Lidocaine hcl - hydrocortisone acetate cream

Description:

Anti-Inflammatory Anesthetic for Relief of Hemorrhoid Pain, Swelling and Inflammation.
Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), and has the following structure:

Lidocaine HCl - Hydrocortisone Acetate

Hydrocortisone acetate has a chemical name pregn-4-ene-3, 20-dione, 21-(acetyloxy)-11, 17-dihydroxy-(11)-, and has the following structural formula:

Lidocaine HCl - Hydrocortisone Acetate

NGREDIENTS: PharmaPure Rx Lidocaine HCl 3% - Hydrocortisone Acetate 1% CreamEach gram contains Lidocaine HCl 30 mg, Hydrocortisone Acetate 10 mg.

ACTIVE INGREDIENTS:

LIDOCAINE HCl 3%
HYDROCORTISONE ACETATE 1%

Inactive ingredients:

ALUMINUM SULFATE, CALCIUM ACETATE, CARBOMER, CETYL ALCOHOL, CITRIC ACID, DIAZOLIDINYL UREA, GLYCERIN, GLYCERYL STEARATE, METHYLPARABEN, MINERAL OIL, PEG-100 STEARATE, PETROLATUM, PROPYLENE GLYCOL, PROPYLPARABEN, PURIFIED WATER, SODIUM CITRATE, SODIUM HYDROXIDE, SODIUM LAURYL SULFATE, SORBITAN STEARATE, STEARIC ACID, STEARYL ALCOHOL, TROLAMINE.

Clinical pharmacology:


Mechanism of action:

Product releases lidocaine to stabilize the neuronalmembrane by inhibiting the ionic fluxes required for initiation andconduction of impulses, thereby effecting local anesthetic action.Hydrocortisone acetate provides relief of inflammatory and pruriticmanifestations of corticosteroid responsive dermatoses.

Pharmacokinetics:

Lidocaine may be absorbed following topicaladministration to mucous membranes, its rate and extent of absorptiondepending upon the specific site of application, duration of exposure,concentration, and total dosage. In general, the rate of absorption oflocal anesthetic agents following topical application occurs mostrapidly after intratracheal administration. Lidocaine is alsowell-absorbed from the gastrointestinal tract, but little intact drugappears in the circulation because of biotransformation of the liver.

Lidocaineis metabolized rapidly by the liver, and metabolites and unchanged drugare excreted by the kidneys. Biotransformation includes oxidativeN-dealkylation, ring hydroxylation, cleavage of the amide linkage, andconjungation. N-dealkylation, a major pathway of biotransformation,yields the metabolites monoethylglycinexylidide and glycinexylidide. Thepharmacological/toxicological actions of these metabolites are similarto, but less potent than, those of lidocaine. Approximately 90% oflidocaine administered is excreted in the form of various metabolites,and less than 10% is excreted unchanged. The primary metabolite inurine is a conjugate of 4-hydroxy-2, 6-dimethylaniline.

Theplasma binding of lidocaine is dependent of drug concentration, and thefraction bound decreases with increasing concentration. Atconcentrations of 1 to 4 g of free base per mL, 60 to 80 percent oflidocaine is protein bound. Binding is also dependent on the plasmaconcentration of the alpha-1-acid-glycoprotein.

Lidocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

Studiesof lidocaine metabolism following intravenous bolus injections haveshown that the elimination half-life of this agent is typically 1.5 to2 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 liverdysfunction. Renal dysfunction does not affect lidocaine kinetics butmay increase the accumulation of metabolites.

Factors such asacidosis and the use of CNS stimulants and depressants affect the CNSlevels of lidocaine required to produce overt systemic effects.Objective adverse manifestations become increasingly apparent withincreasing venous plasma levels above 6 g free base per mL. In therhesus monkey arterial blood levels of 18-21 g/mL have been shown to bethe threshold for convulsive activity.

The extent of percutaneousabsorption of topical corticosteroids is determined by many factorsincluding the vehicle, the integrity of the epidermal barrier, and theuse of occlusive dressings.

Topical corticosteroids can beabsorbed from normal intact skin. Inflammation and/or other diseaseprocesses in the skin increase percutaneous absorption. Occlusivedressings substantially increase the percutaneous absorption of topicalcorticosteroids. Thus, occlusive dressings may be a valuabletherapeutic adjunct for treatment of resistant dermatoses.

Onceabsorbed through the skin, topical corticosteroids are handled throughpharmacokinetic pathways similar to systemically administeredcorticosteroids. Corticosteroids are bound to plasma protein in varyingdegrees. Corticosteroids are metabolized primarily in the liver and arethen excreted by the kidneys. Some of the topical corticosteroids andtheir metabolites are also excreted into the bile.

Indications:

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:

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 in patients receiving antiarrhythmic drugs of Class I since the adverse effects are additive and generally synergistic. 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.

Warnings:

For external use only. Not for ophthalmic use. Product and used applicators could harm small children if chewed or swallowed.

Keep out of reach of children.

Topicalformulations of lidocaine may be absorbed to a greater extent throughmucous membranes and abraded, fissured or irritated skin than throughintact skin. Product should not be ingested or applied into the mouth,inside of the nose or in the eyes. Product should not be used in theears. Any situation where lidocaine penetrates beyond the tympanicmembrane into the middle ear is contraindicted because of ototoxictyassociated with lidocaine observed in animals when instilled in themiddle ear. Product should not come into contact with the eye or beapplied into the eye because of the risk of severe eye irritation andthe loss of eye surface sensation, which reduces protective reflexes andcan lead to corneal irritation and possibly abrasion. If eye contactoccurs, rinse out the eye immediately with saline or water and protectthe eye surface until sensation is restored.

Precautions:

Ifirritation or sensitivity occurs or infection appears, discontinue useand institute appropriate therapy. If extensive areas are treated, thepossibility of systemic absorption exists. Systemic absorption of topicalsteroids has produced reversible hypothalamic-pituitary-adrenal (HPA)axis suppression, manifestation of Cushings syndrome, hyperglycemia,and glycosuria in some patients. Conditions which augment systemicabsorption include the application of the more potent steroids, use overlarge surface areas, prolonged use, and the addition of occlusivedressings. Therefore, patients receiving a large dose of potent topicalsteroids applied to a large surface area, or under an occlusivedressing, should be evaluated periodically for evidence of HPA axissuppression. If noted, an attempt should be made to withdraw the drug,to reduce the frequency of application, or to substitute a less potentsteroid. Recovery of the HPA axis function is generally prompt and completeupon discontinuation of the drug. Infrequently, signs and symptoms ofsteroid withdrawal may occur, requiring supplemental systemiccorticosteroids. Children may absorb proportionately larger amounts oftopical corticosteroids and thus be more susceptible to systemictoxicity. If irritation develops, topical steroids should bediscontinued and appropriate therapy instituted. In the presence ofdermatological infections, the use of an appropriate antifungal orantibacterial agent should be instituted. If a favorable response doesnot occur promptly, the corticosteroid should be discontinued until theinfection 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 havebeen performed for lidocaine in rats at doses up to 6.6 times the humandose and have revealed no evidence of harm to the fetus caused bylidocaine. There are, however, no adequate and well-controlled studiesin pregnant women. Animal reproduction studies are not alwayspredictive of human response. General consideration should be given tothis fact before administering lidocaine to women of childbearingpotential, especially during early pregnancy when maximum organogenesistakes place. Corticosteroids are generally teratogenic in laboratoryanimals when administered systemically at relatively low dosage levels.The more potent corticosteroids have been shown to be teratogenic afterdermal application in laboratory animals. There are no adequate andwell controlled studies in pregnant women on teratogenic effects fromtopically applied corticosteroids. Therefore, topical corticosteroidsshould be used during pregnancy only if the potential benefit justifiesthe potential risk to the fetus. Drugs of this class should not be usedextensively on pregnant patients, in large amounts or for prolongedperiods of time.

Nursing mothers:

It is notknown whether this drug is excreted in human milk. Because many drugsare excreted in human milk, caution should be exercised when this drugis administered to a nursing mother.

Pediatric use:

Safety and efficacy in children have not been established.

Adverse reactions:

During or immediately 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.

Dosage and administration:

Apply product to the affected area(s) twice daily or as directed by a physician. Product 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 product or should worsen, discontinue use and seek the advice of your physician.

Products without Applicators:Remove the child-resistant cap and foil seal from the tube. Apply a thin film to the affected area. Replace the cap after use.

Products with Single-Use Tubes and Applicators:Tear open one cleansing wipe packet (if the product kit contains such item), gently clean the affected area and discard the used cleansing wipe. Remove the child-resistant cap and foil seal from one tube and firmly screw one applicator onto the tube. Do not over tighten. Squeeze the tube to fill the applicator until a small amount of cream/gel comes out of and lubricates the applicator openings. Gently insert the applicator tip with attached tube into anal area. Continue squeezing the body of the tube as it is moved around the areas of discomfort, and lastly, around and in the anal opening (if directed by physician). Do not completely insert the applicator and tube into the anus or insert deep into the rectum. Do not insert a loose applicator tip into the anus or rectum. Once application is completed, both the tube and applicator should be gently removed and discarded.

How supplied:

PharmaPure Rx Lidocaine HCl 3% - Hydrocortisone Acetate 1% Cream KIT contains 20 Single-Use 1/4 oz (7 g) Tubes, Applicators and Cleansing Wipes. NDC 59088-771-20.

Keep this and all medications out of reach of children.

Store at 20-25C (68-77F) [see USP Controlled Room Temperature]. Protect from freezing.

Ingredients and appearance - Product information

Lidocaine hcl - hydrocortisone acetate cream- Lidocaine hcl and hydrocortisone acetate

Product information

Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC: 59088-771
Route of Administration Rectal

Active Ingredient/Active Moiety

Ingredient Name Strength
Lidocaine hydrochloride ( UNII: V13007Z41A)( Lidocaine - UNII: 98PI200987 ) 30 mgin 1 g
Hydrocortisone acetate ( UNII: 3X7931PO74)( Hydrocortisone - UNII: WI4X0X7BPJ ) 10 mgin 1 g

Inactive Ingredients

Ingredient Name Code
Aluminum sulfate ( UNII: 34S289N54E)
Calcium acetate ( UNII: Y882YXF34X)
Carbomer homopolymer type b (allyl sucrose crosslinked) ( UNII: Z135WT9208)
Cetyl alcohol ( UNII: 936JST6JCN)
Citric acid monohydrate ( UNII: 2968PHW8QP)
Diazolidinyl urea ( UNII: H5RIZ3MPW4)
Glycerin ( UNII: PDC6A3C0OX)
Glyceryl monostearate ( UNII: 230OU9XXE4)
Methylparaben ( UNII: A2I8C7HI9T)
Mineral oil ( UNII: T5L8T28FGP)
Peg-100 stearate ( UNII: YD01N1999R)
Petrolatum ( UNII: 4T6H12BN9U)
Propanediol ( UNII: 5965N8W85T)
Propylparaben ( UNII: Z8IX2SC1OH)
Water ( UNII: 059QF0KO0R)
Sodium citrate ( UNII: 1Q73Q2JULR)
Sodium hydroxide ( UNII: 55X04QC32I)
Sodium lauryl sulfate ( UNII: 368GB5141J)
Sorbitan monostearate ( UNII: NVZ4I0H58X)
Stearic acid ( UNII: 4ELV7Z65AP)
Stearyl alcohol ( UNII: 2KR89I4H1Y)
Trolamine ( UNII: 9O3K93S3TK)

Product Characteristics

Marketing Information

Marketing Category Application Number or Monograph Citation Territorial Authority Marketing Start Date
unapproved drug other USA

Labeler - PureTek Corporation( 785961046)

Tube (7 g)

Carton (20 units)