Franko T G, Powell D A, Nahata M C
Eur J Clin Pharmacol. 1982;23(2):123-7. doi: 10.1007/BF00545965.
Theophylline pharmacokinetics were studied in 12 infants (age 3 weeks-6.5 months) with bronchiolitis. 9 of the 12 patients received a single dose of aminophylline (5.0-8.5 mg/kg) whereas the remainder were at steady-state receiving multiple doses (2.5-5.0 mg/kg) of aminophylline. The dose was administered IV over 0.5-1.0 h. An HPLC method was used to measure theophylline concentrations in serum and urine. Peak serum concentrations of theophylline measured by HPLC ranged from 8.48-21.6 micrograms/ml. Total, renal and nonrenal clearance of theophylline ranged from 4.66 to 19.25, 1.07 to 5.76 and 3.59 to 16.83 ml/min/m2, respectively. Mean apparent volume of distribution and elimination half-life were 8.75 l/m2 and 11.38 h, respectively. Although no significant correlation was observed between age and theophylline kinetic parameters, clearance appeared to increase and half-life decrease with age. Our patients had a substantially lower clearance and longer half-life as compared to published data in children greater than 1 year of age. A five-fold variation in theophylline clearance demonstrates the need for monitoring theophylline serum concentration to minimize the risk of potential toxicity.
对12例患有细支气管炎的婴儿(年龄3周 - 6.5个月)进行了茶碱药代动力学研究。12例患者中有9例接受了单剂量氨茶碱(5.0 - 8.5mg/kg),其余患者处于接受多剂量(2.5 - 5.0mg/kg)氨茶碱的稳态。剂量在0.5 - 1.0小时内静脉注射。采用高效液相色谱法测定血清和尿液中的茶碱浓度。通过高效液相色谱法测得的血清茶碱峰值浓度范围为8.48 - 21.6微克/毫升。茶碱的总清除率、肾清除率和非肾清除率分别为4.66至19.25、1.07至5.76和3.59至16.83毫升/分钟/平方米。平均表观分布容积和消除半衰期分别为8.75升/平方米和11.38小时。虽然未观察到年龄与茶碱动力学参数之间存在显著相关性,但清除率似乎随年龄增加而增加,半衰期随年龄降低。与1岁以上儿童的已发表数据相比,我们的患者清除率显著更低,半衰期更长。茶碱清除率的五倍差异表明需要监测茶碱血清浓度,以将潜在毒性风险降至最低。