Stamatakis G, Montes C, Trouvin J H, Farinotti R, Fessi H, Kenouch S, Méry J P
Nephrology Service, Hôpital Bichat, Paris, France.
Clin Nephrol. 1988 Oct;30(4):230-4.
Pharmacokinetics of pyrazinamide and its major metabolite, pyrazinoic acid, were assessed in 10 chronic uremic patients treated by maintenance hemodialysis in comparison with 10 normal subjects. All subjects ingested a single dose of 1 g of pyrazinamide, the patients receiving the drug immediately after the end of a dialysis session. Bioavailability of pyrazinamide was only slightly increased in patients, its dialysis extraction coefficient being 55.3%. In contrast, pyrazinoic acid has an elimination rate-dependent metabolism with a bioavailability markedly increased in patients and a dialysis extraction coefficient of 59.8%. These data may lead to recommendations of a reduction in the dosage of pyrazinamide in dialysis patients. However, administering the usual dosage of the drug at the end of each dialysis session seems preferable to the daily administration of a reduced dosage.
在10例接受维持性血液透析治疗的慢性尿毒症患者中评估了吡嗪酰胺及其主要代谢产物吡嗪酸的药代动力学，并与10名正常受试者进行了比较。所有受试者均单次口服1g吡嗪酰胺，患者在透析结束后立即服用该药物。吡嗪酰胺在患者中的生物利用度仅略有增加，其透析提取系数为55.3%。相比之下，吡嗪酸具有消除速率依赖性代谢，患者的生物利用度显著增加，透析提取系数为59.8%。这些数据可能会导致建议降低透析患者中吡嗪酰胺的剂量。然而，在每次透析结束时给予常规剂量的药物似乎比每日给予降低剂量更为可取。
