Skip to Content

Bupivacaine

Pronunciation

(byoo PIV a kane)

Index Terms

  • Bupivacaine HCl
  • Bupivacaine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Injection, as hydrochloride:

Marcaine: 0.25% (50 mL); 0.5% (50 mL) [contains methylparaben]

Sensorcaine: 0.25% (50 mL); 0.5% (50 mL) [contains methylparaben]

Sensorcaine-MPF: 0.25% (10 mL, 30 mL); 0.5% (10 mL, 30 mL); 0.75% (10 mL, 30 mL) [methylparaben free]

Generic: 0.25% (10 mL, 30 mL, 50 mL); 0.5% (10 mL, 30 mL, 50 mL); 0.75% (10 mL, 30 mL)

Solution, Injection, as hydrochloride [preservative free]:

Marcaine: 0.75% (10 mL, 30 mL)

Marcaine Preservative Free: 0.25% (10 mL, 30 mL); 0.5% (10 mL, 30 mL)

Generic: 0.25% (10 mL, 20 mL [DSC], 30 mL); 0.5% (10 mL, 20 mL [DSC], 30 mL); 0.75% (10 mL, 20 mL [DSC], 30 mL)

Solution, Intrathecal, as hydrochloride:

Generic: 0.75% [7.5 mg/mL] (2 mL)

Solution, Intrathecal, as hydrochloride [preservative free]:

Bupivacaine Spinal: 0.75% [7.5 mg/mL] (2 mL)

Marcaine Spinal: 0.75% [7.5 mg/mL] (2 mL)

Sensorcaine-MPF Spinal: 0.75% [7.5 mg/mL] (2 mL)

Brand Names: U.S.

  • Bupivacaine Spinal
  • Marcaine
  • Marcaine Preservative Free
  • Marcaine Spinal
  • Sensorcaine
  • Sensorcaine-MPF
  • Sensorcaine-MPF Spinal

Pharmacologic Category

  • Local Anesthetic

Pharmacology

Blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction

Distribution

Infants: 3.9 ± 2 L/kg

Children: 2.7 ± 0.2 L/kg

Metabolism

Hepatic; forms metabolite (pipecoloxylidine [PPX])

Excretion

Excretion: Urine (~6% unchanged)

Clearance: Infants: 7.1 ± 3.2 mL/kg/minute; Children: 10 ± 0.7 mL/kg/minute

Onset of Action

Anesthesia (route and dose dependent):

Epidural: Up to 17 minutes to spread to T6 dermatome (Scott 1980)

Infiltration: Fast (Barash 2009); Dental injection: 2 to 10 minutes

Spinal: Within 1 minute; maximum dermatome level achieved within 15 minutes in most cases

Time to Peak

Plasma: Caudal, epidural, or peripheral nerve block: 30 to 45 minutes

Duration of Action

Route and dose dependent:

Epidural: 2 to 7.7 hours (Barash 2009)

Infiltration: 2 to 8 hours (Barash 2009); Dental injection: Up to 7 hours

Spinal: 1.5 to 2.5 hours (Hadzic 2007)

Half-Life Elimination

Age dependent: Neonates: 8.1 hours; Adults: 2.7 hours

Protein Binding

84% to 95%

Use: Labeled Indications

Local or regional anesthesia; spinal anesthesia (0.75% in dextrose 8.25% injection); diagnostic and therapeutic procedures; obstetrical procedures (only 0.25% and 0.5% concentrations)

0.25%: Local infiltration, peripheral nerve block, sympathetic block, caudal or epidural block

0.5%: Peripheral nerve block, caudal and epidural block

0.75% (not for obstetrical anesthesia): Retrobulbar block, epidural block. Note: Reserve for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary

Contraindications

Hypersensitivity to bupivacaine hydrochloride, amide-type local anesthetics, or any component of the formulation; obstetrical paracervical block anesthesia

Note: Use as intravenous regional anesthesia (Bier block) is considered contraindicated per accepted clinical practice due to reports of cardiac arrest and death.

Dosing: Adult

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).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

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.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Administration

Solutions containing preservatives should not be used for epidural or caudal blocks. The On-Q infusion pump is used to slowly administer local anesthetics (eg, bupivacaine, lidocaine, ropivacaine) to or around surgical wound sites and/or in close proximity to peripheral nerves for postoperative analgesia. When infused directly into the shoulder, destruction of articular cartilage (chondrolysis) has occurred. On-Q pumps should never be placed directly into any joint (see https://www.ismp.org/Newsletters/acutecare/archives/May09.asp).

Compatibility

Stable in NS.

Storage

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

Drug Interactions

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Beta-Blockers: May increase the serum concentration of Bupivacaine. Monitor therapy

Blood Pressure Lowering Agents: May enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Bupivacaine (Liposomal): Bupivacaine may enhance the adverse/toxic effect of Bupivacaine (Liposomal). Management: Bupivacaine may be administered immediately before, or administered in the same admixture syringe as liposomal bupivacaine as long as the ratio of the milligram dose of bupivacaine to liposomal bupivacaine does not exceed 1:2. Consider therapy modification

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Levodopa: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa. Monitor therapy

Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Monitor therapy

Adverse Reactions

Note: Incidence of adverse reactions is difficult to define. Most effects are dose related, and are often due to accelerated absorption from the injection site, unintentional intravascular injection, or slow metabolic degradation. The development of any central nervous system symptoms may be an early indication of more significant toxicity (seizure).

Cardiovascular: Bradycardia, cardiac arrest, heart block, hypotension, palpitations, ventricular arrhythmia

Central nervous system: Anxiety, dizziness, restlessness

Gastrointestinal: Nausea, vomiting

Hypersensitivity: Anaphylactoid reaction, hypersensitivity reaction (urticaria, pruritus, angioedema)

Neuromuscular & skeletal: Chondrolysis (continuous intra-articular administration), weakness

Ophthalmic: Blurred vision, miosis

Otic: Tinnitus

Respiratory: Apnea, hypoventilation (usually associated with unintentional subarachnoid injection during high spinal anesthesia)

<1% (Limited to important or life-threatening): Seizure; usually associated with unintentional subarachnoid injection during high spinal anesthesia: cranial nerve palsy, fecal incontinence, headache, loss of anal sphincter control, loss of perineal sensation, paralysis, paresthesia, persistent anesthesia, septic meningitis, sexual disorder (loss of function), urinary incontinence

ALERT: U.S. Boxed Warning

Obstetrical anesthesia:

The bupivacaine 0.75% concentration is not recommended for obstetrical anesthesia. There have been reports of cardiac arrest with difficult resuscitation or death during use of bupivacaine for epidural anesthesia in obstetrical patients. In most cases, this has followed use of the 0.75% concentration. Resuscitation has been difficult or impossible despite apparently adequate preparation and appropriate management. Cardiac arrest has occurred after convulsions resulting from systemic toxicity, presumably following unintentional intravascular injection. The 0.75% concentration should be reserved for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary.

Warnings/Precautions

Concerns related to adverse effects:

• Cardiovascular effects: Bupivacaine-containing products have been associated with rare occurrences of arrhythmias, cardiac arrest, and death.

• Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily shoulder joint) has occurred following infusion, with some patients requiring arthroplasty or shoulder replacement.

• Respiratory arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest, especially when administered near the head or neck.

• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection or administration near the head or neck.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiovascular disease including patients with hypotension or heart block.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

Special populations:

• Acutely ill patients: Use with caution in acutely ill patients; dose reduction may be required.

• Debilitated patients: Use with caution in debilitated patients; dose reduction may be required.

• Elderly: Use with caution in the elderly; dose reduction may be required.

Dosage form specific issues:

• Obstetrical anesthesia: [US Boxed Warning]: The 0.75% concentration is not recommended for obstetrical anesthesia; cardiac arrest with difficult resuscitation or death has occurred.

• Preservative-containing solutions: Do not use solutions containing preservatives for caudal or epidural block.

• Sodium metabisulfite: May contain sodium metabisulfite; use caution in patients with asthma or a sulfite allergy.

Other warnings/precautions:

• Administration: Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided. Intravenous regional anesthesia (Bier block) is not recommended; cardiac arrest and death have occurred with this method of administration.

• Test dose: A test dose is recommended prior to epidural administration (prior to initial dose) and all reinforcing doses with continuous catheter technique.

• Trained personnel: Clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.

Monitoring Parameters

Vital signs, state of consciousness; signs of CNS toxicity

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in animal reproduction studies. Bupivacaine crosses the placenta. Bupivacaine is approved for use at term in obstetrical anesthesia or analgesia. [U.S. Boxed Warning]: The 0.75% is not recommended for obstetrical anesthesia. Bupivacaine 0.75% solutions have been associated with cardiac arrest following epidural anesthesia in obstetrical patients and use of this concentration is not recommended for this purpose. Use in obstetrical paracervical block anesthesia is contraindicated.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber bradycardia, abnormal heartbeat, angina, tachycardia, severe dizziness, passing out, change in balance, confusion, agitation, tremors, blurred vision, tinnitus, depression, difficulty breathing, slow breathing, shallow breathing, seizures, severe nausea, or vomiting (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Hide