第一階及第二階慢性腎病不用減量
第三階以上需減量
第三階慢性腎病 eGFR < 30, 劑量 2.5 mg QD.
第四階與第五階或洗腎患者, 劑量 2.5 mg qd.
Saxagliptin (Onglyza)主要是在肝臟透過 cytochrome P450 3A4/5 (CYP3A4/5) 代謝, 主要代謝物有生理活性, 強度是原型藥物的一半.
Saxagliptin is primarily hepatic metabolized by the cytochrome P450 3A4/5 (CYP3A4/5). The major metabolite of this drug is also active as also a DPP-4 inhibitor, and retains half of the potency of parent drug.
其他經由 cytochrome P450 3A4/5 (CYP3A4/5) 代謝的藥物, 可能會影響 saxagliptin 及其活性代謝物的藥物代謝動力學, 24% 以原型藥物從尿液排出, 36% 以活性代謝物從尿液排出, 腎臟也有一些分泌功能可將 saxagliptin 排出體外. 相當大的一部分 (超過20%) 從糞便排出, 包括膽汁排出及沒有被吸收入體內的原型藥.
All the drugs, which are also metabolized in this cytochrome CYP3A4/5, may alter the pharmacokinetics of the drug and its active metabolite. Twenty-four percent of the drug is excreted in the urine as saxagliptin and 36% as its active metabolite. There is also some active renal excretion of the drug. A significant part (more than 20%) can be found in the feces as a sum of excreted in bile drug and unabsorbed drug[29].
第一階及第二階的慢性腎病患者, 血中saxagliptin 及活性代謝物濃度會增加, 但臨床效果不顯著, 所以不用調整劑量.
In diabetic patients with chronic kidney disease stages 1 and 2 increased concentration of saxagliptin and its active metabolite remains clinically irrelevant and no dose adjustment is needed.
第三階慢性腎病建議減一半劑量 2.5 mg qd, 使血中濃度與腎功能正常的人相近
末期腎病包括洗腎患者也是 2.5 mg qd.
In diabetic subjects with chronic kidney disease stages ≥ 3 half dose is recommended (2.5 mg × 1 daily) to achieve the same plasma concentrations compared to subjects with normal renal function. The same dose is recommended in patients with end-stage renal disease (requiring hemodialysis).
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