bupivacaine liposome (Rx)

Brand and Other Names:Exparel
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable suspension

  • 133mg/10mL single-dose vial
  • 266mg/20mL single-dose vial

Postsurgical Local Analgesia

Indicated for single-dose infiltration 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

Dosage Forms & Strengths

injectable suspension

  • 133mg/10mL single-dose vial
  • 266mg/20mL single-dose vial

Postsurgical Local Analgesia

Indicated for single-dose infiltration to produce postsurgical local analgesia in children aged ≥6 years

<6 years: Safety and efficacy not established

≥6 years: 4 mg/kg (not to exceed 266 mg) once via infiltration of surgical site

Dose based upon 2 studies of pediatric patients undergoing either spine surgery or cardiac surgery

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
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Interactions

Interaction Checker

and bupivacaine liposome

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            Contraindicated (4)

            • chloroprocaine

              chloroprocaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine.

            • lidocaine

              lidocaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine; may administer after waiting at least 20 minutes following local administration of lidocaine.

            • mepivacaine

              mepivacaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine.

            • ropivacaine

              ropivacaine increases toxicity of bupivacaine liposome by Other (see comment). Contraindicated. Comment: Do not admix with other local nonbupivacaine-based local anesthetics; admixing results in a rapid increase in free (unencapsulated) bupivacaine.

            Serious - Use Alternative (1)

            • bupivacaine implant

              bupivacaine liposome, bupivacaine implant. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid additional local anesthetic administration within 96 hr following bupivacaine implantation. If use of additional local anesthetics is unavoidable based on clinical need, monitor for neurologic and cardiovascular effects related to local anesthetic systemic toxicity.

              bupivacaine liposome, bupivacaine implant. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Local anesthetics may increase the risk of developing methemoglobinemia when concurrently exposed to drugs that also cause methemoglobinemia.

            Monitor Closely (1)

            • bupivacaine

              bupivacaine will increase the level or effect of bupivacaine liposome by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Bupivacaine HCl, when injected immediately before bupivacaine liposome, may impact the pharmacokinetic and/or physicochemical properties when the mg dose of bupivacaine HCl solution exceeds 50% of the bupivacaine liposome dose

            Minor (0)

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              Adverse Effects

              >10%

              Adults

              • Nausea (2.1-40.2%)
              • Vomiting (2.1-27.8%)
              • Dizziness (11.3%)

              Children

              • Hypotension (11.1-93.3%)
              • Muscle twitching (8.3-60%)
              • Nausea (6.9-60%)
              • Tachycardia (2.8-53.3%)
              • Vomiting (13.8-53.3%)
              • Constipation (13.8-46.7%)
              • Pruritus (8.3-40%)
              • Tachypnea (2.8-40%)
              • Bradycardia (5.6-33.3%)
              • Pyrexia (20%)
              • Hypoesthesia (20%)
              • Muscle spasms (20%)
              • Dizziness (5.6-20%)
              • Blurred vision (3.4-20%)
              • Anemia (13.9%)
              • Muscle weakness (13.3%)
              • Back pain (13.3%)
              • Oral hypoesthesia (11.1-13.3%)
              • Hematuria (13%)

              1-10%

              Adults

              • Headache (5.2%)
              • Somnolence (5.2%)
              • Tachycardia (3.9%)
              • Pruritus (3.1-5.2%)
              • AST increased (3.1%)
              • Body temperature increased (3.2%)
              • ALT increased (1.1-3.1%)
              • BUN increased (2.1%)
              • Constipation (2.1%)
              • Syncope (2.1%)
              • Pyrexia (2.1%)
              • Fungal infection (2.1%)
              • Postprocedural swelling (2.1%)
              • Decreased appetite (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 infiltrative use only; do not use for epidural, intrathecal, regional nerve blocks, or intravascular or intra-articular administration; caution to avoid accidental intravascular injection; convulsions and cardiac arrest have occurred following intravascular injection

              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

              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

              Drug interactions overview

              • Other local anesthetics
                • Avoid use of other local anesthetics within 94 hr after bupivacaine liposome administration
                • Potential for additive adverse effects
              • Methemoglobinemia
                • Caution/monitor
                • Increased risk of developing methemoglobinemia if coadministered with other local anesthetics, nitrates/nitrites, acetaminophen, metoclopramide, quinine, sulfasalazine, or other certain antineoplastic agents, antibiotics, antimalarials, or anticonvulsants
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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

              Adults

              • 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)

              Children

              • Peak plasma time: 1.2 hr (spine surgery); 23 hr (cardiac surgery)
              • Peak plasma concentration: 353 ng/mL (spine surgery); 447 ng/mL (cardiac surgery)
              • AUC (0-40 hr): 8,782 hr⋅ng/mL (spine surgery); 11,296 hr⋅ng/mL (cardiac surgery)

              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

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

              No images available for this drug.
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              Patient Handout

              Patient Education
              bupivacaine liposome (PF) local infiltration

              NO MONOGRAPH AVAILABLE AT THIS TIME

              USES: Consult your pharmacist.

              HOW TO USE: Consult your pharmacist.

              SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

              PRECAUTIONS: Consult your pharmacist.

              DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

              OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

              NOTES: No monograph available at this time.

              MISSED DOSE: Consult your pharmacist.

              STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

              Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

              IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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              Formulary

              FormularyPatient Discounts

              Adding plans allows you to compare formulary status to other drugs in the same class.

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              • Compare formulary status to other drugs in the same class.
              • Access your plan list on any device – mobile or desktop.

              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.
              4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
              NC NOT COVERED – Drugs that are not covered by the plan.
              Code Definition
              PA Prior Authorization
              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
              QL Quantity Limits
              Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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              Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.