Facebenz A

Facebenz A Uses, Dosage, Side Effects, Food Interaction and all others data.

Adapalene is a retinoid-like compound. Biochemical and pharmacological profile studies have demonstrated that adapalene is a potent modulator of cellular differentiation, keratinisation and inflammatory processes all of which represent important features in the pathology of acne vulgaris. Adapalene binds to specific retinoic acid nuclear receptors that normalises the differentiation of follicular epithelial cells resulting in decreased microcomedone formation.

Adapalene is anticomedogenic, preventing the formation of new comedones and inflammatory lesions, and also acts to reduce inflammation by modulating the innate immune response. Like other retinoid compounds, adapalene is chemically stable but photosensitive; use with sunscreen is recommended. Minor skin irritations, including erythema, scaling, dryness, and stinging/burning, have been reported.

Benzoyl peroxide has mild keratolytic effect and antimicrobial activity due to release of free-radical oxygen which oxidizes bacterial protein. It is active against Staphylococcus epidermidis and Propionibacterium acnes.

Benzoyl peroxide is a topical treatment for acne that generates free radicals to break down comedones and increase the rate of epithelial cell turnover. It has a short duration of action as its active free radical metabolites quickly react to form inactive metabolites. The therapeutic index is wide, as overdoses are rare, however patients may still experience skin peeling. Patients should be counselled regarding increased risks of skin irritation, dryness, and sunburn.

Facebenz A
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Facebenz A
Generic	Benzoyl Peroxide + Adapalene
Weight	2.5%
Type	Gel
Therapeutic Class
Manufacturer	Zydus Cadila Healthcare Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Adapalene cream is used for the topical treatment of acne vulgaris of the face, chest or back.

Topical therapy for the treatment of acne vulgaris.

Facebenz A is also used to associated treatment for these conditions: Acne VulgarisAcne, Acne Vulgaris, Inflammatory Acne Vulgaris

How Facebenz A works

Adapalene is used for the treatment/maintenance of mild-to-severe acne (acne vulgaris). Acne is a multifactorial condition, and evidence exists to support multiple mechanisms of action for adapalene. Adapalene binds to retinoic acid receptor (RAR)-beta and RAR-gamma; this complex subsequently binds to one of three retinoid X receptors (RXRs), which as a complex is capable of binding DNA to modulate transcriptional activity. Although the full extent of transcriptional modulation is not described, retinoid activation is generally known to affect cellular proliferation and differentiation, and adapalene has been shown to inhibit HeLa cell proliferation and human keratinocyte differentiation. These effects primarily account for adapalene's comedolytic and anticomedogenic properties.

In addition, adapalene modulates the immune response by down-regulating toll-like receptor 2 (TLR-2) expression and inhibiting the transcription factor activator protein 1 (AP-1). TLR-2 recognizes Cutibacterium acnes (formerly Propionibacterium acnes), the bacterium primarily associated with acne. TLR-2 activation causes nuclear translocation of AP-1 and downstream pro-inflammatory gene regulation. Therefore, adapalene has a general anti-inflammatory effect, which reduces inflammation-mediated acne symptoms.

When used with benzoyl peroxide, which possesses free radical-mediated bactericidal effects, the combination acts synergistically to reduced comedones and inflammatory lesions.

Acne vulgaris is caused by inflammation in the pilosebaceous gland. Acne is generally caused by increased excretion of sebum from pilosebaceous glands, endocrine factors such as androgenic hormones, keratin developing around follicles, bacterial growth, and inflammation. These factors contribute to the formation of comedones (whiteheads and blackheads).

The peroxide bond of benzoyl peroxide is cleaved to form 2 benzoyloxy radicals. These radicals interact nonspecifically with bacterial proteins, interfering with their function, and survival of the bacteria. Over time, free radical interactions with bacterial proteins lead to decreased keratin and sebum around follicles.

Benzoyl peroxide can also increase the turnover rate of epithelial cells, leading to skin peeling, and breaking down comedones.

Dosage

Facebenz A dosage

A thin film topical cream should be applied to the affected areas once a day before bedtime, after washing. The affected areas should be dry before application.

Adult: As 2.5-10% preparation: Apply 1-2 times daily after cleansing, may gradually increase to tid if needed. Start with lower strength preparations.

As cleanser: Wash 1-2 times daily.

Child: ≥12 yr Same as adult dose.

Side Effects

Local reactions include burning, erythema, stinging, pruritus, dry or peeling skin. Increased sensitivity to UVB light or sunlight occurs.

The major adverse reaction reported to date with Benzoyl Peroxide cutaneous therapy is irritation of the skin including erythema, burning, peeling, dryness, itching, stinging, feeling of skin tension locally at the site of application. This is reversible when treatment is reduced in frequency or discontinued. Allergic contact dermatitis, including face oedema, may occur.

Toxicity

Toxicity information regarding adapalene is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as redness, scaling, and skin discomfort. Symptomatic and supportive measures are recommended.

Adapalene has an acute oral LD₅₀ in S-D rats and CD-1 mice of over 5000 mg/kg. The LD₅₀ of 0.3% applied topically to Credo OF1 mice is over 10 ml/kg (30 mg/kg). No systemic or local toxicity was observed in rats treated topically with 6 mg/kg/day of 0.3% adapalene.

Data regarding overdoses of benzoyl peroxide are not readily available. During an overdose patients may experience and increased risk or severity of adverse effects such as skin itching, burning, peeling, inflammation, and erythema.

The oral LD₅₀ in rats is 490 mg/kg.

Precaution

Adapalene cream should not come into contact with the eyes, lips mouth and mucous membranes, angles of the nose or broken skin (cuts and abrasions). If product enters the eye, wash with warm water. Because of a potential for increased irritation Adapalene cream should not be used by patients with eczema or seborrhoeic dermatitis. If a reaction suggesting severe irritation occurs, discontinue use of the medication. If the irritation is not severe, use the medication less frequently, discontinue use temporarily until symptoms subside, or discontinue use altogether.

Children, Pregnancy and lactation.

Interaction

Concomitant use of other potentially irritating topical products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect, products with high concentrations of alcohol, astringents, spices or lime) should be approached with caution.

Exercise particular caution in using preparations containing sulfur, resorcinol or salicylic acid in combination with Adapalene.

If any of these preparations have been used, it is advisable not to start therapy with Adapalene until the effects of such preparations in skin have subsided. If combined use of both medications is important, it is better to use in two different times.

There is no known interaction with other medications which might be used cutaneously and concurrently with Benzoyl Peroxide; however, drugs with desquamative, irritant and drying effects should not be used concurrently with Benzoyl Peroxide gel.

Elimination Route

Adapalene is applied topically and absorbed through the skin. In one clinical study treating patients once per day with 2g of 0.3% gel applied to 2 mg/cm² of skin, 15 patients had detectable blood plasma adapalene levels (0.1 ng/ml) resulting in a mean C_max of 0.553 ± 0.466 ng/ml and a mean AUC of 8.37 ± 8.46 ng*h/ml on day 10.

In a sample of excised skin, 1.9% of a radiolabelled topical dose fully penetrates the skin, and 2.6% remains in the skin. The radiolabelled dose that fully penetrates the skin is recovered as benzoic acid, while the dose in the skin is approximately half benzoic acid and half benzoyl peroxide. 95.5% of a radiolabelled dose is not absorbed or metabolized after 8 hours.

Half Life

In one clinical study, after ten days of treatment with 2g of 0.3% cream or gel, the terminal half-life was between 7 and 51 hours, with a mean of 17.2 ± 10.2.

Clearance

Adapalene is rapidly cleared from blood plasma, typically undetectable after 72 hours following topical application.

Elimination Route

Adapalene is primarily excreted by the biliary route at about 30 ng/g of the topically applied amount. Approximately 75% of the drug remains unchanged.

Benzoyl peroxide's metabolite benzoic acid, is eliminated in the urine. Data regarding fecal elimination is not readily available.

Pregnancy & Breastfeeding use

Pregnancy: Category C. There are no well-controlled studies in pregnant women.

Nursing Mothers: It is not known whether Adapalene is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Adapalene 0.1% cream is administered to a lactating mother.

Pregnancy Category C. Either studies in animals have revealed adverse effects on the fetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the fetus.

Contraindication

Adapalene should not be administered to individuals who are hypersensitive to Adapalene or any of its components.

Benzoyl Peroxide gel is contra-indicated in patients with known hypersensitivity to Benzoyl Peroxide.

Special Warning

Safety and effectiveness in children below 12 years of age have not been established.

Acute Overdose

If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, peeling or discomfort may occur.

Benzoyl Peroxide gel is a preparation indicated for topical treatment only. If the medication is applied excessively, no more rapid or better results will be obtained and severe irritation might develop. In this event, treatment must be discontinued and appropriate symptomatic therapy should be instituted.