Dabigatran etexilate.
Dabigatran etexilate is an orally administered prodrug of dabigatran, which is a potent, concentration-dependent inhibitor of thrombus formation and thrombin-induced platelet aggregation. Dabigatran etexilate pharmacokinetics were linear across a wide dosage range. There were no clinically important pharmacokinetic interactions with digoxin (a P-glycoprotein substrate), pantoprazole (a proton-pump inhibitor) or drugs that are substrates and/or inhibitors of hepatic cytochrome P450 enzymes. In two large, randomized, double-blind trials of the prevention of venous thromboembolism (VTE) in patients undergoing total hip or total knee replacement surgery, orally administered dabigatran etexilate 220 mg/day was noninferior to subcutaneous enoxaparin sodium 40 mg/day for the primary composite endpoint of total VTE events or all-cause mortality during the treatment period. There were no significant differences between dabigatran etexilate and enoxaparin sodium in major VTE events and VTE-related mortality. Across trials, < or =0.5% of patients experienced a symptomatic pulmonary embolus or died. Dabigatran etexilate was generally well tolerated. In patients undergoing total hip or total knee replacement surgery, there was no significant difference between dabigatran etexilate and enoxaparin sodium recipients in the incidence of major or minor bleeding.
Sanford
Mark
M
Wolters Kluwer Health | Adis, Auckland, New Zealand, an editorial office of Wolters Kluwer Health, Conshohocken, Pennsylvania, USA. demail@adis.co.nz
Plosker
Greg L
GL
D000740:Anemia / Q000139:chemically induced; D000925:Anticoagulants / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019540:Area Under Curve; D001562:Benzimidazoles / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000069604:Dabigatran; D006207:Half-Life; D006470:Hemorrhage / Q000139:chemically induced; D006801:Humans; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects; D011355:Prodrugs; D011725:Pyridines / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D016032:Randomized Controlled Trials as Topic; D013492:Suppuration / Q000139:chemically induced; D013530:Surgical Wound Infection / Q000139:chemically induced; D013923:Thromboembolism / Q000188:drug therapy; D013927:Thrombosis / Q000188:drug therapy / Q000517:prevention & control; D016896:Treatment Outcome
D000925:Anticoagulants; D001562:Benzimidazoles; D011355:Prodrugs; D011725:Pyridines; D000069604:Dabigatran