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Tranzarel Gel

Generic Name: lidocaine
Dosage Form: gel

Disclaimer: This drug has not been found by FDA to be safe and effective, and this labeling has not been approved by FDA. For further information about unapproved drugs, click here.

Rx Only

For External Use Only
Do Not Use in the Eyes

Tranzarel Gel Description

TRANZAREL 4% is comprised of a topical anesthetic that is indicated for relief of minor pain.

Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), and has the following structure:

C14H22N2O Mol. wt. 234.34

Each gram contains 40 mg of lidocaine hydrochloride in an aqueous gel base. It also contains the following inactive ingredients: Aloe Barbadensis Leaf Juice, Calendula Officinalis Flower Extract, Camellia Sinensis (Green Tea) Leaf Extract, Carbomer, Chamomilla Recutita (Matricaria) Flower Extract, Diazolidinyl Urea, Disodium EDTA, Glycerin, Menthol, Methylparaben, Propylene Glycol, Propylparaben, Purified Water, SD Alcohol 40-2, Symphytum Officinale (Comfrey) Leaf Extract, Triethanolamine.

Tranzarel Gel - Clinical Pharmacology

Pharmacodynamics

Lidocaine is an amide-type local anesthetic agent and is suggested to stabilize the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby producing a localized analgesic effect.

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 in 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 conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide. 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 concentrations 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.

INDICATION AND USAGE

TRANZAREL 4% is comprised of a topical anesthetic that is indicated for relief of minor pain.

Contraindications

TRANZAREL is contraindicated in patients with a history of sensitivity to any of its ingredients or adverse reactions to lidocaine or amide anesthetics. If excessive irritation and significant worsening occur, discontinue use and seek the advice of your physician.

Warnings

For external use only. Do not use in eyes.

Keep out of reach of children.

Do not use in large quantities, particularly over raw surfaces or blistered areas. If swallowed, get medical help or contact Poison Control Center right away.

Precautions

General

Lidocaine should be used cautiously in those with impaired liver function, as well as the very ill or very elderly and those with significant liver disease. Product should be used with caution in patients receiving antiarrhythmic drugs of Class I since the adverse effects are additive and generally synergistic.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Studies of lidocaine in animals to evaluate the carcinogenic and mutagenic potential of the effect on fertility have not been conducted.

Pregnancy

Teratogenic Effects

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. Since 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.

Nursing Mothers

TRANZAREL has not been studied in nursing mothers. Since lidocaine is excreted in human milk and the clinical significance of this observation is unknown, caution should be exercised when lidocaine is administered to a nursing woman.

Pediatric Use

Safety and efficacy in children have not been established.

Adverse Reactions

During or immediately following application of TRANZAREL, there may be transient stinging or burning from open areas of skin, or transient blanching (lightening), or erythema (redness) of the skin.

Allergic Reactions

Allergic and anaphylactoid reactions associated with lidocaine, although rare, can occur. Such reactions are characterized by angioedema, bronchospasm, dermatitis, dyspnea, hypersensitivity, laryngospasm, pruritus, shock, and urticaria. If they occur, they should be managed by conventional means.

Systemic (Dose-Related) Reactions

Systemic adverse reactions of lidocaine are similar in nature to those observed with other amide local anesthetic agents, including CNS excitation and/or depression (light headedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations 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. Cardiovascular manifestations may include bradycardia, hypotension and cardiovascular collapse leading to arrest.

Tranzarel Gel Dosage and Administration

Apply TRANZAREL to affected area(s) of pain three to four times a day or as directed by a physician. TRANZAREL should only be applied to intact skin. The cap and foil should be removed from the tube prior to use.

To open tube: Turn cap, push down, turn and lift off.
To close tube: Turn on cap until it locks into place.

May be applied under occlusive dressing. Consult with your physician first.

How is Tranzarel Gel Supplied

TRANZAREL (Lidocaine HCl) 4% Pain Relieving Gel is available as the following:

4 fl. oz. (120 mL) laminate tube with a child-resistant cap, NDC 70877-2324-4

Store at 25°C (77°F); excursions permitted: 15°-30°C (59°-86°F) [See USP Controlled Room Temperature]

Manufactured for:
Taleos Pharma Inc.
Eatontown, NJ 07724

Tranzarel and TALEOS are trademarks of Taleos Pharma Inc.

PRINCIPAL DISPLAY PANEL - 120 ml Tube Label

NDC 70877-2324-04

Rx Only

Tranzarel®
( Lidocaine Topical Gel ) 4%

Pain Relieving Gel

For External Use Only
Do Not Use in Eyes

Net Wt. 4 fl.oz (120ml)

TALEOS®
PHARMA

TRANZAREL 
lidocaine gel
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:70877-2324
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Lidocaine (Lidocaine) Lidocaine 4 g  in 100 mL
Inactive Ingredients
Ingredient Name Strength
Aloe Vera Leaf  
Calendula Officinalis Flower  
Green Tea Leaf  
Chamomile  
Diazolidinyl Urea  
Edetate Disodium  
Glycerin  
Menthol, Unspecified Form  
Methylparaben  
Propylene Glycol  
Propylparaben  
Water  
Alcohol  
Comfrey Leaf  
Trolamine  
Packaging
# Item Code Package Description
1 NDC:70877-2324-4 120 mL in 1 TUBE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
UNAPPROVED DRUG OTHER 01/01/2017
Labeler - Taleos Pharma (080318529)
Revised: 03/2017
 
Taleos Pharma
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