Bupivacaine (Local)

Drug class: Antineoplastic Agents

Usage of Bupivacaine (Local)

Local or Regional Anesthesia or Analgesia

Local or regional anesthesia or analgesia in surgical, obstetrical, dental, diagnostic, and therapeutic procedures.

Available as conventional Bupivacaine hydrochloride preparations with or without epinephrine or as a liposomal injection containing bupivacaine in an aqueous suspension of multivesicular liposomes (Exparel).

Conventional preparations are used for local infiltration and nerve block techniques including peripheral, sympathetic, epidural (including caudal), retrobulbar, and dental block. Do not use 0.75% concentration for obstetrical anesthesia. (See Boxed Warning.) A hyperbaric solution containing 0.75% bupivacaine hydrochloride in 8.25% dextrose is used for spinal anesthesia.

Liposomal bupivacaine (Exparel) is used for local infiltration or interscalene brachial plexus nerve block to provide postsurgical analgesia; safety and efficacy not established for other nerve blocks. Because of possible differences in physiochemical and functional properties, do not use liposomal bupivacaine interchangeably with other bupivacaine-containing preparations.

Local anesthetics should be used as a component of multimodal analgesia (i.e., simultaneous use of a combination of analgesic drugs and techniques that target different mechanisms) in the management of postoperative pain.

Studies comparing relative efficacy of liposomal bupivacaine and conventional bupivacaine hydrochloride for postsurgical analgesia have shown variable results.

Do not use for obstetric paracervical block.

Relate drugs

How to use Bupivacaine (Local)

General

Dispensing and Administration Precautions

  • Administer only by clinicians experienced in the diagnosis and management of toxicities and other complications associated with local anesthetics.
  • Resuscitative equipment, oxygen, drugs, and personnel required for treatment of adverse reactions should be immediately available.
  • Administer slowly in incremental doses to reduce risk of adverse effects (e.g., local anesthetic systemic toxicity).
  • Perform frequent aspirations for blood or cerebrospinal fluid (when applicable) to avoid intravascular administration and to either confirm entry into the subarachnoid space (for spinal anesthesia) or avoid inadvertent subarachnoid injection.
  • During major regional nerve blocks, administer IV fluids via an indwelling catheter to ensure a functioning IV pathway.
  • Injections into the head and neck area (e.g., retrobulbar, dental, or stellate ganglion blocks) require particular care; serious adverse effects reported due to complications from the anesthetic technique.
  • Carefully and constantly monitor patients for possible cardiovascular, respiratory, or CNS complications during and after administration.

    • Administration

    Injection

    For solution and drug compatibility information, see Compatibility under Stability.

    Administer conventional bupivacaine hydrochloride preparations by local infiltration, peripheral nerve block, retrobulbar block, sympathetic block, lumbar epidural block, caudal block, or dental block. Administer 0.75% bupivacaine hydrochloride in 8.25% dextrose solution by subarachnoid injection for spinal anesthesia.

    Administer liposomal bupivacaine (Exparel) by local infiltration or interscalene brachial plexus nerve block; do not administer liposomal formulation by epidural or intrathecal routes, or for other regional nerve blocks.

    Do not administer using Bier block technique (IV regional anesthesia) due to risk of cardiac arrest and death.

    Has been administered by continuous intra-articular infusion† [off-label] (e.g., for control of postoperative pain); however, such use associated with chondrolysis. (See Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics under Cautions.)

    Consult specialized references for specific techniques and procedures for administering local anesthetics.

    Do not use liposomal bupivacaine interchangeably with other bupivacaine formulations.

    Do not use bupivacaine solutions containing preservatives for epidural or caudal block; discard partially used solutions that do not contain preservatives.

    Liposomal Bupivacaine

    May administer undiluted or diluted (if an increased volume of drug is necessary to cover a larger surgical area).

    If dilution desired, dilute with preservative-free 0.9% sodium chloride injection or lactated Ringer’s injection up to a final concentration of 0.89 mg/mL (1:14 dilution by volume); do not use sterile water for injection or other hypotonic solution since disruption of liposomal particles may occur. Use diluted suspension within 4 hours of preparation in a syringe.

    Invert vial multiple times to resuspend drug particles immediately prior to drug withdrawal. Administer using 25-gauge or larger bore needle. Do not filter.

    When administered concomitantly with lidocaine (or other non-bupivacaine local anesthetic), immediate release of free (unencapsulated) bupivacaine may occur, potentially resulting in toxic plasma concentrations. Delay administration of liposomal bupivacaine for ≥20 minutes after administration of lidocaine.

    Compatibility between liposomal bupivacaine and conventional bupivacaine hydrochloride is concentration dependent. May administer bupivacaine hydrochloride and liposomal bupivacaine simultaneously in the same syringe, or inject bupivacaine hydrochloride immediately before liposomal bupivacaine as long as the ratio (based on mg dose) of conventional to liposomal drug does not exceed 1:2. Consider potential for additive toxic effects when the drugs are used concomitantly. Avoid additional administration of local anesthetics for ≥96 hours after liposomal bupivacaine is administered.

    Avoid contact with topical antiseptics (e.g., povidone iodine); allow topical antiseptic to dry before liposomal bupivacaine is administered.

    Potential Administration Errors

    Because of similarity in appearance (milky white suspension), potential exists for confusion between liposomal bupivacaine and propofol.

    Take special precautions (e.g., proper labeling of syringes, storage segregation, routine double-checks) to ensure that such confusion does not occur.

    If mistaken for propofol, inadvertent IV administration of liposomal bupivacaine may occur and cause substantial patient harm (e.g., cardiac arrhythmias, arrest).

    Instructions for treatment of bupivacaine toxicity should be readily available in all surgical areas where liposomal bupivacaine is used.

    Dosage

    Conventional preparations available as bupivacaine hydrochloride, as fixed combination containing bupivacaine hydrochloride and epinephrine bitartrate, and as bupivacaine hydrochloride in dextrose injection; dosage expressed in terms of bupivacaine hydrochloride.

    Liposomal preparation available as bupivacaine (as free base) in suspension of multivesicular liposomes.

    Individualize dosage based on anesthetic procedure, degree of anesthesia required, surgical site, and individual patient response. Use lowest effective dosage.

    Prior to epidural anesthesia, administer test dose and monitor patient (e.g., pulse, BP, signs of spinal block) to detect accidental intravascular or subarachnoid injection. Test dose should contain 10–15 mcg epinephrine (when clinical conditions permit) and 10–15 mg (2–3 mL of a 0.5% solution) of bupivacaine hydrochloride (or equivalent dose of another local anesthetic). Following injection of test dose, monitor for increase in heart rate.

    Pediatric Patients

    Local or Regional Anesthesia/Analgesia Local Infiltration, Peripheral/Sympathetic Nerve Block, Lumbar Epidural/Caudal Block

    Children ≥12 years of age: Manufacturer makes no specific dosage recommendations; individualize dosage. (See Pediatric Use under Cautions.)

    Adults

    Local or Regional Anesthesia/Analgesia Local Infiltration

    Conventional bupivacaine hydrochloride: Administer 0.25% solution (with or without epinephrine) up to maximum recommended dose (see Prescribing Limits under Dosage and Administration).

    Liposomal bupivacaine: Single dose of up to 266 mg recommended. In clinical studies, patients undergoing bunionectomy received a single dose of 106 mg (total volume of 8 mL, with 7 mL infiltrated into tissues surrounding osteotomy and 1 mL infiltrated throughout the suBCutaneous tissue). Patients undergoing hemorrhoidectomy received a single dose of 266 mg (20 mL of drug diluted with 10 mL of 0.9% sodium chloride injection); the total volume of 30 mL was divided into 5-mL increments and infiltrated into 6 sites in the perianal tissue using a standard anal block procedure with moving-needle technique.

    Lumbar Epidural Block (Bupivacaine Hydrochloride)

    0.75% solution is for single-dose use; not for intermittent epidural technique. Reserve for surgical procedures requiring a high degree of muscle relaxation and prolonged anesthetic effect.

    0.75% solution is not for obstetrical anesthesia; in obstetrics, use 0.25 or 0.5% solutions only. (See Boxed Warning and see Risks Associated with Obstetrical Use of Bupivacaine Hydrochloride 0.75% Injection under Cautions.)

    75–150 mg (10–20 mL) of bupivacaine hydrochloride 0.75% solution (with or without epinephrine) produces complete motor blockade. Administer in incremental doses of 3–5 mL. Allow sufficient time between doses to detect toxic manifestations of unintentional intravascular or intrathecal injection.

    50–100 mg (10–20 mL) of bupivacaine hydrochloride 0.5% solution (with or without epinephrine) produces moderate to complete motor blockade. Administer in incremental doses of 3–5 mL. Allow sufficient time between doses to detect toxic manifestations of unintentional intravascular or intrathecal injection.

    25–50 mg (10–20 mL) of bupivacaine hydrochloride 0.25% solution (with or without epinephrine) produces partial motor blockade.

    Caudal Block (Bupivacaine Hydrochloride)

    75–150 mg (15–30 mL) of bupivacaine hydrochloride 0.5% solution (with or without epinephrine) produces moderate to complete motor blockade.

    37.5–75 mg (15–30 mL) of bupivacaine hydrochloride 0.25% solution (with or without epinephrine) produces moderate motor blockade.

    Peripheral Nerve Block (Bupivacaine Hydrochloride)

    25 mg (5 mL) to maximum dosage (see Prescribing Limits under Dosage and Administration) of bupivacaine hydrochloride 0.5% solution (with or without epinephrine) produces moderate to complete motor blockade.

    12.5 mg (5 mL) to maximum dosage (see Prescribing Limits under Dosage and Administration) of bupivacaine hydrochloride 0.25% solution (with or without epinephrine) produces moderate to complete motor blockade.

    Interscalene Brachial Plexus Nerve Block (Liposomal Bupivacaine)

    Single dose of 133 mg (10 mL) of liposomal bupivacaine recommended based on a study in patients undergoing total shoulder arthroplasty or rotator cuff repair.

    Retrobulbar Block (Bupivacaine Hydrochloride)

    15–30 mg (2–4 mL) of bupivacaine hydrochloride 0.75% solution (with or without epinephrine) produces complete motor blockade.

    Sympathetic Block (Bupivacaine Hydrochloride)

    50–125 mg (20–50 mL) of bupivacaine hydrochloride 0.25% solution.

    Dental Infiltration or Block Injection into Maxillary and Mandibular Area (Bupivacaine Hydrochloride)

    9 mg (1.8 mL) up to 90 mg (18 mL) of bupivacaine hydrochloride 0.5% solution per dental sitting.

    Subarachnoid (Spinal) Block for Vaginal Delivery (Bupivacaine Hydrochloride 0.75% in Dextrose 8.25%)

    6 mg (0.8 mL) of bupivacaine hydrochloride 0.75% in dextrose 8.25% injection produces complete motor and sensory block.

    Subarachnoid (Spinal) Block for Cesarean Section (Bupivacaine Hydrochloride 0.75% in Dextrose 8.25%)

    7.5–10.5 mg (1–1.4 mL) of bupivacaine hydrochloride 0.75% in dextrose 8.25% injection produces complete motor and sensory block.

    Subarachnoid (Spinal) Block for Lower Extremity and Perineal Procedures (Bupivacaine Hydrochloride 0.75% in Dextrose 8.25%)

    7.5 mg (1 mL) of bupivacaine hydrochloride 0.75% in dextrose 8.25% injection produces complete motor and sensory block.

    Subarachnoid (Spinal) Block for Lower Abdominal Procedures (Bupivacaine Hydrochloride 0.75% in Dextrose 8.25%)

    12 mg (1.6 mL) of bupivacaine hydrochloride 0.75% in dextrose 8.25% injection produces complete motor and sensory block.

    Prescribing Limits

    Adults

    Local or Regional Anesthesia/Analgesia Bupivacaine Hydrochloride Local Infiltration, Peripheral/Sympathetic Nerve Block, Epidural/Caudal Block, Retrobulbar Block, Dental Block

    Individualize maximum dosage limit for each patient.

    Most experience to date has involved single doses up to 175 mg (without epinephrine) or 225 mg (with epinephrine 1:200,000).

    Until further experience, manufacturer recommends that a maximum dose of 400 mg not be exceeded in any 24-hour period.

    Liposomal Bupivacaine Local Infiltration

    Maximum dose of 266 mg.

    Special Populations

    Hepatic Impairment

    Use with caution and monitor carefully in patients with liver disease.

    Renal Impairment

    Consider possibility of increased risk of toxicity in patients with renal impairment and select appropriate dosage accordingly.

    Geriatric Patients

    Geriatric patients may require reduced dosages.

    Other Populations

    Patients with cardiac disease, debilitated patients, and acutely ill patients may require reduced dosages. Reduced dosages also may be required in patients with increased intra-abdominal pressure (including obstetrical patients) undergoing spinal anesthesia.

    Warnings

    Contraindications

  • Obstetrical paracervical block (this technique has resulted in fetal bradycardia and death).
  • Contraindications to spinal anesthesia: Severe hemorrhage, severe hypotension or shock, arrhythmias (e.g., complete heart block) that severely restrict cardiac output, local infection at site of lumbar puncture, and septicemia.
  • Known hypersensitivity to bupivacaine, other local anesthetics of the amide type, or any ingredients in the formulation.

    • Warnings/Precautions

    Warnings

    Risks Associated with Obstetrical Use of Bupivacaine Hydrochloride 0.75% Injection

    Risk of seizures, cardiac arrest, difficult resuscitation, or death following obstetrical epidural block (possibly due to systemic toxicity secondary to unintentional intravascular injection) with 0.75% bupivacaine hydrochloride. (See Boxed Warning.)

    Not recommended for obstetrical anesthesia. Reserve for surgical procedures requiring a high degree of muscle relaxation and prolonged anesthetic effect.

    Administration Precautions

    Because of the potential for serious adverse effects, take special precautions during administration. (See General and see Potential Administration Errors under Dosage and Administration.)

    Ensure that oxygen, resuscitative equipment, drugs, and personnel required for treatment of adverse reactions are immediately available. Delay in proper management of dose-related toxicity may result in acidosis, cardiac arrest, and, possibly, death.

    Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics

    Chondrolysis (necrosis and destruction of articular cartilage) reported in patients receiving continuous intra-articular infusions of local anesthetics, administered for 48–72 hours via elastomeric infusion devices, for treatment of postoperative pain. Primarily observed in the shoulder joint following arthroscopic or other shoulder surgery. May result in long-term disability; often requires intervention (e.g., debridement, arthroplasty). Not known whether the drug, infusion device, and/or other factors contributed to the development of chondrolysis. Neither local anesthetics nor elastomeric infusion devices are approved for use for continuous intra-articular infusion therapy.

    Accidental Intravascular Injection

    Accidental intravascular injection may result in confusion, seizures, CNS excitement and/or depression, myocardial depression, coma, and/or respiratory arrest. (See CNS Effects and also see Cardiovascular Effects, under Cautions.)

    Aspirate prior to administration to guard against intravascular injection.

    Warnings Associated with Spinal Anesthesia

    Do not inject spinal anesthetics during uterine contractions, since spinal fluid current may carry drug further cephalad than desired.

    Epinephrine Administration

    Some bupivacaine hydrochloride preparations contain epinephrine, which may cause ischemic injury or necrosis. Consider usual precautions associated with epinephrine administration. (See Cardiovascular Effects under Cautions.)

    Sensitivity Reactions

    Hypersensitivity Reactions and Cross Hypersensitivity

    Allergic reactions are rare. May be caused by sensitivity to the local anesthetic or other ingredient in the formulation (e.g., methylparaben, sulfites).

    Manifestations include urticaria, pruritus, erythema, angioedema (including laryngeal edema), tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and anaphylactoid reactions (including severe hypotension).

    Cross hypersensitivity between amide-type local anesthetics reported.

    Sulfite Sensitivity

    Some epinephrine-containing bupivacaine preparations contain sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.

    General Precautions

    CNS Effects

    Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse CNS effects (e.g., restlessness, anxiety, dizziness, tinnitus, blurred vision, tremors, drowsiness, seizures).

    Carefully monitor level of consciousness after each local anesthetic injection.

    Cardiovascular Effects

    Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse cardiovascular effects (e.g., decreased cardiac output, heart block, hypotension, bradycardia, ventricular arrhythmias, cardiac arrest). Carefully monitor cardiovascular and respiratory vital signs after each local anesthetic injection.

    Use with caution in patients with impaired cardiovascular function, hypotension, or heart block.

    Possible peripheral vasodilation and hypotension following spinal anesthesia; monitor BP carefully, particularly in early phases of anesthesia. Use spinal anesthesia with caution in patients with severe disturbances of cardiac rhythm, shock, or heart block.

    Some bupivacaine hydrochloride preparations contain epinephrine; risk of exaggerated vasoconstrictor response in patients with hypertensive vascular disease. Use with caution and in carefully restricted quantities in areas of the body supplied by end arteries or having otherwise compromised blood supply (e.g., digits, nose, external ear, penis).

    Familial Malignant Hyperthermia

    Many drugs used during the conduct of anesthesia may trigger familial malignant hyperthermia; not known whether amide-type local anesthetics trigger this reaction. However, standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile BP, and metabolic acidosis may precede temperature elevation. If familial malignant hyperthermia is confirmed, discontinue triggering agent and initiate appropriate therapy (e.g., oxygen, dantrolene) and other supportive measures.

    Preexisting Conditions Precluding Use of Spinal Anesthesia

    Conditions that may preclude the use of spinal anesthesia (depending upon the clinician’s evaluation of the situation and ability to manage potential complications) include preexisting CNS disease (e.g., disease associated with pernicious anemia, poliomyelitis, syphilis, tumor); hematological disorders predisposing to coagulopathies; current anticoagulant therapy; chronic backache; preoperative headache; hypotension or hypertension; technical problems (persistent paresthesias, persistent bloody tap); arthritis or spinal deformity; extremes of age; and psychosis or other causes of poor patient cooperation.

    Use of Fixed Combination

    When used in fixed combination with other agents, consider the cautions, precautions, and contraindications associated with the concomitant agents.

    Specific Populations

    Pregnancy

    No adequate and well-controlled studies in pregnant women; developmental toxicity and embryofetal deaths (following sub-Q administration) observed in animals. Use during pregnancy only if potential benefit justifies potential risk to fetus.

    Labor and Delivery

    Maternal hypotension reported. To prevent decreases in BP, elevate patient’s legs and position patient on her left side. Monitor fetal heart rate continuously; electronic fetal monitoring highly advisable.

    Epidural anesthesia may prolong second stage of labor (by removing parturient’s reflex urge to bear down or by interfering with motor function); may increase need for forceps assistance.

    Possible diminished muscle strength and tone on neonate’s first or second day of life.

    Lactation

    Distributed into milk. Discontinue nursing or the drug.

    Pediatric Use

    Conventional bupivacaine hydrochloride with or without epinephrine not recommended in children <12 years of age.

    Bupivacaine hydrochloride in dextrose injection for spinal anesthesia not recommended in children <18 years of age.

    Efficacy and safety of liposomal bupivacaine not established in pediatric patients.

    Continuous infusions in children have resulted in high plasma concentrations (which may increase the risk of adverse cardiovascular effects) and seizures.

    Geriatric Use

    Geriatric patients ≥65 years of age, particularly those with hypertension, may be more sensitive to the hypotensive effects of bupivacaine. Some manufacturers recommend reduced dosages.

    Possible increased risk of toxicity in geriatric patients with renal impairment; monitor renal function.

    No overall differences in safety or efficacy of liposomal bupivacaine in geriatric patients ≥65 years of age compared with younger patients.

    Hepatic Impairment

    Possible increased risk of toxicity, particularly in patients with severe hepatic impairment. Use with caution and closely monitor for local anesthetic systemic toxicity in patients with moderate to severe hepatic impairment. (See Hepatic Impairment under Dosage and Administration.)

    Renal Impairment

    Substantially excreted by kidneys; possible increased risk of toxicity in patients with renal impairment. (See Renal Impairment under Dosage and Administration.)

    Common Adverse Effects

    Adverse effects are similar to those of other amide-type local anesthetics. Most common adverse effects are usually a result of excessive plasma concentrations and include CNS and cardiovascular effects. (See CNS Effects and also see Cardiovascular Effects, under Cautions.)

    Most common serious adverse effects following spinal anesthesia include hypotension, respiratory paralysis, and underventilation.

    Most common adverse effects of liposomal bupivacaine via local infiltration include nausea, constipation, vomiting; most common adverse effects of liposomal bupivacaine via interscalene brachial plexus nerve block include nausea, pyrexia, and constipation.

    What other drugs will affect Bupivacaine (Local)

    Consider usual drug interactions associated with epinephrine administration.

    Specific Drugs

    Drug

    Interaction

    Comments

    Anesthetics, general

    Bupivacaine preparations containing epinephrine: Possible serious cardiac arrhythmias due to epinephrine component

    Antidepressants, tricyclics

    Bupivacaine preparations containing epinephrine: Possible severe, prolonged hypertension due to epinephrine component

    Avoid concomitant use; if concomitant use is necessary, carefully monitor patient

    Butyrophenones

    Bupivacaine preparations containing epinephrine: Possible reduction or reversal of pressor effect of epinephrine

    Ergot alkaloid oxytocics (ergonovine, methylergonovine)

    Bupivacaine preparations containing epinephrine: Possible severe, persistent hypertension or cerebrovascular accidents due to epinephrine component

    Avoid concomitant use

    MAO inhibitors

    Bupivacaine preparations containing epinephrine: Possible severe, prolonged hypertension due to epinephrine component

    Avoid concomitant use; if concomitant use is necessary, carefully monitor patient

    Phenothiazines

    Bupivacaine preparations containing epinephrine: Possible reduction or reversal of pressor effect of epinephrine

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