Bupivacaine Liposome

Bupivacaine Liposome is a non-opioid postsurgical analgesic used in the management of postsurgical pain. 

• Bupivacaine Liposome is available under various brand names: Exparel

Common side effects of Bupivacaine Liposome include:

• dizziness,
• drowsiness,
• nausea,
• constipation,
• vomiting,
• itching,
• headache,
• back pain, or
• swelling in the hands or feet.

Serious side effects of Bupivacaine Liposome include:

• ringing in the ears;
• feeling restless or anxious;
• light-headedness;
• speech or vision problems, a metallic taste in the mouth;
• numbness or tingling around the mouth;
• tremors, twitching, mood changes;
• fast heart rate, feeling short of breath, feeling unusually hot or cold;
• numbness, weakness, or loss of movement where the injection was given; or
• numbness for several hours after the surgery.

Rare side effects of Bupivacaine Liposome include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Injectable Suspension

• 133 mg/1 mL single-dose vial
• 266 mg/20 mL single-dose vial

Postsurgical Local Analgesia

Adult dosage

Bunionectomy

• 106 mg (8 mL) once via infiltration of the surgical site
• Infiltrate 7 mL into tissues surrounding osteotomy and 1 mL into the subcutaneous tissue

Hemorrhoidectomy

• 266 mg (20 mL) once via infiltration of the surgical site
• Dilute 20 mL with 10 mL of saline, for a total of 30 mL, and divide the mixture into six 5 mL aliquots

Pediatric dosage

• Aged below 6 years: Safety and efficacy not established
• Aged above 6 years: 4 mg/kg (not to exceed 266 mg) once via infiltration of surgical site
• Regional Analgesia via Interscalene Brachial Plexus Nerve Block

Adult dosage

• 133 mg (10 mL) once via infiltration of the surgical site

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Bupivacaine Liposome has severe interactions with the following drugs:
  • chloroprocaine
  • lidocaine
  • mepivacaine
  • ropivacaine
• Bupivacaine Liposome has serious interactions with the following drug:
  • bupivacaine implant
• Bupivacaine Liposome has moderate interactions with the following drug:
  • bupivacaine
• Bupivacaine Liposome has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Obstetrical paracervical block anesthesia; use of bupivacaine for the paracervical block has resulted in fetal bradycardia and death

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Bupivacaine Liposome?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Bupivacaine Liposome?”

Cautions

• For infiltrative use only; do not use for epidural, intrathecal, regional nerve blocks, or intravascular or intra-articular administration; caution to avoid accidental intravascular injection; convulsions and cardiac arrest have occurred following intravascular injection
• Use only in a setting where trained personnel and equipment are available to promptly treat patients who show evidence of neurological or cardiac toxicity
• Monitor cardiovascular/neurological status and vital signs during and after injection
• Bupivacaine and other amide-containing products should be used with caution in patients with impaired cardiovascular function because they may be less able to compensate for functional changes associated with the prolongation of AV conduction produced by these drugs
• CNS reactions may occur, including excitation and/or depression, restlessness, anxiety, dizziness, tinnitus, blurred vision, tremors, or convulsions; other CNS effects may include nausea, vomiting, chills, miosis, twitching, depression, or drowsiness, which may be early warning signs of central nervous system toxicity
• Toxic blood concentrations may depress cardiac conductivity and excitability that leads to AV block, ventricular arrhythmias, and cardiac arrest; additionally, myocardial contractility is depressed and peripheral vasodilation occurs, leading to decreased cardiac output and arterial blood pressure
• Injection of multiple doses of bupivacaine and other amide-containing products may cause significant increases in plasma concentrations with each repeated dose due to slow accumulation of the drug or its metabolites, or slow metabolic degradation; tolerance to elevated blood concentrations varies with the status of the patient
• Allergic-type reactions are characterized by signs such as urticaria, pruritus, erythema, angioneurotic edema (including laryngeal edema), tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly anaphylactoid-like symptoms (including severe hypotension); cross-sensitivity among members of the amide-type local anesthetic group reported; the usefulness of screening for sensitivity has not been definitively established
• Because amide-type local anesthetics, such as bupivacaine, are metabolized by the liver and use cautiously with hepatic disease; greater risk for toxic plasma concentrations with severe hepatic disease
• Sensory and/or motor loss with therapy may occur but is temporary and varies in degree and duration depending on the site of injection and dosage administered and may last for up to 5 days as seen in clinical trials
• The potential sensory and/or motor loss with this drug is temporary and varies in degree and duration depending on the site of injection and dosage administered and may last for up to 5 days
• Avoid additional use of local anesthetics within 96 hours following administration of this drug
• Chondrolysis
  • There have been postmarketing reports of chondrolysis in patients receiving intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures, which is an unapproved use
  • Majority of reported cases of chondrolysis have involved the shoulder joint; cases of glenohumeral chondrolysis described in pediatric patients and adult patients following intra-articular infusions of local anesthetics with and without epinephrine for periods of 48 to 72 hours
  • There is insufficient information to determine whether shorter infusion periods are not associated with these findings; the time of onset of symptoms, such as joint pain, stiffness, and loss of motion can be variable but may begin as early as the second month after surgery
  • Currently, there is no effective treatment for chondrolysis; patients who have experienced chondrolysis have required additional diagnostic and therapeutic procedures, and some required arthroplasty or shoulder replacement
• Methemoglobinemia
  • Cases of methemoglobinemia reported in association with local anesthetic use; although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
  • If local anesthetics must be used, close monitoring for symptoms and signs of methemoglobinemia is recommended; signs of methemoglobinemia may occur immediately or may be delayed some hours after exposure, and are characterized by cyanotic skin discoloration and/or abnormal coloration of the blood
  • Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avert more serious central nervous system and cardiovascular adverse effects, including seizures, coma, arrhythmias, and death; discontinue treatment and any oxidizing agents
  • Depending on the severity of signs and symptoms, patients may respond to supportive care, eg, oxygen therapy, and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen
• Drug interactions overview
  • Other local anesthetics
  • Avoid the use of other local anesthetics within 94 hr after bupivacaine Liposome administration
• Potential for additive adverse effects
  • Increased risk of developing methemoglobinemia if coadministered with other local anesthetics, nitrates/nitrites, acetaminophen, metoclopramide, quinine, sulfasalazine, or other certain antineoplastic agents, antibiotics, antimalarials, or anticonvulsants

Pregnancy & Lactation

• There are no studies conducted on pregnant women
• In animal reproduction studies, embryofetal deaths were observed with SC administration of bupivacaine to rabbits during organogenesis at a dose equivalent to 1.6 times the maximum recommended human dose (MRHD) of 266 mg; SC administration of bupivacaine to rats from implantation through weaning produced decreased pup survival at a dose equivalent to 1.5 times the MRHD
• Based on animal data, advise pregnant women of the potential risks to a fetus
• Contraindicated for obstetrical paracervical block anesthesia (see Contraindications)
• Bupivacaine can rapidly cross the placenta, and when used for epidural, caudal, or pudendal block anesthesia, can cause varying degrees of maternal, fetal, and neonatal toxicity
• Lactation
  • Limited published literature reports that bupivacaine and its metabolite, pipecoloxylidide, are present in human milk at low levels
  • There is no available information on the effects of the drug in the breastfed infant or the effects of the drug on milk production