Drugs List

Therapeutic Indications

Uses

Anaesthesia - spinal
Epidural/perineural block in surgical anaesthesia
Local anaesthetic for central nerve block (caudal or epidural)
Local anaesthetic for infiltration anaesthesia
Local anaesthetic for lumbar epidural block to relieve pain during labour
Local anaesthetic for nerve block peripheral

Dosage

Due to the complexity and specialist nature of using anaesthesia, specific dosing information on this agent is not included. When using this agent, specialist literature, national guidelines and Trust policies should be consulted to ensure appropriate dosage and assessment of all relevant patient factors.

Administration

For local, perineural, epidural, lumbar and caudal injection.

In incremental doses, the dose of bupivacaine should be injected slowly (25 to 50 mg/minute), while closely observing the patient's vital functions and maintaining verbal contact.

Contraindications

Children under 1 year
Hypovolaemic shock
Meningitis
Cardiogenic shock
Central nervous system disorder
Central nervous system neoplasm
Coagulopathy
Expanding cerebral lesion
Intracranial haemorrhage
Poliomyelitis
Subacute combined degeneration of spinal cord due to B12 deficiency
Tuberculosis of spine

Precautions and Warnings

Administration site infection
Children aged 1 to 12 years
Debilitation
Elderly
Obesity
Restricted sodium intake
Septicaemia
Cardiac conduction defects
Cardiovascular disorder
Decompensated cardiac failure
Dehydration
Epileptic disorder
Hypotension
Hypovolaemia
Myasthenia gravis
Obstetric paracervical anaesthesia
Pleural disorder
Pregnancy
Respiratory impairment
Severe hepatic impairment
Severe renal impairment

Septicaemia increases risk of post-op intraspinal abscess formation
Sodium content of formulation may be significant
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Aspirate prior to injection to avoid intravascular administration
Discard any unused portion
Discontinue immediately if toxic symptoms occur, especially in epidural use
Do not inject near site of skin infection
Resuscitation facilities must be immediately available
Monitor vital signs, respiration & cardiac function
May cause anaphylactic / anaphylactoid reactions
Discontinue if hepatic function deteriorates
In obese patients dosing should be based on ideal weight

Repeated doses may cause significant increases in blood levels with each dose due to the slow accumulation of bupivacaine. When prolonged blocks are used by repeated bolus injection, the risks of reaching toxic plasma concentrations or causing local neural injury must be considered.

Bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems if used for procedures that result in high plasma concentrations of the drug.

Bupivacaine should be used with caution when used for epidural anaesthesia in patients with impaired cardiovascular function. This is because they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by bupivacaine.

Epidural anaesthesia can lead to hypotension and bradycardia. Precautions against these effects should be taken and may include pre-loading the circulation with crystalloid or colloid solution. If hypotension occurs, it should be treated appropriately. Marked hypotension should be avoided in patients with cardiac decompensation.
Severe hypotension may result from hypovolaemia due to haemorrhage or dehydration, or from aorto-caval occlusion in patients with massive ascites, large abdominal tumours or late pregnancy.
Patients with hypovolaemia due to any cause can develop sudden and severe hypotension during epidural or spinal anaesthesia. Epidural anaesthesia should therefore be avoided or performed with caution in patients with untreated hypovolaemia or significantly impaired venous return.

Epidural anaesthesia can cause intercostal paralysis. This can lead to hypoxia in patients with pleural effusions.

Septicaemia can increase the risk of postoperative intraspinal abscess formation.

There have been reports of respiratory arrest following retrobulbar blocks. Necessary equipment, drugs and personnel should be immediately available prior to retrobulbar block.
Retrobulbar injections may rarely reach the cranial subarachnoid space and cause serious reactions such as temporary blindness, cardiovascular collapse, apnoea or convulsions.
Retro- and peribulbar injections carry a low risk of persistent ocular muscle impairment due to trauma and/or local effects on the muscles/nerves. The severity of these reactions depend on the degree of trauma, the concentration of the anaesthetic and the duration of exposure of the tissue to the anaesthetic.

Caution is advised when bupivacaine is administered as intra-articular injection where recent major intra-articular trauma is suspected or extensive raw surfaces within the joint have been created by the surgical procedure, as that may accelerate absorption and result in higher plasma concentrations.

Hepatic dysfunction including transient increases in alanine aminotransferase, alkaline phosphates and bilirubin have been reported with repeated injections or long-term infusions of bupivacaine. Discontinue treatment with bupivacaine if signs of hepatic dysfunction occur.

Pregnancy and Lactation

Pregnancy

Use bupivacaine with caution in pregnancy.

Bupivacaine should not be administered in early pregnancy unless the benefits outweigh the risks.

Bupivacaine readily crosses the placenta and equilibrium with regard to the unbound concentration is rapidly reached. The degree of plasma protein binding in the foetus is less than in the mother, which results in lower total plasma concentrations in the foetus.

There is no evidence of untoward effects in human pregnancy.

Paracervical nerve block may cause foetal bradycardia. Labour may be prolonged so that Caesarean section is required.

Decreased pup survival in rats and an embryological effect in rabbits has been observed when large doses were administered.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Bupivacaine is considered safe for use in breastfeeding.

Bupivacaine enters human breast milk, but the quantities are so small that there is no risk to the child at therapeutic dose levels.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Allergic reaction
Anaphylactic shock
Apnoea
Arachnoiditis
Bradycardia
Cardiac arrest
Cardiovascular effects
CNS effects
Convulsions
Diplopia
Dizziness
Drug-induced liver injury
Dysarthria
Hepatic impairment
Hyperacusis
Hypercapnia
Hypertension
Hypotension
Hypoxia
Increase in alkaline phosphatase
Increase in serum ALT/AST
Light-headedness
Localised areas of anaesthesia
Localised areas of paraesthesia
Loss of sphincter control
Muscle twitch
Muscle weakness
Nausea
Neurological damage
Neuropathy
Paraplegia
Paresis
Peripheral neuropathy
Respiratory depression
Serum bilirubin increased
Systemic toxicity (if accidental intravascular injection)
Tinnitus
Tongue numbness
Tremor
Unconsciousness
Urinary retention
Ventricular arrhythmias
Ventricular fibrillation
Visual disturbances
Vomiting

Presentation

Injection containing bupivacaine hydrochloride

Drugs List

Therapeutic Indications

Uses

Anaesthesia - spinal
Epidural/perineural block in surgical anaesthesia
Local anaesthetic for central nerve block (caudal or epidural)
Local anaesthetic for infiltration anaesthesia
Local anaesthetic for lumbar epidural block to relieve pain during labour
Local anaesthetic for nerve block peripheral

Dosage

Due to the complexity and specialist nature of using anaesthesia, specific dosing information on this agent is not included. When using this agent, specialist literature, national guidelines and Trust policies should be consulted to ensure appropriate dosage and assessment of all relevant patient factors.

Administration

For local, perineural, epidural, lumbar and caudal injection.

In incremental doses, the dose of bupivacaine should be injected slowly (25 to 50 mg/minute), while closely observing the patient's vital functions and maintaining verbal contact.

Contraindications

Children under 1 year
Hypovolaemic shock
Meningitis
Cardiogenic shock
Central nervous system disorder
Central nervous system neoplasm
Coagulopathy
Expanding cerebral lesion
Intracranial haemorrhage
Poliomyelitis
Subacute combined degeneration of spinal cord due to B12 deficiency
Tuberculosis of spine

Precautions and Warnings

Administration site infection
Children aged 1 to 12 years
Debilitation
Elderly
Obesity
Restricted sodium intake
Septicaemia
Cardiac conduction defects
Cardiovascular disorder
Decompensated cardiac failure
Dehydration
Epileptic disorder
Hypotension
Hypovolaemia
Myasthenia gravis
Obstetric paracervical anaesthesia
Pleural disorder
Pregnancy
Respiratory impairment
Severe hepatic impairment
Severe renal impairment

Septicaemia increases risk of post-op intraspinal abscess formation
Sodium content of formulation may be significant
Advise ability to drive/operate machinery may be affected by side effects
Treatment to be initiated and supervised by a specialist
Aspirate prior to injection to avoid intravascular administration
Discard any unused portion
Discontinue immediately if toxic symptoms occur, especially in epidural use
Do not inject near site of skin infection
Resuscitation facilities must be immediately available
Monitor vital signs, respiration & cardiac function
May cause anaphylactic / anaphylactoid reactions
Discontinue if hepatic function deteriorates
In obese patients dosing should be based on ideal weight

Repeated doses may cause significant increases in blood levels with each dose due to the slow accumulation of bupivacaine. When prolonged blocks are used by repeated bolus injection, the risks of reaching toxic plasma concentrations or causing local neural injury must be considered.

Bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems if used for procedures that result in high plasma concentrations of the drug.

Bupivacaine should be used with caution when used for epidural anaesthesia in patients with impaired cardiovascular function. This is because they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by bupivacaine.

Epidural anaesthesia can lead to hypotension and bradycardia. Precautions against these effects should be taken and may include pre-loading the circulation with crystalloid or colloid solution. If hypotension occurs, it should be treated appropriately. Marked hypotension should be avoided in patients with cardiac decompensation.
Severe hypotension may result from hypovolaemia due to haemorrhage or dehydration, or from aorto-caval occlusion in patients with massive ascites, large abdominal tumours or late pregnancy.
Patients with hypovolaemia due to any cause can develop sudden and severe hypotension during epidural or spinal anaesthesia. Epidural anaesthesia should therefore be avoided or performed with caution in patients with untreated hypovolaemia or significantly impaired venous return.

Epidural anaesthesia can cause intercostal paralysis. This can lead to hypoxia in patients with pleural effusions.

Septicaemia can increase the risk of postoperative intraspinal abscess formation.

There have been reports of respiratory arrest following retrobulbar blocks. Necessary equipment, drugs and personnel should be immediately available prior to retrobulbar block.
Retrobulbar injections may rarely reach the cranial subarachnoid space and cause serious reactions such as temporary blindness, cardiovascular collapse, apnoea or convulsions.
Retro- and peribulbar injections carry a low risk of persistent ocular muscle impairment due to trauma and/or local effects on the muscles/nerves. The severity of these reactions depend on the degree of trauma, the concentration of the anaesthetic and the duration of exposure of the tissue to the anaesthetic.

Caution is advised when bupivacaine is administered as intra-articular injection where recent major intra-articular trauma is suspected or extensive raw surfaces within the joint have been created by the surgical procedure, as that may accelerate absorption and result in higher plasma concentrations.

Hepatic dysfunction including transient increases in alanine aminotransferase, alkaline phosphates and bilirubin have been reported with repeated injections or long-term infusions of bupivacaine. Discontinue treatment with bupivacaine if signs of hepatic dysfunction occur.

Pregnancy and Lactation

Pregnancy

Use bupivacaine with caution in pregnancy.

Bupivacaine should not be administered in early pregnancy unless the benefits outweigh the risks.

Bupivacaine readily crosses the placenta and equilibrium with regard to the unbound concentration is rapidly reached. The degree of plasma protein binding in the foetus is less than in the mother, which results in lower total plasma concentrations in the foetus.

There is no evidence of untoward effects in human pregnancy.

Paracervical nerve block may cause foetal bradycardia. Labour may be prolonged so that Caesarean section is required.

Decreased pup survival in rats and an embryological effect in rabbits has been observed when large doses were administered.

The use of all medication in pregnancy should be avoided whenever possible; particularly in the first trimester. Non-drug treatments should also be considered. When essential, a medication with the best safety record over time should be chosen, employing the lowest effective dose for the shortest possible time. Polypharmacy should be avoided. Teratogens taken in the pre-embryonic period, often quoted as lasting until 14 to 17 days post-conception, are believed to have an all-or-nothing effect. Where drugs have a short half-life, and when the date of conception is certain, this may allow women to be reassured where drug exposure has occurred within this time frame. Further advice may be available from the UK National Teratology Information Service (NTIS) and through ToxBase, available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Lactation

Bupivacaine is considered safe for use in breastfeeding.

Bupivacaine enters human breast milk, but the quantities are so small that there is no risk to the child at therapeutic dose levels.

Neonates, infants born prematurely, those with low birth weight, those with an unstable gastrointestinal function or who have serious illnesses may require special consideration. For any infant, if a drug is prescribed to the nursing mother, it should be at the lowest practical dose and for the shortest time. When drug administration is unavoidable and breastfeeding is to continue, minimisation of exposure of the infant to the drug may sometimes be achieved by timing the maternal doses to just after a feeding episode. Infants exposed to drugs via breast milk should be monitored for unusual signs or symptoms. Interactions between the drug received by the infant from the mother's milk and medication prescribed for the infant should also be considered, for example, when the drug given to the infant may prevent metabolism of the drug received via breast milk.
Specialist advice is available from the UK Drugs in Lactation Advisory Service at https://www.midlandsmedicines.nhs.uk/content.asp?section=6&subsection=17&pageIdx=1

Side Effects

Allergic reaction
Anaphylactic shock
Apnoea
Arachnoiditis
Bradycardia
Cardiac arrest
Cardiovascular effects
CNS effects
Convulsions
Diplopia
Dizziness
Drug-induced liver injury
Dysarthria
Hepatic impairment
Hyperacusis
Hypercapnia
Hypertension
Hypotension
Hypoxia
Increase in alkaline phosphatase
Increase in serum ALT/AST
Light-headedness
Localised areas of anaesthesia
Localised areas of paraesthesia
Loss of sphincter control
Muscle twitch
Muscle weakness
Nausea
Neurological damage
Neuropathy
Paraplegia
Paresis
Peripheral neuropathy
Respiratory depression
Serum bilirubin increased
Systemic toxicity (if accidental intravascular injection)
Tinnitus
Tongue numbness
Tremor
Unconsciousness
Urinary retention
Ventricular arrhythmias
Ventricular fibrillation
Visual disturbances
Vomiting

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

The following number will direct the caller to the relevant local centre (0844) 892 0111

Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: October 2015

Reference Sources

Joint Formulary Committee. British National Formulary (online) London: BMJ Group and Pharmaceutical Press Accessed on 22 October 2015.

Paediatric Formulary Committee. BNF for Children (online) London: BMJ Group, Pharmaceutical Press, and RCPCH Publications Accessed on 22 October 2015.

Summary of Product Characteristics: Bupivacaine 0.5%w/v solution for injection. Accord Healthcare Limited. Revised October 2014.

Summary of Product Characteristics: Bupivacaine Hydrochloride 0.25%w/v solution for injection. Amdipharm Mercury Company Limited. Revised February 2014.
Summary of Product Characteristics: Bupivacaine Hydrochloride 0.5%w/v solution for injection (plastic ampoules). Amdipharm Mercury Company Limited. Revised February 2014.
Summary of Product Characteristics: Bupivacaine Hydrochloride 0.5%w/v solution for injection (glass ampoules). Amdipharm Mercury Company Limited. Revised February 2014.

Summary of Product Characteristics: Marcain Polyamp Steripack 0.25% and 0.5%. Aspen. Revised April 2021.