Ulipristal

DB08867

small molecule approved

Deskripsi

Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception (Ella) and for the treatment of uterine fibroids (Fibristal). It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor, however compared to mifepristone (a progesterone receptor antagonist), ulipristal is more tolerable and has lower glucocorticoid activity and better binding affinity.

Ulipristal is currently recommended as first line therapy for emergency contraception, due to improved efficacy and similar side effect profile as compared to the traditional use of levonorgestrel or the Yuzpe regimen. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. A recent systematic review proclaimed that the majority of available evidence demonstrates an inhibitory effect on ovulation rather than a post-fertilization effect on the endometrium, which has been heavily debated due to ethical concerns related to abortion (Rosato et al, 2016). Nevertheless, current and ongoing research into the agent's mechanism of action as an emergency contraceptive continue to provide potentially plausible evidence that ulipristal may, in fact, elicit activity on the endometrium that prevents embryo implantation A175372, A175375, A175378.

Struktur Molekul 2D

Berat 433.592
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean elimination half-life, single oral dose, healthy subject = 32.4 ± 6.3 hours
Volume Distribusi -
Klirens (Clearance) Mean oral clearance, single oral dose, healthy subject (CL/F) = 76.8 ± 64.0L/h

Absorpsi

Tmax, healthy subjects, single oral dose = 60-90 minutes; Cmax, healthy subjects, single oral dose = 176 ± 89 ng/mL; AUC(0-?), healthy subjects, single oral dose = 556 ± 260 ng·h/mL;

Metabolisme

Ulipristal is metabolized by CYP3A4 and to a lesser extent by CYP1A2 into mono-demethylated (active) and di-methylated (inactive) metabolites.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. High-fat food increases drug absorption, but not to a clinically significant extent.

Interaksi Obat

511 Data
Thiamylal The serum concentration of Ulipristal can be decreased when it is combined with Thiamylal.
Butalbital The serum concentration of Ulipristal can be decreased when it is combined with Butalbital.
Secobarbital The serum concentration of Ulipristal can be decreased when it is combined with Secobarbital.
Methohexital The serum concentration of Ulipristal can be decreased when it is combined with Methohexital.
Thiopental The serum concentration of Ulipristal can be decreased when it is combined with Thiopental.
Methylphenobarbital The serum concentration of Ulipristal can be decreased when it is combined with Methylphenobarbital.
Amobarbital The serum concentration of Ulipristal can be decreased when it is combined with Amobarbital.
Barbital The serum concentration of Ulipristal can be decreased when it is combined with Barbital.
Barbexaclone The serum concentration of Ulipristal can be decreased when it is combined with Barbexaclone.
Hexobarbital The serum concentration of Ulipristal can be decreased when it is combined with Hexobarbital.
Butabarbital The serum concentration of Ulipristal can be decreased when it is combined with Butabarbital.
Aprepitant The serum concentration of Ulipristal can be decreased when it is combined with Aprepitant.
Exenatide Exenatide can cause a decrease in the absorption of Ulipristal resulting in a reduced serum concentration and potentially a decrease in efficacy.
Thalidomide Ulipristal may increase the thrombogenic activities of Thalidomide.
Etonogestrel The therapeutic efficacy of Etonogestrel can be decreased when used in combination with Ulipristal.
Desogestrel The therapeutic efficacy of Desogestrel can be decreased when used in combination with Ulipristal.
Megestrol acetate The therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Ulipristal.
Levonorgestrel The therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Ulipristal.
Dydrogesterone The therapeutic efficacy of Dydrogesterone can be decreased when used in combination with Ulipristal.
Progesterone The therapeutic efficacy of Progesterone can be decreased when used in combination with Ulipristal.
Medroxyprogesterone acetate The therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Ulipristal.
Norethisterone The therapeutic efficacy of Norethisterone can be decreased when used in combination with Ulipristal.
Ethynodiol diacetate The therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Ulipristal.
Norgestimate The therapeutic efficacy of Norgestimate can be decreased when used in combination with Ulipristal.
Drospirenone The therapeutic efficacy of Drospirenone can be decreased when used in combination with Ulipristal.
Allylestrenol The therapeutic efficacy of Allylestrenol can be decreased when used in combination with Ulipristal.
Cyproterone acetate The therapeutic efficacy of Cyproterone acetate can be decreased when used in combination with Ulipristal.
Norelgestromin The therapeutic efficacy of Norelgestromin can be decreased when used in combination with Ulipristal.
Gestodene The therapeutic efficacy of Gestodene can be decreased when used in combination with Ulipristal.
Hydroxyprogesterone caproate The therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Ulipristal.
Dienogest The therapeutic efficacy of Dienogest can be decreased when used in combination with Ulipristal.
Medrogestone The therapeutic efficacy of Medrogestone can be decreased when used in combination with Ulipristal.
Norethynodrel The therapeutic efficacy of Norethynodrel can be decreased when used in combination with Ulipristal.
Norgestrel The therapeutic efficacy of Norgestrel can be decreased when used in combination with Ulipristal.
Altrenogest The therapeutic efficacy of Altrenogest can be decreased when used in combination with Ulipristal.
Gestrinone The therapeutic efficacy of Gestrinone can be decreased when used in combination with Ulipristal.
Nomegestrol The therapeutic efficacy of Nomegestrol can be decreased when used in combination with Ulipristal.
Lynestrenol The therapeutic efficacy of Lynestrenol can be decreased when used in combination with Ulipristal.
Gestonorone The therapeutic efficacy of Gestonorone can be decreased when used in combination with Ulipristal.
Chlormadinone The therapeutic efficacy of Chlormadinone can be decreased when used in combination with Ulipristal.
Methylestrenolone The therapeutic efficacy of Methylestrenolone can be decreased when used in combination with Ulipristal.
Norgestrienone The therapeutic efficacy of Norgestrienone can be decreased when used in combination with Ulipristal.
Promegestone The therapeutic efficacy of Promegestone can be decreased when used in combination with Ulipristal.
Quingestanol The therapeutic efficacy of Quingestanol can be decreased when used in combination with Ulipristal.
Demegestone The therapeutic efficacy of Demegestone can be decreased when used in combination with Ulipristal.
Etynodiol The therapeutic efficacy of Etynodiol can be decreased when used in combination with Ulipristal.
Nomegestrol acetate The therapeutic efficacy of Nomegestrol acetate can be decreased when used in combination with Ulipristal.
Hydroxyprogesterone The therapeutic efficacy of Hydroxyprogesterone can be decreased when used in combination with Ulipristal.
Norethindrone enanthate The therapeutic efficacy of Norethindrone enanthate can be decreased when used in combination with Ulipristal.
Quingestanol acetate The therapeutic efficacy of Quingestanol acetate can be decreased when used in combination with Ulipristal.
Algestone acetophenide The therapeutic efficacy of Algestone acetophenide can be decreased when used in combination with Ulipristal.
Bosentan The serum concentration of Ulipristal can be decreased when it is combined with Bosentan.
Tranexamic acid Ulipristal may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Ulipristal can be decreased when it is combined with Clobazam.
Griseofulvin The metabolism of Ulipristal can be increased when combined with Griseofulvin.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Ulipristal.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Ulipristal.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Ulipristal.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Ulipristal.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Ulipristal.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Ulipristal.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Ulipristal.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Ulipristal.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Ulipristal.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Ulipristal.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Ulipristal.
Fludrocortisone The serum concentration of Fludrocortisone can be increased when it is combined with Ulipristal.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Ulipristal.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Ulipristal.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Ulipristal.
Trilostane The serum concentration of Trilostane can be increased when it is combined with Ulipristal.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Ulipristal.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Ulipristal.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Ulipristal.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Ulipristal.
Ciclesonide The serum concentration of Ciclesonide can be increased when it is combined with Ulipristal.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Ulipristal.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Ulipristal.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Ulipristal.
Fluprednisolone The serum concentration of Fluprednisolone can be increased when it is combined with Ulipristal.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Ulipristal.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Ulipristal.
Melengestrol The serum concentration of Melengestrol can be increased when it is combined with Ulipristal.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Ulipristal.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Ulipristal.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Ulipristal.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Ulipristal.
Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Ulipristal.
Mometasone furoate The serum concentration of Mometasone furoate can be increased when it is combined with Ulipristal.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Ulipristal.
Hydrocortisone cypionate The serum concentration of Hydrocortisone cypionate can be increased when it is combined with Ulipristal.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Ulipristal.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Ulipristal.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Ulipristal.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Ulipristal.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Ulipristal.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Ulipristal.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Ulipristal.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Ulipristal.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Ulipristal.

Target Protein

Progesterone receptor PGR
Glucocorticoid receptor NR3C1
Androgen receptor AR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23550906
    Pohl O, Osterloh I, Gotteland JP: Ulipristal acetate - safety and pharmacokinetics following multiple doses of 10-50 mg per day. J Clin Pharm Ther. 2013 Aug;38(4):314-20. doi: 10.1111/jcpt.12065. Epub 2013 Apr 3.
  • PMID: 22681335
    Melis GB, Piras B, Marotto MF, Orru' MM, Maricosu G, Pilloni M, Guerriero S, Angiolucci M, Lello S, Paoletti AM: Pharmacokinetic evaluation of ulipristal acetate for uterine leiomyoma treatment. Expert Opin Drug Metab Toxicol. 2012 Jul;8(7):901-8. doi: 10.1517/17425255.2012.695775. Epub 2012 Jun 10.
  • PMID: 23437846
    Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591.
  • PMID: 22770536
    Martinez AM, Thomas MA: Ulipristal acetate as an emergency contraceptive agent. Expert Opin Pharmacother. 2012 Sep;13(13):1937-42. doi: 10.1517/14656566.2012.705832. Epub 2012 Jul 7.
  • PMID: 17531625
    Maruo T, Ohara N, Matsuo H, Xu Q, Chen W, Sitruk-Ware R, Johansson ED: Effects of levonorgestrel-releasing IUS and progesterone receptor modulator PRM CDB-2914 on uterine leiomyomas. Contraception. 2007 Jun;75(6 Suppl):S99-103. Epub 2007 Mar 21.
  • PMID: 17077229
    Creinin MD, Schlaff W, Archer DF, Wan L, Frezieres R, Thomas M, Rosenberg M, Higgins J: Progesterone receptor modulator for emergency contraception: a randomized controlled trial. Obstet Gynecol. 2006 Nov;108(5):1089-97.
  • PMID: 14667994
    Blithe DL, Nieman LK, Blye RP, Stratton P, Passaro M: Development of the selective progesterone receptor modulator CDB-2914 for clinical indications. Steroids. 2003 Nov;68(10-13):1013-7.
  • PMID: 15120421
    Attardi BJ, Burgenson J, Hild SA, Reel JR: In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88.
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