Peringatan Keamanan

Excessive topical use may lead to marked redness, peeling, or discomfort. Oral ingestion of the drug may affect liver function causing hypertriglyceridemia. Other symptoms may include conjunctival irritation, hair loss, headache, edema, fatigue, dermatitis, nausea, and visual disturbances. Oral administration of this material to rats and rabbits at doses of 0.20 mg/kg/day (rabbits) and 0.25 mg/kg/day (rats) resulted in developmental toxicity. A no effect level of 0.05 mg/kg/day was established. Similar teratogenic effects have been reported for other retinoid compounds.

Tazarotene

DB00799

small molecule approved investigational

Deskripsi

Tazarotene, commonly marketed as Tazorac®, Avage®, and Zorac®, is member of the acetylenic class of retinoids. It is a prodrug that is found in topical formulations used in the treatment of various conditons, such as psoriasis, acne, and sun damaged skin (photodamage).

Struktur Molekul 2D

Berat 351.462
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of the active form of the drug, tazarotenic acid, is approximately 18 hours in normal and psoriatic patients.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Minimal systemic absorption of tazarotene occurs due to its rapid metabolism in the skin to the active metabolite, tazarotenic acid, which can be systemically absorbed and further metabolized. Gender had no influence on the systemic bioavailability of tazarotenic acid.

Metabolisme

Undergoes esterase hydrolysis in skin to form its active metabolite, tazarotenic acid. Tazarotenic acid is further metabolized in skin and, after systemic absorption, hepatically metabolized to sulfoxides, sulfones, and other polar products for elimination.

Rute Eliminasi

Tazarotene and tazarotenic acid were metabolized to sulfoxides, sulfones and other polar metabolites which were eliminated through urinary and fecal pathways.

Interaksi Obat

263 Data
Mifepristone The serum concentration of Tazarotene can be increased when it is combined with Mifepristone.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Tazarotene.
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Tazarotene.
Megestrol acetate The therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Tazarotene.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Tazarotene.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Tazarotene.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Tazarotene.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Tazarotene.
Drospirenone The therapeutic efficacy of Drospirenone can be decreased when used in combination with Tazarotene.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Tazarotene.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Tazarotene.
Hydroxyprogesterone caproate The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Tazarotene.
Dienogest The therapeutic efficacy of Dienogest can be decreased when used in combination with Tazarotene.
Norethynodrel The therapeutic efficacy of Norethynodrel can be decreased when used in combination with Tazarotene.
Norgestrel The therapeutic efficacy of Norgestrel can be decreased when used in combination with Tazarotene.
Gestrinone The therapeutic efficacy of Gestrinone can be decreased when used in combination with Tazarotene.
Lynestrenol The therapeutic efficacy of Lynestrenol can be decreased when used in combination with Tazarotene.
Chlormadinone The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Tazarotene.
Norgestrienone The therapeutic efficacy of Norgestrienone can be decreased when used in combination with Tazarotene.
Quingestanol The therapeutic efficacy of Quingestanol can be decreased when used in combination with Tazarotene.
Demegestone The therapeutic efficacy of Demegestone can be decreased when used in combination with Tazarotene.
Nomegestrol acetate The therapeutic efficacy of Nomegestrol acetate can be decreased when used in combination with Tazarotene.
Vitamin A The risk or severity of adverse effects can be increased when Vitamin A is combined with Tazarotene.
Secobarbital The metabolism of Tazarotene can be increased when combined with Secobarbital.
Rifampin The metabolism of Tazarotene can be increased when combined with Rifampicin.
Bexarotene The metabolism of Tazarotene can be decreased when combined with Bexarotene.
Diltiazem The metabolism of Tazarotene can be decreased when combined with Diltiazem.
Levothyroxine The metabolism of Tazarotene can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Tazarotene can be decreased when combined with Loratadine.
Quinine The metabolism of Tazarotene can be decreased when combined with Quinine.
Medroxyprogesterone acetate The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Tazarotene.
Nicardipine The metabolism of Tazarotene can be decreased when combined with Nicardipine.
Efavirenz The metabolism of Tazarotene can be decreased when combined with Efavirenz.
Tamoxifen The metabolism of Tazarotene can be decreased when combined with Tamoxifen.
Ketoconazole The metabolism of Tazarotene can be decreased when combined with Ketoconazole.
Irbesartan The metabolism of Tazarotene can be decreased when combined with Irbesartan.
Oxybutynin The metabolism of Tazarotene can be decreased when combined with Oxybutynin.
Fluvastatin The metabolism of Tazarotene can be decreased when combined with Fluvastatin.
Pioglitazone The metabolism of Tazarotene can be decreased when combined with Pioglitazone.
Saquinavir The metabolism of Tazarotene can be decreased when combined with Saquinavir.
Genistein The metabolism of Tazarotene can be decreased when combined with Genistein.
Topiroxostat The metabolism of Tazarotene can be decreased when combined with Topiroxostat.
Abiraterone The metabolism of Tazarotene can be decreased when combined with Abiraterone.
Eltrombopag The metabolism of Tazarotene can be decreased when combined with Eltrombopag.
Teriflunomide The metabolism of Tazarotene can be decreased when combined with Teriflunomide.
Enzalutamide The metabolism of Tazarotene can be decreased when combined with Enzalutamide.
Trimethoprim The metabolism of Tazarotene can be decreased when combined with Trimethoprim.
Ritonavir The metabolism of Tazarotene can be decreased when combined with Ritonavir.
Fluticasone propionate The metabolism of Tazarotene can be decreased when combined with Fluticasone propionate.
Clopidogrel The metabolism of Tazarotene can be decreased when combined with Clopidogrel.
Candesartan cilexetil The metabolism of Tazarotene can be decreased when combined with Candesartan cilexetil.
Salmeterol The metabolism of Tazarotene can be decreased when combined with Salmeterol.
Felodipine The metabolism of Tazarotene can be decreased when combined with Felodipine.
Gemfibrozil The metabolism of Tazarotene can be decreased when combined with Gemfibrozil.
Fluticasone The metabolism of Tazarotene can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Tazarotene can be decreased when combined with Mometasone furoate.
Pyrimethamine The metabolism of Tazarotene can be decreased when combined with Pyrimethamine.
Ticlopidine The metabolism of Tazarotene can be decreased when combined with Ticlopidine.
Cimetidine The metabolism of Tazarotene can be decreased when combined with Cimetidine.
Rofecoxib The metabolism of Tazarotene can be decreased when combined with Rofecoxib.
Quinidine The metabolism of Tazarotene can be decreased when combined with Quinidine.
Ketoprofen The metabolism of Tazarotene can be decreased when combined with Ketoprofen.
Fenofibrate The metabolism of Tazarotene can be decreased when combined with Fenofibrate.
Atazanavir The metabolism of Tazarotene can be decreased when combined with Atazanavir.
Tegaserod The metabolism of Tazarotene can be decreased when combined with Tegaserod.
Cabozantinib The metabolism of Tazarotene can be decreased when combined with Cabozantinib.
Diethylstilbestrol The therapeutic efficacy of Diethylstilbestrol can be decreased when used in combination with Tazarotene.
Terfenadine The metabolism of Tazarotene can be decreased when combined with Terfenadine.
Cerivastatin The metabolism of Tazarotene can be decreased when combined with Cerivastatin.
Raloxifene The metabolism of Tazarotene can be decreased when combined with Raloxifene.
Simvastatin The metabolism of Tazarotene can be decreased when combined with Simvastatin.
Nilutamide The metabolism of Tazarotene can be decreased when combined with Nilutamide.
Metronidazole The metabolism of Tazarotene can be decreased when combined with Metronidazole.
Ethinylestradiol The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Tazarotene.
Bezafibrate The metabolism of Tazarotene can be decreased when combined with Bezafibrate.
Deferasirox The metabolism of Tazarotene can be decreased when combined with Deferasirox.
Quercetin The metabolism of Tazarotene can be decreased when combined with Quercetin.
Licofelone The metabolism of Tazarotene can be decreased when combined with Licofelone.
Nilvadipine The metabolism of Tazarotene can be decreased when combined with Nilvadipine.
Sulfaphenazole The metabolism of Tazarotene can be decreased when combined with Sulfaphenazole.
Vemurafenib The metabolism of Tazarotene can be decreased when combined with Vemurafenib.
Lumacaftor The metabolism of Tazarotene can be decreased when combined with Lumacaftor.
Isavuconazole The metabolism of Tazarotene can be decreased when combined with Isavuconazole.
Alpelisib The metabolism of Tazarotene can be decreased when combined with Alpelisib.
Letermovir The metabolism of Tazarotene can be decreased when combined with Letermovir.
Triclabendazole The metabolism of Tazarotene can be decreased when combined with Triclabendazole.
Candesartan The metabolism of Tazarotene can be decreased when combined with Candesartan.
Favipiravir The metabolism of Tazarotene can be decreased when combined with Favipiravir.
Methylene blue The metabolism of Tazarotene can be decreased when combined with Methylene blue.
Mometasone The metabolism of Tazarotene can be decreased when combined with Mometasone.
Pralsetinib The metabolism of Tazarotene can be decreased when combined with Pralsetinib.
Miconazole The metabolism of Tazarotene can be decreased when combined with Miconazole.
Rilpivirine The metabolism of Tazarotene can be decreased when combined with Rilpivirine.
Rifabutin The metabolism of Tazarotene can be increased when combined with Rifabutin.
Cyclophosphamide The metabolism of Tazarotene can be increased when combined with Cyclophosphamide.
Hydrocortisone The metabolism of Tazarotene can be increased when combined with Hydrocortisone.
Probenecid The metabolism of Tazarotene can be increased when combined with Probenecid.
Ifosfamide The metabolism of Tazarotene can be increased when combined with Ifosfamide.
Rifapentine The metabolism of Tazarotene can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Tazarotene can be increased when combined with Dexamethasone.

Target Protein

Retinoic acid receptor alpha RARA
Retinoic acid receptor RXR-beta RXRB
Retinoic acid receptor gamma RARG
Retinoic acid receptor beta RARB

Referensi & Sumber

Synthesis reference: Samuele Frigoli, Claudio Fuganti, Stefano Serra, Francesco Pizzocaro, Angelo Bedeschi, Paolo Tubertini, "Process for the preparation of Tazarotene." U.S. Patent US20060205950, issued September 14, 2006.

Contoh Produk & Brand

Produk: 49 • International brands: 1
Produk
  • 011312 Niacinamide 4% / Tazarotene 0.05%
    Cream • - • Topical • US
  • Arazlo
    Lotion • 0.45 mg/1g • Topical • US • Approved
  • Arazlo
    Lotion • 0.045 % w/w • Topical • Canada • Approved
  • Avage
    Cream • 1 mg/1g • Cutaneous • US • Approved
  • Clindamycin 1% / Niacinamide 2% / Tazarotene 0.05%
    Gel • - • Topical • US
  • Duobrii
    Lotion • - • Topical • US • Approved
  • Duobrii
    Lotion • - • Topical • Canada • Approved
  • Fabior
    Aerosol, foam • 1 mg/1g • Topical • US • Approved
Menampilkan 8 dari 49 produk.
International Brands
  • Zorac

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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