Domínguez Granados R, Pita Calandre E, Girón Caro F, Gómez Rubio M, Molina Font J A
Departamento de Pediatría y Farmacología, Hospital Clínico San Cecilio, Granada.
An Esp Pediatr. 1987 Nov;27(5):357-61.
The pharmacokinetic and clinical efficacy of three theophylline slow-release formulations was studied in 29 children suffering chronic bronchial asthma. Theophylline loading dose was of 6 mg/kg; maintenance dose was adjusted according to therapeutic effect and drug plasma concentrations and ranged to 11.1 to 31.3 mg/kg/daily (means = 22.32 +/- 6.6 mg/kg/daily). Peak theophylline plasma levels were 13.38 +/- 4.83 micrograms/ml and through plasma levels were 8.73 +/- 3.78 micrograms/ml. No difference was found among theophylline formulations for clinical response nor kinetic parameters. Drug plasma half-life varied from 2.9 to 18.2 hr (means = 8.85 +/- 3.64 hr). Theophylline total body clearance and apparent volume of distribution exhibited a marked decrease during chronic drug administration in relation to the values observed after intake of the loading dose. Twenty three of the children reached a good degree of control of bronchospasm and did not require any associated medication.
在29名患有慢性支气管哮喘的儿童中研究了三种茶碱缓释制剂的药代动力学和临床疗效。茶碱负荷剂量为6mg/kg;维持剂量根据治疗效果和药物血浆浓度进行调整,范围为每日11.1至31.3mg/kg(平均=22.32±6.6mg/kg/每日)。茶碱血浆峰值水平为13.38±4.83μg/ml,血浆谷值水平为8.73±3.78μg/ml。在临床反应和动力学参数方面,茶碱制剂之间未发现差异。药物血浆半衰期从2.9至18.2小时不等(平均=8.85±3.64小时)。与服用负荷剂量后观察到的值相比,在长期给药期间,茶碱的全身清除率和表观分布容积显著降低。23名儿童达到了良好的支气管痉挛控制程度,不需要任何联合用药。