Ambator Lidocaine Patch: Package Insert / Prescribing Information - Drugs.com

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# Ambator Lidocaine Patch

Package insert / prescribing information
Generic name: lidocaine hydrochloride
Dosage form: patch
Drug class: Topical anesthetics

Medically reviewed by Drugs.com. Last updated on Nov 21, 2022.

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.

Active ingredient:

Lidocaine HCL

Topical Anesthetic

Indications: For the temporary relief of minor pain, swelling, inflammation and stiffness caused by

arthritis, simpe backache, sprains, bruises and strains.

Warnings:

•For external use only.
•Avoid contact with eyes.
•Do not apply to wounds or damaged skin.
•Do not use with bandage, wrap, brace, stocking or similar device or garment.
•Do not use in combination with any other external analgesic products.
•If symptoms persist for more than seven days, discontinue use and consult a physician.
•Keep out of reach of children. If swallowed, consult physician.
•Do not bandage tightly.
•If pregnant of breast feeding, contact physician prior to use.

Directions:

Clean and dry affected area.
Remove patch from backing and apply to affected area.
Use only one patch at a time, and not more than four patches r day.
Children under 12 should consult physician prior to use.

Additional information: Store at room temperature. avoid direct sunlight.

Other ingredients:

Aloe Barbadensis Leaf (Aloe Vera Gel) Juice, Aqua (Purified Water), Arnica Montana Flower Extract, Boswellia Serrata Extract,

Camellia Sinensis (Green Tea) Leaf Extract, Dihydroxyaluminum Aminoacetate, Gycerol, Kaolin, Methyl Paraben, Polyacrylic

Acid, Polysorbate-80, Propyl Paraben, Propylene Glycol, PVP, Sodium Polyacrylate, Tartaric Acid, Titanium Dioxide.

AMBATOR LIDOCAINE 5% - lidocaine patch 7T PHARMA
----------

AMBATOR LIDOCAINE 5%®
(Lidocaine Patch 5%)
Lidocaine Patch 5%
Revised: September 2017
Rx Only

DESCRIPTION
Ambator Lidocaine Patch 5% is comprised of an adhesive material containing 5% lidocaine, which is
applied to a white non-woven polyethylene terephthalate (PET) material backing and covered with a
transparent PET release liner. The release liner is removed prior to application to the skin. The
size of the patch is 12.5 cm x 8.5 cm.
Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), has an
octanol:water partition ratio of 43 at pH 7.4, and has the following structure:

Each adhesive patch contains 700 mg of lidocaine (50 mg per gram adhesive) in an aqueous base. It
also contains the following inactive ingredients: Aloe Barbadensis Leaf (Aloe Vera Gel) Juice, Aqua
(Purified water), Arnica Montana Flower Extract, Boswellia Serrata Extract, Camellia Sinensis
(Green Tea) Leaf Extract, DihydroxyaluminumAminoacetate, Glycerol, Kaolin, Methyl Paraben,
Polyacrylic Acid, Polysorbate-80, Propyl Paraben, Propylene Glycol, PVP, Sodium Polyacrylate,
Tartaric Acid, Titanium Dioxide.

CLINICAL PHARMACOLOGY

Pharmacodynamics
Lidocaine is an amide-type local anesthetic agent and is suggested to stabilize neuronal membranes
by inhibiting the ionic fluxes required for the initiation and conduction of impulses.
The penetration of lidocaine into intact skin after application of lidocaine patch is sufficient to
produce an analgesic effect, but less than the amount necessary to produce a complete sensory
block.

Pharmacokinetics

Absorption:
The amount of lidocaine systemically absorbed from lidocaine patch is directly related to both the
duration of application and the surface area over which it is applied. In a pharmacokinetic study,
three lidocaine patches were applied over an area of 420 cm2 of intact skin on the back of normal
volunteers for 12 hours. Blood samples were withdrawn for determination of lidocaine concentration
during the application and for 12 hours after removal of patches. The results are summarized in
Table 1.
Table 1 Absorption of lidocaine from Lidocaine Patch Normal volunteers (n= 15, 12-hour wearing
time)

Lidocaine Patch

Application
Site Area (cm2)

Dose Absorbed (mg)

Cmax (mcg/mL)

Tmax (hr)

3 patches
(2100 mg)

Back 420 64 ± 32
0.13 ± 0.06 11 hr

When lidocaine patch is used according to the recommended dosing instructions, only 3 ± 2% of the
dose applied is expected to be absorbed. At least 95% (665 mg) of lidocaine will remain in a used
patch. Mean peak blood concentration of lidocaine is about 0.13 mcg/mL (about 1/10 of the
therapeutic concentration required to treat cardiac arrhythmias). Repeated application of three
patches simultaneously for 12 hours (recommended maximum daily dose), once per day for three days,
indicated that the lidocaine concentration does not increase with daily use. The mean plasma
pharmacokinetic profile for the 15 healthy volunteers is shown in Figure 1.

Figure 1 Mean lidocaine blood concentrations after three consecutive daily applications of three
lidocaine patches simultaneously for 12 hours per day in healthy volunteers (n = 15).

Distribution:
When lidocaine is administered intravenously to healthy volunteers, the volume of distribution is
0.7 to 2.7 L/kg (mean 1.5 ± 0.6 SD, n=15). At concentrations produced by application of lidocaine
patch, lidocaine is approximately 70% bound to plasma proteins, primarily alpha-1-acid
glycoprotein. At much higher plasma concentrations (1 to 4 mcg/mL of free base), the plasma protein
binding of lidocaine is concentration dependent. Lidocaine crosses the placental and blood brain
barriers, presumably by passive diffusion.

Metabolism:
It is not known if lidocaine is metabolized in the skin. Lidocaine is metabolized rapidly by the
liver to a number of metabolites, including monoethylglycinexylidide (MEGX) and glycinexylidide
(GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine.
A minor metabolite, 2, 6-xylidine, has unknown pharmacologic activity but is carcinogenic in rats.
The blood concentration of this metabolite is negligible following application of lidocaine patch
5%. Following intravenous administration, MEGX and GX concentrations in serum range from 11 to 36%
and from 5 to 11% of lidocaine concentrations, respectively.

Excretion:
Lidocaine and its metabolites are excreted by the kidneys. Less than 10% of lidocaine is excreted
unchanged. The half-life of lidocaine elimination from the plasma following IV administration is 81
to 149 minutes (mean 107 ± 22 SD, n = 15). The systemic clearance is 0.33 to 0.90 L/min (mean 0.64
± 0.18 SD, n = 15).

CLINICAL STUDIES
Single-dose treatment with lidocaine patch was compared to treatment with vehicle patch (without
lidocaine), and to no treatment (observation only) in a double-blind, crossover clinical trial with
35 post-herpetic neuralgia patients. Pain intensity and pain relief scores were evaluated
periodically for 12 hours. Lidocaine patch performed statistically better than vehicle patch in
terms of pain intensity from 4 to 12 hours.
Multiple-dose, two-week treatment with lidocaine patch was compared to vehicle patch (without
lidocaine) in a double-blind, crossover clinical trial of withdrawal-type design conducted in 32
patients, who were considered as responders to the open-label use of lidocaine patch prior to the
study. The constant type of pain was evaluated but not the pain induced by sensory stimuli
(dysesthesia). Statistically significant differences favoring lidocaine patch were observed in
terms of time to exit from the trial (14 versus 3.8 days at p-value <0.001), daily average pain
relief, and patient’s preference of treatment. About half of the patients also took oral medication
commonly used in the treatment of post-herpetic neuralgia. The extent of use of concomitant
medication was similar in the two treatment groups.

INDICATION AND USAGE
Ambator Lidocaine Patch is for the temporary relief of pain associated with minor cuts, minor
burns, scrapes and minor skin irritations.

CONTRAINDICATIONS

Ambator LidocainePatch is contraindicated in patients with a known history of sensitivity to local
anesthetics of the amide type, or to any other component of the product.

WARNINGS

Accidental Exposure in Children
Even a used Ambator Lidocaine Patch contains a large amount of lidocaine (at least 665 mg). The
potential exists for a small child or a pet to suffer serious adverse effects from chewing or
ingesting a new or used lidocaine patch, although the risk with this formulation has not been
evaluated. It is important for patients to store and dispose of Ambator LidocainePatch out of the
reach of children, pets and others. (See HANDLING AND DISPOSAL)

Excessive Dosing
Excessive dosing by applying Ambator LidocainePatch to larger areas or for longer than the
recommended wearing time could result in increased absorption of lidocaine and high blood
concentrations, leading to serious adverse effects (see ADVERSE REACTIONS, Systemic Reactions).
Lidocaine toxicity could be expected at lidocaine blood concentrations above 5 mcg/mL. The blood
concentration of lidocaine is determined by the rate of systemic absorption and elimination. Longer
duration of application, application of more than the recommended number of patches, smaller
patients, or impaired elimination may all contribute to increasing the blood concentration of
lidocaine. With recommended dosing of lidocaine patch 5%, the average peak blood concentration is
about 0.13 mcg/mL, but concentrations higher than 0.25 mcg/mL have been observed in some
individuals.

PRECAUTIONS

General
Hepatic Disease: Patients with severe hepatic disease are at greater risk of developing toxic blood
concentrations of lidocaine, because of their inability to metabolize lidocaine normally.
Allergic Reactions: Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine,
benzocaine, etc.) have not shown cross sensitivity to lidocaine. However, lidocaine patch 5% should
be used with caution in patients with a history of drug sensitivities, especially if the etiologic
agent is uncertain.
Non-intact Skin: Application to broken or inflamed skin, although not tested, may result in higher
blood concentrations of lidocaine from increased absorption. Lidocaine patch 5% is only recommended
for use on intact skin.
External Heat Sources: Placement of external heat sources, such as heating pads or electric
blankets, over lidocaine patch 5% is not recommended as this has not been evaluated and may
increase plasma lidocaine levels.
Eye Exposure: The contact of lidocaine patch 5% with eyes, although not studied, should be avoided
based on the findings of severe eye irritation with the use of similar products in animals. If eye
contact occurs, immediately wash out the eye with water or saline and protect the eye until
sensation returns.

Drug Interactions
Antiarrhythmic Drugs: Ambator LidocainePatch should be used with caution in patients receiving
Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the toxic effects are
additive and potentially synergistic.
Local Anesthetics: When Ambator LidocainePatch is used concomitantly with other products containing
local anesthetic agents, the amount absorbed from all formulations must be considered.

Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenesis: A minor metabolite, 2,6-xylidine, has been found to be carcinogenic in rats. The
blood concentration of this metabolite is negligible following application of Ambator
LidocainePatch.
Mutagenesis: Lidocaine HCl is not mutagenic in Salmonella/mammalian microsome test nor clastogenic
in chromosome aberration assay with human lymphocytes and mouse micronucleus test.
Impairment of Fertility: The effect of Ambator LidocainePatch on fertility has not been studied.

Pregnancy
Teratogenic Effects: Pregnancy Category B. Ambator LidocainePatch has not been studied in
pregnancy. Reproduction studies with lidocaine have been performed in rats at doses up to 30 mg/kg
subcutaneously and have revealed no evidence of harm to the fetus due to lidocaine. There are,
however, no adequate and well-controlled studies in pregnant women. Because animal reproduction
studies are not always predictive of human response, Ambator LidocainePatch should be used during
pregnancy only if clearly needed.

Labor and Delivery
Ambator LidocainePatch has not been studied in labor and delivery. Lidocaine is not contraindicated
in labor and delivery. Should Ambator LidocainePatch be used concomitantly with other products
containing lidocaine, total doses contributed by all formulations must be considered.

Nursing Mothers
Ambator LidocainePatch has not been studied in nursing mothers. Lidocaine is excreted in human
milk, and the milk:plasma ratio of lidocaine is 0.4. Caution should be exercised when Ambator
LidocainePatch is administered to a nursing woman.

Pediatric Use
Safety and effectiveness in pediatric patients have not been established.

ADVERSE REACTIONS

Application Site Reactions
During or immediately after treatment with Ambator LidocainePatch, the skin at the site of
application may develop blisters, bruising, burning sensation, depigmentation, dermatitis,
discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles, or
may be the locus of abnormal sensation. These reactions are generally mild and transient, resolving
spontaneously within a few minutes to hours.

Allergic Reactions
Allergic and anaphylactoid reactions associated with lidocaine, although rare, can occur. They are
characterized by angioedema, bronchospasm, dermatitis, dyspnea, hypersensitivity, laryngospasm,
pruritus, shock, and urticaria. If they occur, they should be managed by conventional means. The
detection of sensitivity by skin testing is of doubtful value.

Other Adverse Events
Due to the nature and limitation of spontaneous reports in postmarketing surveillance, causality
has not been established for additional reported adverse events including:
Asthenia, confusion, disorientation, dizziness, headache, hyperesthesia, hypoesthesia,
lightheadedness, metallic taste, nausea, nervousness, pain exacerbated, paresthesia, somnolence,
taste alteration, vomiting, visual disturbances such as blurred vision, flushing, tinnitus, and
tremor.

Systemic (Dose-Related) Reactions
Systemic adverse reactions following appropriate use of Ambator LidocainePatch are unlikely, due to
the small dose absorbed (see CLINICAL PHARMACOLOGY, Pharmacokinetics). Systemic adverse effects of
lidocaine are similar in nature to those observed with other amide local anesthetic agents,
including CNS excitation and/or depression (light-headedness, 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). Excitatory CNS reactions may be brief or not occur at all, in which case the first
manifestation may be drowsiness merging into unconsciousness. Cardiovascular manifestations may
include bradycardia, hypotension and cardiovascular collapse leading to arrest.
To report SUSPECTED ADVERSE REACTIONS, contact 7T Pharma at 1-800-941-2848 or FDA at 1-800-FDA-1088
or www.fda.gov/medwatch for voluntary reporting of adverse reactions.

OVERDOSAGE
Lidocaine overdose from cutaneous absorption is rare, but could occur. If there is any suspicion of
lidocaine overdose (see ADVERSE REACTIONS, Systemic Reactions), drug blood concentration should be
checked. The management of overdose includes close monitoring, supportive care, and symptomatic
treatment. Dialysis is of negligible value in the treatment of acute overdose with lidocaine.
In the absence of massive topical overdose or oral ingestion, evaluation of symptoms of toxicity
should include consideration of other etiologies for the clinical effects, or overdosage from other
sources of lidocaine or other local anesthetics.
The oral LD50 of lidocaine HCl is 459 (346 to 773) mg/kg (as the salt) in non-fasted female rats
and 214 (159 to 324) mg/kg (as the salt) in fasted female rats, which are equivalent to roughly
4000 mg and 2000 mg, respectively, in a 60 to 70 kg man based on the equivalent surface area dosage
conversion factors between species.

DOSAGE AND ADMINISTRATION
Apply Ambator LidocainePatch to intact skin to cover the most painful area. Apply the prescribed
number of patches (maximum of 3), only once for up to 12 hours within a 24-hour period. Patches may
be cut into smaller sizes with scissors prior to removal of the release liner. (See HANDLING AND
DISPOSAL) Clothing may be worn over the area of application. Smaller areas of treatment are
recommended in a debilitated patient, or a patient with impaired elimination.

If irritation or a burning sensation occurs during application, remove the patch(es) and do not
reapply until the irritation subsides.
When Ambator LidocainePatch is used concomitantly with other products containing local anesthetic
agents, the amount absorbed from all formulations must be considered.
Ambator LidocainePatch may not stick if it gets wet. Avoid contact with water, such as bathing,
swimming or showering.

HANDLING AND DISPOSAL
Hands should be washed after the handling of Ambator LidocainePatch, and eye contact with Ambator
LidocainePatch should be avoided. Do not store patch outside the sealed envelope. Apply immediately
after removal from the protective envelope. Fold used patches so that the adhesive side sticks to
itself and safely discard used patches or pieces of cut patches where children and pets cannot get
to them. Ambator LidocainePatch should be kept out of the reach of children.

HOW SUPPLIED
Ambator LidocainePatch is available as the following:
Carton of 10 patches, packaged into individual child-resistant envelopes. NDC 70645-415-01
Store at 20o to 25oC (68o to 77oF) [See USP Controlled Room Temperature].
Manufactured for: 7T Pharma
Los Angeles, CA 90064
For more information, call 7T Pharma at 1-800-941-2848. Revised: September 2017
Ambator Lidocaine Patch is a registered trademark of the manufacturer.

PRINCIPAL DISPLAY PANEL NDC70645-415-01
Ambator LidocainePatch 5%
Rx only 10 Patches

Ambator Lidocaine Patch lidocaine hcl patch

Product Information
Product Type | HUMAN PRESCRIPTION DRUG LABEL | Item Code (Source) | NDC:70645-415
Route of Administration | TOPICAL | DEA Schedule |

Active Ingredient/Active Moiety
Ingredient Name | Basis of Strength | Strength
LIDOCAINE HYDROCHLORIDE (LIDOCAINE) | LIDOCAINE HYDROCHLORIDE ANHYDROUS | 1 g in 10 g

Inactive Ingredients
Ingredient Name | Strength
ALOE VERA LEAF |
WATER |
INDIAN FRANKINCENSE |
GREEN TEA LEAF |
DIHYDROXYALUMINUM AMINOACETATE |
GLYCERIN |
KAOLIN |
METHYLPARABEN |
POLYACRYLIC ACID (8000 MW) |
POLYSORBATE 80 |
PROPYLPARABEN |
PROPYLENE GLYCOL |
POVIDONE, UNSPECIFIED |
SODIUM POLYACRYLATE (8000 MW) |
TARTARIC ACID |
TITANIUM DIOXIDE |

Packaging
# | Item Code | Package Description
1 | NDC:70645-415-01 | 10 PATCH in 1 PACKAGE
1 |  | 8 g in 1 PATCH

Marketing Information
Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date
unapproved drug other |  | 12/15/2017 |

Labeler - 7T Pharma LLC (080220022)

7T Pharma LLC

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