Bivalirudin

What it is and how it works

Mechanism of Action Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.

Mechanism class: Thrombin Inhibitors

Indications

Bivalirudin for Injection is indicated for use as an anticoagulant for use in patients undergoing percutaneous coronary intervention (PCI) including patients with heparin-induced thrombocytopenia and heparin-induced thrombocytopenia and thrombosis syndrome. Bivalirudin for Injection is a direct thrombin inhibitor indicated for use as an anticoagulant in patients undergoing percutaneous coronary intervention (PCI) including patients with heparin-induced thrombocytopenia (HIT) or heparin-induced thrombocytopenia and thrombosis syndrome (HITTS).

Dosage and administration (summary)

The recommended dosage is a 0.75 mg/kg intravenous bolus dose followed immediately by a 1.75 mg/kg/h intravenous infusion for the duration of the procedure. Five minutes after the bolus dose has been administered, an activated clotting time (ACT) should be performed and an additional bolus dose of 0.3 mg/kg should be given if needed. Extending duration of infusion post-procedure up to 4 hours should be considered in patients with ST segment elevation MI (STEMI). Recommended Dosage Bivalirudin for injection has been studied only in patients receiving concomitant aspirin.

Contraindications

Bivalirudin is contraindicated in patients with: Active major bleeding; Hypersensitivity (e.g., anaphylaxis) to bivalirudin or its components . Active major bleeding Hypersensitivity to bivalirudin or its components

Warnings and precautions

Bleeding Events: Bivalirudin increases the risk of bleeding. ( 5.1 , 6.1 , 12.2 ) Acute Stent Thrombosis: Increased incidence of acute stent thrombosis in STEMI patients undergoing primary PCI. ( 2.1 , 5.2 ) Thrombotic Risk with Coronary Artery Brachytherapy: An increased risk of thrombus formation, including fatal outcomes, in gamma brachytherapy. Bleeding Events Bivalirudin for injection increases the risk of bleeding . An unexplained fall in blood pressure or hematocrit should lead to serious consideration of a hemorrhagic event and cessation of bivalirudin for injection administration.

Pregnancy

Pregnancy Risk Summary There are no data available on use of bivalirudin in pregnant women to inform a drug-associated risk of adverse developmental outcomes. Reproduction studies in rats and rabbits administered subcutaneously doses up to 1.6 times and 3.2 times the maximum recommended human dose (MRHD) of 15 mg/kg/day based on body surface area (…

Storage and supply

Storage Storage Conditions Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). Discard unused portion. Sterile, Nonpyrogenic, Preservative-free. The container closure is not made with natural rubber latex.

Source: Bivalirudin (Bivalirudin) — US FDA prescribing information, 2024-04-04, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.