Bonati M, Traina G L, Gentile M G, Fellin G, Rosina R, Cavenaghi L, Buniva G
Laboratory of Clinical Pharmacology, Istituto di Ricerche Farmacologiche Mario Negri, Milano, Italy.
Br J Clin Pharmacol. 1988 Jun;25(6):761-5. doi: 10.1111/j.1365-2125.1988.tb05265.x.
The pharmacokinetic profile of teicoplanin, a new glycopeptide antibiotic active against Gram-positive aerobic and anaerobic bacteria, is described in five patients with end-stage renal disease on continuous ambulatory peritoneal dialysis (CAPD). A single 3 mg kg-1 dose was given intraperitoneally in the dialysate during a 6 h dwell time. The drug appeared in the plasma within 15 min at 1.00-0.28 mg l-1 (mean +/- s.d. = 0.70 +/- 0.45) in all five subjects, and peak serum concentrations ranged from 5.53 to 2.80 mg l-1 (4.84 +/- 1.43) at 6 h. Approximately 70% (71 +/- 12) of teicoplanin was absorbed from the peritoneal dialysis fluid during a single 6 h dwell time. The rate constant for peritoneal transfer (lambda d) averaged 0.318 h-1 and the half-life (t1/2 lambda d) was 2.18 h. Further values were serum elimination half-life 114-173 h; total body clearance 263-532 ml h-1; steady-state volume of distribution 68-93 l. This drug profile closely agrees with data reported after intravenous injection in patients on CAPD and suggests that teicoplanin has bidirectional exchange characteristics through the peritoneal membrane, although transfer from the systemic circulation to peritoneal fluid is consistently low. Instillation of teicoplanin in CAPD fluid may be a useful route of administration for treatment of peritonitis and exit site infections in CAPD patients.
在5例终末期肾病且持续非卧床腹膜透析(CAPD)的患者中,描述了替考拉宁(一种对革兰氏阳性需氧菌和厌氧菌有效的新型糖肽类抗生素)的药代动力学特征。在6小时的驻留时间内,将单次3mg/kg的剂量腹腔内注入透析液中。在所有5名受试者中,药物在15分钟内出现在血浆中,浓度为1.00 - 0.28mg/L(平均值±标准差 = 0.70±0.45),6小时时血清峰值浓度范围为5.53至2.80mg/L(4.84±1.43)。在单次6小时驻留时间内,约70%(71±12)的替考拉宁从腹膜透析液中吸收。腹膜转运速率常数(λd)平均为0.318h-1,半衰期(t1/2λd)为2.18小时。其他值为血清消除半衰期114 - 173小时;全身清除率263 - 532ml/h;稳态分布容积68 - 93L。该药物特征与CAPD患者静脉注射后报道的数据密切一致,表明替考拉宁通过腹膜具有双向交换特征,尽管从体循环到腹膜液的转运一直较低。在CAPD液中注入替考拉宁可能是治疗CAPD患者腹膜炎和出口部位感染的一种有用给药途径。