Efficacy of Reproterol Assessed by the Acetylcholine Provocation Test

Lode, H; Huettemann, U.; Huckauf, H.; Macha, H.-N.; Aurich, R

doi:10.1159/000194093

Cited by 2 publications

(1 citation statement)

References 15 publications

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“…This hyper reactivity can be measured by inhalation provocation tests with different agents such as histamine, acetylcholine, and pro pranolol [16]. These tests have shown to be well reproducible in patients with mild complaints, and provide useful informa tion about the severity of the disease [7,15], To protect asthmatic patients against the effects of inhaled irritants, bronchodilators can be administered [3,10], For this purpose theophylline is frequently used. The bronchodilating activity of this drug is well established [11], but conflicting re sults have been described concerning the protective qualities of theophylline against inhaled irritants [5,9], In this study we have examined the pro tective effect of a relatively low dose of choline theophyllinate on histamine, ace tylcholine, and propranolol-induced bronchial obstruction.…”

Section: Introductionmentioning

confidence: 99%

Protective Effect of Choline Theophyllinate on Histamine, Acetylcholine, and Propranolol-Induced Airflow Obstruction

Koeter

Jonkman²,

Devries

1984

Respiration

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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 2^{3.8 ± 1.0} mg/ml (p < 0.001). With acetylcholine an initial value of 24.2 ± 1.4 mg/ml was determined, which changed to 2^{5.5 ± 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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Section: Introductionmentioning

confidence: 99%

Protective Effect of Choline Theophyllinate on Histamine, Acetylcholine, and Propranolol-Induced Airflow Obstruction

Koeter

Jonkman²,

Devries

1984

Respiration

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Plasma levels, heart rate, and blood pressure after intravenous, oral, and aerosol administration of reproterol in man

Hageman

Zeeuw

Greving

et al. 1988

Biopharm & Drug Disp

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Three healthy volunteers received single doses of reproterol (D 1959) by means of intravenous infusion, oral and aerosol application, respectively. Administrations were separated by at least 1 week. Plasma levels were measured by means of high performance liquid chromatography. After infusion, plasma levels showed a steep decline, indicative for a rapid distribution. Even though relatively large amounts of drug were given (up to 540 micrograms), this phenomenon caused reproterol levels to drop to values near or below the limit of reliable quantitation (1 ng ml-1) within 60 to 90 min. After oral administration of one or two tablets (containing 20 mg reproterol HCl per tablet), a very short lag time could be observed, indicating fast absorption. After one tablet, plasma level maxima (of plateau-type) were 5-6 ng ml-1 and 2-3 ng ml-1 in two subjects, respectively. After two tablets, plateau level maxima around 18 ng ml-1 and 9 ng ml-1 were found, respectively. After inhalation of a metered aerosol (two puffs of 500 micrograms each) the drug appeared in plasma within minutes, albeit at very low levels, and usually remained detectable at the sub-nanogram level during the time of the experiment (2 h). Due to the very low levels and to some oscillations in the plasma concentration-time curves, a detailed pharmacokinetic assessment could not be carried out. Effects on heart rate and blood pressure were negligible. Only during the infusion of high doses (540 micrograms) was there an increase in heart rate of about 50 to 120 beats min-1. Other side-effects were also negligible.

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Efficacy of Reproterol Assessed by the Acetylcholine Provocation Test

Cited by 2 publications

References 15 publications

Protective Effect of Choline Theophyllinate on Histamine, Acetylcholine, and Propranolol-Induced Airflow Obstruction

Protective Effect of Choline Theophyllinate on Histamine, Acetylcholine, and Propranolol-Induced Airflow Obstruction

Plasma levels, heart rate, and blood pressure after intravenous, oral, and aerosol administration of reproterol in man

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