Also found in: Wikipedia.
Pharmacologic class: Thrombin inhibitor
Therapeutic class: Anticoagulant
Pregnancy risk category B
Selectively inhibits thrombin by binding to its receptor sites, causing inactivation of coagulation factors V, VIII, and XII and thus preventing conversion of fibrinogen to fibrin
Powder for injection: 250 mg/vial
Indications and dosages
➣ Patients with unstable angina who are undergoing percutaneous transluminal coronary angioplasty (PTCA); patients with or at risk for heparin-induced thrombocytopenia or heparin-induced thrombocytopenia and thrombosis syndrome undergoing percutaneous coronary intervention
Adults: 0.75 mg by I.V. bolus followed by 1.75 mg/kg/hour by I.V. infusion for duration of procedure. Five minutes after bolus is administered, an activated clotting time should be obtained and an additional bolus of 0.3 mg/kg should be given if needed. Continuation of infusion for up to 4 hours post-procedure is optional, and at discretion of treating physician. After 4 hours, an additional I.V. infusion may be initiated at rate of 0.2 mg/kg/hour for up to 20 hours if needed.
• Renal impairment
• Dialysis patients
• PCTA (regardless of history of unstable angina)
• Anticoagulation during orthopedic surgery
• Hypersensitivity to drug
• Active major bleeding
Use cautiously in:
• renal impairment, severe hepatic dysfunction, bacterial endocarditis, cerebrovascular accident, severe hypertension, heparin-induced thrombocytopenia, thrombosis syndrome
• diseases associated with increased risk of bleeding
• concurrent use of other platelet aggregation inhibitors
• pregnant or breastfeeding patients
• For I.V. injection and infusion, add 5 ml of sterile water to each 250-mg vial; gently mix until dissolved. Further dilute in 50 ml of dextrose 5% in water or normal saline solution for injection to a final concentration of 5 mg/ml.
• Don't mix with other drugs.
• Don't give by I.M. route.
• Know that drug is intended for use with aspirin.
CNS: headache, anxiety, nervousness, insomnia
CV: hypotension, hypertension, bradycardia, ventricular fibrillation
GI: nausea, vomiting, abdominal pain, dyspepsia, severe spontaneous GI bleeding
GU: urinary retention, severe spontaneous GU bleeding
Hematologic: severe spontaneous bleeding
Musculoskeletal: pelvic or back pain
Other: fever, pain at injection site
Drug-drug. Abciximab, anticoagulants (including heparin, low-molecular-weight heparins, and heparinoids),
thrombolytics, ticlopidine, warfarin: increased risk of bleeding
Drug-diagnostic tests. Activated partial thromboplastin time, prothrombin time: increased
Drug-herbs. Ginkgo biloba: increased risk of bleeding
☞ Monitor blood pressure, hemoglobin, and hematocrit. Be aware that decrease in blood pressure or hematocrit may signal hemorrhagic event.
• Monitor venipuncture site closely for bleeding.
☞ Instruct patient to immediately report bleeding, bruising, or tarry stools.
• Tell patient to avoid activities that can cause injury. Advise him to use soft toothbrush and electric razor to avoid gum and skin injury.
bivalirudinA specific direct-thrombin inhibitor, a synthetic analogue of hirudin, which is found in the saliva of Hirudo medicinalis, the medicinal leech. It is better than heparin in that it has a rapid onset of action, shorter half-life, is potent, specifically binds to thrombin and is reversible.
Anticoagulant for unstable angina and percutaneous coronary interventions, especially patients with heparin induced thrombocytopenia/heparin induced thrombosis-thrombocytopenia syndrome (HIT/HITTS).