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bupivacaine liposome (injection)

General

Pronunciation:
byoo-pi-vi-kane lye-poe-some


Trade Name(s)

  • Exparel

Pregnancy Category
Category C

Ther. Class.
anesthetics (topical/local)

Pharm. Class.
amides

Indications

Postoperative single-use infiltration of surgical sites.

Action

Local anesthetics inhibit initiation and conduction of sensory nerve impulses by altering the influx of sodium and efflux of potassium in neurons, slowing or stopping pain transmission. Liposome formulation prolongs the duration of action.

Therapeutic Effect(s):

Lessened postoperative pain.

Pharmacokinetics

Absorption: Depends on amount injected and vascularity of administration site. Some systemic absorption occurs; however action is primarily local.

Distribution: Widely distributed following release from liposomes, high concentrations in highly perfused organs (heart, lungs, liver, brain). Crosses the placenta.

Protein Binding: 95%.

Metabolism and Excretion: Mostly metabolized by the liver, metabolites are primarily renally excreted; 6% excreted unchanged in urine.

Half-life: Following bunionectomy– 34.1 hr; following hemorrhoidectomy– 23.8 hr.

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
infiltrationunknown0.5–2 hr96 hr†
† Pain relief lasted for 24 hr.

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity; cross-sensitivity with other amide local anesthetics (ropivacaine, lidocaine, mepivacaine, prilocaine) may occur;
  • OB: Obstetrical paracervical block anesthesia (may cause fetal bradycardia/death).

Use Cautiously in:

  • Impaired cardiovascular function;
  • Hepatic disease (blood levels ↑ in severe hepatic impairment);
  • Renal impairment (risk of toxic reactions may be ↑);
  • OB: Lactation:Pedi: Pregnancy, lactation, and children<18 yr (safety not established)

Adverse Reactions/Side Effects

CNS: CENTRAL NERVOUS SYSTEM TOXICITY, dizziness, drowsiness, headache, insomnia

CV: peripheral edema, prolonged AV conduction, tachycardia

GI: constipation, nausea, vomiting

Derm: pruritus

Hemat: anemia

MS: back pain, muscle spasm

Misc: HYPERSENSITIVITY REACTIONS INCLUDING ANAPHYLACTOID-LIKE REACTIONS AND LARYNGEAL EDEMA, fever, procedural pain

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • Should not be administered concurrently with local lidocaine, wait at least 20 minutes before infiltration with bupivacaine liposome.
  • Should not be admixed with other local anesthetics.
  • Should not be used within 96 hr of other formulations of bupivacaine; overall exposure and risk of toxicity/adverse reactions will be ↑.

Route/Dosage

Infiltration: (Adults) Bunionectomy– 106 mg (8 mL) given as 7 mL into osteotomy and 1 mL into subcutaneous tissue; Hemorrhoidectomy– 266 mg (20 mL) diluted to a volume of 30 mL and given as six 5 mL aliquots.

Availability

Liposome injectable suspension (for infiltration only): 13.3 mg/mL

Assessment

  • Assess infiltrated area for pain following administration and periodically during therapy.
  • Monitor cardiovascular and respiratory status (vital signs, level of consciousness) constantly following infiltration. Notify health care professional immediately if signs of cardiac toxicity (atrioventricular block, ventricular arrhythmias, cardiac arrest) occur.
  • Monitor for central nervous system toxicity. Notify health care professional promptly if they occur. Early signs of central nervous system toxicity include (restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, depression or drowsiness).
  • Monitor for signs and symptoms of allergic reactions (urticaria, pruritus, erythema, angioneurotic edema, laryngeal edema, tachycardia, sneezing, nausea, vomiting, syncope, excessive sweating, elevated temperature, severe hypotension). Have resuscitative equipment available.

Potential Diagnoses

Implementation

  • Do not confuse with propofol. In a syringe suspension is milky white and may be mistaken for other medications. Label syringe to ensure dose is not administered IV.
  • Infiltration: May be administered undiluted or diluted with 0.9% NaCl or Lactated Ringers solution up to 0.89 mg/mL. Invert vial multiple times to re-suspend particles immediately prior to withdrawal from vial. Injected with a 25 gauge or larger bore needle slowly into soft tissues of surgical site with frequent aspiration to check for blood and minimize risk of intravascular injection. Use diluted suspension within 4 hrs of preparation in a syringe. Vials are for single dose; discard unused portions. May be stored in refrigerator for up to 30 days prior to opening. Do not use if solution is discolored or has been frozen or exposed to high temperatures for extended period.
  • Do not administer in an area with povidone iodine until dry. If administered with other non-bupivacaine local anesthetics, administer other agents first and wait at least 20 min before infiltrating with bupivacaine liposome. Do not administer other forms of bupivacaine within 96 hr of bupivacaine liposome.

Patient/Family Teaching

  • Inform patient that infiltration may cause temporary loss of sensation or motor activity in infiltrated area.
  • Instruct patient to notify health care professional of pregnancy is known or suspected or if breast feeding.

Evaluation/Desired Outcomes

Prolongation of postoperative analgesia.

bupivacaine liposome (injection) is a sample topic from the Davis's Drug Guide.

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Citation

Quiring, Courtney, et al. "Bupivacaine Liposome (injection)." Davis's Drug Guide, 16th ed., F.A. Davis Company, 2019. Emergency Central, emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110535/all/bupivacaine_liposome__injection_.
Quiring C, Sanoski CA, Vallerand AH. Bupivacaine liposome (injection). Davis's Drug Guide. 16th ed. F.A. Davis Company; 2019. https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110535/all/bupivacaine_liposome__injection_. Accessed April 24, 2019.
Quiring, C., Sanoski, C. A., & Vallerand, A. H. (2019). Bupivacaine liposome (injection). In Davis's Drug Guide. Available from https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110535/all/bupivacaine_liposome__injection_
Quiring C, Sanoski CA, Vallerand AH. Bupivacaine Liposome (injection) [Internet]. In: Davis's Drug Guide. F.A. Davis Company; 2019. [cited 2019 April 24]. Available from: https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110535/all/bupivacaine_liposome__injection_.
* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - bupivacaine liposome (injection) ID - 110535 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://emergency.unboundmedicine.com/emergency/view/Davis-Drug-Guide/110535/all/bupivacaine_liposome__injection_ PB - F.A. Davis Company ET - 16 DB - Emergency Central DP - Unbound Medicine ER -