Bittencourt P R, Gracia C M, Gorz A M, Oliveira T V
Clinical Neurology Unit, Hospital Nossa Senhora das Graças, Curitiba, Brasil.
Acta Neurol Scand. 1990 Jul;82(1):28-33. doi: 10.1111/j.1600-0404.1990.tb01583.x.
Serum and CSF concentrations of praziquantel were analyzed in 8 patients with active neurocysticercosis aged 35 +/- 16 (mean +/- sd) years, in order to determine factors that may improve the therapeutic ratio. Praziquantel was given orally at 6-h intervals for 10 days at a daily dose of 100 mg/kg. Serum concentrations were determined at 1, 2 and 4 h, and CSF concentrations at 2 h after the morning dose. Peak serum concentrations occurred between 1 and 2 h after administration. There was a trend towards a drop in serum concentration from Days 1 through 5 to 10 of therapy. A fourfold increase in oral dose led to an eightfold rise in serum and CSF concentration, indicating saturation of hepatic metabolism. There were linear correlations (p less than 0.01) between serum and CSF concentrations of praziquantel, indicating free flow across the blood-brain barrier, above an apparent threshold, which may be related to occupation of plasma protein-binding sites. The results indicate that monitoring of serum concentrations may be clinically useful.
对8例年龄为35±16（均数±标准差）岁的活动性神经囊尾蚴病患者的血清和脑脊液中吡喹酮浓度进行了分析，以确定可能提高治疗比率的因素。吡喹酮以每日100mg/kg的剂量，每6小时口服一次，共给药10天。在上午服药后1、2和4小时测定血清浓度，在2小时测定脑脊液浓度。给药后1至2小时出现血清浓度峰值。在治疗的第1天至第5天至第10天期间，血清浓度有下降趋势。口服剂量增加四倍导致血清和脑脊液浓度升高八倍，表明肝脏代谢已饱和。吡喹酮的血清和脑脊液浓度之间存在线性相关性（p<0.01），表明在高于一个明显阈值时，吡喹酮可自由通过血脑屏障，这可能与血浆蛋白结合位点被占据有关。结果表明，监测血清浓度可能具有临床意义。
