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Current Allergy and Asthma Reports Mar 2003Levalbuterol, the pure (R)-isomer of racemic albuterol, is a new therapeutic option for patients with asthma. Racemic albuterol comprises a 50:50 mixture of (R)- and... (Comparative Study)
Comparative Study Review
Levalbuterol, the pure (R)-isomer of racemic albuterol, is a new therapeutic option for patients with asthma. Racemic albuterol comprises a 50:50 mixture of (R)- and (S)-albuterol, with (R)-albuterol conferring all of the bronchodilator effects of the racemate. Numerous preclinical and in vitro studies have indicated that (S)-albuterol is not an inert isomer, but may have proinflammatory effects. Results from clinical trials in adults and children with asthma have demonstrated that 0.63 mg levalbuterol provides effective bronchodilation with lower b-mediated side effects compared with 2.5 mg racemic albuterol. In the emergency department, levalbuterol provided greater bronchodilation and significantly reduced hospital admissions compared with racemic albuterol. Recent studies have supported that levalbuterol use in acute settings may reduce the cost of asthma treatment by decreasing the total treatments and subsequent respiratory therapy resources. Levalbuterol provides heath care professionals with a safe, effective, and potentially cost-saving alternative to racemic albuterol for the treatment of patients with asthma.
Topics: Acute Disease; Albuterol; Asthma; Bronchodilator Agents; Humans
PubMed: 12562558
DOI: 10.1007/s11882-003-0031-8 -
The Journal of Allergy and Clinical... Dec 1998Racemic albuterol is an equal mixture of (R)-albuterol (levalbuterol), which is responsible for the bronchodilator effect, and (S)-albuterol, which provides no benefit... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
BACKGROUND
Racemic albuterol is an equal mixture of (R)-albuterol (levalbuterol), which is responsible for the bronchodilator effect, and (S)-albuterol, which provides no benefit and may be detrimental.
OBJECTIVE
We sought to compare 2 doses of a single enantiomer, levalbuterol (0.63 mg and 1.25 mg), and equivalent amounts of levalbuterol administered as racemic albuterol with placebo in patients with moderate-to-severe asthma.
METHODS
This was a randomized, double-blind, parallel-group trial. Three hundred sixty-two patients 12 years of age or older were treated with study drug administered by means of nebulization 3 times daily for 28 days. The primary endpoint was peak change in FEV1 after 4 weeks.
RESULTS
The change in peak FEV1 response to the first dose in the combined levalbuterol group was significantly greater compared with the combined racemic albuterol group (0.92 and 0.82 L, respectively; P =.03), with similar but nonsignificant results after 4 weeks (0.84 and 0.74 L, respectively). Improvement in FEV1 was similar for levalbuterol 0.63 mg and racemic albuterol 2.5 mg and greatest for levalbuterol 1.25 mg. Racemic albuterol 1.25 mg demonstrated the weakest bronchodilator effect, particularly after chronic dosing. The greatest increase in FEV1 was seen after levalbuterol 1.25 mg, especially in subjects with severe asthma. All active treatments were well tolerated, and beta-adrenergic side effects after administration of levalbuterol 0.63 mg were reduced relative to levalbuterol 1.25 mg or racemic albuterol 2.5 mg. At week 4, the predose FEV1 value was greatest in patients who received levalbuterol or placebo when compared with those who received racemic albuterol. The difference was more evident and was statistically significant in patients who were not receiving inhaled corticosteroids.
CONCLUSION
Levalbuterol appears to provide a better therapeutic index than the standard dose of racemic albuterol. These results support the concept that (S)-albuterol may have detrimental effects on pulmonary function.
Topics: Adolescent; Adult; Aged; Aged, 80 and over; Albuterol; Asthma; Bronchodilator Agents; Child; Female; Forced Expiratory Volume; Humans; Male; Middle Aged; Risk Assessment; Stereoisomerism
PubMed: 9847435
DOI: 10.1016/s0091-6749(98)70332-x -
The Journal of Emergency Medicine Jul 2003Albuterol is an effective treatment for hyperkalemia through beta-adrenergic induction of potassium (K+) uptake. Levalbuterol, the R-enantiomer of racemic albuterol, is... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Albuterol is an effective treatment for hyperkalemia through beta-adrenergic induction of potassium (K+) uptake. Levalbuterol, the R-enantiomer of racemic albuterol, is used for the treatment of asthma and 0.63 mg of levalbuterol has the same therapeutic efficacy as 2.5 mg of albuterol but with a decreased adverse effects profile. We hypothesized that levalbuterol can reduce serum K+ levels similarly to albuterol when used in equipotent doses. In a randomized, double blind, placebo-controlled prospective study, we compared the K+-lowering effects of nebulized saline and equipotent bronchodilatory doses of albuterol (10 mg) and levalbuterol (2.5 mg) in healthy adult volunteers. Nine subjects entered each of the three study groups. Serum K+ was measured at baseline, at 30 min (immediately after treatment), at 60 min, and at 90 min. All adverse effects were recorded. The three groups had similar baseline K+ values. Immediately after nebulization, only levalbuterol showed a significant decrease in potassium level (p = 0.024). At 30 and 60 min after treatment, both albuterol and levalbuterol groups had significantly lower K+ values compared to placebo. No significant difference occurred between the albuterol and levalbuterol groups. Levalbuterol caused fewer reported adverse effects compared to albuterol.
Topics: Adrenergic beta-Agonists; Adult; Albuterol; Double-Blind Method; Humans; Nebulizers and Vaporizers; Potassium; Prospective Studies; Reference Values; Tachycardia; Treatment Outcome
PubMed: 12865102
DOI: 10.1016/s0736-4679(03)00133-1 -
Lung Apr 2017Albuterol is the most commonly used β agonist to treat reversible lower airway obstruction. Albuterol contains a racemic mixture of two enantiomers. Levalbuterol... (Comparative Study)
Comparative Study Randomized Controlled Trial
BACKGROUND
Albuterol is the most commonly used β agonist to treat reversible lower airway obstruction. Albuterol contains a racemic mixture of two enantiomers. Levalbuterol contains the single R form enantiomer. Levalbuterol is frequently prescribed to limit cardiovascular toxicity.
OBJECTIVE
We examined changes in oxygen consumption (V'O) and heart rate (HR) following administration of albuterol and levalbuterol.
METHODS
This is a prospective, randomized, single-blinded, controlled study of healthy adult volunteers. Subjects separately received albuterol (5 mg) and levalbuterol (2.5 mg) aerosolized over 15 min. V'O and vital signs were measured before the medications and 5, 10, 20, 40, and 60 min after.
RESULTS
We enrolled 24 volunteers with a median age of 32 years. Compared to baseline, there was a significant maximum increase in V'O following administration of both albuterol (median 17% (1, 3 IQR 9, 43%) p < 0.001) and levalbuterol (median 23% (1, 3 IQR 10, 32%) p < 0.001). There was no significant difference between the maximum increase in V'O following administration of albuterol compared to levalbuterol (p = 0.57). Compared to baseline, there was a significant maximal increase in HR with both albuterol (median 30% (1, 3 IQR 19, 43%) p < 0.001) and levalbuterol (median 23% (1, 3 IQR 19, 31%) p < 0.001). There was a statistically significant greater increase in maximal HR following administration of albuterol as compared to levalbuterol (p = 0.009).
CONCLUSION
Albuterol and levalbuterol both cause a significant increase in V'O and HR. There was no significant difference between albuterol and levalbuterol regarding the maximum increase in V'O. There was a statistically significant but likely clinically insignificant difference in maximum increase in HR in patients with adequate oxygen delivery when comparing albuterol to levalbuterol.
Topics: Administration, Inhalation; Adult; Albuterol; Bronchodilator Agents; Healthy Volunteers; Heart Rate; Humans; Levalbuterol; Middle Aged; Oxygen Consumption; Prospective Studies; Single-Blind Method; Young Adult
PubMed: 28210808
DOI: 10.1007/s00408-017-9982-8 -
Current Allergy and Asthma Reports Jul 2007The purpose of this review is to determine whether the proinflammatory actions identified in vitro for (S)-albuterol provide a clinically significant therapeutic... (Comparative Study)
Comparative Study Review
The purpose of this review is to determine whether the proinflammatory actions identified in vitro for (S)-albuterol provide a clinically significant therapeutic advantage for levalbuterol over racemic albuterol. Clinical trials evaluating the bronchodilation in chronic and acute asthma provide conflicting evidence. Older trials suggested an advantage for levalbuterol; however, the newer trials have failed to confirm those advantages. Although (S)-albuterol produces increased bronchial hyperresponsiveness in vitro and in animal models, this has not been consistently confirmed in clinical trials; however, the heterogeneity of the trials precludes definitive conclusions. Current clinical trials do not provide evidence of a substantial advantage of levalbuterol over racemic albuterol although the data are insufficient to determine whether subsets of the patient population might benefit from single isomer therapy.
Topics: Albuterol; Animals; Asthma; Bronchial Hyperreactivity; Bronchodilator Agents; Clinical Trials as Topic; Disease Models, Animal; Humans
PubMed: 17547854
DOI: 10.1007/s11882-007-0046-7 -
The Journal of Pediatrics Dec 2003To determine whether levalbuterol resulted in fewer hospital admissions than racemic albuterol when used for treatment of acute asthma. Study design A randomized,... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
OBJECTIVE
To determine whether levalbuterol resulted in fewer hospital admissions than racemic albuterol when used for treatment of acute asthma. Study design A randomized, double-blind, controlled trial was conducted in the emergency department (ED) and inpatient asthma care unit of an urban tertiary children's hospital. Children age 1 to 18 years (n=482) provided a total of 547 enrollments. Patients received a nebulized solution of either 2.5 mg racemic albuterol or 1.25 mg levalbuterol every 20 minutes (maximum six doses). Patients admitted to the asthma care unit were treated in a standardized fashion by using the same blinded drug assigned in the ED. Hospitalization rate was the primary outcome.
RESULTS
Hospitalization rate was significantly lower in the levalbuterol group (36%) than in the racemic albuterol group (45 %, P=.02). The adjusted relative risk of admission in the racemic group compared with the levalbuterol group was 1.25 (95% confidence interval, 1.01-1.57). Hospital length of stay was not significantly shorter in the levalbuterol group (levalbuterol, 44.9 hours; racemic albuterol, 50.3 hours; P=.63). No significant adverse events occurred in either group.
CONCLUSIONS
Substituting levalbuterol for racemic albuterol in the ED management of acute asthma significantly reduced the number of hospitalizations.
Topics: Acute Disease; Adolescent; Albuterol; Asthma; Bronchodilator Agents; Child; Child, Preschool; Double-Blind Method; Emergency Service, Hospital; Female; Hospitalization; Humans; Infant; Isomerism; Male
PubMed: 14657817
DOI: 10.1067/S0022-3476(03)00493-1 -
The Medical Letter on Drugs and... Jun 1999
Topics: Adrenergic beta-Agonists; Albuterol; Asthma; Child; Digoxin; Drug Interactions; Humans; Isomerism
PubMed: 10368697
DOI: No ID Found -
Lancet (London, England) Jan 1977
Clinical Trial Randomized Controlled Trial
Topics: Albuterol; Child, Preschool; Cough; Drug Evaluation; Humans; Infant; Placebos; Whooping Cough
PubMed: 64689
DOI: 10.1016/s0140-6736(77)91752-4 -
The Journal of Asthma : Official... Jun 2000Albuterol, in all marketed forms, is sold as a racemate, composed of a 50:50 mixture of (R)- and (S)-isomers. Racemic albuterol and the single isomer version... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Albuterol, in all marketed forms, is sold as a racemate, composed of a 50:50 mixture of (R)- and (S)-isomers. Racemic albuterol and the single isomer version (R)-albuterol (levalbuterol) were compared in a randomized, double-blind, dose-ranging five-way crossover study in patients (n = 20) with mild persistent to moderate persistent asthma. Placebo, racemic albuterol (2.50 mg), or levalbuterol (0.31, 0.63, or 1.25 mg) were delivered as single, nebulized doses to 5 male and 15 female nonsmoking patients with asthma aged 18-50 years. Serial pulmonary function was assessed at 15-min intervals and mean time to onset of activity and duration of improvement of forced expiratory volume in 1 sec (FEV1) were measured. In addition, blood chemistries, electrocardiogram (ECG) readings, and patient subjective assessment of adverse symptoms were recorded. Levalbuterol was found to provide significant bronchodilatory activity and was well tolerated. Levalbuterol 1.25 mg provided the greatest increase and duration in FEV1 improvement, whereas racemic albuterol (2.50 mg) and levalbuterol 0.63 mg provided comparable effects. The lower doses of levalbuterol were associated with a less marked effect on heart rate and potassium than racemic albuterol or high-dose levalbuterol. These data suggest that 0.63 mg levalbuterol provides bronchodilation equivalent to 2.50 mg racemic albuterol with less beta-mediated side effects.
Topics: Adolescent; Adult; Albuterol; Asthma; Bronchodilator Agents; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Female; Forced Expiratory Volume; Humans; Male; Middle Aged; Racemases and Epimerases; Stereoisomerism
PubMed: 10883742
DOI: 10.3109/02770900009055455 -
JAMA Dec 1988Orally or intravenously administered beta 2-adrenergic drugs have been found to inhibit esophageal motor function. Since inhalation of these drugs results in less... (Clinical Trial)
Clinical Trial
Orally or intravenously administered beta 2-adrenergic drugs have been found to inhibit esophageal motor function. Since inhalation of these drugs results in less systemic side effects, the present double-blind study was designed to investigate the influence of inhalation of the beta 2-adrenergic agonist albuterol (salbutamol) on esophageal motor function and gastroesophageal reflux in ten healthy volunteers. Esophageal motor function was recorded using a pneumohydraulically perfused multilumen manometry tube. Twenty-four-hour pH profiles were measured while the volunteers were ambulatory using a combined glass electrode connected to a portable recorder. Inhalation decreased neither lower esophageal sphincter pressure nor esophageal peristaltic amplitudes. Gastroesophageal reflux was similar on both occasions during inhalation of albuterol (3.1% [range, 1.0% to 25.5%] median upright time, with esophageal pH less than 4; and 0.1% [range, 0.0% to 10.7%] supine time) and during placebo treatment (3.6% [range, 1.6% to 19.8%] upright and 0.0% [range, 0.0% to 2.5%] supine time). Our data support the study of inhalation of beta 2-adrenergic drugs in asthmatic patients with accompanying gastroesophageal reflux.
Topics: Administration, Inhalation; Adult; Albuterol; Asthma; Double-Blind Method; Esophagus; Female; Gastroesophageal Reflux; Humans; Hydrogen-Ion Concentration; Male; Manometry
PubMed: 3184393
DOI: No ID Found