氟卡尼的新陈代谢。
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康纳德GJ,欧博再保险
氟卡尼的新陈代谢。
心功能杂志。1984年2月27日,53 (5):41 b-51b。0002 - 9149 . doi: 10.1016 / (84) 90501 - 0。
- PubMed ID
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6364769 (在PubMed]
- 文摘
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在健康人体,口服后吸收氟卡尼是提示(平均峰值水平在3 - 4小时),几乎完整的(至少90%);氟卡尼似乎并不接受间接presystemic生物转化。口服吸收心律失常患者,肾脏疾病和充血性心力衰竭(CHF)也是很好的。等离子体水平的氟卡尼是在治疗范围内与剂量成正比。既没有食物也没有抗酸剂影响氟卡尼吸收的程度。在健康受试者,不变氟卡尼的血浆半衰期相对较长(平均13小时后单剂和16小时后多个剂量)。患者心室过早复合物,半衰期较长(平均20小时),和每天口服剂量是有效的。氟卡尼消除的速率从等离子体在老年患者可能会减少。总的来说,等离子体的药物氟卡尼似乎合理的线性(不是剂量或浓度)。在人类,大多数(平均86%)的单剂量口服氟卡尼和其代谢物;随着尿液排出 only a small portion (mean 5%) is found in feces. Thus, flecainide does not appear to undergo extensive biliary excretion. A substantial portion (mean 27%) of a dose is excreted in urine as unchanged flecainide. Under alkaline urinary conditions, flecainide elimination may be decreased. Only 2 major and 2 or 3 minor metabolites are found in human urine. The 2 major urinary metabolites possess little or no detectable antiarrhythmic activity and are also the major metabolites present in human plasma (primarily conjugated); since free metabolite levels are very low in plasma, metabolites are not likely to contribute any consequential pharmacologic activity. The rate of flecainide elimination from plasma is somewhat slower in patients with moderate renal failure and in patients with CHF than that for healthy persons, and is markedly slower in some patients with end-stage renal disease. Urinary excretion of unchanged flecainide is somewhat less in moderate renal patients and is markedly less in end-stage renal patients, but is not altered in CHF patients. Dosage should be reduced in patients with more severe renal disease and, if indicated, in some CHF patients. Hemodialysis is not an effective means for removal of unchanged flecainide, but does provide more substantial removal of metabolites. Flecainide is not extensively bound (mean 40%) to human plasma proteins in vitro and binding is independent of total drug level.(ABSTRACT TRUNCATED AT 400 WORDS)
