Lidocaine (ointment)

Lidocaine (ointment)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Adeel Jamil, M.D. [2]

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Overview

Lidocaine (ointment) is an amino amide, local and anesthetic agent that is FDA approved for the treatment of temporary relief of pain associated with minor burns, including sunburn, abrasions of the skin, and insect bites. Common adverse reactions include hypotension, nausea, urticaria, edema or anaphylactoid reactions..

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

• 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.

Dosing Information

• 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 17-20 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.

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 throughout the fitting period.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lidocaine (ointment) in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lidocaine (ointment) in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

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 (2.0 mg/lb) of body weight.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Lidocaine (ointment) in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Lidocaine (ointment) in pediatric patients.

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).

Adverse Reactions

Clinical Trials Experience

• 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.

Postmarketing Experience

There is limited information regarding Lidocaine (ointment) Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Lidocaine (ointment) Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): 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.

Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Lidocaine (ointment) in women who are pregnant.

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 woma

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.

Geriatic Use

There is no FDA guidance on the use of Lidocaine (ointment) in geriatric settings.

Gender

There is no FDA guidance on the use of Lidocaine (ointment) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Lidocaine (ointment) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Lidocaine (ointment) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Lidocaine (ointment) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Lidocaine (ointment) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Lidocaine (ointment) in patients who are immunocompromised.

Administration and Monitoring

Administration

• Ointment

Monitoring

There is limited information regarding Lidocaine (ointment) Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Lidocaine (ointment) and IV administrations.

Overdosage

• Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics.

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 by 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 LD50 of lidocaine HCI in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats.

Pharmacology

Lidocaine (ointment)
Systematic (IUPAC) name
2-(diethylamino)- N-(2,6-dimethylphenyl)acetamide
Identifiers
CAS number	137-58-6 73-78-9 (hydrochloride)
ATC code	C01BB01 C05AD01 (WHO) D04AB01 (WHO) N01BB02 (WHO) R02AD02 (WHO) S01HA07 (WHO) S02DA01 (WHO)
PubChem	367
DrugBank	DB00281
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	234.34 g/mol
SMILES	eMolecules & PubChem
Synonyms	N-(2,6-dimethylphenyl)-N2,N2-diethylglycinamide
Physical data
Melt. point	68 °C (154 °F)
Pharmacokinetic data
Bioavailability	35% (oral) 3% (topical)
Metabolism	Hepatic, 90% CYP1A2-mediated
Half life	1.5–2 hours
Excretion	renal
Therapeutic considerations
Pregnancy cat.	A(AU) B(US)
Legal status	Prescription Only (S4)(AU) ?(US)
Routes	intravenous, subcutaneous, topical, oral

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.

Structure

• Lidocaine Ointment 5% contains lidocaine, which is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, and has the following structural formula:

This image is provided by the National Library of Medicine.

Pharmacodynamics

• Lidocaine Ointment 5% effects local, topical anesthesia. The onset of action is 3-5 minutes. It is ineffective when applied to intact skin.

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 μg 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 2.0 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 6.0 μg free base per mL. In the rhesus monkey arterial blood levels of 18-21 μg/mL have been shown to be threshold for convulsive activity.

Nonclinical Toxicology

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

Clinical Studies

There is limited information regarding Lidocaine (ointment) Clinical Studies in the drug label.

How Supplied

Lidocaine Ointment USP, 5% is available in 35.44 g (11/4 oz) laminate tubes with a child-resistant cap, NDC 0168-0204-37.

Store at controlled room temperature 15°-30°C (59°-86°F).

E. FOUGERA & CO. A division of Fougera PHARMACEUTICALS INC. Melville, New York 11747

I220437K R10/11

1. 277

Storage

There is limited information regarding Lidocaine (ointment) Storage in the drug label.

Images

Drug Images

{{#ask: Page Name::Lidocaine (ointment) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 35.44 G CONTAINER

NDC 0168-0204-37

FOUGERA®

Rx only

CHILD-RESISTANT PACKAGE

LIDOCAINE OINTMENT USP, 5%

DO NOT USE IN THE EYES NET WT 35.44 g (1¼ Oz)

This image is provided by the National Library of Medicine.

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 35.44 G CARTON

NDC 0168-0204-37

Rx only

FOUGERA®

LIDOCAINE OINTMENT USP, 5%

Laminate Tube with Child-Resistant Cap

DO NOT USE IN THE EYES NET WT 35.44 g (1¼ Oz)

This image is provided by the National Library of Medicine.

{{#ask: Label Page::Lidocaine (ointment) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

• 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.

Precautions with Alcohol

Alcohol-Lidocaine (ointment) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Lidocaine (ointment) Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Lidocaine (ointment) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.