Prilocaine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : Parenteral Epidural anaesthesia Lumbar epidural: 300 mg (as 1% solution) or 300-500 mg (as 2% solution); Thoracic epidural: 100-300 mg (as 1% solution) or 200-300 mg (as 2% solution). Caudal epidural: 200-300 mg (as 1% solution) or 300-500 mg (as 2% solution). Local anaesthesia Local infiltration: ≤500 mg (as 0.5 or 1% solution). Dental infiltration: 40-80 mg (as 4% solution). Max: <70 kg: 8 mg/kg; ≥70 kg: 600mg. Peripheral nerve block Brachial plexus block: 300-500 mg (as 1% solution). Sciatic block: 300-400 mg (as 2% solution). Femoral, obturator and lateral cutaneous block: 300-400 mg (as 1% solution). Digital block: 10-50 mg (as 1% solution). Intercostal nerve block: 20-50 mg (as 1% solution). Paravertebral: 30-50 mg (as 1% solution). Retrobulbar: 80 mg (as 2% solution). Peribulbar: 100-150 mg (as 1% solution). Dental block: 40-80 mg (as 4% solution). Max: <70 kg: 8 mg/kg; ≥70 kg: 600mg. Intravenous As an intravenous regional anaesthesia As 0.5% solution: 200-300 mg. Intrathecal Spinal Anaesthesia For short term surgical procedures: 40-60 mg (as a 2% solution). Max: 80 mg.
Dosage Details
Intrathecal
Spinal anaesthesia
Adult: For short term surgical procedures: 40-60 mg (as a 2% solution). Max: 80 mg.

Intravenous
Intravenous regional anaesthesia
Adult: As 0.5% solution: 200-300 mg.
Elderly: Dosage reduction may be necessary.

Parenteral
Epidural anaesthesia
Adult: Lumbar epidural: 300 mg (as 1% solution) or 300-500 mg (as 2% solution); Thoracic epidural: 100-300 mg (as 1% solution) or 200-300 mg (as 2% solution). Caudal epidural: 200-300 mg (as 1% solution) or 300-500 mg (as 2% solution).
Child: >6 months Caudal epidural: 5 mg/kg (as 1% solution).
Elderly: Dosage reduction may be necessary.

Parenteral
Local anaesthesia
Adult: Local infiltration: ≤500 mg (as 0.5 or 1% solution). Dental infiltration: 40-80 mg (as 4% solution). Max: <70 kg: 8 mg/kg; ≥70 kg: 600mg.
Elderly: Dosage reduction may be necessary.

Parenteral
Peripheral nerve block
Adult: Brachial plexus block: 300-500 mg (as 1% solution). Sciatic block: 300-400 mg (as 2% solution). Femoral, obturator and lateral cutaneous block: 300-400 mg (as 1% solution). Digital block: 10-50 mg (as 1% solution). Intercostal nerve block: 20-50 mg (as 1% solution). Paravertebral: 30-50 mg (as 1% solution). Retrobulbar: 80 mg (as 2% solution). Peribulbar: 100-150 mg (as 1% solution). Dental block: 40-80 mg (as 4% solution). Max: <70 kg: 8 mg/kg; ≥70 kg: 600mg.
Elderly: Dosage reduction may be necessary.
Renal Impairment
Intrathecal
Dosage reduction may be necessary.
Hepatic Impairment
Intrathecal
Dosage reduction may be necessary.
Incompatibility
May cause precipitation with alkaline solutions.
Contraindications
Hypersensitivity. Congenital or idiopathic methaemoglobinaemia, serious cardiac conduction problem, severe anaemia, cardiogenic and hypovolemic shock. Sepsis in administration site. Children <6 months (as 2% solution).
Special Precautions
Patient with anaemia, CV disorders (e.g. arteriosclerosis, hypo-/hypertension, bradycardia, cardiac impairment or block), neurological or neuromuscular disorders (e.g. multiple sclerosis, hemiplegia, paraplegia), diabetes mellitus, respiratory impairment, familial malignant hyperthermia, G6PD, porphyria; debilitations. Renal and hepatic impairment. Elderly, children. Pregnancy and lactation. Not intended for paracervical and pudendal blocks in an obstetric patient; post-operative intra-articular continuous infusion.
Adverse Reactions
Significant: Methaemoglobinaemia, cardiovascular reactions (e.g. hypotension, bradycardia), porphyria; temporary blindness, convulsion (with retrobulbar block); ocular muscle dysfunction (with retro-/peri-bulbar blocks); rarely, cardiovascular and respiratory depression.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Blurred vision.
Gastrointestinal disorders: Nausea, vomiting.
Musculoskeletal and connective tissue disorders: Muscle weakness, back pain.
Nervous system disorders: Drowsiness, disorientation, dizziness, paraesthesia.
Vascular disorders: Hypertension.
Potentially Fatal: Rarely, hypersensitivity reactions.
Patient Counseling Information
This drug may impair locomotion and alertness, if affected, do not drive or operate machinery.
Overdosage
Symptoms: CNS toxicity including paraesthesia in the areas of the mouth and tongue, light-headedness, hearing problems (e.g. tinnitus), visual problems, abnormal muscular contractions, unconsciousness, generalised convulsions, hypoxia, hypercapnia; CV toxicity including hypotension, bradycardia, arrhythmia, cardiac arrest; methaemoglobinaemia. Management: Provide respiratory support (e.g. oxygenation, ventilation). Manage generalised convulsions with an anticonvulsant agent; cardiac arrest by cardiopulmonary resuscitation and provision of circulatory support; CV depression (manifested by hypotension, bradycardia) with IV fluids and vasopressor, chronotropic and/or inotropic agents; methaemoglobinaemia with IV 1% methylene blue.
Drug Interactions
Increased cardiac related reactions with antiarrhythmic agents (e.g. amiodarone). Increased risk of methaemoglobinaemia with sulfonamides, antimalarials (e.g. chloroquine), certain nitric compounds (e.g. sodium nitroprussiate).
Action
Description: Prilocaine is an amide type local anaesthetic. It selectively binds to the intracellular surface of Na channels and reversibly inhibits influx of Na along nerve fibres thereby, preventing depolarization and conduction of nerve impulses. As a result, it decreases perception of pain, cold, heat, pressure and touch.
Onset: As 4% solution: Infiltration: <2 minutes. Inferior alveolar nerve block: <3 minutes.
Duration: As 2% solution: Peripheral nerve block: Up to 4 hours. Epidural block: 1.5-2 hours. As 4% solution: Infiltration: Approx 20 minutes. Inferior alveolar nerve block: Approx 2.5 hours.
Pharmacokinetics:
Distribution: Crosses the placenta and the blood-brain barrier; enters breast milk. Apparent volume of distribution: 190-260 L. Plasma protein binding: 40-55% to α1 acid glycoprotein.
Metabolism: Metabolised in the liver and to a lesser extent, in the kidney by amidases via amide hydrolysis into O-toluidine and N-propylalanine; may be further metabolised via ring hydroxylation (e.g. O-toluidine into 2-amino-3-hydroxytoluene and 2-amino-5-hydroxytoluene).
Excretion: Via urine (as O-toluidine metabolite; <5% as unchanged drug). Terminal elimination half-life: 1.6 hours.
Chemical Structure

Chemical Structure Image
Prilocaine

Source: National Center for Biotechnology Information. PubChem Database. Prilocaine, CID=4906, https://pubchem.ncbi.nlm.nih.gov/compound/Prilocaine (accessed on Jan. 23, 2020)

Storage
Store between 20-25°C. Protect from light.
ATC Classification
N01BB04 - prilocaine ; Belongs to the class of amides. Used as local anesthetics.
References
Anon. Prilocaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 19/03/2018.

Buckingham R (ed). Prilocaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/03/2018.

Joint Formulary Committee. Prilocaine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/03/2018.

Pharmacy Retailing (NZ) Limited. Citanest Solution for Injection data sheet 10 November 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 19/03/2018.

Prilocaine Hydrochloride Injection, Solution (Septodont Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 19/03/2018.

Disclaimer: This information is independently developed by MIMS based on Prilocaine 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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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