Bupivacaine

Brand Names: Marcaine, Sensorcaine, Bupivacaine HCl

Drug Class: Amide local anesthetic

Overview

Bupivacaine is a long-acting amide local anesthetic used for local infiltration, peripheral nerve blocks, epidural anesthesia, and spinal anesthesia. It provides prolonged anesthesia with a slow onset of action (5-10 minutes).

Mechanism of Action

Bupivacaine blocks voltage-gated sodium channels in neuronal cell membranes, inhibiting depolarization and propagation of action potentials, thereby preventing nerve signal transmission and producing local anesthesia.

Indications

  • Local infiltration anesthesia
  • Peripheral nerve blocks
  • Epidural anesthesia
  • Spinal anesthesia
  • Postoperative pain management

Dosage

Dosage varies by route and procedure. Maximum recommended dose: 400 mg per 24 hours (or 2 mg/kg). For epidural anesthesia: 10-20 mL of 0.25% to 0.75% solution. Always use lowest effective dose.

Black Box Warning

WARNING: LOCAL ANESTHETIC TOXICITY. Bupivacaine can cause dose-related toxicity. Use in obstetrical paracervical block anesthesia is contraindicated. Use the lowest effective dose.

Contraindications

  • Hypersensitivity to amide local anesthetics
  • Severe hypotension
  • Septicemia
  • Infection at injection site
  • Coagulopathy or anticoagulant therapy (for neuraxial blocks)

Side Effects

  • Hypotension
  • Bradycardia
  • Nausea
  • Vomiting
  • Headache
  • Back pain
  • Urinary retention
  • Paresthesia
  • Seizures (with systemic toxicity)
  • Cardiac arrest (with intravascular injection)

Interactions

  • MAO inhibitors: increased risk of hypotension
  • Beta-blockers: additive bradycardia
  • Other local anesthetics: additive toxicity
  • Vasoconstrictors (epinephrine): may enhance duration but increase cardiovascular effects