Bupivacaine

DEA Class;  Rx

Common Brand Names; Marcaine, Sensorcaine, Posimir, Exparel, XaraColl

  • Local Anesthetics, Amides; 
  • Local Anesthetics, Dental; 
  • Local Anesthetics, Parenteral
  • Amides

Amide local anesthetic
Used for local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and obstetrical procedures
Not all blocks indicated for use with bupivacaine given clinically significant risks associated with use

Marcaine spinal, Sensorcaine-MPF Spinal, generic

Indicated for the production of subarachnoid block (spinal anesthesia)

For local anesthesia, including infiltration anesthesia.
For regional anesthesia, including caudal anesthesia, epidural anesthesia, or obstetric anesthesia.
For nerve block anesthesia, including peripheral nerve block and sympathetic nerve block.
For ophthalmic anesthesia, including retrobulbar nerve block.
For spinal anesthesia, including Caesarean section anesthesia.
For postsurgical local analgesia.

Hypersensitivity to any amide local anesthetics, or other product components

Marcaine

  • Undergoing obstetrical paracervical block anesthesia

  • IV regional anesthesia (Bier Block)

Bupivacaine spinal

  • Severe hemorrhage, severe hypotension or shock and arrhythmias (eg, complete heart block)

  • Local infection at the site of proposed lumbar puncture

  • Septicemia

  • Intravenous regional anesthesia (Bier Block)

  • Obstetrical paracervical block anesthesia; its use in this technique has resulted in fetal bradycardia and death

Posimir

  • Undergoing obstetrical paracervical block anesthesia; use of bupivacaine HCl with this technique has resulted in fetal bradycardia and death

  • Visible bruising (91.1%)
  • Postprocedural contusion (14-71.2%)
  • Nausea (20-55.8%)
  • Surgical site bleeding (8.7-48.9%)
  • Dizziness (15-40.3%)
  • Somnolence (8.3-40%)
  • Constipation (30.4%)
  • Vomiting (4.4-29%)
  • Bradycardia (22.9%)
  • Headache (11.1-27.2%)
  • Pruritus generalized (2.2-21.6%)
  • Paresthesia (7.5-18.4%)
  • Dysgeusia (13-17.6%)
  • Hypoesthesia (17.3%)
  • Anemia (4.5-16.7%)
  • Tinnitus (13.2%)
  • C-reactive protein increased (11.7%)
  • Pyrexia (6-11.7%)
  • Procedural pain (<11.4%)
  • Dysuria (10.1%)

Safety and effectiveness of local anesthetics depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies; resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use

Caution with impaired cardiovascular function (eg, hypotension, heart block), as patients may be unable to compensate for functional changes associated with prolongation of AV conduction produced by bupivacaine; consider reduced dosing; closely monitor for blood pressure, heart rate, and ECG changes

Many drugs used during anesthesia may trigger malignant familial hyperthermia; potential for amide-type local anesthetics to also trigger such a response is unknown; consider a standard protocol for therapeutic management to be available

Avoid solutions containing antimicrobial preservatives, (ie, multiple-dose vials), for epidural or caudal anesthesia; safety not established for use

Infants and neonates are at greater risk for bupivacaine toxicity owing to a lower amount of serum alpha-1-acid-glycoprotein concentration compared with older children; this protein is the major binding site for bupivacaine, therefore, infants and neonates may have an increase of free fraction of local anesthetics

Bupivacaine is known to be substantially excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with renal impairment; this should be considered when selecting the dosage

Because of long duration of anesthesia, when used for dental injections, warn patients about possibility of inadvertent trauma to tongue, lips, and buccal mucosa and advise them not to chew solid foods until sensation returns

Contraindicated for obstetrical paracervical block anesthesia; use has resulted in fetal bradycardia and death

Data are unavailable on use in pregnant women to inform a drug-associated risks of adverse developmental outcomes

Not studied in nursing mothers

The bupivacaine dose varies with the procedure, area to be anesthetized, tissue vascularity, number of neuronal segments to be blocked, required depth of anesthesia and degree of muscle relaxation, desired duration of anesthesia, as well as patient tolerance and physical condition.

Adults

175 mg/dose and 400 mg/24 hours for all parenteral routes; 300 mg/procedure for implant; 660 mg/procedure for subacromial space infiltration.

Geriatric

175 mg/dose and 400 mg/24 hours for all parenteral routes; 300 mg/procedure for implant; 660 mg/procedure for subacromial space infiltration.

Adolescents

175 mg/dose and 400 mg/24 hours for all parenteral routes. Safety and efficacy have not been established for implant or subacromial space infiltration.

Children

12 years: 175 mg/dose and 400 mg/24 hours for all parenteral routes. Safety and efficacy have not been established for implant or subacromial space infiltration.
1 to 11 years: 2.5 mg/kg/dose (Max: 175 mg/dose) and 400 mg/24 hours for all parenteral routes. Safety and efficacy have not been established for implant or subacromial space infiltration.

Infants

6 to 11 months: 2.5 mg/kg/dose for all parenteral routes. Safety and efficacy have not been established for implant or subacromial space infiltration.
1 to 5 months: 1.75 mg/kg/dose for all parenteral routes. Safety and efficacy have not been established for implant or subacromial space infiltration.

Neonates

Safety and efficacy have not been established.

Bupivacaine Hydrochloride

injectable solution

  • 0.25% (Sensorcaine, Marcaine, generic)
  • 0.5% (Sensorcaine, Marcaine, generic)
  • Contains methylparaben

injectable solution, preservative-free

  • 0.25% (Sensorcaine-MPF, Marcaine, generic)
  • 0.5% (Sensorcaine-MPF, Marcaine, generic)
  • 0.75% (Sensorcaine-MPF, Marcaine Preservative Free, generic)

injection, spinal

  • 0.75% (Sensorcaine MPF Spinal, Marcaine Spinal, generic)
  • Each 2-mL ampule contains 15 mg bupivacaine HCL with 165 mg dextrose

injection, single-dose vial

  • 660mg/5mL (Posimir)

injectable suspension

  • 133mg/10mL single-dose vial
  • 266mg/20mL single-dose vial

surgical implant

  • 100mg/implant
  • Each single-dose package (pouch) contains 3 implants totaling 300 mg

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