COMPARISON OF BRONCHODILATORY EFFICACY POTENTIAL OF RACEMIC SALBUTAMOL AND LEVOSALBUTAMOL IN PATIENTS WITH MILD TO MODERATE PERSISTENT ASTHMA (original) (raw)
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European Journal of Clinical Pharmacology, 1999
In this double-blind, placebo-controlled, crossover study we compared the bronchoprotective effects of formoterol 12 g inhaled via an HFA-134a inhaler (Modulite ® HFA) versus a CFC and a DPI device in 38 patients with mildto-moderate persistent asthma. All three formoterol preparations signifi cantly increased methacholine PD 20 and FEV 1 and improved small airway function parameters compared with placebo (p ! 0.001). No signifi cant differences were observed between formoterol formulations. In conclusion, Modulite ® HFA formoterol was found to be an effective and well tolerated treatment in patients with asthma, with comparable effi cacy to current formoterol preparations.
Keywords: Asthma, Levosalbutamol, Racemic salbutamol. Aim: The present study was conducted to compare the efficacy and safety of racemic salbutamol with levosalbutamol in patients of bronchial asthma Methods: A prospective, randomized, open label 8 weeks study. After taking informed consent of 100 patients of either sex were randomly divided in to racemic salbutamol (group A) and levosalbutamol (group B) group of 50 patients each. At first visit (0 week) Spirometry parameters like FEV1, FVC, PEFR and heart rate changes were recorded before and 20 minutes after drug administration via MDI. Patients were prescribed the study drug for further 4 weeks for safety assessment. At 4 weeks spirometry parameters and heart rate changes were recorded before and 20 minutes after drug administration. At both the visits patients were interviewed for side effects. Results were analysed at 0 and 4 weeks. Result: At 0 and 4 weeks mean percentage increase of FEV1, FVC, PEFR in levosalbutamol group after drug administration was significantly higher. Conclusion: Levosalbutamol was found to be more efficacious and safer than racemic salbutamol.
Canadian Respiratory Journal, 1997
STUDY OBJECTIVE: To compare two dosing regimens of salbutamol in acute asthma.DESIGN: Prospective randomized double-blind trial.SETTING: Urban emergency department.TYPE OF PARTICIPANTS: Patients who presented to the emergency department with moderate to severe asthma.INTERVENTIONS: All patients had pulmonary function testing and were randomized to group A (control; n=25) or group B (experimental; n=23). Group A (control) patients received salbutamol 2.5 mg delivered by wet aerosol at 0, 1 and 2 h (total dose 7.5 mg). At 20, 40, 80 and 100 mins a placebo aerosol was given. Group B patients received salbutamol 5 mg at 0 min and one-third the initial dose every 20 mins for a total of six doses by wet aerosol (total dose 15 mg).RESULTS: There were no differences in age, sex, preadmission medications or initial forced expiratory volume in 1 s (FEV1) between the groups. Forty-eight patients completed the study. Both groups of patients improved with mean absolute change in FEV1of 700 mL in...
Medical Journal of Australia, 1989
Twenty-one patients with mild-to-moderately-severe asthma participated in a placebo-controlled, double-blind, cross-over, randomized bronchodilator study of 200 Ilg of salbutamol (Glaxo) and 200 Ilg of salbutamol in the form of salbutamol sulphate (Riker;SO-Illand 2SiJl valves) that were administered by metered-dose inhalers. The mean baseline forced expired volumes in one second (FEY1) were similar for the four separate study days. The three active treatments caused a significantly-greater FEY1 response than did placebo for four hours (P<O.OS) and no difference was found between the treatments (P> O.OS). The power of the study was 7S% with a clinically-significant difference in the FEY 1 response of 2S%. The administration of 200 Ilg of salbutamol (Glaxo) caused the same FEY1 response as did that of 400 Ilg of salbutamol at the end of that study day (P> O.OS), but both 200-llg doses of salbutamol sulphate (Riker) caused a smaller FEY 1 response than did the 400 Ilg of salbutamol sulphate (P<O.OS). These observations indicate that no clinically-significant difference occurs between the bronchodilator effects of salbutamol and those of salbutamol sulphate which is administered as 200 Ilg of salbutamol equivalent, with different propellant mixtures, dispersal agents and valvular systems.
Respiratory Medicine, 2007
Background: Salbutamol, the most widely used short-acting b 2-agonist, consists of a racemic mixture of equal amounts of two enantiomers, (R)-salbutamol and (S)-salbutamol. The bronchodilator effects of salbutamol are attributed entirely to (R)-salbutamol (levosalbutamol), while (S)-salbutamol has been shown to possess bronchospastic and pro-inflammatory effects both in vitro and in vivo studies. Levosalbutamol, the (R)enantiomer of salbutamol is currently available only in a liquid formulation for use via a nebulizer. Recently, levosalbutamol to be administered via a pressurized metered dose inhaler (pMDI) has been developed. Aims: To compare the time-dependent bronchodilator responses of single doses of 100 mcg levosalbutamol and 200 mcg racemic salbutamol administered via a pMDI in subjects with stable mild-to-moderate bronchial asthma over a period of 6 h. Methods: Single doses of 100 mcg levosalbutamol, 200 mcg salbutamol and placebo were administered with a pMDI in 30 stable asthmatic subjects in a randomized, double-blind, placebo-controlled, three-way cross over study. Forced expiratory volume in 1 s (FEV 1) and forced vital capacity (FVC) were measured at baseline, and over 6 h post-study drug administration.
Comparison of bronchodilator responses of levosalbutamol
2007
Background: Salbutamol, the most widely used short-acting b 2-agonist, consists of a racemic mixture of equal amounts of two enantiomers, (R)-salbutamol and (S)-salbutamol. The bronchodilator effects of salbutamol are attributed entirely to (R)-salbutamol (levosalbutamol), while (S)-salbutamol has been shown to possess bronchospastic and pro-inflammatory effects both in vitro and in vivo studies. Levosalbutamol, the (R)enantiomer of salbutamol is currently available only in a liquid formulation for use via a nebulizer. Recently, levosalbutamol to be administered via a pressurized metered dose inhaler (pMDI) has been developed. Aims: To compare the time-dependent bronchodilator responses of single doses of 100 mcg levosalbutamol and 200 mcg racemic salbutamol administered via a pMDI in subjects with stable mild-to-moderate bronchial asthma over a period of 6 h. Methods: Single doses of 100 mcg levosalbutamol, 200 mcg salbutamol and placebo were administered with a pMDI in 30 stable asthmatic subjects in a randomized, double-blind, placebo-controlled, three-way cross over study. Forced expiratory volume in 1 s (FEV 1) and forced vital capacity (FVC) were measured at baseline, and over 6 h post-study drug administration.
American Journal of Emergency Medicine, 1996
Two cumulative doses of salbutamol delivered by metered dose inhaler (MDI) with a pear-shaped spacer were compared (400 I~g vs 600 I~g at 10-minute intervals). Twenty-two patients (mean age 35.1 -+ 11.1 years) with acute exacerbation of asthma were randomly assigned, in a doubleblind fashion, to receive salbutamol delivered with MDI into a spacer device in 4 puffs at 10-minute intervals (100 I~g or 150 Fg per actuation) during 3 hours (1200 t~g or 1800 I~g each 30 minutes). Mean peak expiratory flow rate (PEFR) and forced expiratory volume in the first second (FEVl) improved significantly over baseline values for both groups (P < .001). Nevertheless, there were no significant differences between both groups for PEFR and FEVI at any time point studied. A significant net reduction of heart rate was observed in the 400 ~g group (P < .01). On the other hand, a significant increase in heart rate was observed in the 600 iLg group (P < .001). The QTc interval did not show a significant prolongation, and the two groups presented moderate decreases of serum potassium levels. There was a significant dose-related increase (P = .027) in Sao2. Additionally, the 600 ~g group generated a serum glucose level increase from 0.85 + 0.12 mg/100 mL to 1.04 + 0.25 mg/100 mL (P = .02). At the end of treatment, the salbutamol plasma levels were 10.0 -+ 1.67 ng/mL for the 400 I~g group, and 14.0 + 2.17 for the 600 Izg group (P = .001). Finally, the overall symptom score in patients in the 600 ~g group was significantly greater than the score in the low dose group (P = ,02), with a higher incidence in 4 symptoms (tremor, headache, palpitations, and anxiety). These data support the notion that the treatment of acute asthma patients in the emergency department setting with salbutamol, 2.4 rag/h, delivered by MDI and spacer (4 puffs at 10-minute intervals) produces satisfactory bronchodilation, low serum concentration, and minimal extrapulmonary effects, However, an increase of 50% of the dose (600 p,g at 10-minute intervals) produced a nonsignificant, slightly better therapeutic response but with greater side effects, probably related to higher salbutamol levels.
Journal of Allergy and Clinical Immunology, 1995
Background: New formulations of non-chlorofluorocarbon-containing propellants for pressurized metered-dose inhaler delivery systems must be developed in response to the forthcoming ban on chlorofluorocarbon (CFC) production. Objective: This study compared the bronchodilator effects of 100, 200, and 300 lag (base equivalent) of salbutamol in a novel CFC-free propellant system (Airomir in the 3M CFC-Free System; 3M Pharmaceuticals, St. Paul, Minn.; 108 IN of salbutamol sulfate or 90 IN of salbutamol base equivalent per inhalation) with that of 100 and 200 ixg of salbutamol base in a conventional CFC propellant system (Ventolin, CFC-11/12; Allen and Hanburys, Division of Glaxo Inc., Research Triangle Park, N.C.; 90 tN of salbutamol base per inhalation) and placebo. Methods: Twenty-six patients with chronic, stable asthma, who had a forced expiratory volume in 1 second (FEV1) between 50.0% and 75.0% of predicted normal value, entered this randomized, double-blind, double-dummy, 6-period, crossover study. FEV 1 was measured before and at multiple time points (ranging from 10 to 480 minutes) after administration of one, two, and three inhalations of salbutamol/CFC-free (100, 200, and 300 IN); one and two inhalations of salbutamol/CFC ; and placebo. Safety parameters included adverse events, heart rate, blood pressure, physical examinations, electrocardiograms, and clinical laboratory tests. Parametric analysis of variance models appropriate for a 6-period crossover design were used, along with multiple comparisons according to Tukey's method. Results: All active treatments produced significantly (p < O. 0001) greater bronchodilation than placebo. The bronchodilator effect, as measured by FEV z (peak percent change, peak as a percent of predicted value, duration, and area under the curve) after two inhalations of salbutumol/CFC-free was clinically comparable to two inhalations of salbutamol/CFC, with no clinically meaningful differences in safety parameters between the two delivery systems or between different dose levels. Conclusion: These results suggest that salbutamol/CFC-free may offer a suitable alternative for salbutamol/CFC when the need arises to change from CFC-containing salbutamol products. (J ALLERGY CLIN IMMUNOL 1995;96.'50-6.)
Journal of Allergy and Clinical Immunology, 1997
Background: A long-acting inhaled bronchodilator that is both well tolerated and effective could allow for improved control of both daytime and nighttime symptoms in patients with asthma who use frequent as-needed short-acting bronchodilators despite antiinflammatory treatment.Objective and methods: We compared the efficacy and safety of inhaled salmeterol, 50 μgtwice daily, with inhaled salbutamol, 200 μg four times daily, delivered through a metereddose inhaler for 3 months in a multicenter, randomized, double-blind, parallel-group study of 228 patients (aged 12 to 76 years) with mild-to-moderate asthma.Results: A single morning dose of salmeterol produced improvement in FEV1 that was significantly greater (p≤0.012) than that produced by two doses of salbutamol (taken 6 hours apart) when patients were assessed 3 to 6 hours and 10 to 12 hours after the dose. This greater bronchodilation was present on day 1 of the study and after 4, 8, and 12 weeks of regular treatment. Over the 12 weeks, compared with salbutamol, salmeterol treatment was associated with a greater mean improvement in morning peak expiratory flow (35 L/min vs −3 L/min, p<0.001), a higher percentage of days with no symptoms (29% vs 15%; p=0.012), and a higher percentage of nights with no awakenings (14% vs −1%; p<0.001). Adverse events were similar for both treatments.Conclusions: In this study salmeterol, 50 μg twice daily, was well tolerated and more effectivethan salbutamol, 200 μg four times daily, in improving symptoms and lung function in patients with mild-to-moderate asthma.
Journal of Allergy and Clinical Immunology, 1995
Background: New formulations of non-chlorofluorocarbon-containing propellants for pressurized metered-dose inhaler delivery systems must be developed in response to the forthcoming ban on chlorofluorocarbon (CFC) production. Objective: This study compared the bronchodilator effects of 100, 200, and 300 lag (base equivalent) of salbutamol in a novel CFC-free propellant system (Airomir in the 3M CFC-Free System; 3M Pharmaceuticals, St. Paul, Minn.; 108 IN of salbutamol sulfate or 90 IN of salbutamol base equivalent per inhalation) with that of 100 and 200 ixg of salbutamol base in a conventional CFC propellant system (Ventolin, CFC-11/12; Allen and Hanburys, Division of Glaxo Inc., Research Triangle Park, N.C.; 90 tN of salbutamol base per inhalation) and placebo. Methods: Twenty-six patients with chronic, stable asthma, who had a forced expiratory volume in 1 second (FEV1) between 50.0% and 75.0% of predicted normal value, entered this randomized, double-blind, double-dummy, 6-period, crossover study. FEV 1 was measured before and at multiple time points (ranging from 10 to 480 minutes) after administration of one, two, and three inhalations of salbutamol/CFC-free (100, 200, and 300 IN); one and two inhalations of salbutamol/CFC ; and placebo. Safety parameters included adverse events, heart rate, blood pressure, physical examinations, electrocardiograms, and clinical laboratory tests. Parametric analysis of variance models appropriate for a 6-period crossover design were used, along with multiple comparisons according to Tukey's method. Results: All active treatments produced significantly (p < O. 0001) greater bronchodilation than placebo. The bronchodilator effect, as measured by FEV z (peak percent change, peak as a percent of predicted value, duration, and area under the curve) after two inhalations of salbutumol/CFC-free was clinically comparable to two inhalations of salbutamol/CFC, with no clinically meaningful differences in safety parameters between the two delivery systems or between different dose levels. Conclusion: These results suggest that salbutamol/CFC-free may offer a suitable alternative for salbutamol/CFC when the need arises to change from CFC-containing salbutamol products. (J ALLERGY CLIN IMMUNOL 1995;96.'50-6.)