Bupivacaine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Parenteral Surgical anaesth Local infiltration: 0.25% soln: Up to 150 mg. Peripheral nerve block: 0.25% soln: 12.5 mg; 0.5% soln: 25 mg; doses of up to 150 mg may also be given. Retrobulbar block in ophth surgery: 0.75% soln: 15-30 mg. Sympathetic nerve block: 0.25% soln: 50-125 mg. Lumbar epidural block: 0.25% soln: 25-50 mg; 0.5% soln: 50-100 mg; 0.75% soln in non-obstetric surgery: 75-150 mg as single dose. Caudal block: 0.25% soln: 37.5-75 mg; 0.75% soln: 75-150 mg. Spinal block: 0.5% soln: 10-20 mg. Acute pain Lumbar block in labour pain: 0.25% soln: 15-30 mg; 0.375% soln: 22.5-45 mg; 0.5% soln: 30-60 mg. Alternatively, 0.1% soln: 10-15 mg/hr; 0.125% soln: 10-15 mg/hr via infusion. Caudal block in labour pain: 0.25% soln: 25-50 mg; 0.375% soln: 37.5-75 mg; 0.5% soln: 50-100 mg. Post-op pain 0.1% soln: 4-15 mg/hr; 0.125% soln: 5-15 mg/hr via epidural infusion. 1.3% liposomal susp: Bunionectomy: 106 mg as single dose; haemorrhoidectomy: 266 mg as single dose.
Dosage Details
Parenteral
Acute pain
Adult: Lumbar block in labour pain: 0.25% soln: 15-30 mg (6-12 mL); 0.375% soln: 22.5-45 mg (6-12 mL); 0.5% soln: 30-60 mg (6-12 mL). Alternatively, 0.1% soln: 10-15 mg (10-15 mL) per hr; 0.125% soln: 10-15 mg (8-12 mL) per hr via infusion. Caudal block in labour pain: 0.25% soln: 25-50 mg (10-20 mL); 0.375% soln: 37.5-75 mg (10-20 mL); 0.5% soln: 50-100 mg (10-20 mL).
Child: 1-12 yr Caudal/Lumbar/Thoracic epidural block: 0.25% soln: 1.5-2 mg/kg. Field block/Peripheral nerve block: 0.25 or 0.5% soln: 0.5-2 mg/kg.

Parenteral
Postoperative pain
Adult: 0.1% soln: 4-15 mg (4-15 mL) per hr; 0.125% soln: 5-15 mg (4-12 mL) per hr via epidural infusion. 1.3% liposomal susp: Bunionectomy: 106 mg (8 mL) as single dose (7 mL into surrounding tissues and 1 mL into SC tissue); haemorrhoidectomy: 266 mg (20 mL) as single dose, diluted to 30 mL preservative-free 0.9% NaCl for inj and infiltrated around the anal sphincter in 6 equally-divided portions.

Parenteral
Surgical anaesthesia
Adult: Local infiltration: 0.25% soln: Up to 150 mg (60 mL). Peripheral nerve block: 0.25% soln: 12.5 mg (5 mL); 0.5% soln: 25 mg (5 mL); doses of up to 150 mg may also be given. Retrobulbar block in ophth surgery: 0.75% soln: 15-30 mg (2-4 mL). Sympathetic nerve block: 0.25% soln: 50-125 mg (20-50 mL). Lumbar epidural block: 0.25% soln: 25-50 mg (10-20 mL); 0.5% soln: 50-100 mg (10-20 mL); 0.75% soln in non-obstetric surgery: 75-150 mg (10-20 mL) as single dose. Caudal block: 0.25% soln: 37.5-75 mg (15-30 mL); 0.75% soln: 75-150 mg (15-30 mL). Spinal block: 0.5% soln: 10-20 mg (2-4 mL).
Contraindications
Patient w/ active CNS disease (e.g. meningitis, intracranial haemorrhage), TB of the spine, pyogenic infection on inj site, pre-anaesth elevated intracranial pressure. Not intended for IV regional anaesth (Bier's block) and paracervical block in obstetrics; obstetric epidural block (0.75% soln).
Special Precautions
Patient w/ partial or complete heart block, impaired CV function and hypovolaemia; marked obesity, senility, cerebral atheroma, myocardial degeneration, toxaemia (epidural and spinal anaesth). May cause chondrolysis when given via intra-articular continuous infusion. Severe hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Bradycardia, hypotension, HTN, nausea, vomiting, diplopia, neuropathy, peripheral nerve injury, arachnoiditis, paresis and paraplegia, signs of CNS toxicity (e.g. convulsions, paraesthesia, tremor), dizziness, allergic reactions.
Potentially Fatal: Cardiac arrhythmia, cardiac and resp arrest.
Epidural/Intraspinal/IT/Parenteral/Perineural/SC: C
Patient Counseling Information
May temporarily impair locomotion and alertness.
MonitoringParameters
Monitor CV and resp vital signs, state of consciousness, signs of CNS toxicity.
Overdosage
Symptoms: Convulsions, circulatory arrest, cardiac arrest, resp paralysis, hypotension, bradycardia. Management: Establish and maintain a patent airway, oxygen may be needed. If necessary, may give anticonvulsant drugs.
Drug Interactions
Additive systemic toxic effect w/ other local anaesth or agents structurally related to amide-type local anaesth (e.g. lidocaine and mexiletine). Increased risk of myocardial depression w/ antiarrhythmics. Enhanced adverse effects w/ hyaluronidase. Decreased clearance resulting to increased plasma concentrations w/ cimetidine and ranitidine. Increased risk of adverse effects w/ β-blockers and Ca channel blockers.
Action
Description: Bupivacaine blocks both the initiation and conduction of nerve impulses reducing the permeability of neuronal membranes to Na ions resulting in inhibition of depolarization w/ resultant blockade of conduction.
Onset: 1-17 min (route and dose dependent).
Duration: 2-9 hr (route and dose dependent).
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 30-45 min.
Distribution: Crosses the placenta, diffuses into CSF and enters breast milk (small amounts). Plasma protein-binding: Approx 95%.
Metabolism: Hepatic via conjugation w/ glucuronic acid; converted to pipecoloxylidine (major metabolite).
Excretion: Via urine mainly as metabolites; 5-6% as unchanged drug. Half-life: 1.5-5.5 hr
Storage
Soln for inj: Store between 20-25°C. Protect from light; Liposomal susp: Store between 2-8°C.
References
Anon. Bupivacaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 25/07/2014.

Buckingham R (ed). Bupivacaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/07/2014.

Exparel Injection, Suspension, Liposomal (Pacira Pharmaceuticals Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 25/07/2014.

Wickersham RM. Bupivacaine HCl Injection. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed 25/07/2014.

Disclaimer: This information is independently developed by MIMS based on Bupivacaine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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