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  • 1
    ISSN: 1432-1041
    Keywords: salbutamol ; asthma ; beta-adrenoceptor ; controlled release formulation ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of the present study was to compare the efficacy and systemic effects of 4 mg and 8 mg doses of salbutamol controlled release (SCR) after single dosing and at steady state in patients with asthma. Fifteen asthmatic patients (Age 36 y, FEV1 85% predicted) were given SCR 4 mg and 8 mg twice daily for 7 days in a randomised double-blind cross-over design, with at least 7 days washout between treatments. There were no differences between the bronchodilator effects of 4 mg and 8 mg doses. There was no evidence of tolerance to the bronchodilator effects after chronic dosing. Morning and evening PEFR measurements also showed improvements during treatment with SCR 4 mg and SCR 8 mg, although there were no differences between the two formulations. Both doses of SCR caused significant objective tremor responses which were maintained after chronic dosing. The 8 mg dose produced a larger tremor response after single dosing, but not at steady-state. Subjective tremor occurred in 7 patients with SCR 8 mg, and in 2 patients with SCR 4 mg. There were no cardiac arrhythmias on Holter ECG monitoring. These results suggest that the 8 mg dose of SCR was no more effective than the 4 mg formulation, and was associated with more systemic adverse effects.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 36 (1989), S. 239-245 
    ISSN: 1432-1041
    Keywords: beta-adrenoceptor ; salbutamol ; airways response ; tremor ; haemodynamic response ; metabolic response
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The aim of the present study was to quantify and compare the airways and systemic beta-adrenoceptor responses to inhaled salbutamol in normal subjects. Seven non-atopic, normal subjects were given cumulative doubling doses of inhaled salbutamol (100 µg to 4000 µg) or placebo in a single-blind cross-over design. Airways (sGaw, FEF 50%, FEF 25%), tremor, haemodynamic and metabolic responses were measured at each dose increment. There were dose-related changes in sGaw, FEF 50% and FEF 25% up to a plateau at 1.0 mg. Analysis of individual responses showed that most subjects required either 1.0 or 2.0 mg for maximum bronchodilatation, independent of the parameter of airflow. There was no correlation between maximum response and baseline airway calibre. In contrast to airways effects, systemic beta-adrenoceptor responses did not occur until 500 µg, and a ceiling in the dose-response curve was not reached. Therer were significant correlations between air-ways, tremor and haemodynamic responses, and between different metabolic variables. The intraindividual variability was greatest for tremor and sGaw, although this was small in comparison to the size of maximum change with salbutamol. The converse applied to the hypomagnesaemic response.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1041
    Keywords: Salbutamol isoprenaline ; beta-adrenoceptor ; electrocardiogram ; elderly
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The purpose of the study was to compare beta-adrenoceptor responsiveness to salbutamol (beta-2 selective agonist) and isoprenaline (non-selective) in young (n=10, age 23 y) and elderly (n=7, age 71 y) subjects. Subjects were given cumulative doubling doses of inhaled isoprenaline or salbutamol (500–4000 μg), and placebo, in a single-blind randomised cross-over design. Plasma potassium, electrocardiographic (R-R, T-wave, Q-Tc) and blood pressure responses were measured at baseline and at each dose step. There were no difference between baseline values for each of the three study days within each group of subjects. Hypokalaemia was significantly greater in response to salbutamol compared with isoprenaline in both the young (as change from baseline): −0.61 versus −0.10 mmol·1−1; and in the elderly: −0.68 versus −0.20 mmol·1−1. There were no differences between young and elderly responses. T-wave amplitude fell significantly in repsonse to isoprenaline and salbutamol, although this effect was progressively attenuated with increasing doses of isoprenaline. Maximum T-wave response (change from baseline) was greater with salbutamol than isoprenaline in the young: −0.22 versus −0.11 mV; and in the elderly: −0.17 versus −0.08 mV, and there were no differences between the two groups. There were no differences between the effects of isoprenaline and salbutamol on Q-Tc prolongation or heart rate. Chronotropic responses to salbutamol were greater in the elderly: 39 versus 24 beats·min−1. There were larger increases in SBP with isoprenaline in both groups. Falls in DBP in response to isoprenaline and salbutamol were significantly greater in the elderly. These findings suggest that inhaled isoprenaline is a less potent stimulant of extrapulmonary beta-2 adrenoceptors compared with salbutamol, but has a greater effect on cardiac beta-1 adrenoceptors. There was no evidence of a decline with ageing in the function of beta-1 or beta-2 adrenoceptors.
    Type of Medium: Electronic Resource
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