Oral bambuterol compared to inhaled salmeterol in patients with partially reversible chronic obstructive pulmonary disease

• Published in: European journal of clinical pharmacology 1999-01, Vol.54 (11), p.829-833
• Main Authors: CAZZOLA, M, CALDERARO, F, CALIFANO, C, DI PEMA, F, VINCIGUERRA, A, DONNER, C. F, MATERA, M. G
• Format: Article
• Language: English
• Subjects: Administration, Inhalation; Administration, Oral; Adult; Aged; Albuterol - administration & dosage; Albuterol - adverse effects; Albuterol - analogs & derivatives; Albuterol - therapeutic use; Arrhythmias, Cardiac - chemically induced; Biological and medical sciences; Blood pressure; Bronchodilation; Bronchodilator Agents - adverse effects; Bronchodilator Agents - therapeutic use; Chronic obstructive pulmonary disease; Clinical trials; Cross-Over Studies; Data processing; Double-Blind Method; Drug therapy; Drugs; Forced Expiratory Flow Rates - drug effects; Forced Expiratory Volume - drug effects; Heart rate; Heart Rate - drug effects; Humans; Inhalation; Lung Diseases, Obstructive - drug therapy; Lung Diseases, Obstructive - physiopathology; Male; Medical sciences; Middle Aged; Pharmacology. Drug treatments; Respiratory system; Respiratory tract; salmeterol; Salmeterol Xinafoate; Statistical analysis; Tachycardia; Terbutaline - administration & dosage; Terbutaline - adverse effects; Terbutaline - analogs & derivatives; Terbutaline - therapeutic use; Time Factors; tremor; Tremor - chemically induced
• ISSN: 0031-6970; 1432-1041
• DOI: 10.1007/s002280050561

There is now good evidence that inhaled salmeterol is an effective agent in chronic obstructive pulmonary disease (COPD),but, at the present time, data on the effects of bambuterol, which is an oral tarbutaline pro-drug, in patients with COPD are scarce. Moreover, no comparative study between bambuterol and salmeterol in patients with chronic obstructive airway disorders has been published. The objective of this research was, consequently, to compare the efficacy and safety of 20 mg oral bambuterol and 50 microg inhaled salmeterol in patients with partially reversible COPD. The speed and length of bronchodilation with 20 mg bambuterol and 50 microg inhaled salmeterol were compared in 16 patients with partially reversible COPD. The investigation and designed as a double-blind, double-dummy, cross-over, placebo controlled and randomised study. Lung function (FEV1, FVC) and systemic variables (subjective tremor, heart rate, blood pressure) were monitored prior to the administration of the drug and for 12 h after each agent on 3 non-consecutive days. Inhalation of salmeterol induced a significant (P < 0.05) increase of lung function when compared with placebo. In addition, oral bambuterol elicited good bronchodilation, with its maximum slightly later than for salmeterol. The mean (+/- SE) AUC(0-12h)S for all patients were 3.134 1 +/- 0.553 for salmeterol and 1963 1 +/- 0.573 for bambuterol. Both AUC(0-12h)S were significantly greater than for placebo (P < 0.05), but there was no significant difference (P = 0.077) between the salmeterol and bambuterol AUC(0-12h)S. Bambuterol, but not salmeterol, caused tremor in four patients. Moreover, it induced a higher heart rate when compared with salmeterol at each considered time after the administration of the drug; differences after 9 and 12 h were statistically significant (P < 0.05). Both oral bambuterol and inhaled salmeterol resulted in good bronchodilation in patients with stable COPD. However, bambuterol, but not salmeterol, caused tremor in several subjects and elicited a more pronounced tachycardia.