Peringatan Keamanan

If a mequinol and tretinoin combination topical product is applied excessively, some potential adverse effects like marked redness, peeling of skin, discomfort, discoloration, or hypopigmentation may occur FDA Label. Such products are not indicated for oral ingestion FDA Label.

MSDS data reports that chronic exposure to a dose of 25 UMOL/L in humans can result in mutagenic effects like DNA inhibition in lymphocytes MSDS.

Mequinol

DB09516

small molecule approved

Deskripsi

Mequinol is a phenol used in various applications. It is used as an inhibitor for acrylic monomers and acrylonitirles, as a stabilizer for chlorinated hydrocarbons and ethyl cellulose, as an ultraviolet inhibitor, as a chemical intermediate in the manufacture of antioxidants, pharmaceuticals, plasticizers, and dyestuffs L993. It is found as an active ingredient in topical drugs used for skin depigmentation indicated for the treatment of solar lentigines.

Struktur Molekul 2D

Berat 124.1372
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mequinol demonstrated an elimination half-life of 30 to 90 minutes following intravenous infusion of 5 or 10 grams/m^2 over 3 to 5 hours in melanoma patients; similar values were reported after intra-arterial infusion [L2532].
Volume Distribusi The volume of distribution is one that suggests mequinol is distributed throughout the total body water, and intracellular concentrations are not expected to vary greatly from gross measurements [L2534].
Klirens (Clearance) Readily accessible data regarding the clearance of mequinol is not available. The use of mequinol containing products is typically indicated for topical use.

Absorpsi

The systemic exposure to mequinol was assessed in eight healthy subjects following two weeks of twice-daily topical treatment of a tretinoin and mequinol combination product FDA Label. About dose of the product corresponding to about 37.3 ug/cm^2 of mequinol was applied to the subjects' backs FDA Label. The mean Cmax for mequinol was 9.92 ng/mL (range between 4.22 and 23.62 ng/mL) and the Tmax was 2 hours (range between 1 to 2 hours) FDA Label. The safety of mequinol in this combination formulation is supported by the low systemic exposures of the agent in the subjects L993.

Metabolisme

Urine samples from melanoma patients treated with mequinol were analyzed and various mequinol metabolites were identified, including 3,4-dihydroxyanisole, the two o-methyl derivatives 3-hydroxy-4-methoxyanisole and 4-hydroxy-3-methoxyanisole, and even hydroquinone which may have originated at least partly from mequinol A32735. All these identified metabolites were excreted predominantly as sulphates and glucuronides - only a small portion of the substances were present in urine in an unconjugated form A32735. Ultimately, the 3,4-dihydroxyanisole is considered the most important metabolite of mequinol A32735.

Rute Eliminasi

Mequinol is predominantly renally eliminated as its metabolites L2532, A32735.

Interaksi Obat

0 Data
Tidak ada data.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21144881
    Kumar CM, Sathisha UV, Dharmesh S, Rao AG, Singh SA: Interaction of sesamol (3,4-methylenedioxyphenol) with tyrosinase and its effect on melanin synthesis. Biochimie. 2011 Mar;93(3):562-9. doi: 10.1016/j.biochi.2010.11.014. Epub 2010 Dec 7.
  • PMID: 2587513
    Pavel S, Holden JL, Riley PA: Metabolism of 4-hydroxyanisole: identification of major urinary excretory products. Pigment Cell Res. 1989 Sep-Oct;2(5):421-6.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Solage
    Solution • - • Topical • US • Approved
  • Solagé
    Solution • - • Topical • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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