Bannwarth B, Netter P, Lapicque F, Gillet P, Péré P, Boccard E, Royer R J, Gaucher A
URA CNRS 1288, Faculté de Médecine de Nancy, France.
Br J Clin Pharmacol. 1992 Jul;34(1):79-81. doi: 10.1111/j.1365-2125.1992.tb04112.x.
Since the antipyretic and probably the analgesic effects of paracetamol are, at least in part, centrally mediated, its plasma and cerebrospinal fluid (CSF) concentrations were measured in 43 patients with nerve-root compression pain. Each subject was given a short i.v. infusion of 2 g propacetamol, a prodrug which is hydrolysed to paracetamol within 7 min. Single blood and CSF samples were drawn concomitantly in each patient at intervals between 20 min and 12 h. Maximum CSF drug concentrations were observed at the 4th hour, subsequent concentrations exceeding those in plasma. The elimination half-life of paracetamol calculated from pooled data was shorter in plasma (2.4 h) than in CSF (3.2 h). The time-course of paracetamol in CSF may parallel that of analgesic effect.
由于对乙酰氨基酚的退热作用以及可能的镇痛作用至少部分是由中枢介导的,因此对43例神经根压迫性疼痛患者测量了其血浆和脑脊液(CSF)浓度。每位受试者接受了2g丙帕他莫的短时间静脉输注,丙帕他莫是一种前体药物,在7分钟内可水解为对乙酰氨基酚。在每位患者中,于20分钟至12小时的间隔时间内同时采集单次血液和脑脊液样本。在第4小时观察到脑脊液药物浓度最高,随后的浓度超过血浆浓度。根据汇总数据计算得出,对乙酰氨基酚在血浆中的消除半衰期(2.4小时)短于在脑脊液中的消除半衰期(3.2小时)。脑脊液中对乙酰氨基酚的时间进程可能与镇痛作用的时间进程平行。