Lidocaine Hydrochloride

LIDOCAINE HYDROCHLORIDE- lidocaine hydrochloride lotion
Stratus Pharamceuticals

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.

Topical Anesthetic

Rx only

DESCRIPTION

Contains lidocaine HCl 3%. Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), and has the following structure:

Chemical Structure
(click image for full-size original)

C14 H22 N2 O Mol.wt.234.34

Each gram of Lidocaine HCl 3% Lotion contains ACTIVE: Lidocaine HCl 30 mg in a lotion base of INACTIVES: Aluminum sulfate, calcium acetate, cetyl alcohol, glycerine, mineral oil, methyl paraben, white petrolatum, glyceryl monostearate SE, propyl paraben, purified water, sodium hydroxide, sorbitan stearate, stearic acid and stearyl alcohol

CLINICAL PHARMACOLOGY

MECHANISM OF ACTION

Lidocaine HCl 3% Lotion releases lidocaine which stabilizes the neuronal membrane by inhibiting the ionic fluxes required for initiation and conduction of impulses, thereby effecting local anesthetic action.

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 1-4 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

Pruritus, pruritic eczemas, abrasions, minor burns, insect bites, pain, soreness and discomfort due to pruritus ani, pruritus vulvae, hemorrhoids, anal fissures, and similar conditions of the skin and mucous membranes.

CONTRAINDICATIONS

Traumatized mucosa, secondary bacterial infection of the area of proposed application and known hypersensitivity to any of the 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 treatment and institute appropriate therapy. Lidocaine HCl 3% Lotion 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 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 to Lidocaine Hydrochloride

During or immediately after treatment, the skin at the site of treatment may develop erythema or edema or maybe 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

Lidocaine HCl 3% Lotion is supplied in the following size:

Size NDC#
6oz. (177 mL) Bottle 58980-822-60

KEEP THIS AND ALL MEDICATION OUT OF THE REACH OF CHILDREN.

STORAGE

Store at 25°C (77°F); excursions permitted to 15° — 30°C (59° — 86°F). Protect from freezing [See USP Controlled Room Temperature].

Distributed by:
STRATUS

Stratus Pharmaceuticals Inc.
12379 SW 130th Street
Miami, Florida 33186

Customer Service: 1-800-442-7882

Manufactured by:
Sonar Products, Inc.
Carlstadt, NJ 07072

VC-LH3%LI-2011-312

PRINCIPAL DISPLAY PANEL — 177 mL Bottle Carton

NDC 58980-822-60

TOPICAL ANESTHETIC

LIDOCAINE HCl 3% LOTION

Smooth Easily Spreadable

Rx only

STRATUS
PHARMACEUTICALS INC

Net WT. 6 OZ (177 mL)

PRINCIPAL DISPLAY PANEL -- 177 mL Bottle Carton
(click image for full-size original)
LIDOCAINE HYDROCHLORIDE
lidocaine hydrochloride lotion
Product Information
Product Type HUMAN PRESCRIPTION DRUG Item Code (Source) NDC:58980-822
Route of Administration TOPICAL DEA Schedule
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Lidocaine Hydrochloride (Lidocaine) Lidocaine Hydrochloride 5.31 mL in 177 mL
Inactive Ingredients
Ingredient Name Strength
ALUMINUM SULFATE
CALCIUM ACETATE
CETYL ALCOHOL
GLYCERIN
MINERAL OIL
METHYLPARABEN
PETROLATUM
GLYCERYL MONOSTEARATE
PROPYLPARABEN
Water
SODIUM HYDROXIDE
Sorbitan Monostearate
STEARIC ACID
STEARYL ALCOHOL
Product Characteristics
Color WHITE Score
Shape Size
Flavor Imprint Code
Contains
Packaging
# Item Code Package Description Multilevel Packaging
1 NDC:58980-822-60 1 BOTTLE (BOTTLE) in 1 BOX contains a BOTTLE
1 177 mL in 1 BOTTLE This package is contained within the BOX (58980-822-60)
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
UNAPPROVED DRUG OTHER 03/01/2012
Labeler — Stratus Pharamceuticals (789001641)
Establishment
Name Address ID/FEI Operations
Sonar Products, Inc. 104283945 MANUFACTURE (58980-822)

Revised: 01/2012 Stratus Pharamceuticals

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