Peringatan Keamanan

Oral LD50 in mouse is 4 mg/kg MSDS. In a long-term carcinogenicity study involving rats and mice, exposure of 10 times the dose of maximum recommended clinical dose of dienogest resulted in increased incidences of pituitary adenomas, fibroepithelial mammary tumours, stromal polyps of the uterus and malignant lymphoma L932. These tumors are thought to arise from marked species differences in the optimal oestrogen:progestogen ratio for reproductive function. In rat liver foci assay, dienogest did not induce tumor promotion activity L932. Dienogest does not display genotoxic potential.

Dienogest

DB09123

small molecule approved

Deskripsi

Dienogest is an orally-active semisynthetic progestogen which also possesses the properties of 17?-hydroxyprogesterone. It is a derivative of 19-nortestosterone and has antiandrogenic properties. It is primarily used as a contraceptive in combination with ethinylestradiol, or in other combination form pills approved in United States and Europe however it is not available in the US by itself. In Europe, Australia, Malaysia, Singapore and Japan, dienogest single therapy is an approved treatment for endometriosis to alleviate painful symptoms of endometriosis and reduce endometriotic lesions A20330. Dienogest is commonly marketed as Visanne, Natazia and Qlaira.

Struktur Molekul 2D

Berat 311.425
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination half-life of dienogest is around 9-10 hours. The half-life of urinary metabolites excretion is 14 hours [L931].
Volume Distribusi The apparent volume of distribution (Vd/F) of dienogest is 40 L [L931].
Klirens (Clearance) The metabolic clearance rate from serum (Cl/F) is 64 mL/min [L931].

Absorpsi

Dienogest is rapidly absorbed following oral administration, with 91% bioavailability. The peak plasma concentration of 47 ng/mL is reached at about 1.5 hours after single ingestion of 2 mg L931. The stable concentrations of the drug are reached after two days of initial treatment A20331.

Metabolisme

Dienogest undergoes complete metabolism that is mainly mediated by CYP3A4. The metabolites are pharmacologically inactive and rapidly eliminated from the plasma.

Rute Eliminasi

The ratio of renal elimination to fecal elimination of dienogest is 3:1, where dienogest is predominantly excreted in the form of inactive metabolites. Most of orally administered drug is excreted in the urine within the first 24 hours of ingestion L931.

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of dienogest, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of dienogest and may reduce its serum concentration.
  • 3. Take at the same time every day.

Interaksi Obat

1260 Data
Acitretin The therapeutic efficacy of Dienogest can be decreased when used in combination with Acitretin.
Aprepitant The serum concentration of Dienogest can be decreased when it is combined with Aprepitant.
Atazanavir The serum concentration of Dienogest can be increased when it is combined with Atazanavir.
Boceprevir The serum concentration of Dienogest can be increased when it is combined with Boceprevir.
Prucalopride The serum concentration of Dienogest can be decreased when it is combined with Prucalopride.
Sugammadex The serum concentration of Dienogest can be decreased when it is combined with Sugammadex.
Thalidomide Dienogest may increase the thrombogenic activities of Thalidomide.
Ulipristal The therapeutic efficacy of Dienogest can be decreased when used in combination with Ulipristal.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Dienogest.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Dienogest.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Dienogest.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Dienogest.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Dienogest.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Dienogest.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Dienogest.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Dienogest.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Dienogest.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Dienogest.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Dienogest.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Dienogest.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Dienogest.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Dienogest.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Dienogest.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Dienogest.
Tranexamic acid Dienogest may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Dienogest can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Dienogest resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Dienogest resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Dienogest resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Dienogest resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Dienogest can be increased when combined with Griseofulvin.
Clobetasol propionate The serum concentration of Clobetasol propionate can be increased when it is combined with Dienogest.
Fluocinonide The serum concentration of Fluocinonide can be increased when it is combined with Dienogest.
Hydrocortisone butyrate The serum concentration of Hydrocortisone butyrate can be increased when it is combined with Dienogest.
Desoximetasone The serum concentration of Desoximetasone can be increased when it is combined with Dienogest.
Mometasone The serum concentration of Mometasone can be increased when it is combined with Dienogest.
Fluocortolone The serum concentration of Fluocortolone can be increased when it is combined with Dienogest.
Prednisolone acetate The serum concentration of Prednisolone acetate can be increased when it is combined with Dienogest.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Dienogest.
Difluocortolone The serum concentration of Difluocortolone can be increased when it is combined with Dienogest.
Flumethasone The serum concentration of Flumethasone can be increased when it is combined with Dienogest.
Methylprednisolone aceponate The serum concentration of Methylprednisolone aceponate can be increased when it is combined with Dienogest.
Vitamin A The therapeutic efficacy of Dienogest can be decreased when used in combination with Vitamin A.
Bexarotene The therapeutic efficacy of Dienogest can be decreased when used in combination with Bexarotene.
Alitretinoin The therapeutic efficacy of Dienogest can be decreased when used in combination with Alitretinoin.
Tretinoin The therapeutic efficacy of Dienogest can be decreased when used in combination with Tretinoin.
Tazarotene The therapeutic efficacy of Dienogest can be decreased when used in combination with Tazarotene.
Etretinate The therapeutic efficacy of Dienogest can be decreased when used in combination with Etretinate.
4-Oxoretinol The therapeutic efficacy of Dienogest can be decreased when used in combination with 4-Oxoretinol.
Fenretinide The therapeutic efficacy of Dienogest can be decreased when used in combination with Fenretinide.
Ro 12-7310 The therapeutic efficacy of Dienogest can be decreased when used in combination with Ro 12-7310.
Zuretinol acetate The therapeutic efficacy of Dienogest can be decreased when used in combination with Zuretinol acetate.
Motretinide The therapeutic efficacy of Dienogest can be decreased when used in combination with Motretinide.
Isotretinoin The therapeutic efficacy of Dienogest can be decreased when used in combination with Isotretinoin.
Bosentan The serum concentration of Dienogest can be decreased when it is combined with Bosentan.
Phenoxymethylpenicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Phenoxymethylpenicillin.
Carbenicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Carbenicillin.
Hetacillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Hetacillin.
Benzylpenicilloyl polylysine The therapeutic efficacy of Dienogest can be decreased when used in combination with Benzylpenicilloyl polylysine.
Mezlocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Mezlocillin.
Cyclacillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Cyclacillin.
Benzylpenicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Benzylpenicillin.
Azlocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Azlocillin.
Cloxacillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Cloxacillin.
Amdinocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Amdinocillin.
Bacampicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Bacampicillin.
Meticillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Meticillin.
Pivampicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Pivampicillin.
Pivmecillinam The therapeutic efficacy of Dienogest can be decreased when used in combination with Pivmecillinam.
Ticarcillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Ticarcillin.
Azidocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Azidocillin.
Carindacillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Carindacillin.
Sultamicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Sultamicillin.
Temocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Temocillin.
Epicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Epicillin.
Pheneticillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Pheneticillin.
Carfecillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Carfecillin.
Propicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Propicillin.
Clometocillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Clometocillin.
Sulbenicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Sulbenicillin.
Penamecillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Penamecillin.
Talampicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Talampicillin.
Aspoxicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Aspoxicillin.
Metampicillin The therapeutic efficacy of Dienogest can be decreased when used in combination with Metampicillin.
Mycophenolate mofetil The serum concentration of Dienogest can be decreased when it is combined with Mycophenolate mofetil.
Mycophenolic acid The serum concentration of Dienogest can be decreased when it is combined with Mycophenolic acid.
Nafcillin The metabolism of Dienogest can be increased when combined with Nafcillin.
Modafinil The metabolism of Dienogest can be increased when combined with Modafinil.
Etravirine The metabolism of Dienogest can be increased when combined with Etravirine.
Avasimibe The metabolism of Dienogest can be increased when combined with Avasimibe.
Echinacea The metabolism of Dienogest can be increased when combined with Echinacea.
Dexamethasone acetate The serum concentration of Dexamethasone acetate can be increased when it is combined with Dienogest.
Selegiline The bioavailability of Selegiline can be increased when combined with Dienogest.
Exenatide Exenatide can cause a decrease in the absorption of Dienogest resulting in a reduced serum concentration and potentially a decrease in efficacy.
Flibanserin The risk or severity of adverse effects can be increased when Dienogest is combined with Flibanserin.
Telaprevir The serum concentration of Dienogest can be decreased when it is combined with Telaprevir.
Cobicistat The serum concentration of Dienogest can be decreased when it is combined with Cobicistat.
Elvitegravir The serum concentration of Dienogest can be decreased when it is combined with Elvitegravir.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Dienogest.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Dienogest.

Target Protein

Progesterone receptor PGR
Androgen receptor AR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21792339
    Schindler AE: Dienogest in long-term treatment of endometriosis. Int J Womens Health. 2011;3:175-84. doi: 10.2147/IJWH.S5633. Epub 2011 Jul 6.
  • PMID: 26327902
    Binkowska M, Woron J: Progestogens in menopausal hormone therapy. Prz Menopauzalny. 2015 Jun;14(2):134-43. doi: 10.5114/pm.2015.52154. Epub 2015 Jun 22.
  • PMID: 23113924
    Hayashi A, Tanabe A, Kawabe S, Hayashi M, Yuguchi H, Yamashita Y, Okuda K, Ohmichi M: Dienogest increases the progesterone receptor isoform B/A ratio in patients with ovarian endometriosis. J Ovarian Res. 2012 Nov 1;5(1):31. doi: 10.1186/1757-2215-5-31.
  • PMID: 18061638
    Sasagawa S, Shimizu Y, Kami H, Takeuchi T, Mita S, Imada K, Kato S, Mizuguchi K: Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008 Feb;73(2):222-31. Epub 2007 Oct 22.

Contoh Produk & Brand

Produk: 13 • International brands: 0
Produk
  • Aspen-dienogest
    Tablet • 2 mg • Oral • Canada • Approved
  • Estradiol Valerate and Estradiol Valerate/Dienogest
    Kit; Tablet, film coated • - • Oral • US • Generic • Approved
  • Estradiol Valerate and Estradiol Valerate/Dienogest
    Kit; Tablet, film coated • - • Oral • US • Generic • Approved
  • Jamp Dienogest
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • M-dienogest
    Tablet • 2 mg • Oral • Canada • Approved
  • Mar-dienogest
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Natazia
    Kit • - • Oral • US • Approved
  • Natazia
    Kit • - • Oral • US • Approved
Menampilkan 8 dari 13 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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