Peringatan Keamanan

Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo.

Acitretin

DB00459

small molecule approved

Deskripsi

An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of etretinate with the advantage of a much shorter half-life when compared with etretinate.

Struktur Molekul 2D

Berat 326.4293
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 49 hours (range 33 to 96 hours)
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Oral absorption of acitretin is optimal when given with food, and is linear and proportional with increasing doses from 25 to 100 mg. Approximately 72% (range 47% to 109%) of the administered dose was absorbed after a single 50 mg dose of acitretin was given to 12 healthy subjects.

Metabolisme

Following oral absorption, acitretin undergoes extensive metabolism and interconversion by simple isomerization to its 13-cis form (cis-acitretin). Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted.

Rute Eliminasi

Both parent compound and isomer are further metabolized into chain-shortened breakdown products and conjugates, which are excreted. The chain-shortened metabolites and conjugates of acitretin and cis-acitretin are ultimately excreted in the feces (34% to 54%) and urine (16% to 53%).

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Women of childbearing age should avoid ingesting any alcohol during treatment and two months after discontinuation of acitretin. Alcohol intake increases the duration of risk for birth defects to beyond three years post acitretin discontinuation.
  • 2. Take with food. Taking acitretin with the main meal of the day improves oral absorption.

Interaksi Obat

51 Data
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Acitretin.
Megestrol acetate The therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Acitretin.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Acitretin.
Medroxyprogesterone acetate The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Acitretin.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Acitretin.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Acitretin.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Acitretin.
Drospirenone The therapeutic efficacy of Drospirenone can be decreased when used in combination with Acitretin.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Acitretin.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Acitretin.
Hydroxyprogesterone caproate The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Acitretin.
Dienogest The therapeutic efficacy of Dienogest can be decreased when used in combination with Acitretin.
Norethynodrel The therapeutic efficacy of Norethynodrel can be decreased when used in combination with Acitretin.
Norgestrel The therapeutic efficacy of Norgestrel can be decreased when used in combination with Acitretin.
Gestrinone The therapeutic efficacy of Gestrinone can be decreased when used in combination with Acitretin.
Lynestrenol The therapeutic efficacy of Lynestrenol can be decreased when used in combination with Acitretin.
Chlormadinone The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Acitretin.
Norgestrienone The therapeutic efficacy of Norgestrienone can be decreased when used in combination with Acitretin.
Quingestanol The therapeutic efficacy of Quingestanol can be decreased when used in combination with Acitretin.
Demegestone The therapeutic efficacy of Demegestone can be decreased when used in combination with Acitretin.
Nomegestrol acetate The therapeutic efficacy of Nomegestrol acetate can be decreased when used in combination with Acitretin.
Methotrexate The risk or severity of liver damage can be increased when Acitretin is combined with Methotrexate.
Ethanol Ethanol may increase the teratogenic activities of Acitretin.
Diethylstilbestrol The therapeutic efficacy of Diethylstilbestrol can be decreased when used in combination with Acitretin.
Estradiol The therapeutic efficacy of Estradiol can be decreased when used in combination with Acitretin.
Ethinylestradiol The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Acitretin.
Mestranol The therapeutic efficacy of Mestranol can be decreased when used in combination with Acitretin.
Estradiol cypionate The therapeutic efficacy of Estradiol cypionate can be decreased when used in combination with Acitretin.
Estradiol valerate The therapeutic efficacy of Estradiol valerate can be decreased when used in combination with Acitretin.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Acitretin.
Vitamin A The risk or severity of adverse effects can be increased when Vitamin A is combined with Acitretin.
Valproic acid Valproic acid may increase the Pseudotumor Cerebri activities of Acitretin.
Doxycycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Doxycycline.
Clomocycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Clomocycline.
Tigecycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Tigecycline.
Oxytetracycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Oxytetracycline.
Demeclocycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Demeclocycline.
Tetracycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Tetracycline.
Metacycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Metacycline.
Minocycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Minocycline.
Rolitetracycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Rolitetracycline.
Sarecycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Sarecycline.
Eravacycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Eravacycline.
Omadacycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Omadacycline.
Penimepicycline The risk or severity of pseudotumor cerebri can be increased when Acitretin is combined with Penimepicycline.
Pexidartinib Acitretin may increase the hepatotoxic activities of Pexidartinib.
Lymecycline The risk or severity of pseudotumor cerebri can be increased when Lymecycline is combined with Acitretin.
Palovarotene The risk or severity of adverse effects can be increased when Acitretin is combined with Palovarotene.
Valoctocogene roxaparvovec The therapeutic efficacy of Valoctocogene roxaparvovec can be decreased when used in combination with Acitretin.
Leflunomide The risk or severity of liver damage can be increased when Acitretin is combined with Leflunomide.
Teriflunomide The risk or severity of liver damage can be increased when Acitretin is combined with Teriflunomide.

Target Protein

Retinoic acid receptor RXR-alpha RXRA
Signal transducer and activator of transcription 3 STAT3
Retinoic acid receptor alpha RARA
Retinoic acid receptor beta RARB
Retinoic acid receptor gamma RARG
Retinoic acid receptor RXR-gamma RXRG
Retinoic acid receptor RXR-beta RXRB
Retinol-binding protein 1 RBP1
Retinoic acid receptor RXR

Referensi & Sumber

Synthesis reference: Yatendra Kumar, "Process for the preparation of acitretin." U.S. Patent US20040192949, issued September 30, 2004.

Contoh Produk & Brand

Produk: 51 • International brands: 1
Produk
  • Acitretin
    Capsule • 10 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 17.5 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 22.5 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 25 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 22.5 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 10 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 25 mg/1 • Oral • US • Generic • Approved
  • Acitretin
    Capsule • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 51 produk.
International Brands
  • Neotigason

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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