LIDOCAINE ointment

United States - English - NLM (National Library of Medicine)

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Active ingredient:
LIDOCAINE (UNII: 98PI200987) (LIDOCAINE - UNII:98PI200987)
Available from:
St. Mary's Medical Park Pharmacy
Administration route:
TOPICAL
Prescription type:
PRESCRIPTION DRUG
Therapeutic indications:
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. 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%.
Product summary:
Lidocaine Ointment USP, 5% is supplied as a white color ointment. It is available as follows: 50 g (1 ¾ oz) double wall jar, with a child-resistant cap, NDC 60760-918-50 Pharmacist: If dispensed to a consumer, provide child resistant package for dispensing. Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Distributed by: Amneal Pharmaceuticals LLC Bridgewater, NJ 08807 Rev. 10-2017-05
Authorization status:
Abbreviated New Drug Application
Authorization number:
60760-918-50

LIDOCAINE- lidocaine ointment

St. Mary's Medical Park Pharmacy

----------

Lidocaine Ointment USP, 5%

FOR TOPICAL USE

DO NOT USE IN THE EYES

Rx Only

DESCRIPTION

Lidocaine Ointment USP, 5% contains a local anesthetic agent and is administered topically. See

INDICATIONS AND USAGE for specific uses.

Lidocaine Ointment USP, 5% contains lidocaine, USP, which is chemically designated as acetamide, 2-

(diethylamino)- N-(2,6-dimethylphenyl)-,and has the following structural formula:

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

(lidocaine) 5% in a water miscible ointment vehicle containing polyethylene glycols.

CLINICAL PHARMACOLOGY

Mechanism of action

Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and

conduction of impulses, thereby effecting local anesthetic action.

Onset of anesthesia

Lidocaine Ointment 5% effects local, topical anesthesia. The onset of action is 3 to 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

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 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-l-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 mcg free base per mL. In the rhesus

monkey arterial blood levels of 18 to 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, OXYGEN, 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 of 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 hyperthermia. 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 reason,

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.

Carcinogenesis, 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.

Usage 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.

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

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 from

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, drowsiness, 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 or 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.

To report SUSPECTED ADVERSE REACTIONS, contact Amneal Pharmaceuticals at 1-877-

835-5472 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

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 evaluated, 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 barbiturate (such as thiopental or thiamylal) or a benzodiazepine

(such as diazepam) may be administered intravenously. The clinician should be familiar, prior to use of

local anesthetics, with these anticonvulsant drugs. Supportive treatment of circulatory depression 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, arrhythmias 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 LD

of lidocaine HCI in non-fasted female rats is 459 (346 to 773) mg/kg (as the salt) and

214 (159 to 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 from the tube. In a 70 kg adult this dose

equals 3.6 mg/kg (1.6 mg/lb) lidocaine base. No more than one-half tube, approximately 17 g to 20 g of

ointment or 850 mg to 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 mg to 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.

Adminis tration

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 throughout the

fitting period.

HOW SUPPLIED

Lidocaine Ointment USP, 5% is supplied as a white color ointment.

It is available as follows:

50 g (1 ¾ oz) double wall jar, with a child-resistant cap, NDC 60760-918-50

Pharmacist: If dispensed to a consumer, provide child resistant package for dispensing.

Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F) [see USP

Controlled Room Temperature].

Distributed by:

Amneal Pharmaceuticals LLC

Bridgewater, NJ 08807

Rev. 10-2017-05

PRINCIPAL DISPLAY PANEL

LIDOCAINE

lidocaine ointment

Product Information

Product T ype

HUMAN PRESCRIPTION DRUG

Ite m Code (Source )

NDC:6 0 76 0 -9 18 (NDC:6 516 2-9 18 )

Route of Administration

TOPICAL

Active Ingredient/Active Moiety

Ingredient Name

Basis of Strength

Stre ng th

LIDO CAINE (UNII: 9 8 PI20 0 9 8 7) (LIDOCAINE - UNII:9 8 PI20 0 9 8 7)

LIDOCAINE

50 mg in 1 g

Inactive Ingredients

Ingredient Name

Stre ng th

PO LYETHYLENE GLYCO L, UNSPECIFIED (UNII: 3WJQ0 SDW1A)

Product Characteristics

Color

white

S core

S hap e

S iz e

Flavor

Imprint Code

Contains

Packag ing

#

Item Code

Package Description

Marketing Start Date

Marketing End Date

1

NDC:6 0 76 0 -9 18 -50

50 g in 1 JAR; Type 0 : No t a Co mbinatio n Pro duct

0 9 /17/20 19

St. Mary's Medical Park Pharmacy

Marketing Information

Marke ting Cate gory

Application Numbe r or Monograph Citation

Marke ting Start Date

Marke ting End Date

ANDA

ANDA20 6 29 7

0 9 /17/20 19

Labeler -

St. Mary's Medical Park Pharmacy (063050751)

Establishment

Name

Ad d re s s

ID/FEI

Busine ss Ope rations

St. Mary's Medical Park Pharmacy

0 6 30 50 751

re la be l(6 0 76 0 -9 18 )

Revised: 9/2019

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