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Lidocaine (Topical)

Pronunciation

Pronunciation

(LYE doe kane)

Index Terms

  • Lidocaine HCl
  • Lidocaine Hydrochloride
  • Lidocaine Patch
  • Lignocaine Hydrochloride
  • Viscous Lidocaine
  • Xylocaine Viscous

Dosage Forms

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]

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:

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)]

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)]

Lidotrans 5 Pak: 5% [contains polyethylene glycol]

LMX 4 Plus: 4% [contains benzyl alcohol]

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

Generic: 4%

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, 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)

Brand Names: U.S.

  • Anastia
  • AneCream [OTC]
  • AneCream5 [OTC]
  • Astero
  • CidalEaze
  • Eha
  • EnovaRX-Lidocaine HCl
  • Glydo
  • LC-4 Lidocaine [OTC]
  • LC-5 Lidocaine [OTC]
  • LDO Plus
  • Lido-K
  • Lidocaine PAK
  • Lidocin [DSC]
  • Lidoderm
  • Lidopin
  • LidoRx
  • Lidotral
  • Lidotrans 5 Pak
  • Lidovex
  • Lidovin
  • Lidozol
  • LMX 4 Plus [OTC]
  • LMX 4 [OTC]
  • LMX 5 [OTC]
  • LTA 360 Kit [DSC]
  • Numbonex
  • Predator [OTC]
  • Premium Lidocaine
  • Prozena [DSC]
  • Prozena [OTC] [DSC]
  • RectaSmoothe [OTC]
  • RectiCare [OTC]
  • Topicaine 5 [OTC]
  • Topicaine [OTC] [DSC]
  • Xolido XP [OTC]
  • Xolido [OTC]
  • Xryliderm
  • Xylocaine
  • Zingo

Pharmacologic Category

  • Analgesic, Topical
  • Local Anesthetic

Pharmacology

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)

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)

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

60% to 80%

Special Populations: Renal Function Impairment

Accumulation of metabolites may occur.

Use: Labeled Indications

Intradermal injection (Zingo): Topical local analgesia prior to venipuncture or peripheral intravenous (IV) cannulation in children ≥3 years; 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): Relief of pain associated with postherpetic neuralgia

Patch (LidoPatch): Temporary relief of 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).

Dosing: Adult

Anesthesia, topical:

Cream:

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.

Topical solution: Apply 1 to 5 mL (40 to 200 mg) to affected area

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 <1 minute or 600 mg for procedure >5 minutes)

Oropharyngeal: 20 to 200 mg (maximum dose: 500 mg for procedure <1 minute or 600 mg for procedure >5 minutes)

Respiratory tract: 50 to 400 mg (maximum dose: 400 mg for procedure <1 minute or 600 mg for procedure >5 minutes)

Trachea, larynx, bronchi: 50 to 200 mg (maximum dose: 200 mg for procedure <1 minute or 400 mg for procedure >5 minutes)

Patch:

Lidoderm: 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.

LidoPatch: 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.

Dosing: Geriatric

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

Dosing: Pediatric

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)

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment

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

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. 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.

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

Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

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. Monitor therapy

Beta-Blockers: May increase the serum concentration of Lidocaine (Topical). Monitor therapy

CloZAPine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP1A2 Inhibitors (Moderate): May decrease the metabolism of CYP1A2 Substrates. Monitor therapy

CYP1A2 Inhibitors (Strong): May decrease the metabolism of CYP1A2 Substrates. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Consider therapy modification

Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May increase the serum concentration of CYP1A2 Substrates. 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

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. 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. 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. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when nitric oxide is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine. Monitor therapy

Obeticholic Acid: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Peginterferon Alfa-2b: May increase the serum concentration of CYP1A2 Substrates. 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. 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. 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

Tetracaine (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use cannot be avoided, initiate tizanidine at an adult dose of 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification

Vemurafenib: May increase the serum concentration of CYP1A2 Substrates. Management: Consider alternatives to such combinations whenever possible, particularly if the CYP1A2 substrate has a relatively narrow therapeutic index. Consider therapy modification

Adverse Reactions

Frequency not always defined. Note: Adverse effects vary with formulation and extent of systemic absorption; children may be at increased risk.

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

Central nervous system: Apprehension, confusion, dizziness, drowsiness, paresthesia

Dermatologic: Erythema (adults, intradermal powder: 67%; children 3 to 18 years, intradermal powder: 53%), petechia (intradermal powder: 44% to 46%), pruritus (intradermal powder: 9%), dermatitis, exacerbation of pain (topical patch), skin depigmentation (topical patch), skin edema (topical patch), skin rash, urticaria

Gastrointestinal: Nausea (intradermal powder: 2%), vomiting (intradermal powder: 1%)

Hematologic and oncologic: Bruise (topical patch), methemoglobinemia

Hypersensitivity: Anaphylactoid reaction, angioedema, hypersensitivity reaction

Local: Local irritation (topical patch)

Neuromuscular & skeletal: Weakness

ALERT: U.S. 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.

Warnings/Precautions

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.

Pregnancy Risk Factor

B

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

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience redness, edema, or skin discoloration. Have patient report immediately to prescriber signs of infection, difficulty breathing, slow breathing, shallow breathing, shortness of breath, severe application site irritation, burning or numbness feeling, abnormal heartbeat, rectal bleeding, rectal pain, seizures, lightheadedness, fatigue, blurred vision, confusion, or vision changes (HCAHPS).

• 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.

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