Version May 2024
Anesthesia, topical:
Cream: Superficial dermatological procedures: Prior to procedure, apply to intact skin for 20 to 60 minutes. Amount of cream varies depending on size of the surface area to be treated; see manufacturer's labeling for detailed information.
Patch:
Venipuncture or intravenous cannulation: Prior to procedure, apply to intact skin for 20 to 30 minutes; Note: May use another patch at a new location to facilitate venous access after a failed attempt; remove previous patch.
Superficial dermatological procedures: Prior to procedure, apply to intact skin for 30 minutes
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. Lidocaine primarily undergoes hepatic metabolism and its pharmacokinetics are not expected to be changed significantly following topical administration of recommended doses in renal impairment.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). Use caution in patients with severe hepatic dysfunction.
Refer to adult dosing.
(For additional information see "Lidocaine and tetracaine: Pediatric drug information")
Anesthesia, topical: Children ≥3 years and Adolescents: Patch:
Venipuncture or IV cannulation: Prior to procedure, apply to intact skin for 20 to 30 minutes. Note: May use another patch at a new location to facilitate venous access after a failed attempt; remove previous patch. Otherwise, simultaneous or sequential application of multiple patches is not recommended.
Superficial dermatologic procedures: Prior to procedure, apply to intact skin for 30 minutes.
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. Lidocaine primarily undergoes hepatic metabolism and its pharmacokinetics are not expected to be changed significantly following topical administration of recommended doses in renal impairment.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). Use caution in patients with severe hepatic dysfunction.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Also see individual agents.
>10%:
Cardiovascular: Localized blanching (12% to 16%)
Dermatologic: Erythema (47% to 71%)
Local: Skin edema (12% to 14%)
1% to 10%:
Central nervous system: Dizziness (≤1%), drowsiness (≤1%), headache (≤1%), paresthesia (≤1%)
Dermatologic: Acne vulgaris (≤1%), contact dermatitis (≤1%), ecchymosis (≤1%), maculopapular rash (≤1%), skin blister (≤1%), urticaria (≤1%), vesicobullous dermatitis (≤1%), xeroderma (≤1%)
Gastrointestinal: Nausea (≤1%), vomiting (≤1%)
Hematologic & oncologic: Petechial rash (≤1%)
Hypersensitivity: Hypersensitivity reaction (≤1%)
Infection: Infection (≤1%)
Local: Application-site dermatitis (<4%), application site rash (<4%), local discoloration (<4%), application site pain (≤1%), application-site pruritus (≤1%)
<1%, postmarketing, and/or case reports: Anaphylactoid shock, angioedema, blepharitis, bronchospasm, burning sensation of skin, confusion, dehydration, diaphoresis, fever, hyperventilation, hypotension, nervousness, pallor, pharyngitis, stupor, syncope, tremor
Hypersensitivity to lidocaine, tetracaine, amide or ester-type anesthetic agents, para-aminobenzoic acid (PABA), or any other component of the formulation
Canadian labeling: Additional contraindications (not in US labeling): Cream: Congenital or idiopathic methemoglobinemia; procedures requiring large amounts over large areas of the body (>400 cm2).
Concerns related to adverse effects:
• Hypersensitivity: Hypersensitivity or anaphylactic reactions, including angioedema, bronchospasm, shock, and urticaria, may occur. Discontinue use and institute appropriate therapy if hypersensitivity occurs.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with severe hepatic impairment.
Concurrent drug therapy issues:
• Other local anesthetics: If being used with other products containing local anesthetic, consider potential for additive effects.
Special populations:
• Acutely ill patients: Use with caution in acutely ill patients.
• Debilitated patients: Use with caution in debilitated patients.
• Older adult: Use with caution in the elderly.
• Pseudocholinesterase deficiency: Use with caution in patients with pseudocholinesterase deficiency; greater risk of lidocaine/tetracaine toxicity.
Dosage form specific issues:
• Topical cream: Application of cream for longer duration than recommended, or application over larger surface areas is not recommended because of the risk for increased drug absorption and possible adverse reactions.
• Transdermal patch: Application of patch for longer duration than recommended, or simultaneous or sequential application of multiple patches is not recommended because of the risk for increased drug absorption and possible adverse reactions. Patch may contain conducting metal (eg, iron); remove patch prior to MRI. Proper storage and disposal of used patches are essential to prevent accidental exposures, especially in children; accidental exposure may result in serious adverse effects.
Other warnings/precautions:
• Appropriate use: Avoid contact with eye and lip; loss of protective reflexes may predispose to corneal irritation and/or abrasion. Application to broken or inflamed skin or mucous membranes may lead to increased systemic absorption. Not for use at home. Do not use prior to vaccine injections.
In a clinical trial, lidocaine/tetracaine cream (Pliaglis) applied for 30 minutes was not shown to be effective at providing venipuncture analgesia in pediatric patients 5 to 17 years. Topical patches and cream (both used and unused) may cause toxicities in children; used patches and cream still contain large amounts of lidocaine and tetracaine; store and dispose out of the reach of children.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Cream, external:
Pliaglis: Lidocaine 7% and tetracaine 7% (30 g, 100 g [DSC]) [contains methylparaben, propylparaben]
Generic: Lidocaine 7% and tetracaine 7% (30 g [DSC])
Patch, transdermal:
Synera: Lidocaine 70 mg and tetracaine 70 mg (10s) [contains heating component, metal; each patch is ~50 cm2] [DSC]
Yes: cream
Cream (Pliaglis External)
7-7% (per gram): $46.14
Kit (Pliaglis External)
7-7% (per each): $1,400.00
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. [DSC] = Discontinued product
Cream, external:
Pliaglis: Lidocaine 7% and tetracaine 7% (30 g) [contains methylparaben, propylparaben]
Topical cream: Apply to intact, healthy skin. Avoid contact with eyes and lips. Prior to procedure, spread self-occluding cream evenly and thinly (approximately 1 mm) across the treatment area using a flat-surfaced tool (eg, metal spatula, tongue depressor). After waiting the required application time, remove the cream by grasping a free-edge with fingers and pulling it away from the skin. Alternatively, the cream may be removed with gauze. Do not apply to the procedure site after the procedure has been performed. If skin irritation or a burning sensation occurs, remove cream. Wash hands after handling cream. Carefully discard the used cream out of the reach of children and pets.
Transdermal patch: Apply to intact, healthy skin. Use immediately after opening pouch. Patch begins to heat once removed from pouch. May increase skin temperature by 5°C, will not exceed 40°C. If irritation or burning sensation occurs during application, remove patch. Wash hands after applying. Do not cut the patch or remove the top cover. Do not cover the holes on the top side of the patch. Carefully dispose of used patches as they contain large amounts of lidocaine and tetracaine. Fold adhesive together following use.
Topical:
Topical cream: Apply to intact, healthy skin. Spread self-occluding cream evenly and thinly (approximately 1 mm) across the treatment area using a flat-surfaced tool (eg, metal spatula, tongue depressor). After waiting the required application time, remove the cream by grasping a free-edge with fingers and pulling it away from the skin. Alternatively, the cream may be removed with gauze. If skin irritation or a burning sensation occurs, remove cream. Wash hands after handling cream. Carefully discard the used cream out of the reach of children and pets.
Transdermal patch: Apply to intact, healthy skin. Use immediately after opening pouch. Patch begins to heat once removed from pouch. May increase skin temperature by 5°C, will not exceed 40°C. If irritation or burning sensation occurs during application, remove patch. Wash hands after applying. Do not cut the patch or remove the top cover; this could result in thermal injury. Do not cover the holes on the top side of the patch as this could cause the patch not to heat up. Carefully dispose of used patches as they contain large amounts of lidocaine and tetracaine. Fold adhesive together following use.
Anesthesia, topical:
Cream: For use on intact skin in adults to provide topical local analgesia for superficial dermatological procedures, including dermal filler injection, pulsed dye laser therapy, facial laser resurfacing, and laser-assisted tattoo removal.
Patch: For use on intact skin in patients ≥3 years to provide local analgesia for superficial venous access and superficial dermatological procedures, including excision, electrodesiccation, and shave biopsy of skin lesions.
Transdermal patch may contain conducting metal (eg, iron); remove patch prior to MRI.
Refer to individual components.
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 Lexicomp 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 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. 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
Systemic absorption following topical application is expected to be low compared to parenteral administration, and is related to duration of exposure and surface area of application site. Systemic absorption would be required in order for lidocaine and tetracaine to cross the placenta and reach the fetus.
Refer to Lidocaine (Systemic), Lidocaine (Topical), and Tetracaine (Systemic) monographs.
Lidocaine is present in breast milk; it is not known if tetracaine is present in breast milk.
The amount of lidocaine in breast milk following topical application is not known. Systemic absorption following topical application is expected to be low compared to parenteral administration, and is related to duration of exposure and surface area of application site. Do not apply to the nipple or surrounding breast area to avoid direct exposure to the breastfeeding infant. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Refer to Lidocaine (Systemic), Lidocaine (Topical), and Tetracaine (Systemic) monographs.
Effectiveness of anesthesia
Local anesthetic action occurs by stabilization of neuronal membranes and inhibiting the sodium ion fluxes required for the initiation and conduction of impulses.
Also see individual agents.
Onset: Within 20 to 30 minutes
Duration: Cream: 11 hours
Absorption: Related to duration of application and area where applied.
Distribution: Lidocaine crosses the blood-brain barrier
Vd: Lidocaine: Neonates: 2.75 L/kg; Adults: 1.1 L/kg
Protein binding: Lidocaine: 70%
Metabolism:
Lidocaine: Metabolized in the liver by cytochrome P450 CYP1A2 and partially by CYP3A4 to inactive and active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX)
Tetracaine: Hydrolysis by plasma esterases to primary metabolites para-aminobenzoic acid and diethylaminoethanol
Half-life elimination: Lidocaine: Adults: 1.8 hours
Excretion: Lidocaine: Excreted in urine as metabolites and parent drug
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