preloder

Adapalene


Adapalene

is a third-generation
topical

retinoid

primarily used in the treatment of mild-moderate

acne

, and is also used off-label to treat keratosis pilaris as well as other
skin
conditions. It is effective against

acne

conditions where comedones are predominant
Dosing
Adult dosing:

Acne

vulgaris:

  • After washing, apply a thin film topically to affected area(s) once daily; use cream and gel at bedtime

  • Pediatric dosing:
    General Dosage Information:
  • Safety and efficacy have not been established in children less than 12 years of age

  • Acne

    vulgaris:

    12 years or older:
  • After washing, apply a thin film topically to affected area(s) once daily; use cream and gel at bedtime

  • Indications
    FDA-Labeled Indications:
  • Acne

    vulgaris

  • Mechanism of Action
    Topical:
  • The exact mechanism is not known.

    Adapalene

    exhibits some
    retinoic acid
    -like activity but it also has additional effects. It is thought that

    adapalene

    reduces important features of the pathology of

    acne

    vulgaris by normalizing the differentiation of follicular epithelial cells and keratinization to prevent microcomedone formation, similar to the mechanism of
    retinoic acid
    . Unlike
    retinoic acid
    ,

    adapalene

    selectively binds to some nuclear
    retinoic acid
    receptors (RARs) and does not bind to cellular receptors called cytosolic
    retinoic acid
    binding proteins (CRABPs). It is hypothesized that by selectively binding to certain nuclear
    retinoic acid
    receptors and not others,

    adapalene

    enhances keratinocyte differentiation without inducing epidermal hyperplasia and severe

    irritation

    , such as is seen with
    retinoic acid
    . Also,

    adapalene

    may help reduce cell-mediated inflammation, an effect demonstrated by in vitro studies.

    Adapalene

    decreases formation of comedones and inflammatory and noninflammatory

    acne

    lesions.

  • Adverse Effect
    Common:
    Dermatologic:
  • Dry
    skin
    (36.1% or less)
  • Erythema (0.2% to 21.8%)
  • Scaly
    skin
    (25.3% or less)

  • Post Marketing experience:
  • Skin

    irritation

  • Application site pain
  • Face edema
  • Eyelid edema
  • Lip swelling
  • Angioedema

  • Contraindication
    Hypersensitivity to

    adapalene

    or any of the components of the product
    Interaction
    Concomitant Topical Medications:
  • As

    adapalene

    Gel, 0.3% has the potential to induce local

    irritation

    in some
    patients
    , concomitant use of other potentially irritating
    topical
    products (medicated or abrasive soaps and cleansers, soaps and cosmetics that have a strong drying effect, and products with high concentrations of alcohol, astringents, spices, or lime) should be approached with caution. Particular caution should be exercised in using preparations containing sulfur, resorcinol, or salicylic acid in combination with

    adapalene

    Gel, 0.3%. If these preparations have been used, it is advisable not to start therapy with

    adapalene

    Gel, 0.3%, until the effects of such preparations have subsided.
  • No formal drug-drug

    interaction

    studies were conducted with

    adapalene

    Gel, 0.3%.
  • Phamacokinetics
    Absorption:
  • Bioavailability: low

  • Distribution:
  • Maximum Plasma Concentration (Cmax) of 0.553 ± 0.466 ng/mL

  • Excretion:
  • Topical
    : Biliary, major route

  • Elimination:
  • 17.2 +/- 10.2 hours

  • Precaution
  • Concurrent use of other potentially irritating
    topical
    products; increased risk of
    skin
    toxicity
  • Cuts, abrasions, eczematous, or sunburned
    skin
  • Sensitivity to sun, inherent; greater risk of
    skin
    toxicity when exposed to the sun
  • Sun exposure, high levels, including sunlamps; greater risk of
    skin
    toxicity
  • Waxing (depilatory method) of areas treated with

    adapalene

    ; risk of
    skin
    erosions
  • Pregnancy Category
  • C (FDA)
  • D (AUS)
  • Breast Feeding
  • Infant risk cannot be ruled out.
  • Monitoring
  • Improvement of

    acne

    vulgaris is indicative of efficacy
  • How to Take or Administration
  • Apply a thin film of Gel, 0.3% to the entire face and any other affected areas of the
    skin
    once daily in the evening, after washing gently with a non- medicated soap.
  • Avoid application to the areas of
    skin
    around eyes, lips, and mucous membranes. A mild transitory sensation of warmth or slight stinging may occur shortly after the application of Gel, 0.3%.
    patients
    should be instructed to minimize sun exposure.
  • Patients
    may be instructed to use moisturizers for relief of dry
    skin
    or

    irritation

    .
  • If therapeutic results are not noticed after 12 weeks of treatment, therapy should be re-evaluated.
  • For
    topical
    use only. Not for ophthalmic, oral or intravaginal use.
  • Dosage Form
    Topical
    Cream:

  • 0.1 %

  • Topical
    Gel/Jelly:

  • 0.1 %
  • 0.3 %

  • Topical
    Lotion:

  • 0.1 %

  • Patient Counselling or Clinical Teaching
  • Drug causes sun-sensitivity. Advise
    patient
    to use sunscreen and avoid tanning beds.
  • Instruct
    patient
    that cold temperatures or wind may also increase
    skin

    irritation

    during drug therapy.
  • This drug may cause a burning sensation, erythema, or dry, scaly, or irritated
    skin
    .
  • Advise
    patient
    that symptomatic improvement may not be seen for a few months.
  • Patients
    should avoid contact with the eyes, lips, angles of nose, and mucous membranes.
  • Tell
    patients
    to avoid concurrent use of
    topical
    products which may dry or irritate the
    skin
    .












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