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NERVOUS SYSTEM › ANESTHETICS › ANESTHETICS, LOCAL › Amides
bupivacaine
N01BB01
Forms & Strengths
- Injectable solution: 0.25%, 0.5%, 0.75%
- Injectable solution with epinephrine: 0.25%, 0.5% (1:200,000)
- Liposomal injectable suspension: 1.33 mg/mL
Adult Dosing
- Local infiltration: 5 mg to 150 mg (0.25% or 0.5%), individualized based on area
- Epidural block: 10 mg to 150 mg depending on segment and desired depth of anesthesia
- Spinal block: 7.5 mg to 15 mg (typically 0.75% in dextrose 8.25%)
- Maximum safe dose (plain): 2 mg/kg (not to exceed 175 mg) without epinephrine
- Maximum safe dose (with epinephrine): 3 mg/kg (not to exceed 225 mg)
Pediatric Dosing
- Not recommended for children under 12 years for certain regional blocks
- Caudal block (children > 1 year): 1 to 2 mg/kg of 0.125% or 0.25% solution
- Peripheral nerve block: 1 to 1.25 mg/kg of 0.25% solution
Indications
- Local or regional anesthesia for surgery
- Dental procedures
- Labor and delivery (epidural/caudal)
- Postoperative pain management
Mechanism of Action
- Amide-type local anesthetic that reversibly binds to voltage-gated sodium channels in nerve fibers
- Blocks the influx of sodium ions, preventing depolarization and propagation of nerve impulses
Contraindications
- Known hypersensitivity to local anesthetics of the amide type
- Obstetric paracervical block (associated with fetal bradycardia and death)
- Intravenous regional anesthesia (Bier block) due to risk of systemic toxicity
Adverse Reactions
- Central nervous system: Tinnitus, metallic taste, dizziness, circumoral numbness, tremors, seizures
- Cardiovascular: Myocardial depression, hypotension, bradycardia, ventricular arrhythmias, cardiac arrest
- Neurologic: Transient root symptoms, arachnoiditis (with spinal use)
- Other: Urinary retention, nausea, vomiting, pruritus
Drug Interactions
- Class III antiarrhythmics (e.g., amiodarone): Additive cardiac depressant effects
- Other local anesthetics or structurally related agents: Additive systemic toxicity
- CNS depressants (sedatives, opioids): Enhanced central nervous system depression
- Vasopressors (when used with epinephrine): Severe persistent hypertension or cerebrovascular accidents
Curated Content: Needs Vetting Before Put to Clinical Use