Bivalirudin In 0.9% Sodium Chloride

Uses

Bivalirudin In 0.9% Sodium Chloride is used for:

• Anticoagulant in Patients Undergoing PTCA/PCI or PCI with HITS/HITTS
• Unstable Angina/Non-ST-Elevation MI (Off-label)
• STEMI Undergoing Primary PCI (Off-label)
• Heparin-induced Thrombocytopenia

• ClCr 30 to 50 mL/min: Administer infusion at rate of 1.75 mg/kg/h.
• ClCr less than 30 mL/min: Reduce infusion rate to 1 mg/kg/h.

Bivalirudin In 0.9% Sodium Chloride is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Thrombotic events

How Bivalirudin In 0.9% Sodium Chloride works

Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.

Dosage

Bivalirudin In 0.9% Sodium Chloride dosage

PCI/PTCA: IV Bolus dose of 0.75 mg/kg followed by an infusion of 1.75 mg/kg/h for duration of PCI procedure. Five minutes after bolus dose, obtain ACT and administer additional bolus of 0.3 mg/kg if indicated.

HIT/HITTS: IV Bolus dose of 0.75 mg/kg, followed by a continuous infusion at a rate of 1.75 mg/kg/h for the duration of the procedure.

Continuation of Therapy: IV Infusion may be continued for up to 4 h post-procedure as indicated. After 4 h, an additional IV infusion of 0.2 mg/kg/h for up to 20 h may be given if needed.

Concomitant Therapy: Bivalirudin In 0.9% Sodium Chloride is intended for concurrent use with aspirin (300 to 325 mg/day).

• For IV administration only. Not for intradermal, subcutaneous, IM, or intra-arterial administration.
• Reconstitute powder for injection with 5 mL sterile water for injection. Gently swirl until powder is dissolved.
• For initial bolus infusion, further dilute each reconstituted via in 50 mL of 5% dextrose in water or sodium chloride 0.9% for injection to yield a final concentration of 5 mg/mL.
• For low rate infusion, further dilute each reconstituted vial in 500 mL of 5% dextrose in water or sodium chloride 0.9% for injection to yield a final concentration of 0.5 mg/mL.
• Do not mix with the following drugs in the same IV line: alteplase, amiodarone, amphotericin B, chlorpromazine, diazepam, dobutamine, prochlorperazine, reteplase, streptokinase, vancomycin.
• Reconstituted bivalirudin should be a clear to slightly opalescent, colorless to slightly yellow solution. Do not administer if reconstituted or diluted solution is discolored, cloudy, or contains particulate matter.
• Maintain meticulous catheter technique, with frequent aspiration and flushing, paying special attention to minimizing conditions of stasis within the catheter or vessels.
• Discard any unused reconstituted or diluted solution.

Side Effects

• Bleeding, Body as a Whole: fever,infection, sepsis;
• Cardiovascular: hypotension, syncope, vascular anomaly,ventricular fibrillation;
• Nervous: cerebral ischemia, confusion, facialparalysis;
• Respiratory: lung edema;
• Urogenital: kidney failure, oliguria.

Toxicity

Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.

Precaution

Bleeding Events: Although most bleeding associated with the use of Bivalirudin In 0.9% Sodium Chloride in PCI/PTCA occurs at the site of arterial puncture, hemorrhage can occur at any site. An unexplained fall in blood pressure or hematocrit should lead to serious consideration of a hemorrhagic event and cessation of Bivalirudin In 0.9% Sodium Chloride administration. Bivalirudin In 0.9% Sodium Chloride should be used with caution in patients with disease states associated with an increased risk of bleeding.

Coronary Artery Brachy therapy: An increased risk of thrombus formation, including fatal outcomes, has been associated with the use of Bivalirudin In 0.9% Sodium Chloride in gamma brachytherapy. If a decision is made to use Bivalirudin In 0.9% Sodium Chloride during brachytherapy procedures, maintain meticulous catheter technique, with frequent aspiration and flushing, paying special attention to minimizing conditions of stasis within the catheter or vessels.

Interaction

Co-administration of Bivalirudin In 0.9% Sodium Chloride with heparin, warfarin, thrombolytics, or GPIs was associated with increased risks of major bleeding events.

Food Interaction

• Avoid echinacea.
• Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Bivalirudin In 0.9% Sodium Chloride Drug Interaction

Unknown: arginine, arginine, levocarnitine, levocarnitine, cysteine, cysteine, lithium, lithium, valproic acid, valproic acid, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, cholecalciferol, cholecalciferol, phytonadione, phytonadione, menaquinone, menaquinone

Bivalirudin In 0.9% Sodium Chloride Disease Interaction

Major: active bleedingModerate: renal impairment

Volume of Distribution

0.2L/kg

Elimination Route

Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours.

Half Life

• Normal renal function: 25 min (in normal conditions)
• Creatinine clearance 10-29mL/min: 57min
• Dialysis-dependant patients: 3.5h

Clearance

• 3.4 mL/min/kg [Normal renal function]
• 3.4 mL/min/kg [mild renal function]
• 2.7 mL/min/kg [moderate renal function]
• 2.8 mL/min/kg [severe renal function]
• 1 mL/min/kg [Dialysis-dependent patients]

Elimination Route

Bivalirudin In 0.9% Sodium Chloride is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage.

Pregnancy & Breastfeeding use

Pregnancy Category B. No adequate and well-controlled studies in pregnant women. As animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Bivalirudin In 0.9% Sodium Chloride is intended for use with aspirin . Because of possible adverse effects on the neonate and the potential for increased maternal bleeding, particularly during the third trimester, Bivalirudin In 0.9% Sodium Chloride and aspirin should be used together during pregnancy only if clearly needed.

Nursing Mothers: It is not known whether bivalirudin is excreted in human milk. As many drugs are excreted in human milk, caution should be exercised when Bivalirudin In 0.9% Sodium Chloride is administered to a nursing woman.

Contraindication

Bivalirudin In 0.9% Sodium Chloride is contraindicated in patients with: Active major
bleeding & Hypersensitivity (e.g., anaphylaxis) to Bivalirudin In 0.9% Sodium Chloride or its components

Acute Overdose

Cases of overdose of up to 10 times the recommended bolus or continuous infusion dose of Bivalirudin In 0.9% Sodium Chloride have been reported in clinical trials and in postmarketing reports. A number of the reported overdoses were due to failure to adjust the infusion dose of bivalirudin in persons with renal dysfunction including persons on hemodialysis . Bleeding, as well as deaths due to hemorrhage, have been observed in some reports of overdose. In cases of suspected overdosage, discontinue Bivalirudin In 0.9% Sodium Chloride immediately and monitor the patient closely for signs of bleeding. There is no known antidote to Bivalirudin In 0.9% Sodium Chloride. Bivalirudin In 0.9% Sodium Chloride is hemodialyzable

Storage Condition

Store at temperature not exceeding 30º C in a dry place. Do not freeze. Keep out of reach of children

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