Causes bronchodilatation, diuresis, CNS and cardiac stimulation, and gastric acid secretion by blocking phosphodiesterase which increases tissue concentrations of cyclic adenine monophosphate (cAMP) which in turn promotes catecholamine stimulation of lipolysis, glycogenolysis, and gluconeogenesis and induces release of epinephrine from adrenal medulla cells.
藥動學
Metabolism: Children >1 year and Adults: Hepatic; involves CYP1A2, 2E1 and 3A4; forms active metabolites (caffeine and 3-methylxanthine); Protein binding: ∼ 60%(less in neonates), primarily to albumin; Vd: 0.5±0.1 L/kg; Elimination Half-life: 8±2 hrs in adult nonsmokers; 4.4 ±1 hrs in adult smokers (1-2 packs/day); 3.7±1.1 hrs in children 1-9 yrs. In newborn infants, older patients with COPD or cor pulmonale, and patients with CHF or liver disease, theophylline can have a half-life >24 hrs.
禁忌症
Same as aminophylline
懷孕分類
C
哺乳分類
Avoided, The concentration of theophylline in breast milk is similar to the maternal serum concentration. Irritability may be observed in the nursing infant. Serious adverse events in the infant are unlikely unless toxic serum levels are present in the mo
Adults and Children >45 kg:300 mg/day initial, administered in divided doses every 6-8 hours; Maintenance: 400-600 mg/day (maximum: 600 mg/day). Children ≧1 year and <45 kg : Initial dose: 10-14 mg/kg/day (maximum 300 mg/day) administered in divided doses every 4-6 hours; Maintenance: Up to 20 mg/kg/day (maximum: 600 mg/day) Full-term infants <1 year:Total daily dose (mg)= [(0.2 x age in weeks) +5] x (weight in kg) Infants <26 weeks:Administered in divided doses every 8 hours Infants ≧26 weeks:Administered in divided doses every 6 hours