Bivalirudin
- Atc Codes:B01AE06
- CAS Codes:128270-60-0
- PHARMGKB ID:128270-60-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Angiox; Belgium: Angiox; Bulgaria: Angiox; Cyprus: Angiox; Czech Republic: Angiox; Denmark: Angiox; Estonia: Angiox; Finland: Angiox; France: Angiox; Germany: Angiox; Greece: Angiox; Hungary: Angiox; Ireland: Angiox; Italy: Angiox; Latvia: Angiox; Lithuania: Angiox; Luxembourg: Angiox; Malta: Angiox; Netherlands: Angiox; Poland: Angiox; Portugal: Angiox; Romania: Angiox; Slovakia: Angiox; Slovenia: Angiox; Spain: Angiox; Sweden: Angiox; UK: Angiox.
North America
Canada: Angiomax; USA: Angiomax.
Latin America
Argentina: Angiomax.
Drug combinations
Chemistry
Bivalirudin: C~98~H~138~N~24~O~33~. Mw: 2180.29. (1) L-Leucine, D-phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamyl-L-α-glutamyl-L-tyrosyl-; (2) D-Phenylalanyl-L-prolyl-L-arginyl-L-prolylglycylglycylglycylglycyl-L-asparaginylglycyl-L-α-aspartyl-L-phenylalanyl-L-α-glutamyl-L-α-glutamyl-L-isoleucyl-L-prolyl-L-α-glutamyl-L-α-glutamyl-L-tyrosyl-L-leucine. CAS-128270-60-0 (1994).
Pharmacologic Category
Anticoagulants; Direct Thrombin Inhibitors. (ATC-Code: B01AE06).
Mechanism of action
Bivalirudin acts as a specific and reversible direct thrombin inhibitor by binding to the catalytic and anionic exosite of both circulating and clot-bound thrombin, and so preventing thrombin-mediated cleavage of fibrinogen to fibrin monomers, activation of factors V, VIII, and XIII, conversion of fibrinogen to fibrin, and platelet activation and aggregation. Prolongs activated clotting time, activated partial thromboplastin time (APTT), thrombin time (TT), and prothrombin time (PT).
Therapeutic use
Bivalirudin is used with aspirin to reduce the risk of acute ischemic complications in patients with unstable angina undergoing percutaneous coronary intervention (e.g. percutaneous transluminal coronary angioplasty). Bivalirudin is also used with aspirin and «provisional» treatment with a glycoprotein IIb/IIIa-receptor inhibitor to reduce acute ischemic events in selected patients undergoing percutaneous coronary intervention. Also, as an alternative to unfractionated heparin for adjunctive use with a GP~IIb/IIIa~-receptor inhibitor in patients undergoing percutaneous coronary intervention who are at low risk for ischemic complications.
Pregnancy and lactiation implications
Bivalirudin is used in conjunction with aspirin, which may lead to maternal or fetal adverse effects, especially during the third trimester. Use during pregnancy only if clearly needed. Excretion in breast milk unknown (use with caution during lactation).
Unlabeled use
Heparin-induced thrombocytopenia.
Contraindications
Hypersensitivity to bivalirudin or any component of the formulation. Active major bleeding.
Warnings and precautions
Bleeding is the most common complication. Increased risk of thrombus formation with use in γ-brachytherapy. Caution in renal impairment. Not for intramuscular use. PT/INR levels may become elevated in the absence of warfarin. May cause insomnia, anxiety, nervousness, or nausea (additive effect with concurrent use of SSRIs, lithium, or valproate). Do not administer bivalirudin in the same intravenous line with chlorpromazine, diazepam, or prochlorperazine (results in haze formation, microparticulate formation, or gross precipitation).