FDA Label for Premium Lidocaine 5% Extra

Description

Usual Dosage:  See package insert for full prescribing information. 

Uses: For the temporary relief of minor aches and pains

associate with arthritis, simple backache, strain, muscle

soreness, stiffness and anorectal disorders

Warnings

WARNING: Keep out of reach of children

Store at controlled room temperature 20-25 C (68 - 77 F)

Do not permit to freeze

Dosage & Administration

DIRECTIONS: Clean area with mild soap and warm water.

Rinse and dry thoroughly. Adults and children 12 years old

and older: Apply externally to the affected area up to 6 times a day.

Children under 12 years of age: Consult a doctor.

Spl Patient Package Insert

Lidocaine - lidocaine ointment

Alivio Medical Products, LLC

LIDOCAINE OINTMENT, 5%

FOR TOPICAL USE ONLY

Rx only

DESCRIPTION

Lidocaine Ointment 5% contains a local anesthetic agent and is adminstered topically. See INDICATIONS

AND USAGE for specific uses.

Lidocaine Ointment 5% contians lidocaine, which is chemically designated as acetamide, 2-(diethylamino)-

N-(2,6-dimethylphenyl)-.

Composition of Lidocaine Ointment 5%: acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, (lidocaine)

5% in a water miscible ointment vehicle containing polyethylene glycols and peppermint oil.

CLINICAL PHARMACOLOGY

Mechanism of action

conduction of impulses, thereby affecting local anesthetic action.

Onset of anesthesia

Lidocaine OIntment 5% effects local, topical anesthesia. The onset of action is 3-5 minutes. It is ineffective

when applied to intact skin.

Hemodynamics

Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial

pressure. These changes may be attributable to a direct depressant effect of the local anesthetic agent on

various components of the cardiovascular system.

Pharmacokinetics and metabolism

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 gasdtrointestinal

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

monoethylglyvonrxylidide 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 mcg 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

halflife of this agent is typically 1.5 to 2.0 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 mcg free base per mL. In the rhesus monkey arterial blood

levels of 18-21 mcg/mL have been shown to be threshold for convulsive activity.

INDICATIONS AND USAGE

Lidocaine Ointment 5% is indicated for production of anesthesia of accessible mucous membranes of the oropharynx.

It is also useful as an anesthetic lubricant for intubation and for the temporary relief of pain associated with

minor burns, including sunburn, abrasions of the skin, and insect bites.

CONTRAINDICATIONS

Lidocaine is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the

amide type or to other components of Lidocaine Ointment 5%.

WARNINGS

EXCESSIVE DOSAGE, OR SHORT INTERVALS BETWEEN DOSES, CAN RESULT IN HIGH

PLASMA LEVELS AND SERIOUS ADVERSE EFFECTS. PATIENTS SHOULD BE INSTRUCTED

TO STRICTLY ADHERE TO THE RECOMMENDED DOSAGE AND ADMINISTRATION

GUIDELINES AS SET FORTH IN THIS PACKAGE INSERT.

THE MANAGEMENT OF SERIOUS ADVERSE REACTIONS MAY REQUIRE THE USE OF

RESUSCITATIVE EQUIPMENT, PXYGEN, AND OTHER RESUSCITATIVE DRUGS.

Lidocaine Ointment 5% should be used with extreme caution in the presence of sepsis or severely

traumatized mucosa in the area o application, since under such conditions there is the potential for rapid systemic absorption.

PRECAUTIONS

General

The safety and effectiveness of lidocaine depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies.

(See WARNINGS  and ADVERSE REACTIONS). The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels

and serious adverse effects. Repeated doses of lidocaine may cause significant increases in blood levels

with each repeated dose because of slow accumulation of the drug and/or its metabolites. Tolerance

to elevated blood levels varies with the status of the patient. Debilitated, elderly patients, acutely ill patients, and children

should be given reduced doses commensurate with their age and physical condition. Lidocaine should

also be used with caution in patients with severe shock or heart block.

Lidocaine Ointment 5% should be used with caution in patients with known drug sensitivities. Patients

allergic to paraaminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross

sensitivity to lidocaine. Many drugs used during the conduct of anesthesia are considered potential

triggering agents for familial malignant hylerthermia. Since it is not known whether amide-type local

anesthetics may trigger this reaction and since the need for supplemental general anesthesia cannot be

predicted in advance, it is suggested that a standard protocol for the management of malignant

hyperthermia should be available. Early unexplained signs of tachycardia, tachypnea, labile blood pressure

and metabolic acidosis may precede temperature elevation. Successful outcome is dependent on early

diagnosis, prompt discontinuance of the suspect triggering agent(s) and institution of treatment, including

oxygen therapy, indicated supportive measures and dantrolene (consult dantrolene sodium intravenous

package insert before using).

Information for Patients

When topical anesthetics are used in the mouth, the patient should be aware that the production of topical

anesthesia may impair swallowing and thus enhance the danger of aspiration. For this reaosn, food should

not be ingested for 60 minutes following the use of local anesthetic preparations in the mouth or throat area.

This is particularly important in children because of their frequency of eating.

Numbness of the tongue or buccal mucosa may enhance the danger of unintentional biting trauma. Food

and chewing gum should not be taken while the mouth or throat area is anesthetized.

Carcinogensis, mutagenesis, impairment of fertility

Studies of lidocaine in animals to evaluate the carcinogenic and mutagenic potential or 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 predicive 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.

Labor and Delivery

Lidocaine is not contraindicated in labor and delivery. Should Lidocaine Ointment 5% be used

concomitantly with other products containing lidocaine, the total dose contributed by all formulations

must be kept in mind.

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 lidocaine is administered to a nursing woman.

Pediatric use

Dosage in children should be reduced, commensurate with age, body weight and physical condition.

Caution must be taken to avoid overdosage when applying Lidocaine Ointment 5% to large areas of injured

or abraded skin, since the systemic absorption of lidocaine may be increased under such conditions. See

DOSAGE and ADMINISTRATION

ADVERSE REACTIONS

To report SUSPECTED ADVERSE REACTIONS, contact Hi-Tech Pharmacal Co., Inc. at 1-800-262-9010

or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Adverse experiences following the administration of lidocaine are similar in nature to those observed with

other amide local anesthetic agents. These adverse experiences are, in general, dose-related and may result

from high plasma levels caused by excessive dosage or rapid absorption, or may result form a

hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient. Serious adverse

experiences are generally systemic in nature. The following types are those most commonly reported:

Central nervous system

CNS manifestations are excitatory and/or depressant and may be characterized by lightheadedness,

nervousness, apprehension, euphoria, confusion, dizziness, tinnitus, blurred or double vision,

vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness,

respiratory depression and arrest. The excitatory manifestations may be very brief or may not occur at all,

in which case the first manifestation of toxicity may be drowsiness merging into unconsciousness and

respiratory arrest. Drowsiness following the administration of lidocaine is usually an early sign of a high blood

level of the drug and may occur as a consequence of rapid absorption/

Cardiovascular system

Cardiovascular manifestations are usually depressant and are characterized by bradycardia, hypotension,

and cardiovascular collapse, which may lead to cardiac arrest.

Allergic

Allergic reactions are characterized by cutaneous lesions, urticaria, edema or anaphylactoid reactions.

Allergic reactions may occur as a result of sensitivity either to the local anesthetic agent of to other

components in the formulation. Allergic reactions as a result of sensitivity to lidocaine are extremely rare

and, if they occur, should be managed by conventional means. The detection of sensitivity by skin testing is

of doubtful value.

OVERDOSAGE

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during

therapeutic use of local anesthetics (see ADVERSE REACTIONS, WARNINGS, and PRECAUTIONS)

Management of local anesthetic emergencies

The first consideration is prevention, best accomplished by careful and constant monitoring of

cardiovascular and respiratory vital signs  and the patient's state of consciousness after each local anesthetic

administration. At the first sign of change, oxygen should be administered.

The first step in the management of convulsions consists of immediate attention to the maintenance of a

patent airway and assisted or controlled ventilation with oxygen and a delivery system capable of

permitting immediate positive airway pressure by mask. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be elevated

keeping in mind that drugs used to treat convulsions sometimes depress the circulation when administered intravenously.

Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, small

increments of an ultra-short acting barbituate (such as thiopental or thiamylal) or a benzodiazepine (such

as diazepam) may be administered intravenously. Supportive treatment of circulatory depressions may require

administration of intravenous fluids and, when appropriate, a vasopressor as directed by the clinical

situation (e.g. ephedrine).

If not treated immediately, both convulsions and cardiovascular depression can result in hypoxia, acidosis,

bradycardia, arrythmias and cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary

resuscitative measures should be instituted.

Dialysis is of negligible value in the treatment of acute overdosage with lidocaine.

The oral LD50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the sdalt) and 214

(159-324) mg/kg (as the salt) in fasted female rats.

DOSAGE AND ADMINISTRATION

When Lidocaine Ointment 5% is used concomitantly with other products containing lidocaine, the total

dose contributed by all formulations must be kept in mind.

Adult

A single application should not exceed 5 g of Lidocaine Ointment 5%, containing 250 mg of lidocaine base

(equivalent chemically to approximately 300 mg of lidocaine hydrochloride). This is roughly equivalent to

squeezing a six (6) inch length of ointment form the tube. In a 70 kg adult this dose equals 3.6 mg/kg (1.6

mg/lb) loidocaine base. No more than one-half tube or one-third of a jar, approximately 17-20 g of ointment

or 850-1000 mg lidocaine base should be administered in any one day.

Although the incidence of adverse effects with Lidocaine Ointment 5% is quite low, caution should be

exercised, particularly when employing large amounts, since the incidence of adverse effects is directly

proportional to the total dose of local anesthetic agent administered.

Dosage for children

It is difficult to recommend a maximum dose of any drug for children since this varies as a function of age

and weight. For children less than ten years who have a normal lean body mass and a normal lean body

development, the maximum dose may be determined by the application of one of the standard pediatric

drug formulas (e.g. Clark's rule). For example a child of five years weighing 50 lbs., the dose of lidocaine

should not exceed 75-100 mg when calculated according to Clark's rule. In any case, the maximum amount of

lidocaine administered should not exceed 4.5 mg/kg (2 mg/lb) of body weight.

Administration

For medical use, apply topically for adequate control of symptoms. The use of a sterile gauze pad is

suggested for application to broken skin tissue. Apply to the tube prior to intubation.

In dentistry, apply to previously dried oral mucosa. Subsequent removal of excess saliva with cotton rolls

or saliva ejector minimizes dilution of the ointment, permits maximum penetration, and minimizes the

possibility of swallowing the topical ointment.

For use in connection with the insertion of new dentures, apply to all denture surfaces contacting mucosa.

IMPORTANT: Patients should consult a dentist at intervals not exceeding 48 hours throughou the

fitting period

HOW SUPPLIED

Lidocaine Ointment, 5% is available in 50 g (1.76 oz) laminate tube

Store at controlled room temperature 20-25 C (68-77 F). Do not permit to freeze.

Distributed By:

Alivio Medical Products, LLC

PRINCIPAL DISPLAY PANEL 50g (1.76

oz) Tube Carton

Alivio Medical Products, LLC

Hollywood, Fla.  33020

NDC 69512-030-03

Lidocaine Ointment, 5%

Rx Only

Laminate Tube

FOR TOPICAL USE ONLY

NET WT 50 g (1.76 oz)

Package Label.Principal Display Panel

copy of label - Ointment 150