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達格列淨

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達格列淨
Haworth projection (bottom)
臨床資料
讀音/ˌdæpəɡlɪˈfloʊzɪn/ DAP-ə-glif-LOH-zin
商品名Forxiga, Farxiga, others
其他名稱BMS-512148; (1S)-1,5-anhydro-1-C4-chloro-3-[(4-ethoxyphenyl)methyl]phenylD-glucitol
AHFS/Drugs.comMonograph
核准狀況
懷孕分級
給藥途徑口服（錠劑）
藥物類別SGLT2抑制劑
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度78%（投予10毫克劑量後）
血漿蛋白結合率~91%
藥物代謝UGT1A9（主要）、CYP（次要）
代謝產物Dapagliflozin 3-O-glucuronide（非活性）
生物半衰期~12.9 小時
排泄途徑尿 (75%)、糞 (21%)[2]
識別資訊
  • (2S,3R,4R,5S,6R)-2-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
CAS號461432-26-8  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.167.331 編輯維基數據鏈接
化學資訊
化學式C21H25ClO6
摩爾質量408.873
3D模型（JSmol）
  • Clc1ccc(cc1Cc2ccc(OCC)cc2)[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O
  • InChI=1S/C21H25ClO6/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1 checkY
  • Key:JVHXJTBJCFBINQ-ADAARDCZSA-N checkY

達格列淨（英語：Dapagliflozin，中文品牌名：安達唐(大陸地區)、福適佳(台灣地區)， 英文品牌名： Forxiga ）， 由阿斯利康研發，是第一種獲批的SGLT2抑制劑，歐盟在2011年首先批准了此藥物。2014年FDA批准其在美國銷售。[3] 達格列淨於2017年獲得中國食品和藥品監督管理總局批准，用於2型糖尿病成人患者改善其血糖控制。[4]

醫療用途

[編輯]

達格列淨可配合飲食和運動單藥治療，或和其他降糖藥物連用。來改善二型糖尿病成人患者的血糖控制。研究表明，非糖尿病和二型糖尿病成年患者，當在現有治療方案中加入達格列淨或其他SGLT2抑制劑時，能夠減緩腎小球濾過率下降和腎衰竭的進程。[5][6][7][8]

歐洲心臟病學會和美國心臟協會的治療指南，認為SGLT2抑制劑可以作為射血分數降低（LVEF < 40%）[[心力衰竭]]患者的標準療法。[9][10]這得到了兩項大型隨機對照試驗[11][12]以及2023年的一項系統性回顧和薈萃分析的支持。[13]

多項研究證據表明，在標準心力衰竭治療中加入達格列淨及其他SGLT2抑制劑類藥物，無論患者是否患有糖尿病，均可降低心力衰竭惡化、因心力衰竭住院以及心血管死亡的風險。[14][11][12][13][15][16]這些研究主要招募射血分數降低（LVEF < 40%）的患者。但是新的研究也表明，該藥物對射血分數輕度降低或保留的患者也可能有一些益處。[17]SGLT2抑制劑能夠降低因心血管疾病死亡，或心力衰竭住院和緊急就診的風險。[18][19]一些薈萃分析和隊列研究顯示，在降低特定心力衰竭患者的住院風險上，達格列淨可能比恩格列淨等同類藥物效果更好。然而，目前研究的結論尚不統一，仍需進一步的比較研究證實。[11][16][20]

達格列淨不能用於治療一型糖尿病，藥品上市許可持有人撤回了本藥在一型糖尿病的適應症。[21]和糖尿病酮症酸中毒，因為會增加中毒的風險。[22]

對於非糖尿病性慢性腎臟病

[編輯]

2021年，FDA和EMA擴展了達格列淨的適應症，批准其用於治療患有慢性腎病但無糖尿病的患者。[23][24]

試驗證實了該療法具有以下效果：

DIAMOND 試驗的結果顯示，在六周的治療期間中患者的蛋白尿沒有改善。腎小球濾過率顯著惡化，在停藥後六周通常可逆。患者的體重降低了1.5公斤。[25][26]

DAPA-CKD 顯示，在已經接受血管緊張素轉換酶抑制劑（ACEI）或血管緊張素受體阻滯劑（ARBs）治療的患者的中位治療期 2.4 年中，治療組比安慰劑組晚 8 個月左右出現腎臟濾過率持續下降、腎衰竭或死亡事件。然而，在治療的前12至16個月期間，治療組的腎臟濾過率低於安慰劑組，之後，其下降速度才開始略慢於安慰劑組。[6][26]

副作用

[編輯]

由於達格列淨導致嚴重的糖尿（有時每天約70克），因此可能導致體重迅速減輕和疲倦。 葡萄糖起滲透性利尿劑的作用（這種作用是糖尿病多尿的原因），可導致脫水。 尿液中葡萄糖含量的增加也可能使已經與糖尿病相關的感染惡化，特別是尿路感染及鵝口瘡（念珠菌病）。 極少數情況下，使用SGLT2藥物（包括達格列淨）與會陰壞死性筋膜炎（也稱為Fournier壞疽）有關。[27]

達格列淨也與低血壓反應有關。 人們擔心它可能會增加糖尿病酮症酸中毒的風險。[28]

參考

[編輯]
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