Medically reviewed by Drugs.com. Last updated on Apr 19, 2019.
(byoo PIV a kane)
- Bupivacaine HCl
- Bupivacaine Hydrochloride
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Kit, Injection, as hydrochloride:
P-Care M: 0.5%
Kit, Injection, as hydrochloride [preservative free]:
ReadySharp Bupivacaine: 0.5% [DSC]
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]
Generic: 0.25% (30 mL [DSC], 50 mL); 0.5% (50 mL)
Solution, Injection, as hydrochloride [preservative free]:
Bupivacaine Fisiopharma: 2.5 mg/mL (5 mL, 10 mL); 5 mg/mL (5 mL, 10 mL)
Marcaine: 0.75% (10 mL, 30 mL)
Marcaine Preservative Free: 0.25% (10 mL, 30 mL); 0.5% (10 mL, 30 mL)
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); 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 [DSC])
Brand Names: U.S.
- Bupivacaine Fisiopharma
- Bupivacaine Spinal
- Marcaine Preservative Free
- Marcaine Spinal
- P-Care M
- ReadySharp Bupivacaine [DSC]
- Sensorcaine-MPF Spinal [DSC]
- Local Anesthetic
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
Infants: 3.9 ± 2 L/kg
Children: 2.7 ± 0.2 L/kg
Hepatic; forms metabolite (pipecoloxylidine [PPX])
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 (Tsai 2007)
Age dependent: Neonates: 8.1 hours; Adults: 2.7 hours
84% to 95%
Special Populations: Elderly
Elderly patients reached the maximal spread of analgesia and maximal motor blockade more rapidly than younger patients. Elderly patients also exhibited higher peak plasma concentrations following administration of this product. The total plasma clearance was decreased in these patients.
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
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.
Canadian labeling: Additional contraindications (not in US labeling): IV regional anesthesia (Bier block); severe shock and in heart block where there is inflammation and/or sepsis near the proposed injection site (Marcaine only).
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).
Refer to adult dosing.
Note: Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient. Preservative-free formulations are recommended for administration into the CNS space (eg, epidural, caudal, spinal). Consider incremental administration with negative aspiration prior to each injection; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided (Mulroy 2010). Should only be administered under the supervision of a qualified physician experienced in the use of anesthetics. In pediatric patients, dosing should be based on lean body mass (Coté 2013).
Central nerve block/anesthesia:
Caudal block: Reported dosing variable based on procedure; dependent on necessary dermatome level and corresponding volume of space:
Infants and Children: Limited data available: Usual concentration ≤0.25% solution with or without epinephrine: Usual reported dose range: 0.5 to 1.3 mL/kg (maximal volume of drug: 20 mL); dose should not exceed 2 mg/kg plain solution, or 3 mg/kg with epinephrine. In infants, routine use of concentrations ≤0.25% have been suggested to reduce risk of bupivacaine cardiotoxicity (Coté 2013; Ingelmo 2007; Ivani 1998; Ivani 2002; Karkera 2016; Miller 2015; Payne 1993; Schrock 2003; Schwartz 2010)
Adolescents: Usual concentration 0.25 to 0.5% solution with or without epinephrine: 15 to 30 mL
Epidural block: Reported dosing variable; among other factors, dose dependent on necessary dermatome level and corresponding volume of epidural space (Coté 2013):
Infants: Limited data available: Usual concentration ≤0.25% with or without epinephrine: 0.7 to 0.75 mL/kg; maximum dose: 2.5 mg/kg; Note: For infants (particularly young infants), if repeat injections necessary, a decreased dose may be necessary to prevent drug accumulation. Some experts suggest if at least 45 minutes since initial dose, reduce dose to 1/3 of the initial or if at least 90 minutes since initial dose, then reduce dose to half of the initial. If additional doses are necessary, doses should be reduced to half of the previous dose (Ivani 1999; Miller 2015; Monsel 2007).
Children: Limited data available: Usual concentration 0.25% solution: Initial: 0.3 to 0.6 mL/kg (maximal volume of drug: 20 mL); maximum dose: 2.5 mg/kg (Ingelmo 2007; Ingelmo 2007a)
Adolescents: 0.25% or 0.5% solution: 10 to 20 mL administered in 3 to 5 mL increments; if high degree of muscle relaxation and prolonged effects needed, may consider 0.75% solution: 10 to 20 mL
Epidural, continuous infusion: Limited data available in infants and children <12 years (Berde 1992; Miller 2015; Moriarty 2012): Note: Use has generally been replaced by other agents (eg, ropivacaine) (Miller 2015; Moriarty 2012).
Loading dose: Usual concentration: 0.25%: 2 to 2.5 mg/kg
Infants <4 months: 0.2 mg/kg/hour
Infants ≥4 months: 0.25 mg/kg/hour
Children and Adolescents: 0.3 mg/kg/hour
Peripheral nerve block: Limited data available in infants and children: Note: Dose varies with location of block (ie, procedure), depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient.
Infants ≥6 months and Children: Usual concentration 0.125% or 0.25% solution with or without epinephrine: The volume of dose (mL/kg) and concentration of solution are site specific based upon anatomy and variable among patients and procedure; see below ranges. For infants <6 months, maximum doses should be reduced by 30% (Coté 2013; Miller 2015). Maximum dose plain solution: 2 mg/kg or 150 mg whichever is less or maximum dose with epinephrine: 3 mg/kg or 200 mg of bupivacaine whichever is less.
Commonly suggested doses (Coté 2013):
Head and neck: 0.05 mL/kg
Brachial plexus: 0.2 to 0.3 mL/kg
Digital nerve: 0.05 mL/kg
Transversus abdominis plane: 0.2 to 0.5 mL (Jöhr 2015)
Rectus sheath: 0.1 mL/kg
Ilioinguinal: 0.075 mL/kg
Lower extremity blocks:
Femoral nerve: 0.2 to 0.3 mL/kg
Sciatic nerve: 0.2 to 0.3 mL/kg
Adolescents: 0.25% or 0.5% solution with or without epinephrine: 5 mL; maximum daily dose: 400 mg/day
Local anesthesia: Infants, Children, and Adolescents: Limited data in infants and children: Usual concentration 0.25% solution: Infiltrate area local; maximum dose in infants and children: 2.5 mg/kg or 150 mg whichever is less; maximum dose in adolescents: 175 mg (Coté 2013)
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).
Store at controlled room temperature of 20°C to 25°C (68°F to 77˚F).
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
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Avoid combination
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-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Monitor therapy
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. 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
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking 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
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. 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
Frequency not defined. Reactions listed are based on reports for other agents in this same pharmacologic class and may not be specifically reported for bupivacaine.
Cardiovascular: Bradycardia, cardiac insufficiency, circulatory shock, heart block, hypotension, ventricular arrhythmia
Central nervous system: Anxiety, arachnoiditis, central nervous system depression, central nervous system stimulation, chills, cranial nerve palsy, dizziness, headache, localized numbness (perineal), meningism, paralysis, paraplegia, paresthesia, persistent anesthesia, restlessness, seizure, shivering
Gastrointestinal: Fecal incontinence, loss of anal sphincter control, nausea, vomiting
Genitourinary: Prolonged labor, sexual disorder (loss of function), urinary incontinence, urinary retention
Hematologic & oncologic: Methemoglobinemia
Hypersensitivity: Hypersensitivity reaction
Infection: Septic meningitis
Neuromuscular & skeletal: Asthenia, back pain, lower extremity weakness, tremor
Ophthalmic: Blurred vision, miosis
Respiratory: Apnea, hypoventilation (usually associated with unintentional subarachnoid injection during high spinal anesthesia), respiratory paralysis
ALERT: U.S. Boxed WarningObstetrical 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.
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.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, light-headedness, fatigue).
• 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.
• 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.
• 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.
• 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.
Vital signs, state of consciousness; signs of CNS toxicity
Adverse events were observed in animal reproduction studies. Bupivacaine crosses the placenta. Bupivacaine is approved for use at term in obstetrical anesthesia or analgesia. [US 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.
What is this drug used for?
• It is used to numb an area before a procedure.
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• Acidosis like confusion, fast breathing, tachycardia, abnormal heartbeat, severe abdominal pain, nausea, vomiting, fatigue, shortness of breath, or loss of strength and energy.
• Methemoglobinemia like blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath.
• Chest pain
• Passing out
• Change in balance
• Change in speech
• Blurred vision
• Difficulty breathing
• Slow breathing
• Shallow breathing
• Numbness or tingling in the mouth
• Metallic taste
• Signs of a significant reaction like 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. Talk to your doctor if you have questions.
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Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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