Clinical beta

FMBM is currently in clinical beta. Content is for professional review/testing and must not replace local protocols, senior clinical judgment, or official prescribing references.

Drug Monograph

Bupivacaine

USE IF: Spinal/epidural anesthesia, peripheral nerve blocks, long-duration surgical analgesia

AVOID IF: Unsafe setting (no lipid rescue), obstetric epidural with 0.75%, IV use, Bier block

Bupivacaine

Amide local anesthetic (long-acting)

Regional anesthesiaNerve blockEpiduralSpinalHigh cardiotoxicityLAST risk

Indication

Spinal/epidural anesthesia, peripheral nerve blocks, long-duration surgical analgesia

At a glance

INDICATION -> Long-acting regional anesthesia (epidural, spinal, nerve blocks)

ADULT DOSE -> 2-2.5 mg/kg (no epi), 2.5-3 mg/kg (with epi)

MAX DOSE -> 175 mg (no epi), 225 mg (with epi), max daily 400 mg

CONTRA -> Unsafe setting (no lipid rescue), obstetric epidural with 0.75%, IV use, Bier block

ANTIDOTE -> Lipid Emulsion 20% (Intralipid)

Quick facts

Onset

1-5 min (spinal), 4-17 min (epidural), 5-15 min (nerve block)

Duration

Peak 30-45 min. Duration 2-5 h (epidural/spinal), 3-8 h (with epinephrine), liposomal up to 96 h. Half-life ~2.7 h (longer in neonates/hepatic disease).

Routes

Epidural, spinal, nerve block, infiltration (NO IV)

Pregnancy

Safe except 0.75% epidural in obstetrics

Renal

Usually no adjustment

Hepatic

Reduce dose

Do not miss

Time to action: depends on route; monitor block spread closely

Cardiotoxicity risk

  • HIGH cardiotoxicity risk -> refractory ventricular arrhythmias and cardiac arrest (harder to resuscitate than lidocaine).
  • 0.75% epidural in obstetrics is black-box level danger and should never be used.
  • Bier block (IV regional anesthesia) is absolutely contraindicated.

Critical actions

  • Lipid rescue may be less effective than with lidocaine; prevention is critical.
  • Always aspirate and inject incrementally.
  • Lipid emulsion MUST be immediately available before administering bupivacaine.

Antidote

  • Lipid emulsion 20%: 1.5 mL/kg bolus -> infusion 0.25 mL/kg/min (repeat bolus if needed).

High-risk scenarios

  • High-concentration obstetric epidural.
  • Intravascular injection risk.

Key interactions

  • Antiarrhythmics/cardiodepressants can worsen instability.
  • Epinephrine interaction cautions apply.

Indications

Primary

  • Spinal anesthesia (C-section, lower surgery)
  • Epidural anesthesia (labor, surgery)
  • Peripheral nerve blocks
  • Local infiltration

Secondary

  • Continuous epidural analgesia
  • Cancer pain/regional pain control

Other

  • Migraine nerve blocks
  • CRPS sympathetic blocks
  • Scalp blocks (neurosurgery)

Dosing

Standard: 2-2.5 mg/kg (no epi), 2.5-3 mg/kg (with epi)

Max daily dose

  • Without epinephrine: 2-2.5 mg/kg (max 175 mg).
  • With epinephrine: 2.5-3 mg/kg (max 225 mg).
  • Maximum dose depends on technique and site; ALWAYS use lowest effective dose and avoid cumulative toxicity.

Adult - PO

  • Not applicable for systemic oral use.

Adult - IV

  • Do NOT use IV for regional anesthesia.
  • Bier block is contraindicated.

Pediatric

  • ~1-2.5 mg/kg depending on route and specialist protocol.

Renal adjustment

  • Usually no formal adjustment.

Hepatic adjustment

  • Reduce dose by ~30-75% depending on severity.

Warnings

Clinical warnings

  • Extreme cardiotoxicity (refractory VF).
  • LAST can skip CNS signs and present as direct cardiac collapse.
  • Hypotension from spinal/epidural sympathetic block.
  • High/total spinal can cause respiratory arrest.
  • Chondrolysis risk with intra-articular infusion.
  • Methemoglobinemia is rare.
  • Incorrect neuraxial dosing can cause catastrophic outcomes.

Adverse effects

  • Common: hypotension, nausea, local numbness/motor block.
  • Serious: refractory arrhythmia, cardiac arrest, severe LAST.

Contraindications / caution

Do not use

  • IV administration (except accidental exposure/toxicity context).
  • Bier block.
  • 0.75% epidural concentration in obstetrics.
  • Hypersensitivity.
  • Severe shock states.

Use caution / avoid high doses

  • Hepatic impairment.
  • Elderly.
  • Cardiac disease.
  • Coagulopathy for neuraxial techniques.
  • Infection at injection site.

Drug interactions

  • Other local anesthetics -> additive toxicity.
  • Class I/III antiarrhythmics -> increased cardiac depression.
  • Beta-blockers + epinephrine -> severe hypertension/bradycardia risk.
  • MAOIs + epinephrine -> hypertensive crisis risk.
  • Ergot drugs + epinephrine -> severe vasoconstriction risk.
  • Methemoglobinemia-inducing drugs -> additive risk.

Special populations

Pediatrics

Specialist dosing required.

Pregnancy

Safe for neuraxial use except 0.75% epidural; avoid paracervical block.

Breastfeeding

Generally safe with minimal transfer.

Elderly

Reduce dose; higher spread and toxicity risk.

Liver disease

Significant dose reduction needed.

Renal impairment

Usually no dose adjustment.

Administration

  • Spinal: preservative-free only; confirm CSF before injection.
  • Epidural: test dose required; incremental 3-5 mL dosing.
  • Nerve block: ultrasound guidance preferred; aspirate before injection.
  • Avoid large doses in highly vascular areas due to increased systemic absorption and LAST risk.
  • Local infiltration: incremental dosing.
  • Liposomal formulation: single dose only (max 266 mg); do not mix with other local anesthetics.

Monitoring

  • ECG during and after block.
  • Frequent blood pressure checks (hypotension risk).
  • CNS signs for early LAST detection.
  • Respiratory status (high spinal risk).
  • Block level (dermatome + motor).
  • Cumulative dose tracking.
  • Lipid emulsion availability confirmation before use.

Overdose / toxicity

STOP injection immediately -> airway + 100% oxygen -> treat as LAST emergency.

Recognition

  • Early signs can include tingling, metallic taste, tinnitus (may be absent).
  • Progression: seizures -> cardiovascular collapse -> arrest.
  • Bupivacaine may cause abrupt cardiac arrest without warning.

Immediate actions

  • Benzodiazepines for seizures.
  • Lipid Emulsion 20% bolus 1.5 mL/kg.
  • Then infusion 0.25 mL/kg/min.

Antidote

  • Lipid Emulsion 20% protocol for LAST.

Decontamination

  • Not typically relevant in parenteral LAST.

Escalation

  • Cardiac arrest may require prolonged CPR (60-90 min).
  • Use low-dose epinephrine (<=1 mcg/kg).
  • Consider VA-ECMO if refractory.

Clinical pearls

Common mistakes, resistance logic, and bedside traps

Not lidocaine-equivalent

  • Bupivacaine is much more dangerous than lidocaine in systemic toxicity.

Obstetric black box

  • 0.75% epidural in obstetrics = NEVER.

Differential block

  • Low-dose epidural can provide analgesia with less motor block.

Prevention first

  • Lipid rescue may be less effective; prevention is key.

Ultrasound safety

  • Ultrasound guidance significantly reduces complications.

Dose tracking

  • Always track cumulative dose across all sources.

Cardiac channel binding

  • Bupivacaine binds strongly to cardiac sodium channels -> prolonged toxicity and difficult resuscitation.

Safer alternative

  • Consider levobupivacaine (Chirocaine) for safer cardiac profile where available.

Pharmacokinetics

  • Highly lipophilic.
  • Protein binding ~95%.
  • Hepatic metabolism (CYP3A4).
  • Active metabolite PPX.
  • Renal excretion of metabolites.
  • Half-life prolongs in neonates and liver disease.

Mechanism of action

  • Blocks voltage-gated sodium channels.
  • Prevents depolarization -> anesthesia.
  • Slow dissociation creates prolonged effect.
  • Strong cardiac binding contributes to persistent toxicity risk.

Common brand names

Saudi Arabia

Marcaine · Marcaine Spinal · Bupivacaine Fresenius Kabi · Chirocaine

Global

Sensorcaine · Exparel · Posimir · Bupivacaine (generic)

Common trade names are curated examples only — formulations and availability vary. Verify the exact product name with your local pharmacy and national regulator before prescribing or dispensing.

Country practice notes

  • Marcaine is the dominant formulation across Saudi Arabia and GCC.
  • Widely used in anesthesia, labor analgesia, and postoperative pain control.
  • UAE also uses Chirocaine (levobupivacaine) with safer cardiac profile context.
  • Essential anesthetic in GCC hospital formularies.

Saudi Arabia — confirm with local formulary.