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.
Anesthesia, topical: Note: Not all available products may be represented in dosing; also refer to manufacturer's labeling.
Cream:
Aspercreme: Pain: Apply a thin layer to affected area every 6 to 8 hours, not to exceed 3 applications in a 24-hour period.
Blue Tube, LMX 4: Skin irritation: Apply up to 3 to 4 times daily to intact skin.
Lidotran 3.88%, Lidocaine 4.12%, Lidovex 3.75%: Skin irritation: Apply a thin film to affected area 2 to 3 times daily as needed.
Lipocaine 5, LMX 5: Relief of anorectal pain and itching: Apply to affected area up to 6 times daily.
Gel: Usual dosage: Apply to affected area ≤4 times daily as needed (maximum dose: 4.5 mg/kg, not to exceed 300 mg).
Product-specific dosing:
Astero 4%; Apply 1 to 4 pumps to affected area; each pump provides 0.25 mL (lidocaine 10 mg) and covers a 2 × 2 inch area. Maximum single application: 4 pumps (lidocaine 40 mg); maximum daily application: 12 pumps/day (lidocaine 120 mg/day).
LidoRx 3%: Apply 1 to 4 pumps to affected area 3 to 4 times daily; each pump provides 0.25 mL (lidocaine 7.5 mg) and covers a 2 × 2 inch area. Maximum single application: 4 pumps (lidocaine 30 mg); maximum daily application: 16 pumps/day (lidocaine 120 mg/day).
Topicaine 5%: Apply to affected area up to 6 times daily.
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).
Lubricant, endotracheal intubation (Glydo): Apply moderate amount to external surface of the endotracheal tube prior to insertion.
Lotion: Apply a thin film to affected area 2 to 4 times daily; product-specific application frequency may vary; also refer to manufacturer's labeling.
Ointment:
Intubation (5% ointment only): Apply 5 g of ointment (equivalent to lidocaine base 250 mg [~6 inches of ointment]) in a single application to the tube prior to intubation; maximum: 20 g of ointment/day (equivalent to lidocaine base 1,000 mg/day).
Pain (eg, skin irritation, sunburn): Apply to affected area 3 to 4 times daily, not to exceed 5 g of ointment (equivalent to lidocaine base 250 mg) in a single application; 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:
Pain (localized):
3.5% products: 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.
4% products: Apply patch to painful area. Note: The manufacturer’s recommendations for the number of patches that can be applied within a 24-hour period varies from 1 to 4 times daily and the duration of application varies from 8 to 24 hours; refer to the manufacturer’s labeling for product-specific recommendations.
Postherpetic neuralgia (1.8% [ZTlido], 5% products): Note: One ZTlido 1.8% patch provides equivalent lidocaine exposure to one 5% patch: 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.
Rectal suppository: Note: Lidocaine suppositories have been discontinued in the United States for >1 year. Insert 1 suppository (50 mg) rectally; maximum of 4 suppositories in 24 hours.
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.
Topical spray (OTC 4% [products labeled for external use only]): Apply to affected area up to 3 to 4 times daily; maximum of 4 applications in 24 hours.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
The renal dosing recommendations are based upon the best available evidence and clinical expertise. Senior Editorial Team: Bruce Mueller, PharmD, FCCP, FASN, FNKF; Jason A. Roberts, PhD, BPharm (Hons), B App Sc, FSHP, FISAC; Michael Heung, MD, MS.
Altered kidney function: Topical: No dosage adjustment necessary (limited absorption, relatively low urinary excretion) (Ref).
Hemodialysis, intermittent (thrice weekly): Topical: No dosage adjustment necessary (Ref).
Peritoneal dialysis: Topical: No dosage adjustment necessary (Ref).
CRRT: Topical: No dosage adjustment necessary (Ref).
PIRRT (eg, sustained, low-efficiency diafiltration): Topical: No dosage adjustment necessary (Ref).
There are no dosage adjustments provided in the manufacturer’s labeling; use caution in patients with severe hepatic disease.
Refer to adult dosing. Administer reduced doses commensurate with age and physical status.
(For additional information see "Lidocaine (topical): Pediatric drug information")
Dosage guidance:
Dosing: Smaller areas of treatment are recommended in younger or smaller patients (<12 months or <10 kg) or those with impaired elimination (Ref); use lowest effective dose.
Anesthetic: Topical: Dose varies with age, weight, and physical condition.
Cream:
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%): 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%):
Infants and Children <4 years: Apply 1 g of cream to site 30 minutes prior to procedure (Ref)
Children ≥4 years and Adolescents ≤17 years: Apply 1 to 2.5 g of cream to site 30 minutes prior to procedure (Ref)
Note: For peripheral IV cannulation, some have recommended application to 6.25 cm2 of skin (Ref).
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 (Ref).
Oral solution (2% viscous): Dose should be adjusted according to patient's age, weight, and physical condition:
Infants and Children <3 years: 24 mg/dose (1.2 mL) applied to area with a cotton-tipped applicator no more frequently than every 3 hours; maximum dose: 4 doses per 12-hour period; should not be swallowed
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 <12 years: Topical: Dose varies with age, weight, and application site.
Maximum dose:
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
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling. Use caution in patients with severe renal impairment; accumulation of active metabolites may occur with long-term treatment.
There are no dosage adjustments provided in the manufacturer's labeling; use caution in patients with severe hepatic disease.
Reports of systemic hypersensitivity reactions following administration of topical lidocaine to mucous membranes, generally in the context of a procedure or nebulized lidocaine where systemic absorption is more likely, are rare (Ref). These reactions may also result from excipients in lidocaine formulations (Ref). Patients allergic to para-aminobenzoic acid (PABA) derivatives (eg, procaine, tetracaine, benzocaine) have not shown cross sensitivity to lidocaine.
Contact dermatitis, a localized delayed Type IV hypersensitivity reaction, has also been reported with the use of lidocaine applied to the skin (Ref). These reactions may also result from excipients in lidocaine formulations (Ref). Type I hypersensitivity reactions are not of concern solely based on the presence of allergic contact dermatitis (Ref). Systemic toxicity has also been reported rarely with topical application (Ref).
Mechanism: Non–dose-related; immunologic. Signs and symptoms of immediate hypersensitivity reactions (eg, anaphylaxis) may be mediated by IgE or non-IgE mechanisms (ie, direct stimulation of mast cell and/or basophils, complement activation) (Ref). Allergic contact dermatitis is a delayed, T-lymphocyte–mediated reaction (Ref).
Onset: Immediate hypersensitivity reactions: Rapid; usually occurs within 1 hour of administration; but may occur up to 6 hours after exposure (Ref). Allergic contact dermatitis generally occurs within 48 hours after application (Ref).
Risk factors:
• Cross-reactivity with other amide anesthetics, including bupivacaine, mepivacaine, and prilocaine, has been reported (Ref).
Topical lidocaine administration to mucous membranes, generally in the context of a procedure or nebulized lidocaine where systemic absorption is more likely, is associated with infrequent but potentially life-threatening local anesthetic systemic toxicity (LAST), a syndrome of CNS excitation and/or depression followed by cardiotoxicity, in some cases (Ref). CNS effects include blurred vision, confusion, dizziness, drowsiness, respiratory depression, seizures, tremors, coma, and respiratory arrest (Ref). Drowsiness may be an early sign of high lidocaine serum concentrations (Ref). Cardiovascular effects include bradycardia, hypotension, cardiovascular collapse, and cardiac arrest (Ref). CNS effects typically precede cardiotoxicity. Symptom severity increases with increasing lidocaine serum concentrations (Ref). Symptoms of LAST may be reversible with prompt treatment (Ref).
Mechanism: Dose-related (Ref); blockage of voltage-gated sodium channels in the CNS disrupts depolarization of inhibitory neurons, leading to neural excitation (Ref). With increasing lidocaine plasma concentrations, CNS depression occurs. Sodium channel blockade in myocardial tissue results in action potential inhibition, decreased contractility, conduction disturbance, and/or arrhythmia (Ref).
Onset: Rapid; typically occurs within minutes of exposure (Ref). Severe symptoms may appear within hours of initial symptoms (Ref).
Risk factors:
• Lidocaine blood concentration >5 mcg/mL
• Application to mucous membranes in high doses (preceding airway instrumentation for awake intubation) (Ref)
• Intentional or unintentional overdose (Ref)
• Extremes of ages (<16 or >60 years of age) (Ref)
• Low muscle mass (neonates, infants, debilitated older patients) (Ref)
• Females (Ref)
• Pregnancy (Ref)
• Chronic malnutrition (Ref)
• Organ dysfunction (eg, cardiac, CNS, hepatic, kidney) (Ref)
• Acidosis (Ref)
• Hypoxia (Ref)
Topical lidocaine administration to mucous membranes, generally in the context of a procedure or nebulized lidocaine where systemic absorption is more likely, is rarely associated with methemoglobinemia, a serious and possibly life-threatening condition that is reversible with prompt treatment. Symptoms of methemoglobinemia include cyanosis (pale, gray, or blue skin), headache, fatigue, shortness of breath, and tachycardia. Severity of symptoms varies based on the level of methemoglobin in the blood (Ref).
Mechanism: Non–dose-related; idiosyncratic. Topical lidocaine exposure via mucous membrane(s) leads to acceleration of heme iron oxidation and conversion from the ferrous to ferric state, producing methemoglobin (Ref). Blood methemoglobin levels increase above the compensatory ability of the body, resulting in clinically significant methemoglobinemia (Ref). Because methemoglobin transports and releases less oxygen into peripheral tissues than normal hemoglobin, hypoxia ensues.
Onset: Rapid; typically occurs within minutes to hours of exposure (Ref)
Risk factors:
• Glucose-6-phosphate dehydrogenase (G6PD) deficiency
• Congenital or idiopathic methemoglobinemia
• Cardiac or pulmonary compromise (acute and/or chronic)
• Age <6 months
• Concurrent exposure to oxidizing agents or their metabolites (eg, dapsone, nitroglycerin, sulfamethoxazole) (Ref)
• Concurrent exposure to other local anesthetics (eg, benzocaine, prilocaine)
The following adverse drug reactions are derived from product labeling unless otherwise specified. Adverse effects may vary with formulation and extent of systemic absorption; children may be at increased risk.
Frequency not defined:
Cardiovascular: Bradycardia, circulatory shock, flushing, hypotension, shock
Dermatologic: Exfoliation of skin, papule of skin, skin blister, skin depigmentation, skin erosion, urticaria
Gastrointestinal: Dysgeusia, metallic taste, nausea, vomiting
Hematologic & oncologic: Bruise
Hypersensitivity: Angioedema, hypersensitivity reaction, nonimmune anaphylaxis
Local: Application-site burning, application-site dermatitis, application-site edema, application-site erythema, application-site irritation, application-site pruritus, application-site purpuric or petechial reaction, application-site scaling, application-site vesicles, local skin discoloration, localized warm feeling
Nervous system: Apprehension, asthenia, central nervous system depression, confusion, disorientation, dizziness, drowsiness, euphoria, excitement, headache, hyperesthesia, hypoesthesia, loss of consciousness, nervousness, numbness, paresthesia, seizure, sensation disorder (including sensation of cold), tremor, twitching
Neuromuscular & skeletal: Laryngospasm
Ophthalmic: Blurred vision, diplopia
Otic: Tinnitus
Respiratory: Bronchospasm, dyspnea, respiratory depression
Postmarketing:
Dermatologic: Contact dermatitis (Montanez-Wiscovich 2018)
Hematologic & oncologic: Methemoglobinemia (Gay 2016)
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, LidoRx, and Lidovex); tuberculous or fungal lesions of skin vaccinia, varicella and acute herpes simplex (3.88% and 4.12% cream).
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.
• Local effects: Irritation, sensitivity and/or infection may occur at the site of application; discontinue use and institute appropriate therapy if local effects occur. Mild and transient application site reactions may occur during or immediately after treatment with patch; spontaneously resolves within a few minutes to hours; may include blisters, bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechial, pruritus, vesicles, or the area may be the locus of abnormal sensation.
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.
• 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.
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/viscous: 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.
• Pediatric: Use with caution; children should be given reduced doses commensurate with their age and physical status.
Other warnings/precautions:
• Self-medication (OTC use): When used for self-medication, discontinue use and notify health care provider if condition worsens, symptoms persist for >7 days, or symptoms clear up but reoccur within a few days.
• 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 heartbeats, 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.
In infants and children, seizures (some fatal) have been reported following topical lidocaine ingestion at serum concentrations within the therapeutic range of 1 to 5 mcg/mL (Curtis 2009); others have reported toxic effects with excessive doses or frequent application of topical oral lidocaine solution that resulted in high plasma concentrations. Multiple cases of seizures, including fatalities, have occurred in pediatric patients using viscous lidocaine for oral discomfort (eg, teething pain, herpetic gingivostomatitis) (Curtis 2009; Giard 1983; Gonzalez del Rey 1994; Hess 1988; Mofenson 1983; Puczynski 1985; Rothstein 1982; Smith 1992). Lidocaine oral solution is not approved for treatment of teething pain or discomfort; off-label use is strongly discouraged and should be avoided. When used for oral irritation, the solution should not be swallowed, but should be applied topically with a cotton swab to individual lesions or the excess should be expectorated (swish and spit). Toxicology data suggests that in infants and children<6 years, ingestion of as little as 5 mL of lidocaine may result in serious toxicity and emergency care should be sought (Curtis 2009). Additionally, the FDA recommends against using topical OTC medications for teething pain as some products may cause harm; the use of OTC topical anesthetics (eg, benzocaine) for teething pain is also discouraged by AAP, and The American Academy of Pediatric Dentistry (AAP 2011; AAPD 2012). The AAP recommends managing teething pain with a chilled (not frozen) teething ring or gently rubbing/massaging with the caregiver's finger.
Topical patches (both used and unused) may cause toxicities in children; used patches still contain large amounts of lidocaine; store and dispose patches out of the reach of children; efficacy of patches in pediatric patients has not been evaluated due to safety concerns.
Some dosage forms may contain propylene glycol; in neonates large amounts of propylene glycol delivered orally, intravenously (eg, >3,000 mg/day), or topically have been associated with potentially fatal toxicities which can include metabolic acidosis, seizures, renal failure, and CNS depression; toxicities have also been reported in children and adults including hyperosmolality, lactic acidosis, seizures, and respiratory depression; use caution (AAP 1997; Shehab 2009).
Lidocaine suppositories have been discontinued in the United States for >1 year.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Aerosol, External:
Alocane Emergency Burn Max Str: 4% (104 mL)
GoodSense Burn Relief: 0.5% (127 g) [contains disodium edta, methylparaben, propylene glycol, propylparaben, trolamine (triethanolamine)]
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) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
Asperflex Lidocaine: 4% (5 g, 15 g, 30 g) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
Blue Tube/ Aloe: 4% (30 g [DSC]) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
Bruselix: 3.88% (57 g) [contains cetearyl alcohol, propylene glycol]
Lidotral: 3.88% (85 g) [contains cetearyl alcohol, methylparaben, propylene glycol, propylparaben]
Lidotran: 3.88% (85 g) [contains cetearyl alcohol, methylparaben, propylene glycol, propylparaben]
Lidovex: 3.75% (60 g [DSC]) [contains cetyl alcohol, propylene glycol, trolamine (triethanolamine)]
Lipocaine 5: 5% (30 g, 113 g) [fragrance free, mineral oil free, no artificial color(s), paraben free; contains cetyl alcohol]
LMX 4: 4% (5 g, 15 g, 30 g) [contains benzyl alcohol]
LMX 5: 5% (15 g, 30 g) [contains benzyl alcohol]
NumbCream: 5% (38 g) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
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)]
RectoProtect: 5% (30 g) [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
Generic: 3% (28.35 g, 85 g [DSC]); 4% (5 g, 15 g, 28 g, 28.35 g, 30 g, 120 g); 5% (14.17 g, 15 g, 28.35 g, 30 g)
Cream, External, as hydrochloride:
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]
Lydexa: 4.12% (28.3 g, 85 g) [contains cetyl alcohol, methylparaben, propylene glycol, propylparaben]
NeuroMed7: 4% (63 g [DSC]) [contains propylene glycol, trolamine (triethanolamine)]
Pain Relieving: 4% (15 g [DSC]) [contains cetearyl alcohol, disodium edta]
Predator: 4% (63 g [DSC]) [contains propylene glycol, trolamine (triethanolamine)]
True Lido: 4% (60 g) [contains cetyl alcohol, trolamine (triethanolamine)]
Xolido: 2% (118 mL [DSC]) [contains methylisothiazolinone]
Xolido XP: 4% (118 mL [DSC]) [contains methylisothiazolinone]
Generic: 3% (28.3 g, 28.35 g, 85 g); 4% (30 g [DSC], 120 g); 4.12% (28.3 g, 85 g)
Gel, External:
DermacinRx Lidogel: 2.8% (100 g) [contains methylparaben, propylene glycol, propylparaben]
Lidogel: 2.8% (100 g [DSC]) [contains methylparaben, propylene glycol, propylparaben]
Lidorex: 2.8% (100 g) [contains methylparaben, propylene glycol, propylparaben]
Lubricaine: 4% (113 g); 5% (113 g) [estrogen free, fragrance free, no artificial color(s), no artificial flavor(s), paraben free, soy free, sugar free; contains benzyl alcohol]
Topicaine: 4% (10 g, 30 g, 113 g) [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)
Alocane Max: 4% (75 mL)
Alocane Plus: 4% (3.4 g [DSC], 3.55 mL, 59 mL, 946 mL)
Astero: 4% (90 mL)
Bruselix: 3.88% (57 g) [contains propylene glycol, sodium benzoate]
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)]
Lidotral: 3.88% (85 g) [contains cetearyl alcohol, disodium edta]
Lidotrex (Aloe Vera): 2% (28.33 g [DSC]) [contains trolamine (triethanolamine)]
Proxivol: 2% (28.33 g) [contains benzethonium chloride, trolamine (triethanolamine)]
Sun Burnt Plus: 4% (118 mL) [dye free, fragrance free, paraben free, phthalate free, sulfate free]
7T Lido: 2% (85 g [DSC]) [contains trolamine (triethanolamine)]
XeroBurn: 2% (3.5 g) [contains methylparaben, propylene glycol, propylparaben, trolamine (triethanolamine)]
Generic: 2% (5 mL [DSC], 30 mL [DSC])
Jet-injector, Intradermal, as hydrochloride [preservative free]:
Zingo: 0.5 mg (1 ea [DSC])
Generic: 0.5 mg (1 ea [DSC])
Kit, External:
AneCream: 4% [contains benzyl alcohol, polysorbate 80, propylene glycol, trolamine (triethanolamine)]
LidoHeal-90: 4% [DSC] [contains cetostearyl alcohol, edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
LidoLite: 5%
Lidopac: 5% [DSC] [contains polyethylene glycol (macrogol)]
LidoPure Patch: 5% [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Lidosol: 5%
Lidosol-50: 5% [contains polyethylene glycol (macrogol)]
Lidovix L: 5% [contains polyethylene glycol (macrogol)]
LMX 4 Plus: 4% [contains benzyl alcohol]
Moxicaine: 5% [DSC] [contains polyethylene glycol (macrogol)]
Xyliderm: 5% [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
ZiloVal: 5% [DSC]
Zylotrol-L: 4% [DSC] [contains polysorbate 80]
Generic: 4%
Kit, External, as hydrochloride:
Venipuncture Px1 Phlebotomy: 2% [latex free; contains methylparaben, propylparaben]
Liquid, External:
Theraworx Diabet Pain Roll-On: 4% (74 mL) [contains benzyl alcohol, edetate (edta) sodium (tetrasodium), sodium benzoate]
Liquid, External, as hydrochloride:
Alocane First Aid Spray: 4% (104 mL) [alcohol free]
Alocane Max Emer Burn w/ Anti: 4% (104 mL)
Bactine Max: 4% (118 mL) [contains edetate (edta) disodium, propylene glycol]
Bactine Max Spray: 4% (148 mL) [contains edetate (edta) disodium, propylene glycol]
LevigoSP: 2.5% (150 mL) [paraben free; contains propylene glycol]
Lotion, External:
Gen7T: 3.5% (120 g [DSC]) [contains edetate (edta) disodium, trolamine (triethanolamine)]
RadiaGuard Advanced: 1% (113 g) [metallic free; contains almond oil, cetyl alcohol, polysorbate 80, trolamine (triethanolamine)]
Lotion, External, as hydrochloride:
Eha: 4% (88 mL) [contains methylisothiazolinone]
Lido-Sorb: 3% (177 mL) [contains cetyl alcohol, edetate (edta) disodium, methylparaben, propylparaben]
Lidozion: 3% (177 mL [DSC]) [contains cetyl alcohol, edetate (edta) disodium, methylparaben, propylparaben]
Zionodil: 3% (177 mL) [contains cetyl alcohol, edetate (edta) disodium, methylparaben, propylparaben]
Zionodil 100: 3% (177 mL) [contains cetyl alcohol, propylene glycol, trolamine (triethanolamine)]
Generic: 3% (177 mL)
Ointment, External:
Premium Lidocaine: 5% (50 g)
Generic: 4% (50 g); 5% (30 g, 35.44 g, 50 g, 2500 g [DSC])
Ointment, External, as hydrochloride:
Asperflex Lidocaine: 4% (100 g) [contains polysorbate 80]
Pad, External:
Alocane Emergency Burn Max Str: 4% (1 ea)
Pad, External, as hydrochloride:
Alocane Max Emer Burn w/ Anti: 4% (10 ea)
Patch, External:
Asperflex Max St: 4% (6 ea) [odor free]
Asperflex Pain Relieving: 4% (5 ea) [fragrance free; contains polysorbate 80, propylene glycol]
First Care Pain Relief: 4% (5 ea) [odor free, paraben free]
First Care Pain Relief: 4% (5 ea [DSC]) [odor free, paraben free; contains propylene glycol]
FT Pain Relief Max Strength: 4% (6 ea) [contains methylparaben, polysorbate 80, propylparaben]
Gen7T: 3.5% (10 ea [DSC], 15 ea [DSC]) [contains propylene glycol]
HealthWise Pain Relief: 4% (15 ea) [odor free; contains methylparaben, polysorbate 80, propylene glycol, propylparaben]
Lido King: 4% (5 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Lidocaine Max St 24 Hours: 4% (15 ea) [odor free]
Lidocaine Pain Relief: 4% (5 ea, 30 ea) [contains methylparaben, polysorbate 80, propylene glycol, propylparaben]
Lidocaine Pain Relief Max St: 4% (1 ea, 5 ea) [odorless; contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Lidocan: 5% (1 ea, 30 ea) [contains disodium edta, methylparaben, propylene glycol, propylparaben]
Lidocan: 5% (1 ea, 30 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Lidocanna: 4% (10 ea) [contains propyl hydroxybenzoate, propylene glycol]
Lidocore: 4% (1 ea) [contains edetate (edta) disodium, methylparaben, polysorbate 80, propylene glycol, propylparaben]
Lidocore: 4% (10 ea) [contains polysorbate 80]
Lidoderm: 5% (1 ea, 30 ea) [contains disodium edta, methylparaben, propylene glycol, propylparaben]
Lidoderm: 5% (1 ea, 30 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
LidoFore Flexipatch: 4% (5 ea [DSC]) [contains polysorbate 80]
Lidotral 1: 4.88% (30 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Pain Relief Maximum Strength: 4% (5 ea) [contains methylparaben, polysorbate 80, propylparaben]
Pharmacist Choice Lidocaine: 4% (1 ea, 5 ea, 30 ea) [fragrance free; contains edetate (edta) disodium, methylparaben, polysorbate 80, propylene glycol, propylparaben]
Pharmacist Choice Pain Relief: 4% (1 ea, 5 ea, 30 ea) [fragrance free; contains polysorbate 80, propylene glycol]
Re-Lieved Maximum Strength: 4% (20 ea [DSC]) [aluminum free, odor free]
Re-Lieved Maximum Strength: 4% (1 ea, 6 ea [DSC], 20 ea) [odor free]
Salonpas Pain Relieving: 4% (6 ea, 15 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
Salonpas Pain Relieving: 4% (7 ea) [contains propylene glycol]
TheraCare Pain Relief: 4% (5 ea) [odor free; contains methylparaben, polysorbate 80, propylene glycol, propylparaben]
Tridacaine: 5% (1 ea, 15 ea) [contains edetate (edta) disodium, methylparaben, propylene glycol, propylparaben]
ZTlido: 1.8% (1 ea, 30 ea)
Generic: 3.5% (5 ea [DSC]); 4% (10 ea, 15 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:
Medi-First Burn Spray: 2% (59.1 mL) [contains methylparaben, propylene glycol, propylparaben]
Solution, External, as hydrochloride:
Generic: 4% (50 mL)
Solution, Mouth/Throat, as hydrochloride:
Generic: 2% (15 mL, 100 mL)
Solution, Mouth/Throat, as hydrochloride [preservative free]:
Generic: 4% (4 mL)
Suppository, Rectal:
Generic: 50 mg (24 ea [DSC])
May be product dependent
Aerosol (Alocane Emergency Burn Max Str External)
4% (per mL): $0.13
Cream (AneCream External)
4% (per gram): $1.28
Cream (AneCream5 External)
5% (per gram): $1.60
Cream (Asperflex Lidocaine External)
4% (per gram): $0.59
Cream (Bruselix External)
3.88% (per gram): $17.46
Cream (Lidocaine (Anorectal) External)
5% (per gram): $0.52 - $1.97
Cream (Lidocaine External)
3% (per gram): $1.60
4% (per gram): $0.74 - $2.07
Cream (Lidocaine HCl External)
3% (per gram): $1.44 - $2.06
4% (per gram): $3.70
4.12% (per gram): $23.32
Cream (Lidotral External)
3.88% (per gram): $17.63
Cream (Lidotran External)
3.88% (per gram): $17.63
Cream (Lipocaine 5 External)
5% (per gram): $0.72
Cream (LMX 4 External)
4% (per gram): $1.68
Cream (LMX 5 External)
5% (per gram): $2.42
Cream (Lydexa External)
4.12% (per gram): $53.00
Cream (RectaSmoothe External)
5% (per gram): $0.64
Cream (RectiCare External)
5% (per gram): $1.23
Cream (RectoProtect External)
5% (per gram): $0.48
Gel (Alocane Emergency Burn Max Str External)
4% (per mL): $0.18
Gel (Alocane Max External)
4-0.13% (per mL): $0.18
Gel (Alocane Plus External)
4-0.13% (per mL): $0.46
Gel (Astero External)
4% (per mL): $11.53
Gel (Bruselix External)
3.88% (per gram): $17.46
Gel (DermacinRx Lidogel External)
2.8% (per gram): $18.95
Gel (LDO Plus External)
4% (per mL): $13.29
Gel (LidoDose External)
3% (per mL): $3.50
Gel (LidoDose Pediatric Bulk Pack External)
3% (per mL): $3.50
Gel (Lidorex External)
2.8% (per gram): $18.95
Gel (Lidotral External)
3.88% (per gram): $11.71
Gel (Lubricaine External)
4% (per gram): $0.30
5% (per gram): $0.30
Gel (Proxivol External)
2% (per gram): $34.87
Gel (Sun Burnt Plus External)
4% (per mL): $0.11
Gel (Topicaine 5 External)
5% (per gram): $0.65
Gel (Topicaine External)
4% (per gram): $1.05
Gel (XeroBurn External)
2% (per gram): $0.04
Kit (AneCream External)
4% (per each): $24.00
Kit (Lidocaine-Transparent Dressing External)
4% (per each): $59.00
Kit (LidoPure Patch External)
5% (per each): $23.44
Kit (LMX 4 Plus External)
4% (per each): $48.07
Kit (Venipuncture Px1 Phlebotomy External)
2% (per each): $981.00
Kit (Xyliderm External)
5% (per each): $3,200.00
Liquid (Alocane First Aid Spray External)
4-0.13% (per mL): $0.13
Liquid (Alocane Max Emer Burn w/ Anti External)
4-0.13% (per mL): $0.13
Liquid (Bactine Max External)
4-0.13% (per mL): $0.04
Liquid (Bactine Max Spray External)
4-0.13% (per mL): $0.04
Liquid (Dologesic Pain Relief Roll-On External)
4% (per mL): $0.13
Lotion (Lido-Sorb External)
3% (per mL): $13.87
Lotion (Lidocaine HCl External)
3% (per mL): $14.10
Ointment (Asperflex Lidocaine External)
4% (per gram): $0.07
Ointment (Lidocaine External)
4% (per gram): $6.00
5% (per gram): $7.50 - $13.00
Pads (Alocane Emergency Burn Max Str External)
4% (per each): $1.31
Pads (Alocane Max Emer Burn w/ Anti External)
4-0.13% (per each): $1.31
Patch (Asperflex Pain Relieving External)
4% (per each): $1.22
Patch (First Care Pain Relief External)
4% (per each): $46.00
Patch (Lido King External)
4% (per each): $1.18
Patch (Lidocaine External)
4% (per each): $46.00 - $49.50
5% (per each): $3.42 - $49.80
Patch (Lidocan External)
5% (per each): $33.17
Patch (Lidoderm External)
5% (per each): $31.81
Patch (Pharmacist Choice Lidocaine External)
4% (per each): $1.50
Patch (Pharmacist Choice Pain Relief External)
4% (per each): $1.50
Patch (Re-Lieved Maximum Strength External)
4% (per each): $8.63
Patch (Salonpas Pain Relieving External)
4% (per each): $1.35
Patch (ZTlido External)
1.8% (per each): $14.16
Prefilled Syringe (Glydo External)
2% (per mL): $1.19
Prefilled Syringe (Lidocaine HCl Urethral/Mucosal External)
2% (per mL): $1.38 - $1.44
Solution (Lidocaine HCl External)
4% (per mL): $0.64 - $1.33
Solution (Lidocaine HCl Mouth/Throat)
4% (per mL): $9.06
Solution (Lidocaine Viscous HCl Mouth/Throat)
2% (per mL): $0.13 - $1.18
Solution (Medi-First Burn Spray External)
2% (per mL): $0.05
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Gel, External, as hydrochloride:
Xylocaine: 2% (30 mL) [contains methylparaben, propylparaben]
Ointment, External:
Lidodan: 5% (15 g, 30 g, 35 g)
Xylocaine: 5% (35 g) [contains polyethylene glycol (macrogol), propylene glycol]
Prefilled Syringe, External, as hydrochloride:
Jelido: 2% (6 mL, 11 mL)
Xylocaine: 2% (10 mL)
Generic: 2% (1 ea)
Solution, Intratracheal, as hydrochloride:
Xylocaine Spray: 10 mg/actuation (50 mL) [contains alcohol, usp, menthol, polyethylene glycol (macrogol), saccharin]
Generic: 10 mcg/actuation (30 mL, 60 mL)
Topical:
Cream, gel, lotion: For external use only; avoid contact with eyes. Also refer to manufacturer's labeling for additional product-specific application instructions.
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.
Jelly:
Urethral anesthesia: Anesthesia occurs within several minutes (full anesthetic effect occurs in 5 to 10 minutes after installation).
Lubricant for endotracheal intubation (Glydo): Avoid introducing jelly into lumen of the tube. Do not use to lubricate endotracheal stylets. Avoid use of endotracheal tubes with dried jelly on the external surface for lack of lubricating effect.
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. Also refer to manufacturer's labeling for additional product-specific application instructions.
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).
Patch: Note: In general, the following instructions are considered applicable to all transdermal products; also refer to manufacturer's labeling for additional product-specific application instructions.
Apply to most painful area of skin immediately after removal from protective envelope. Do not apply to nonintact skin. Some products may be cut to appropriate size (refer to manufacturer's labeling for details). Clothing may be worn over application area. Remove immediately if irritation or a burning sensation occurs. Wash hands after application. Contact with water (eg, bathing, swimming, showering) recommendations vary by product; refer to manufacturer's labeling for details. Avoid exposing application site to external heat sources (eg, heating pad, electric blanket, heat lamp, hot tub). After removal from skin, fold used patch so the adhesive side sticks to itself and dispose of in trash away from children and pets.
Spray: For external use only; avoid contact with eyes. Avoid large quantities of spray, particularly on raw or blistered areas. Shake well. When applying to the face, spray on palm or hand first, then gently apply to face.
Rectal:
Rectal suppository: Remove wrapper; insert suppository into the rectum.
Topical:
Cream, gel: Apply to affected area.
LMX-4: Minor dermal procedure (peripheral IV cannulation, venipuncture): Infants and Children: Apply to skin at least 30 minutes before procedure; in most trials, occlusion of the application site was used (Ref) while another trial showed that occlusion was not required (Ref); however, occlusion of the site may be helpful in active infants and children to hold cream in place
Intradermal injection device (eg, Zingo): 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 peripheral IV cannulation; 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 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 solution (2% viscous): Do not eat or chew gum for 60 minutes following use.
Mouth irritation or inflammation: Have patient swish medication around mouth and then spit it out. In children <3 years, apply small amount to affected area with cotton-tipped applicator (do not use to relieve teething pain).
Pharyngeal anesthesia: Patient should gargle and may swallow medication. In children <3 years, apply to affected area with cotton-tipped applicator.
Rectal gel: Children ≥12 years and Adolescents: If possible, clean affected area with mild soap and water and blot dry prior to application.
Topical patch:
OTC 4%: Children ≥12 years and Adolescents: 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.
Topical oral endotracheal solution, metered-dose spray (10 mg/actuation) [Canadian product]: Attach nozzle and prime pump by actuating 5 to 10 times prior to first use; actuate ~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).
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; lubricant for endotracheal intubation (oral, nasal) (Glydo only).
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:
1.8% (ZTlido): Relief of pain associated with postherpetic neuralgia.
3.5% products: Temporary relief of minor localized pain.
4% products: Temporary relief of minor localized pain.
5% products: Relief of pain associated with postherpetic neuralgia.
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; local management of skin wounds, including pressure ulcers, venous stasis ulcers, first- and second-degree burns, and superficial wounds and scrapes. Indications may vary by product; also refer to manufacturer’s labeling.
KIDs List: Lidocaine viscous oral solution, when used in pediatric patients <2 years of age for teething, is identified on the Key Potentially Inappropriate Drugs in Pediatrics (KIDs) list and should be avoided due to risk of seizures, arrhythmia, and death (from CNS depression, seizures, and dysrhythmias) (strong recommendation; high quality of evidence) (PPA [Meyers 2020]).
Substrate of CYP1A2 (minor), CYP2A6 (minor), CYP2B6 (minor), CYP2C9 (minor), CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Antiarrhythmic Agents (Class IB): Lidocaine (Topical) may enhance the adverse/toxic effect of Antiarrhythmic Agents (Class IB). Risk C: Monitor therapy
Cimetidine: May increase the serum concentration of Lidocaine (Topical). Risk C: Monitor therapy
Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Risk C: Monitor therapy
Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: 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. Risk C: 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 for signs of methemoglobinemia when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid use of these agents with prilocaine/lidocaine cream in infants less than 12 months of age. Risk C: 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. Risk C: Monitor therapy
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.
Information regarding the presence of lidocaine in breast milk following topical administration has not been located. Lidocaine is present in breast milk following systemic administration (Dryden 2000; Giuliani 2001; Lebedevs 1993; Ortega 1999; Zeisler 1986). However, the oral bioavailability is low and rapid biotransformation occurs via the liver. The amount of lidocaine to reach the bloodstream of a breastfed infant is expected to be low and would be unlikely to cause adverse effects (Dryden 2000; Giuliani 2001; Lebedevs 1993; Ortega 1999).
Lidocaine is considered compatible with breastfeeding (WHO 2002). The manufacturer recommends caution be used when administering topical lidocaine to breastfeeding women. Cumulative exposure from all routes of administration should be considered.
Monitor patients for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
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
Onset: Intradermal injection: 1 to 3 minutes; Topical: 3 to 5 minutes; Transdermal: ~4 hours (Davies 2004)
Duration: Intradermal injection: 10 minutes
Absorption: Transdermal (5%): 3% ± 2% (following application of 3 patches), extent and rate variable; dependent upon concentration, dose, application site, and duration of exposure
Protein binding: 60% to 80%
Metabolism: Hepatic via CYP1A2 (major) and CYP3A4 (minor); active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX)
Half-life, elimination: IV: 1.5 to 2 hours; prolonged 2-fold or more in hepatic impairment
Time to peak: Transdermal (5%): 11 hours (following application of 3 patches); Transdermal (1.8%): ~14 hours (following application of 3 patches)
Excretion: Urine (<10% as unchanged drug)
Altered kidney function: Accumulation of metabolites may occur.
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