Pharmacokinetics and pharmacodynamics of the new oral anticoagulants

Baines, Juan Pablo Ordovás; Grana, Eduardo Climent; Botella, Alejandro Jover; García, Isabel Valero

doi:10.1016/s2173-5085(09)70078-4

Cited by 3 publications

(4 citation statements)

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“…The current antithrombotic agents used in clinical practice include (1) parenteral drugs such as unfractionated heparin, low‐molecular‐weight heparins, the derivative synthetic pentasaccharide fondaparinux, and the direct thrombin inhibitors lepirudin and bivalirudin; and (2) oral anticoagulants such as warfarin and acenocoumarol, or even antiaggregation agents such as acetylsalicylic acid or clopidogrel [13–15]. However, there are some important disadvantages to these therapies: heparin must be administered parenterally and requires strict laboratory monitoring of activated partial thromboplastin time.…”

Section: Importance Of Atrial Fibrillation (Af) and Anticoagulationmentioning

confidence: 99%

“…The bioavailability of dabigatran is low. In healthy patients, it is between 5 and 7%, and the time necessary to reach the maximum concentration of the drug in the blood is between 0.5 and 2 h [14,23,24]. Increases in the dosage lead to proportional increases in the maximum concentration and the area under the curve [23].…”

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

“…In patients with creatinine clearance of 30–50 mL/min, there is a 2.7‐fold increase in the area under the curve for dabigatran after oral administration and 6‐fold when creatinine clearance is 10–30 mL/min. However, no changes in dabigatran exposure have been observed in patients with moderate hepatic insufficiency (Child Pugh B) [14,21].…”

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

“…Because strong P‐glycoprotein inhibitors such as verapamil or clarithromycin may interfere with dabigatran, physicians should exercise great caution if administering these drugs. Importantly, the P‐glycoprotein inhibitor quinidine is contraindicated [14,21]. Table 1 summarizes the most important pharmacokinetic and pharmacodynamic properties of dabigatran.…”

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

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REVIEW: Atrial Fibrillation and Dabigatran: Has the Time Come To Use New Anticoagulants?

Escobar

Barrios

Jiménez

2010

Cardiovascular Therapeutics

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SUMMARYAtrial fibrillation (AF) is the most common sustained cardiac rhythm disturbance found in clinical practice, increasing in prevalence with age. AF is often associated with structural heart disease, although a significant proportion has no detectable heart disease. In the last 2 decades, there has been an increase of 66% in hospitalizations for AF, and it is an extremely costly public health problem. AF is associated with an increased long-term risk of stroke, heart failure, and all-cause mortality. In fact, the mortality rate in patients with AF is about double that of patients in normal sinus rhythm. Antithrombotic therapy is recommended for all patients with AF to prevent thromboembolism, except those with lone AF or contraindications. Selection of the antithrombotic agent should be based upon the absolute risks of stroke and bleeding and the relative risk and benefit for a given patient. However, despite oral anticoagulation with vitamin K antagonists (warfarin or acenocoumarol) some patients still have thromboembolic events. Furthermore, for the majority of patients, international normalized ratio (INR) monitoring may be an inconvenience. This is why new anticoagulants, such as the direct thrombin inhibitors, are being investigated. The results of the RE-LY trial have recently been published. In this study, in a population of patients with AF, dabigatran at 110 mg b.i.d was associated with stroke and systemic embolism rates similar to those associated with warfarin, and with lower rates of major hemorrhage. However, when dabigatran was administered at a dose of 150 mg, lower rates of stroke and systemic embolism and similar rates of major hemorrhage were found compared with warfarin. The aim of this review is to update information on the prevention of thromboembolic events in patients with AF and how dabigatran may change daily clinical practice. Importance of Atrial Fibrillation (AF) and AnticoagulationAF is the most common arrhythmia in clinical practice [1]. It has been estimated that 4.5 million in the European Union and 2.2 million people in the United States have paroxysmal or persistent AF [2]. In the last 2 decades, there has been an increase of 66% in hospitalizations for AF. This is most likely a consequence of the aging of the population and improved treatments for acute cardiac syndromes, which have the secondary effect of increasing the prevalence of chronic cardiac disorders [2,3]. This makes AF an extremely costly public health problem. In fact, it has been calculated that, globally, the annual cost per patient is close to €3000(US$3600) [4,5].The prevalence of AF has been estimated to range from 0.4 to 1% in the general population, increasing with age [6]. In patients over 80, the prevalence rises to 8% [7]. As a result, the median age of AF patients is about 75 years. The incidence of AF increases from <0.1% per year in those under 40 to 2% per year in men and 1.5% in women in those >80 [8].However, these figures would not be clinically relevant if it were not for the fact that AF is ...

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Section: Importance Of Atrial Fibrillation (Af) and Anticoagulationmentioning

confidence: 99%

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

Section: Pharmacokinetics and Pharmacodynamics Of Dabigatranmentioning

confidence: 99%

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