Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, External:
AvaDERM: Lidocaine 4% and menthol 1% (120 g) [contains cetearyl alcohol, propylene glycol, trolamine (triethanolamine)]
LevigoLT: Lidocaine 4% and menthol 1% (76.5 g) [paraben free; contains cetearyl alcohol, disodium edta]
Synvexia TC: Lidocaine 4% and menthol 1% (60 g) [contains cetyl alcohol, naproxen, trolamine salicylate]
Veltrix: Lidocaine 4% and menthol 1% (120 g [DSC])
Gel, External:
LenzaGel: Lidocaine 4% and menthol 1% (120 g [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
Lidothol: Lidocaine 4.5% and menthol 5% (105 g) [contains sd alcohol, trolamine (triethanolamine)]
LidozenGel: Lidocaine 4% and menthol 1% (120 mL) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
Kit, External:
LidoStream: Lidocaine 5% and menthol 10% [contains isopropyl alcohol, propylene glycol]
Mentho-Caine: Lidocaine 5% and menthol 8% [DSC]
Liquid, External:
1st Relief Spray: Lidocaine 4% and menthol 1% (118 mL) [contains sodium benzoate]
Lotion, External:
Gen7T Plus: Lidocaine 3.5% and menthol 7% (120 g) [contains edetate disodium, trolamine (triethanolamine)]
Patch, External:
AvaLin: Lidocaine 4% and menthol 1% (15 ea) [contains polysorbate 80]
Endoxcin: Lidocaine 4% and menthol 1% (15 ea [DSC], 30 ea [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
Gen7T Plus: Lidocaine 3.5% and menthol 7% (15 ea) [contains propylene glycol]
LenzaPatch: Lidocaine 4% and menthol 1% (5 ea [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
Lidenza: Lidocaine 4% and menthol 1% (15 ea [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
LidoPatch Pain Relief: Lidocaine 3.99 % and menthol 1.25% (3 ea) [contains disodium edta, iodopropynyl butylcarbamate, methylparaben, polysorbate 80, propylparaben]
LidoPatch Pain Relief: Lidocaine 3.6% and menthol 1.25% (3 ea, 30 ea) [contains disodium edta, methylparaben, polysorbate 80, propylparaben]
Lidothol: Lidocaine 4.5% and menthol 5% (1 ea, 15 ea) [contains polysorbate 80]
LidozenPatch: Lidocaine 4% and menthol 1% (5 ea) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
LidozenPatch: Lidocaine 4% and menthol 1% (5 ea) [contains methylparaben, polysorbate 80, propylene glycol]
LidozenPatch: Lidocaine 4% and menthol 1% (5 ea) [contains polysorbate 80, propylene glycol]
Limencin: Lidocaine 4% and menthol 4% (10 ea) [contains edetate disodium, iodopropynyl butylcarbamate, methylparaben, polysorbate 80, propylparaben]
Lorenza: Lidocaine 4% and menthol 1% (15 ea [DSC]) [contains edetate disodium]
MaL Patch: Lidocaine 4% and menthol 5% (15 ea) [contains disodium edta, iodopropynyl butylcarbamate, methylparaben, polysorbate 80, propylparaben]
Prolida: Lidocaine 4% and menthol 1% (15 ea) [contains polysorbate 80]
Releevia ML: Lidocaine 4% and menthol 1% (15 ea [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]
Siterol: Lidocaine 3.99% and menthol 1% (15 ea) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5)]
Solmara: Lidocaine 4% and menthol 5% (15 ea [DSC])
Synvexia: Lidocaine 4% and menthol 1% (5 ea [DSC], 10 ea [DSC], 15 ea [DSC], 30 ea [DSC]) [contains disodium edta, polysorbate 80]
Terocin: Lidocaine 4% and menthol 4% (10 ea) [contains edetate disodium, iodopropynyl butylcarbamate, methylparaben, polysorbate 80, propylparaben]
Venia: Lidocaine 4% and menthol 4% (10 ea) [contains polysorbate 80]
Zeruvia: Lidocaine 4% and menthol 1% (15 ea, 30 ea) [contains disodium edta, polysorbate 80]
Pharmacology
Mechanism of Action
Lidocaine: Blocks both initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.
Menthol: Dilates the blood vessels, causing a sensation of coldness followed by an analgesic effect; relieves itching.
Use: Labeled Indications
Anesthetic, topical:
OTC products:
Cream, gel, and spray: Temporary relief of pain and itching associated with minor burns and cuts, scrapes, sunburn, insect bites, or skin irritations.
Patch: Temporary relief of mild to moderate muscles/joint aches and pains (eg, arthritis, simple backache, bursitis, tendonitis, muscle soreness/stiffness/strains, sprains, bruises); temporary relief of pain associated with minor cuts, scrapes, or skin irritations.
RX products: Cream: Relief of abrasions, minor burns, insect bites, pain, pruritic eczemas, pruritus, soreness, and discomfort due to anal fissures, hemorrhoids, pruritus ani, pruritus vulvae, and similar conditions of the skin and mucous membranes.
Contraindications
Hypersensitivity to lidocaine, menthol, local anesthetic of the amide type, or any component of the formulation; secondary bacterial infection at application site; traumatized mucosa.
Dosage and Administration
Dosing: Adult
Anesthetic: Topical:
OTC products:
Cream: Apply a thin film to the affected area 3 to 4 times daily.
Gel, spray: Apply to affected areas ≤4 times daily.
Patch:
Avalin, Lidozen: Apply patch to affected area ≤4 times daily. Patch may remain in place for up to 8 hours. Do not use for >5 consecutive days.
LidoPatch: Apply patch to affected area. Patch may remain in place for up to 12 hours (maximum: 1 patch/24 hours).
Lidothol: Apply patch to affected area. Patch may remain in place for 8 to 12 hours (maximum: 2 patches/24 hours).
Siterol: Apply patch to affected area. Patch may remain in place for up to 8 hours (maximum: 4 patches/24 hours). Do not use >5 consecutive days.
Solmara, Terocin: Apply patch to affected area once or twice daily.
Rx products: Cream: Apply a thin film to the affected area 2 or 3 times daily.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Anesthetic: Topical: OTC products:
Cream: Children ≥2 years and Adolescents: Apply a thin film to the affected area 3 to 4 times daily.
Spray: Children ≥2 years and Adolescents: Apply to affected areas ≤4 times daily.
Patch:
Avalin: Children ≥2 years and Adolescents: Apply patch to affected area ≤4 times daily. Patch may remain in place for up to 8 hours. Do not use for longer than 5 consecutive days.
Lidothol: Children ≥12 years and Adolescents: Apply patch to affected area. Patch may remain in place for 8 to 12 hours (maximum: 2 patches/24 hours).
Solmara, Terocin: Children ≥12 years and Adolescents: Apply patch to affected area once or twice daily.
Administration
For external use only; not for ophthalmic, oral, or genital use; do not use on open wounds, cuts, damaged or infected skin or on mucous membranes. Some products are not recommended for use with bandages; consult specific product labeling.
Patch: Clean and dry affected area prior to administration; remove protective film and apply. Wash hands after application. Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub).
Storage
OTC products: Store at room temperature. Protect from moisture and direct sunlight. Discard any used or unused patches by folding adhesive sides together and dispose of in trash away from children and pets.
Rx products: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from freezing.
Drug Interactions
Antiarrhythmic Agents (Class III): Lidocaine (Topical) may enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Antiarrhythmic Agents (Class III) may increase the serum concentration of Lidocaine (Topical). This mechanism specifically applies to amiodarone and dronedarone. Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Beta-Blockers: May increase the serum concentration of Lidocaine (Topical). Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Consider therapy modification
Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy
Disopyramide: May enhance the arrhythmogenic effect of Lidocaine (Topical). Disopyramide may increase the serum concentration of Lidocaine (Topical). Specifically, the unbound/free fraction of lidocaine. Monitor therapy
Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination
Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy
MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification
Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy
Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Prilocaine: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy
Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification
Adverse Reactions
Also see Lidocaine monograph.
Frequency not defined:
Central nervous system: Burning sensation, localized warm feeling, paresthesia (localized), stinging sensation
Dermatologic: Localized erythema
Local: Localized edema
Warnings/Precautions
Concerns related to adverse effects:
- Local effects: Irritation, sensitivity, and/or infection may occur at the site of application; discontinue use and institute appropriate therapy if local effects occur.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- Acutely ill patients: Use with caution; acutely ill patients should be given reduced doses commensurate with their age and physical status.
- Debilitated patients: Use with caution; debilitated patients should be given reduced doses commensurate with their age and physical status.
- Elderly: Use with caution; elderly patients should be given reduced doses commensurate with their age and physical status.
- Pediatric: Use with caution; children should be given reduced doses commensurate with their age and physical status.
Dosage form specific issues:
- Benzyl alcohol: Some dosage forms may contain benzyl alcohol and/or sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982); some data suggest that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol and/or benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.
- Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (alad 1986; CDC 1984). See manufacturer's labeling.
- Topical patch: Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub).
Other warnings/precautions:
- Self-medication (OTC use): When used for self-medication, discontinue use and contact health care provider if symptoms persist >7 days, condition worsens or recurs, or if rash, irritation, or itching develops. Do not use on open wounds, cuts, damaged or infected skin; in the eyes, mouth, genitals; or any other mucous membranes. Do not use in large quantities, particularly over raw or blistered areas. Some products are not recommended for use with bandages; consult specific product labeling.
Pregnancy
Pregnancy Risk Factor
B
Pregnancy Considerations
Animal reproduction studies have not been conducted with this combination. See individual agents.
Patient Education
What is this drug used for?
- It is used to relieve itching and pain from insect bites or skin irritation and to ease muscle and joint aches and pain. Some products may be used to treat signs of hemorrhoids or rectal irritation. It may be given to you for other reasons. Talk with the doctor.
Frequently reported side effects of this drug
- Burning
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Redness
- Application site irritation
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
