Dosing & Uses
Dosage Forms & Strengths
Infiltration: 0.25% infiltrated locally: 175 mg maximum
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%
2-4 mL of 0.75%
Preservative free: 0.75% bupivacaine in 8.25% dextrose
Postherpetic Neuralgia (Orphan)
Relief of persistent pain associated with postherpetic neuralgia
Orphan indication sponsor
- Alpharma Pharmaceuticals, LLC; 400 Crossing Blvd, Subsidiary of King Pharmaceuticals, Inc; Bridgewater, NJ 088
Dosage Forms & Strengths
Caudal Block, Epidural Block, Local Block
- Not recommended
- 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
- Not recommended
- Peripheral Nerve Block: 5 mL of 0.25-0.5%; 400 mg/day maximum
- Sympathetic Nerve Block: 20-50 mL of 0.25%
- Not recommended
- 2-4 mL of 0.75%
Serious - Use Alternative
Significant - Monitor Closely
Frequency Not Defined
Anaphylactoid reactions (sometimes fatal)
HTN (epinephrine-containing solutions)
Loss of consciousness
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
Hypersensitivity, sensitivity to parabens
Obstetrical paracervical block anesthesia
Intravenous regional anesthesia use
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 & Lactation
Pregnancy Category: C
Lactation: excretion in milk unknown/not recommended
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.
Mechanism of Action
Local anesthetics prevent generation/conduction of nerve impulses by reducing sodium permeability & increasing action potential threshold
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)
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)
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