Bupivacaine

Bupivacaine is a local anesthetic used to prevent pain during dental procedures and as nerve blocks for regional anesthesia during various medical procedures including during labor and delivery.

Bupivacaine blocks the nerve impulses that send pain signals from the procedural area to the brain. Bupivacaine only numbs the operative region without depressing consciousness. Bupivacaine belongs to a class of anesthetics known as amides.

Bupivacaine prevents the initiation and conduction of nerve impulses by blocking the influx of sodium ions into nerve cells (neurons). Bupivacaine is administered as injection or infiltration locally around nerves in a specific area to produce loss of sensation selectively.

In addition to dental procedures, bupivacaine is used to inject around parts of the spine such as the lumbar or tailbone area, the shoulder, or during eye procedures.

• Do not administer to patients with hypersensitivity to amides or any of the components of bupivacaine formulation.
• Do not use bupivacaine for paracervical block during labor, may cause slow heartbeat (bradycardia) and death of the fetus. Bupivacaine 0.75% concentration is not recommended for obstetrical anesthesia.
• Do not use bupivacaine for intravenous (IV) regional anesthesia.
• Do not use solutions containing preservatives for caudal or epidural block.
• Do not use bupivacaine in the following conditions:
  • Infection at the site of proposed lumbar puncture
  • Septicemia
  • Severe hemorrhage, severe hypotension or shock, or irregular heart rhythms
• Local anesthetics should be administered only by clinicians well-versed in diagnosis and management of dose-related toxicity. Resuscitative equipment, drugs and oxygen should be readily available.
• Many drugs used during anesthesia may trigger malignant hyperthermia, a life-threatening drug reaction with high fever, rapid heart rate and muscle spasms. Facility should be available to manage the treatment.
• Unintentional injection into a blood vessel can cause systemic toxicity leading to convulsions and cardiac arrest. Administer extremely carefully.
• The lowest dosage that produces effective anesthesia should be used in order to avoid high plasma levels and serious systemic side effects.
• Local anesthetics including bupivacaine have been associated with rare occurrences of sudden respiratory arrest, especially when administered near the head or neck.
• Use bupivacaine with caution in patients with impaired cardiovascular function. Closely monitor blood pressure, heart rate and ECG changes.
• Use with caution in patients with impaired liver function and patients who are acutely ill, debilitated or elderly.
• Local anesthetics have been reported to cause methemoglobinemia, a condition with a high blood level of methemoglobin, a form of hemoglobin that does not deliver oxygen to the tissues efficiently. 
  • Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, and infants younger than 6 months are at a higher risk for methemoglobinemia.
  • Bupivacaine should be immediately discontinued if there are signs of methemoglobinemia and the patient should be monitored and treated appropriately.
• Shoulder (subacromial) injection is not interchangeable with other bupivacaine formulations; bioequivalence is not the same even when milligram dosage is the same.
• Some bupivacaine formulations may contain benzyl alcohol. Do not use these formulations in newborns, can cause a potentially fatal condition known as “gasping syndrome.”
• Bupivacaine may contain sodium metabisulfite. Use with caution in patients with asthma or a sulfite allergy.

Common side effects of bupivacaine include:

• Visible bruising
• Postprocedural contusion
• Surgical site bleeding
• Nausea
• Vomiting
• Constipation
• Dizziness
• Somnolence
• Slow heart rate (bradycardia)
• Headache
• Generalized itching (pruritus)
• Abnormal skin sensation (paresthesia)
• Reduced skin sensation (hypoesthesia)
• Taste perversion (dysgeusia)
• Ringing in the ears (tinnitus)
• Low red blood cell count (anemia)
• Increase in C-reactive protein
• Fever (pyrexia)
• Procedural pain
• Painful urination (dysuria)

Less common side effects of bupivacaine:

• Diarrhea
• Abdominal distension
• Abdominal pain
• Indigestion (dyspepsia)
• Gas (flatulence)
• Incision site reactions such as:
  • Redness (erythema)
  • Hematoma
  • Contusion
  • Swelling
  • Infection
  • Drainage
  • Pruritus
• Separation of wound edges (dehiscence)
• Procedural hemorrhage
• Insomnia
• Decrease in blood potassium
• Low blood potassium (hypokalemia)
• High blood pressure (hypertension)
• Rapid heart rate (tachycardia)
• Abnormality in ECG
• Angina pectoris (chest pain)
• Headache
• Musculoskeletal pain
• Back pain
• Muscle twitching
• Spasm of muscles around the eye (blepharospasm)
• Mouth and throat pain (oropharyngeal pain)
• Dry throat
• Dry mouth
• Nasal congestion
• Inflammation of nose and throat (nasopharyngitis)
• Viral infection
• Shortness of breath (dyspnea)
• Cough
• Upper respiratory tract infection
• Peripheral swelling (edema)
• Vaginal hematoma
• Painful menstruation (dysmenorrhea)
• Testicular swelling
• Excessive sweating (hyperhidrosis)
• Chest pain
• Temporary paralysis of intestinal muscles (Ileus)
• Urinary retention
• Rash
• Pain in extremity
• Fatigue
• Osteoarthritis
• Procedural nausea
• Pulmonary arterial hypertension

Rare side effect of bupivacaine include:

• Underventilation
• Respiratory paralysis
• Cardiovascular effects such as:
  • Myocardium depression
  • Reduced cardiac output
  • Heart block
  • Ventricular arrhythmias
  • Possible cardiac arrest
• Excitement and/or depression
• Restlessness
• Anxiety
• Blurred vision
• Tremors
• Convulsions
• Loss of perineal sensation and sexual function
• Persistent anesthesia
• Weakness and paralysis of the lower extremities
• Loss of sphincter control
• High or total spinal block
• Septic meningitis
• Shivering
• Cranial nerve palsies
• Fecal and urinary incontinence
• Slowing of labor
• Increased incidence of forceps delivery
• Hypersensitivity reactions including:
  • Hives (urticaria)
  • Itching (pruritus)
  • Redness (erythema)
  • Swelling of tissue under the skin and mucous membranes (angioneurotic edema)
  • Laryngeal edema
  • Loss of consciousness (syncope)
  • Severe allergic reaction (anaphylaxis)

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug.

Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

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)

Adult:

Subarachnoid block

• Lower extremity and perineal procedures (e.g., vaginal hysterectomy): 7.5 mg or 1 mL
• Lower abdominal procedures (appendectomy): 12 mg or 1.6 mL

Local Anesthesia

• Local infiltration: 0.25%; may increase up to 175 mg (70 mL) OK

Postsurgical Analgesia for Arthroscopic Subacromial Decompression

• Posimir only
• 660 mg once into subacromial space

Adult and Pediatric Patients Above 12 Years Old:

Regional Anesthesia

Sympathetic block

• 0.25%; 50-125 mg (20-50 mL)

Retrobulbar block

• 0.75%; 15-30 mg (2-4 mL)
• Complete corneal anesthesia usually precedes onset of clinically acceptable external ocular muscle akinesia; determine readiness for surgery based on presence of akinesia rather than anesthesia alone

Peripheral nerve block

• 0.25%; 12.5 -175 mg (5-70 mL) OR
• 0.5%: 25-175 mg (5-35 mL)

Caudal block

• Use as a test dose before caudal epidural blocks when clinical conditions permit
• 0.25%; 15-30 mL (37.5-75 mg) OR
• 0.5%: 15-30 mL (75-150 mg)

Lumbar epidural block

• Use as a test dose before lumbar epidural blocks when clinical conditions permit
• In obstetrics, use ONLY 0.5% and 0.25% concentrations; incremental doses of 3-5 mL of the 0.5% solution not exceeding 50-100 mg at any dosing interval are recommended
• Repeat doses should be preceded by a test dose containing epinephrine if not clinically contraindicated
• 0.25%; 10-20 mL (25-50 mg) OR
• 0.5%: 10-20 mL (50-100 mg) OR
• 0.75%: 10-20 mL (75-150 mg); for single-dose use; not for intermittent epidural technique or obstetrical anesthesia

Dosing Considerations

• Doses of any local anesthetic administered varies with anesthetic procedure, area to be anesthetized, vascularity of tissues, number of neuronal segments to be blocked, depth of anesthesia and degree of muscle relaxation required, duration of anesthesia desired, individual tolerance, and physical condition of patient
• Use smallest dose and concentration required to produce desired result

Posimir

• Different formulations are not bioequivalent even if dosage is the same
• Do not substitute

Limitations of use

• Not all blocks are indicated for use given clinically significant risks associated with use
• Posimir: Safety and efficacy not established in other procedures (e.g., soft tissue surgical procedures, other orthopedic procedures, boney procedures, used for neuraxial or peripheral nerve blockade)

Pediatric:

Local Anesthesia

Children younger than12 years:

• Not recommended; decreased dose by 30% in infants younger than 6 months, if necessary

Children 12 years and older:

• Local infiltration: 0.25%; may increase up to 2.5 mg/kg

Dosing Considerations

• Continuous infusions in pediatric patients reported to result in high systemic levels of bupivacaine and seizures; high plasma levels may also be associated with cardiovascular abnormalities
• Doses of any local anesthetic administered vary with anesthetic procedure, area to be anesthetized, vascularity of tissues, number of neuronal segments to be blocked, depth of anesthesia and degree of muscle relaxation required, duration of anesthesia desired, individual tolerance, and physical condition of patient
• Use smallest dose and concentration required to produce desired result
• Duration of action is dependent on concentration, total dose, and site of administration, use of epinephrine, and age

Limitations of use

• Marcaine: Not all blocks are indicated for use given clinically significant risks associated with use

Geriatric:

• In clinical studies, differences in pharmacokinetics have been observed in older adults compared with younger adults
• Bupivacaine is substantially excreted by kidneys
• Older adults may have decreased renal function and are at greater risk of adverse reactions to bupivacaine
• Consider a lower dose and closely monitor for toxicities

Dosage Modifications

Renal impairment

• Pharmacokinetics not evaluated
• Substantially excreted by the kidneys; may increase bupivacaine exposure and risk of systemic toxicities in patients with renal impairment
• All severities: Use with caution; consider frequent monitoring for adverse reactions

Hepatic impairment

• Pharmacokinetics not evaluated
• Owing to the inability to metabolize local anesthetics normally, patients with hepatic impairment are at risk of increased bupivacaine plasma levels and systemic toxicities
• Moderate-to-severe: Use with caution; consider reducing dosage and closely monitor

• Overdose from local administration of bupivacaine is usually related to systemic absorption and high blood concentration of the drug. Overdose, if not treated immediately, can lead to convulsions, respiratory abnormalities, low oxygen saturation in tissues (hypoxia) and irregular heart rhythms that can lead to cardiac arrest.
• Overdose is managed with intensive supportive care including respiratory support, convulsion treatment and cardiac life support measures, as needed.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Bupivacaine has no known severe interactions with other drugs.
• Serious interactions of bupivacaine include:
  • bupivacaine implant
  • ponesimod
• Moderate interactions of bupivacaine include:
  • benazepril
  • bupivacaine liposome
  • captopril
  • dofetilide
  • nadolol
  • nevirapine
  • pindolol
  • propranolol
  • timolol
• Mild interactions of bupivacaine include:
  • hyaluronidase

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• There are no adequate and well-controlled studies on bupivacaine use in pregnant women. Bupivacaine should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
• Bupivacaine is approved for use during labor and delivery for anesthesia or analgesia. It is used for intra-incisional analgesia at the end of a cesarean section and for pudendal nerve blocks used in the second stage of labor or for repairing perineal lacerations.
• Bupivacaine should not be used for paracervical block anesthesia, may cause fetal bradycardia and death.
• Bupivacaine is excreted in milk. Decision to breastfeed should be made after considering mother’s clinical need for bupivacaine and any potential adverse effects on breastfed child from the drug or the underlying maternal condition.