Non-opioid EXPAREL has a proven safety profile

DepoFoam® Technology provides reliable slow release of bupivacaine over 96 hours1,2

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 thresholds3-7

  • Central nervous system symptoms occurs at a plasma concentration of ≈2000 ng/mL with bupivacaine HCl4
  • Cardiac toxicity is associated with blood levels of ≥4000 ng/mL5
  • Pharmacokinetics demonstrate plasma levels of bupivacaine that can persist for 96 hours3,8
  • At all doses studies, plasma bupivacaine levels are maintained well below toxic thresholds1-3,5,7-8
  • 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

Additional safety information for EXPAREL

Excretion of liposomal bupivacaine in breast milk administered after cesarean birth9

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 minimal10,11

  • Serum bupivacaine levels taken from an infant sample were shown to be undectectable12
  • Bupivacaine is not orally absorbed, therefore amounts received by the infant are small and have not caused any adverse effects in breastfed infants10

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.13

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.13

CNS, central nervous systems; ISBPNB, interscalene brachial plexus nerve block; TKA, total knee arthroplasty.