Lidocaine Topical

To use the cream, lotion, spray, foam, or gel on the skin, clean and dry the affected area as directed. Apply a thin layer of medication to the affected area of skin, usually 2 to 3 times a day or as directed.If you are using the spray, shake the canister well before using. While holding the canister 3-5 inches (8-13 centimeters) from the affected area, spray until wet. If the affected area is on the face, spray the medication onto your hand and apply to the face. Do not spray near your eyes, nose, or mouth.If you are using the foam, shake the canister well before using. Spray the foam onto your hand and apply to the affected area.Do not use on large areas of the body, cover the area with waterproof bandages or plastic, or apply heat unless directed to do so by your doctor. These may increase the risk of serious side effects.Wash hands immediately after use unless you are treating an area on the hands. Avoid getting the product in eyes, nose, or ears. If the medication gets in these areas, rinse the area immediately with clean water.Dosage is based on your medical condition and response to therapy. Do not use more of this product, use it more often, or keep using it longer than prescribed by your doctor. If you are using a nonprescription product, follow all the directions on the product package, or use as directed by your doctor. If there is an infection or sore in the area to be treated, do not use this medication without consulting your doctor first.Inform your doctor if your condition does not improve or worsens.

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Cream, External:

AneCream: 4% (5 g, 15 g, 30 g) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]

AneCream5: 5% (15 g, 30 g [DSC]) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]

LC-4 Lidocaine: 4% (45 g) [contains cetyl alcohol]

LC-5 Lidocaine: 5% (45 g) [contains cetyl alcohol]

Lidotral: 3.88% (85 g) [contains cetearyl alcohol, methylparaben, propylene glycol, propylparaben]

Lidovex: 3.75% (60 g) [contains cetyl alcohol, methylparaben, propylparaben]

Lidovin: 3.95% (60 g) [contains peg-40 castor oil]

Lidozol: 3.75% (60 g) [contains peg-40 castor oil]

LMX 4: 4% (5 g, 15 g, 30 g) [contains benzyl alcohol]

LMX 5: 5% (15 g, 30 g) [contains benzyl alcohol]

RectaSmoothe: 5% (30 g) [contains cetyl alcohol, methylparaben, propylene glycol, propylparaben]

RectiCare: 5% (15 g, 30 g) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]

Generic: 4% (5 g, 15 g, 30 g, 120 g); 5% (15 g, 30 g)

Cream, External, as hydrochloride:

CidalEaze: 3% (453.6 g) [contains aluminum sulfate, calcium acetate, cetyl alcohol, methylparaben, propylparaben]

EnovaRX-Lidocaine HCl: 5% (60 g, 120 g); 10% (60 g, 120 g) [contains cetyl alcohol]

Lidopin: 3% (28 g, 85 g); 3.25% (28 g, 85 g) [contains cetyl alcohol, methylparaben, propylparaben]

Lidtopic Max: 10% (30 mL) [contains cetyl alcohol]

Predator: 4% (63 g) [contains propylene glycol, trolamine (triethanolamine)]

Xolido: 2% (118 mL) [contains methylisothiazolinone]

Xolido XP: 4% (118 mL) [contains methylisothiazolinone]

Generic: 3% (28.3 g, 28.35 g, 85 g)

Gel, External:

Topicaine: 4% (10 g [DSC], 30 g [DSC], 113 g [DSC]) [contains benzyl alcohol, disodium edta]

Topicaine 5: 5% (10 g, 30 g, 113 g) [contains benzyl alcohol, disodium edta]

Gel, External, as hydrochloride:

Alocane Emergency Burn Max Str: 4% (75 mL)

Astero: 4% (30 mL)

LDO Plus: 4% (30 mL)

Lidocin: 3% (30 g [DSC], 120 g [DSC], 240 g [DSC]) [contains brilliant blue fcf (fd&c blue #1), polysorbate 80, tartrazine (fd&c yellow #5), trolamine (triethanolamine)]

LidoRx: 3% (10 mL, 30 mL, 90 mL) [contains isopropyl alcohol, trolamine (triethanolamine)]

Tranzarel: 4% (120 mL) [contains disodium edta, menthol, methylparaben, propylene glycol, propylparaben, trolamine (triethanolamine)]

Generic: 2% (5 mL, 20 mL, 30 mL)

Gel, External, as hydrochloride [preservative free]:

Glydo: 2% (6 mL, 11 mL) [pvc free]

Generic: 2% (5 mL, 10 mL)

Jet-injector, Intradermal, as hydrochloride:

Zingo: 0.5 mg (1 ea)

Kit, External:

AneCream: 4% [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]

Lidopac: 5% [contains polyethylene glycol]

Lidotrans 5 Pak: 5% [contains polyethylene glycol]

LMX 4 Plus: 4% [contains benzyl alcohol]

Xryliderm: 5% [contains edetate disodium, methylparaben, propylene glycol, propylparaben]

Zeyocaine: 5%

Generic: 4%

Kit, External, as hydrochloride:

Venipuncture Px1 Phlebotomy: 2% [latex free; contains methylparaben, propylparaben]

Lotion, External, as hydrochloride:

Anastia: 2.75% (15 g) [contains cetyl alcohol, methylparaben, propylparaben]

Eha: 4% (88 mL) [contains methylisothiazolinone]

Lido-K: 3% (177 mL) [contains cetyl alcohol, methylparaben, propylparaben]

Numbonex: 2.75% (30 g) [contains cetyl alcohol, methylparaben, propylparaben]

Generic: 3% (118 mL, 177 mL)

Ointment, External:

Lidocaine PAK: 5% (30 g) [contains polyethylene glycol, propylene glycol]

Premium Lidocaine: 5% (50 g)

Generic: 5% (30 g, 35.44 g, 50 g, 150 g, 250 g, 2500 g)

Patch, External:

Lidoderm: 5% (1 ea, 30 ea) [contains disodium edta, methylparaben, propylene glycol, propylparaben]

Prozena: 4% (5 ea [DSC], 15 ea [DSC], 30 ea [DSC])

Generic: 5% (1 ea, 15 ea, 30 ea)

Solution, External, as hydrochloride:

Xylocaine: 4% (50 mL) [contains methylparaben]

Generic: 4% (50 mL)

Solution, Mouth/Throat, as hydrochloride:

Generic: 2% (15 mL, 100 mL)

Solution, Mouth/Throat, as hydrochloride [preservative free]:

LTA 360 Kit: 4% (4 mL [DSC])

Generic: 4% (4 mL)

• Analgesic, Topical
• Local Anesthetic

Blocks both the 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

Absorption

Transdermal (5%): 3% ± 2% (following application of 3 patches), extent and rate variable; dependent upon concentration, dose, application site, and duration of exposure

Metabolism

Hepatic via CYP1A2 (major) and CYP3A4 (minor); active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX)

Excretion

Urine (<10% as unchanged drug)

Anesthesia, topical: Note: Smaller areas of treatment recommended in younger or smaller patients (<12 months or <10 kg) or those with impaired elimination (Fein 2012); use lowest effective dose

Cream:

LidaMantle, Lidovex: Skin irritation: Children and Adolescents: Refer to adult dosing.

LMX 4 (liposomal lidocaine 4%):

Skin irritation: Children ≥2 years and Adolescents: Refer to adult dosing.

Minor dermal procedures (eg, IV access, venipuncture, lumbar puncture, abscess drainage, joint aspiration); anesthetic (off-label):

Infants and Children <4 years: 1 g applied to site (6.25 cm2 of skin) 30 minutes prior to procedure (Fein 2012; Taddio 2004)

Children ≥4 years and Adolescents ≤17 years: 1 g to 2.5 g applied to site (6.25 cm2 of skin) 30 minutes prior to procedure (Eichenfield 2002; Fein 2012; Koh 2004; Luhman 2004; Taddio 2004)

LMX 5: Relief of anorectal pain and itching: Children ≥12 years and Adolescents: Refer to adult dosing.

Jelly: Children and Adolescents: Dose varies with age and weight (maximum dose: 4.5 mg/kg)

Intradermal injection: Children ≥3 years and Adolescents: Apply one intradermal lidocaine (0.5 mg) device to the site planned for venipuncture or IV cannulation, 1 to 3 minutes prior to needle insertion.

Lotion: Children and Adolescents: Refer to adult dosing.

Ointment: Children and Adolescents: Dose varies with age and weight, apply single application not exceeding 5 g of ointment (equivalent to lidocaine base 250 mg); maximum dose: lidocaine base 4.5 mg/kg.

Oral topical solution (2% viscous): Note: Not approved for relief of teething pain and discomfort in infants and children; serious adverse (toxic) effects have been reported; AAP, AAPD, and ISMP strongly discourage use (AAP 2011; AAPD 2012; ISMP 2014).

Infants and Children <3 years: ≤1.2 mL applied to area with a cotton-tipped applicator no more frequently than every 3 hours (maximum: 4 doses per 12-hour period; use only if the underlying condition requires treatment with product volume of ≤1.2 mL)

Children ≥3 years and Adolescents: Do not exceed 4.5 mg/kg/dose (or 300 mg per dose); swished in the mouth and spit out no more frequently than every 3 hours (maximum: 4 doses per 12-hour period)

Oral topical solution (4%): Note: For use in mucous membranes of oral and nasal cavities and proximal GI tract. Children and Adolescents: Dose varies with age and weight (maximum dose: 4.5 mg/kg)

Oral topical endotracheal solution, metered-dose spray (10 mg/actuation) [Canadian product]: Children ≥2 years and Adolescents: Dose varies with age and weight (maximum dose [children ≥2 to <12 years]: Laryngotracheal: 3 mg/kg; nasal/oropharyngeal: 4 to 5 mg/kg)

There are no dosage adjustments provided in the manufacturer’s labeling; use caution in patients with severe hepatic disease.

Gel (Topicaine): Apply a moderately thick layer to affected area (~1/8 inch thick). Allow time for numbness to develop (~20 to 60 minutes after application). When used prior to laser surgery, avoid mucous membranes and remove prior to laser treatment.

Intradermal injection: Refer to manufacturer’s labeling for administration technique. Apply intradermal lidocaine 1 to 3 minutes prior to needle insertion; perform procedure within 10 minutes following application. Application of one additional intradermal lidocaine at a new location is acceptable after a failed attempt at venous access; multiple administrations of intradermal lidocaine at the same location are not recommended. Only use on intact skin and on skin locations where an adequate seal can be maintained. Do not use on body orifices, mucous membranes, around the eyes, or on areas with a compromised skin barrier. When removing the device from the pouch, be careful not to touch the purple outlet (open end) to avoid contamination; do not use if the device has been dropped or if the pouch is damaged or torn.

Ointment: Use of a sterile gauze is suggested for application to broken skin; apply to tube prior to intubation. In dentistry, apply to previously dried oral mucosa; subsequent removal of excess saliva with cotton rolls or saliva ejector minimizes dilution of ointment, permits maximum penetration, and minimizes possibility of swallowing the ointment. For use with the insertion of new dentures, apply to all denture surfaces contacting mucosa.

Oral topical solution (2% viscous):

Mouth irritation or inflammation: Have patient swish medication around mouth and then spit it out. In children <3 years, apply to affected area with cotton-tipped applicator (do not use to relieve teething pain). Do not eat or chew gum for 60 minutes following use.

Pharyngeal anesthesia: Patient should gargle and may swallow medication. In children <3 years, apply to affected area with cotton-tipped applicator. Do not eat or chew gum for 60 minutes following use.

Oral topical endotracheal solution, metered-dose spray (10 mg/actuation) [Canadian product]: Attach nozzle and prime pump 5 to 10 times prior to first use; prime ~2 times (to remove air) when switching to a new nozzle. Product should be in upright position while spraying. Do not modify manufacturer supplied nozzle. Discard nozzle after use (do not reuse). Do not use on cuffs or endotracheal tubes made of plastic (may damage cuff).

Patch:

Lidoderm: Apply to most painful area of skin immediately after removal from protective envelope. Do not apply to non-intact skin. May be cut (with scissors, prior to removal of release liner) to appropriate size. Clothing may be worn over application area. After removal from skin, fold used patches so the adhesive side sticks to itself; avoid contact with eyes. Remove immediately if irritation or a burning sensation occurs. Wash hands after application. Avoid contact with water (eg, bathing, swimming, showering). Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub). Discard any used or unused patches by folding adhesive sides together and dispose of in trash away from children and pets.

LidoPatch: Remove protective film and apply to painful area. Avoid contact with eyes or mucous membranes. Wash hands after application. Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub). Discard any used or unused patches by folding adhesive sides together and dispose of in trash away from children and pets.

Life-threatening and fatal events in infants and young children:

Postmarketing cases of seizures, cardiopulmonary arrest, and death in patients under the age of 3 years have been reported with use of lidocaine 2% viscous solution when it was not administered in strict adherence to the dosing and administration recommendations. In the setting of teething pain, lidocaine 2% viscous solution should generally not be used. For other conditions, the use of the product in patients less than 3 years should be limited to those situations where safer alternatives are not available or have been tried but failed.

To decrease the risk of serious adverse events with use of lidocaine 2% viscous solution, instruct caregivers to strictly adhere to the prescribed dose and frequency of administration and store the prescription bottle safely out of reach of children.

Concerns related to adverse effects:

• Familial malignant hyperthermia: Many drugs used during the conduct of anesthesia may trigger familial malignant hyperthermia; not known whether amide-type local anesthetics trigger this reaction. However, standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile blood pressure, and metabolic acidosis may precede temperature elevation. If familial malignant hyperthermia is confirmed, discontinue triggering agent and initiate appropriate therapy (eg, oxygen, dantrolene) and other supportive measures.

• Hypersensitivity: Use with caution in patients with known drug sensitivities. Allergic reactions (cutaneous lesions, urticaria, edema, or anaphylactoid reactions) may be a result of sensitivity to lidocaine (rare) or preservatives used in formulations. Patients allergic to para-aminobenzoic acid (PABA) derivatives (eg, procaine, tetracaine, benzocaine) have not shown cross sensitivity to lidocaine.

• Local effects: Irritation, sensitivity and/or infection may occur at the site of application; discontinue use and institute appropriate therapy if local effects occur.

• Systemic adverse effects: Potentially life-threatening side effects (eg, irregular heart beat, seizures, coma, respiratory depression, death) have occurred when used prior to cosmetic procedures. Excessive dosing for any indication (eg, application to large areas, use above recommended dose, application to denuded or inflamed skin, or wearing of device for longer than recommended), smaller patients, and/or impaired elimination may lead to increased absorption and systemic toxicity; patient should adhere strictly to recommended dosage and administration guidelines; serious adverse effects may require the use of supportive care and resuscitative equipment; lidocaine toxicity may occur at blood concentrations above 5 mcg/mL.

Disease-related concerns:

• Bleeding tendencies/platelet disorders: Intradermal injection: Use with caution; may have a higher risk of superficial dermal bleeding.

• Cardiovascular disease: Use with caution in patients with severe shock or heart block.

• Dermal integrity reduced: Application to broken or inflamed skin may lead to increased systemic absorption; use caution.

• Familial malignant hyperthermia: May potentially trigger malignant hyperthermia; follow standard protocol for identification and treatment.

• Hepatic impairment: Use caution in patients with severe hepatic disease due to diminished ability to metabolize systemically-absorbed lidocaine.

• Pseudocholinesterase deficiency: Use with caution; these patients have a greater risk of developing toxic plasma concentrations of lidocaine.

• Sepsis/severely traumatized mucosa: Use with extreme caution in the presence of sepsis and/or severely traumatized mucosa due to an increased risk of rapid systemic absorption at application site.

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.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain 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 suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

• Intradermal injection: Only use on intact skin and on skin locations where an adequate seal can be maintained. Do not use on body orifices, mucous membranes, around the eyes, or on areas with a compromised skin barrier.

• 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 (Alade 1986; CDC 1984). See manufacturer’s labeling.

• Topical cream, liquid, lotion, gel, and ointment: Do not leave on large body areas for >2 hours. Not for ophthalmic use. Some products are not recommended for use on mucous membranes; consult specific product labeling.

• Topical oral solution: When used in mouth or throat, topical anesthesia may impair swallowing and increase aspiration risk. Avoid food for ≥60 minutes following oral or throat application. This is especially important in the pediatric population. Numbness may increase the danger of tongue/buccal biting trauma; ingesting food or chewing gum should be avoided while mouth or throat is anesthetized. Excessive doses or frequent application may result in high plasma levels and serious adverse effects; strictly adhere to dosing instructions. Use measuring devices to measure the correct volume, if applicable, to ensure accuracy of dose.

• Topical patch: Apply only on intact skin. Do not use around or in the eyes. To avoid accidental ingestion by children, store and dispose of products out of the reach of children. Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub).

Special populations:

• Acutely ill patients: Use with caution; acutely ill patients should be given reduced doses commensurate with their age and physical status.

• Elderly and debilitated patients: Use with caution; elderly and debilitated patients should be given reduced doses commensurate with their age and physical status.

• Oral topical solution/viscous: [US Boxed Warning]: Life-threatening and fatal events in infants and young children: Postmarketing cases of seizures, cardiopulmonary arrest, and death in patients <3 years have been reported with use of lidocaine 2% viscous solution when it was not administered in strict adherence to the dosing and administration recommendations. Lidocaine 2% viscous solution should generally not be used for teething pain. For other conditions, the use of lidocaine 2% viscous solution in patients <3 years should be limited to those situations where safer alternatives are not available or have been tried but failed. To decrease the risk of serious adverse events, instruct caregivers to strictly adhere to the prescribed dose and frequency of administration, and store the prescription bottle safely out of reach of children. Multiple cases of seizures (including fatalities) have occurred in pediatric patients using viscous lidocaine for oral discomfort, including use for teething pain and stomatitis (Curtis 2009; Giard 1983; Gonzalez del Ray 1994; Hess 1988; Mofenson 1983; Puczynski 1985; Rothstein 1982; Smith 1992). The FDA recommends against using topical OTC medications for teething pain as some products may cause harm. The American Academy of Pediatrics (AAP) recommends managing teething pain with a chilled (not frozen) teething ring or gently rubbing/massaging with the caregiver's finger. Use of topical anesthetics for teething is discouraged by the AAP, the American Academy of Pediatric Dentistry, and the ISMP (AAP 2012; AAPD 2012; ISMP 2014).

• Pediatric: Use with caution; children should be given reduced doses commensurate with their age and physical status.

Other warnings/precautions:

• Topical application: When topical anesthetics are used prior to cosmetic or medical procedures, the lowest amount of anesthetic necessary for pain relief should be applied. High systemic levels and toxic effects (eg, methemoglobinemia, irregular heart beats, respiratory depression, seizures, death) have been reported in patients who (without supervision of a trained professional) have applied topical anesthetics in large amounts (or to large areas of the skin), left these products on for prolonged periods of time, or have used wraps/dressings to cover the skin following application.

This medication patch may be harmful if chewed or swallowed. If someone has overdosed, remove the patch if possible. For serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: severe drowsiness, seizures, slowed breathing, slow/fast/irregular heartbeat.

Notes

Do not share this medication with others.

Missed Dose

If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Storage

Store at room temperature away from light and moisture. Do not store in the bathroom. Keep the patch sealed in its protective envelope until ready to use. Keep all medications away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed (See How to Use section).Information last revised July 2016. Copyright(c) 2016 First Databank, Inc.