Rocci M L, Vlasses P H, Cressman M D, Sirgo M A, Plachetka J R
Division of Clinical Pharmacology, Jefferson Medical College, Thomas Jefferson University, Philadelphia, Pennsylvania.
Pharmacotherapy. 1990;10(2):92-9.
Several physiologic changes accompany the aging process and may alter the pharmacokinetics and pharmacodynamics of drugs given to elderly patients. The primary purpose of the present investigation was to compare the pharmacokinetics of labetalol in young and elderly hypertensive patients. Limited data regarding the pharmacodynamics of labetalol in each of these age groups were also evaluated. Ten young (age 32-48 yrs) and nine elderly (age 60-68 yrs) patients with essential hypertension were evaluated after the first and last doses of a 15-day regimen of labetalol. The young group received 200 mg orally at 9:00 P.M. and 9:00 A.M.; the elderly group received 200 mg once daily at 9:00 P.M. No significant differences in the mean (SD) apparent oral clearance of the drug existed between groups after the first [4.8 (1.9) and 4.3 (1.2) L/hr/kg] and final [4.4 (2.2) and 3.4 (1.0) L/hr/kg] doses of labetalol. No changes in any pharmacokinetic values for labetalol were detected as a function of age. Changes in standing blood pressure and heart rate after the first and last doses were generally similar between the young and elderly hypertensives. Labetalol was effective and well tolerated in both groups.
衰老过程会伴随多种生理变化，这些变化可能会改变给予老年患者药物的药代动力学和药效学。本研究的主要目的是比较拉贝洛尔在年轻和老年高血压患者中的药代动力学。同时也评估了关于拉贝洛尔在这两个年龄组中各自药效学的有限数据。在拉贝洛尔15天疗程的首剂和末剂给药后，对10名年轻（年龄32 - 48岁）和9名老年（年龄60 - 68岁）原发性高血压患者进行了评估。年轻组在晚上9点和上午9点各口服200毫克；老年组在晚上9点每日口服一次200毫克。在拉贝洛尔首剂[4.8（1.9）和4.3（1.2）升/小时/千克]和末剂[4.4（2.2）和3.4（1.0）升/小时/千克]给药后，两组间药物的平均（标准差）表观口服清除率无显著差异。未检测到拉贝洛尔的任何药代动力学值随年龄变化。年轻和老年高血压患者首剂和末剂给药后站立血压和心率的变化总体相似。拉贝洛尔在两组中均有效且耐受性良好。
