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days to go: ASP+6% CMS reimbursement for proven non-opioids used in all outpatient surgical settings is coming January 1, 2025.

EXPAREL provides safe, consistent levels of bupivacaine over 4 days1,2

At both maximum doses of EXPAREL (266 mg for infiltration and 133 mg for interscalene brachial plexus nerve block), the plasma levels of bupivacaine remain below toxicity thresholds2-5

  • Central nervous system symptoms occurs at a plasma concentration of ≈2000 ng/mL with bupivacaine HCl2
  • Cardiac toxicity is associated with blood levels of ≥4000 ng/mL2
  • Pharmacokinetics demonstrate plasma levels of bupivacaine that can persist for 4 days3,6
  • At all doses studied, plasma bupivacaine levels are maintained well below cardiac and neurotoxic levels1-4,7,8
  • The rate of systemic absorption of bupivacaine is dependent upon the total dose of drug administered, the route of administration, and the vascularity of the administration site
  • Avoid additional use of local anesthetics within 96 hours following administration of EXPAREL
  • Systemic plasma levels of bupivacaine following administration of EXPAREL are not correlated with local efficacy

EXPAREL Dosing & Procedure

Bupivacaine administered via a CIC FNB
+ Local Infiltration (1210 mg total dose);
Cmax = 1760 ng/mL5

209 133 mg
(ISBPNB) - Adults2
467 133 mg + 10 mL (0.5%)
Bupi HCI + IPACK
(Adductor Canal NB)3
382 133 mg + Bupi HCI (50mg)
as Mayo Block
(Popliteal NB)4
320 4 mg/kg (Spine)7
(ages 6 to <12)
357 4 mg/kg (Spine)7
(ages 12 to <17)
447 4 mg/kg (Cardiac)
(ages 6 to <12)7
340 266 mg1(TKA)
365 266 mg1 (Hernia)
226 266 mg8 (TAP)
0
500
1000
1500
2000
4000

The thresholds for CNS and cardiac effects are 2000 ng/mL
and
4000 ng/mL, respectively2

Cmax of plasma bupivacaine concentration (ng/mL)

Additional safety information for EXPAREL

Excretion of liposomal bupivacaine in breast milk administered after cesarean birth12

Bupivacaine concentrations were evaluated in maternal plasma and transfer into breast milk in women undergoing EXPAREL infiltration in the transversus abdominis plane after cesarean birth.

  • 30 patients were enrolled and received 52 mg bupivacaine HCI hydrochloride 0.25% (20 mL) admixed with 266 mg EXPAREL 1.3% (20 mL)

Results showed:

  • Very little plasma bupivacaine was transferred into breast milk and bupivacaine did not accumulate in breast milk
  • Concentrations of bupivacaine in breast milk peaked at 6 hours, followed by a steady decline to undetectable levels at 96 hours
  • Maternal plasma concentrations had two peaks, first at 6 hours and then at 48 hours, followed by a steady decline

In addition, concentrations of bupivacaine in breast milk following continuous epidural infusion for up to 5 days have been found to be minimal14,15

  • Serum bupivacaine levels taken from an infant sample were shown to be undectectable16
  • Bupivacaine is not orally absorbed, therefore amounts received by the infant are small and have not caused any adverse effects in breastfed infants14

Effects of EXPAREL on wound healing

  • The effects of EXPAREL on various aspects of wound healing were examined in several Phase 2 and Phase 3, randomized, double-blind clinical studies across different surgical models.17
  • Overall, the analyses revealed that wound status, wound scarring, and wound healing profiles of EXPAREL were similar to that of bupivacaine HCl and better than the placebo (saline) group.17

ASP, average sales price; CMS, Centers for Medicare and Medicaid Services.

Important Notice

Indication

EXPAREL® (bupivacaine liposome injectable suspension) is indicated to produce postsurgical local analgesia via infiltration in patients aged 6 years and older and regional analgesia in adults via an interscalene brachial plexus nerve block, sciatic nerve block in the popliteal fossa, and an adductor canal block. Safety and efficacy have not been established in other nerve blocks.

Important Safety Information

  • EXPAREL is contraindicated in obstetrical paracervical block anesthesia.
  • Adverse reactions reported in adults with an incidence greater than or equal to 10% following EXPAREL administration via infiltration were nausea, constipation, and vomiting; adverse reactions reported in adults with an incidence greater than or equal to 10% following EXPAREL administration via nerve block were nausea, pyrexia, headache, and constipation.
  • Adverse reactions with an incidence greater than or equal to 10% following EXPAREL administration via infiltration in pediatric patients six to less than 17 years of age were nausea, vomiting, constipation, hypotension, anemia, muscle twitching, vision blurred, pruritus, and tachycardia.
  • Do not admix lidocaine or other non-bupivacaine local anesthetics with EXPAREL. EXPAREL may be administered at least 20 minutes or more following local administration of lidocaine.
  • EXPAREL is not recommended to be used in the following patient populations: patients <6 years old for infiltration, patients younger than 18 years old for nerve blocks, and/or pregnant patients.
  • Because amide-type local anesthetics, such as bupivacaine, are metabolized by the liver, EXPAREL should be used cautiously in patients with hepatic disease.

Warnings and Precautions Specific to EXPAREL

  • Avoid additional use of local anesthetics within 96 hours following administration of EXPAREL.
  • EXPAREL is not recommended for the following types or routes of administration: epidural, intrathecal, regional nerve blocks other than interscalene brachial plexus nerve block, sciatic nerve block in the popliteal fossa, and adductor canal block, or intravascular or intra-articular use.
  • The potential sensory and/or motor loss with EXPAREL is temporary and varies in degree and duration depending on the site of injection and dosage administered and may last for up to 5 days, as seen in clinical trials.

Warnings and Precautions for Bupivacaine-Containing Products

  • Central Nervous System (CNS) Reactions: There have been reports of adverse neurologic reactions with the use of local anesthetics. These include persistent anesthesia and paresthesia. CNS reactions are characterized by excitation and/or depression.
  • Cardiovascular System Reactions: Toxic blood concentrations depress cardiac conductivity and excitability, which may lead to dysrhythmias, sometimes leading to death.
  • Allergic Reactions: Allergic-type reactions (eg, anaphylaxis and angioedema) are rare and may occur as a result of hypersensitivity to the local anesthetic or to other formulation ingredients.
  • Chondrolysis: There have been reports of chondrolysis (mostly in the shoulder joint) following intra-articular infusion of local anesthetics, which is an unapproved use.
  • Methemoglobinemia: Cases of methemoglobinemia have been reported with local anesthetic use.

Please refer to full Prescribing Information.

References

  1. Hu D, Onel E, Singla N, Kramer WG, Hadzic A. Pharmacokinetic profile of liposome bupivacaine injection following a single administration at the surgical site. Clin Drug Invest. 2013;33(2):109-115.
  2. Patel MA, Gadsden JC, Nedeljkovic SS, et al. Brachial plexus block with liposomal bupivacaine for shoulder surgery improves analgesia and reduces opioid consumption: results from a multicenter, randomized, double-blind, controlled trial. Pain Med. 2020;21(2):387-400.
  3. Gadsden J, et al. Poster presented at: 48th Annual Regional Anesthesiology and Acute Pain Medicine Meeting; April 20, 2023; Hollywood, FL. Poster 4381.
  4. Schwartz G, Gadsden JC, Gonzales J, et al. A phase 3 active-controlled trial of liposomal bupivacaine via sciatic nerve block in the popliteal fossa after bunionectomy. J Clin Anesth. 2024;94:111402.
  5. Marino J, Scuderi G, Dowling O, Farquhar R, Freycinet B, Overdyk F. Periarticular knee injection with liposomal bupivacaine and continuous femoral nerve block for postoperative pain management after total knee arthroplasty: a randomized controlled trial. J Arthroplasty. 2019;34(3):495-500.
  6. Bramlett K, Onel E, Viscusi ER, Jones K. A randomized, double-blind, dose-ranging study comparing wound infiltration of DepoFoam bupivacaine, an extended-release liposomal bupivacaine, to bupivacaine HCl for postsurgical analgesia in total knee arthroplasty. Knee. 2012;19(5):530-536.
  7. Tirotta CF, de Armendi AJ, Horn ND, et al. A multicenter study to evaluate the pharmacokinetics and safety of liposomal bupivacaine for postsurgical analgesia in pediatric patients aged 6 to less than 17 years (PLAY). J Clin Anesth. 2021;75:110503.
  8. Mustafa HJ, Wong HL, Al‐Kofahi M, Schaefer M, Karanam A, Todd MM. Bupivacaine pharmacokinetics and breast milk excretion of liposomal bupivacaine administered after cesarean birth. Obstet Gynecol. 2020;136(1):70‐76.
  9. Bupivacaine. Drugs and Lactation Database (LactMed). National Library of Medicine. https://www.ncbi.nlm.nih.gov/books/NBK501326/ Last revision July 20, 2020. Accessed Aug 24, 2020.
  10. Ortega D, Viviand X, Lorec AM, Gamerre M, Martin C, Bruguerolleet B. Excretion of lidocaine and bupivacaine in breast milk following epidural anesthesia for cesarean delivery. Acta Anaesthesiol Scand. 1999;43(4):394-397.
  11. Baker PA. Schroeder D. Interpleural bupivacaine for postoperative pain during lactation. Anesth Analg. 1989;69(3):400-402.
  12. Baxter R, Bramlett K, Onel E, Daniels S. Impact of local administration of liposome bupivacaine for postsurgical analgesia on wound healing: a review of data from ten prospective, controlled clinical studies. Clin Ther. 2013;35(3):312-320.
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EXPAREL® (bupivacaine liposome injectable suspension) is indicated to produce postsurgical local analgesia via infiltration in patients aged 6 years and older and regional analgesia in adults via an interscalene brachial plexus nerve block, sciatic nerve block in the popliteal fossa, and an adductor canal block. Safety and efficacy have not been established in other nerve blocks.

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