This review discusses atrial fibrillation according to the guidelines of Brazilian Society of Cardiac Arrhythmias and the Brazilian Cardiogeriatrics Guidelines. We stress the thromboembolic burden of atrial fibrillati...This review discusses atrial fibrillation according to the guidelines of Brazilian Society of Cardiac Arrhythmias and the Brazilian Cardiogeriatrics Guidelines. We stress the thromboembolic burden of atrial fibrillation and discuss how to prevent it as well as the best way to conduct cases of atrial fibrillatios in the elderly, reverting the arrhythmia to sinus rhythm, or the option of heart rate control. The new methods to treat atrial fibrillation, such as radiofrequency ablation, new oral direct thrombin inhibitors and Xa factor inhibitors, as well as new antiarrhythmic drugs, are depicted.展开更多
Thrombin,the ultimate proteinase of the coagulation cascade,is an attractive target for the treatment of a variety of cardiovascular diseases.A bromophenol derivative named (+)-3-(2,3-dibromo-4,5-dihydroxy-phenyl)-4-b...Thrombin,the ultimate proteinase of the coagulation cascade,is an attractive target for the treatment of a variety of cardiovascular diseases.A bromophenol derivative named (+)-3-(2,3-dibromo-4,5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1,isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity.In this study,we investigated the inhibition of human thrombin in vitro with this bromophenol derivative,and its antithrombotic efficacy in vivo using the arteriovenous shunt model and the ferric chloride-induced arterial thrombosis model in rats.The results show that the bromophenol derivative is a potential inhibitor of thrombin (IC50=1.03 nmol/L).In antithrombotic experiments in vivo,the bromophenol derivative also shows good effect comparing with the control group.These data indicate that the bromophenol derivative is a potential drug for prophylaxis and the treatment of thrombotic diseases.展开更多
Argatroban is an intravenous DTI （direct synthetic thrombin inhibitor） that is not routinely used for anticoagulation; thus, expertise surrounding its use is very limited. Therefore, this case reviews an unusually h...Argatroban is an intravenous DTI （direct synthetic thrombin inhibitor） that is not routinely used for anticoagulation; thus, expertise surrounding its use is very limited. Therefore, this case reviews an unusually high argatroban infusion rate, which was needed to prevent further emboli formation in a patient. In this case, a 61-year-old Caucasian male patient exhibited heparin resistance during an intraoperative vascular procedure as measured by activated clotting time and PTT （partial thromboplastin time）. The patient had multiple occlusions in his right lower extremities and underwent embolectomies of the right popliteal and posterior tibial arteries. The clinical pharmacist was consulted to manage the argatroban infusion once heparin was discontinued. The therapeutic window required a PTr of 1.5-3 times the patient baseline （35-75 s）. The patient was reported to be 89 kg with a baseline PTT of 24.7 s and INR （international normalized ratio） of 0.98. The starting dose ofargatroban was initiated by the pharmacist at 2 mcg/kg/min （10.7 mL/h） as the patient did not have hepatic failure or sepsis. The patient was maintained on argatroban in the therapeutic PTT window for more than 72 h; however, frequent and aggressive dose increases, to a final rate of 7.5 mcg/kg/min （40 mL/h）, were needed to maintain the therapeutic PTT level. From the case, the cause of heparin resistance still has not been determined despite a hematologic work-up; however, this patient required an unusually high infusion rate of argatroban to maintain a therapeutic PTT during the hospital course before being changed to an anticoagulation regimen for discharge.展开更多
文摘This review discusses atrial fibrillation according to the guidelines of Brazilian Society of Cardiac Arrhythmias and the Brazilian Cardiogeriatrics Guidelines. We stress the thromboembolic burden of atrial fibrillation and discuss how to prevent it as well as the best way to conduct cases of atrial fibrillatios in the elderly, reverting the arrhythmia to sinus rhythm, or the option of heart rate control. The new methods to treat atrial fibrillation, such as radiofrequency ablation, new oral direct thrombin inhibitors and Xa factor inhibitors, as well as new antiarrhythmic drugs, are depicted.
基金Supported by the National High Technology Research and Development Program of China (863 Program) (No. 2007AA09Z410)the National Major Research Program of China "The Creation for Significant Innovative Drugs" (No. 2009ZX09103-148)
文摘Thrombin,the ultimate proteinase of the coagulation cascade,is an attractive target for the treatment of a variety of cardiovascular diseases.A bromophenol derivative named (+)-3-(2,3-dibromo-4,5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1,isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity.In this study,we investigated the inhibition of human thrombin in vitro with this bromophenol derivative,and its antithrombotic efficacy in vivo using the arteriovenous shunt model and the ferric chloride-induced arterial thrombosis model in rats.The results show that the bromophenol derivative is a potential inhibitor of thrombin (IC50=1.03 nmol/L).In antithrombotic experiments in vivo,the bromophenol derivative also shows good effect comparing with the control group.These data indicate that the bromophenol derivative is a potential drug for prophylaxis and the treatment of thrombotic diseases.
文摘Argatroban is an intravenous DTI （direct synthetic thrombin inhibitor） that is not routinely used for anticoagulation; thus, expertise surrounding its use is very limited. Therefore, this case reviews an unusually high argatroban infusion rate, which was needed to prevent further emboli formation in a patient. In this case, a 61-year-old Caucasian male patient exhibited heparin resistance during an intraoperative vascular procedure as measured by activated clotting time and PTT （partial thromboplastin time）. The patient had multiple occlusions in his right lower extremities and underwent embolectomies of the right popliteal and posterior tibial arteries. The clinical pharmacist was consulted to manage the argatroban infusion once heparin was discontinued. The therapeutic window required a PTr of 1.5-3 times the patient baseline （35-75 s）. The patient was reported to be 89 kg with a baseline PTT of 24.7 s and INR （international normalized ratio） of 0.98. The starting dose ofargatroban was initiated by the pharmacist at 2 mcg/kg/min （10.7 mL/h） as the patient did not have hepatic failure or sepsis. The patient was maintained on argatroban in the therapeutic PTT window for more than 72 h; however, frequent and aggressive dose increases, to a final rate of 7.5 mcg/kg/min （40 mL/h）, were needed to maintain the therapeutic PTT level. From the case, the cause of heparin resistance still has not been determined despite a hematologic work-up; however, this patient required an unusually high infusion rate of argatroban to maintain a therapeutic PTT during the hospital course before being changed to an anticoagulation regimen for discharge.
