Bivalirudin

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[edit] BRAND NAMES

[edit] STRUCTURE

File:Bivalirudin.jpg

[edit] MECHANISM OF ACTION

Blood clotting can be a problem when blood flow is disturbed in any way. Bivalirudin is an anticoagulant, which means that it prevents the blood from clotting. Bivalirudin, is a synthetic substance derived from hirudin, the anticoagulant substance produced by leeches. It is a specific and reversible direct thrombin inhibitor (DTI).

Thrombin 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 crosslinked framework that stabilises the thrombus. Thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release. Bivalirudin inhibits each of these thrombin effects

Using Bivalirudin greatly reduces the risk of a blood clot forming. This can improve the effectiveness of Percutaneous coronary intervention (PCI) and help to maintain the flow of blood to the heart in patients with angina or myocardial infarction.

[edit] INDICATIONS

Bivalirudin is indicated for use as an anticoagulant in patients:

  • With unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA).
  • Undergoing percutaneous coronary intervention (PCI) with provisional use of glycoprotein IIb/IIIa inhibitor (GPI).
  • With, or at risk of, heparin-induced thrombocytopenia (HIT) or heparin-induced thrombocytopenia and thrombosis syndrome (HITTS), undergoing PCI.

Bivalirudin is intended for use with aspirin.

[edit] DOSAGE

For patients who do not have HIT/HITTS
• PCI/PTCA: 0.75 mg/kg intravenous (IV) bolus dose followed by a 1.75 mg/kg/h IV infusion for the duration of the procedure. 
• Perform activated clotting time (ACT) test 5 minutes post-bolus dose. If needed, give an additional bolus of 0.3 mg/kg. 
• After PCI/PTCA, IV infusion may be continued for up to 4 hours, after which a rate of 0.2 mg/kg/h can be used for up to 20 more hours, if
needed.
• Consider glycoprotein IIb/IIIa inhibitor (GPI) administration with procedural complications. 

For patients who have HIT/HITTS
• The recommended dose of Bivalirudin in patients with HIT/HITTS undergoing PCI is an IV bolus of 0.75 mg/kg. This should be followed by
an infusion at a rate of 1.75 mg/kg/h for the duration of the procedure. 
• After PCI/PTCA, IV infusion may be continued for up to 4 hours, after which a rate of 0.2 mg/kg/h can be used for up to 20 more hours, if
needed.

For patients with renal impairment
• No reduction in bolus dose required. Consider reduction of the rate of infusion to 1 mg/kg/h for CrCL <30 mL/min or 0.25 mg/kg/h if
on dialysis.

[edit] CONTRAINDICATIONS

  • Active major bleeding
  • Hypersensitivity to bivalirudin or any product components

[edit] PRECAUTIONS

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

[edit] SIDE EFFECTS

The most common side effect with Bivalirudin (seen in more than 1 patient in 10) is minor bleeding. Other adverse reactions (incidence >0.5%) were headache, thrombocytopenia and fever

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