达比加群
拜瑞妥
医学
重症监护医学
抗凝剂
直接凝血酶抑制剂
药品
直接凝血酶抑制剂的发现与发展
凝血酶原复合物浓缩物
华法林
凝血酶
药理学
心房颤动
内科学
血小板
摘要
Summary Orally active small molecules that selectively and specifically inhibit coagulation serine proteases have been developed for clinical use. For some patients these oral direct inhibitors ( ODI s) offer substantial benefits over oral vitamin K antagonists ( VKA ). However, for the majority of patients with good anticoagulant control with VKA s the advantages of the ODI s are primarily convenience and few drug interactions. The drugs are prescribed at fixed dose without the need for monitoring or dose adjustment in the majority of patients and the rapid onset of anticoagulation and short half‐life make initiation and interruption of anticoagulation considerably easier than with VKA s. As yet, specific antidotes to ODI s are not available for clinical use but these are in development as rapid reversal agents. As with all anticoagulants produced so far, there is a correlation between intensity of anticoagulation and bleeding. Consequently, the need to consider the balance of benefit and risk in each individual patient is no less important than with VKA therapy. Dabigatran and rivaroxaban have been chosen for this review as examples of a thrombin inhibitor and an inhibitor of factor X a respectively. The clinical application of these drugs is the focus of the review.
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