Bednarczyk E M, Green J A, Nelson A D, Leisure G P, Little D, Adler L P, Berridge M S, Panacek E A, Miraldi F D
Department of Medicine, Case Western Reserve University School of Medicine, Cleveland, Ohio.
Pharmacotherapy. 1992;12(5):369-75.
The mechanism by which the fluorinated quinolones produce central nervous system (CNS) effects is currently unknown. We measured the effect of lomefloxacin on cerebral blood flow and metabolism using positron emission tomography. Eighteen healthy, nonsmoking volunteers were randomized to receive lomefloxacin 400 mg, ciprofloxacin 750 mg, or placebo given in a single-blind fashion every 12 hours for 72 hours, the time window for maximum lomefloxacin CNS effects. Subjects receiving lomefloxacin had a mean (+/- SEM) cerebral blood flow (CBF) of 46 (2.9) ml/min/100 g, glucose metabolism (FDG) 4.7 (0.4) mg/min/100 g, oxygen metabolism (OM) 3.3 (0.3) ml/min/100 g, and oxygen extraction (%OM) 0.4 (0.04). Posttreatment values were 43 (3.6) ml/min/100 g, 4.2 (0.4) mg/min/100 g, 2.6 (0.3) ml/min/100 g, and 0.4 (0.03), respectively. Values for subjects receiving ciprofloxacin were CBF 44.8 (1.6) ml/min/100 g, FDG 4.9 (0.7) mg/min/100 g, OM 4.1 (0.4) ml/min/100 g, and %OM 0.6 (0.03) at baseline, and 40.3 (3.5), 4.5 (0.6), 3.4 (0.4), and 0.5 (0.09), respectively, after treatment. For placebo-treated subjects, baseline values were CBF 41.4 (1.9) ml/min/100 g, FDG 4.9 (0.5) mg/min/100 g, OM 3.3 (0.4) ml/min/100 g, and %OM 0.5 (0.07), and respective posttreatment values were 42.1 (2.3), 5.0 (0.6), 3.5 (0.3), and 0.5 (0.02). No effect was observed on visual (qualitative), blinded reading of the scans. No significant effect on cerebral blood flow or metabolism was detected. We conclude that short-term administration of lomefloxacin or ciprofloxacin to healthy volunteers does not have a significant effect on cerebral blood flow, or on oxygen or glucose metabolism.(ABSTRACT TRUNCATED AT 250 WORDS)
目前尚不清楚氟喹诺酮类药物产生中枢神经系统（CNS）效应的机制。我们使用正电子发射断层扫描测量了洛美沙星对脑血流量和代谢的影响。18名健康、不吸烟的志愿者被随机分组，以单盲方式每12小时接受400mg洛美沙星、750mg环丙沙星或安慰剂，共72小时，这是洛美沙星产生最大CNS效应的时间窗。接受洛美沙星的受试者平均（±SEM）脑血流量（CBF）为46（2.9）ml/min/100g，葡萄糖代谢（FDG）为4.7（0.4）mg/min/100g，氧代谢（OM）为3.3（0.3）ml/min/100g，氧摄取率（%OM）为0.4（0.04）。治疗后的值分别为43（3.6）ml/min/100g、4.2（0.4）mg/min/100g、2.6（0.3）ml/min/100g和0.4（0.03）。接受环丙沙星的受试者基线时CBF为44.8（1.6）ml/min/100g，FDG为4.9（0.7）mg/min/100g，OM为4.1（0.4）ml/min/100g，%OM为0.6（0.03），治疗后分别为40.3（3.5）、4.5（0.6）、3.4（0.4）和0.5（0.09）。对于接受安慰剂治疗的受试者，基线值为CBF 41.4（1.9）ml/min/100g，FDG 4.9（0.5）mg/min/100g，OM 3.3（0.4）ml/min/100g，%OM 0.5（0.07），治疗后相应值分别为42.1（2.3）、5.0（0.6）、3.5（0.3）和0.5（0.02）。在对扫描结果进行视觉（定性）、盲法解读时未观察到影响。未检测到对脑血流量或代谢有显著影响。我们得出结论，对健康志愿者短期给予洛美沙星或环丙沙星对脑血流量、氧或葡萄糖代谢没有显著影响。（摘要截断于250字）
