Peringatan Keamanan

Nearly all of the women who receive mifepristone will report adverse reactions, and many can be expected to report more than one such reaction. About 90% of patients report adverse reactions following administration of misoprostol on day three of the treatment procedure. Side effects include more heavy bleeding than a heavy menstrual period, abdominal pain, uterine cramping, nausea, vomiting, and diarrhea.

Mifepristone

DB00834

small molecule approved investigational

Deskripsi

Mifepristone is a progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary cushing syndrome. The two marketed forms of mifepristone are Mifeprex® (mifepristone 200mg) and Korlym™ (mifepristone 300mg). Currently under investigation for use in psychotic depression (phase 3 trials).

Struktur Molekul 2D

Berat 429.5937
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 18 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The absolute bioavailability of a 20 mg oral dose is 69%

Metabolisme

Hepatic. Hepatic, by Cytochrome P450 3A4 isoenzyme to the N-monodemethylated metabolite (RU 42 633); RU 42 698, which results from the loss of two methyl groups from position 11 beta; and RU 42 698, which results from terminal hydroxylation of the 17–propynyl chain.

Rute Eliminasi

Fecal: 83%; Renal: 9%.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the metabolism of mifepristone through the CYP3A4 pathway causing increased serum levels of mifepristone.
  • 2. Take with food. Taking mifepristone with meals has been shown to increase serum levels of mifepristone.

Interaksi Obat

1588 Data
Pegvisomant The risk or severity of hypoglycemia can be increased when Pegvisomant is combined with Mifepristone.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Mifepristone.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Mifepristone.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Mifepristone.
Reserpine Reserpine may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Mifepristone.
Cholic Acid Cholic Acid may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Letermovir The metabolism of Mifepristone can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Mifepristone which could result in a higher serum level.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Mifepristone.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Mifepristone.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Mifepristone.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Mifepristone.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Mifepristone.
Silodosin The excretion of Silodosin can be decreased when combined with Mifepristone.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Mifepristone.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Mifepristone.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Mifepristone.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Mifepristone.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Mifepristone.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Mifepristone.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Mifepristone.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Mifepristone.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Mifepristone.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Mifepristone.
Iloperidone The risk or severity of QTc prolongation can be increased when Mifepristone is combined with Iloperidone.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Mifepristone.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Mifepristone.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Mifepristone.
Dabigatran etexilate The serum concentration of Dabigatran etexilate can be decreased when it is combined with Mifepristone.
Linagliptin The serum concentration of Linagliptin can be decreased when it is combined with Mifepristone.
Paliperidone The serum concentration of Paliperidone can be decreased when it is combined with Mifepristone.
Sofosbuvir The serum concentration of Sofosbuvir can be decreased when it is combined with Mifepristone.
Thalidomide Mifepristone may increase the thrombogenic activities of Thalidomide.
Methysergide The serum concentration of Methysergide can be increased when it is combined with Mifepristone.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Mifepristone.
Dihydroergotamine The serum concentration of Dihydroergotamine can be increased when it is combined with Mifepristone.
Methylergometrine The serum concentration of Methylergometrine can be increased when it is combined with Mifepristone.
Lisuride The serum concentration of Lisuride can be increased when it is combined with Mifepristone.
Ergotamine The serum concentration of Ergotamine can be increased when it is combined with Mifepristone.
Nicergoline The serum concentration of Nicergoline can be increased when it is combined with Mifepristone.
Ergoloid mesylate The serum concentration of Ergoloid mesylate can be increased when it is combined with Mifepristone.
Pergolide The serum concentration of Pergolide can be increased when it is combined with Mifepristone.
Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Mifepristone.
Ergometrine The serum concentration of Ergometrine can be increased when it is combined with Mifepristone.
Lysergic acid diethylamide The serum concentration of Lysergic acid diethylamide can be increased when it is combined with Mifepristone.
Dihydroergocornine The serum concentration of Dihydroergocornine can be increased when it is combined with Mifepristone.
Dihydroergocristine The serum concentration of Dihydroergocristine can be increased when it is combined with Mifepristone.
Dihydroergocryptine The serum concentration of Dihydroergocryptine can be increased when it is combined with Mifepristone.
Terguride The serum concentration of Terguride can be increased when it is combined with Mifepristone.
Metergoline The serum concentration of Metergoline can be increased when it is combined with Mifepristone.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Mifepristone.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Mifepristone.
Ketorolac The serum concentration of Ketorolac can be increased when it is combined with Mifepristone.
Dexibuprofen The serum concentration of Dexibuprofen can be increased when it is combined with Mifepristone.
Apomorphine The serum concentration of Apomorphine can be increased when it is combined with Mifepristone.
Hydroxychloroquine The serum concentration of Hydroxychloroquine can be increased when it is combined with Mifepristone.
Troglitazone The serum concentration of Troglitazone can be increased when it is combined with Mifepristone.
Torasemide The serum concentration of Torasemide can be increased when it is combined with Mifepristone.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Mifepristone.
Dapsone The serum concentration of Dapsone can be increased when it is combined with Mifepristone.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Mifepristone.
Diethylstilbestrol The serum concentration of Diethylstilbestrol can be increased when it is combined with Mifepristone.
Theophylline The serum concentration of Theophylline can be increased when it is combined with Mifepristone.
Morphine The serum concentration of Morphine can be increased when it is combined with Mifepristone.
Diltiazem The serum concentration of Diltiazem can be increased when it is combined with Mifepristone.
Trimethadione The serum concentration of Trimethadione can be increased when it is combined with Mifepristone.
Sulfadiazine The serum concentration of Sulfadiazine can be increased when it is combined with Mifepristone.
Sorafenib The risk or severity of QTc prolongation can be increased when Mifepristone is combined with Sorafenib.
Eszopiclone The serum concentration of Eszopiclone can be increased when it is combined with Mifepristone.
Rosiglitazone The serum concentration of Rosiglitazone can be increased when it is combined with Mifepristone.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Mifepristone.
Lansoprazole The serum concentration of Lansoprazole can be increased when it is combined with Mifepristone.
Celecoxib The serum concentration of Celecoxib can be increased when it is combined with Mifepristone.
Zidovudine The serum concentration of Zidovudine can be increased when it is combined with Mifepristone.
Cyclophosphamide The serum concentration of Cyclophosphamide can be increased when it is combined with Mifepristone.
Mephenytoin The serum concentration of Mephenytoin can be increased when it is combined with Mifepristone.
Fluorouracil The serum concentration of Fluorouracil can be increased when it is combined with Mifepristone.
Piroxicam The serum concentration of Piroxicam can be increased when it is combined with Mifepristone.
Diclofenac The serum concentration of Diclofenac can be increased when it is combined with Mifepristone.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Mifepristone.
Chloroquine The serum concentration of Chloroquine can be increased when it is combined with Mifepristone.
Amodiaquine The serum concentration of Amodiaquine can be increased when it is combined with Mifepristone.
Paramethadione The serum concentration of Paramethadione can be increased when it is combined with Mifepristone.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Mifepristone.
Nicardipine The serum concentration of Nicardipine can be increased when it is combined with Mifepristone.
Verapamil The metabolism of Mifepristone can be decreased when combined with Verapamil.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Mifepristone.
Tretinoin The metabolism of Tretinoin can be decreased when combined with Mifepristone.
Estradiol The serum concentration of Estradiol can be increased when it is combined with Mifepristone.
Naproxen The serum concentration of Naproxen can be increased when it is combined with Mifepristone.
Tazarotene The serum concentration of Tazarotene can be increased when it is combined with Mifepristone.
Propofol The serum concentration of Propofol can be increased when it is combined with Mifepristone.
Loperamide The serum concentration of Loperamide can be increased when it is combined with Mifepristone.
Terbinafine The serum concentration of Terbinafine can be increased when it is combined with Mifepristone.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Mifepristone.

Target Protein

Progesterone receptor PGR
Glucocorticoid receptor NR3C1
Prostate-specific antigen KLK3
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Narendra Joshi, Anil Khile, Nitin Pradhan, "Novel polymorph form M of mifepristone and process for its preparation." U.S. Patent US20070105828, issued May 10, 2007.
Artikel (PubMed)
  • PMID: 16781264
    Fiala C, Gemzel-Danielsson K: Review of medical abortion using mifepristone in combination with a prostaglandin analogue. Contraception. 2006 Jul;74(1):66-86. Epub 2006 May 19.
  • PMID: 14698071
    Heikinheimo O, Kekkonen R, Lahteenmaki P: The pharmacokinetics of mifepristone in humans reveal insights into differential mechanisms of antiprogestin action. Contraception. 2003 Dec;68(6):421-6.
  • PMID: 15790602
    Chabbert-Buffet N, Meduri G, Bouchard P, Spitz IM: Selective progesterone receptor modulators and progesterone antagonists: mechanisms of action and clinical applications. Hum Reprod Update. 2005 May-Jun;11(3):293-307. Epub 2005 Mar 24.
  • PMID: 9562577
    Spitz IM, Bardin CW, Benton L, Robbins A: Early pregnancy termination with mifepristone and misoprostol in the United States. N Engl J Med. 1998 Apr 30;338(18):1241-7.
  • PMID: 14698075
    Piaggio G, von Hertzen H, Heng Z, Bilian X, Cheng L: Meta-analyses of randomized trials comparing different doses of mifepristone in emergency contraception. Contraception. 2003 Dec;68(6):447-52.
  • PMID: 19587339
    Fjerstad M, Trussell J, Sivin I, Lichtenberg ES, Cullins V: Rates of serious infection after changes in regimens for medical abortion. N Engl J Med. 2009 Jul 9;361(2):145-51. doi: 10.1056/NEJMoa0809146.

Contoh Produk & Brand

Produk: 10 • International brands: 4
Produk
  • Korlym
    Tablet • 300 mg/1 • Oral • US • Approved
  • Mifegymiso
    Kit; Tablet • - • Buccal; Oral • Canada • Approved
  • Mifepristone
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Mifepristone
    Tablet • 200 mg/1 • Oral • US • Generic • Approved
  • Mifepristone
    Tablet, film coated • 300 mg/1 • Oral • US • Generic • Approved
  • Mifepristone
    Tablet • 300 mg/1 • Oral • US • Approved
  • Mifiso
    Kit; Tablet • - • Buccal; Oral • Canada • Approved
  • Mpm Pak
    Kit; Tablet; Tablet, orally disintegrating • - • Oral • US • Generic • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Corlux — Corcept Therapeutics Incorporated
  • Mefipil — Abbott
  • Mifegyne — Exelgyn Laboratories
  • Mifeprex — Danco Laboratories

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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