bivalirudin


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bivalirudin

 [bi-val´ĭroo-din]
an inhibitor of the clot-promoting activity of thrombin, used in conjunction with aspirin as an anticoagulant in patients with unstable angina pectoris who are undergoing percutaneous transluminal coronary angioplasty; administered intravenously.

bivalirudin

Angiomax, Angiox (UK)

Pharmacologic class: Thrombin inhibitor

Therapeutic class: Anticoagulant

Pregnancy risk category B

Action

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

Availability

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.

Dosage adjustment

• Renal impairment
• Dialysis patients

Off-label uses

• PCTA (regardless of history of unstable angina)
• Anticoagulation during orthopedic surgery

Contraindications

• Hypersensitivity to drug
• Active major bleeding

Precautions

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
• children.

Administration

• 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.

Adverse reactions

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

Interactions

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

Patient monitoring

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.

Patient teaching

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.

hirulog

(her-yū-log),
A synthetic thrombin inhibitor.
Synonym(s): bivalirudin

bivalirudin

/bi·val·i·ru·din/ (bi-val´ĭroo-din) an anticoagulant used with aspirin in patients with unstable angina pectoris who are undergoing percutaneous transluminal coronary angioplasty.

bivalirudin

[bi-val′roo-din]
an inhibitor of the clot-promoting activity of thrombin, used in conjunction with aspirin as an anticoagulant in patients with unstable angina pectoris who are undergoing percutaneous transluminal coronary angioplasty; administered intravenously.

bivalirudin

A 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.

Indications
Anticoagulant for unstable angina and percutaneous coronary interventions, especially patients with heparin induced thrombocytopenia/heparin induced thrombosis-thrombocytopenia syndrome (HIT/HITTS).
References in periodicals archive ?
M2 EQUITYBITES-January 23, 2018-Water Street & medical partner awarded US FDA approval for Bivalirudin in first frozen premixed ready-to-use formulation presentation
M2 PHARMA-January 23, 2018-Water Street & medical partner awarded US FDA approval for Bivalirudin in first frozen premixed ready-to-use formulation presentation
MedCo's form of bivalirudin is prepared using an improved compounding process that reduces the formation of impurities--that otherwise render the drug unusable for human injection--to less than 0.
The active pharmaceutical ingredient in Angiomax[R];, bivalirudin, is an acidic compound that requires processing before it can be injected into patients.
The active pharmaceutical ingredient in AngiomaxA;, bivalirudin, is an acidic compound that requires processing before it can be injected into patients.
This agreement with Sandoz, itself a leader in the generics market, helps to ensure that bivalirudin remains a high-quality product in this market.
The Pediatric Health Information System database was queried for pediatric patients discharged from January 1, 2004 to December 31, 2011 if they received one of the following DUs during admission: argatroban, bivalirudin, desirudin, or lepirudin.
According to the researchers, the drug can reduce rate of repeat heart attacks, as compared to bivalirudin which is more expensive.
The purpose of this study was to assess whether simulation training can improve the clinician's ability to predict the effect of bivalirudin infusion.
The use of bivalirudin (Angiomax) during percutaneous coronary intervention (PCI) resulted in a decreased risk of bleeding compared with unfractionated heparin alone or heparin with glycoprotein IIb-IIIa inhibitors, according to a" study published online in Circulation: Cardiovascular Interventions.
The bivalent DTIs include bivalirudin and lepirudin, and bind both the active site and exosite 1 of thrombin.