Adapalene

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  • Third-generation retinoid that binds to RAR receptor to modulate cellular differentiation, keratinization, and inflammation.
  • Normalization of the differentiation of follicular epithelial cells, resulting in decreased microcomedone formation.
  • Suppression of PMN chemotaxis.
  • Inhibition of  the lipo-oxygenase pathway and arachidonic acid metabolism, leading to decreased leukotriene and prostaglandin production.
  • Downregulation of AP-1 transcription factor.
  • Decreases expression of Toll-like receptor-2 (TLR-2) and decreases secretion of IL-10 cytokine along with increased expression of CD1d

Indications

  • Acne Vulgaris .
  •  Actinic keratoses.
  • Darier’s disease.
  • Dowling-Degos disease.
  • Melasma.
  • Solar lentigines.
  • Hyperpigmentation.                                                        

Dosage

  • Adapalene is available as a 0.1% gel, cream, and solution and 0.3% gel for the treatment of acne.
  • Adapalene may be applied Apply every night.
  • Apply thin film to entire face and other affected areas of the skin qPM after washing gently with non medicated soap.

Side effects

  • Erythema.
  • Scaling.
  • Dryness.
  • Pruritus.
  • Burning.
  •  Acne flaring at treated sites.

Contraindications

  • Hypersensitivity to drug/class.
  • Pregnancy.
  • Use of other topical products containing sulfur or alcohols, which can dry the skin.

Pregnancy &Lactation

  • Pregnancy Category C.
  • Topical adapalene has not been studied during breastfeeding.

Precautions

  • It is recommended that patients exercise caution with respect to ultraviolet light exposure.
  •  Avoid eyes, lips, and mucous membranes.
  •  For external use only.
  •  Adverse reaction risk higher during first month of treatment; generally subsides with use.
  •  Do not apply product to abrasions or cuts or to eczematous or sunburned skin.
  •  Skin irritation: Apply moisturizer, reduce application frequency, or discontinue.
  •  Do not wax treated area or apply topical products that may further irritate skin (eg, astringents, abrasive soaps and cleansers, exfoliants, sulfur, resorcinol, salicylic acid).
  •  Discontinue immediately and consult physician if any anaphylactoid/anaphylactic reactions occur.

Drug Info

  •  It is more stable chemically, less photolabile, and more lipophilic than other topical retenoids which enables it to penetrate follicles quickly.
  • Pharmacokinetic studies have demonstrated that only trace amounts of adapalene are systemically absorbed and
    are excreted through the hepatobiliary route.
  •  There have been no reported carcinogenic, mutagenic, or genotoxic effects of topical adapalene in both in vivo and in vitro studies. 
  •  Adapalene has also shown improvements in fine wrinkling and lentigenes in photodamaged skin.
  •  Acne exacerbation may occur in early weeks of treatment.

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