Atrial Fibrillation (AFib) Support Group
Atrial fibrillation (AF or afib) is an abnormal heart rhythm (cardiac arrhythmia) which involves the two small, upper heart chambers (the atria). Heart beats in a normal heart begin after electricity generated in the atria by the sinoatrial node spread through the heart and cause contraction of the heart muscle and pumping of blood.
I have been "lurking" on this board for a year and a half - when I was first diagnosed with AFIB. I am fortunate to be permanent/persistent and asymptomatic so AFIB doesn't bother me much at this point in time. I am currently on Lisinopril, Metoprolol, Diltiazem and Warfarin which do a pretty good job of keeping my heart rate down.
I want to get off the Warfarin and have hesitated to try Pradaxa or Xeralto. There is a new drug which was just approved for AFIB in January. It is called Eliquis (see link). Has anyone had any early experience with this new drug.
http://www.eliquis.com/index.aspx
I want to get off the Warfarin and have hesitated to try Pradaxa or Xeralto. There is a new drug which was just approved for AFIB in January. It is called Eliquis (see link). Has anyone had any early experience with this new drug.
http://www.eliquis.com/index.aspx
[New anticoagulants - direct factor Xa-inhibitors]. [Review] [German]
Bachli E.
Therapeutische Umschau. 69(11):635-41, 2012 Nov.
[Comparative Study. English Abstract. Journal Article. Review]
UI: 23117666
Authors Full Name
Bachli, E.
AB The direct oral factor Xa-inhibitors are at present in clinical use as antithrombotics, after their efficiency and safety have been proved in clinical studies. Three products are actually in the market, rivaroxaban (Xarelto) apixaban (Eliquis) and edoxaban (Lixiana). Efficacy and safety have been tested for rivaroxaban and apixaban in large study programmes with more than 60'000 patients each. For edoxaban large phase III studies are under way. Based on these data rivaroxaban was registered in the EU and CH for primary prophylaxis against thrombosis after major orthopaedic surgery, such as hip- and knee-joint protheses, for treatment and prophylaxis of deep vein thrombosis and pulmonary embolism and for prophylaxis against thromboembolic stroke in patients with atrial fibrillation. Apixaban is presently registered in the EU and CH for prophylaxis against thrombosis after major orthopaedic surgery, Edoxaban is registered only in Japan for the same indication. These products have been shown to be non-inferior or superior compared with vitamin K antagonists or low-molecular weight heparins, they are administered once or twice a day, they do not need laboratory monitoring. But they have disadvantages also, they depend on renal clearance, they can interact with other medicaments and they lack a specific antidote. In total, though, they are considered as a progress for the appropriate patients in terms of quality of treatment.
Apixaban: a new player in the anticoagulant class. [Review]
Agrawal R. Jain P. Dikshit SN.
Current Drug Targets. 13(6):863-75, 2012 Jun.
[Comparative Study. Journal Article. Review]
UI: 22250655
Authors Full Name
Agrawal, Ritesh. Jain, Pratima. Dikshit, S N.
AB Apixaban (BMS-562247-01) is a compound being investigated as an anticoagulant. Apixaban molecule is developed in a joint venture by Pfizer and Bristol-Myers Squibb. Apixaban, a coagulation factor Xa inhibitor, approved in the E.U. in 2011 for the prevention of venous thromboembolic events in adult patients, who have undergone elective hip or knee replacement. The Apixaban based drug will be marketed under the brand name Eliquis and is expected to rack up annual sales of over $2.5 billion. Apixaban is expected to provide stiff competition to warfarin, a popular blood thinner used in Europe. Warfarin is known to cause some serious side effects in patients. Apixaban, as compared with aspirin, reduced the risk of stroke or systemic embolism in patients experiencing atrial fibrillation by more than 50% (from 3.7% per annum with aspirin to 1.6% per annum with apixaban). Apixaban exhibits superiority to enoxaparin in preventing thrombosis in patients undergoing elective hip replacement surgery with similar bleeding rates. Apixaban is a highly selective and potent Factor Xa Inhibitor with Ki=0 8nM to both free as well as prothrombinase bound FXa. In X-ray crystal structure studies indicate that the pyrazole N-2 nitrogen atom interacts with backbone of Gln192 and the carbonyl oxygen of carboxamide interacts with NH of Gly216. The orientation of phenyllactum in the S4 region indiacates an edge to face interaction with Trp215, which is positioned between the Tyr99 and Phe174. In the present review, we have tried to cover comparative study of various FXa-inhibitors and point out apixaban in the various aspect including molecular chemistry, physical properties, commercial synthesis, current patent status, crystalline polymorphic forms, molecular receptor interaction, pharmacophore rational, mechanism of action, clinical studies, preclinical, adverse effect, available formulation, dose regimen and co-therapy, thus giving emphasis on medicinal chemistry aspects.