Document
DailyMed Label: Lidocaine Hydrochloride and Hydrocortisone Acetate
Title
DailyMed Label: Lidocaine Hydrochloride and Hydrocortisone Acetate
Date
2024
Document type
DailyMed Prescription
Name
Lidocaine Hydrochloride and Hydrocortisone Acetate
Generic name
Lidocaine Hydrochloride and Hydrocortisone Acetate
Manufacturer
Seton Pharmaceuticals
Product information
NDC: 13925-160
Product information
NDC: 13925-160
Description
Lidocaine 3% - Hydrocortisone 0.5% Cream is indicated for the anti-inflammatory and anesthetic relief of itching, pain, soreness, and discomfort due to hemorrhoids, anal fissures, pruritus ani and similar conditions of the anal area.
Indications
Product is used for the anti-inflammatory and anesthetic relief of pruritus, pruritic eczemas, abrasions, minor burns, insect bites, pain, soreness and discomfort due to pruritus ani, pruritus vulvae, hemorrhoids, anal fissures and similar conditions of the skin and mucous membranes.
Dosage
Apply product to the affected area(s) twice daily or as directed by a
physician. If the condition does not respond to repeated courses of
product or should worsen, discontinue use and seek the advice of the
physician.
Contraindications
Product should not be used in patients with
a history of sensitivity to any of its ingredients or adverse reactions
to lidocaine or amide anesthetics, which usually do not cross-react
with “caine” ester type anesthetics. If excessive irritation and
significant worsening occur, discontinue use and seek the advice of
your physician. Product and topical lidocaine should be used
cautiously in those with impaired liver function, as well as the very
ill or very elderly and those with significant liver disease. Product
should be used with caution on patients receiving antiarrhythmic
drugs of Class I since the adverse effects are additive and generally
synergistic. This product is contraindicated for tuberculous or
fungal lesions or skin vaccinia, varicella and acute herpes simplex.
Topical corticosteroids are contraindicated in those patients with a
history of hypersensitivity to any of the components of the
preparation.
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Precautions
If irritation or sensitivity occurs or infection
appears, discontinue use and institute appropriate therapy. If
extensive areas are treated, the possibility of systemic absorption
exists. Systemic absorption of topical steroids has produced
reversible hypothalamic pituitary-adrenal (HPA) axis suppression,
manifestations of Cushing’s syndrome, hyperglycemia, and
glycosuria in some patients. Conditions which augment systemic
absorption include the application of the more potent steroids, use
over large surface areas, prolonged use, and the addition of
occlusive dressings. Therefore, patients receiving a large dose of
potent topical steroids applied to a large surface area, or under an
occlusive dressing, should be evaluated periodically for evidence of
HPA axis suppression. If noted, an attempt should be made to
withdraw the drug to reduce the frequency of application, or to
substitute a less potent steroid.
Recovery of the HPA axis function is generally prompt and complete upon
discontinuation of the drug. Infrequently, signs and symptoms of steroid
withdrawal may occur, requiring supplemental systemic corticosteroids.
Children may absorb proportionately larger amounts of topical
cortico-steroids and thus be more susceptible to systemic toxicity. If
irritation develops, topical steroids should be discontinued and
appropriate therapy instituted. In the presence of dermatological
infections, the use of an appropriate antifungal or antibacterial agent
should be instituted. If a favorable response does not occur promptly, the
corticosteroid should be discontinued until the infection has been
adequately controlled.
Adverse reactions
During, immediately, or following application of
product, there may be transient stinging or burning from open areas of
skin, or transient blanching (lightening), or erythema (redness) of the skin.
How supplied
Lidocaine 3% - Hydrocortisone 0.5% Cream is supplied as a white cream in: 1 oz (28.35 g) tubes NDC 13925-160-01 3 oz (85 g) tubes NDC 13925-160-03
Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-77°F). See USP Controlled Room Temperature. Protect from freezing.
Clinical pharmacology
Product releases lidocaine to stabilize the neuronal membrane by inhibiting the ionic fluxes required for initiation and conduction of impulses, thereby effecting local anesthetic action. Hydrocortisone acetate provides relief of inflammatory and pruritic manifestations of corticosteroid responsive dermatoses. Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), and has the following structure:
Hydrocortisone acetate has a chemical name pregn-4-ene-3, 20-dione, 21-(acetyloxy)- 11,17- dihydroxy-(11ß)-. It has the following structural formula:
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 g 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 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 g free
base per mL. In the rhesus monkey arterial blood levels of 18-21 g/mL have
been shown to be threshold for convulsive activity.
The extent of percutaneous absorption of topical corticosteroids is
determined by many factors including the vehicle, the integrity of
the epidermal barrier, and the use of occlusive dressings.
Topical corticosteroids can be absorbed from normal intact skin.
Inflammation and/or other disease processes in the skin increase
percutaneous absorption. Occlusive dressings substantially
increase the percutaneous absorption of topical corticosteroids.
Thus, occlusive dressings may be a valuable therapeutic adjunct
for treatment of resistant dermatoses.
Once absorbed through the skin, topical corticosteroids are handled
through pharmacokinetic pathways similar to systemically
administered corticosteroids. Corticosteroids are bound to plasma
protein in varying degrees. Corticosteroids are metabolized
primarily in the liver and are then excreted by the kidneys. Some of
the topical corticosteroids and their metabolites are also excreted
into the bile.
Package label
Rx Only NDC-13925-160-03 Net Wt. 3 oz. (85 g)
Lidocaine 3% Hydrocortisone 0.5% Cream
Anti-Inflammatory Anesthetic
FOR EXTERNAL USE ONLY. NOT FOR OPHTHALMIC USE.
SETON PHARMACEUTICALS
Lidocaine 3% - Hydrocortisone 0.5% Cream
1 organization
1 product
Organization
Seton Pharmaceuticals