Bupivacaine

Registered South African indications:

• Spinal anaesthesia
• Regional nerve blocks

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Intravenous regional anaesthesia (Bier's block)

Cautions

• Pregnancy
• Breastfeeding
• Renal impairment
• Hepatic impairment
• Elderly
• Hypovolaemia
• Impaired cardiovascular function
• Partial or complete heart block
• Paracervical blocks
• Retrobulbar blocks
• Dental blocks
• Stellate ganglion blocks
• Massive ascites
• Large abdominal tumours
• Pleural effusion
• Intra-articular injection
• Low salt diet
• Children

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

Spinal anaesthesia

General dosage range 

• Intrathecal: 2-3mg/kg; Max: 300mg/4 hours or 400mg/24hrs

Regional nerve blocks

General dosage range 

• Local infiltration: 2-3mg/kg; Max: 300mg/4 hours or 400mg/24hrs

See additional prescribing points

For field blocks and neuraxial anaesthesia 0.5% (5mg/ml) solution is adequate

For nerve blocks and epidural infusions, 0.125-0.25% solution can be used. 

Unless performed with direct ultrasound guidance, a larger volume at a lower concentration is advised, rather than a higher concentration but smaller volume for nerve blocks

Dosage depends on the site to be anaesthetised, the area and vascularity thereof, condition of patient, duration of anaesthesia required and the technique used

Only preservative-free medications may be used for nerve blocks

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

Spinal anaesthesia
Regional nerve blocks

• Max dose: 0.5% sol. 0.4ml/kg (2mg/kg)

Only for use in subspecialist paediatric anaesthesia

See additional prescribing points

Only preservative-free medications may be used for nerve blocks

Pregnancy

• Caution
• There is no evidence of untoward effects in human pregnancy. In large doses, there is evidence of decreased pup survival in rats and an embryological effect in rabbits if bupivacaine is administered in pregnancy. Bupivacaine should not, therefore, be given in early pregnancy unless the benefits are considered to outweigh the risks. It should be noted that the dose should be reduced in patients in the late stages of pregnancy

Breastfeeding

• Caution
• Bupivacaine enters the mother's milk, but in such small quantities that there is generally no risk of affecting the child at therapeutic dose levels

Renal Impairment

• Caution: no dose adjustment recommended

Hepatic Impairment

• Caution: no dose adjustment recommended

Elderly

• Caution; no dose adjustment recommended
  Use with caution in the elderly; dose reduction may be required

Porphyria Information

• Not porphyrinogenic (NP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Paraesthesia
• Dizziness
• Convulsions
• Cicumoral paraesthesia
• Numbness of the tongue
• Hyperacusis
• Visual disturbances
• Loss of consciousness
• Tremor
• Neuropathy
• Peripheral nerve injury
• Arachnoiditis
• Paresis
• Paraplegia

Cardiovascular Disorders

• Bradycardia
• Cardiac arrest
• Hypotension
• Hypertension

Respiratory Disorders

• Respiratory depression

Gastrointestinal Disorders

• Nausea and vomiting 

Genitourinary Disorders

• Urinary retention

Musculoskeletal Disorders

• Dysarthria
• Muscle twitching

Immune, Blood and Lymphatic System Disorders

• Allergic reactions
• Anaphylaxis

Sensory Disorders

• Tinnitus
• Diplopia
• Hyperacusis
• Visual disturbances

• Antiarrhythmics (Class III) [Amiodarone]
• Anticoagulants
• Mexiletine
• Local anaesthetics

• Vital signs
• Signs of central nervous system toxicity

Specific cases may require

• Cardiac monitoring

• Adequate resuscitation equipment should be available whenever local or general anaesthesia is administered
• The clinician responsible should take the necessary precautions to avoid intravascular injection
• Before any nerve block is attempted, IV access for resuscitation purposes should be established. Clinicians should have received adequate and appropriate training in the procedure to be performed and should be familiar with the diagnosis and treatment of side effects, systemic toxicity or other complications
• Major peripheral nerve blocks may require the administration of a large volume of local anaesthetic in areas of high vascularity, often close to large vessels where there is an increased risk of intravascular injection and/ or systemic absorption. This may lead to high plasma concentrations

Effects on the ability to drive and use machines

• In general, it is sufficient to allow 2 - 4 hours post nerve block or until full functions have returned following regional nerve block. In many situations, patients receive a sedative or other C.N.S. depressant drug e.g. diazepam, midazolam to allow the block to be performed. One must allow adequate time for the effects of these drugs to clear
• Depending on dosage, local anaesthetics may have a very mild effect on mental function and co-ordination even in the absence of overt CNS toxicity and may temporarily impair locomotion and alertness

Bupivacaine is a long acting local anaesthetic with both anaesthetic and analgesic effects. At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block with less pronounced motor block. It causes reversible blockade of impulse propagation along nerve fibres by binding to sodium channels and preventing the inward movement of sodium ions through the cell membrane of the nerve fibres.

Injection (per ml) 5mg

• Macaine HCL 0.5% (Adcock)
• Macaine HCL 0.5% Spinal Injection (Adcock)
• Micro Bupivacaine (Micro)
• Pharma-Q Bupivacaine (Pharma-Q)