bupivacaine liposome

bupivacaine liposome (injection)

(byoo-pi-vi-kane lye-poe-some) ,

Exparel

(trade name)

Classification

Therapeutic: anesthetics topical local
Pharmacologic: amides
Pregnancy Category: C

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 effects

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.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; cross-sensitivity with other amide local anesthetics (ropivacaine, lidocaine, mepivacaine, prilocaine) may occur; Obstetric: 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 ↑); Obstetric / Lactation / Pediatric: Pregnancy, lactation, and children<18 yr (safety has not been established)

Adverse Reactions/Side Effects

Central nervous system

  • central nervous system toxicity (life-threatening)
  • dizziness
  • drowsiness
  • headache
  • insomnia

Cardiovascular

  • peripheral edema
  • prolonged AV conduction
  • tachycardia

Gastrointestinal

  • constipation (most frequent)
  • nausea (most frequent)
  • vomiting (most frequent)

Dermatologic

  • pruritus

Hematologic

  • anemia

Musculoskeletal

  • back pain
  • muscle spasm

Miscellaneous

  • hypersensitivity reactions including anaphylactoid-like reactions and laryngeal edema (life-threatening)
  • fever
  • procedural pain

Interactions

Drug-Drug interaction

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): 1.3% in 10- and 20-mL single use vials

Nursing implications

Nursing 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 Nursing Diagnoses

Acute pain (Indications)

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 preservative–free 0.9% NaCl 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 1 month prior to opening. Do not use if solution is discolored or has been frozen; freeze indicator turns from green to white if exposed to freezing temperatures.
  • 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.
References in periodicals archive ?
An FDA panel is hosting a meeting on February 14 and 15 to discuss Pacira Pharmaceutical's supplemental New Drug Application for bupivacaine liposome injectable suspension.
Phase 4 clinical trial results for bupivacaine liposome injectable suspension as the foundation of a multimodal analgesic regimen versus a standard opioid-based regimen for postsurgical pain control were published in the January issue of Current Therapeutic Research.
The results found that compared to patients in the standard opioid-based treatment arm - who received IV opioids via patient-controlled analgesia devices - patients who underwent the same procedure and received a bupivacaine liposome injectable suspension experienced the following:
today announced a global licensing agreement for the development and commercialization of bupivacaine liposome injectable suspension for animal health indications.
Any statements in this press release about our future expectations, plans and prospects, including statements about our plans to develop and commercialize a bupivacaine liposome injectable suspension product for animal health indications, the size of the market for such a product and the level and rate of adoption for such a product and other statements containing the words "believes," "anticipates," "plans," "expects," and similar expressions, constitute forward-looking statements within the meaning of The Private Securities Litigation Reform Act of 1995.