bupivacaine liposome (Rx)

Brand and Other Names:Exparel
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable suspension

  • 1.3% (13.3mg/mL)
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Postsurgical Local Analgesia

Indicated for single-dose infiltration in adults to produce postsurgical local analgesia

Recommended dose based on size of the surgical site; volume required to cover the area, and patient factors that may impact the safety of an amide local anesthetic; not to exceed 266 mg (20 mL)

As general guidance in selecting the proper dosing for the planned surgical site, examples of dosing are provided below

Bunionectomy

  • 106 mg (8 mL) once via infiltration of surgical site
  • Infiltrate 7 mL into tissues surrounding osteotomy and 1 mL into subcutaneous tissue

Hemorrhoidectomy

  • 266 mg (20 mL) once via infiltration of surgical site
  • Dilute 20 mL with 10 mL of saline, for a total of 30 mL, and divide the mixture into six 5 mL aliquots
  • Perform the anal block by visualizing the anal sphincter as a clock face and slowly infiltrating one aliquot to each of the even numbers

Regional Analgesia via Interscalene Brachial Plexus Nerve Block

Indicated for single-dose infiltration in adults to produce postsurgical regional analgesia as an interscalene brachial plexus nerve block

133 mg (10 mL) once via infiltration of surgical site

Based upon one study of patients undergoing either total shoulder arthroplasty or rotator cuff repair

Dosage Modifications

Renal impairment

  • Bupivacaine is substantially excreted by the kidney
  • Risk of toxicity may be greater in patients with impaired renal function; use caution

Hepatic impairment

  • Amide-type local anesthetics (eg, bupivacaine) are metabolized by the liver
  • Severe hepatic impairment: Greater risk of developing toxic plasma concentrations; use caution

Dosing Considerations

Limitation of use

  • Safety and efficacy has not been established in other nerve blocks

Safety and efficacy not established

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Interactions

Interaction Checker

and bupivacaine liposome

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Nausea (2.1-40.2%)

            Vomiting (2.1-27.8%)

            1-10%

            Dizziness (6.2%)

            Tachycardia (3.9%)

            Headache (3.8%)

            Somnolence (2.1%)

            Bradycardia (1.6%)

            Hypoesthesia (1.5%)

            Lethargy (1.3%)

            Postmarketing Reports

            Injury, poisoning, and procedural complications: Drug-drug interaction, procedural pain

            Nervous system disorders: Palsy, seizure

            General disorders and administration site conditions: Lack of efficacy, pain

            Skin and subcutaneous tissue disorders: erythema, rash

            Cardiac disorders: Bradycardia, cardiac arrest

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            Warnings

            Contraindications

            Obstetrical paracervical block anesthesia; use of bupivacaine for paracervical block has resulted in fetal bradycardia and death

            Cautions

            For single administration only (see Administration)

            Not interchangeable with other forms of bupivacaine (see Administration)

            For infiltrative use only; do not use for epidural, intrathecal, regional nerve blocks, or intravascular or intra-articular administration

            Has not been evaluated for patients <18 years, pregnant or nursing patients (see Pregnancy)

            Use only in a setting where trained personnel and equipment are available to promptly treat patients who show evidence of neurological or cardiac toxicity

            Monitor cardiovascular/neurological status and vital signs during and after injection

            CNS reactions characterized by excitation and/or depression, restlessness, anxiety, dizziness, tinnitus, blurred vision, tremors, or convulsions; other CNS effects may include nausea, vomiting, chills, and miosis

            Toxic blood concentrations may depress cardiac conductivity and excitability that leads to AV block, ventricular arrhythmias, and cardiac arrest; additionally, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure

            Allergic-type reactions are rare; cross-sensitivity to other amide-type local anesthetics reported

            Chondrolysis: Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been postmarketing reports of chondrolysis in patients receiving such infusions

            Because amide-type local anesthetics, such as bupivacaine, are metabolized by the liver, use cautiously with hepatic disease; greater risk for toxic plasma concentrations with severe hepatic disease

            Avoid additional use of local anesthetics within 96 hours following administration

            Drug has not been evaluated for epidural, intrathecal, regional nerve blocks other than interscalene, brachial plexus nerve block, intravascular or intra-articular use

            Sensory and/or motor loss with therapy may occur but is temporary and varies in degree and duration depending on site of injection and dosage administered and may last for up to 5 days as seen in clinical trials

            Not for administration within 96 hours of administering other bupivacaine formulations

            Drug interactions overview

            • See Administration
            • Bupivacaine HCl administered together with bupivacaine liposome suspension may impact the pharmacokinetic and/or physicochemical properties, and this effect is concentration dependent
            • Nonbupivacaine based local anesthetics, including lidocaine, may cause an immediate release of bupivacaine from bupivacaine liposome suspension if administered together locally; there are no data to support administration of other local anesthetics prior to administration
            • Do not dilute with water or other hypotonic agents, as it will result in disruption of the liposomal particles
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            Pregnancy & Lactation

            Pregnancy

            There are no studies conducted with pregnant women

            In animal reproduction studies, embryofetal deaths were observed with SC administration of bupivacaine to rabbits during organogenesis at a dose equivalent to 1.6 times the maximum recommended human dose (MRHD) of 266 mg; SC administration of bupivacaine to rats from implantation through weaning produced decreased pup survival at a dose equivalent to 1.5 times the MRHD

            Based on animal data, advise pregnant women of the potential risks to a fetus

            Contraindicated for obstetrical paracervical block anesthesia (see Contraindications)

            Bupivacaine can rapidly cross the placenta, and when used for epidural, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity

            Lactation

            Limited published literature reports that bupivacaine and its metabolite, pipecoloxylidide, are present in human milk at low levels

            There is no available information on effects of the drug in the breastfed infant or effects of the drug on milk production

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Local anesthetic; blocks generation and conduction of nerve impulses presumably by increasing the electrical excitation threshold in the nerve, by slowing nerve impulse propagation, and by reducing the rate of action potential rise

            Liposomal suspension of bupivacaine

            Absorption

            Absorption rate dependent on total dose, administration route, and administration site vascularity

            Duration: Up to 96 hr after local infiltration; 120 hr after interscalene brachial plexus nerve block

            Peak plasma time: 2 hr (bunionectomy); 0.5 hr (hemorrhoidectomy); 48 hr (total shoulder arthroplasty)

            Peak plasma concentration: 166 ng/mL (bunionectomy); 867 ng/mL (hemorrhoidectomy); 207 ng/mL (total shoulder arthroplasty)

            AUC: 5864-7105 hr•ng/mL (bunionectomy); 16,867-18,289 hr•ng/mL; 11,484 hr•ng/mL (total shoulder arthroplasty)

            Distribution

            Protein Bound: 95%

            Widely distributed to some extent to all body tissues; high concentrations found in highly perfused organs (eg, liver, lungs, heart, brain)

            Metabolism

            Metabolized primarily by the liver via conjugation with glucuronic acid

            Metabolites: ~5% converted to the major metabolite, pipecolylxylidine (PPX)

            Elimination

            Half-life: 34.1 hr (bunionectomy); 23.8 hr (hemorrhoidectomy); 11 hr (total shoulder arthroplasty)

            Excretion: Urine (mainly metabolites; 6% [unchanged])

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            Administration

            Compatibility Considerations

            Incompatibilities: Nonbupivacaine based local anesthetics (eg, lidocaine) may cause an immediate release of bupivacaine from the drug if administered together locally

            Bupivacaine liposome may follow lidocaine administration after waiting at least 20 minutes

            Bupivacaine HCl administered together with bupivacaine liposome suspension may impact the pharmacokinetic and/or physicochemical properties of Exparel, and this effect is concentration dependent; therefore, bupivacaine HCl and Exparel may be administered simultaneously in the same syringe, and bupivacaine HCl may be injected immediately before; ratio of dose of bupivacaine HCl solution to bupivacaine liposome suspension should not exceed 1:2

            Toxic effects of simultaneous use of both forms of bupivacaine are additive and their administration should be used with caution including monitoring for neurologic and cardiovascular effects related to toxicity

            Using Exparel followed by other bupivacaine formulations has not been studied in clinical trials; formulations of bupivacaine other than Exparel should not be administered within 96 hr following administration of Exparel

            When a topical antiseptic (eg, povidone iodine) is applied, the site should be allowed to dry before bupivacaine liposome is administered into the surgical site; bupivacaine liposome should not be allowed to come into contact with antiseptics such as povidone iodine in solution

            Preparation

            For single-dose infiltration only

            Different formulations of bupivacaine are not bioequivalent even if the milligram strength is the same; therefore, it is not possible to convert dosing from any other formulations of bupivacaine to bupivacaine liposome

            Invert vial multiple times to resuspend particles immediately prior to withdrawing drug from vial; multiple inversions may be necessary to resuspend if particles have settled

            Use diluted suspensions within 4 hr of preparation in a syringe

            Visually inspect vials before use

            Do not filter; do not heat before use; do not autoclave

            Administration

            Inject slowly into soft tissue via infiltration surgical site with frequent aspiration to check for blood and minimize the risk of intravascular injection

            Do not exceed 266 mg (20 mL, 1.3% of undiluted drug) for infiltration and 133 mg (10 mL) for interscalene brachial plexus nerve block

            Administer undiluted or diluted up to 0.89 mg/mL (ie, 1:14 dilution by volume) with preservative-free 0.9% NaCl or Lactated ringer’s solution

            Invert vials of multiple times to resuspend the particles immediately prior to withdrawal from the vial Administer with a 25 gauge or larger

            Do not administer if product discolored

            Do not administer if the vial has been frozen as reflected by the temperature indicator or exposed to high temperature (>40°C or 104°F) for an extended period

            Storage

            Unopened vials

            • Store refrigerated between 2-8°C (36-46°F)
            • May store at room temperature of 20-25°C (68-77°F) for up to 1 month in sealed, intact (unopened) vials; do not be re-refrigerated
            • Should not be frozen as reflected by the temperature indicator or exposed to high temperatures (>40°C [104°F]) for an extended period

            Opened vials

            • Store at controlled room temperature of 20-25°C (68-77°F) for up to 4 hr prior to administration
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            Formulary

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            NC NOT COVERED – Drugs that are not covered by the plan.
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