Theophylline: Distribution: 0.45 L/kg based on ideal body weight. Protein binding: ~40%, primarily to albumin. Metabolism: Hepatic via demethylation (CYP 1A2) and hydroxylation (CYP 2E1 and 3A4); forms active metabolites (caffeine and 3-methylxanthine). Half-life elimination: 8.7 hours. Time to peak, serum: Within 30 minutes. Excretion: Urine (10% as unchanged drug).
禁忌症
Hypersensitivity to aminophylline, theophylline, ethylenediamine, or any component of the formulation.
Bronchodilator: IV: 250~500mg/6hr. Acute attack: Loading dose: IV 6 mg/kg , the infusion time must be more than 20 minutes. Maintenance dose: (1) Elderly or patients with pulmonary heart disease: IV 0.6mg/kg for 12 hours, and then 0.3mg/kg/hr. (2) Non-smoking healthy adults: IV 0.7mg/kg for 12 hours, and then 0.5mg/kg/hr. (3) congestive heart failure or liver failure: IV 0.5mg/kg for 12 hours, and then 0.1-0.2mg/kg/hr. (4) Young smoking adults: 1 mg/kg for 12 hours, and then 0.8 mg /kg /hr. Cardiac stimulant: IV 0.5mg, administered slowly.
小兒調整劑量
Bronchodilator: IV 5 mg/kg/6hr. Acute attack: Loading Dose (≥ 6 months and < 16 years) : IV 6 mg/kg , the infusion time must be more than 20 minutes. Maintenance dose: (1)≥6 months and < 9 years: IV 1.2 mg/kg for 12 hours; then 1 mg/kg/hr. (2)9 to 16 years: IV 1 mg/kg for 12 hours, then 0.8mg/kg/hr.