Levobupivacaine

Registered South African indications:

• Surgical anaesthesia
• Pain management 

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• Known hypersensitivity to any local anaesthetic agent of the amide type
• Intravenous regional anaesthesia (Bier’s Block)
• Severe renal impairment
• Severe hepatic impairment
• Solutions of levobupivacaine should not be used for the production of obstetrical paracervical block anaesthesia. There are no data to support such use and there is additional risk of foetal bradycardia and death
• Concomitant use with known CYP3A4 inducers (eg. phenytoin, phenobarbital, rifampin)
• Concomitant use with known CYP3A4 inhibitors (azole antimycotics, eg. ketoconazole)

Cautions

• Pregnancy
• Mild to moderate renal impairment 
• Mild to moderate hepatic impairment 
• Elderly
• Debiliated patients 
• Impaired cardiovascular function
• Pre-existing central nervous system disease
• High doses
• Infusion > 24 hours
• Blocks in the head and neck 
• Retrobulbar block
• Acutely ill patients
• Low sodium diet 

Forms avail. in SA and covered in this monograph: inj

Major block
- Epidural block for surgery

• Intrathecal: 50-150mg, bolus given as a slow injection over 5min; Max dose: 400mg/24hrs

- Epidural for caesarean section

• Intrathecal: 75-150mg, bolus given as a slow injection over 15-20min

- Intrathecal block

• Intrathecal: 15mg, bolus given as a slow injection

- Peripheral nerve block 

• Local infiltration (inj): 2.5-150mg, bolus given as a slow injection

Minor block
- Local infiltration

• Local infiltration (inj): 2.5-150mg, bolus given as a slow injection

- Peribulbar block in ophthalmic surgery

• Local infiltration (inj): 37.5-112.5mg

- Dental procedures 

• Local infiltration (inj): 25-75mg

Pain management
- Epidural for labour analgesia 

• Intrathecal: 15-50mg, bolus given as a slow injection
  OR
• Intrathecal: 5-12.5mg/hr, as an infusion; Max dose: 400mg/24hrs

- Post-operative pain

• Intrathecal: 12.5-18.75mg/hr, as an infusion; Max dose: 400mg/24hrs

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Careful aspiration before and during injection is recommended to prevent inadvertant  intravascular injection

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When a large dose is to be injected, a test dose of 3-5ml lignocaine with adrenaline is recommended

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The minimum recommended interval between intermittent injections is 15min

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Bolus doses should be administered at a rate of 7.5–30mg/min

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Dilutions of levobupivacaine should be made with 0.9% sodium chloride solution

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Clonidine, morphine and fentanyl have been shown to be compatible with levobupivacaine in 0.9% sodium chloride

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In cases where levobupivacaine is combined with other agents the dose should be reduced and use of a lower concentration is preferable

Paed. forms avail. in SA and covered in this monograph: inj

Pain management
- Ilioinguinal block
- Iliohypogastric block

Younger than 6 months 

• Not established for use 

Between 6 months-12 years

• IV: 1.25mg/kg/side

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Careful aspiration before and during injection is recommended to prevent inadvertant  intravascular injection

---

When a large dose is to be injected, a test dose of 3-5ml lignocaine with adrenaline is recommended

---

The minimum recommended interval between intermittent injections is 15min

---

Bolus doses should be administered at a rate of 7.5–30mg/min

---

Dilutions of levobupivacaine should be made with 0.9% sodium chloride solution

---

Clonidine, morphine and fentanyl have been shown to be compatible with levobupivacaine in 0.9% sodium chloride

---

In cases where levobupivacaine is combined with other agents the dose should be reduced and use of a lower concentration is preferable

Pregnancy

• FDA Pregnancy Category Not Rated (NR) 

Breastfeeding 

• Compatible

Renal Impairment 

• Mild to moderate: Caution; no information available
  There are no data in patients with renal impairment
• Severe: Contraindicated

Hepatic Impairment 

• Mild to moderate: Caution; no information available
  There are no data in patients with hepatic impairment
• Severe: Contraindicated

Elderly 

• Caution; dose adjustment recommended  

Central Nervous System Disorders

• Dizziness
• Headache
• Seizures 
• Loss of consciousness
• Somnolence
• Syncope
• Paraesthesia
• Paraplegia
• Paralysis

Cardiovascular Disorders

• Atrioventricular block
• Cardiac arrest
• Ventricular tachyarrhythmia
• Tachycardia
• Bradycardia
• Hypotension
• Change in electrocardiogram 
• Flushing
• Hypoaesthesia
• Decreased cardiac output

Respiratory Disorders

• Respiratory arrest
• Laryngeal oedema
• Apnoea
• Sneezing

Gastrointestinal Disorders

• Nausea and vomiting
• Oral hypoaesthesia 
• Loss of sphincter control

Genitourinary Disorders

• Bladder dysfunction
• Priapism

Musculoskeletal Disorders

• Back pain
• Muscle twitching
• Muscular weakness

Skin and Subcutaneous Tissue Disorders

• Angioedema
• Urticaria
• Pruritus
• Hyperhidrosis
• Anhidrosis
• Erythema

Immune, Blood and Lymphatic System Disorders

• Allergic reactions 
• Hypersensitivity
• Fever
• Anaemia

Sensory Disorders

• Vision blurred
• Ptosis
• Miosis
• Enophthalmos

Others 

• Foetal distress syndrome

• CYP3A4 inducers
• Phenytoin
• Phenobarbital
• Rifampin
• CYP3A4 inhibitors
• Azole antimycotics
• Ketoconazole
• CYP1A2 inhibitors
• Anti-arrhythmics with local anaesthetic activity
• Anti-arrhythmic agents (Class III)
• Adrenaline 

None routine

Levobupivacaine blocks the generation and the conduction of nerve impulses, by increasing the threshold for electrical excitation in the nerve. It binds to the intracellular portion of sodium channels and blocks sodium influx into nerve cells, which prevents depolarization.

Injection (per ml) 5mg

• Chirocane (AbbVie) originator

Injection (per ml) 7.5mg

• Chirocane (AbbVie) originator