Lidocaine And Tetracaine
FDA Drug Information • Also known as: Pliaglis
- Brand Names
- Pliaglis
- Drug Class
- Amide Local Anesthetic [EPC], Antiarrhythmic [EPC], Ester Local Anesthetic [EPC]
- Route
- TOPICAL
- Dosage Form
- CREAM
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION PLIAGLIS (lidocaine and tetracaine) Cream 7% / 7% is a topical local anesthetic cream that forms a pliable peel on the skin when exposed to air. The drug formulation is an emulsion in which the oil phase is a 1:1 eutectic mixture of lidocaine 7% and tetracaine 7%. The eutectic mixture has a melting point below room temperature and therefore both local anesthetics exist as a liquid oil rather than as crystals. The net weight of lidocaine is 2.1 g and of tetracaine is 2.1 g per 30 g tube. Lidocaine, an amide local anesthetic, is chemically designated as acetamide,2-(diethylamino)-N-(2,6-dimethylphenyl) and has an octanol: water partition ratio of 182 at pH 7.3. The molecular weight of lidocaine is 234.3, and the molecular formula is C14H22N2O. The structural formula is: Tetracaine, an ester local anesthetic, is chemically designated as 2-dimethylaminoethyl 4-n-butyl-aminobenzoate and has an octanol:water partition ratio of 5370 at pH 7.3. The molecular weight of tetracaine is 264.4, and the molecular formula is C15H24N2O2. The structural formula is: Each gram of PLIAGLIS contains lidocaine 70 mg and tetracaine 70 mg in a 1:1 eutectic mixture and it also contains the following inactive ingredients: anhydrous dibasic calcium phosphate, methylparaben, polyvinyl alcohol, propylparaben, purified water, sorbitan monopalmitate, and white petrolatum. image description image description
What Is Lidocaine And Tetracaine Used For?
1 INDICATIONS AND USAGE PLIAGLIS is indicated for use on intact skin in adults to provide topical local analgesia for superficial dermatological procedures such as dermal filler injection, pulsed dye laser therapy, facial laser resurfacing, and laser-assisted tattoo removal. PLIAGLIS is a combination of lidocaine, an amide local anesthetic, and tetracaine, an ester local anesthetic, indicated for use on intact skin in adults to provide topical local analgesia for superficial dermatological procedures such as dermal filler injection, pulsed dye laser therapy, facial laser resurfacing, and laser-assisted tattoo removal. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Apply only to intact skin. ( 2.1 ) Do not exceed the recommended dose of drug or duration of application. ( 2.1 ) Recommended duration of application ( 2.2 ): For dermal filler injection ablative laser facial resurfacing, or pulsed-dye laser therapy 20-30 minutes prior to procedure For superficial dermatological procedures such as laserassisted tattoo removal 60 minutes prior to procedure See Full Prescribing Information for amount to apply based upon treatment site surface area. ( 2.3 ) 2.1 Important Dosage and Administration Instructions For use in adults only. PLIAGLIS should only be applied to intact skin. PLIAGLIS should not be applied to a procedure site after the procedure has been performed. Remove PLIAGLIS if skin irritation or a burning sensation occurs during application. In order to minimize the risk of systemic toxicity, do not exceed the recommended amount of drug to apply or the duration of the application [see Overdosage (10) ] . Avoid eye and lip contact with PLIAGLIS. Wash hands after handling PLIAGLIS. Upon removal from the treatment site, discard the used PLIAGLIS in a location that is out of the reach of children and pets. Access to PLIAGLIS by children or pets should be prevented during usage and storage of the product [see Warnings and Precautions (5.2) ] . Use only as directed. 2.2 Recommended Dosing Duration For superficial dermatological procedures, such as dermal filler injection, non-ablative laser facial resurfacing, or pulsed-dye laser therapy, apply PLIAGLIS to intact skin for 20 to 30 minutes prior to the procedure. See Table 1 for instructions on the amount to apply. For superficial dermatological procedures, such as laser-assisted tattoo removal, apply PLIAGLIS to intact skin for 60 minutes prior to the procedure. See Table 1 for instructions on the amount to apply. 2.3 Recommended Dosage The dose of PLIAGLIS that provides effective local dermal analgesia depends on the duration of the application. Although not specifically studied, a shorter duration of application may result in a less complete dermal analgesia or a shorter duration of adequate dermal analgesia. Determine the amount of drug to apply The amount (length) of PLIAGLIS that should be dispensed is determined by the size of the area to be treated (see Table 1 ). Using the ruler on the applicator included in the carton, squeeze out and measure the amount of PLIAGLIS that approximates the amount required to achieve proper coverage. Spread PLIAGLIS evenly and thinly (approximately 1 mm or the thickness of a dime) across the treatment area using a flat-surfaced tool such as a metal spatula or tongue depressor. After waiting the required application time, remove the PLIAGLIS by grasping a free-edge with your fingers and pulling it away from the skin. Table 1. Amount of PLIAGLIS According to Treatment Site Surface Area Surface Area of Treatment Site (inch 2 ) Length of PLIAGLIS for 1 mm Thickness (inch) Weight of PLIAGLIS...
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: Methemoglobinemia [see Warnings and Precautions (5.1) ] Overexposure [see Warnings and Precautions (5.2) ] Risks of Secondary Exposure in Children and Pets [see Warnings and Precautions (5.3) ] Anaphylactic Reactions [see Warnings and Precautions (5.4) ] Eye Irritation [see Warnings and Precautions (5.5) ] Most common local reactions were erythema (47%), skin discoloration (16%), and edema (14%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact IPG Pharmaceuticals, Inc. at 1-888-711-7116 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. However, the adverse reaction information from clinical trials does provide a basis for identifying the adverse events that appear to be related to drug use and for approximating their incidence in clinical practice. PLIAGLIS has been evaluated for safety in 2159 persons undergoing a superficial dermal procedure. PLIAGLIS was studied in 11 placebo-controlled and 1 active-controlled trials, and in open-label safety trials. All 2159 persons were exposed to only a single application of PLIAGLIS. Adverse reactions were assessed by collecting spontaneously reported adverse reactions, and observations made on formal evaluation of the skin for specific reactions. Most common adverse reactions in clinical trials Localized Reactions: In clinical studies, the most common local reactions were erythema (47%), skin discoloration (e.g., blanching, ecchymosis, and purpura) (16%), and edema (14%). There were no serious adverse reactions. However, one patient withdrew due to burning pain at the treatment site. Other Localized Reactions: The following dermal adverse reactions occurred in 1% or less of PLIAGLIS-treated patients: ecchymosis, petechial rash, vesiculobullous rash, perifollicular erythema, perifollicular edema, pruritus, rash, maculopapular rash, dry skin, contact dermatitis, and acne. Systemic (Dose-Related) Reactions: Across all trials, 19 subjects experienced a systemic adverse reaction, 15 of whom were treated with PLIAGLIS and 4 with placebo. The frequency of systemic adverse reactions was greater for the PLIAGLIS group (1%) than the placebo group (0.3%). The most common systemic adverse events were headache, vomiting, dizziness, and fever, all of which occurred with a frequency of <1%. Other systemic reactions were syncope, nausea, confusion, dehydration, hyperventilation, hypotension, nervousness, paresthesia, pharyngitis, stupor, pallor, and sweating. Systemic adverse reactions of lidocaine and tetracaine are similar in nature to those observed with other amide and ester local anesthetic agents, including CNS excitation and/or depression (lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensation of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest). Excitatory CNS reactions may be brief or not occur at all, in which case the first manifestation may be drowsiness merging into unconsciousness. Signs of CNS toxicity may start at plasma concentrations of lidocaine at 1000 ng/mL. The plasma concentrations at which tetracaine toxicity may occur are less well characterized; however, systemic toxicity with tetracaine is thought to occur with much lower plasma concentrations compared with lidocaine. The toxicity of co-administered local anesthetics is thought to be at least additive. Cardiovascular manifestations may include bradycardia, hypotension and cardiovascular collapse leading to arrest. 6.2 Postmarketing Experience The following adverse reactions have been identified...
Drug Interactions
7 DRUG INTERACTIONS Antiarrhythmic Drugs : Use with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) because the systemic toxic effects are thought to be additive and potentially synergistic with lidocaine and tetracaine. ( 7.1 ) 7.1 Antiarrhythmic Drugs PLIAGLIS should be used with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the systemic toxic effects are thought to be additive and potentially synergistic with lidocaine and tetracaine. 7.2 Local Anesthetics When PLIAGLIS is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations should be considered since the systemic toxic effects are thought to be additive and potentially synergistic with lidocaine and tetracaine. 7.3 Drugs That May Cause Methemoglobinemia When Used with PLIAGLIS Patients who are administered local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following drugs, which could include other local anesthetics: Examples of Drugs Associated with Methemoglobinemia: Class Examples Nitrates/Nitrites nitric oxide, nitroglycerin, nitroprusside, nitrous oxide Local anesthetics articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine Antineoplastic agents cyclophosphamide, flutamide, hydroxyurea, ifosfamide, rasburicase Antibiotics dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides Antimalarials chloroquine, primaquine Anticonvulsants phenobarbital, phenytoin, sodium valproate Other drugs acetaminophen, metoclopramide, quinine, sulfasalazine
Contraindications
4 CONTRAINDICATIONS PLIAGLIS is contraindicated in patients with a known history of sensitivity to lidocaine or tetracaine, local anesthetics of the amide or ester type, or to any other component of the product [ see Warnings and Precautions (5.4) ]. PLIAGLIS is contraindicated in patients with para-aminobenzoic acid (PABA) hypersensitivity. Known history of sensitivity to lidocaine or tetracaine, or local anesthetics of the amide or ester type. ( 4 ) Para-aminobenzoic acid (PABA) hypersensitivity. ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary There are no available data on PLIAGLIS use in pregnant women to determine a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Available data from an epidemiologic study and case series with parenteral lidocaine use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes. Published data on tetracaine use in pregnant women are not sufficient to determine any drug-associated risks. The amount of lidocaine and tetracaine systemically absorbed from PLIAGLIS is low compared to the parenteral route of administration and is not expected to result in significant fetal exposure. Systemic exposure of PLIAGLIS is directly related to both the duration of application and the surface area over which it is applied [ see Clinical Pharmacology (12.3) ] . In a published animal reproduction study, pregnant rats administered lidocaine by continuous subcutaneous infusion at doses approximately 1.3 times the maximum recommended human dose (MRHD) of 53 grams of PLIAGLIS during the period of organogenesis resulted in lower fetal body weights. In a published animal reproduction study, pregnant rats administered lidocaine, containing 1:100,000 epinephrine, injected into the masseter muscle of the jaw or into the gum of the lower jaw on Gestation Day 11 at 0.02 times the MRHD of PLIAGLIS resulted in developmental delays in neonates. Subcutaneous administration of tetracaine to pregnant rats and rabbits during organogenesis did not produce adverse embryofetal effects at 0.03 times the MRHD of PLIAGLIS (see Data ) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized...
Overdosage
10 OVERDOSAGE Application of 59 g of PLIAGLIS over 400 cm 2 (62 inch 2 ) for up to 120 minutes to adults produces peak plasma concentrations of lidocaine of 220 ng/mL. Toxic levels of lidocaine (>5000 ng/mL) cause CNS toxicity, including the risk of seizure. Signs of CNS toxicity may start at plasma concentrations of lidocaine as low as 1000 ng/mL, and the risk of seizures generally increases with increasing plasma levels. Very high levels of lidocaine can cause respiratory arrest, coma, decreases in cardiac output, total peripheral resistance and mean arterial pressure, ventricular arrhythmias and cardiac arrest. Tetracaine is associated with a profile of systemic CNS and cardiovascular adverse events similar to lidocaine, although toxicity associated with tetracaine is thought to occur at lower doses compared to lidocaine. The toxicity of co-administered local anesthetics is thought to be at least additive. In the absence of massive topical overdose or oral ingestion, other etiologies for the clinical effects or overdosage from other sources of lidocaine, tetracaine or other local anesthetics should be considered. The management of overdosage includes close monitoring, supportive care and symptomatic treatment. Dialysis is of negligible value in the treatment of acute overdosage of lidocaine or tetracaine.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING PLIAGLIS (lidocaine and tetracaine) Cream (70 mg of lidocaine and 70 mg of tetracaine in 1 gram), 7% / 7%, appears smooth and white to off-white and is available as the following: NDC 71085-100-30 30 gram tube (with Child Resistant Cap) with applicator Refrigerate at 2 to 8°C (36 to 46°F). Do not freeze. PLIAGLIS can be stored at room temperature for up to 3 months. Discard PLIAGLIS after storing at room temperature for 3 months.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.