Exparel

Generic name: bupivacaine liposome
Drug class: Local injectable anesthetics

Medically reviewed by A Ras MD.

What is Exparel?

Exparel is a prescription medicine that is used to ease pain at the surgery site.

Description

EXPAREL is a sterile, non-pyrogenic white to off-white preservative-free aqueous suspension consisting of proprietary multivesicular liposomes (pMVL) containing bupivacaine. Bupivacaine is present at a concentration of 13.3 mg/mL. After injection of EXPAREL, bupivacaine is released from the multivesicular liposomes over a period of time.

Active Ingredient

Bupivacaine is related chemically and pharmacologically to the amide-type local anesthetics. It is a homologue of mepivacaine and is related chemically to lidocaine. All three of these anesthetics contain an amide linkage between the aromatic nucleus and the amino, or piperidine group. They differ in this respect from the procaine-type local anesthetics, which have an ester linkage. Chemically, bupivacaine is 1-butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide with a molecular weight of 288.4. Bupivacaine has the following structural formula:

Lipid Formulation

The median diameter of the liposome particles ranges from 24 to 31 μm. The liposomes are suspended in a 0.9% sodium chloride solution. Each vial contains bupivacaine at a nominal concentration of 13.3 mg/mL. Inactive ingredients and their nominal concentrations are: cholesterol, 4.7 mg/mL; 1, 2-dipalmitoyl-sn-glycero-3 phospho-rac-(1-glycerol) (DPPG), 0.9 mg/mL; tricaprylin, 2.0 mg/mL; 1, 2-dierucoylphosphatidylcholine (DEPC), 8.2 mg/mL; and phosphoric acid to adjust pH. The pH of EXPAREL is in the range of 5.8 to 7.4.

Liposomal encapsulation or incorporation in a lipid complex can substantially affect a drug’s functional properties relative to those of the unencapsulated or nonlipid-associated drug. In addition, different liposomal or lipid-complexed products with a common active ingredient may vary from one another in the chemical composition and physical form of the lipid component. Such differences may affect functional properties of these drug products. Do not substitute.

Mechanism of Action

Local anesthetics block the generation and the conduction of nerve impulses presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: (1) pain, (2) temperature, (3) touch, (4) proprioception, and (5) skeletal muscle tone.

Before taking Exparel, tell your doctor:

If you are allergic to Exparel; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.

This medicine may interact with other drugs or health problems.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take Exparel with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take Exparel?

Tell all of your health care providers that you take Exparel. This includes your doctors, nurses, pharmacists, and dentists.
This medicine may cause dizziness. If this happens, do not drive or do other tasks or actions that call for you to be alert. Talk with your doctor.
This medicine may cause short-term loss of feeling and motor activity in the body. This may last for up to 5 days. Do not try to get out of bed or do other tasks or actions until feeling and motor activity have returned to normal.
A severe blood problem called methemoglobinemia has happened with drugs like this one. The risk may be raised in people who have glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. The risk may also be raised while taking certain other drugs and in infants younger than 6 months of age. Tell your doctor if you have ever had methemoglobinemia.
Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using Exparel while you are pregnant.
Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is Exparel best taken?

Use Exparel as ordered by your doctor. Read all information given to you. Follow all instructions closely.

It is given as a shot.
Your doctor will give Exparel.

What do I do if I miss a dose?

Call your doctor to find out what to do.

What are the side effects of Exparel that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Signs of high or low blood pressure like very bad headache or dizziness, passing out, or change in eyesight.
Signs of methemoglobinemia like a blue or gray color of the lips, nails, or skin; a heartbeat that does not feel normal; seizures; very bad dizziness or passing out; very bad headache; feeling very sleepy; feeling tired or weak; or shortness of breath. This effect is rare but may be deadly if it happens.
Change in balance.
Restlessness.
Anxiety.
Change in speech.
Change in taste.
Dizziness or passing out.
Feeling lightheaded, sleepy, confused, or having blurred eyesight.
Ringing in ears.
Shakiness.
Twitching.
Low mood (depression).
Feeling nervous and excitable.
Seizures.
Upset stomach or throwing up.
Fever or chills.
Small pupils.
Chest pain or pressure or a fast heartbeat.
Slow heartbeat.
Sneezing.
Sweating a lot.
Joint pain.
Joint stiffness.
Weakness, numbness, or tingling.
Swelling in the arms or legs.
Feeling very tired or weak.
Trouble passing urine.

What are some other side effects of Exparel?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

Headache.
Trouble sleeping.
Muscle spasm.
Back pain.
Feeling tired or weak.
Hiccups.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.