Tjandramaga T B, Verbeeck R, Thomas J, Verbesselt R, Verberckmoes R, Schepper P J
Br J Clin Pharmacol. 1976 Apr;3(2):259-65. doi: 10.1111/j.1365-2125.1976.tb00601.x.
A single oral dose of sotalol (160 mg) was administered to control subjects with normal renal function and patients with chronic renal failure in the interdialysis period to estimate the elimination kinetics of the drug. Sotalol concentrations in body fluids were measured fluorimetrically using a modified Garrett and Schnelle (1971) method. Mean plasma half-life (T 1/2) was approximately 5 h in normals, 42 h in patients off-dialysis. During haemodialysis the mean plasma half-time was on the average 7 hours. Comulative urinary excretion of the drug was considerably lower in the patient group: 9% of the dose in 48 h as opposed to 61% in normals. Comparison of sotalol concentrations in plasma versus ultrafiltrate from the coil kidney indicates that the drug in vivo is negligible bound to plasma proteins in remal patients. The net-lowering effect of a 6 to 7 h haemodialysis on the plasma concentration decay line was by 20%. Post-dialysis plasma concentration data suggest that the rate at which sotalol returns to plasma from body tissues appears to be the rate-controlling factor in the elimination of sotalol by haemodialysis.
对肾功能正常的对照受试者和处于透析间期的慢性肾衰竭患者口服单剂量索他洛尔(160毫克),以评估该药物的消除动力学。采用改良的加勒特和施内尔(1971年)方法通过荧光法测量体液中的索他洛尔浓度。正常受试者的平均血浆半衰期(T 1/2)约为5小时,未透析患者为42小时。血液透析期间,平均血浆半衰期平均为7小时。患者组药物的累积尿排泄量显著较低:48小时内为剂量的9%,而正常人为61%。血浆中索他洛尔浓度与肾性肾病超滤液的比较表明,该药物在体内与血浆蛋白的结合在肾性患者中可忽略不计。6至7小时的血液透析对血浆浓度衰减线的净降低作用为20%。透析后血浆浓度数据表明,索他洛尔从身体组织返回血浆的速率似乎是血液透析消除索他洛尔的速率控制因素。