Dabigatran/Dabigatran etexilate

Sorbera, L. A.; Bozzo, J.; Castañer, J.

doi:10.1358/dof.2005.030.09.938760

Cited by 41 publications

(37 citation statements)

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“…All these agents are synthetic low-molecular-weight compounds that act as direct, selective and reversible inhibitors of a specific step in the coagulation cascade [41][42][43][44][45][46][47]. The anticoagulant effect of these agents is more predictable compared to that of heparin or vitamin K antagonists, allowing their administration in fixed doses without the need for laboratory monitoring or dose adjustment.…”

Section: Direct Oral Anticoagulantsmentioning

confidence: 99%

Anticoagulant treatment for acute pulmonary embolism: a pathophysiology-based clinical approach

Agnelli

Becattini

2015

Eur Respir J

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The management of patients with acute pulmonary embolism is made challenging by its wide spectrum of clinical presentation and outcome, which is mainly related to patient haemodynamic status and right ventricular overload. Mechanical embolic obstruction and neurohumorally mediated pulmonary vasoconstriction are responsible for right ventricular overload. The pathophysiology of acute pulmonary embolism is the basis for risk stratification of patients as being at high, intermediate and low risk of adverse outcomes. This risk stratification has been advocated to tailor clinical management according to the severity of pulmonary embolism.Anticoagulation is the mainstay of the treatment of acute pulmonary embolism. New direct oral anticoagulants, which are easier to use than conventional anticoagulants, have been compared with conventional anticoagulation in five randomised clinical trials including >11 000 patients with pulmonary embolism. Patients at high risk of pulmonary embolism (those with haemodynamic compromise) were excluded from these studies. Direct oral anticoagulants have been shown to be as effective and at least as safe as conventional anticoagulation in patients with pulmonary embolism without haemodynamic compromise, who are the majority of patients with this disease. Whether these agents are appropriate for the acute-phase treatment of patients at intermediate-high risk pulmonary embolism (those with both right ventricle dysfunction and injury) regardless of any risk stratification remains undefined. @ERSpublications New oral anticoagulants are efficacious and safe in haemodynamically stable patients with acute pulmonary embolism http://ow.ly/I2iP5

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Section: Direct Oral Anticoagulantsmentioning

confidence: 99%

Anticoagulant treatment for acute pulmonary embolism: a pathophysiology-based clinical approach

Agnelli

Becattini

2015

Eur Respir J

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“…Dabigatran etexilate is a synthetic low molecular weight peptidomimetic that binds directly and reversibly to the catalytic site of thrombin (5). Dabigatran etexilate is a prodrug that has ϳ6% bioavailability after oral administration.…”

Section: New Anticoagulants: General Pharmacologymentioning

confidence: 99%

“…Dabigatran is eliminated unchanged primarily by the kidneys; therefore plasma concentrations are increased in patients with moderately impaired renal function (creatinine clearance [CrCl] Ͻ50 ml/min). The therapeutic window, however, is fairly wide, and the drug has been tested in fixed doses in patients with CrCl Ͼ30 ml/min (5). Close clinical surveillance is recommended in patients with renal impairment.…”

Section: New Anticoagulants: General Pharmacologymentioning

confidence: 99%

New Oral Anticoagulants in Atrial Fibrillation and Acute Coronary Syndromes

Caterina

Husted

Wallentin

et al. 2012

Journal of the American College of Cardiology

246

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Until recently, vitamin K antagonists were the only available oral anticoagulants, but with numerous limitations that prompted the introduction of new oral anticoagulants targeting the single coagulation enzymes thrombin (dabigatran) or factor Xa (apixaban, rivaroxaban, and edoxaban) and given in fixed doses without coagulation monitoring. Here we review the pharmacology and the results of clinical trials with these new agents in stroke prevention in atrial fibrillation and secondary prevention after acute coronary syndromes, providing perspectives on their future incorporation into clinical practice. In phase III trials in atrial fibrillation, compared with warfarin, dabigatran etexilate 150 mg B.I.D. reduced the rates of stroke/systemic embolism without any difference in major bleeding; dabigatran etexilate 110 mg B.I.D. had similar efficacy with decreased bleeding; apixaban 5 mg B.I.D. reduced stroke, systemic embolism, and mortality as well as major bleeding; and rivaroxaban 20 mg Q.D. was noninferior to warfarin for stroke and systemic embolism without a difference in major bleeding. All these agents reduced intracranial hemorrhage. Edoxaban is currently being evaluated in a further large phase III trial. Apixaban and rivaroxaban were evaluated in phase III trials for prevention of recurrent ischemia in patients with acute coronary syndromes who were mostly receiving dual antiplatelet therapy, with conflicting results on efficacy but consistent results for increased major bleeding. Overall, the new oral anticoagulants are poised to replace vitamin K antagonists for many patients with atrial fibrillation and may have a role after acute coronary syndromes. Although convenient to administer and manage, they present challenges that need to be addressed.

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“…For in vivo studies we employed dabigatran etexilate, the oral prodrug of dabigatran. The prodrug does not have antithrombin activity; however, after oral administration dabigatran etexilate is rapidly converted by ubiquitous esterases to the active moiety, dabigatran (Sorbera et al, 2005, Wienen et al, 2007. Drugs administrated during the early phase of tissue injury act predominantly as anti-inflammatory agents and should be considered as "preventive treatment", whereas "true" antifibrotic agents might be effective irrespective of timing, particularly if administrated during the "fibrotic" or later phase of the model (Moeller et al, 2008).…”

Section: In Vivo Antifibrotic Effects Of Direct Thrombin Inhibition Wmentioning

confidence: 99%

Inhibition of Thrombin as a Novel Strategy in the Treatment of Scleroderma-Associated Interstitial Lung Disease

Bogatkevich¹,

Highland²,

Akter³

et al. 2012

Systemic Sclerosis - An Update on the Aberrant Immune System and Clinical Features

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Dabigatran/Dabigatran etexilate

Cited by 41 publications

References 0 publications

Anticoagulant treatment for acute pulmonary embolism: a pathophysiology-based clinical approach

Anticoagulant treatment for acute pulmonary embolism: a pathophysiology-based clinical approach

New Oral Anticoagulants in Atrial Fibrillation and Acute Coronary Syndromes

Inhibition of Thrombin as a Novel Strategy in the Treatment of Scleroderma-Associated Interstitial Lung Disease

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