Drugs List

Therapeutic Indications

Uses

Anaesthesia - spinal

Dosage

Due to the complexity and specialist nature of dosage regimens for anaesthetics, specific dosing information on this agent is not included.

The duration of action for prilocaine 2% injection is dose dependant.

Administration

For intrathecal injection only, into the intervertebral space L2/L3, L3/L4 and L4/L5.

Contraindications

Children under 18 years
Hypovolaemic shock
Cardiogenic shock
Coagulopathy
Decompensated cardiac failure
Methaemoglobinaemia
Severe anaemia
Severe cardiac conduction defects

Precautions and Warnings

Debilitation
Elderly
Arteriosclerosis
Atrioventricular block
Breastfeeding
Diabetic autonomic neuropathy
Glucose-galactose malabsorption syndrome
Hemiplegia
Hepatic impairment
Multiple sclerosis
Neuromuscular disorder
Obstetric paracervical anaesthesia
Occlusive peripheral vascular disorder
Paraplegia
Porphyria
Pregnancy
Renal impairment

Reduce dose in patients with hepatic impairment
Reduce dose in patients with renal impairment
Advise ability to drive/operate machinery may be affected by side effects
Advise patient not to drive or operate machinery until assessed
Treatment to be initiated and supervised by a specialist
Contains glucose
Administer injection slowly
Aspirate prior to injection to avoid intravascular administration
Avoid local anaesthetics if inflammation in region of proposed injection
Do not inject near site of skin infection
Resuscitation facilities must be immediately available
Treatment to be administered by or under supervision of specialist
Monitor closely patient with previous or current arrhythmic disorder
Monitor vital signs, respiration & cardiac function
Discontinue immediately on the first signs of toxicity
In obese patients dosing should be based on ideal weight
Reduce dose in elderly
Breastfeeding: Do not breastfeed & discard milk for 24 hours after therapy

In high risk patients, the general condition of the patient should be improved prior to administration.

The manufacturer advises reducing the dose in patients with established concomitant disorders (e.g. vascular occlusion, arteriosclerosis, diabetic polyneuropathy), in debilitated patients or in late pregnancy.

High or total spinal block, with consequent cardiovascular and respiratory depression, can rarely be experienced with prilocaine. Severe hypotension and bradycardia may also be induced by prolonged block of the sympathetic nervous system, even to the point of cardiac arrest. A drop in arterial pressure and cardiac frequency may also occur. Elderly patients and patients in the final period of pregnancy are more at risk.

Neurological damage may rarely be seen after spinal anaesthesia, marked by paraesthesia, loss of sensitivity, motor weakness and paralysis. There is no evidence that spinal anaesthesia is negatively influenced by neurological disorders such as multiple sclerosis, hemiplegia, paraplegia or neuromuscular disorders, but appropriate care should be taken when administering prilocaine to these patients, with thorough consideration of the benefits and risks of prilocaine administration.

Pregnancy and Lactation

Pregnancy

Use prilocaine with caution in pregnancy.

Prilocaine is contraindicated for paracervical block or pudendal block.

There is no published information on the use of prilocaine in pregnant women. The manufacturer states that prilocaine should only be given in pregnancy if the expected benefits clearly outweigh the potential risks, and a dose reduction should be considered in late pregnancy.

Prilocaine is known to cross the placenta.

Animal studies have shown reproductive toxicity.

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

Use prilocaine with caution in breastfeeding.

It is not known if prilocaine is present in human breast milk. The effect on the nursing infant is also unknown. The manufacturer states that if administration is clinically necessary, breastfeeding can be resumed approximately 24 hours after use of prilocaine 2% injection.

LactMed suggests that alternative anaesthetics may be preferable when breastfeeding.

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 reaction
Arachnoiditis
Arrhythmias
Asystole
Blurred vision
Bradycardia
Cardiac arrest
Cardiovascular depression
Cardiovascular disturbances
Cardiovascular toxicity
Cerebrovascular disorders
Changes in pulse
Circumoral paraesthesia
CNS effects
CNS toxicity
Coma
Convulsions
Cramp
Cyanosis
Dazed feeling
Depression
Diplopia
Disorientation
Dizziness
Drowsiness
Excitation
Feeling hot
Headache
Hearing disturbances
Hypertension
Hypotension
Light-headedness
Meningitis
Methaemoglobinaemia
Motor disturbances
Mouth numbness
Muscle contraction
Muscle twitch
Mydriasis
Myocardial depression
Nausea
Nervousness
Neuropathy
Paraesthesia
Paralysis
Peripheral vasodilatation
Respiratory arrest
Respiratory depression
Respiratory failure
Restlessness
Sedation
Sensation of cold
Shaking
Speech disturbances
Spinal Haematoma
Tinnitus
Tongue numbness
Tremor
Unconsciousness
Urinary retention
Visual disturbances
Vomiting

Presentation

Parenteral formulations of prilocaine 2%, used for intrathecal injection.

Drugs List

Therapeutic Indications

Uses

Anaesthesia - spinal

Dosage

Due to the complexity and specialist nature of dosage regimens for anaesthetics, specific dosing information on this agent is not included.

The duration of action for prilocaine 2% injection is dose dependant.

Administration

For intrathecal injection only, into the intervertebral space L2/L3, L3/L4 and L4/L5.

Contraindications

Children under 18 years
Hypovolaemic shock
Cardiogenic shock
Coagulopathy
Decompensated cardiac failure
Methaemoglobinaemia
Severe anaemia
Severe cardiac conduction defects

Precautions and Warnings

Debilitation
Elderly
Arteriosclerosis
Atrioventricular block
Breastfeeding
Diabetic autonomic neuropathy
Glucose-galactose malabsorption syndrome
Hemiplegia
Hepatic impairment
Multiple sclerosis
Neuromuscular disorder
Obstetric paracervical anaesthesia
Occlusive peripheral vascular disorder
Paraplegia
Porphyria
Pregnancy
Renal impairment

Reduce dose in patients with hepatic impairment
Reduce dose in patients with renal impairment
Advise ability to drive/operate machinery may be affected by side effects
Advise patient not to drive or operate machinery until assessed
Treatment to be initiated and supervised by a specialist
Contains glucose
Administer injection slowly
Aspirate prior to injection to avoid intravascular administration
Avoid local anaesthetics if inflammation in region of proposed injection
Do not inject near site of skin infection
Resuscitation facilities must be immediately available
Treatment to be administered by or under supervision of specialist
Monitor closely patient with previous or current arrhythmic disorder
Monitor vital signs, respiration & cardiac function
Discontinue immediately on the first signs of toxicity
In obese patients dosing should be based on ideal weight
Reduce dose in elderly
Breastfeeding: Do not breastfeed & discard milk for 24 hours after therapy

In high risk patients, the general condition of the patient should be improved prior to administration.

The manufacturer advises reducing the dose in patients with established concomitant disorders (e.g. vascular occlusion, arteriosclerosis, diabetic polyneuropathy), in debilitated patients or in late pregnancy.

High or total spinal block, with consequent cardiovascular and respiratory depression, can rarely be experienced with prilocaine. Severe hypotension and bradycardia may also be induced by prolonged block of the sympathetic nervous system, even to the point of cardiac arrest. A drop in arterial pressure and cardiac frequency may also occur. Elderly patients and patients in the final period of pregnancy are more at risk.

Neurological damage may rarely be seen after spinal anaesthesia, marked by paraesthesia, loss of sensitivity, motor weakness and paralysis. There is no evidence that spinal anaesthesia is negatively influenced by neurological disorders such as multiple sclerosis, hemiplegia, paraplegia or neuromuscular disorders, but appropriate care should be taken when administering prilocaine to these patients, with thorough consideration of the benefits and risks of prilocaine administration.

Pregnancy and Lactation

Pregnancy

Use prilocaine with caution in pregnancy.

Prilocaine is contraindicated for paracervical block or pudendal block.

There is no published information on the use of prilocaine in pregnant women. The manufacturer states that prilocaine should only be given in pregnancy if the expected benefits clearly outweigh the potential risks, and a dose reduction should be considered in late pregnancy.

Prilocaine is known to cross the placenta.

Animal studies have shown reproductive toxicity.

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

Use prilocaine with caution in breastfeeding.

It is not known if prilocaine is present in human breast milk. The effect on the nursing infant is also unknown. The manufacturer states that if administration is clinically necessary, breastfeeding can be resumed approximately 24 hours after use of prilocaine 2% injection.

LactMed suggests that alternative anaesthetics may be preferable when breastfeeding.

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 reaction
Arachnoiditis
Arrhythmias
Asystole
Blurred vision
Bradycardia
Cardiac arrest
Cardiovascular depression
Cardiovascular disturbances
Cardiovascular toxicity
Cerebrovascular disorders
Changes in pulse
Circumoral paraesthesia
CNS effects
CNS toxicity
Coma
Convulsions
Cramp
Cyanosis
Dazed feeling
Depression
Diplopia
Disorientation
Dizziness
Drowsiness
Excitation
Feeling hot
Headache
Hearing disturbances
Hypertension
Hypotension
Light-headedness
Meningitis
Methaemoglobinaemia
Motor disturbances
Mouth numbness
Muscle contraction
Muscle twitch
Mydriasis
Myocardial depression
Nausea
Nervousness
Neuropathy
Paraesthesia
Paralysis
Peripheral vasodilatation
Respiratory arrest
Respiratory depression
Respiratory failure
Restlessness
Sedation
Sensation of cold
Shaking
Speech disturbances
Spinal Haematoma
Tinnitus
Tongue numbness
Tremor
Unconsciousness
Urinary retention
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: May 2018

Reference Sources

Drugs During Pregnancy and Lactation: Treatment Options and Risk Assessment, 3rd edition (2015) ed. Schaefer, C., Peters, P. and Miller, R. Elsevier, London.

NICE Evidence Services Available at: www.nice.org.uk Last accessed: 09 May 2018

Summary of Product Characteristics: Prilotekal 20mg/ml solution for injection. Sintetica Limited. Revised February 2017.

US National Library of Medicine. Toxicology Data Network. Drugs and Lactation Database (LactMed).
Available at: https://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT
Prilocaine Last revised: 08 September 2013
Last accessed: 10 May 2018