Bivalirudin Injection

It is a standard anticoagulant drug in PCI surgery, especially suitable for the following scenarios:
Acute coronary syndrome (ACS): including unstable angina and non ST segment elevation myocardial infarction (NSTEMI). The HORIZONS-AMI trial showed that it can reduce the risk of adverse clinical events (death, myocardial infarction, target vessel reconstruction) and major bleeding within 30 days, and its efficacy is superior to heparin combined with glycoprotein IIb/IIIa inhibitors (GPI).
ST segment elevation myocardial infarction (STEMI): The use of bivalirudin during direct PCI can reduce thrombus burden and lower the risk of stent thrombosis.
Heparin induced thrombocytopenia (HIT): independent of antithrombin III (AT-III), it can directly inhibit thrombin and is a safe alternative for HIT patients.

Bivalirudin has a dual advantage in the treatment of ACS:
Reduce ischemic risk: By inhibiting thrombin mediated fibrin formation and platelet activation, reduce thrombotic events.
Reducing bleeding complications: The ACUITY study included 13819 high-risk NSTEMI patients, and the results showed that the incidence of major bleeding in the bivalirudin group alone was 47% lower than that in the heparin+GPI group (3.0% vs 5.7%), and the overall clinical outcome (ischemia+bleeding) was improved by 14%.

By inhibiting thrombin activity and blocking the coagulation cascade reaction, effectively preventing venous thromboembolism (VTE):
Surgical procedures: The risk of VTE is reduced by 30% -50% after major orthopedic surgeries such as hip replacement.
Tumor patients: Late stage tumor patients are prone to VTE due to hypercoagulability, and bivalirudin can be used as an alternative to low molecular weight heparin.
Long term immobilization: For patients with acute spinal cord injury or long-term bed rest, it can reduce the incidence of lower limb DVT.

With its direct and reversible thrombin inhibition effect, it occupies an important position in the treatment of cardiovascular diseases, thrombosis prevention, and special clinical scenarios.

Its uniqueness lies in the fact that whether thrombin is in the bloodstream or binds to blood clots, it can bind to them, and this binding is reversible. Thrombin inactivates the peptide bond between bivalirudin Arg3-Pro4 through slow enzymatic hydrolysis, thus the inhibitory effect is reversible and short-lived. More importantly, it can exert anticoagulant effects without relying on auxiliary factors such as AT-III and hepatic factor II, which enables it to effectively anticoagulate in patients with AT-III deficiency - an advantage that heparin drugs cannot match.
In vitro experiments were conducted to extend activated partial thromboplastin time (APTT), thrombin time (TT), prothrombin time (PT), and activated clotting time (ACT) in a concentration dependent manner. Healthy volunteer trials have shown that intravenous injection immediately produces anticoagulant effects, and coagulation function returns to normal about 1-2 hours after discontinuation.

2. Primary use: The 'golden partner' for percutaneous coronary intervention (PCI)
The most core and extensive use of bivalirudin is to prevent acute ischemic complications during elective percutaneous coronary intervention (PCI) in adults.
2.1 PCI anticoagulation in patients with unstable angina pectoris
For coronary heart disease patients undergoing PTCA treatment due to vascular infarction ≥ 70%, the standard medication regimen for bivalirudin is: intravenous injection of 1 mg/kg as the loading dose, followed by continuous infusion of 2.5 mg/kg per hour for 4 hours, adjusted to 0.2 mg/kg per hour if necessary, and continued infusion for 14 to 20 hours. Clinical data shows that among 291 patients receiving PTCA treatment, with increasing dose, the ACT time of most patients reached 300 or 350 seconds, and the APTT value of all patients exceeded 300 seconds, indicating an accurate and predictable anticoagulant effect.

2.2 Comprehensive management of acute coronary syndrome (ACS)
Widely applicable to acute coronary syndrome, including unstable angina and acute myocardial infarction. When ACS patients undergo PCI, it can effectively prevent intravascular thrombosis, stabilize plaques, and prevent the occurrence of acute coronary events, thereby reducing the incidence of cardiovascular events.
2.3 Continued anticoagulation after stent implantation surgery
Four hours after PCI, if necessary, the infusion can be maintained at a dose of 0.2 mg/kg per hour for no more than 20 hours. This continued anticoagulation strategy can effectively prevent stent thrombosis and ensure the long-term effectiveness of interventional therapy.

3. The 'life-saving straw' for HIT/HITTS patients
Heparin induced thrombocytopenia (HIT) is the most severe immune-mediated complication after the use of heparin, with an incidence rate of approximately 1% -5%. Once it occurs, all heparin drugs must be immediately discontinued. And without causing HIT, it is the preferred anticoagulant drug for HIT/HITTS patients undergoing PCI.
For patients diagnosed or highly suspected of HIT/HITTS, the medication regimen for bivalirudin is: intravenous injection of 0.75 mg/kg first, followed by intravenous drip of 1.75 mg/kg/h during PCI. This plan has been explicitly recommended by international guidelines, saving countless patients who have been trapped in a "no drug available" situation due to HIT.