Bivalirudin

Bivalirudin 화학적 특성, 용도, 생산

• 개요

  Bivalirudin was launched in New Zealand as an anticoagulant for i.v. treatment of patients with unstable angina undergoing percutaneous transluminal coronary angioplasty. Bivalirubin is a synthetic 20 amino acid peptide rationally modeled on hirudin (residues 53- 64), the most potent and specific naturally-occuring known inhibitor of thrombin, the enzyme that plays a key role in hemostasis and blood clot formation. This peptide is a direct thrombin inhibitor that maintains the unique bivalent binding properties of hirudin to the catalytic site and to the fibrin-recognition exosite of the enzyme, so acting directly on thrombin with high affinity and specificity. In vitro studies demonstrated that alpha- and zeta-thrombins, both with the higher fibrinogen-procoagulant activities, were inhibited. In rats receiving high doses of bivalirudin, the platelet deposition in carotide was reduced by 63% compared to controls. The results of clinical studies, conducted only in patients receiving concomitant aspirin, suggested that the use of bivalirudin was more efficacious and more predictable than unfractionated heparin, with fewer bleeding complications. Despite some unresolved developmental issues, the attractive properties of this novel agent could make it a useful alternative to heparin in a variety of coagulation disorders.

• 용도

  Anticoagulant; antithrombotic.

• 정의

  ChEBI: A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva o the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.

• Mechanism of action

  Bivalirudin is a rapid-onset, short-acting DTI that binds to both the active site and the exosite-1 of thrombin. Unlike lepirudin, bivalirudin is a reversible inhibitor of both free thrombin and thrombin bound to fibrin. This reversibility is possible because the bound bivalirudin undergoes cleavage at the second N-terminal proline to release the portion of the drug bound to the active site. The carboxyl-terminal portion of bivalirudin dissociates from thrombin to regenerate thrombin. Bivalirudin does not bind to plasma protein.

• Pharmacokinetics

  Bivalirudin is administered via intravenous bolus injection, followed by continuous infusion (Table 31.4). The drug exhibits a rapid onset and a short duration of action. Bivalirudin is eliminated by renal excretion. It has been suggested that dosage adjustments be made in patients with severe renal impairment and in patients undergoing dialysis. Approximately 30% is eliminated unchanged along with proteolytic cleavage products. Because of the reversible nature of bivalirudin the drug exhibits less risk of bleeding than other antithrombotics, and there have been no reported cases of antibody formation to bivalirudin.

• Clinical Use

  Bivalirudin, a 20-amino-acid peptide, has been approved for use in patients with unstable angina undergoing percutaneous coronary intervention.

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