over racemic albuterol; however, levalbuterol's effects may be greatest in moderate to severe asthma patients, especially with racemic albuterol overuse. Recent adoption of the hydrofluoroalkane formulation has narrowed the cost gap between levalbuterol and racemic albuterol metered-dose inhalers, but it remains for the nebulized formulations. Thus, physician selection of these drugs has remained dependent on experience, pharmaceutical knowledge, and established prescribing habits combined with cost factors, formulary structures, and availability, such that racemic albuterol is still used significantly compared with levalbuterol to treat acute asthma exacerbations.
Topics: Administration, Inhalation; Adrenergic beta-Agonists; Albuterol; Animals; Asthma; Clinical Trials as Topic; Humans
PubMed: 19671384
DOI: 10.1007/s11882-009-0058-6 -
The Medical Letter on Drugs and... Nov 2020
Topics: Albuterol; Anti-Asthmatic Agents; Asthma; Bronchodilator Agents; Humans; Preservatives, Pharmaceutical
PubMed: 33429403
DOI: No ID Found -
Archives of Toxicology 1994This paper reviews the published toxicology of salbutamol. Salbutamol is a relatively selective beta 2-adrenoreceptor stimulant with rapid, potent bronchodilator... (Review)
Review
This paper reviews the published toxicology of salbutamol. Salbutamol is a relatively selective beta 2-adrenoreceptor stimulant with rapid, potent bronchodilator activity and only minor inotropic or chronotropic effects. It was not found to be mutagenic. LD50 values and other acute studies indicated low toxicity. Findings published for repeat dose studies were mainly uneventful. Tachycardia and flushing of the skin were observed in dogs. There were several findings peculiar to the rat--growth of the salivary gland, enlargement of the Harderian gland, an increase in colloid in the pituitary, and mesovarian leiomyomas. Increases in heart weights associated with inflammation, hypertrophy of muscle fibres, focal myocardial necrosis and fibrosis were seen in rats. Malformation, in the form of cleft palate, was reported in mice but not in rats or rabbits. These treatment related effects reported for salbutamol are not compound-related but rather are class-related. They are an expression of pharmacological activity brought about by the excessive beta stimulant action of high dosage with the drug.
Topics: Albuterol; Animals; Carcinogens; Mutagens; Reproduction
PubMed: 8067892
DOI: 10.1007/s002040050059 -
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 -
Pharmacotherapy Feb 2000Albuterol is a 50:50 mixture of R-albuterol, the active enantiomer, and S-albuterol, which appears to be inactive in humans. The Food and Drug Administration recently... (Review)
Review
Albuterol is a 50:50 mixture of R-albuterol, the active enantiomer, and S-albuterol, which appears to be inactive in humans. The Food and Drug Administration recently approved levalbuterol, the pure R-isomer, as a preservative-free nebulizer solution. Published studies indicate that it is neither safer nor more effective than an equimolar dose of racemic albuterol (levalbuterol 1.25 mg = albuterol 2.5 mg). However, these studies were conducted in patients with stable asthma (at the top of the dose-response curve), whereas a nebulized bronchodilator most likely would be used by patients with an acute exacerbation. Because such patients, in the hospital setting, often require higher doses of albuterol, the manufacturer's recommended dose of levalbuterol is likely to be too low for rescue therapy. Levalbuterol may cost as much as 5 times more than racemic albuterol, depending on purchase method. We conclude that levalbuterol offers no advantage over albuterol but is likely to be more costly.
Topics: Administration, Inhalation; Adrenergic beta-Agonists; Albuterol; Anti-Asthmatic Agents; Asthma; Humans; Nebulizers and Vaporizers; Pharmaceutical Solutions; Stereoisomerism
PubMed: 10678290
DOI: 10.1592/phco.20.3.123.34776 -
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 -
The Medical Letter on Drugs and... Mar 2024
Topics: Humans; Albuterol; Budesonide; Asthma
PubMed: 38466211
DOI: 10.58347/tml.2024.1698a -
Emergency Medicine Journal : EMJ May 2005A short cut review was carried out to establish whether nebulised levalbuterol is better than or equivalent to albuterol for lowering serum potassium. Seven papers were... (Review)
Review
A short cut review was carried out to establish whether nebulised levalbuterol is better than or equivalent to albuterol for lowering serum potassium. Seven papers were found using the reported search, of which three presented the best evidence to answer the clinical question. The author, date and country of publication, patient group studied, study type, relevant outcomes, results and study weaknesses of these best papers are tabulated. A clinical bottom line is stated.
Topics: Adrenergic beta-Agonists; Albuterol; Emergencies; Evidence-Based Medicine; Humans; Hyperkalemia; Nebulizers and Vaporizers
PubMed: 15843710
DOI: 10.1136/emj.2005.024414 -
American Journal of Respiratory and... Nov 2006Is there scientific evidence to support the replacement of the beta-agonist racemic albuterol with levalbuterol--that is, (R)-albuterol? The argument presented further...
Is there scientific evidence to support the replacement of the beta-agonist racemic albuterol with levalbuterol--that is, (R)-albuterol? The argument presented further refines the question as "Do we wish to continue to treat asthma with a mixture of albuterol, of which half is an agent with no known benefit--that is, (S)-albuterol--and which may exacerbate the disease?"
Topics: Adrenergic beta-Agonists; Albuterol; Animals; Asthma; Cost of Illness; Disease Models, Animal; Disease Progression; Humans; Stereoisomerism
PubMed: 17060667
DOI: 10.1164/rccm.2606001 -
The Journal of Allergy and Clinical... Nov 2001
Topics: Adrenergic beta-Agonists; Albuterol; Asthma; Bronchial Hyperreactivity; Bronchial Spasm; Bronchodilator Agents; Drug Tolerance; Humans; Stereoisomerism
PubMed: 11692088
DOI: 10.1067/mai.2001.119407