bupivacaine
Amide local anesthetic· Brands: Marcaine, Sensorcaine, BupivanSC
Mechanism of action
Bupivacaine is an amide-type local anesthetic that blocks voltage-gated sodium channels on nerve membranes. By inhibiting sodium influx, it prevents the generation and conduction of action potentials, producing reversible regional anaesthesia. Bupivacaine blocks both sensory and motor fibres, with a relatively slow onset and long duration of action.
Pharmacokinetics
Bupivacaine is well absorbed from injection sites. It is approximately 95% bound to plasma proteins, mainly alpha-1 acid glycoprotein. It undergoes hepatic metabolism via CYP3A4 to pipecoloxylidine and other metabolites, with less than 10% excreted unchanged in urine. The elimination half-life is about 2.7 hours in adults. Onset of action is 5-10 minutes, with duration of 3-12 hours depending on dose and route.
Indications & dosing
Local infiltration anaesthesia for minor surgical procedures
Administered as 0.25% or 0.5% solution. Dose depends on extent of anaesthesia and patient weight. Maximum dose without epinephrine is 175 mg; with epinephrine, 225 mg.
- adult · SC: 25–150 mg single dose · Administered as 0.25% or 0.5% solution. Dose depends on extent of anaesthesia and patient weight. Maximum dose without epinephrine is 175 mg; with epinephrine, 225 mg.
Peripheral nerve block (e.g., brachial plexus, femoral nerve)
Typically 20-30 mL of 0.25% or 0.5% solution, often with epinephrine. Provides prolonged anaesthesia and analgesia. Maximum single dose without epinephrine is 175 mg.
- adult · SC: 50–150 mg single dose · Typically 20-30 mL of 0.25% or 0.5% solution, often with epinephrine. Provides prolonged anaesthesia and analgesia. Maximum single dose without epinephrine is 175 mg.
Contraindications & precautions
- Known hypersensitivity to bupivacaine or other amide local anaesthetics · Includes previous allergic reaction to amide agents.
- Intravenous regional anaesthesia (Bier's block) · Risk of severe systemic toxicity and cardiac arrest.
- Obstetric paracervical block · Associated with fetal bradycardia and neonatal toxicity.
- Severe hepatic impairment · Reduced metabolism increases systemic toxicity risk.
- Severe hypotension · May exacerbate cardiovascular compromise.
- Use the lowest effective dose and aspirate before injection to avoid intravascular injection.
- Avoid use in patients with severe hepatic impairment as metabolism is reduced.
- Use with caution in patients with cardiac disease, especially conduction disorders.
- Avoid injection into inflamed or infected tissues as it may increase absorption.
- Have resuscitation equipment and emergency drugs available in case of systemic toxicity.
- Use with caution in elderly and debilitated patients as they are more susceptible to toxicity.
Adverse effects
- Hypotension
- Bradycardia
- Nausea
- Dizziness or lightheadedness
- Seizuresserious
- Cardiac arrhythmiasserious
- Cardiac arrestserious
- Anaphylaxisserious
Renal & hepatic adjustment
- Hepatic impairment (moderate): Reduce dose or use lower concentration; monitor closely for toxicity.
- Hepatic impairment (severe): Avoid use or use with extreme caution in severe hepatic impairment due to increased risk of toxicity. (avoid)
Monitoring, pregnancy & toxicity
- Blood pressure and heart rate · During and after administration
- ECG · Continuous monitoring during high-dose or epidural use
- Neurological status (CNS symptoms: tinnitus, confusion, seizures) · After administration and for at least 30 minutes after block
- Signs of local anaesthetic systemic toxicity (LAST) · During and after administration; monitor for early signs of intravascular injection
- Injection site · Check for accidental intravascular injection before and during injection
- Pregnancy: Bupivacaine is used for regional anaesthesia in pregnancy. It may be used when clinically indicated; the lowest effective dose is recommended. Fetal monitoring may be required during labour epidural use.
- Toxicity: CNS excitation: restlessness, tinnitus, visual disturbances, seizures. · Stop administration, provide oxygen, manage seizures with benzodiazepines, call for help.
- Toxicity: CNS depression: drowsiness, coma, respiratory depression. · Support airway, breathing and circulation; consider lipid emulsion therapy.
- Toxicity: Cardiovascular toxicity: hypotension, bradycardia, ventricular arrhythmias, cardiac arrest. · Start Advanced Life Support, administer IV 20% lipid emulsion at 1.5 mL/kg bolus, then infusion.
- Toxicity: Allergic reactions: skin rash, bronchospasm, anaphylaxis. · Stop bupivacaine, treat with adrenaline, antihistamines, steroids as per anaphylaxis protocol.
Antidotes & reversal
- 20% lipid emulsion ( Intralipid ) · Local anaesthetic systemic toxicity: 1.5 mL/kg bolus then infusion per LAST protocol; resuscitation may be prolonged.
Clinical notes
Bupivacaine is used for local infiltration, peripheral nerve blocks, epidural and spinal anaesthesia, and postoperative pain management. It is more cardiotoxic than lidocaine, so care must be taken to avoid accidental intravascular injection and to respect maximum recommended doses. Bupivacaine is contraindicated for intravenous regional anaesthesia (Bier's block) due to risk of systemic toxicity. Regional formularies may specify different concentrations and preparations.
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BNF; local formulary