Bupivacaine

Tell your doctor if you have ever had an allergic reaction to any type of numbing medicine.

To make sure bupivacaine is safe for you, tell your doctor if you have:

• anemia (lack of red blood cells);

• kidney or liver disease;

• a bleeding or blood clotting disorder;

• syphilis, polio, a brain or spinal cord tumor;

• numbness or tingling;

• chronic back pain, headache caused by surgery;

• low or high blood pressure;

• abnormal curvature of the spine; or

• arthritis.

It is not known whether bupivacaine will harm an unborn baby. Tell your doctor if you are pregnant.

It is not known whether bupivacaine passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby.

Get emergency medical help if you have signs of an allergic reaction: hives, red rash, itching; sneezing, difficulty breathing; severe dizziness, vomiting; swelling of your face, lips, tongue, or throat.

Tell your caregivers at once if you have any of these serious side effects:

• feeling anxious, restless, confused, or like you might pass out;

• problems with speech or vision;

• ringing in the ears, metallic taste, numbness or tingling around your mouth, or tremors;

• seizure (convulsions);

• weak or shallow breathing;

• fast heart rate, gasping, feeling unusually hot;

• slow heart rate, weak pulse;

• urinating less than usual or not at all.

Common side effects include:

• nausea, vomiting;

• chills or shivering;

• headache; or

• back pain.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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 or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Slow heartbeat.
• A heartbeat that does not feel normal.
• Chest pain or pressure or a fast heartbeat.
• Fast breathing.
• Very bad dizziness or passing out.
• Change in balance.
• Feeling confused.
• Restlessness.
• Shakiness.
• Blurred eyesight.
• Ringing in ears.
• Low mood (depression).
• Trouble breathing, slow breathing, or shallow breathing.
• Seizures.
• Very upset stomach or throwing up.
• Feeling very sleepy.
• Feeling very tired or weak.

30 mL
Single-use Ampul

0.5% Bupivacaine
Hydrochloride
Injection, USP

150 mg/30 mL (5 mg/mL)

For NERVE BLOCK, CAUDAL and
EPIDURAL ANESTHESIA.

Not for spinal anesthesia.

10 mL Single-use Teartop Vial

Preservative-Free

0.5% Bupivacaine
Hydrochloride Injection, USP

50 mg/10 mL (5 mg/mL)

For NERVE BLOCK, CAUDAL
and EPIDURAL ANESTHESIA.

Not for spinal
anesthesia.

50 mL Multiple-use Fliptop Vial
25/NDC 0409-1163-01
Rx only

0.5% Bupivacaine
Hydrochloride Injection, USP
250 mg/50 mL (5 mg/mL)

For NERVE BLOCK.
Not for caudal, epidural or spinal anesthesia.

Hospira

10 mL Single-use Teartop Vial

Preservative-Free

0.75% Bupivacaine
Hydrochloride Injection, USP

75 mg/10 mL (7.5 mg/mL)

For EPIDURAL and RETROBULBAR ANESTHESIA.

Not for OBSTETRIC or SPINAL ANESTHESIA.

10 mL Single-use Teartop Vial
Rx only
25/NDC 0409-1165-01

Preservative-Free
0.75% Bupivacaine
Hydrochloride Injection, USP
75 mg/10 mL (7.5 mg/mL)

For EPIDURAL and
RETROBULBAR ANESTHESIA.

Not for OBSTETRIC or SPINAL
ANESTHESIA.

Hospira

(byoo PIV a kane)

• Bupivacaine Spinal
• Marcaine
• Marcaine Preservative Free
• Marcaine Spinal
• P-Care M
• ReadySharp Bupivacaine
• Sensorcaine
• Sensorcaine-MPF
• Sensorcaine-MPF Spinal

Note: Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient. Do not use solutions containing preservatives for caudal or epidural block.

Local anesthesia: Infiltration: 0.25% infiltrated locally; maximum: 175 mg. Note: Aspiration should be performed prior to each injection; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided (Mulroy 2010).

Caudal block (preservative free): 15 to 30 mL of 0.25% or 0.5%

Epidural block (other than caudal block; preservative free): Administer in 3 to 5 mL increments, allowing sufficient time to detect toxic manifestations of inadvertent IV or intrathecal administration: 10 to 20 mL of 0.25% or 0.5%

Surgical procedures requiring a high degree of muscle relaxation and prolonged effects only: 10 to 20 mL of 0.75% (Note: Not to be used in obstetrical cases)

Peripheral nerve block: 5 mL of 0.25% or 0.5%; maximum: 400 mg/day

Sympathetic nerve block: 20 to 50 mL of 0.25%

Retrobulbar anesthesia: 2 to 4 mL of 0.75%

Spinal anesthesia: Preservative free solution of 0.75% bupivacaine in 8.25% dextrose:

Lower extremity and perineal procedures: 1 mL

Lower abdominal procedures: 1.6 mL

Normal vaginal delivery: 0.8 mL (higher doses may be required in some patients)

Cesarean delivery: 1 to 1.4 mL

Combined spinal-epidural (CSE) technique for labor analgesia (off-label dosing [spinal component]): 1.75 to 2.5 mg combined with fentanyl 15 mcg (Eltzschig 2003; Ngan Kee 2014; Whitty 2007).

Combined spinal-epidural (CSE) technique for anesthesia for Cesarean delivery (off-label dosing [spinal component]): 9 to 12 mg combined with fentanyl 15 mcg; in addition to fentanyl, may also include a longer-acting opioid (ie, morphine 100 to 150 mcg) for postoperative analgesia (Santos 2015).

Note: Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient. Do not use solutions containing preservatives for caudal or epidural block.

Caudal block, epidural block, local anesthesia: Adolescents: Refer to adult dosing.

Peripheral or sympathetic nerve block: Adolescents: Refer to adult dosing.

Retrobulbar anesthesia: Adolescents: Refer to adult dosing.

Store at controlled room temperature of 20°C to 25°C (68°F to 77˚F).

Bupivacaine is contraindicated in obstetrical paracervical block anesthesia. Bupivacaine in dextrose injection is contraindicated in patients with severe hemorrhage, severe hypotension or shock, arrhythmias (such as complete heart block) which severely restrict cardiac output, local infection at the site of proposed lumbar puncture, and septicemia.

The 0.75% concentration of bupivacaine is not recommended for obstetrical anesthesia. There have been reports of cardiac arrest with difficult resuscitation or death during epidural anesthesia in obstetrical patients, in most cases following the use of the 0.75% concentration of bupivacaine. Cardiac arrest has occurred following convulsions resulting from systemic toxicity, presumably after accidental intravascular injection. The 0.75% concentration should be saved for use when a high level of muscle relaxation and prolonged effect are required during surgery.

Bupivacaine should not be used for intravenous regional anesthesia (Bier Block).

Bupivacaine should only be used by clinicians well versed in the potential toxicities that may occur with local anesthetics and the management of those toxicities. Adequate oxygen, resuscitative equipment and personnel resources should be immediately available prior to the administration of any local anesthetic.

Spinal anesthetics should not be injected during uterine contractions because the drug may be carried further than desired via spinal fluid current.

The general condition of the patient should be optimized and an intravenous line inserted prior to receiving major blocks. All necessary precautions should be taken to prevent intravascular injection.

The lowest dosage of local anesthetic that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects. The rapid injection of a large volume of local anesthetic solution should be avoided. Bupivacaine should be dosed in increments when possible.

Repeated doses of local anesthetics may cause significant increases in plasma levels due to slow accumulation or slow metabolic degradation. Tolerance to elevated blood levels varies with the status of the patient. Debilitated, elderly, and acutely ill patients should be given reduced doses appropriate for their age and physical status. Local anesthetics should be used with caution in patients with hypotension or heart block. Spinal anesthetics should be used with caution in patients with severe disturbances of cardiac rhythm, shock or heart block.

Careful and constant monitoring of cardiovascular and respiratory vital signs and the patient's state of consciousness is recommended after each local anesthetic injection. Restlessness, anxiety, incoherent speech, lightheadedness, numbness and tingling of the mouth and lips, metallic taste, tinnitus, dizziness, blurred vision, tremors, twitching, depression, or drowsiness may be early warning signs of central nervous system toxicity.

Bupivacaine should be used cautiously in patients with liver disease and cardiovascular abnormalities. Patients with liver disease may not be able to adequately metabolize bupivacaine for excretion increasing the risk for toxic plasma concentrations. Additionally, patients with cardiovascular disease may not be able to compensate for the functional changes associated with the prolongation of atrioventricular conduction induced by amide-type local anesthetics.

Caution is recommended when bupivacaine is used for local anesthesia in the head and neck area. Dosage recommendations should not be exceeded.

Local anesthetics containing antimicrobial preservatives should not be used for epidural or caudal anesthesia. The safety of intrathecal injection of such preservatives has not been established.

Aspiration for blood or cerebrospinal fluid is recommended prior to injecting any local anesthetic, both the original dose and all subsequent doses, to avoid intravascular or subarachnoid injection. However, a negative aspiration does not ensure against an intravascular or subarachnoid injection.

Mixing or the prior or intercurrent use of other local anesthetics with bupivacaine is not recommended due to insufficient data on the clinical use of such mixtures.

Safety and effectiveness of bupivacaine have not been established in pediatric patients less than 12 years of age. Safety and effectiveness of bupivacaine with dextrose have not been established in pediatric patients less than 18 years of age.

The dose of any local anesthetic administered varies with the anesthetic procedure, the area to be anesthetized, the vascularity of the tissues, the number of neuronal segments to be blocked, the depth of anesthesia and degree of muscle relaxation needed, the duration of anesthesia desired, individual tolerance, and the physical condition of the patient. The lowest dosage and concentration that results in desired anesthesia should be used.

Bupivacaine produces complete sensory block at recommended doses, but the effect on motor function differs among the 3 concentrations.

0.25% concentration: Produces partial motor block when used for caudal, epidural, or peripheral nerve block. Should be used for surgeries in which muscle relaxation is not essential, or when muscle relaxation is provided through other means. Onset of action may be slower than with the 0.5% or 0.75% solutions.

0.5% concentration: Provides motor blockade for caudal, epidural, or nerve block, but muscle relaxation may be insufficient for surgeries in which complete muscle relaxation is needed.

0.75% concentration: Produces complete motor block. It is most useful for epidural block in abdominal surgeries requiring total muscle relaxation and for retrobulbar anesthesia. Not for obstetrical anesthesia.

The anesthetic duration of bupivacaine is such that a single dose is adequate for most indications.

Bupivacaine in dextrose injection for spinal anesthesia produces complete sensory and motor block at recommended doses.

For bupivacaine administration, standard textbooks should be consulted for specific techniques and procedures.

Bupivacaine has been assigned to pregnancy category C by the FDA. Animal studies have revealed evidence of embryolethality at doses exceeding the maximum recommended daily human dose and developmental toxicity when administered subcutaneously at clinically relevant doses. There are no controlled data in human pregnancy. Bupivacaine in only recommended for use during pregnancy when benefit outweighs risk. This recommendation does not exclude the use of bupivacaine at term for obstetrical anesthesia or analgesia.

Bupivacaine with a high protein binding capacity has a low fetal/maternal ratio of 0.2 to 0.4. Local anesthetics rapidly cross the placenta. Adverse reactions in the mother and/or neonate are dependent upon the route of administration, procedure, and amount of drug used. Toxic reactions may include alterations in the central nervous system, peripheral vascular tone, and cardiac function. Maternal hypotension during obstetrical procedures has occurred during regional anesthesia. Elevating the patient's legs and positioning on the left side will help to prevent this effect. The fetal heart rate should be continuously monitored.

Bupivacaine is excreted into human milk. The manufacturer recommends that due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or not administer the drug, taking into account the importance of the drug to the mother.

Substance Name

Bupivacaine

CAS Registry Number

38396-39-3

Drug Class

Anesthetics, Local

LactMed Record Number

450

Last Revision Date

20170411

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

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 you have any side effects that bother you or do not go away.

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-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.