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Prizotral II

Lidocaine 2.5% and Prilocaine 2.5% Cream, USP is an emulsion in which the oil phase is a eutectic mixture of lidocaine and prilocaine cream in a ratio of 1:1 by weight. This eutectic mixture has a melting point below room temperature and therefore both local anesthetics exist as a liquid oil rather than as crystals. It is packaged in 5 gram and 30 gram tubes.

Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), has an octanol: water partition ratio of 43 at pH 7.4, and has the following structure:

Prilocaine is chemically designated as propanamide, N-(2-methylphenyl)-2-(propylamino), has an octanol: water partition ratio of 25 at pH 7.4, and has the following structure:

Each gram of lidocaine and prilocaine cream contains lidocaine 25 mg, prilocaine 25 mg, polyoxyethylene fatty acid esters (as emulsifiers), carboxypolymethylene (as a thickening agent), sodium hydroxide to adjust to a pH approximating 9, and purified water to 1 gram. Lidocaine and prilocaine cream contains no preservative, however it passes the USP antimicrobial effectiveness test due to the pH. The specific gravity of lidocaine and prilocaine cream is 1.00.

Prizotral II - Clinical Pharmacology

Mechanism of Action: Lidocaine and prilocaine cream applied to intact skin under occlusive dressing, provides dermal analgesia by the release of lidocaine and prilocaine from the cream into the epidermal and dermal layers of the skin and by the accumulation of lidocaine and prilocaine in the vicinity of dermal pain receptors and nerve endings. Lidocaine and prilocaine are amide-type local anesthetic agents. Both lidocaine and prilocaine stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

The onset, depth and duration of dermal analgesia on intact skin provided by lidocaine and prilocaine cream depend primarily on the duration of application. To provide sufficient analgesia for clinical procedures such as intravenous catheter placement and venipuncture, lidocaine and prilocaine cream should be applied under an occlusive dressing for at least 1 hour. To provide dermal analgesia for clinical procedures such as split skin graft harvesting, lidocaine and prilocaine cream should be applied under occlusive dressing for at least 2 hours. Satisfactory dermal analgesia is achieved 1 hour after application, reaches maximum at 2 to 3 hours, and persists for 1 to 2 hours after removal. Absorption from the genital mucosa is more rapid and onset time is shorter (5 to 10 minutes) than after application to intact skin. After a 5 to 10 minute application of lidocaine and prilocaine cream to female genital mucosa, the average duration of effective analgesia to an argon laser stimulus (which produced a sharp, pricking pain) was 15 to 20 minutes (individual variations in the range of 5 to 45 minutes).

Dermal application of lidocaine and prilocaine cream may cause a transient, local blanching followed by a transient, local redness or erythema.

Pharmacokinetics: Lidocaine and prilocaine cream is a eutectic mixture of lidocaine 2.5% and prilocaine 2.5% formulated as an oil in water emulsion. In this eutectic mixture, both anesthetics are liquid at room temperature (see DESCRIPTION) and the penetration and subsequent systemic absorption of both prilocaine and lidocaine are enhanced over that which would be seen if each component in crystalline form was applied separately as a 2.5% topical cream.

Absorption: The amount of lidocaine and prilocaine systemically absorbed from lidocaine and prilocaine cream is directly related to both the duration of application and to the area over which it is applied. In two pharmacokinetic studies, 60 g of lidocaine and prilocaine cream (1.5 g lidocaine and 1.5 g prilocaine) was applied to 400 cm 2 of intact skin on the lateral thigh and then covered by an occlusive dressing. The subjects were then randomized such that one-half of the subjects had the occlusive dressing and residual cream removed after 3 hours, while the remainder left the dressing in place for 24 hours. The results from these studies are summarized below.

TABLE 1 Absorption of Lidocaine and Prilocaine from Lidocaine and Prilocaine Cream: Normal Volunteers (N=16)
*Maximum recommended duration of exposure is 4 hours.
Lidocaine and

Prilocaine

Cream (g)
Area

(cm 2)
Time on

(hrs)
Drug Content

(mg)
Absorbed

(mg)
C max

(μg/mL)
T max

(hr)
60 400 3 lidocaine 1500 54 0.12 4
prilocaine 1500 92 0.07 4
60 400 24* lidocaine 1500 243 0.28 10
prilocaine 1500 503 0.14 10

When 60 g of lidocaine and prilocaine cream was applied over 400 cm 2 for 24 hours, peak blood levels of lidocaine are approximately 1/20 the systemic toxic level. Likewise, the maximum prilocaine level is about 1/36 the toxic level. In a pharmacokinetic study, lidocaine and prilocaine cream was applied to penile skin in 20 adult male patients in doses ranging from 0.5 g to 3.3 g for 15 minutes. Plasma concentrations of lidocaine and prilocaine following lidocaine and prilocaine cream application in this study were consistently low (2.5 to 16 ng/mL for lidocaine and 2.5 to 7 ng/mL for prilocaine). The application of lidocaine and prilocaine cream to broken or inflamed skin, or to 2,000 cm 2 or more of skin where more of both anesthetics are absorbed, could result in higher plasma levels that could, in susceptible individuals, produce a systemic pharmacologic response.

The absorption of lidocaine and prilocaine cream applied to genital mucous membranes was studied in two open-label clinical trials. Twenty-nine patients received 10 g of lidocaine and prilocaine cream applied for 10 to 60 minutes in the vaginal fornices. Plasma concentrations of lidocaine and prilocaine following lidocaine and prilocaine cream application in these studies ranged from 148 to 641 ng/mL for lidocaine and 40 to 346 ng/mL for prilocaine and time to reach maximum concentration (t max) ranged from 21 to 125 minutes for lidocaine and from 21 to 95 minutes for prilocaine. These levels are well below the concentrations anticipated to give rise to systemic toxicity (approximately 5000 ng/mL for lidocaine and prilocaine).

Distribution: When each drug is administered intravenously, the steady-state volume of distribution is 1.1 to 2.1 L/kg (mean 1.5, ±0.3 SD, n=13) for lidocaine and is 0.7 to 4.4 L/kg (mean 2.6, ±1.3 SD, n=13) for prilocaine. The larger distribution volume for prilocaine produces the lower plasma concentrations of prilocaine observed when equal amounts of prilocaine and lidocaine are administered. At concentrations produced by application of lidocaine and prilocaine cream, lidocaine is approximately 70% bound to plasma proteins, primarily alpha-1-acid glycoprotein. At much higher plasma concentrations (1 to 4 μg/mL of free base) the plasma protein binding of lidocaine is concentration dependent. Prilocaine is 55% bound to plasma proteins. Both lidocaine and prilocaine cross the placental and blood brain barrier, presumably by passive diffusion.

Metabolism: It is not known if lidocaine or prilocaine are metabolized in the skin. Lidocaine is metabolized rapidly by the liver to a number of metabolites including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine. The metabolite, 2,6-xylidine, has unknown pharmacologic activity. Following intravenous administration, MEGX and GX concentrations in serum range from 11 to 36% and from 5 to 11% of lidocaine concentrations, respectively. Prilocaine is metabolized in both the liver and kidneys by amidases to various metabolites including ortho-toluidine and N-n-propylalanine. It is not metabolized by plasma esterases. The ortho-toluidine metabolite has been shown to be carcinogenic in several animal models (see Carcinogenesis subsection of PRECAUTIONS). In addition, ortho-toluidine can produce methemoglobinemia following systemic doses of prilocaine approximating 8 mg/kg (see ADVERSE REACTIONS). Very young patients, patients with glucose-6-phosphate dehydro- genase deficiencies and patients taking oxidizing drugs such as antimalarials and sulfonamides are more susceptible to methemoglobinemia (see Methemoglobinemia subsection of WARNINGS).

Elimination: The terminal elimination half-life of lidocaine from the plasma following IV administration is approximately 65 to 150 minutes (mean 110, ±24 SD, n=13). More than 98% of an absorbed dose of lidocaine can be recovered in the urine as metabolites or parent drug. The systemic clearance is 10 to 20 mL/min/kg (mean 13, ±3 SD, n=13). The elimination half-life of prilocaine is approximately 10 to 150 minutes (mean 70, ±48 SD, n=13). The systemic clearance is 18 to 64 mL/min/kg (mean 38, ±15 SD, n=13). During intravenous studies, the elimination half-life of lidocaine was statistically significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours). No studies are available on the intravenous pharmacokinetics of prilocaine in elderly patients.

Pediatrics: Some pharmacokinetic (PK) data are available in infants (1 month to 5 kg 2 g 20 cm 2 4 hours 1 to 6 years and > 10 kg 10 g 100 cm 2 4 hours 7 to 12 years and > 20 kg 20 g 200 cm 2 4 hours

Please note: If a patient greater than 3 months old does not meet the minimum weight requirement, the maximum total dose of lidocaine and prilocaine cream should be restricted to that which corresponds to the patient's weight (see INSTRUCTIONS FOR APPLICATION).

Practitioners should carefully instruct caregivers to avoid application of excessive amounts of lidocaine and prilocaine cream (see PRECAUTIONS).

When applying lidocaine and prilocaine cream to the skin of young children, care must be taken to maintain careful observation of the child to prevent accidental ingestion of lidocaine and prilocaine cream or the occlusive dressing. A secondary protective covering to prevent inadvertent disruption of the application site may be useful.

Lidocaine and prilocaine cream should not be used in neonates with a gestational age less than 37 weeks nor in infants under the age of 12 months who are receiving treatment with methemoglobin-inducing agents (see Methemoglobinemia subsection of WARNINGS).

When lidocaine and prilocaine cream (lidocaine 2.5% and prilocaine 2.5%) is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered (see Individualization of Dose). The amount absorbed in the case of lidocaine and prilocaine cream is determined by the area over which it is applied and the duration of application under occlusion (see Table 2, ** footnote, in Individualization of Dose).

Although the incidence of systemic adverse reactions with lidocaine and prilocaine cream is very low, caution should be exercised, particularly when applying it over large areas and leaving it on for longer than 2 hours. The incidence of systemic adverse reactions can be expected to be directly proportional to the area and time of exposure (see Individualization of Dose).

INSTRUCTIONS FOR APPLICATION:

To measure 1 gram of lidocaine and prilocaine cream, the Cream should be gently squeezed out of the tube as a narrow strip that is 1.5 inches (3.8 cm) long and 0.2 inches (5 mm) wide. The strip of lidocaine and prilocaine cream should be contained within the lines of the diagram shown below.

Use the number of strips that equals your dose, like the examples in the table below.

Dosing Information

1 gram = 1 strip

2 grams = 2 strips

2.5 grams = 2.5 strips

For adult and pediatric patients, apply ONLY as prescribed by your physician.

If your child is below the age of 3 months or small for their age, please inform your doctor before applying lidocaine and prilocaine cream, which can be harmful, if applied over too much skin at one time in young children.

When applying lidocaine and prilocaine cream to the intact skin of young children, it is important that they be carefully observed by an adult in order to prevent the accidental ingestion of or eye contact with lidocaine and prilocaine cream.

Lidocaine and prilocaine cream must be applied to intact skin at least 1 hour before the start of a routine procedure and for 2 hours before the start of a painful procedure. A protective covering of the cream is not necessary for absorption but may be helpful to keep the cream in place.

If using a protective covering, your doctor will remove it, wipe off the lidocaine and prilocaine cream, and clean the entire area with an antiseptic solution before the procedure. The duration of effective skin anesthesia will be at least 1 hour after removal of the protective covering.

Precautions
  • Do not apply near eyes or open wounds.
  • Keep out of the reach of children.
  • If your child becomes very dizzy, excessively sleepy, or develops duskiness of the face or lips after applying lidocaine and prilocaine cream, remove the cream and contact the child's physician at once.
  • How is Prizotral II Supplied

    Lidocaine 2.5% and Prilocaine 2.5% Cream, USP is available as the following:

    NDC 52565-007-30 gram/tube packed individually, in a child-resistant tube.

    NOT FOR OPHTHALMIC USE.

    KEEP CONTAINER TIGHTLY CLOSED AT ALL TIMES WHEN NOT IN USE.

    Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Do Not Freeze.

    Manufactured by:

    Teligent Pharma, Inc.
    Buena, New Jersey 08310

    Rev.10/2018

    Prizotral II Description

    Lidotral™ (Lidocaine HCl) 3.88% Cream contains Lidocaine HCl 3.88% in a mild acidic vehicle. Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), and has the following structure:

    Ingredients: Each gram of Lidotral™ 3.88% Cream contains Lidocaine HCl USP 38.8 mg. Inactive Ingredients include: Calcium Acetate, Ceteareth 20, Cetearyl Alcohol, Glycerin, Methylparaben, Mineral Oil, Petrolatum, Propylene Glycol, Propylparaben, Purified Water, Sodium Phosphate Monobasic.

    Prizotral II - Clinical Pharmacology

    Mechanism of Action: Lidotral™ 3.88% Cream releases lidocaine from a mild acidic vehicle to stabilize the neuronal membrane by inhibiting the ionic fluxes required for initiation and conduction of impulses, thereby effecting local anesthetic action. A mild acidic vehicle lowers pH to increase protection against alkaline irritations and to provide a favorable environment for healing.

    Pharmacokinetics: Lidocaine may be absorbed following topical administration to mucous membranes, its rate and extent of absorption depending upon the specific site of application, duration of exposure, concentration, and total dosage. In general, the rate of absorption of local anesthetic agents following topical application occurs most rapidly after intratracheal administration. Lidocaine is also well-absorbed from the gastrointestinal tract, but little intact drug appears in the circulation because of biotransformation of the liver.

    Lidocaine is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjungation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexlidide. The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine. Approximately 90% of lidocaine administered is excreted in the form of various metabolites and less than 10% is excreted unchanged. The primary metabolite in urine is a conjugate of 4-hydroxy-2, 6-dimethylaniline. The plasma binding of lidocaine is dependent on drug concentration and the fraction bound decreases with increasing concentration. At concentration of 1 to 4 g of free base per mL, 60 to 80 percent of lidocaine is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid-glycoprotein. Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion. Studies of lidocaine metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 1.5 to 2 hours. Because of the rapid rate at which lidocaine is metabolized, any condition that affects liver function may alter lidocaine kinetics. The half-life may be prolonged two-fold or more in patients with liver dysfunction. Renal dysfunction does not affect lidocaine kinetics but may increase the accumulation of metabolites. Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 g free base per mL. In the rhesus monkey, arterial blood levels of 18-21 g/mL have been shown to be threshold for convulsive activity.

    INDICATIONS

    For the temporary relief of pain and itching associated with minor burns, sunburn, minor cuts, scrapes, insect bites, and minor skin irritation.

    Contraindications

    Tuberculous or fungal lesions of skin vaccinia, varicella and acute herpes simplex and in persons who have shown hypersensitivity to any of its components. Lidocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type.

    Warnings

    For external use only. Not for ophthalmic use.

    Precautions

    If irritation or sensitivity occurs or infection appears, discontinue use and institute appropriate therapy. Lidotral™ (Lidocaine HCl) 3.88% Cream should be used with caution in ill, elderly, debilitated patients and children who may be more sensitive to the systemic effects of lidocaine.

    Carcinogenesis, Mutagenesis, and Impairment of Fertility: Studies of lidocaine in animals to evaluate the carcinogenic and mutagenic potential of the effect on fertility have not been conducted.

    Use in Pregnancy: Teratogenic Effects; Pregnancy Category B. Reproduction studies have been performed for lidocaine in rats at doses up to 6.6 times the human dose and have revealed no evidence of harm to the fetus caused by lidocaine. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. General consideration should be given to this fact before administering lidocaine to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place.

    Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when this drug is administered to a nursing mother.

    Pediatric Use: Dosage in pediatric patients would be reduced commensurate with age, body weight and physical condition.

    Adverse Reactions

    During or immediately after treatment, the skin at the site of treatment may develop erythema or edema or may be the locus of abnormal sensation.

    Prizotral II Dosage and Administration

    Apply a thin film to the affected area two or three times daily or as directed by a physician.

    How is Prizotral II Supplied

    DermacinRx® Lidotral™ (Lidocaine HCl) 3.88% Cream

    3 oz (85 g) tube - NDC 59088-371-07

    KEEP THIS AND ALL MEDICATIONS OUT OF REACH OF CHILDREN.

    Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature]. Protect from freezing.

    Manufactured by:

    PureTek Corporation, San Fernando, CA 91340

    Rev. 37744 10/15

    Prizotral-II

    (Lidocaine 2.5% and Prilocaine 2.5% Cream, Lidocaine HCl 3.88% Cream)

    Packaged in the USA by:

    PureTek Corporation

    Panorama City, CA 91402

    For questions or information

    call toll-free: 877-921-7873

    Rev.38134

    Prizotral II 
    lidocaine and prilocaine, lidocaine hydrochloride kit
    Product Information
    Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:59088-757
    Packaging
    # Item Code Package Description
    1 NDC:59088-757-00 1 KIT in 1 PACKAGE
    Quantity of Parts
    Part # Package Quantity Total Product Quantity
    Part 1 1 TUBE 30 g
    Part 2 1 TUBE 85 g
    Part 1 of 2
    LIDOCAINE AND PRILOCAINE 
    lidocaine and prilocaine cream
    Product Information
    Item Code (Source) NDC:52565-007
    Route of Administration TOPICAL DEA Schedule     
    Active Ingredient/Active Moiety
    Ingredient Name Basis of Strength Strength
    LIDOCAINE (LIDOCAINE) LIDOCAINE 25 mg  in 1 g
    PRILOCAINE (PRILOCAINE) PRILOCAINE 25 mg  in 1 g
    Inactive Ingredients
    Ingredient Name Strength
    PEG-60 HYDROGENATED CASTOR OIL  
    CARBOMER HOMOPOLYMER TYPE B (ALLYL SUCROSE CROSSLINKED)  
    WATER  
    SODIUM HYDROXIDE  
    Packaging
    # Item Code Package Description
    1 NDC:52565-007-30 1 TUBE in 1 CARTON
    1 30 g in 1 TUBE
    Marketing Information
    Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
    ANDA ANDA205887 06/29/2018
    Part 2 of 2
    DERMACINRX LIDOTRAL 
    lidocaine hydrochloride cream
    Product Information
    Item Code (Source) NDC:59088-371
    Route of Administration TOPICAL DEA Schedule     
    Active Ingredient/Active Moiety
    Ingredient Name Basis of Strength Strength
    LIDOCAINE HYDROCHLORIDE (LIDOCAINE) LIDOCAINE HYDROCHLORIDE ANHYDROUS 38.8 mg  in 1 g
    Inactive Ingredients
    Ingredient Name Strength
    CALCIUM ACETATE  
    POLYOXYL 20 CETOSTEARYL ETHER  
    CETOSTEARYL ALCOHOL  
    GLYCERIN  
    METHYLPARABEN  
    MINERAL OIL  
    PETROLATUM  
    PROPYLENE GLYCOL  
    PROPYLPARABEN  
    WATER  
    SODIUM PHOSPHATE, MONOBASIC, ANHYDROUS  
    Packaging
    # Item Code Package Description
    1 NDC:59088-371-07 1 TUBE in 1 CARTON
    1 85 g in 1 TUBE
    Marketing Information
    Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
    unapproved drug other 12/03/2015
    Marketing Information
    Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
    ANDA ANDA205887 06/02/2020
    Labeler - PureTek Corporation (785961046)
    Establishment
    Name Address ID/FEI Operations
    Teligent Pharma, Inc. 011036910 manufacture(52565-007)
    Establishment
    Name Address ID/FEI Operations
    PureTek Corporation 785961046 pack(59088-757)
      PureTek Corporation

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