Peringatan Keamanan

Toxicity information regarding ormeloxifene is not readily available. Patients experiencing an overdose are at an increased risk of severe cardiovascular adverse effects.A251485 Symptomatic and supportive measures are recommended.

Ormeloxifene

DB13310

small molecule experimental

Deskripsi

Ormeloxifene is a third-generation selective estrogen receptor (ER) modulator. In India, ormeloxifene has been marketed since the 1990s as a non-hormonal, non-steroidal oral contraceptive taken once a week,A251450 and it was later introduced for the treatment of dysfunctional uterine bleeding.A251470 Similar to other selective estrogen receptor modulators (SERMs), ormeloxifene has estrogenic activity in the vagina, bone, cardiovascular, and central nervous system tissues, and anti-estrogenic activity in the uterus and breast.A251450,A251465 The use of ormeloxifene for the treatment of perimenopausal bleeding and the management of menorrhagia has also been investigated.A251450,A251460 Ormeloxifene is marketed in India as a racemic mixture of the l- (levormeloxifene) and d-isomers (d-ormeloxifene) of trans-ormeloxifene.A251475 The use of levormeloxifene for the treatment of reduced bone turnover and the prevention of atherosclerosis has been evaluated; however, drug development was discontinued due to adverse events.A251480

Struktur Molekul 2D

Berat 457.614
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the half-life is 165 h.[A251470]
Volume Distribusi In healthy women, the apparent volume of distribution (Vd/F) was higher than the total body fluid, and the nursing state does not have an effect on this parameter.[A251470]
Klirens (Clearance) In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the clearance is 0.14 L/h.[A251470]

Absorpsi

In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the Cmax, tmax and AUC0-? were 55.5 ng/mL, 5.2 h, and 5199 ng?h/mL, respectively.A251470

Metabolisme

In vivo studies suggest that ormeloxifene is quickly metabolized by the liver.A251490 In rats, the active metabolite of this drug is 7-desmethylated ormeloxifene.A251490

Rute Eliminasi

In vivo studies suggest that ormeloxifene is excreted from the body primarily via feces.A251490

Interaksi Obat

454 Data
Aprepitant The serum concentration of Ormeloxifene can be decreased when it is combined with Aprepitant.
Prucalopride The serum concentration of Ormeloxifene can be decreased when it is combined with Prucalopride.
Thalidomide Ormeloxifene may increase the thrombogenic activities of Thalidomide.
Ospemifene The risk or severity of adverse effects can be increased when Ormeloxifene is combined with Ospemifene.
Ursodeoxycholic acid The therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Ormeloxifene.
Glycochenodeoxycholic Acid The therapeutic efficacy of Glycochenodeoxycholic Acid can be decreased when used in combination with Ormeloxifene.
Cholic Acid The therapeutic efficacy of Cholic Acid can be decreased when used in combination with Ormeloxifene.
Glycocholic acid The therapeutic efficacy of Glycocholic acid can be decreased when used in combination with Ormeloxifene.
Deoxycholic acid The therapeutic efficacy of Deoxycholic acid can be decreased when used in combination with Ormeloxifene.
Taurocholic acid The therapeutic efficacy of Taurocholic acid can be decreased when used in combination with Ormeloxifene.
Obeticholic acid The therapeutic efficacy of Obeticholic acid can be decreased when used in combination with Ormeloxifene.
Chenodeoxycholic acid The therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Ormeloxifene.
Taurochenodeoxycholic acid The therapeutic efficacy of Taurochenodeoxycholic acid can be decreased when used in combination with Ormeloxifene.
Tauroursodeoxycholic acid The therapeutic efficacy of Tauroursodeoxycholic acid can be decreased when used in combination with Ormeloxifene.
Bamet-UD2 The therapeutic efficacy of Bamet-UD2 can be decreased when used in combination with Ormeloxifene.
cis-Diamminechlorocholylglycinateplatinum(II) The therapeutic efficacy of cis-Diamminechlorocholylglycinateplatinum(II) can be decreased when used in combination with Ormeloxifene.
Dehydrocholic acid The therapeutic efficacy of Dehydrocholic acid can be decreased when used in combination with Ormeloxifene.
Hyodeoxycholic Acid The therapeutic efficacy of Hyodeoxycholic Acid can be decreased when used in combination with Ormeloxifene.
Aramchol The therapeutic efficacy of Aramchol can be decreased when used in combination with Ormeloxifene.
Ox bile extract The therapeutic efficacy of Ox bile extract can be decreased when used in combination with Ormeloxifene.
Tranexamic acid Ormeloxifene may increase the thrombogenic activities of Tranexamic acid.
Clobazam The serum concentration of Ormeloxifene can be decreased when it is combined with Clobazam.
Colestipol Colestipol can cause a decrease in the absorption of Ormeloxifene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Ormeloxifene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Ormeloxifene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Ormeloxifene resulting in a reduced serum concentration and potentially a decrease in efficacy.
Griseofulvin The metabolism of Ormeloxifene can be increased when combined with Griseofulvin.
Fluticasone propionate The serum concentration of Fluticasone propionate can be increased when it is combined with Ormeloxifene.
Trilostane The serum concentration of Trilostane can be increased when it is combined with Ormeloxifene.
Aldosterone The serum concentration of Aldosterone can be increased when it is combined with Ormeloxifene.
Tixocortol The serum concentration of Tixocortol can be increased when it is combined with Ormeloxifene.
Fluprednisolone The serum concentration of Fluprednisolone can be increased when it is combined with Ormeloxifene.
Melengestrol The serum concentration of Melengestrol can be increased when it is combined with Ormeloxifene.
Fluocortin The serum concentration of Fluocortin can be increased when it is combined with Ormeloxifene.
Fluperolone The serum concentration of Fluperolone can be increased when it is combined with Ormeloxifene.
Fluclorolone The serum concentration of Fluclorolone can be increased when it is combined with Ormeloxifene.
Hydrocortisone cypionate The serum concentration of Hydrocortisone cypionate can be increased when it is combined with Ormeloxifene.
Dexamethasone The serum concentration of Dexamethasone can be increased when it is combined with Ormeloxifene.
Flunisolide The serum concentration of Flunisolide can be increased when it is combined with Ormeloxifene.
Beclomethasone dipropionate The serum concentration of Beclomethasone dipropionate can be increased when it is combined with Ormeloxifene.
Betamethasone The serum concentration of Betamethasone can be increased when it is combined with Ormeloxifene.
Fluocinolone acetonide The serum concentration of Fluocinolone acetonide can be increased when it is combined with Ormeloxifene.
Triamcinolone The serum concentration of Triamcinolone can be increased when it is combined with Ormeloxifene.
Prednisone The serum concentration of Prednisone can be increased when it is combined with Ormeloxifene.
Hydrocortisone The serum concentration of Hydrocortisone can be increased when it is combined with Ormeloxifene.
Prednisolone The serum concentration of Prednisolone can be increased when it is combined with Ormeloxifene.
Methylprednisolone The serum concentration of Methylprednisolone can be increased when it is combined with Ormeloxifene.
Budesonide The serum concentration of Budesonide can be increased when it is combined with Ormeloxifene.
Corticotropin The serum concentration of Corticotropin can be increased when it is combined with Ormeloxifene.
Cortisone acetate The serum concentration of Cortisone acetate can be increased when it is combined with Ormeloxifene.
Paramethasone The serum concentration of Paramethasone can be increased when it is combined with Ormeloxifene.
Fluticasone furoate The serum concentration of Fluticasone furoate can be increased when it is combined with Ormeloxifene.
Fluprednidene The serum concentration of Fluprednidene can be increased when it is combined with Ormeloxifene.
Meprednisone The serum concentration of Meprednisone can be increased when it is combined with Ormeloxifene.
Dexamethasone isonicotinate The serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Ormeloxifene.
Deflazacort The serum concentration of Deflazacort can be increased when it is combined with Ormeloxifene.
Cortivazol The serum concentration of Cortivazol can be increased when it is combined with Ormeloxifene.
Prednylidene The serum concentration of Prednylidene can be increased when it is combined with Ormeloxifene.
Cloprednol The serum concentration of Cloprednol can be increased when it is combined with Ormeloxifene.
Fluticasone The serum concentration of Fluticasone can be increased when it is combined with Ormeloxifene.
Mometasone furoate The serum concentration of Mometasone furoate can be increased when it is combined with Ormeloxifene.
Hydrocortisone acetate The serum concentration of Hydrocortisone acetate can be increased when it is combined with Ormeloxifene.
Hydrocortisone succinate The serum concentration of Hydrocortisone succinate can be increased when it is combined with Ormeloxifene.
Prednisolone phosphate The serum concentration of Prednisolone phosphate can be increased when it is combined with Ormeloxifene.
Prednisolone hemisuccinate The serum concentration of Prednisolone hemisuccinate can be increased when it is combined with Ormeloxifene.
Methylprednisolone hemisuccinate The serum concentration of Methylprednisolone hemisuccinate can be increased when it is combined with Ormeloxifene.
Prednisone acetate The serum concentration of Prednisone acetate can be increased when it is combined with Ormeloxifene.
Clocortolone acetate The serum concentration of Clocortolone acetate can be increased when it is combined with Ormeloxifene.
Melengestrol acetate The serum concentration of Melengestrol acetate can be increased when it is combined with Ormeloxifene.
Betamethasone phosphate The serum concentration of Betamethasone phosphate can be increased when it is combined with Ormeloxifene.
Cortisone The serum concentration of Cortisone can be increased when it is combined with Ormeloxifene.
Fludrocortisone The serum concentration of Fludrocortisone can be increased when it is combined with Ormeloxifene.
Ciclesonide The serum concentration of Ciclesonide can be increased when it is combined with Ormeloxifene.
Clobetasol propionate The serum concentration of Clobetasol propionate can be increased when it is combined with Ormeloxifene.
Fluocinonide The serum concentration of Fluocinonide can be increased when it is combined with Ormeloxifene.
Hydrocortisone butyrate The serum concentration of Hydrocortisone butyrate can be increased when it is combined with Ormeloxifene.
Desoximetasone The serum concentration of Desoximetasone can be increased when it is combined with Ormeloxifene.
Mometasone The serum concentration of Mometasone can be increased when it is combined with Ormeloxifene.
Fluocortolone The serum concentration of Fluocortolone can be increased when it is combined with Ormeloxifene.
Prednisolone acetate The serum concentration of Prednisolone acetate can be increased when it is combined with Ormeloxifene.
Fluorometholone The serum concentration of Fluorometholone can be increased when it is combined with Ormeloxifene.
Difluocortolone The serum concentration of Difluocortolone can be increased when it is combined with Ormeloxifene.
Flumethasone The serum concentration of Flumethasone can be increased when it is combined with Ormeloxifene.
Methylprednisolone aceponate The serum concentration of Methylprednisolone aceponate can be increased when it is combined with Ormeloxifene.
Bosentan The serum concentration of Ormeloxifene can be decreased when it is combined with Bosentan.
Carbamazepine The serum concentration of Ormeloxifene can be decreased when it is combined with Carbamazepine.
Piperacillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Piperacillin.
Ampicillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Ampicillin.
Phenoxymethylpenicillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Phenoxymethylpenicillin.
Carbenicillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Carbenicillin.
Oxacillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Oxacillin.
Hetacillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Hetacillin.
Benzylpenicilloyl polylysine The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Benzylpenicilloyl polylysine.
Mezlocillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Mezlocillin.
Cyclacillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Cyclacillin.
Benzylpenicillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Benzylpenicillin.
Amoxicillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Amoxicillin.
Azlocillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Azlocillin.
Cloxacillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Cloxacillin.
Amdinocillin The therapeutic efficacy of Ormeloxifene can be decreased when used in combination with Amdinocillin.

Target Protein

Estrogen receptor ESR1
Estrogen receptor beta ESR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28458475
    Pati T, Chanania K, Marandi S, Hansa J: Ormeloxifene - Looking beyond contraception. J Midlife Health. 2017 Jan-Mar;8(1):17-20. doi: 10.4103/jmh.JMH7116.
  • PMID: 19751337
    Kriplani A, Kulshrestha V, Agarwal N: Efficacy and safety of ormeloxifene in management of menorrhagia: a pilot study. J Obstet Gynaecol Res. 2009 Aug;35(4):746-52. doi: 10.1111/j.1447-0756.2008.00987.x.
  • PMID: 24278556
    Chang BY, Kim SA, Malla B, Kim SY: The Effect of Selective Estrogen Receptor Modulators (SERMs) on the Tamoxifen Resistant Breast Cancer Cells. Toxicol Res. 2011 Jun;27(2):85-93. doi: 10.5487/TR.2011.27.2.085.
  • PMID: 20227542
    Lal J: Clinical pharmacokinetics and interaction of centchroman--a mini review. Contraception. 2010 Apr;81(4):275-80. doi: 10.1016/j.contraception.2009.11.007. Epub 2010 Jan 4.
  • PMID: 9351399
    Holm P, Shalmi M, Korsgaard N, Guldhammer B, Skouby SO, Stender S: A partial estrogen receptor agonist with strong antiatherogenic properties without noticeable effect on reproductive tissue in cholesterol-fed female and male rabbits. Arterioscler Thromb Vasc Biol. 1997 Oct;17(10):2264-72. doi: 10.1161/01.atv.17.10.2264.
  • PMID: 16532904
    Ravn P, Nielsen TF, Christiansen C: What can be learned from the levormeloxifene experience? Acta Obstet Gynecol Scand. 2006;85(2):135-42. doi: 10.1080/00016340500345691.
  • PMID: 21772767
    Bhalla H, Pant KK, Dikshit M, Surin WR, Singh MM: Effect of ormeloxifene, a nonsteroidal once-a-week oral contraceptive, on systemic hemodynamics in adult female rats. J Pharmacol Pharmacother. 2011 Apr;2(2):90-4. doi: 10.4103/0976-500X.81898.
  • PMID: 23895678
    Gara RK, Sundram V, Chauhan SC, Jaggi M: Anti-cancer potential of a novel SERM ormeloxifene. Curr Med Chem. 2013;20(33):4177-84. doi: 10.2174/09298673113209990197.

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