bupivacaine liposome

(redirected from Exparel)

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 ?
Pacira Pharmaceuticals, has won approval from the US Food and Drug Administration (FDA) for an additional bulk manufacturing suite, referred to as Suite C, for Exparel (bupivacaine liposome injectable suspension).
EXPAREL and two other products have utilized the Pacira proprietary product delivery technology DepoFoam([R]), a unique platform that encapsulates drugs without altering their molecular structure and then releases them over a desired period of time.
Pacira's lead candidate is EXPAREL, an injectable local anesthetic.
Specifically, on April 16, 2015, PCRX announced that it received a subpoena from the DoJ requiring the production of a broad range of documents pertaining to marketing and promotional practices related to the product EXPAREL.
The Company's flagship product, EXPAREL (bupivacaine liposome injectable suspension), a non-opioid local analgesic for postsurgical pain control, was commercially launched in the United States in April 2012.
The complaint alleges that the Company misstated and/or failed to disclose that it: (a) overstated the efficacy of its product EXPAREL; (b) improperly promoted EXPAREL as able to work for up to 72 hours despite it being only approved for 24-hour pain relief; (c) improperly claimed EXPAREL as safe and effective for use in cholecystectomy and colectomy, though its approved labeling does not provide for such use; and (d) derives a substantial portion of its revenues from off-label marketing.
Pacira intends to use approximately $30 million of the net proceeds of the offering to repay all amounts outstanding under, and to terminate, its senior secured credit facility, and the remainder of the net proceeds from the offering (including from any exercise by the initial purchasers of their option to purchase additional notes) to fund the continued commercialization of EXPAREL[R] and the development of additional indications for EXPAREL and for general corporate purposes.
Its product pipeline includes EXPAREL, which has completed Phase III clinical trials for postsurgical analgesia-nerve block administration.
Through 2018, market growth attributable to a growing patient population and continued uptake of several branded pain therapies-most notably Mallinckrodt's Ofirmev and Pacira's Exparel in the United States and fast-acting fentanyl formulations across all markets under study-will be tempered by generic erosion of several sales-leading pain therapies, such as Pfizer/Astellas' Celebrex/Celecox.
Specifically, the action alleges that during the Class Period, Pacira falsely stated that one its drugs, EXPAREL, was effective for pain relief for up to 72 hours and safe for use in cholecystectomy and colectomy procedures, and failed to disclose that a substantial portion of the Company's revenues were derived from off-label marketing.