LIDOCAINE HYDROCHLORIDE HYDROCORTISONE ACETATE
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lidocaine hydrochloride and
hydrocortisone acetate gel
River's Edge Pharmaceuticals, LLC
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Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with AloeDESCRIPTION:
Lidocaine is chemically designated as acetamide, 2-(diethylamino)- N-(2,6 dimethylphenyl).Hydrocortisone acetate has a chemical name pregn-4-ene-3, 20-dione, 21-(acetyloxy)-11, 17-dihydroxy-(11ß)-.
ACTIVE INGREDIENTS: Lidocaine HCl 2.8%, Hydrocortisone Acetate 0.55%
INACTIVE INGREDIENTS: Purified Water, Polyethyleneglycol 200, Propylene Glycol NF, Hydroxyethylcellulose, Methylparaben NF, Citric Acid Anhydrous USP, Aloe Barbadensis (Aloe Vera) Leaf Juice, Propylparaben NF.
CLINICAL PHARMACOLOGY:
MECHANISM OF ACTION: 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.
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 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 systematic 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 (as hydrocortisone acetate) 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 skin, topical corticosteroids are handled through pharmacokinetic pathways similar to systematically administered corticosteroids. Corticosteroids are bound to plasma protein in varying degrees. Corticosteroids are metabolized primarily in the liver and are excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.
INDICATIONS:
This product is used 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.
CONTRAINDICATIONS:
This 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. River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe 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. River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe should be used with caution in patients receiving antiarrhythmic drugs of Class I since the adverse effects are additive and generally synergistic. River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe 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.
WARNINGS:
For external use only. Not for ophthalmic use. This product and used applicators could harm small children if chewed or swallowed. Individual tubes are NOT child resistant.Keep this product and applicators out of reach of children.
Topical formulations of lidocaine may be absorbed to a greater extent through mucous membranes and abraded, fissured or irritated skin rather than through intact skin. This product should not be ingested or applied into the mouth, inside of the nose or in the eyes. This product should not be used in the ears. Any situation where lidocaine penetrates beyond the tympanic membrane into the middle ear is contraindicated because of ototoxicity associated with lidocaine observed in animals when instilled in the middle ear. This product should not come into contact with the eye or be applied into the eye because of the risk of severe eye irritation and the loss of eye surface sensation which reduces protective reflexes and can lead to corneal irritation and possible abrasion. If eye contact occurs, rinse out the eye immediately with saline or water and protect the eye surface until sensation is restored.
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 corticosteroids 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.
CARCINOGENESIS, MUTAGENESIS AND IMPAIRMENT OF FERTILITY:
Long-term animal studies have not been performed to evaluate the carcinogenic potential or the effect on fertility of topical corticosteroids.
Studies to determine mutagenicity with prednisolone and hydrocortisone have revealed negative results.
Studies of lidocaine in animals to evaluate the carcinogenic and mutagenic potential of the effect on fertility have not been conducted.
USE IN PREGNANCY:
Teratogenic Effects: Pregnancy Category C
Reproduction studies have been performed for lidocaine 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. Corticosteroids are generally teratogenic in laboratory animals when administered systematically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well controlled studies in pregnant women on teratogenic effects from topical applied corticosteroids. Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.
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 this drug is administered to a nursing mother.PEDIATRIC USE:
Safety and efficacy in children have not been established.ADVERSE REACTIONS:
During or immediately following application of River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe, there may be transient stinging or burning from open areas of skin, or transient blanching (lightening), or erythema (redness) of the skin.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
DOSAGE AND ADMINISTRATION:
Apply River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe to the affected area(s) three times daily or as directed by a physician. Remove the tube from the unit box and unscrew the cap. The first time the tube is opened, remove the safety seal from the tube. Remove an applicator from the unit box and firmly screw the threaded tip onto the open tube. Do not over tighten. Squeeze the tube to push gel into the applicator until the plunger stops. While maintaining neutral pressure on the tube, separate the applicator from the tube, replace the cap, and roll the tube up from the bottom. Gently insert the tip of the filled applicator approximately ½ inch into the anal area and apply steady even pressure on the plunger applying 5 mL of River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe to the anus and the peri-anal area. Do not insert the applicator any additional length into the anus or into the rectum. Remove both parts of the applicator and discard. After the final use, also discard the tube. If directed by a physician, a small amount of the gel may be applied to the anal area using a fingertip.River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe should not be used in excess of recommendations or for prolonged use in the anal canal. If the condition does not respond to repeated courses of this product or should worsen, discontinue use and seek the advice of your physician.
HOW SUPPLIED:
River’s Edge Lidocaine HCl 2.8% - Hydrocortisone Acetate 0.55% Gel with Aloe, NDC 68032-318-15, contains one (1) multi-use 100 g tube, NDC 68032-318-95, and 15 single-use applicators.
KEEP THIS AND ALL MEDICATIONS OUT OF REACH OF CHILDREN.
Store at controlled room temperature 20°-25°C (68°-77°F).
Protect from freezing.
Manufactured for:
River’s Edge Pharmaceuticals, LLC
Suwanee, GA 30024
318-11 Iss. 09/09
PACKAGING:
| LIDOCAINE HYDROCHLORIDE HYDROCORTISONE ACETATE
lidocaine hydrochloride, hydrocortisone acetate gel |
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| Marketing Information | |||
| Marketing Category | Application Number or Monograph Citation | Marketing Start Date | Marketing End Date |
| unapproved drug other | 09/01/2008 | 04/30/2012 | |
| Labeler - River's Edge Pharmaceuticals, LLC (133879135) |