Lidocaine hcl cream

Description

Contains lidocaine HCl 3% in a mild acidic vehicle. Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl).

Lidocaine HCl

INGREDIENTS:Each gram of PharmaPure Rx Lidocaine HCl 3% Creamcontains Lidocaine HCl USP 3%, Inactive ingredients include: Aluminum Sulfate, Calcium Acetate, Cetyl Alcohol, Methylparaben, Mineral Oil, Petrolatum, Polysorbate 60, Propylene Glycol, Propylparaben, Purified Water, Sodium Hydroxide, Sorbitan Stearate, Stearic Acid, Stearyl Alcohol.

Clinical pharmacology

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Mechanism of action

PharmaPure Rx Lidocaine HCl 3% Cream releaseslidocaine from a mild acidic vehicle to stabilize the neuronal membraneby inhibiting the ionic fluxes required for initiation and conductionof impulses, thereby effecting local anesthetic action. A mild acidicvehicle lowers pH to increase protection against alkaline irritationsand to provide a favorable environment for healing.

Pharmacokinetics

Lidocaine may beabsorbed following topical administration to mucous membranes, its rateand extent of absorption depending upon the specific site ofapplication, duration of exposure, concentration, and total dosage. Ingeneral, the rate of absorption of local anesthetic agents followingtopical application occurs most rapidly after intratrachealadministration. Lidocaine is also well-absorbed from thegastrointestinal tract, but little intact drug appears in thecirculation because of biotransformation of the liver.

Lidocaine ismetabolized rapidly by the liver, and metabolites and unchanged drugare excreted by the kidneys. Biotransformation includes oxidativeN-dealkylation, ring hydroxylation, cleavage of the amide linkage, andconjungation. N-dealkylation, a major pathway of biotransformation,yields the metabolites monoethylglycinexylidide and glycinexlidide. Thepharmacological/toxicological actions of these metabolites are similarto, but less potent than, those of lidocaine. Approximately 90% oflidocaine administered is excreted in the form of various metabolites,and less than 10% is excreted unchanged. The primary metabolite inurine is a conjugate of 4-hydroxy-2, 6-dimethylaniline. The plasmabinding of lidocaine is dependent on drug concentration, and thefraction bound decreases with increasing concentration. Atconcentration of 1 to 4 g of free base per mL, 60 to 80 percent oflidocaine is protein bound. Binding is also dependent on the plasmaconcentration of the alpha-1-acid-glycoprotein. Lidocaine crosses theblood-brain and placental barriers, presumably by passive diffusion.Studies of lidocaine metabolism following intravenous bolus injectionshave shown that the elimination half-life of this agent is typically1.5 to 2 hours. Because of the rapid rate at which lidocaine ismetabolized, any condition that affects liver function may alterlidocaine kinetics. The half-life may be prolonged two-fold or more inpatients with liver dysfunction. Renal dysfunction does not affectlidocaine kinetics but may increase the accumulation of metabolites.Factors such as acidosis and the use of CNS stimulants and depressantsaffect the CNS levels of lidocaine required to produce overt systemiceffects. Objective adverse manifestations become increasingly apparentwith increasing venous plasma levels above 6 g free base per mL. In therhesus monkey arterial blood levels of 18-21 g/mL have been shown to bethreshold for convulsive activity.

Indications

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 shownhypersensitivity to any of its components. Lidocaine is contraindicatedin patients with a known history of hypersensitivity to localanesthetics of the amide type.

Warnings

For external use only. Not for ophthalmic use.
Keep out of reach of children.

Precautions

If irritation or sensitivity occurs or infection appears, discontinue use and institute appropriate therapy. Pharmapure Rx Lidocaine HCl 3% Creamshould be used with caution in ill, elderly, debilitated patients andchildren 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 potential of the effect on fertility have not been conducted.

Use in pregnancy


Teratogenic effects:

Teratogenic Effects; Pregnancy Category B. Reproduction studies havebeen performed for lidocaine in rats at doses up to 6.6 times the humandose and have revealed no evidence of harm to the fetus caused bylidocaine. There are, however, no adequate and well-controlled studiesin pregnant women. Animal reproduction studies are not alwayspredictive of human response. General consideration should be given tothis fact before administering lidocaine to women of childbearingpotential, especially during early pregnancy when maximum organogenesistakes place.

Nursing mothers:

It is notknown whether this drug is excreted in human milk. Because many drugsare excreted in human milk, caution should be exercised when this drugis 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 orimmediately after treatment, the skin at the site of treatment maydevelop erythema or edema or may be the locus of abnormal sensation.

Dosage and administration:

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

How supplied:

PharmaPure Rx Lidocaine HCl 3% Cream


1 oz (28.3g) tube - NDC 59088-997-03

3 oz (85 g) tube - NDC 59088-997-07

Storage and handling

Store at controlled room temperature 15 - 30 C (59 -86 F). Protect from freezing.

Ingredients and appearance - Product information

Lidocaine hcl cream- Lidocaine hcl

Product information

Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC: 59088-997
Route of Administration Topical

Active Ingredient/Active Moiety

Ingredient Name Strength
Lidocaine hydrochloride ( UNII: V13007Z41A)( Lidocaine - UNII: 98PI200987 ) 30 mgin 1 g

Inactive Ingredients

Ingredient Name Code
Aluminum sulfate ( UNII: 34S289N54E)
Calcium acetate ( UNII: Y882YXF34X)
Cetyl alcohol ( UNII: 936JST6JCN)
Methylparaben ( UNII: A2I8C7HI9T)
Mineral oil ( UNII: T5L8T28FGP)
Petrolatum ( UNII: 4T6H12BN9U)
Polysorbate 60 ( UNII: CAL22UVI4M)
Propanediol ( UNII: 5965N8W85T)
Propylparaben ( UNII: Z8IX2SC1OH)
Water ( UNII: 059QF0KO0R)
Sodium hydroxide ( UNII: 55X04QC32I)
Sorbitan monostearate ( UNII: NVZ4I0H58X)
Stearic acid ( UNII: 4ELV7Z65AP)
Stearyl alcohol ( UNII: 2KR89I4H1Y)

Product Characteristics

Marketing Information

Marketing Category Application Number or Monograph Citation Territorial Authority Marketing Start Date
unapproved drug other USA

Labeler - PureTek Corporation( 785961046)

Establishment

Name ID/FEI Business Operations
PureTek Corporation 785961046 manufacture( 59088-997)

1 oz carton label