This study was carried out on 14 asthmatic childen aged 7–13 years. They all received three preparations (aminophylline by intravenous infusion, lysine theophyllinate orally in solution and slow release theophylline orally as capsules) in a single dose of 100 mg active ingredient in a crossover design. Plasma theophylline concentrations, determined by a fluorescent polarization immunoassay, were evaluated both by compartmental and non-compartmental analysis. After administration of slow release theophylline, its maximum plasma concentration and the time needed to reach this were (± SD) 3.19 ± 0.63 μg/ml and 8.71 ± 2.30 h, respectively, compared to 4.51 ± 0.94 μg/ml and 1.96 ± 0.85 h, respectively, for the oral normal release solution. Mean absolute and relative percentage bioavailabilities for slow release theophylline in asthmatic children were (± SD) 92.7 ± 23.2% and 83.14 ± 14.69%, respectively. These are similar to the values found with other slow release formulations in paediatric patients.

1985-03-01·Thorax1区 · 医学

Bronchodilator actions of xanthine derivatives administered by inhalation in asthma.

1区 · 医学

Article

作者: Cushley, M J ; Holgate, S T

The airway response to the inhalation of four alkyl xanthines was studied in 17 subjects with moderately severe asthma (mean FEV1 1.19 litres, 42% predicted). Theophylline (10 mg/ml), glycine theophyllinate (50 mg/ml), theophylline ethylenediamine (aminophylline 50 mg/ml), and diprophylline (125 mg/ml) were administered by nebulisation and the airway response was measured as percentage change from baseline of specific airway conductance (sGaw). All xanthine derivatives had an unpleasant taste and produced coughing at the onset of nebulisation. All four xanthines produced a significant increase in sGaw by comparison with saline placebo, with a maximum mean increase from baseline of 35% for theophylline, 40% for glycine theophyllinate, 60% for aminophylline, and 32% for diprophylline. Inhalation of 200 micrograms salbutamol from a metered dose inhaler produced an additional increase in sGaw of 149%. Thus alkyl substituted xanthines administered by inhalation to patients with asthma cause significant short lived bronchodilatation, but this effect is small compared with that of a conventional dose of an inhaled beta 2 adrenoceptor agonist.

1980-08-01·British Journal of Clinical Pharmacology2区 · 医学

Oral sustained‐release aminophylline in medical inpatients: factors related to toxicity and plasma theophylline concentrations.

2区 · 医学

Article

作者: Mackay, A ; Oliver, JS ; Ramsay, LE ; Eppel, ML

1 Consecutive medical inpatients expected to benefit from a theophyllinate were treated with sustained‐release aminophylline in a protocol conforming with ordinary practice. Of 16 patients, five had toxicity with aminophylline 450 mg daily, and a further three with 900 mg daily. Toxicity was serious in three patients. 2 Toxicity was significantly less common in cigarette smokers, and was related to higher plasma theophylline concentrations. However, there was a large overlap between concentrations associated with toxicity (as low as 9 micrograms/ml) and the accepted therapeutic range (5‐20 micrograms/ml). Most patients with toxicity had theophylline levels within the therapeutic range. 3 For the same dose of aminophylline there was sevenfold variation between patients in plasma theophylline, with higher concentrations in non‐smokers, infrequent alcohol users, older patients, those with left ventricular failure and those with lower serum transaminases. There variables could not be separated completely because of the small number of observations. 4 A nomogram for aminophylline dosage or monitoring of serum theophylline levels would have prevented little of the toxicity observed in these patients, although these measures would ensure that therapeutic concentrations were attained, and might prevent life‐threatening toxicity.

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