United States - English - NLM (National Library of Medicine)
LIDOCAINE- lidocaine ointment
St. Mary's Medical Park Pharmacy
Lidocaine Ointment USP, 5%
FOR TOPICAL USE
DO NOT USE IN THE EYES
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.
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.
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
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
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
INDICATIONS AND USAGE
Lidocaine Ointment 5% is indicated for production of anesthesia of accessible mucous membranes of
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%.
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
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.
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.
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 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 manifestations are usually depressant and are characterized by bradycardia, hypotension,
and cardiovascular collapse, which may lead to cardiac arrest.
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.
Acute emergencies from local anesthetics are generally related to high plasma levels encountered
during therapeutic use of local anesthetics (see ADVERSE REACTIONS, WARNINGS, and
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.
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.
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
IMPORTANT: Patients should consult a dentist at intervals not exceeding 48 hours throughout the
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].
Amneal Pharmaceuticals LLC
Bridgewater, NJ 08807
PRINCIPAL DISPLAY PANEL
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
Active Ingredient/Active Moiety
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)
50 mg in 1 g
Stre ng th
PO LYETHYLENE GLYCO L, UNSPECIFIED (UNII: 3WJQ0 SDW1A)
S hap e
S iz e
Marketing Start Date
Marketing End Date
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
Marke ting Cate gory
Application Numbe r or Monograph Citation
Marke ting Start Date
Marke ting End Date
ANDA20 6 29 7
0 9 /17/20 19
St. Mary's Medical Park Pharmacy (063050751)
Ad d re s s
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 )