New Anticoagulants in Atrial Fibrillation

被引:19
作者
Harenberg, Job [1 ]
机构
[1] Heidelberg Univ, Fac Med Mannheim, D-68169 Mannheim, Germany
关键词
Atrial fibrillation; oral anticoagulants; idraparinux; oral factor Xa inhibitor; oral thrombin inhibitor; FACTOR XA INHIBITOR; DIRECT THROMBIN INHIBITOR; DEEP-VEIN THROMBOSIS; ORAL DIRECT THROMBIN; ANTITHROMBOTIC THERAPY; VENOUS THROMBOEMBOLISM; STROKE PREVENTION; IDRAPARINUX; WARFARIN; XIMELAGATRAN;
D O I
10.1055/s-0029-1240018
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Atrial fibrillation (AF) requires anticoagulation for prevention of arterial embolism, especially in the presence of defined risk factors summarized in the CHADS(2) score (congestive heart disease, hypertension, age >75 years, diabetes, history of ischemic stroke or transient cerebral ischemia). Vitamin K antagonists as drugs of choice have several limitations. International normalized ratio (INR) adjustment to 2.0 to 3.0 may be difficult to maintain, and doses vary widely between patients. Inherited variations of the vitamin K epoxide reductase C1 enzyme and of the cytochrome P450 2C9 system influence the dosage as well as exogenous factors such as food and drug intake or intercurrent diseases. Increasing age and risk of falling are the main factors behind the underuse of anticoagulation in AF. Anticoagulants with a lack of all or most of these characteristics and without need of regular monitoring for dose adjustment may improve the adherence to the indication for anticoagulation. Indirect systemic and oral direct factor Xa and oral direct thrombin inhibitors are currently being developed for the prevention of embolism in patients with AF.
引用
收藏
页码:574 / 585
页数:12
相关论文
共 60 条
[41]   Hepatic findings in long-term clinical trials of ximelagatran [J].
Lee, WM ;
Larrey, D ;
Olsson, R ;
Lewis, JH ;
Keisu, M ;
Auclert, L ;
Sheth, S .
DRUG SAFETY, 2005, 28 (04) :351-370
[42]   Pharmacology and clinical potential of direct thrombin inhibitors [J].
Linkins, LA ;
Weitz, JI .
CURRENT PHARMACEUTICAL DESIGN, 2005, 11 (30) :3877-3884
[43]  
Ma Q, 2004, IDRUGS, V7, P1028
[44]  
Pengo V, 2001, THROMB HAEMOSTASIS, V85, P418
[45]   Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa [J].
Pinto, Donald J. P. ;
Orwat, Michael J. ;
Koch, Stephanie ;
Rossi, Karen A. ;
Alexander, Richard S. ;
Smallwood, Angela ;
Wong, Pancras C. ;
Rendina, Alan R. ;
Luettgen, Joseph M. ;
Knabb, Robert M. ;
He, Kan ;
Xin, Baomin ;
Wexler, Ruth R. ;
Lam, Patrick Y. S. .
JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (22) :5339-5356
[46]   Apixaban Metabolism and Pharmacokinetics after Oral Administration to Humans [J].
Raghavan, Nirmala ;
Frost, Charles E. ;
Yu, Zhigang ;
He, Kan ;
Zhang, Haiying ;
Humphreys, W. Griffith ;
Pinto, Donald ;
Chen, Shiangyuan ;
Bonacorsi, Samuel ;
Wong, Pancras C. ;
Zhang, Donglu .
DRUG METABOLISM AND DISPOSITION, 2009, 37 (01) :74-81
[47]   Small molecule coagulation cascade inhibitors in the clinic [J].
Saiah, E ;
Soares, C .
CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2005, 5 (16) :1677-1695
[48]   Reversible biotinylated oligosaccharides: a new approach for a better management of anticoagulant therapy [J].
Savi, P. ;
Herault, J. P. ;
Duchaussoy, P. ;
Millet, L. ;
Schaeffer, P. ;
Petitou, M. ;
Bono, F. ;
Herbert, J. M. .
JOURNAL OF THROMBOSIS AND HAEMOSTASIS, 2008, 6 (10) :1697-1706
[49]   Hemorrhagic complications of anticoagulant and thrombolytic treatment [J].
Schulman, Sam ;
Beyth, Rebecca J. ;
Kearon, Clive ;
Levine, Mark N. .
CHEST, 2008, 133 (06) :257S-298S
[50]   Antithrombotic therapy in atrial fibrillation [J].
Singer, Daniel E. ;
Albers, Gregory W. ;
Dalen, James E. ;
Fang, Margaret C. ;
Go, Alan S. ;
Halperin, Jonathan L. ;
Lip, Gregory Y. H. ;
Manning, Warren J. .
CHEST, 2008, 133 (06) :546S-592S