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 ?
The company's long-acting local analgesic, EXPAREL (bupivacaine liposome injectable suspension) was commercially launched in the United States in April 2012.
Pet therapeutics company Aratana Therapeutics Inc (Nasdaq:PETX) reported on Monday the receipt of approval from the US Food and Drug Administration's Center for Veterinary Medicine (CVM) for an additional vial size in 10 ml for NOCITA (bupivacaine liposome injectable suspension) for the management of pain in dogs and cats.
Myoscience's iovera system will be part of the Pacira non-opioid product portfolio, which currently includes Exparel (bupivacaine liposome injectable suspension), a single-dose, long-acting local and regional analgesic.
The iovera[degrees] system will be part of the Pacira non-opioid product portfolio, which currently includes EXPAREL (bupivacaine liposome injectable suspension), a single-dose, long-acting local and regional analgesic.
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.
Bruce Ramshaw, MD, FACS, and Clinical Associate Professor at Florida State University's College of Medicine, as well as Chairman and CMO of Surgical Momentum, recently began working with Pacira Pharmaceuticals in the development of Exparel (bupivacaine liposome injectable suspension).
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).
The debt refinancing along with a recently announced equity financing for net proceeds of USD63.2m have enhanced the company's balance-sheet strength to pursue its business objectives including the expansion of the indications for its lead postsurgical analgesia product, EXPAREL (bupivacaine liposome injectable suspension), which was commercially launched in the USA last month.
Pet therapeutics company Aratana Therapeutics Inc (Nasdaq:PETX) revealed on Friday that it has filed its supplemental New Animal Drug Application (NADA) for the analgesia NOCITA (bupivacaine liposome injectable suspension) with the US Food and Drug Administration Center for Veterinary Medicine (CVM).
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 company's lead product, EXPAREL (bupivacaine liposome injectable suspension), was approved by the US drug regulator FDA in October 2011 for administration to the surgical site for postsurgical analgesia.
Pharmaceutical company Pacira Pharmaceuticals (NasdaqGS:PCRX) reported on Wednesday the receipt of a Warning Letter from the US Food and Drug Administration's (FDA) Office of Prescription Drug Promotion (OPDP) referencing certain promotional materials on EXPAREL (bupivacaine liposome injectable suspension).