Bivalirudin pharmacology

Given that thrombin is the central mediator of coagulation and amplifies its own production, it is a natural target for pharmacologic intervention. Direct thrombin inhibitors (DTIs) bind thrombin and prevent interactions with its substrates (Fig. 7-7). Several injectable DTIs are approved for use in the United States including lepirudin, bivalirudin, arga-troban, and desirudin. Several oral DTIs are currently in... 

Pharmacology Bivalirudin directly inhibits thrombin by specifically binding to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. The binding of bivalirudin to thrombin is reversible. 

Sciulli TM, Mauro VE Pharmacology and clinical use of bivalirudin. Ann Pharmacother 2002 36 1028-1041. 

Reed MD, Bell D. Clinical pharmacology of bivalirudin. Pharmacotherapy 2002 22(part2) 105S-I I IS. 

Lui HK. Dosage, pharmacological effects and clinical outcomes for bivalirudin in percutaneous coronary intervention. J Invasive Cardiol 2000 I2(suppl F) 41 F—52F... 

Bivalirudin is a direct thrombin inhibitor that has found utility for reducing the rate of acute reocclusion in patients treated with PCI. It is preferential to heparin in PCI when HIT is present. This drug is a derivative of hirudin, which is a dedicated thrombin inhibitor with no other in vivo activities of significance. The molecule is semisynthetic the C-terminal of hirudin is linked by a polyglycine spacer to the tetrapeptide region of the N-terminal that reacts with the thrombin active site (22). It is monitored by the activated clotting time test. Its pharmacologic properties are shown in Table I. 

FIGURE 19-6. Pharmacologic activity of lepirudin, bivalirudin, argatroban, and ximelagatran. 

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