Bupivacaine

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Contents 1 More Specific Terms 2 Introduction 3 Indications 4 Contraindications 5 Dosage 6 Pharmacokinetics 7 Adverse-effects 8 Mechanism-of-action 9 More General Terms 10 Internet Database 11 References

More Specific Terms

• levobupivacaine (Chirocaine)

Introduction

• Tradenames: Marcaine, Sensorcaine.

Indications

• local anesthetic
• used in "blocks" for anesthesia & analgesia

• sympathetic block
• caudal or epidural block
• retrobulbar block

Contraindications

• use with caution in patients with liver disease
• do not use in children < 12 years of age
• do not use for spinal anesthesia in children < 18 years of age
  

Dosage

• caudal block (with or without epinephrine)

• adults: 15-30 mL of 0.25% or 0.5%
• children: 1-3.7 mg/kg

• epidural block (other than caudal block)

• adults: 10-20 mL of 0.25% or 0.5%
• children: 1.25 mg/kg/dose

• peripheral nerve block:

• 5 mL dose of 0.25% or 0.5% (12.5-25 mg)
• maximum:

• 2.5 mg/kg (without epinephrine)
• 3 mg/kg (with epinephrine)
• up to 400 mg/day

• sympathetic nerve block

• 25-50 mL of 0.25% solution without epinephrine

• Injection: 0.25%, 0.5%, 0.75% with or without epinephrine.

Pharmacokinetics

• onset of action 2-15 minutes depending upon site of injection
• duration 3-7 hours (longer acting local anesthetic than lidocaine)
• highly protein bound (low transfer across placenta)
• co-administration of epinephrine prolongs the action & localizes the anesthesia
• small amount (6%) excreted in urine
  

• elimination via liver
• elimination via kidney
• 1/2life = 1.5-5 hours

Adverse-effects

• not common (1-10%, dose-related) [3]

• cardiac arrest*, hypotension, bradycardia, palpitations, seizures*, restlessness, anxiety, dizziness, weakness, nausea/vomiting, blurred vision, tinnitus, apnea

• other [2]

• confusion
• bradycardia
• drowsiness
• paresthesias
• agitation
• tremors
• psychosis
• visual disturbances
• respiratory depression
• urticaria
• allergic reactions
• sulfite reactions in sulfite-containing preparations

• * cardiac arrest & convulsions associated with high plasma concentrations after inadvertant intravascular administration

Mechanism-of-action

• amide-type local anesthetic
• reversibly blocks nerve conduction in all nerve fibers ( sensory, motor & autonomic fibers)
• decreases permeability of nerves to Na+
• increases threshold of excitability
• prevents propogation of action potential
• autonomic activity lost 1st, followed by sensory & motor function

More General Terms

• local anesthetic

Internet Database

PubChem: 2474
PubChem: 64737
PubChem: 5282419
PubChem: 117963
PubChem: 92253

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
3. Kaiser Permanente Northern California Regional Drug Formulary, 1998

bupivacaine (Marcaine, Sensorcaine)