Peringatan Keamanan

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.L12873

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.L12897

Adapalene

DB00210

small molecule approved

Deskripsi

Acne vulgaris is a multifactorial disorder of the pilosebaceous unit involving increased sebum production, inflammation, and hyperproliferation/hyperkeratinization of the follicular infundibulum. It is also associated with Cutibacterium acnes (also known as Propionibacterium acnes). Adapalene is a third-generation topical retinoid used for the treatment of acne vulgaris.A193518 Adapalene has similar efficacy but a superior safety profile compared to tretinoin.A193521 Tazarotene is more efficacious than adapalene but is designated as pregnancy category X and hence is contraindicated in pregnant women.A193518 Adapalene can also be combined with benzoyl peroxide (BPO), which possesses bactericidal propertiesA193524, and either adapalene alone, or adapalene BPO combination products, are commonly used to treat mild-to-severe acne.A193518

Differin®, produced by Galderma Labs, was first granted FDA approval on May 31st, 1996, as a 0.1% adapalene topical solution. Differin was later made available as 0.1% gel, cream, or lotion, or 0.3% gel products. On December 8th, 2008, Galderma Labs gained FDA approval for Epiduo®, a 0.1% adapalene, 2.5% BPO combination gel.L12873

Struktur Molekul 2D

Berat 412.5201
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.[L12873]
Volume Distribusi -
Klirens (Clearance) Adapalene is rapidly cleared from blood plasma, typically undetectable after 72 hours following topical application.[L12873]

Absorpsi

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 Cmax of 0.553 ± 0.466 ng/ml and a mean AUC of 8.37 ± 8.46 ng\*h/ml on day 10.L12873

Metabolisme

Extensive information regarding adapalene metabolism in humans is unavailable, although it is known to accumulate in the liver and GI-tract. In human, mouse, rat, rabbit, and dog cultured hepatocytes, metabolism appears to affect the methoxybenzene moiety but remains incompletely characterized. The major products of metabolism are glucuronides. Approximately 25% of the drug is metabolized; the rest is excreted as parent drug.L12897

Rute Eliminasi

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.A193509

Interaksi Obat

2 Data
Salicylic acid The risk or severity of adverse effects can be increased when Salicylic acid is combined with Adapalene.
Resorcinol The risk or severity of adverse effects can be increased when Resorcinol is combined with Adapalene.

Target Protein

Retinoic acid receptor beta RARB
Retinoic acid receptor gamma RARG
Retinoic acid receptor RXR-beta RXRB
Retinoic acid receptor RXR-gamma RXRG
Retinoic acid receptor RXR-alpha RXRA
Transcription factor Jun JUN
Toll-like receptor 2 TLR2
Retinoic acid receptor alpha RARA
Aspartate aminotransferase, cytoplasmic GOT1

Referensi & Sumber

Synthesis reference: Graziano Castaldi, Pietro Allegrini, Gabriele Razzetti, Mauro Ercoli, "Process for the preparation of adapalene." U.S. Patent US20060229465, issued October 12, 2006.
Artikel (PubMed)
  • PMID: 19929446
    Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
  • PMID: 26947815
    Leyden J: Recent advances in the use of adapalene 0.1%/benzoyl peroxide 2.5% to treat patients with moderate to severe acne. J Dermatolog Treat. 2016;27 Suppl 1:S4-13. doi: 10.3109/09546634.2016.1145338.
  • PMID: 9703119
    Shroot B: Pharmacodynamics and pharmacokinetics of topical adapalene. J Am Acad Dermatol. 1998 Aug;39(2 Pt 3):S17-24. doi: 10.1016/s0190-9622(98)70440-2.
  • PMID: 30281982
    Zaenglein AL: Acne Vulgaris. N Engl J Med. 2018 Oct 4;379(14):1343-1352. doi: 10.1056/NEJMcp1702493.
  • PMID: 9990418
    Grosshans E, Marks R, Mascaro JM, Torras H, Meynadier J, Alirezai M, Finlay AY, Soto P, Poncet M, Verschoore M, Clucas A: Evaluation of clinical efficacy and safety of adapalene 0.1% gel versus tretinoin 0.025% gel in the treatment of acne vulgaris, with particular reference to the onset of action and impact on quality of life. Br J Dermatol. 1998 Oct;139 Suppl 52:26-33. doi: 10.1046/j.1365-2133.1998.1390s2026.x.
  • PMID: 19181031
    Leyden JJ, Wortzman M, Baldwin EK: Antibiotic-resistant Propionibacterium acnes suppressed by a benzoyl peroxide cleanser 6%. Cutis. 2008 Dec;82(6):417-21.
  • PMID: 26069148
    Beckenbach L, Baron JM, Merk HF, Loffler H, Amann PM: Retinoid treatment of skin diseases. Eur J Dermatol. 2015 Sep-Oct;25(5):384-91. doi: 10.1684/ejd.2015.2544.

Contoh Produk & Brand

Produk: 124 • International brands: 2
Produk
  • Adapalene
    Gel • 1 mg/1g • Topical • US • Generic • Approved
  • Adapalene
    Cream • 1 mg/1g • Topical • US • Generic • Approved
  • Adapalene
    Gel • 3 mg/1g • Topical • US • Generic • Approved
  • Adapalene
    Gel • 1 mg/1g • Topical • US • Generic • Approved
  • Adapalene
    Cream • 0.1 g/100g • Topical • US • Generic • Approved
  • Adapalene
    Gel • 45 g/1g • Topical • US • Generic • Approved
  • Adapalene
    Gel • 1 mg/1g • Topical • US • Generic • Approved
  • Adapalene
    Gel • 3 mg/1g • Topical • US • Generic • Approved
Menampilkan 8 dari 124 produk.
International Brands
  • Adaferin
  • Differine

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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