Bivalirudin Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
Anticoagulant; antithrombotic.
Definition
ChEBI:
Bivalirudin is 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 of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. It has a role as an anticoagulant and an EC 3.4.21.5 (thrombin) inhibitor.
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.
Pharmakokinetik
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.
Bivalirudin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
