Levobupivacaine


Generic Medicine Info
Indications and Dosage
Epidural
Acute pain
Adult: For labour pain: 15-25 mg (6-10 mL) or 25-50 mg (10-20 mL) via epidural bolus, may be repeated at intervals of at least 15 minutes, as 0.25% solution. Max cumulative dose: 400 mg/24 hours. Alternatively, 5-12.5 mg/hour via continuous epidural infusion as 0.0625% solution (8-20 mL/hour) or as 0.125% solution (4-10 mL/hour). Max infusion rate: 12.5 mg/hour. Max cumulative dose: 400 mg/24 hours. For postoperative pain: 12.5-18.75 mg/hour via continuous epidural infusion as 0.0625% solution (20-30 mL/hour), or 0.125% solution (10-15 mL/hour), or 0.25% solution (5-7.5 mL/hour). Max infusion rate: 18.75 mg/hour. Max cumulative dose: 400 mg/24 hours. Use the lowest effective dose and concentration. Dosage may depend on inj site, procedure and status of the patient.
Elderly: Dose reduction may be required.

Epidural
Surgical anaesthesia
Adult: For surgery: 50-150 mg (10-20 mL) via slow epidural bolus over 5 minutes as 0.5-0.75% solution. Max single dose: 150 mg. Max cumulative dose: 400 mg/24 hours. For caesarean section: 75-150 mg (15-30 mL) via slow epidural bolus over 15-20 minutes as 0.5% solution. Max single dose: 150 mg. Prior to starting epidural anaesthesia, a test dose of 3-5 mL lidocaine with epinephrine is recommended to observe for any toxic effects of unintended intravascular or intrathecal inj. Use the lowest effective dose and concentration. Dosage may depend on inj site, procedure and status of the patient.
Elderly: Dose reduction may be required.

Intrathecal
Surgical anaesthesia
Adult: 15 mg (3 mL) as 0.5% solution. Use the lowest effective dose and concentration. Dosage may depend on inj site, procedure and status of the patient.
Elderly: Dose reduction may be required.

Parenteral
Surgical anaesthesia
Adult: For local infiltration: 2.5-150 mg (1-60 mL) as 0.25% solution. Max: 150 mg. For peribulbar block in ophthalmic procedures: 37.5-112.5 mg (5-15 mL) as 0.75% solution. For peripheral nerve block: 2.5-150 mg (1-40 mL) as 0.25% or 0.5% solution. Max: 150 mg. Use the lowest effective dose and concentration. Dosage may depend on inj site, procedure and status of the patient.
Child: >6 months to <12 years For local infiltration (ilioinguinal or iliohypogastric block): 1.25 mg/kg/side (0.5 mL/kg/side) as 0.25% solution or 1.25 mg/kg/side (0.25 mL/kg/side) as 0.5% solution. Max: 1.25 mg/kg/side.
Elderly: Dose reduction may be required.
Special Patient Group
Acutely ill or debilitated patients: Dose reduction may be required.
Reconstitution
Dilute with 0.9% NaCl solution for inj; use immediately or within 24 hours of preparation. Refer to the detailed product guideline for compatible in combination agents (e.g. with clonidine, morphine, fentanyl) and their stability.
Incompatibility
May be precipitated with alkaline solutions (e.g. Na bicarbonate inj).
Contraindications
Severe hypotension (e.g. cardiogenic or hypovolaemic shock). Administration into inflamed or infected tissue, via IV regional anaesthesia (e.g. Bier’s block), obstetric paracervical block; obstetric epidural blocks (as 0.75% solution); epidural, caudal, or spinal block (preparations with preservatives).
Special Precautions
Patient with hypotension, CV disease (e.g. severe cardiac arrhythmia, heart block), respiratory disease, pre-existing CNS disease (e.g. epilepsy, myasthenia gravis), hypovolaemia, shock; cirrhosis, alcoholism. Acutely ill or debilitated patients. Hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Acute allergic reactions (e.g. anaphylactic shock), CV effects (e.g. depression of cardiac conduction, reduction in myocardial excitability and contractility), convulsion, cauda equina syndrome, transient Horner’s syndrome (characterised by ptosis, miosis, enophthalmos, unilateral sweating and/or flushing). Rarely, neurological damage.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Atrioventricular block, tachycardia, ventricular tachyarrhythmia.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Constipation, nausea, oral hypoaesthesia, vomiting.
General disorders and administration site conditions: Fever.
Injury, poisoning and procedural complications: Procedural pain.
Investigations: Decreased cardiac output, changes in ECG.
Musculoskeletal and connective tissue disorders: Back pain, muscle twitching or weakness.
Nervous system disorders: Dizziness, headache, paraesthesia, loss of consciousness, paraplegia, paralysis.
Pregnancy, puerperium and perinatal conditions: Foetal distress syndrome.
Renal and urinary disorders: Bladder dysfunction.
Reproductive system and breast disorders: Priapism.
Respiratory, thoracic and mediastinal disorders: Apnoea, sneezing.
Skin and subcutaneous tissue disorders: Anhidrosis, erythema, hyperhidrosis, pruritus.
Potentially Fatal: Severe bradycardia, hypotension, respiratory compromise, cardiac arrest.
Patient Counseling Information
This drug may impair your mental alertness or ability for some time after administration; if affected, do not drive or operate machinery.
Monitoring Parameters
Closely monitor patient’s state of consciousness, neurological, CV, circulatory, and respiratory (e.g. adequacy of ventilation) vital signs during administration; for signs and symptoms of adverse effects due to unintended intravascular or intrathecal inj.
Overdosage
Symptoms: Hypotension, severe bradycardia; convulsions which, if untreated immediately, may result in hypoxia, hypercarbia, myocardial depression and subsequent cardiac arrhythmia, ventricular fibrillation and cardiac arrest. Management: Provide oxygen support. May give IV thiopentone or diazepam with caution to treat convulsion; neuro-muscular blockers may be used only if a patent airway can be maintained and a fully paralysed patient can be managed. May administer IV fluids and vasopressors to prevent hypotension; IV crystalloids or colloids and/or incremental dose of vasopressor (e.g. 5-10 mg ephedrine) to treat hypotension; 0.3-1 mg atropine to restore heart rate for severe bradycardia. Perform cardioversion to treat ventricular fibrillation and as necessary treatment for cardiac arrhythmia.
Drug Interactions
May cause additive toxic effects with other local anaesthetics and antiarrhythmics with local anaesthetic activity (e.g. mexiletine, class III antiarrhythmic agents). May decrease the plasma concentrations with CYP3A4 inducers (e.g. phenytoin, rifampicin). May reduce the metabolism and increase the plasma levels with CYP3A4 inhibitors (e.g. ketoconazole, erythromycin, verapamil) and CYP1A2 inhibitors (e.g. methylxanthines).
Action
Description: Levobupivacaine, the S-enantiomer of bupivacaine, is a long-acting local anaesthetic of the amino amide class. It blocks the nerve impulse generation and conduction in sensory and motor nerves by mainly interacting with the intracellular portion of voltage-gated Na channel on the cell membrane. Additionally, levobupivacaine also interferes with the transmission and conduction of impulse in other tissues.
Pharmacokinetics:
Distribution: Crosses the placenta. Plasma protein binding: >97%.
Metabolism: Extensively metabolised in the liver by CYP3A4 isoenzyme into desbutyl-levobupivacaine and by CYP1A2 isoenzyme into 3-hydroxy-levobupivacaine (major metabolite). 3-hydroxy-levobupivacaine is further metabolised into glucuronide and sulfate conjugates.
Chemical Structure

Chemical Structure Image
Levobupivacaine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 92253, Levobupivacaine. https://pubchem.ncbi.nlm.nih.gov/compound/Levobupivacaine. Accessed Jan. 26, 2021.

Storage
Store between 15-30°C. Solutions diluted in 0.9% NaCl may be stored between 20-22°C for 7 days.
ATC Classification
N01BB10 - levobupivacaine ; Belongs to the class of amides. Used as local anesthetics.
References
Anon. Levobupivacaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/11/2020.

Buckingham R (ed). Levobupivacaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/11/2020.

Chirocaine (AbbVie Pte Ltd). MIMS Singapore. http://www.mims.com/singapore. Accessed 13/11/2020.

Chirocaine 5.0 mg/mL Injection (AbbVie Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 03/12/2020.

Joint Formulary Committee. Levobupivacaine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/11/2020.

Levobupivacaine 0.625 mg/mL Solution for Infusion (Fresenius Kabi Limited). MHRA. https://products.mhra.gov.uk/. Accessed 18/11/2020.

Levobupivacaine Altan 2.5 mg/mL Solution for Injection/Infusion (Altan Pharma Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 03/12/2020.

Levobupivacaine Altan 7.5 mg/mL Solution for Injection/Infusion (Altan Pharma Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 03/12/2020.

Levobupivacaine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com/. Accessed 18/11/2020.

Disclaimer: This information is independently developed by MIMS based on Levobupivacaine 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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
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