Acnedap Plus

Acnedap Plus 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.

Dapsone inhibits folic acid synthesis by preventing normal bacterial utilization of PABA (Para-aminobenzoic acid).

Dapsone is a sulfone with anti-inflammatory immunosuppressive properties as well as antibacterial and antibiotic properties. Dapsone is the principal drug in a multidrug regimen recommended by the World Health Organization for the treatment of leprosy. As an anti-infective agent, it is also used for treating malaria and, recently, for Pneumocystic carinii pneumonia in AIDS patients. Dapsone is absorbed rapidly and nearly completely from the gastrointestinal tract. Dapsone is distributed throughout total body water and is present in all tissues. However, it tends to be retained in skin and muscle and especially in the liver and kidney: traces of the drug are present in these organs up to 3 weeks after therapy cessation.

Acnedap Plus
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	Acnedap Plus
Generic	Adapalene + Dapsone
Weight	0.1%
Type	Gel
Therapeutic Class
Manufacturer	Cipla Limited
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.

Dapsone is used for Primary and secondary prophylaxis of Pneumocystis (carinii) jirovecii pneumonia, Multibacillary leprosy, Paucibacillary leprosy, Dermatitis herpetiformis, Acne

Acnedap Plus is also used to associated treatment for these conditions: Acne VulgarisAcne Vulgaris, Bullous Systemic Lupus Erythematosus, Bullous dermatitis herpetiformis, Hansen's Disease, Pemphigus Vulgaris (PV), Relapsing Polychondritis, Mild Pneumocystis pneumonia, Mild Toxoplasma gondii encephalitis, Moderate Pneumocystis pneumonia, Moderate Toxoplasma gondii encephalitis, Refractory Idiopathic thrombocytopenic purpura

How Acnedap Plus 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.

Dapsone acts against bacteria and protozoa in the same way as sulphonamides, that is by inhibiting the synthesis of dihydrofolic acid through competition with para-amino-benzoate for the active site of dihydropteroate synthetase. The anti-inflammatory action of the drug is unrelated to its antibacterial action and is still not fully understood.

Dosage

Acnedap Plus 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.

Primary and secondary prophylaxis of Pneumocystis (carinii) jirovecii pneumonia:

Adult: 50 mg daily, with pyrimethamine 50 mg once wkly. Alternatively, 100 mg with pyrimethamine 50 mg twice wkly.
Child: 1 mth-18 yr: 2 mg/kg daily (max: 100 mg daily) or 4 mg/kg wkly (max: 200 mg wkly).

Multibacillary leprosy:

Adult: 100 mg daily with clofazimine 50 mg daily, together with rifampicin 600 mg and clofazimine 300 mg once a mth for 12 mth.
Child: and child 10-14 yr old: daily doses of dapsone 50 mg, or 1 to 2 mg/kg if their body-weight is low

Paucibacillary leprosy:

Adult: 100 mg daily with 600 mg rifampicin once a mth, both given for 6 mth.
Child: Reduce dose as for multibacillary leprosy.

Dermatitis herpetiformis:

Adult: Initially, 50 mg daily increased gradually to 300 mg daily if required.

Side Effects

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

Anaemia, peripheral neuropathy, haemolysis and methaemoglobinaemia (dose-related), nephrotic syndrome, psychological changes, hepatitis. Others: Nausea, vomiting, anorexia, headache, maculopapular rash, toxic epidermal necrolysis, Stevens-Johnson syndrome. Topical: Dryness, redness, oiliness and peeling at application site.

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.

Overdosage might be expected to produce nasal congestion, syncope, or hallucinations. Measures to support blood pressure should be taken if necessary.

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.

G6PD deficiency, methaemoglobin or Hb M. Perform regular blood counts and monitor liver function regularly. 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.

Decreased serum conc of dapsone when used with rifampicin. Increased plasma conc with probenecid, trimethoprim. Antagonize clofazimine.

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.

Bioavailability is 70 to 80% following oral administration.

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.

28 hours (range 10-50 hours)

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.

Renal

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 foetus (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 foetus.

Contraindication

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

Hypersensitivity. Severe anaemia, porphyria.

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.

Symptoms: nausea, vomiting, hyperexcitability (within a few min to up to 24 hr later), methemoglobin-induced depression, haemolysis (7-14 days after ingestion), seizures and severe cyanosis.

Treatment: activated charcoal (20g four times daily) and haemolysis may enhance elimination of dapsone and its monoacetyl derivative. For patients without G6PD deficiency, methemoglobinemia may be treated with methylene blue 1-2 mg/kg given by slow IV injection (repeated if methemoglobin reaccumulates) or in less severe cases, 3-5 mg/kg every 4-6 hr orally.