Adult: Dosage is individualised based on the inj site, procedure and patient status. As 2% solution: 40-60 mg (2-3 mL). Max: 80 mg (4 mL). Use the lowest effective dose. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines). Elderly: Dose reduction may be required.
Parenteral Local anaesthesia
Adult: Dosage is individualised based on the inj site, procedure and patient status. As 1% solution: Max: 400 mg. Use the lowest effective dose. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines). Elderly: Dose reduction may be required.
Parenteral Local dental anaesthesia
Adult: Dosage is individualised based on the inj site, procedure and patient status. Infiltration or nerve block: As 4% solution: Initial: 40-80 mg (1-2 mL). Max dose within a 2-hour period: <70 kg: 8 mg/kg; ≥70 kg: 600 mg (15 mL). Use the lowest effective dose. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines). Elderly: Dose reduction may be required.
Special Patient Group
Acutely ill and debilitated patients: Dose reduction may be required.
Contraindications
Congenital or idiopathic methaemoglobinaemia, severe anaemia; serious cardiac conduction disorders (intrathecal).
Special Precautions
Patient with cardiovascular disease, severe shock, heart block, cardiac conduction disturbances, severe or untreated hypertension; epilepsy; risk factors for methaemoglobinaemia (e.g. G6PD deficiency, cardiac or pulmonay compromise); acute porphyria. Acutely ill and debilitated patients. Avoid intravascular inj, inj into inflamed or infected area. Not approved for postoperative continuous intra-articular infusion. Renal and hepatic impairment. Elderly. Pregnancy and lactation.
This drug may temporarily impair locomotion and alertness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor state of consciousness, CV and respiratory vital signs during and after each administration. Assess for signs and symptoms of methaemoglobinaemia.
Overdosage
Symptoms: Paraesthesia in the mouth, numbness of the tongue, feeling dazed, problems with hearing, tinnitus, visual problems, muscle contractions, convulsions, loss of consciousness, hypoxia, hypercapnia, respiratory arrest, hypotension, bradycardia, arrhythmia, cardiac arrest, methaemoglobinaemia and cyanosis.
Management: Symptomatic and supportive treatment. Ensure appropriate airway or respiratory support, oxygenation, ventilation and circulatory support. Administer anticonvulsants in case of convulsions. Institute cardiopulmonary resuscitation for circulatory arrest. Give IV fluids, vasopressors, chronotropics and/or inotropic agents for cardiovascular depression. Administer 1% methylthioninium chloride (also known as methylene blue) solution via IV inj to treat methaemoglobinaemia.
Drug Interactions
Increased risk of adverse effects with other local or amide-type anaesthetics. Increased risk of methaemoglobinaemia with sulfonamides (e.g. sulfamethoxazole/trimethoprim combination), antimalarials (e.g. primaquine), nitrates/nitrites (e.g. nitroglycerin, nitroprusside, nitric oxide), anticonvulsants (e.g. phenobarbital, phenytoin) or antineoplastic agents (e.g. cyclophosphamide, flutamide, ifosfamide). Increased cardiac effects with class III antiarrhythmic drugs (e.g. amiodarone). Increased risk of severe, persistent hypertension or CVA with vasopressor drugs and ergot-type oxytocic drugs.
Action
Description: Overview: Prilocaine is an intermediate-acting amide-type local anaesthetic. Mechanism of Action: Prilocaine reversibly and selectively binds to the intracellular surface of sodium channels to block sodium influx into the axon. This results in the prevention of depolarisation needed for action potential propagation and subsequent nerve function. Pharmacodynamics: The systemic absorption of prilocaine may cause depression and/or stimulation on both the cardiovascular and central nervous systems. If blood concentrations are within the normal therapeutic range, changes in cardiac conduction, contractility, excitability, refractoriness and peripheral vascular resistance are present. However, at toxic blood concentrations, cardiac excitability and conduction are depressed which may lead to AV block, ventricular arrhythmia and cardiac arrest. Furthermore, myocardial contractility is depressed and peripheral vasodilation occurs, resulting in a reduced cardiac output and arterial blood pressure. Onset: Infiltration: <2 minutes. Duration: Infiltration: Complete anaesthesia for procedures lasting 20 minutes. Pharmacokinetics: Distribution: Crosses the blood-brain barrier and placenta; enters breast milk. Volume of distribution: 190-260 L. Plasma protein binding: 40-55%. Metabolism: Primarily metabolised in the liver via hydrolysis by amidases into ortho-toluidine and N-propylamine, which may undergo ring hydroxylation. Excretion: Via urine (<5% as unchanged drug). Elimination half-life: 1.6 hours.
Chemical Structure
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)
N01BB04 - prilocaine ; Belongs to the class of amides. Used as local anesthetics.
References
4% Citanest Plain Dental Injection, Solution (Dentsply Pharmaceutical Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 29/10/2025.Brayfield A, Cadart C (eds). Prilocaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/10/2025.Joint Formulary Committee. Prilocaine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/10/2025.Pharmacy Retailing (NZ) Limited trading as Healthcare Logistics. Citanest Solution for Injection data sheet 10 November 2017. Medsafe. http://www.medsafe.govt.nz. Accessed 29/10/2025.Prilocaine Hydrochloride 1% Solution for Injection (Aspen Pharma Trading Limited). MHRA. https://products.mhra.gov.uk. Accessed 29/10/2025.Prilocaine Hydrochloride. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 29/10/2025.Prilocaine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 18/11/2025.Prilocaine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 29/10/2025.Prilotekal 20 mg/mL Solution for Injection (Sintetica Limited). MHRA. https://products.mhra.gov.uk. Accessed 18/11/2025.Takipril 20 mg/ml Solution for Injection (B.Braun Medical Industries Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 29/10/2025.
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