cholinophyllin and Lung-Diseases--Obstructive

Topics: Adult; Albuterol; Choline; Clinical Trials as Topic; Female; Forced Expiratory Flow Rates; Humans; Lung Diseases, Obstructive; Male; Peak Expiratory Flow Rate; Theophylline; Vital Capacity

Controlled-released choline theophyllinate tablets (Sabidal SR 270, Zyma) were administered to 17 elderly patients aged between 68 and 86 years (mean 76 +/- 7 years) until steady state was obtained. The dosage form was one tablet every 12 hours for four days. Plasma theophylline concentrations were measured by high-performance liquid chromatography after the first dose and during the fourth day for a 12-hour period. The tablets showed evidence of controlled-release properties: the maximum plasma concentration (10.8 +/- 2.5 mg/l) was obtained after 3.4 +/- 1.6 hours. The mean trough level was 6.6 +/- 1.5 mg/l and the difference between the peak and trough levels was 4.1 +/- 1.2 mg/l. The mean steady-state plasma theophylline concentration was 8.5 +/- 2.2 mg/l. The mean elimination half-life was 14 +/- 7 hours. The mean volume of distribution was 0.8 +/- 0.4 l/kg. The mean total body clearance was 0.05 +/- 1/h/kg. All values, the half-life excepted, were found to be within the ranges for the patients reported in the literature. The values show the usual interindividual variation.

Topics: Aged; Aged, 80 and over; Bronchodilator Agents; Choline; Delayed-Action Preparations; Female; Half-Life; Humans; Lung Diseases, Obstructive; Male; Peak Expiratory Flow Rate; Theophylline

We studied the effect of cimetidine and theophylline on the metabolism of each drug in 19 elderly patients with stable chronic obstructive pulmonary disease. Each patient received either regular release or sustained release oxtriphylline. Cimetidine was given to some patients in both groups after steady state for theophylline was achieved. Multiple serum theophylline and cimetidine measurements were performed. Cimetidine decreased theophylline clearance by an average of 37.8% (26.2 to 46.7) for regular release and 33.4% (22.2 to 45.0) for sustained release oxtriphylline. The apparent volume of distribution was not changed; however, the half-life for theophylline was increased. As there is a linear relationship between the theophylline clearance before and after the addition of cimetidine and a linear relationship between trough and peak values before and after cimetidine, these 2 relationships may be used to predict clearance values and serum levels after cimetidine treatment when the initial values are known.

Topics: Age Factors; Aged; Bronchodilator Agents; Choline; Cimetidine; Drug Interactions; Half-Life; Humans; Lung Diseases, Obstructive; Male; Middle Aged; Theophylline; Time Factors