bupivacaine (Marcaine, Sensorcaine)

Dosing and uses of Marcaine, Sensorcaine (bupivacaine)

• Adult
• Pediatric

 

Adult dosage forms and strengths

injectable solution

• 0.25%
• 0.5%
• 0.75%

 

Local Anesthesia

Infiltration: 0.25% infiltrated locally: 175 mg maximum

 

Caudal Block

Preservative free: 15-30 mL of 0.25% or 0.5%

 

Epidural Block Other Than Caudal Block

Preservative free: 10-20 mL of 0.25% or 0.5%; administer in 3-5 mL increments allowing sufficient time to detect toxic manifestations of inadvertent IV or IT administration

Surgical procedures requiring high degree of muscle relaxation and prolonged effects: 10-20 mL of 0.75%; not to be used in obstetrical cases

 

Peripheral Nerve Block

5 mL of 0.25-0.5%; 400 mg/day maximum

 

Sympathetic Nerve Block

20-50 mL of 0.25%

 

Retrotubular Anesthesia

2-4 mL of 0.75%

 

Spinal Anesthesia

Preservative free: 0.75% bupivacaine in 8.25% dextrose

 

Postherpetic Neuralgia (Orphan)

Relief of persistent pain associated with postherpetic neuralgia

Administration: TransdermaL

Orphan indication sponsor

• Alpharma Pharmaceuticals, LLC; 400 Crossing Blvd, Subsidiary of King Pharmaceuticals, Inc; Bridgewater, NJ 088

 

Pediatric dosage forms and strengths

injectable solution

• 0.25%
• 0.5%
• 0.75%

 

Caudal Block, Epidural Block, Local Block

<12 years

• Not recommended

>12 years

• Local Anesthesia: Infiltration 0.25% infiltrated locally: 175 mg maximum
• Caudal Block: 15-30 mL of 0.25% or 0.5% (preservative free)
• Epidural Block Other Than Caudal Block: 10-20 mL of 0.25% or 0.5%; administer in 3-5 mL increments allowing sufficient time to detect toxic manifestations of inadvertent IV or IT administration (preservative free); for surgical procedures requiring high degree of muscle relaxation and prolonged effects administer10-20 mL of 0.75%; not to be used in obstetrical cases

 

Peripheral or Sympathetic Nerve Block

<12 years

• Not recommended

>12 years

• Peripheral Nerve Block: 5 mL of 0.25-0.5%; 400 mg/day maximum
• Sympathetic Nerve Block: 20-50 mL of 0.25%

 

Retrotubular Anesthesia

<12 years

• Not recommended

>12 years

• 2-4 mL of 0.75%

 

Marcaine, Sensorcaine (bupivacaine) adverse (side) effects

Frequency not defined

Anaphylactoid reactions (sometimes fatal)

Anginal pain

Anxiety

Apprehension

Blurred vision

Bradycardia

Cardiovascular collapse

Cardiac arrest

Cardiac arrhythmias

Chills

Confusion/disorientation

Dizziness

Drowsiness

Edema

Headache

Hypotension

Hypoventilation

HTN (epinephrine-containing solutions)

Loss of consciousness

Miosis

Myocardial depression

Nausea

Nervousness

Palpitation

Respiratory arrest

Restlessness

Shivering

Seizures

Status asthmaticus

Tachycardia

Tinnitus

Tremors

Vomiting

 

Warnings

Black box warnings

The 0.75% concentration of bupivacaine is not recommended for obstetrical anesthesia; cardiac arrest with difficult resuscitation or death reported when used as epidural anesthesia in obstetrical patients; reserve the 0.75% concentration for surgical procedures where a high degree of muscle relaxation and prolonged effect are necessary

Preservative-containing solutions should not be used for caudal or epidural block

 

Contraindications

Hypersensitivity, sensitivity to parabens

Obstetrical paracervical block anesthesia

Intravenous regional anesthesia use

 

Cautions

History of malignant hyperthermia

DO NOT use solutions with epinephrine in distal areas of body (eg, digit, nose, ear, etc)

Use preservative-free preparations for spinal or epidural anesthesia

Avoid intravascular administration

Addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase duration of action

Test dose recommended for epidural administration

Caution in cardiovascular disease including hypotension or heart block

Cardiac arrest, arrhythmia and death reported with use of bupivacaine containing products

Confusion, convulsions, respiratory depression, and/or respiratory arrest, and cardiovascular stimulation or depression reported

Use caution in patients with hepatic impairment

Use caution in the elderly, the acutely ill or debilitated patient (may require dose reduction)

Chondrolysis associated with intra-articular infusions following arthroscopic and other surgical procedures (off-label use)

 

Pregnancy and lactation

Pregnancy category: C

Lactation: excretion in milk unknown/not recommended

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Marcaine, Sensorcaine (bupivacaine)

Mechanism of action

Local anesthetics prevent generation/conduction of nerve impulses by reducing sodium permeability & increasing action potential threshold

 

Pharmacokinetics

Duration: 2-9 hr (The greater the degree of vasodilation produced by the local anesthetic, the faster the absorption rate & the shorter the duration of action; bupivacaine has a long duration of action)

Protein bound: 95%

Onset of action: 1-17 min (route and dose dependent)

Metabolism: Liver

Peak plasma time: 30-45 min (caudal, epidural, or peripheral nerve block)

Half-life: 8.1 hr (neonates); 2.7 hr (adults)

Metabolites: Ester- & amide-type local anesthetics

Excretion: Urine (principally)