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NERVOUS SYSTEM › ANESTHETICS › ANESTHETICS, LOCAL › Amides
bupivacaine, combinations
N01BB51
Forms & Strengths
- Injectable solution: Bupivacaine HCl 0.25%, 0.5%, 0.75% (often combined with epinephrine 1:200,000)
Adult Dosing
- Local infiltration: 5 mg to 60 mg (0.25%)
- Epidural block: 10 mg to 150 mg depending on segment and desired depth
- Spinal block: 7.5 mg to 15 mg (0.75% in dextrose 8.25%)
- Maximum recommended dose without epinephrine: 2 mg/kg (up to 150 mg)
- Maximum recommended dose with epinephrine: 3 mg/kg (up to 200 mg)
Pediatric Dosing
- Caudal block (>12 months): 1.0 to 1.25 mg/kg of 0.125% or 0.25% solution
- Safety and efficacy in neonates and infants under 12 months not fully established for all regional blocks
Indications
- Production of local or regional anesthesia or analgesia for surgery, dental procedures, and obstetric procedures
- Epidural, caudal, peripheral nerve block, and local infiltration
Mechanism of Action
- Amide-type local anesthetic; blocks nerve impulses by decreasing neuronal membrane permeability to sodium ions
- Inhibits depolarization, preventing initiation and conduction of nerve impulses
- Epinephrine addition causes local vasoconstriction, decreasing systemic absorption and prolonging duration of action
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
- Severe shock or heart block (for spinal/epidural routes)
Adverse Reactions
- Cardiovascular: Hypotension, bradycardia, arrhythmias, cardiac arrest (due to systemic toxicity)
- Central Nervous System: Tinnitus, metallic taste, circumoral numbness, dizziness, tremors, seizures, CNS depression
- Respiratory: Respiratory depression, apnea
- Allergic: Anaphylactoid reactions, urticaria, angioedema
Drug Interactions
- Class III antiarrhythmic drugs (e.g., amiodarone): Additive cardiac effects
- Other local anesthetics or structurally related agents: Additive systemic toxicity
- Monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants: Severe hypertension or arrhythmias when combined with epinephrine formulations
- Non-depolarizing muscle relaxants: Prolongation of neuromuscular blockade
Curated Content: Needs Vetting Before Put to Clinical Use