Shanghai Jiaotong University School of Medicine
Affiliated to the Ninth People's Hospital Huangpu Branch
Liu Min
recommended anticoagulants include warfarin and heparin in textbooks, as well as thrombin inhibitors and PAR-1 antagonist , etc., the anticoagulant drug family continues to grow. If warfarin is the "old senior" in the anticoagulant family, then the new oral anticoagulant dabigatran ester is one of the "newcomers" in the anticoagulant family. Today, the editor will take you to unveil the mystery of this "newcomers" and see its "predecessors".
dabigatran ester is a new anticoagulant drug developed by German Boehringer Ingelheim . It was first launched in the UK and Germany in 2008. It was approved by the US FDA in October 2010 and approved by the CFDA (China Food and Drug Administration) in February 2013, and officially entered the Chinese market. What is the mechanism of action of
dabigatran ester?
dabigatran ester is an oral thrombin inhibitor that can be converted into active dabigatran in the body and plays a role. It can bind to the activation site of thrombin to inhibit thrombin, and the process of converting fibrinogen into fibrin is inhibited. At the same time, activation factors (FVa, FVIIIa, FIXa, FXIIIa), as well as platelet kinase activation receptors are also inhibited, thereby blocking the final step of the coagulation waterfall grid and thrombosis. Its anticoagulation process does not require cofactors and is not related to vitamin K. What should I pay attention to when taking dabigatran ester? The indications of
dabigatran ester are very widespread, especially in patients with nonvalvular atrial fibrillation and ischemic stroke. As a "upstart", dabigatran ester is not picky about food and has no food taboos. However, you should pay attention to the following points when taking the medicine: First, it is best to swallow the whole tablet when eating, and never bite or chew it, because the capsule is broken or opened and then taken orally, the risk of bleeding will increase significantly; Second, if missed, if missed, if the next time you take the medicine, you can take it again. Otherwise, you need to wait until the next time to take the medicine again, and try to avoid missed medication; Third, you should pay attention to amiodarone and azole antifungal drugs that can increase their blood concentration, and the contrary, if you need to avoid taking the medicine by Chinese herbal medicine, you should avoid taking St. John's Wort, but there are currently no other Chinese herbal medicines found to have an impact on it. What should I do if there is adverse reactions in
? About 10% of patients will experience stomach discomfort when they start taking
, which will often relieve themselves after a few days. Taking Chinese medicine can reduce the incidence of stomach discomfort; patients with non-fatal bleeding should be closely observed in addition to local hemostasis measures. If necessary, oral activated carbon can be taken to reduce drug absorption and diuretics can be used to promote excretion. How should I take
in special circumstances?
high-risk stroke (CHADS2 at least 3 points) or atrial fibrillation patients with a history of stroke can use dabigatran ester 150 mg twice a day. For patients with high-risk bleeding, 110 mg twice a day; if the teeth are washed or removed, tranexamic acid can be used before and after the operation, or the day before the operation can be stopped, and it is only necessary to resume use on the same night after the operation; it is not recommended during pregnancy, and women of childbearing age who plan to be pregnant should not take it; for patients with renal insufficiency, creatinine clearance (Ccr) 50 mL/min, 150 mg or 110 mg twice a day, and Ccr is reviewed every 12 months; when Ccr is between 30 and 50 mL/min, 110 mg or 150 mg twice a day, and Ccr is reviewed every 6 months; Ccr30 When mL/min, try not to use it.
In general, dabigatran ester, as the first new oral anticoagulant approved by the FDA in more than 50 years after warfarin, has become a major breakthrough in the field of anticoagulation due to its oral administration, strong, no special drug monitoring, and few drug interactions. However, its disadvantages are also obvious, such as the lack of specific antigens and the lack of effective laboratory methods to evaluate the anticoagulant effect, serious complications may occur after a short half-life missed use, because 85% of it is excreted by the kidneys, renal function needs to be checked every 6 to 12 months, and it is also expensive.As an anticoagulant drug "update",
dabigatran ester is indeed a bit "expensive". Its price discourages many patients. The good news is that it has been included in the national medical insurance catalog in 2017, reducing the burden on patients. At present, dabigatran ester has passed the patent protection period, and generic drugs will be released soon, so that the "update" is not "expensive" and benefits the majority of patients.
■ China Pharmaceutical Industry Information Center compiled and edited by
(Specially supported by Shanghai Pharmaceutical Group)
The copyright of this article belongs to Shanghai Pharmaceutical News, and the pictures are from the Internet. Reprinting is welcome. Please indicate the source when reprinting.
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-