Pharmacokinetics of Sustain-Released Theophylline in Asthmatic Patients with Nocturnal Dyspnea

持續釋放型茶鹼對夜間氣促之氣喘病人之藥物動力學研究

彭萬誠(Wann-Cherng Perng) ； 吳清平(Chin-Pyng Wu) ； 徐剛(Kang Hsu) ； 沈建業(Chien-Yeh Shen) ； 汪大衛(David Wang)

《Journal of Medical Sciences》 11卷6期 (1991/12) Pp. 419-429

摘要

對11位患有夜間氣促之氣喘病人，投與單一每日晚間持續釋放型茶鹼（Uniphyllin）。經每日口服600毫克（每公斤9.91±1.13毫克）茶鹼，四天後在穩定狀態下，血清茶鹼濃度在服後6.9±1.0小時到達最高點18.5±2.1毫克／升（平均值±標準誤），24小時到達最低點5.3 ±0.8毫克／升。血清治療茶鹼濃度可保持11.0±1.7小時。穩定狀態下血清茶鹼濃度比單一初劑量濃度約高3～5毫克／升。經每日清晨加與225毫克aminophylline （Phyllocontin），四天後血清治療茶鹼可維持延長達17.9±1.4小時，並且有較低之最高／最低比值（2.3±0.2） 。所有夜間氣促症狀對此治療皆獲進步。唯開始時短暫的腸胃道不適頗常見（6／11位病人）。其似乎與血清茶鹼濃度不一定相關。個人血清茶鹼濃度差異頗大，顯示血清茶鹼濃度監測是必需的。故適當之口服單一夜間持續放血型茶鹼（10毫克／公斤Uniphyllin）不能確保維持整日之血清治療茶鹼濃度。然而此劑量對氣喘病人夜間氣促之緩解為一有效之治療。

關鍵字

持續釋放型茶鹼 ； 氣喘 ； 高效率渡相層析

並列摘要

Eleven asthmatic patients with nocturnal dyspnea were given a single evening dose of sustain- released theophylline preparation (Uniphyllin Unicontin tablets) daily. After four days of receiving 600 mg (9.91±0.34 mg/Kg) theophylline by oral daily， serum theophylline levels in steady state reach a peak of 18.5±2.1 mg/L (mean±SE) at 6.9±1.0 hours, with a trough of 5.3±0.8 mg/L at 24 hours. A therapeutic period of l1.0±1.7 hours for serum theophylline levels (10-20 mg/L) was obtained. The steady state values were about 3-5 mg/L higher than that of the initial phase. After a further four days of aminophylline 225 mg (Phyllocontin) daily was prescribed in the early morning, we obtained a significantly longer therapeutic period (17.9±1.4 hours) and lower peak/trough ratio (2.3±0.2). Nocturnal dyspnea was improved. Unwanted effect of initial transient gastrointestinal intolerance was high (6 of 11 patients), which was unrelated to serum theophylline levels. The wide fluctuation of individual serum theophylline levels suggested that monitoring of serum theophylline is necessary. We concluded that an adequate oral single evening sustain-released theophylline (10 mg/Kg of Uniphyllin) could not ensure that the serum therapeutic theophylline levels could be maintained all day long, but it was an effective treatment for relieving nocturnal dyspnea in asthmatics.

並列關鍵字

Sustain-released theophylline ； Asthma ； High performance liquid chromotography