Peringatan Keamanan

The oral LD50 in rats is 2000 mg/kg. The dermal LD50 in rabbits is >2500 mg/kg.L45409

Reversible signs of hypervitaminosis A, such as headache, nausea, vomiting, and mucocutaneous symptoms, are expected to appear in tretinoin overdose. Overdosage with other retinoids has been associated with transient headache, facial flushing, cheilosis, abdominal pain, dizziness and ataxia: these symptoms have quickly resolved without apparent residual effects. here is no specific treatment in the case of an overdose and it is advised to treat patients experiencing tretinoin overdose in a special hematological unit.L45349

Tretinoin

DB00755

small molecule approved investigational nutraceutical

Deskripsi

Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol).A257474 It is an oxidation product in the physiological pathway of vitamin A metabolism.A257689 In human circulation, tretinoin is normally found at very low concentrations, approximately 4 to 14 nmol/L.A257689 Tretinoin exhibits anti-inflammatory, antineoplastic, antioxidant, and free radical-scavenging activities.A257689 It has been used in dermatology for many years to treat various skin conditions ranging from acne to wrinkles A257474,A258185 and activates nuclear receptors to regulate epithelial cell growth and differentiation.A257474,A257629,A257609 Tretinoin is given orally to treat acute promyelocytic leukemia L45349 and topically to treat skin conditions such as acne.L45389,L34869,L45384

Struktur Molekul 2D

Berat 300.442
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of tretinoin following initial dosing is 0.5 to 2 hours in patients with APL.[L45349]
Volume Distribusi Tretinoin is rapidly and extensively distributed to tissues following oral administration but does not cross the blood-brain barrier. The apparent volume of distribution (V<sub>d</sub>) of intravenous tretinoin is dose-dependent and significantly greater at low doses. The V<sub>d</sub> was 0.52 ± 0.12 L/kg after 0.0125 mg/kg and 0.21 ± 0.05 L/kg after 0.25 mg/kg.[A257689]
Klirens (Clearance) No information is available.

Absorpsi

Tretinoin applied topically is expected to remain on the stratum corneum and undergo minimal systemic absorption.A257684,A257699 In one study, the topical application of radiolabelled tretinoin for 28 days was associated with a total percutaneous absorption of 2%.A257684 The extent of absorption was examined after a once-daily application of 1.9 g of the combination product with benzoyl peroxide for 14 days. On Day 14, at steady-state, the mean Cmax was 0.15-0.19 ng/mL for tretinoin, 0.27-0.34 ng/mL for the metabolite 4-keto 13-cis retinoic acid, and 0.13-0.28 ng/mL for 13-cis retinoic acid, respectively. The Cmax varied across different age groups (children, adolescents, and adults). The corresponding ranges for the mean AUC0-24 were 0.63-2.06, 2.39-2.89, and 0.96-1.99 ng\*h/mL.L34869 Following oral administration, the absolute bioavailability of tretinoin was approximately 50%.L45349 While the effect of food on tretinoin is unclear, food increases the oral absorption of retinoids, as a class.L45349,L13083 When the oral dose of 22.5 mg/m2 tretinoin was administered twice daily, the mean ± SD Cmax was 394 ± 89 ng/mL after the first dose and 138 ± 139 ng/mL after one week of continuous treatment. The area under the curve (AUC) was 537 ± 191 ng·h/mL after the first dose and 249 ± 185 ng·h/mL after one week of continuous treatment. The Tmax was between one and two hours.L45349

Metabolisme

Tretinoin is rapidly metabolized to form various oxidized and conjugated metabolites. It forms several metabolites stereoisomerization derivatives (9-cis-retinoic acid or alitretinoin and 13-cis-retinoic acid or isotretinoin), oxidation derivatives (4-hydroxy-retinoic acid, 4-oxo-retinoic acid, 18-hydroxy-retinoic acid, 5,6-epoxy-retinoic acid, 3,4-didehydro-retinoic acid and retinotaurine), stereoisomerization and oxidation derivatives (13-cis-4-oxo-retinoic acid), glucuronidation derivatives (retinoyl beta-glucuronide, 13-cis-retinoyl beta-glucuronide, 4-oxo-retinoyl beta-glucuronide, 5,6-epoxyretinoyl beta-glucuronide and 13-cis-4-oxo-retinoyl beta-glucuronide), nonpolar metabolites of retinoic acid, and retinoic acid esters.A257689 Tretinoin is metabolized by several CYP enzymes, including CYP3A4, CYP2C8, and CYP2E. It also undergoes glucuronidation by UGT2B7. The metabolites 4-oxo retinoic acid and 4-oxo trans retinoic acid glucuronide have one-third of the pharmacological activity of the parent compound.A14890,L45349 When the plasma concentrations decreased to one-third of their day-one concentrations after one week of continuous therapy, tretinoin induced its own metabolism.A257689,L45349

Rute Eliminasi

Tretinoin metabolites are excreted in bile and urine.L13083 Following administration of radiolabeled tretinoin at doses of 2.75 mg and 50 mg - which are 0.53 to 9.6 times the approved recommended dosage based on 1.7 m2, respectively - approximately 63% of the radioactivity was recovered in the urine within 72 hours, and 31% appeared in the feces within six days.L45349

Interaksi Makanan

1 Data
  • 1. Take with food. Effect of food on tretinoin absorption is unclear, but food increases the bioavailability of retinoids drug class.

Interaksi Obat

985 Data
Peginterferon alfa-2a The risk or severity of cardiotoxicity can be increased when Peginterferon alfa-2a is combined with Tretinoin.
Bortezomib The risk or severity of cardiotoxicity can be increased when Bortezomib is combined with Tretinoin.
Cladribine The risk or severity of cardiotoxicity can be increased when Cladribine is combined with Tretinoin.
Carmustine The risk or severity of cardiotoxicity can be increased when Carmustine is combined with Tretinoin.
Amsacrine The risk or severity of cardiotoxicity can be increased when Amsacrine is combined with Tretinoin.
Bleomycin The risk or severity of cardiotoxicity can be increased when Bleomycin is combined with Tretinoin.
Mitomycin The risk or severity of cardiotoxicity can be increased when Mitomycin is combined with Tretinoin.
Vindesine The risk or severity of cardiotoxicity can be increased when Vindesine is combined with Tretinoin.
Indomethacin The risk or severity of elevated intracranial pressure can be increased when Indomethacin is combined with Tretinoin.
Vinorelbine The risk or severity of cardiotoxicity can be increased when Vinorelbine is combined with Tretinoin.
Beclomethasone dipropionate The metabolism of Tretinoin can be increased when combined with Beclomethasone dipropionate.
Betamethasone The metabolism of Tretinoin can be increased when combined with Betamethasone.
Epirubicin The risk or severity of cardiotoxicity can be increased when Epirubicin is combined with Tretinoin.
Chloramphenicol The metabolism of Tretinoin can be decreased when combined with Chloramphenicol.
Cisplatin The risk or severity of cardiotoxicity can be increased when Cisplatin is combined with Tretinoin.
Pentostatin The risk or severity of cardiotoxicity can be increased when Pentostatin is combined with Tretinoin.
Vinblastine The risk or severity of cardiotoxicity can be increased when Vinblastine is combined with Tretinoin.
Fluticasone propionate The metabolism of Tretinoin can be decreased when combined with Fluticasone propionate.
Linezolid The risk or severity of elevated intracranial pressure can be increased when Linezolid is combined with Tretinoin.
Imatinib The risk or severity of cardiotoxicity can be increased when Imatinib is combined with Tretinoin.
Triamcinolone The metabolism of Tretinoin can be increased when combined with Triamcinolone.
Mycophenolate mofetil The metabolism of Tretinoin can be decreased when combined with Mycophenolate mofetil.
Daunorubicin The risk or severity of cardiotoxicity can be increased when Daunorubicin is combined with Tretinoin.
Irinotecan The metabolism of Irinotecan can be decreased when combined with Tretinoin.
Sulfasalazine The risk or severity of elevated intracranial pressure can be increased when Sulfasalazine is combined with Tretinoin.
Mechlorethamine The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Mechlorethamine.
Doxorubicin The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Doxorubicin.
Thalidomide The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Thalidomide.
Fludarabine The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Fludarabine.
Arsenic trioxide The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Arsenic trioxide.
Idarubicin The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Idarubicin.
Mitoxantrone The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Mitoxantrone.
Dexamethasone The metabolism of Tretinoin can be increased when combined with Dexamethasone.
Cortisone acetate The metabolism of Tretinoin can be increased when combined with Cortisone acetate.
Paramethasone The metabolism of Tretinoin can be increased when combined with Paramethasone.
Fluticasone furoate The metabolism of Fluticasone furoate can be decreased when combined with Tretinoin.
Fluprednidene The metabolism of Tretinoin can be increased when combined with Fluprednidene.
Vilanterol The risk or severity of elevated intracranial pressure can be increased when Vilanterol is combined with Tretinoin.
Meprednisone The metabolism of Tretinoin can be increased when combined with Meprednisone.
Tepoxalin The risk or severity of elevated intracranial pressure can be increased when Tepoxalin is combined with Tretinoin.
Dexamethasone isonicotinate The metabolism of Tretinoin can be increased when combined with Dexamethasone isonicotinate.
Cortivazol The metabolism of Tretinoin can be increased when combined with Cortivazol.
Prednylidene The metabolism of Tretinoin can be increased when combined with Prednylidene.
Cloprednol The metabolism of Tretinoin can be increased when combined with Cloprednol.
Fluticasone The metabolism of Tretinoin can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Tretinoin can be increased when combined with Mometasone furoate.
Hydrocortisone acetate The metabolism of Hydrocortisone acetate can be decreased when combined with Tretinoin.
Budesonide The metabolism of Tretinoin can be increased when combined with Budesonide.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Tretinoin.
Busulfan The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Busulfan.
Clobetasol propionate The metabolism of Tretinoin can be increased when combined with Clobetasol propionate.
Fluocinonide The metabolism of Tretinoin can be increased when combined with Fluocinonide.
Hydrocortisone butyrate The metabolism of Hydrocortisone butyrate can be decreased when combined with Tretinoin.
Mometasone The metabolism of Tretinoin can be increased when combined with Mometasone.
Fluocortolone The metabolism of Tretinoin can be increased when combined with Fluocortolone.
Difluocortolone The metabolism of Tretinoin can be increased when combined with Difluocortolone.
Ponesimod The metabolism of Ponesimod can be decreased when combined with Tretinoin.
Risperidone The risk or severity of elevated intracranial pressure can be increased when Risperidone is combined with Tretinoin.
Orlistat Orlistat can cause a decrease in the absorption of Tretinoin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Mifepristone The metabolism of Tretinoin can be decreased when combined with Mifepristone.
Trastuzumab The risk or severity of cardiotoxicity can be increased when Trastuzumab is combined with Tretinoin.
Nicorandil Tretinoin may decrease the antihypertensive activities of Nicorandil.
Tacrolimus The metabolism of Tacrolimus can be decreased when combined with Tretinoin.
Menadione The risk or severity of Thrombosis can be increased when Menadione is combined with Tretinoin.
Aminocaproic acid The risk or severity of Thrombosis can be increased when Aminocaproic acid is combined with Tretinoin.
Hydrogen peroxide The risk or severity of Thrombosis can be increased when Hydrogen peroxide is combined with Tretinoin.
Aminomethylbenzoic acid The risk or severity of Thrombosis can be increased when Aminomethylbenzoic acid is combined with Tretinoin.
Camostat The risk or severity of Thrombosis can be increased when Camostat is combined with Tretinoin.
Menadione bisulfite The risk or severity of Thrombosis can be increased when Menadione bisulfite is combined with Tretinoin.
Digoxin Digoxin may decrease the cardiotoxic activities of Tretinoin.
Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Tretinoin.
Deslanoside Deslanoside may decrease the cardiotoxic activities of Tretinoin.
Ouabain Ouabain may decrease the cardiotoxic activities of Tretinoin.
Oleandrin Oleandrin may decrease the cardiotoxic activities of Tretinoin.
Cymarin Cymarin may decrease the cardiotoxic activities of Tretinoin.
Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Tretinoin.
Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Tretinoin.
Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Tretinoin.
Gitoformate Gitoformate may decrease the cardiotoxic activities of Tretinoin.
Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Tretinoin.
Peruvoside Peruvoside may decrease the cardiotoxic activities of Tretinoin.
Digitoxin Digitoxin may decrease the cardiotoxic activities of Tretinoin.
Diethylstilbestrol The therapeutic efficacy of Diethylstilbestrol can be decreased when used in combination with Tretinoin.
Estradiol The therapeutic efficacy of Estradiol can be decreased when used in combination with Tretinoin.
Ethinylestradiol The therapeutic efficacy of Ethinylestradiol can be decreased when used in combination with Tretinoin.
Mestranol The therapeutic efficacy of Mestranol can be decreased when used in combination with Tretinoin.
Estradiol cypionate The therapeutic efficacy of Estradiol cypionate can be decreased when used in combination with Tretinoin.
Estradiol valerate The therapeutic efficacy of Estradiol valerate can be decreased when used in combination with Tretinoin.
Estetrol The therapeutic efficacy of Estetrol can be decreased when used in combination with Tretinoin.
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Tretinoin.
Megestrol acetate The therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Tretinoin.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Tretinoin.
Medroxyprogesterone acetate The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Tretinoin.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Tretinoin.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Tretinoin.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Tretinoin.
Drospirenone The therapeutic efficacy of Drospirenone can be decreased when used in combination with Tretinoin.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Tretinoin.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Tretinoin.
Hydroxyprogesterone caproate The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Tretinoin.

Target Protein

Retinoic acid receptor alpha RARA
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
Cellular retinoic acid-binding protein 1 CRABP1
Retinoic acid receptor responder protein 1 RARRES1
Aldehyde dehydrogenase 1A1 ALDH1A1
Retinal dehydrogenase 2 ALDH1A2
Retinoic acid-induced protein 3 GPRC5A
Lipocalin-1 LCN1
Odorant-binding protein 2a OBP2A
Retinol-binding protein 4 RBP4
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial PDK4
Carcinoembryonic antigen

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32491410
    Yoham AL, Casadesus D: Tretinoin. .
  • PMID: 15773538
    Kang S: The mechanism of action of topical retinoids. Cutis. 2005 Feb;75(2 Suppl):10-3; discussion 13.
  • PMID: 23839179
    Baldwin HE, Nighland M, Kendall C, Mays DA, Grossman R, Newburger J: 40 years of topical tretinoin use in review. J Drugs Dermatol. 2013 Jun 1;12(6):638-42.
  • PMID: 1390184
    Thorne EG: Long-term clinical experience with a topical retinoid. Br J Dermatol. 1992 Sep;127 Suppl 41:31-6. doi: 10.1111/j.1365-2133.1992.tb16985.x.
  • PMID: 9160172
    Regazzi MB, Iacona I, Gervasutti C, Lazzarino M, Toma S: Clinical pharmacokinetics of tretinoin. Clin Pharmacokinet. 1997 May;32(5):382-402. doi: 10.2165/00003088-199732050-00004.
  • PMID: 8586032
    Gillis JC, Goa KL: Tretinoin. A review of its pharmacodynamic and pharmacokinetic properties and use in the management of acute promyelocytic leukaemia. Drugs. 1995 Nov;50(5):897-923. doi: 10.2165/00003495-199550050-00008.
  • PMID: 7663068
    Noble S, Wagstaff AJ: Tretinoin. A review of its pharmacological properties and clinical efficacy in the topical treatment of photodamaged skin. Drugs Aging. 1995 Jun;6(6):479-96. doi: 10.2165/00002512-199506060-00008.
  • PMID: 11093772
    Marill J, Cresteil T, Lanotte M, Chabot GG: Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites. Mol Pharmacol. 2000 Dec;58(6):1341-8.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 321 • International brands: 9
Produk
  • 011010 Niacinamide 4% / Tretinoin 0.025%
    Gel • - • Topical • US
  • 011013 Niacinamide 4% / Tretinoin 0.025%
    Cream • - • Topical • US
  • 011020 Niacinamide 4% / Tretinoin 0.05%
    Gel • - • Topical • US
  • 011021 Niacinamide 4% / Tretinoin 0.05%
    Cream • - • Topical • US
  • 011218 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.025%
    Gel • - • Topical • US
  • 011220 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.05%
    Gel • - • Topical • US
  • 141016 Hydrocortisone 0.5% / Hydroquinone 4% / Tretinoin 0.025%
    Emulsion • - • Topical • US
  • 141017 Hydrocortisone 0.5% / Hydroquinone 6% / Tretinoin 0.025%
    Emulsion • - • Topical • US
Menampilkan 8 dari 321 produk.
International Brands
  • Aberel — Janssen
  • Aberela — Janssen
  • Airol — Pierre Fabre Dermo
  • Dermairol — Roche
  • Eudyna — Zydus
  • Kétrel — Bailleul
  • Sotret — Ranbaxy Laboratories Inc.
  • Stieva-A — Stiefel
  • Vitinoin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul