慢性腎病可使用, 需減量.
副作用~~ 震顫、頭痛、頭暈、噁心、低血糖。
Vildagliptin 不經 cytochrome(CYP)P450 代謝. 不會改變 CYP450酵素活性.
Vildagliptin (Galvus) 屬於DPP4i , 吸收快速, 服用之後 1.1 小時到達最大血中濃度
Vildagliptin is absorbed quickly (85.4% of the drug). The maximum plasma level is detected at 1.1-h post dose.
藥物在血中的濃度, 原型藥 25.7%, 代謝產物 M20.7=55%半衰期 2.8 小時,
85% 經尿液排出, 22.6% 以原型藥排出, 其他是不具生理活性的代謝物. 15% 從糞便排出 (4.54% 是原型藥)
Vildagliptin 主要代謝途徑是透過羧化作用 (carboxylation), 產生具生理活性的代謝物 M20.7, 主要是藉由 DPP-4 轉化. 其他代謝物則不具生理活性.
Plasma radioactivity (after the administration of radioactive labeled drug) due to vildagliptin is 25.7% and to its major metabolite M20.7 is 55%. The half- life of vildagliptin is 2.8 h. Eighty-five percent of the drug is excreted in the urine (22.6% as vildagliptin the rest as inactive metabolites) and the remaining 15% in feces (4.54% as vildagliptin). In humans, the main pathway of metabolism of the drug is carboxylation, which results in the form of the active metabolite M20.7. DPP-4 contributes to formation of this metabolite. Other minor metabolites are: M15.3, which results from hydrolysis of amide bonds, M20.2 from glucuronidation of the pyrrolidine ring and M20.9, M21.6 from oxidation of the pyrrolidine ring. All these metabolites are inactive[27].
Vildagliptin 在很多組織或器官內, 經水解作用代謝, 對於各階段的第二型DM合併慢性腎病患者, 因腎臟在排除藥物僅是一個小角色, 無法準確預測病患體內 vildagliptin 濃度.
Hydrolysis takes place in multiple tissues or organs. Exposure to vildagliptin in subjects with type 2 diabetes and renal disease of various stages cannot be accurately predicted because the kidneys play a small role in the removal of the drug while participating in metabolism via hydrolysis[28].
第一階段和第二階段的慢性腎病患者 (eGFR>50), 不需調整劑量. 50 mg bid
In diabetic subjects with chronic kidney disease stage 1 or 2 (eGFR > 50 mL/min per 1.73 m2), dose adjustment of vildagliptin is not required.
第三階慢性腎病患者, 經由腎臟排除 vildagliptin 及其活性代謝物 M20.7 會減少, 所以需降低劑量
eGFR < 50 劑量 50mg qd.
In patients with chronic kidney disease stage ≥ 3, both vildagliptin and its active metabolite M20.7 are less excreted via the kidneys. In these patients a dose adjustment is required. (When eGFR is < 50 mg/mL per 1.73 m2 the dose is 50 mg × 1).
沒有留言:
張貼留言