ダビガトランエテキシラート 化学特性,用途語,生産方法
用途
ダビガトランエテキシラート（Dabigatran etexilate）は、直接トロンビン阻害剤（英語版）に属する経口抗凝固薬である。
日本での効能?効果は、「非弁膜症性心房細動患者における虚血性脳卒中および全身性塞栓症の発症抑制」である。海外では非経口的に5?10日間の低分子ヘパリン投与を受けた後の患者の深部静脈血栓症（DVT）や肺塞栓症（PE）の治療や予防にも使用される。
効能
抗凝固薬, トロンビン阻害薬
説明
Dabigatran etexilate is an orally administered pro-drug of dabigatran,
which is a direct inhibitor of thrombin and a potent anticoagulant. The serine protease thrombin is the final mediator in the coagulation cascade
that leads to the production of fibrin, the main protein component of
blood clots. Thrombin is also a potent activator of platelets. Consequently, thrombin inhibitors have found utility as anticoagulants in
treating arterial and venous thrombosis.
Warfarin, although orally available, has a
narrow therapeutic index and requires frequent monitoring and dosage
adjustment. Low-molecular-weight heparins provide better safety profile
and less inter-patient variability; however, these agents are only available
for parenteral administration. Direct thrombin inhibitors (DTIs) are a
new class of anticoagulants that act by directly binding to thrombin at its
catalytic or fibrinogen-binding sites, or both. Unlike the heparins, DTIs do not require the activation of secondary factors such as antithrombin to derive their activity, which makes their action more predictable. In addition, their ability to inhibit both free and clot-bound thrombin predisposes them for enhanced anticoagulation effect.
使用
Dabigatran Etexilate is an oral anticoagulant and direct thrombin inhibitor.
定義
ChEBI: An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-{N'-[(hexyloxy)carbonyl]carbamimidoyl}phenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amino group of
thyl N-pyridin-2-yl-beta-alaninate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.
ダビガトランエテキシラート 上流と下流の製品情報
原材料
準備製品