Kawakatsu K, Kino T, Yasuba H, Kawaguchi H, Tsubata R, Satake N, Oshima S
Department of Hospital Pharmacy, Kyoto University, Japan.
Int J Clin Pharmacol Ther Toxicol. 1990 Apr;28(4):158-63.
The effect of ozagrel (OKY-046), a selective thromboxane A2 synthetase inhibitor, on theophylline disposition was studied in 12 asthmatic patients. Ozagrel was administered at a dose of 200 mg twice daily for 24 weeks to 4 outpatients receiving oral theophylline medication. Blood samples were drawn from each patient visiting the hospital at one to four-week intervals. There were no clinical significant changes between the time course profiles of serum theophylline concentration during the treatment and those after the cessation of ozagrel dosing. In addition, another 8 hospitalized patients received a single intravenous infusion of aminophylline (200 mg as theophylline) before and after ozagrel treatment of 200 mg twice daily for 7 days. No statistical significant alteration in elimination half-life, total body clearance or volume of distribution of theophylline was observed by the administration of ozagrel. These results suggest that ozagrel does not inhibit the metabolism of theophylline despite having an imidazole ring in its chemical structure.
在12例哮喘患者中研究了选择性血栓素A2合成酶抑制剂奥扎格雷（OKY-046）对茶碱处置的影响。4例接受口服茶碱治疗的门诊患者，给予奥扎格雷200mg，每日2次，共24周。每隔1至4周从每位前来医院就诊的患者采集血样。治疗期间血清茶碱浓度的时间过程曲线与奥扎格雷给药停止后的曲线之间无临床显著变化。此外，另外8例住院患者在每日2次给予200mg奥扎格雷治疗7天前后，接受了单次静脉输注氨茶碱（相当于200mg茶碱）。给予奥扎格雷后，未观察到茶碱的消除半衰期、总体清除率或分布容积有统计学显著改变。这些结果表明，尽管奥扎格雷的化学结构中有咪唑环，但它并不抑制茶碱的代谢。
