Lidocaine (Topical)

Brand names: Lidosense 5, LMX 5, LidaMantle, Xylocaine Jelly, Bactine, Xylocaine Topical, Anestacon, Xylocaine Viscous, Lidomar, Xylocaine 10% Oral, Dermaflex, Solarcaine Burn Relief, Medi-Quik Spray, Protech First Aid Stik, Ela-Max, Lidoderm, Ela-Max 5, LMX Plus, LMX 4 with Tegaderm, LMX 4

Reviewed by Medicine.com on February 10, 2020

Boxed Warning

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.

Dosage Forms

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

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 [DSC]) [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 [DSC]) [contains cetyl alcohol, methylparaben, propylparaben]

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

Lidozol: 3.75% (60 g [DSC]) [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: 3.88% (85 g [DSC]); 4% (5 g, 15 g, 30 g, 120 g); 5% (15 g, 30 g)

Cream, External, as hydrochloride:

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

Lidocaine Plus: 4% (120 g) [contains cetearyl alcohol, propylene glycol, trolamine (triethanolamine)]

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

NeuroMed7: 4% (63 g) [contains propylene glycol, trolamine (triethanolamine)]

Pain Relieving: 4% (15 g, 30 g [DSC]) [contains cetearyl alcohol, disodium edta]

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); 4% (120 g); 4.12% (28.3 g, 85 g)

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 [DSC], 90 mL)

LDO Plus: 4% (30 mL)

LidoDose: 3% (1 mL) [contains isopropyl alcohol, trolamine (triethanolamine)]

LidoDose Pediatric Bulk Pack: 3% (1 mL) [contains isopropyl alcohol, trolamine (triethanolamine)]

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

Lidotrex: 2% (28.33 g) [contains trolamine (triethanolamine)]

7T Lido: 2% (85 g) [contains trolamine (triethanolamine)]

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

Generic: 2% (5 mL, 30 mL)

Jet-injector, Intradermal, as hydrochloride:

Zingo: 0.5 mg (1 ea [DSC])

Jet-injector, Intradermal, as hydrochloride [preservative free]:

Zingo: 0.5 mg (1 ea)

Generic: 0.5 mg (1 ea)

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

Lidopac: 5% [contains polyethylene glycol]

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

Lidotrans 5 Pak: 5% [DSC] [contains polyethylene glycol]

LMX 4 Plus: 4% [contains benzyl alcohol]

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

Zeyocaine: 5% [DSC]

Kit, External, as hydrochloride:

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

Liquid, External, as hydrochloride:

LevigoSP: 2.5% (150 mL) [paraben free; contains propylene glycol]

Gen7T: 3.5% (120 g) [contains edetate disodium, trolamine (triethanolamine)]

Lotion, External, as hydrochloride:

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

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

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

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

Lidozion: 3% (177 mL) [contains cetyl alcohol, edetate disodium, methylparaben, propylparaben]

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

Zionodil: 3% (177 mL) [contains cetyl alcohol, edetate disodium, methylparaben, propylparaben]

Zionodil 100: 3% (177 mL) [contains cetyl alcohol, propylene glycol, trolamine (triethanolamine)]

Generic: 3% (118 mL [DSC], 177 mL)

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

Premium Lidocaine: 5% (50 g)

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

Gen7T: 3.5% (15 ea) [contains propylene glycol]

Lido King: 4% (5 ea) [contains edetate disodium, methylparaben, propylene glycol, propylparaben]

Lidocaine Pain Relief: 4% (5 ea) [contains methylparaben, polysorbate 80, propylene glycol, propylparaben]

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

Re-Lieved Maximum Strength: 4% (6 ea) [odor free]

ZTlido: 1.8% (1 ea, 30 ea)

Generic: 4% (5 ea); 5% (1 ea, 15 ea, 30 ea)

Prefilled Syringe, External, as hydrochloride:

Generic: 2% (20 mL)

Prefilled Syringe, External, as hydrochloride [preservative free]:

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

Generic: 2% (5 mL, 10 mL)

Solution, External, as hydrochloride:

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

Generic: 4% (50 mL)

Solution, Mouth/Throat, as hydrochloride:

Generic: 2% (15 mL, 100 mL)

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

Pharmacology

Mechanism of Action

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

Pharmacokinetics/Pharmacodynamics

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

Onset of Action

Intradermal injection: 1 to 3 minutes; Topical: 3 to 5 minutes; Transdermal: ~4 hours (Davies 2004)

Time to Peak

Transdermal (5%): 11 hours (following application of 3 patches); Transdermal (1.8%): ~14 hours (following application of 3 patches)

Duration of Action

Intradermal injection: 10 minutes

Half-Life Elimination

IV: 1.5 to 2 hours; prolonged 2-fold or more in hepatic impairment

Protein Binding

Use in Specific Populations

Special Populations: Renal Function Impairment

Accumulation of metabolites may occur.

Use: Labeled Indications

Intradermal injection (Zingo): Topical local analgesia prior to venipuncture or peripheral IV cannulation in children ≥3 years of age; topical local analgesia prior to venipuncture in adults.

Jelly: Prevention and control of pain in procedures involving the male and female urethra; for topical treatment of painful urethritis

Oral topical solution (2% viscous): Topical anesthesia of irritated or inflamed oral mucous membranes and pharyngeal tissue; reducing gagging during the taking of x-ray. Note: Not approved for relief of teething pain and discomfort in infants and children; serious adverse (toxic) effects have been reported (AAP 2011; AAPD 2012; ISMP 2014).

Oral topical solution (4%): Topical anesthesia of accessible mucous membranes of the oral and nasal cavities and proximal portions of the digestive tract. Note: Not approved for relief of teething pain and discomfort in infants and children; serious adverse (toxic) effects have been reported (AAP 2011; AAPD 2012; ISMP 2014).

Oral topical solution (metered-dose spray) [Canadian product]: Topical anesthesia of accessible mucous membranes of the oral and nasal cavities and proximal portions of the digestive tract.

Patch (Lidoderm, ZTlido): Relief of pain associated with postherpetic neuralgia

Patch (OTC 4%): Temporary relief of minor localized pain

Rectal: Temporary relief of pain and itching due to anorectal disorders

Topical: Local anesthetic for mucous membrane of the oropharynx; lubricant for intubation; use in laser/cosmetic surgeries; pruritus, pruritic eczemas, insect bites, pain, soreness, minor burns (including sunburns), cuts, and abrasions of the skin; discomfort due to pruritus ani, pruritus vulvae, hemorrhoids, anal fissures, and similar conditions of the skin and mucous membranes

Contraindications

Hypersensitivity to lidocaine or any component of the formulation; hypersensitivity to another local anesthetic of the amide type; traumatized mucosa, bacterial infection at the site of application (lotion and Lidovex only).

Dosage and Administration

Dosing: Adult

Anesthesia, topical:

LidaMantle, Lidovex: Skin irritation: Apply a thin film to affected area 2 to 3 times daily as needed

LMX 4: Skin irritation: Apply up to 3 to 4 times daily to intact skin

LMX 5: Relief of anorectal pain and itching: Apply to affected area up to 6 times daily

Gel: Apply to affected area ≤4 times daily as needed (maximum dose: 4.5 mg/kg, not to exceed 300 mg)

Intradermal injection: Apply one intradermal lidocaine (0.5 mg) device to the site planned for venipuncture, 1 to 3 minutes prior to needle insertion.

Jelly: Maximum dose: 30 mL (600 mg) in any 12-hour period:

Anesthesia of male urethra: 5 to 30 mL (100 to 600 mg)

Anesthesia of female urethra: 3 to 5 mL (60 to 100 mg)

Lotion: Apply a thin film to affected area 2 or 3 times daily.

Ointment: Apply as a single application not exceeding 5 g of ointment (equivalent to lidocaine base 250 mg); maximum: 20 g of ointment/day (equivalent to lidocaine base 1,000 mg/day).

Oral topical solution (2% viscous):

Anesthesia of the mouth: 15 mL swished in the mouth and spit out no more frequently than every 3 hours (maximum: 4.5 mg/kg [or 300 mg per dose]; 8 doses per 24-hour period)

Anesthesia of the pharynx: 15 mL gargled no more frequently than every 3 hours (maximum: 4.5 mg/kg [or 300 mg per dose]; 8 doses per 24-hour period); may be swallowed

Oral topical solution (4%): Note: For use in mucous membranes of oral and nasal cavities and proximal GI tract. Apply 1 to 5 mL (40 to 200 mg) to affected area (maximum dose: 4.5 mg/kg, not to exceed 300 mg per dose)

Oral topical endotracheal solution, metered-dose spray (10 mg/actuation) [Canadian product]:

Nasal: 20 to 60 mg (maximum dose: 500 mg for procedure 5 minutes)

Oropharyngeal: 20 to 200 mg (maximum dose: 500 mg for procedure 5 minutes)

Respiratory tract: 50 to 400 mg (maximum dose: 400 mg for procedure 5 minutes)

Trachea, larynx, bronchi: 50 to 200 mg (maximum dose: 200 mg for procedure 5 minutes)

Patch: Note: One ZTlido 1.8% patch provides equivalent lidocaine exposure to one Lidoderm 5% patch.

Lidoderm, ZTlido: Postherpetic neuralgia: Apply patch to most painful area. Up to 3 patches may be applied in a single application. Patch(es) may remain in place for up to 12 hours in any 24-hour period.

OTC 4%: Pain (localized): Apply patch to painful area. Patch may remain in place for up to 12 hours in any 24-hour period. No more than 1 patch should be used in a 24-hour period.

Topical solution (OTC 4% [products labeled for external use only]): Apply thin layer to affected area every 6 to 8 hours; maximum of 3 applications in 24 hours

Dosing: Geriatric

Refer to adult dosing. Administer reduced doses commensurate with age and physical status.

Dosing: Pediatric

Note: Smaller areas of treatment are recommended in younger or smaller patients (

Anesthetic: Topical: Dose varies with age, weight, and physical condition.

Lidovex (lidocaine 3.75%), Lidocaine 4.12%: Infants, Children, and Adolescents: Apply a thin film to affected area 2 to 3 times daily as needed; maximum dose: 4.5 mg/kg/dose; not to exceed 300 mg/dose

LMX 4 (lidocaine 4%, liposomal): Children >2 years and Adolescents: Apply a thin film to affected area up to 3 to 4 times daily as needed; maximum dose: 4.5 mg/kg/dose; not to exceed 300 mg/dose

Gel: Children ≥2 years and Adolescents: Apply to affected area up to 3 to 4 times daily as needed; maximum dose: 4.5 mg/kg/dose; not to exceed 300 mg/dose

Jelly: Children and Adolescents: Dose varies with age and weight; maximum dose: 4.5 mg/kg/dose; not to exceed 600 mg in a 12-hour period

Lotion: Children and Adolescents: Apply to affected area up to 2 to 3 times daily as needed; maximum dose: 4.5 mg/kg/dose; not to exceed 300 mg/dose

Ointment: Children and Adolescents: Apply to affected area; maximum dose: 4.5 mg/kg/dose; not to exceed 300 mg/dose

Patch: OTC 4%: Children ≥12 years and Adolescents: Apply patch to painful area. Patch may remain in place for up to 12 hours. No more than 1 patch should be used in a 24-hour period.

Minor dermal procedures (eg, peripheral IV cannulation, venipuncture, lumbar puncture, abscess drainage, joint aspiration); anesthetic: Limited data available:

Intradermal injection: Zingo: Venipuncture or peripheral IV catheter insertion: Children ≥3 years and Adolescents: Apply one intradermal lidocaine (0.5 mg) device to the site planned for venipuncture, administer 1 to 3 minutes prior to the IV needle insertion; perform procedure within 10 minutes of application

Topical: Cream LMX 4 (lidocaine 4%):

Children ≥4 years and Adolescents ≤17 years: Apply 1 to 2.5 g of cream to site 30 minutes prior to procedure (Eichenfield 2002; Fein 2012; Koh 2004; Luhmann 2004; Taddio 2005)

Note: For peripheral IV cannulation, some have recommended application to 6.25 cm 2 of skin (Sobanko 2012).

Oral inflammation or irritation: Topical: Note: Not approved for relief of teething pain and discomfort in infants and children; serious adverse (toxic) effects, including fatalities, have been reported; AAP, AAPD, and ISMP strongly discourage use (AAP 2011; AAPD 2012; ISMP 2014).

Oral solution (2% viscous): Dose should be adjusted according to patient's age, weight, and physical condition:

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

Topical solution (4%): Note: For use on mucous membranes of the oral and nasal cavities and proximal portions of the digestive tract; use lowest effective dose. Children and Adolescents: Do not exceed 4.5 mg/kg/dose; maximum dose: 300 mg/dose; applied with cotton applicator, cotton pack, or via spray; should not be swallowed

Topical endotracheal solution, metered-dose spray (10 mg/actuation) [Canadian product]: Children 2 to

Laryngotracheal: 3 mg/kg/dose

Nasal/oropharyngeal: 4 to 5 mg/kg/dose

Rectal pain, itching: Topical:

Cream: LMX 5 (lidocaine 5%): Children ≥12 years and Adolescents: Apply to affected area up to 6 times daily

Gel: Topicaine (lidocaine 5%): Children ≥12 years and Adolescents: Apply to affected area up to 6 times daily

Skin irritation: Topical: Cream: LMX 4 (lidocaine 4%): Children ≥2 years and Adolescents: Apply up to 3 to 4 times daily to intact skin

Administration

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. Do not eat or chew gum for 60 minutes following use.

Pharyngeal anesthesia: Patient should gargle and may swallow medication. 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).

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.

ZTlido: 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). May be used during moderate exercise (eg, biking for 30 minutes). Discard any used or unused patches by folding adhesive sides together and dispose of in trash away from children and pets. Throw away any patch that comes off and will not stick to skin; a new patch can be applied for a total duration of 12 hours of used and new patch together.

OTC 4%: 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.

Storage

All formulations: Store at room temperature; see product-specific labeling for any additional storage requirements. Store and dispose of products out of the reach of children and pets.

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

Adverse effects vary with formulation and extent of systemic absorption; children may be at increased risk.

Dermatologic: Erythema (intradermal powder: adults - 67%; children & adolescents - 53%)

Hematologic & oncologic: Petechia (intradermal powder: 44% to 46%)

Cardiovascular: Edema (intradermal powder: 4% to 8%)

Dermatologic: Pruritus (intradermal powder: 9%; also occurs with topical patch)

Gastrointestinal: Nausea (intradermal powder: 2%; also occurs with topical patch), vomiting

Frequency not defined:

Cardiovascular: Bradycardia, circulatory shock, flushing (topical patch), hypotension, shock

Central nervous system: Apprehension, central nervous system depression, confusion, disorientation (topical patch), dizziness, drowsiness, euphoria, excitement, headache (topical patch), hyperesthesia (topical patch), hypoesthesia (topical patch), localized warm feeling, loss of consciousness, metallic taste (topical patch), nervousness, numbness, pain (exacerbation; topical patch), paresthesia, seizure, sensation disorder (topical patch), sensation of cold, twitching

Dermatologic: Dermatitis, exfoliation of skin (topical patch), papule (topical patch), skin blister (topical patch), skin depigmentation (topical patch), skin edema (topical patch), skin erosion (topical patch), urticaria

Gastrointestinal: Dysgeusia (topical patch)

Hematologic & oncologic: Bruise (topical patch), methemoglobinemia

Hypersensitivity: Anaphylactoid shock, angioedema, hypersensitivity reaction

Local: Application site burning (topical patch), application site erythema (topical patch), application site vesicles (topical patch), local discoloration (topical patch), local irritation (topical patch)

Neuromuscular & skeletal: Asthenia, laryngospasm, tremor

Ophthalmic: Blurred vision, diplopia

Respiratory: Bronchospasm, dyspnea, respiratory depression

Warnings/Precautions

Concerns related to adverse effects:

Disease-related concerns:

Concurrent drug therapy issues:

Dosage form specific issues:

Special populations:

Other warnings/precautions:

Pregnancy

Pregnancy Risk Factor

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies using the systemic injection. Lidocaine and its metabolites cross the placenta and can be detected in the fetal circulation following injection (Cavalli 2004; Mitani 1987). The amount of lidocaine absorbed topically (and therefore available systemically to potentially reach the fetus) varies by dose administered, duration of exposure, and site of application. Cumulative exposure from all routes of administration should be considered.

Patient Education

What is this drug used for?

Frequently reported side effects of this drug

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Source: Wolters Kluwer Health. Last updated February 6, 2020.