Lidocaine + Prilocaine


Generic Medicine Info
Indications and Dosage
Periodontal
Local anaesthesia
Adult: Available preparation:
Each g of periodontal gel contains lidocaine 25 mg and prilocaine 25 mg

In patients who require localised anaesthesia in periodontal pockets for diagnostic and treatment procedures (e.g. probing, scaling, root planing): Usual dose: 1 cartridge (1.7 g containing 42.5 mg lidocaine and 42.5 mg prilocaine) or less will be sufficient for 1 quadrant of dentition. Max: 5 cartridges (8.5 g containing 212.5 mg lidocaine and 212.5 mg prilocaine) per 1 treatment session. Refer to the detailed product guideline for specific dosing application instructions.
Elderly: May require smaller treatment area or lower doses based on physical status.

Topical/Cutaneous
Topical anaesthesia
Adult: Available preparations:
Each g of cream contains lidocaine 25 mg and prilocaine 25 mg
Each g of emulsion for cutaneous patch of 10 cm2 contains lidocaine 25 mg and prilocaine 25 mg

As cream: Apply a thick layer onto the skin and cover with occlusive dressing prior to procedures. For use on intact skin in minor procedures (e.g. needle insertion, surgical treatment of localised lesions): Apply 2 g (approx 1/2 of a 5 g tube) or approx 1.5 g per 10 cm2 for at least 1 hour up to Max 5 hours. Alternatively, 2.5 g over 20-25 cm2 of skin surface area for at least 1 hour. For more extensive superficial surgical procedures (e.g. split-skin grafting): Apply 1.5-2 g per 10 cm2 for at least 2 hours up to Max 5 hours. For the skin of genital organs prior to local anaesthetic inj: In men: Apply 1 g per 10 cm2 for 15 minutes; In women: Apply 1-2 g per 10 cm2 for 60 minutes. For the genital mucosa (e.g. removal of genital warts, prior to superficial procedures or infiltration anaesthesia): Apply approx 5-10 g for 5-10 minutes, depending on the treatment area; occlusion is not necessary. For the genital mucosa prior to cervical curettage: Apply 10 g in the lateral vaginal fornices for 10 minutes. For leg ulcers (e.g. mechanical cleansing, surgical debridement): Apply approx 1-2 g per 10 cm2 up to Max 10 g for 30-60 minutes, depending on the difficulty of tissue penetration. As patch: For use on intact skin in minor procedures (e.g. needle insertion): Apply ≥1 patch(es) to <10 cm2 skin surface area for at least 1 hour up to Max 5 hours. Refer to the detailed product guideline for specific dosing application instructions.
Child: Available preparations:
Each g of cream contains lidocaine 25 mg and prilocaine 25 mg
Each g of emulsion for cutaneous patch of 10 cm2 contains lidocaine 25 mg and prilocaine 25 mg

As cream: Apply a thick layer onto the skin and cover with occlusive dressing prior to procedures. For use on intact skin in needle insertion, curettage of lesions caused by mollusca contagiosa, and other minor surgical procedures: Apply approx 1 g per 10 cm2. Dosage must be individualised based on age, weight, procedure, and application area. 0-2 months or <5 kg: Max: 1 g and 10 cm2 for 1 hour as single dose within 24 hours; 3-11 months and >5-10 kg: Max: 2 g and 20 cm2 for 1 hour; 1-5 years and >10-20 kg: Max: 10 g and 100 cm2 for at least 1 hour up to 5 hours; 6-11 years and >20 kg: Max: 20 g and 200 cm2 for at least 1 hour up to 5 hours; ≥12 years Same as adult dose. As patch: For use on intact skin in minor procedures (e.g. needle insertion): 0-2 months Max: 1 patch for up to 1 hour; 3-11 months Max: 2 patches and for up to 1 hour; 1-5 years Max: 10 patches and for at least 1 hour up to 5 hours; 6-11 years Max: 20 patches and for at least 1 hour up to 5 hours; ≥12 years Same as adult dose. Refer to the detailed product guideline for specific dosing application instructions.
Elderly: May require smaller treatment area based on physical status.

Topical/Cutaneous
Premature ejaculation
Adult: Available preparation:
Each mL of spray solution contains lidocaine 150 mg and prilocaine 50 mg

For the treatment of primary premature ejaculation in men: Each dose is equal to 3 actuations. Recommended dose: Apply 3 actuations (containing total of 22.5 mg lidocaine and 7.5 mg prilocaine per application) to cover the glans penis. Max: 3 doses 24 hourly with at least 4 hours between doses. Wipe off excess spray after 5 minutes and prior to intercourse. Refer to the detailed product guideline for specific dosing application instructions.
Special Patient Group
Acutely ill and debilitated patients: May require smaller treatment area based on physical status.

Patients with atopic dermatitis: Reduced application time (15-30 minutes) may be necessary.
Hepatic Impairment
Topical anaesthesia:
Severe: May require smaller treatment area.
Contraindications
Congenital, idiopathic or acquired methaemoglobinaemia; newborn infants or infants ≤12 months receiving concomitant treatment with methaemoglobin-inducing agents. Pre-term newborn infants with gestational age <37 weeks. Application to broken or inflamed skin, open wounds (except leg ulcers), or near the eyes.
Special Precautions
Patient with history of drug sensitivities; G6PD deficiency, anaemia, severe impairment of impulse initiation and heart conduction (e.g. grade II and III atrioventricular block, pronounced bradycardia), cardiac or pulmonary compromise, concurrent exposure to oxidising agents or their metabolites; atopic dermatitis. Patients who are in remission from porphyria; asymptomatic carriers of mutated genes responsible for porphyria development. Acutely ill or debilitated patients. Not recommended for use in situations where penetration or migration past the tympanic membrane into the middle ear is possible. Similar precautions must be observed for the partner of the patient when using the spray solution. Do not apply periodontal gel to ulcerative lesions or during acute oral cavity infections. Severe hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Allergic and anaphylactic reactions, eye irritation, numbness of oral mucosa (periodontal gel); erectile dysfunction and male genital hypoaesthesia.
Gastrointestinal disorders: Nausea, taste perversion, throat irritation.
General disorders and administration site conditions: Fatigue, flu-like disorder, pyrexia, local alteration in temperature sensations; application site reactions such as pruritus, erythema, burning or stinging sensation, warmth, pallor; rarely, purpuric or petechial lesions (cream/patch); local pain, oedema, numbness, soreness, irritation, ulceration, abscess, vesicles (periodontal gel).
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia.
Nervous system disorders: Headache, dizziness.
Reproductive system and breast disorders: Genital burning sensation; hypoaesthesia, vulvovaginal burning sensation in female partners (spray solution).
Respiratory, thoracic and mediastinal disorders: Respiratory tract infection, rhinitis.
Skin and subcutaneous tissue disorders: Urticaria. Rarely, hyperpigmentation.
Potentially Fatal: Methaemoglobinaemia.
Patient Counseling Information
Spray solution: May deteriorate polyurethane-based condoms; use alternative contraceptive measures.
MonitoringParameters
Monitor serum methaemoglobin prior to, during, and after use in neonates and infants up to 3 months; ECG in patients treated with class III antiarrhythmics (e.g. amiodarone).
Overdosage
Symptoms: CNS excitation or depression (e.g. visual disturbances, hyperacusis, muscular tremors, light-headedness, general convulsions), CV manifestations (e.g. hypotension, bradycardia, arrhythmia, CV collapse); rarely, clinically significant methaemoglobinaemia. Management: Symptomatic and supportive treatment. May administer anticonvulsant agents and initiate respiratory support for severe neurological symptoms (e.g. convulsions, CNS depression); initiate CV resuscitation as necessary. Administer slow IV inj of methylthioninium Cl to treat clinically significant methaemoglobinaemia.
Drug Interactions
May cause additive toxic effects with dental inj anaesthesia, class I antiarrhythmics (e.g. mexiletine, tocainide). Additive cardiac effects may be produced by class III antiarrhythmics (e.g. amiodarone, dofetilide, sotalol).
Potentially Fatal: Increased risk of methaemoglobinaemia with other local anaesthetics (e.g. benzocaine, procaine, tetracaine), nitrates/nitrites (e.g. nitric oxide, nitroprusside), antineoplastic agents (e.g. cyclophosphamide, flutamide), antibiotics (e.g. dapsone, nitrofurantoin, sulfonamides), antimalarials (e.g. chloroquine, primaquine, quinine), anticonvulsants (e.g. phenytoin, phenobarbital), paracetamol, and metoclopramide.
Lab Interference
May cause positive result in anti-doping controls.
Action
Description: Lidocaine and prilocaine are amide-type local anaesthetic agents. Both produce local anaesthetic activity by stabilising the neuronal membranes and blocking the Na ion channels necessary for the initiation and conduction of nerve impulses.
Synonym: lidocaine: lignocaine.
Onset: Periodontal gel: ≤30 seconds. Cream: 1 hour; 5-10 minutes (genital mucosa).
Duration: Periodontal gel: Approx 20 minutes. Cream: 1-2 hours (after removal, except in the face); 15-20 (range: 5-45) minutes (after application on genital mucosa).
Pharmacokinetics:
Absorption: Dependent on the duration of exposure and area of application. Absorbed from oral mucous membranes (periodontal gel). Bioavailability: Approx 20-40% (periodontal gel). Time to peak plasma concentration: 2-6 hours (patch, cream); 20-45 minutes (cream [vaginal mucosa]).
Distribution: Crosses blood-brain barrier and placenta.
Lidocaine: Enters breast milk (small amounts). Plasma protein binding: 60-80%, mainly to α1-acid glycoprotein.
Prilocaine: Possibly enters breast milk. Plasma protein binding: Approx 40-55%, mainly to α1-acid glycoprotein.
Metabolism: Lidocaine: Rapidly metabolised in the liver primarily by CYP1A2 and to a lesser extent by CYP3A4 via N-dealkylation to active metabolites, monoethylglycinexylidide (MEGX) and glycinexylidide (GX).
Prilocaine: Rapidly metabolised mainly in the liver by CYP450 and to a lesser extent in the kidneys by amidases via hydrolysis into o-toluidine and N-propylalanine which may undergo ring hydroxylation.
Excretion: Lidocaine: Via urine (<10% as unchanged drug). Terminal elimination half-life: 3.6 hours (periodontal gel).
Prilocaine: Via urine (<5% as unchanged drug). Terminal elimination half-life: 2.8 hours (periodontal gel).
Chemical Structure

Chemical Structure Image
Lidocaine

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3676, Lidocaine. https://pubchem.ncbi.nlm.nih.gov/compound/Lidocaine. Accessed Sept. 29, 2020.


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
Cream/patch: Store between 15-30°C. Do not refrigerate or freeze. Periodontal gel/spray solution: Store below 25°C. Do not freeze.
ATC Classification
N01BB52 - lidocaine, combinations ; Belongs to the class of amides. Used as local anesthetics.
N01BB54 - prilocaine, combinations ; Belongs to the class of amides. Used as local anesthetics.
References
Anon. Lidocaine (Topical). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2020.

Anon. Lidocaine and Prilocaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2020.

Anon. Prilocaine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/06/2020.

Buckingham R (ed). Lidocaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2020.

Buckingham R (ed). Prilocaine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2020.

EMLA Cream 5% (Aspen Pharmacare). MIMS Singapore. http://www.mims.com/singapore. Accessed 01/06/2020.

Fortacin 150 mg/mL + 50 mg/mL Cutaneous Spray Solution (Recordati Ireland Ltd.). European Medicines Agency [online]. Accessed 01/06/2020.

Joint Formulary Committee. Lidocaine with Prilocaine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/06/2020.

Lidocaine and Prilocaine Cream (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/06/2020.

Lidocaine/Prilocaine 5 % Cutaneous Patch (Morningside Healthcare Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 01/06/2020.

Nulbia 5% Cream (Glenmark Pharmaceuticals Europe Limited). MHRA. https://products.mhra.gov.uk/. Accessed 01/06/2020.

Oraqix 25/25 mg per gram Periodontal Gel (Dentsply Limited). DailyMed. Source: U.S. National Library of Medicine. https://products.mhra.gov.uk/. Accessed 01/06/2020.

Oraqix Gel (Dentsply Pharmaceutical). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/06/2020.

Disclaimer: This information is independently developed by MIMS based on Lidocaine + 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 © 2021 MIMS. All rights reserved. Powered by MIMS.com
  • Emla
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in