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Home > Medications (Drugs) > Bupivacaine > More information about Bupivacaine

More information about Bupivacaine

Pronunciation

(byoo PIV a kane)


U.S. Brand Names

Marcaine®; Marcaine® Spinal; Sensorcaine®; Sensorcaine®-MPF

Synonyms

Bupivacaine Hydrochloride

Generic Available

Yes

Canadian Brand Names

Marcaine®; Sensorcaine®

Use

Local anesthetic (injectable) for peripheral nerve block, infiltration, sympathetic block, caudal or epidural block, retrobulbar block

Pregnancy Risk Factor

C

Lactation

Enters breast milk/contraindicated

Contraindications

Hypersensitivity to bupivacaine hydrochloride, amide-type local anesthetics (etidocaine, lidocaine, mepivacaine, prilocaine, ropivacaine) or any component of the formulation (para-aminobenzoic acid or parabens in specific formulations); not to be used for obstetrical paracervical block anesthesia

Warnings/Precautions

Use with caution in patients with hepatic impairment. Some commercially available formulations contain sodium metabisulfite, which may cause allergic-type reactions; not recommended for use in children <12 years of age. The solution for spinal anesthesia should not be used in children <18 years of age. Do not use solutions containing preservatives for caudal or epidural block. Local anesthetics have been associated with rare occurrences of sudden respiratory arrest; convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection. The 0.75% is not recommended for obstetrical anesthesia. A test dose is recommended prior to epidural administration (prior to initial dose) and all reinforcing doses with continuous catheter technique.

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: Hypotension, bradycardia, palpitation, heart block, ventricular arrhythmia, cardiac arrest

Central nervous system: Restlessness, anxiety, dizziness, seizure (0.1%); rare symptoms (usually associated with unintentional subarachnoid injection during high spinal anesthesia) include persistent anesthesia, paresthesia, paralysis, headache, septic meningitis, and cranial nerve palsies

Gastrointestinal: Nausea, vomiting; rare symptoms (usually associated with unintentional subarachnoid injection during high spinal anesthesia) include fecal incontinence and loss of sphincter control

Genitourinary: Rare symptoms (usually associated with unintentional subarachnoid injection during high spinal anesthesia) include urinary incontinence, loss of perineal sensation, and loss of sexual function

Neuromuscular & skeletal: Weakness

Ocular: Blurred vision, pupillary constriction

Otic: Tinnitus

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

Miscellaneous; Allergic reactions (urticaria, pruritus, angioedema), anaphylactoid reactions

Overdosage/Toxicology

Treatment is symptomatic and supportive. Termination of anesthesia by pneumatic tourniquet inflation should be attempted when bupivacaine is administered by infiltration or regional injection. Treatment is symptomatic and supportive. Methemoglobinemia should be treated with methylene blue 1-2 mg/kg in a 1% sterile aqueous solution by I.V. push over 4-6 minutes, repeated up to a total dose of 7 mg/kg.

Drug Interactions

Substrate (minor) of CYP1A2, 2C19, 2D6, 3A4

Increased effect: Hyaluronidase

Increased toxicity: Beta-blockers, ergot-type oxytocics, MAO inhibitors, TCAs, phenothiazines, vasopressors

Stability

Solutions with epinephrine should be protected from light

Compatibility

Stable in NS

Compatibility in syringe: Compatible:   Clonidine with morphine, diamorphine, fentanyl with ketamine, hydromorphone, iohexol, morphine. Variable (consult detailed reference):   Sodium bicarbonate

Compatibility when admixed: Compatible:   Buprenorphine, diamorphine, epinephrine, fentanyl, hydromorphone, morphine, sufentanil

Mechanism of Action

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

Pharmacodynamics/Kinetics

Onset of action: Anesthesia (route dependent): 4-10 minutes

Duration: 1.5-8.5 hours

Metabolism: Hepatic

Half-life elimination (age dependent): Neonates: 8.1 hours; Adults: 1.5-5.5 hours

Excretion: Urine (~6%)

Dosage

Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia and condition of patient. Some formulations contain metabisulfites (in epinephrine-containing injection); do not use solutions containing preservatives for caudal or epidural block.

Local anesthesia: Infiltration: 0.25% infiltrated locally; maximum: 175 mg

Caudal block (with or without epinephrine, preservative free):

Children: 1-3.7 mg/kg

Adults: 15-30 mL of 0.25% or 0.5%

Epidural block (other than caudal block - with or without epinephrine, preservative free):

Administer in 3-5 mL increments, allowing sufficient time to detect toxic manifestations of inadvertent I.V. or I.T. administration:

Children: 1.25 mg/kg/dose

Adults: 10-20 mL of 0.25% or 0.5%

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

Maxillary and mandibular infiltration and nerve block: 9 mg (1.8 mL) of 0.5% (with epinephrine) per injection site; a second dose may be administered if necessary to produce adequate anesthesia after allowing up to 10 minutes for onset, up to a maximum of 90 mg per dental appointment

Obstetrical anesthesia: Incremental dose: 3-5 mL of 0.5% (not exceeding 50-100 mg in any dosing interval); allow sufficient time to detect toxic manifestations or inadvertent I.V. or I.T. injection

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

Sympathetic nerve block: 20-50 mL of 0.25%

Retrobulbar anesthesia: 2-4 mL of 0.75%

Spinal anesthesia: Solution of 0.75% bupivacaine in 8.25% dextrose is used:

Lower extremity and perineal procedures: 1 mL

Lower abdominal procedures: 1.6 mL

Obstetrical:

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

Cesarean section: 1-1.4 mL

Administration

Solutions containing preservatives should not be used for epidural or caudal blocks

Monitoring Parameters

Monitor fetal heart rate during paracervical anesthesia

Patient Education

This medication is given to reduce sensation in the injected area. You will experience decreased sensation to pain, heat, or cold in the area and/or decreased muscle strength (depending on area of application) until the effects wear off; use necessary caution to reduce incidence of possible injury until full sensation returns. If used in mouth, do not eat or drink until full sensation returns. Immediately report chest pain or palpitations; increased restlessness, anxiety, or dizziness; skeletal or muscle weakness; respiratory difficulty; ringing in ears; or vision changes. Pregnancy/breast-feeding precautions:   Inform prescriber if you are pregnant. Do not breast-feed.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause anxiety and restlessness

Mental Health: Effects on Psychiatric Treatment

Use with caution in patients receiving phenothiazines, MAO inhibitors, or TCAs; severe hypertension or hypotension may result

Dosage Forms

Injection, solution, as hydrochloride [preservative free]: 0.25% [2.5 mg/mL] (10 mL, 20 mL, 30 mL, 50 mL); 0.5% [5 mg/mL] (10 mL, 20 mL, 30 mL); 0.75% [7.5 mg/mL] (10 mL, 20 mL, 30 mL)

Marcaine®: 0.25% [2.5 mg/mL] (10 mL, 30 mL, 50 mL); 0.5% [5 mg/mL] (10 mL, 30 mL); 0.75% [7.5 mg/mL] (10 mL, 30 mL)

Marcaine® Spinal: 0.75% [7.5 mg/mL] (2 mL) [in dextrose 8.25%]

Sensorcaine®-MPF: 0.25% [2.5 mg/mL] (10 mL, 30 mL); 0.5% [5 mg/mL] (10 mL, 30 mL); 0.75% [7.5 mg/mL] (10 mL, 30 mL)

Injection, solution, as hydrochloride (Marcaine®, Sensorcaine®): 0.25% [2.5 mg/mL] (50 mL); 0.5% [5 mg/mL] (50 mL) [contains methylparaben]

Injection, solution, with epinephrine 1:200,000, as hydrochloride [preservative free]: 0.25% [2.5 mg/mL] (10 mL, 30 mL); 0.5 % [5 mg/mL] (30 mL)

Marcaine®: 0.25% [2.5 mg/mL] (10 mL, 30 mL); 0.5% [5 mg/mL] (3 mL, 10 mL, 30 mL); 0.75% [7.5 mg/mL] (30 mL) [contains sodium metabisulfite]

Sensorcaine®-MPF: 0.25% [2.5 mg/mL] (10 mL, 30 mL); 0.5% [5 mg/mL] (10 mL, 30 mL); 0.75% [7.5 mg/mL] (30 mL) [contains sodium metabisulfite]

Injection, solution, with epinephrine 1:200,000, as hydrochloride [with preservative] (Marcaine®, Sensorcaine®): 0.25% [2.5 mg/mL] (50 mL); 0.5% [5 mg/mL] (50 mL) [contains methylparaben and sodium metabisulfite]

References

Lehmann LJ and Pallares VS, "Subdural Injection of a Local Anesthetic With Steroids: Complication of Epidural Anesthesia,"South Med J, 1995, 88(4):467-9.

Long WB, Rosenblum S, and Grady IP, "Successful Resuscitation of Bupivacaine-Induced Cardiac Arrest Using Cardiopulmonary Bypass,"Anesth Analg, 1989, 69(3):403-6.

Scott DB, Lee A, Fagan D, et al, "Acute Toxicity of Ropivacaine Compared With That of Bupivacaine,"Anesth Analg, 1989, 69(5):563-9.

Sun KO, "Convulsion Following Spinal Anaesthesia,"Anaesth Intensive Care, 1995, 23(4):520-1.

Tuominen MK, Pere P, and Rosenberg PH, "Unintentional Arterial Catheterization and Bupivacaine Toxicity Associated With Continuous Interscalene Brachial Plexus Block,"Anesthesiology, 1991, 75(2):356-8.

International Brand Names

Anekain® (RU); Bicain® (FI); Bucain® (AT, DE, HU); Bucaine® (EG, JO, KW, LB, SY); Bupibil® (IT); Bupicaina® (AR); Bupicain® (IT); Bupiforan® (IT); Bupigobbi® (AR); Bupinex® (AR); Bupirop® (CO); Bupisen® (IT); Bupivacaina Angelini® (IT); Bupivacaina Braun® (ES); Bupivacaina Clorhidrato® (CL); Bupivacaina® (CL, RO); Bupivacain ACS Dobfar Info® (CH); Bupivacaina Gemepe® (AR); Bupivacaina Hiperbarica® (CL); Bupivacaina Pulitzer® (IT); Bupivacaina Recordati® (IT); Bupivacaine Bioren® (CH); Bupivacaine® (CH, GB, NZ); Bupivacaine Hydrochloride® (AU); Bupivacaine hyperbar Bioren® (CH); Bupivacaine Spinal® (RO); Bupivacain INFOsint® (CH); Bupivacain Jenapharm® (DE); Bupivacain-RPR® (DE); Bupivacain SAD® (DK); Bupivacain Sintetica® (CH); Bupivacainum hydrochloricum® (PL); Bupivakain® (NO); Bupixamol® (IT); Buvacaina® (MX); Carbostesin® (AT, CH, DE); Cloridrato de Bupivacaina® (BR); Dolanaest® (AT, DE); Duracain® (CH); Macaine® (ZA); Marcaina® (BR, IT); Marcain® (AU, DK, FI, GB, HU, ID, IN, NO, NZ, SE, SG, TH); Marcaine® (BE, BG, CA, CY, CZ, EG); Marca&iuml;ne® (FR); Marcaine® (IL, JO, KW, LB, LU, MT, NL, PL, RO, RU, SI, SY, TR, YU); Marcaine Spinal® (CZ, ID, IL, PL, RO, TH); Marcain Spinal® (DK, HU, SE); Marcain spinal tung® (SE); Neocaina® (BR); Regibloc® (ZA); Sensorcaine® (CA, IN); Svedocain Sin Vasoconstr® (ES); Ultracaine® (BD); Vexelit® (YU)

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