cholinophyllin and Airway-Obstruction

Exercise-induced asthma (EIA) was provoked by standardized treadmill running for 6 minutes in 15 asthmatic children. The tests were carried out after the administration of a placebo, salbutamol, sodium cromoglycate, choline theophyllinate, and atrophine methonitrate aerosol in randomized fashion on different days. The mean post-exercise percent fall in peak expiratory flow rate was 45-2, 4-1, 19-6, 18-3, and 24-9 respectively. The proportion of children having significant amelioration of their EIA compared with those taking the placebo was 100% for salbutamol, 80% for cromoglycate and theophyllinate, and 60% for atropine. Salbutamol, choline theophyllinate, and atropine were bronchodilators at rest whereas cromoglycate was not, and the ability to suppress EIA was unrelated to bronchodilator effect. Even after bronchodilatation at rest, further broncho-dilatation occurred during the exercise period.

Topics: Adolescent; Airway Obstruction; Albuterol; Asthma; Atropine Derivatives; Bronchodilator Agents; Child; Child, Preschool; Choline; Clinical Trials as Topic; Cromolyn Sodium; Humans; Peak Expiratory Flow Rate; Physical Exertion; Placebos; Theophylline

The protective effect of choline theophyllinate, 600 mg orally, was studied by examining the effects on inhaled histamine, acetylcholine, and propranolol in 19 asthmatic patients. Only 9 of them showed a propranolol threshold. This bronchodilator significantly increased the threshold values of histamine and acetylcholine, but showed no protective effect on propranolol thresholds. The histamine threshold changed from 2(2.5 +/- (SD)1.2) to 2(3.8 +/- 1.0) mg/ml (p less than 0.001). With acetylcholine an initial value of 2(4.2 +/- 1.4 mg/ml was determined, which changed to 2(5.5 +/- 1.1 mg/ml (p less than 0.01). The propranolol threshold changed from 1.17% +/- 0.40 to 1.36% +/- 0.40 indicating that theophylline has no statistically significant protective effect on propranolol inhalation. The reproducibility of the challenges was assessed in 8 control patients. A placebo did not significantly change the initial airway reactivity to the three agents. The protective effect of choline theophyllinate on histamine and acetylcholine correlated with the initial degree of reactivity on both agents (r = -0.60; p less than 0.01 and r = -0.84; p less than 0.001, respectively), whereas no significant correlation with the degree of bronchodilation was observed. The latter observation indicates that the protective effect of theophylline does not depend on its bronchodilating activity.

Topics: Acetylcholine; Adolescent; Adult; Airway Obstruction; Bronchodilator Agents; Choline; Female; Forced Expiratory Volume; Histamine; Humans; Male; Propranolol; Respiratory System; Theophylline

Using a randomized double-blind procedure, seventeen patients with chronic airways obstruction completed a placebo-controlled study to compare bronchodilator effects of single doses of choline theophyllinate 400 mg and salbutamol 4 mg. As determined by a range of spirometric measurements, the effects of the two drugs were remarkably similar and there were no statistically significant differences in any of the parameters measured. Both drugs produced highly significant differences in comparison with placebo response. Side-effects were mainly complaints of digital tremor; this was seen in four of the patients after salbutamol and in less pronounced form in two patients after choline theophyllinate.

Topics: Administration, Oral; Adult; Aged; Airway Obstruction; Albuterol; Bronchodilator Agents; Choline; Clinical Trials as Topic; Double-Blind Method; Female; Humans; Male; Middle Aged; Placebos; Random Allocation; Theophylline

Exercise-induced asthma (EIA) was provoked by standardized treadmill running for 6 minutes in 15 asthmatic children. The tests were carried out after the administration of a placebo, salbutamol, sodium cromoglycate, choline theophyllinate, and atrophine methonitrate aerosol in randomized fashion on different days. The mean post-exercise percent fall in peak expiratory flow rate was 45-2, 4-1, 19-6, 18-3, and 24-9 respectively. The proportion of children having significant amelioration of their EIA compared with those taking the placebo was 100% for salbutamol, 80% for cromoglycate and theophyllinate, and 60% for atropine. Salbutamol, choline theophyllinate, and atropine were bronchodilators at rest whereas cromoglycate was not, and the ability to suppress EIA was unrelated to bronchodilator effect. Even after bronchodilatation at rest, further broncho-dilatation occurred during the exercise period.

Topics: Adolescent; Airway Obstruction; Albuterol; Asthma; Atropine Derivatives; Bronchodilator Agents; Child; Child, Preschool; Choline; Clinical Trials as Topic; Cromolyn Sodium; Humans; Peak Expiratory Flow Rate; Physical Exertion; Placebos; Theophylline

In a double blind cross-over comparison of a single dose 450-mg slow-release aminophylline (SRA) with placebo in eleven patients with stable, reversible airways obstruction SRA produced significantly greater increase in FEV1 and vital capacity from 2 to 9 hr after administration. A second double-blind cross-over comparison of 450-mg SRA with 400 mg of choline theophyllinate (CT) in eleven similar patients showed that SRA produced a slower rise in FEV1 and VC than CT. However, the increase in spirometric readings following SRA was sustained at 9 hr after administration where the spirometric recordings after CT were falling. Whereas CT produced a peak value in plasma theophylline at 1 hr, the highest values after SRA occurred at 4 or 8 hr after administration. The plasma theophylline level at 8 hr after SRA was significantly higher than that following CT. In this single-dose study, plasma theophylline levels obtained were within the normal therapeutic range and this was not exceeded and no side effects were recorded.

Topics: Adult; Aged; Airway Obstruction; Aminophylline; Choline; Delayed-Action Preparations; Double-Blind Method; Female; Humans; Male; Middle Aged; Placebos; Respiratory Function Tests; Theophylline

Serum theophylline levels were studied in relation to oral doses of oxtriphylline in 30 patients with reversible airway obstruction. A wide scattering of levels was observed and was attributed to widely differing rates of metabolism of the drug. From the data obtained it was concluded that the most commonly prescribed daily dose of oxtriphylline, 800 mg, will produce a therapeutic level of theophylline in only about one quarter of patients. A daily starting dose of 15 to 20 mg/kg, however, will produce therapeutic levels in approximately one third of patients without significant toxic effects. Once the patient's conditions is stable the serum theophylline concentration should be measured; if it is subtherapeutic the dose of oxtriphylline should be increased slowly and the serum theophylline concentration remeasured until a level of 10 to 20 microgram/ml is achieved.

Topics: Administration, Oral; Adult; Aged; Airway Obstruction; Choline; Dose-Response Relationship, Drug; Female; Humans; Immunoenzyme Techniques; Kinetics; Male; Middle Aged; Theophylline