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| {{Bivalirudin}}
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| {{CMG}}; {{AE}} {{JH}}
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| '''''For patient information about Bivalirudin, click [[Bivalirudin (patient information)|here]].'''''
| | {{Ticlopidine}} |
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| {{SB}} ANGIOMAX<sup>®</sup> | | {{CMG}}; {{AE}} {{AZ}} |
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| ==Overview==
| | '''''For patient information, click <u>[[Ticlopidine (patient information)|here]]'''''</u>. |
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| '''Bivalirudin''' (Angiomax or Angiox, manufactured by The Medicines Company) is a specific and reversible [[direct thrombin inhibitor]] (DTI).
| | {{SB}} Ticlopidine<sup>®</sup> |
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| Chemically, it is a synthetic congener of the naturally occurring drug [[hirudin]] (found in the saliva of the medicinal leech ''Hirudo medicinalis'').
| | ==Overview== |
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| Bivalirudin is a DTI that overcomes many limitations seen with indirect thrombin inhibitors, such as [[heparin]]. Bivalirudin is a short, synthetic peptide that is potent, highly specific, and a reversible inhibitor of [[thrombin]]. It inhibits both circulating and clot-bound thrombin, while also inhibiting thrombin-mediated platelet activation and aggregation. It does not bind to plasma proteins (other than thrombin) or to red blood cells. Therefore it has a predictable antithrombotic response. There is no risk for [[Heparin-induced thrombocytopenia|Heparin Induced Thrombocytopenia]]/Heparin Induced Thrombosis-Thrombocytopenia Syndrome (HIT/HITTS). It does not require a binding cofactor such as antithrombin and does not activate platelets. These characteristics make bivalirudin an ideal alternative to heparin.
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| Bivalirudin clinical studies demonstrated consistent positive outcomes in patients with stable [[angina]], unstable angina (UA), non-ST segment elevation myocardial infarction ([[NSTEMI]]), and ST-segment elevation myocardial infarction ([[STEMI]]) undergoing [[PCI]] in 7 major randomized trials.
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| ==Category== | | ==Category== |
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| Direct thrombin inhibitor.
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| ==FDA Package Insert== | | ==FDA Package Insert== |
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| ====Label Title====
| | '''| [[Ticlopidine indications and usage|Indications and Usage]]''' |
| | | '''| [[Ticlopidine dosage and administration|Dosage and Administration]]''' |
| ''' [[Bivalirudin indications and usage|Indications and Usage]]''' | | '''| [[Ticlopidine dosage forms and strengths|Dosage Forms and Strengths]]''' |
| '''| [[Bivalirudin dosage and administration|Dosage and Administration]]''' | | '''| [[Ticlopidine contraindications|Contraindications]]''' |
| '''| [[Bivalirudin dosage forms and strengths|Dosage Forms and Strengths]]''' | | '''| [[Ticlopidine warnings|Warnings and Precautions]]''' |
| '''| [[Bivalirudin contraindications|Contraindications]]''' | | '''| [[Ticlopidine adverse reactions|Adverse Reactions]]''' |
| '''| [[Bivalirudin warnings and precautions|Warnings and Precautions]]''' | | '''| [[Ticlopidine drug interactions|Drug Interactions]]''' |
| '''| [[Bivalirudin adverse reactions|Adverse Reactions]]''' | | '''| [[Ticlopidine use in specific populations|Use in Specific Populations]]''' |
| '''| [[Bivalirudin drug interactions|Drug Interactions]]''' | | '''| [[Ticlopidine overdosage|Overdosage]]''' |
| '''| [[Bivalirudin use in specific populations|Use in Specific Populations]]''' | | '''| [[Ticlopidine description|Description]]''' |
| '''| [[Bivalirudin overdosage|Overdosage]]''' | | '''| [[Ticlopidine clinical pharmacology|Clinical Pharmacology]]''' |
| '''| [[Bivalirudin description|Description]]''' | | '''| [[Ticlopidine nonclinical toxicology|Nonclinical Toxicology]]''' |
| '''| [[Bivalirudin clinical pharmacology|Clinical Pharmacology]]''' | | '''| [[Ticlopidine clinical studies|Clinical Studies]]''' |
| '''| [[Bivalirudin nonclinical toxicology|Nonclinical Toxicology]]''' | | '''| [[Ticlopidine how supplied storage and handling|How Supplied/Storage and Handling]]''' |
| '''| [[Bivalirudin clinical studies|Clinical Studies]]''' | | '''| [[Ticlopidine patient counseling information|Patient Counseling Information]]''' |
| '''| [[Bivalirudin how supplied storage and handling|How Supplied/Storage and Handling]]''' | | '''| [[Ticlopidine labels and packages|Labels and Packages]]''' |
| '''| [[Bivalirudin patient counseling information|Patient Counseling Information]]''' | |
| '''| [[Bivalirudin labels and packages|Labels and Packages]]''' | |
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| ==Mechanism of Action== | | ==Mechanism of Action== |
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| Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Thrombin is a serine proteinase that plays a central role in the thrombotic process. It cleaves [[fibrinogen]] into fibrin monomers, activates Factor V, VIII, and XIII, allowing fibrin to develop a covalently cross-linked framework that stabilizes the thrombus. [[Thrombin]] also promotes further [[thrombin]] generation, and activates platelets, stimulating aggregation and granule release. The binding of bivalirudin to thrombin is reversible as [[thrombin]] slowly cleaves the bivalirudin-Arg<sub>3</sub>-Pro<sub>4</sub> bond, resulting in recovery of thrombin active site functions.
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| '''Pharmacokinetics'''
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| *Following an IV bolus of bivalirudin of 1 mg/kg and a 4-hour 2.5 mg/kg/h IV infusion a mean steady state concentration of 12.3 ± 1.7 µg/mL is achieved
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| *Bivalirudin is cleared from plasma by a combination of renal mechanisms and proteolytic cleavage
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| *Half-life:
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| : Normal renal function (≥ 90 mL/min) = 25 minutes
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| : Mild renal dysfunction (60–89 mL/min) = 22 minutes
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| : Moderate renal dysfunction (30-59 mL/min) = 34 minutes
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| : Severe renal dysfunction (≤ 29 mL/min) = 57 minutes
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| : Dialysis-dependent = 3.5 hours
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| *Clearance is reduced approximately 20% in patients with moderate and severe renal impairment and by 80% in [[dialysis]]-dependent patients
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| *Bivalirudin is hemodialyzable and approximately 25% is cleared by hemodialysis.
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| '''Pharmacodynamics'''
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| [[Coagulation]] times return to baseline approximately 1 hour following cessation of bivalirudin administration.
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| ==References== | | ==References== |
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| {{Reflist|2}} | | {{Reflist|2}} |
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| [[Category:Cardiovascular Drugs]]
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| [[Category:Drugs]] | | [[Category:Drugs]] |