Pharmacokinetics of an emerging new class of anticoagulant/antithrombotic drugs. A review of small-molecule thrombin inhibitors.

摘要: Small-molecule direct thrombin inhibitors represent a new class of anticoagulants and are emerging as antithrombotic drugs with range indications. The tripeptide type or peptidomimetic compounds, including argatroban, efegatran, inogatran napsagatran, hitherto clinically studied first generation that pharmacokinetically characterised by relatively rapid hepato-biliary clearance short half-lives necessitating their administration intravenous infusion. They not orally bioavailable because poor enteral absorption presystemic hepatic extraction. Melagatran can be administered subcutaneously, prodrug form melagatran, ximelagatran, is at present the only oral inhibitor available. Direct produce predictable, stable rapidly reversible anticoagulation measurable common coagulation assays. Significant pharmacokinetic drug-drug interactions have been reported. Possible pharmacodynamic interactions, in terms prolongation plasma clotting times, other anticoagulant must taken into account when monitoring using