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 22.5 ± (SD)1.2 to 23.8 ± 1.0 mg/ml (p < 0.001). With acetylcholine an initial value of 24.2 ± 1.4 mg/ml was determined, which changed to 25.5 ± 1.1 mg/ml (p < 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 re-producibility 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 < 0.01 and r = -0.84; p < 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.

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