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

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 ?
According to the company, the decline in worldwide net revenue is a result of lower worldwide net revenue from sales of Angiomax (bivalirudin)/Angiox (bivalirudin), which it expects to be in the range of USD97m to USD105m compared to USD155.7m in the first quarter of 2014.
Research and development expenses of USD4.0m were announced for the three months ended 31 December 2014, a rise by USD1.4m versus the R&D of USD2.6m in the three months ended 31 December 2013, primarily as a result of a net increase in project spending specifically for RTU bivalirudin and the bendamustine projects.
Healthcare company The Medicines Company (NasdaqGS:MDCO) reported on Monday the receipt of renewal of marketing approval for Angiox (bivalirudin) in Europe, reconfirming its favorable risk-benefit profile, for treating adult patients undergoing percutaneous coronary intervention (PCI).
REGULATE-PCI is a PROBE (prospective, randomised, open-label, blinded-endpoint) study aimed at determining the efficacy of REG1 compared to bivalirudin.The company is testing REG1 in patients undergoing percutaneous coronary intervention or for the treatment of unstable angina or non-ST elevated myocardial infarction.
23 January 2012 - The Medicines Company (NASDAQ:MDCO), or MDCO, said on Monday that it had reached a settlement agreement on the lawsuit relating to the Abbreviated New Drug Application (ANDA) filed by APP Pharmaceuticals LLC (APP) for a generic version of Angiomax (bivalirudin for injection).
In conjunction, a joint development committee and commercialisation committee have been formed to prepare and deliver global development and commercialisation plans related to AstraZeneca's BRILINTA and The Medicines Company's Angiomax (bivalirudin) for injection and cangrelor, which is in development as an acute intravenous antiplatelet agent.
9 November 2011 - First data from a pilot study on the use of anticoagulant Angiomax (bivalirudin) as an adjunct to catheter-based procedures in patients with severe defects of aortic heart valves who cannot undergo surgery have been presented at the annual Transcatheter Cardiovascular Therapeutics (TCT) conference, The Medicines Company (NASDAQ:MDCO), which makes Angiomax, said.
3 October 2011 - US-based The Medicines Company (NASDAQ:MDCO) said on Monday it had settled the lawsuits filed by the firm relating to the Abbreviated New Drug Applications (ANDAs) submitted by Teva Parenteral Medicines Inc and its affiliate, Pliva Hrvatska d.o.o., for generic versions of its anticoagulant Angiomax (bivalirudin for injection).
1 December 2009 - US-based pharmaceutical company The Medicines Company (NASDAQ: MDCO) announced today that it has received European approval for the use of Angiox (bivalirudin) as an anticoagulant in patients with heart attacks (so-called ST-segment elevation myocardial infarction (STEMI)) undergoing emergency heart procedures called primary percutaneous coronary intervention (PCI).
[170 Pages Report] Peptide Based Cardiovascular Therapeutics Market research report categorizes the global market by Drug (Bivalirudin, Eptifibatide), By Distribution Channel (Hospital Pharmacies, Retail Pharmacies, Online Pharmacies), & By Region (North America, Latin America, Europe, Japan, APEJ, MEA)
As per the forecast of FactMR, the bivalirudin segment is expected to reach a value of nearly US$ 1,360 Mn in the year 2022.
SunGen Pharma announced to launch Bivalirudin for Injection in the near future through their joint venture Peterson Athenex with Athenex Pharmaceuticals.