Peringatan Keamanan

The reported oral LD50 in the rat is of more than 5000 mg/kg.F3895 Serious overdosage symptoms have not been reported. There have been only reports of nausea, vomiting, and withdrawal in bleeding in females.FDA label

Long-term continuous administration of estrogens is correlated to increased risk on the incidence of carcinomas of the breast, uterus, cervix, vagina, testis, and liver.FDA label

Conjugated estrogens

DB00286

small molecule approved

Deskripsi

The conjugated estrogens are noncrystalline mixtures of purified female sex hormones obtained either by its isolation from the urine of pregnant mares or by synthetic generation from vegetal material. Both of these products are later conjugated to natrium sulfate by ester bonds in order to make them more water soluble.L5605, T475

The conjugated estrogen product contains a mix of estrogen from which about 50% is represented by estrone sulfate followed by 25% of equilin sulfate, 15% of 17-alpha-dehydroequilenin sulfate, 3% of equilenin sulfate, 5% of 17-alpha and 17-beta-dihydroequilenin sulfate, 2% of 17-alpha-estradiolsulfate and 3% of 17-beta-estradiolsulfate. It also presents a large number of unidentified molecules with weak estrogenic activity as well as non-human molecules when it is obtained from pregnant mares urine.T475

The conjugated estrogen mixture was approved for marketing in US in 1942 based on the efficacy against certain conditions. However, until 1986 official clinical trials were performed and this product was determined to be effective for the treatment of osteoporosis.T484 The currently approved product of conjugated estrogens was developed by Wyeth Ayerst and FDA approved in 2003.L5608

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The median half-life of the conjugated estrogens is reported to be of 17 hours.[A175552]
Volume Distribusi The physiological distribution of estrogens in the body is very similar to what is seen in endogenous estrogens and hence, it is widely distributed.[A38238] The conjugated estrogens are mainly found in the sex hormone target organs.[L5632]
Klirens (Clearance) The reported normal clearance rate for estrogens is of approximately 615 L/m2.[A175633]

Absorpsi

The conjugated estrogens are well absorbed in the gastrointestinal tract and the maximum plasma concentration of the conjugated estrogens is reached after 7 hours depending on the estrone component.A175552 The maximal plasma concentration of conjugated estrogens after multiple doses of 0.45 mg is reported to be of 2.6 ng/ml with an AUC in the steady state of 35 ng.h/ml.A38238 Unconjugated estrogens are known to be cleared from the circulation at a faster rate than their ester forms.A175594

Metabolisme

The conjugated estrogens are metabolized by a number of different pathways. One of the metabolic pathways of the conjugated estrogens is driven by the action of the cytochrome isoenzyme CYP3A4.A175552 On the other hand, the conjugated estrogens can also be processed by a dynamic equilibrium of metabolic interconversion and sulfate conjugation. Some of the principal metabolic reactions of the conjugated estrogens are driven by the conversion of 17beta-estradiol to estrone and the further change to estriol. A portion of the administered conjugated estrogens will remain in the blood as sulfate conjugates which serve as a circulating reservoir for the generation of new estrogens.A38238 In the endometrium, equilin is metabolized to 2-hydroxy and 4-hydroxy equilin as well as 2-hydroxy and 4-hydroxy estradiol. This hydroxylation process is very large in various of the components of the conjugated estrogens and hence, the major metabolites in urine are known to be 17-ketosteroid-16-alpha-hydroxy estrone, 16-alpha-hydroxy-17-beta-dihydro equilin and 16-alpha-hydroxy-17-beta-dihydroequilenin.A175594

Rute Eliminasi

The conjugated estrogens are eliminated mainly in the urine.A175552 In this renal elimination, it is possible to find 17 beta-estradiol, estrone, estriol, as well as the glucuronide and sulfate conjugates of the estrogens.A38238

Interaksi Makanan

1 Data
  • 1. Take with or without food. Consult individual product monograph for specific instructions.

Interaksi Obat

1755 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Conjugated estrogens.
Deferasirox The serum concentration of Conjugated estrogens can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Conjugated estrogens can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Conjugated estrogens can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Conjugated estrogens can be decreased when it is combined with Teriflunomide.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Conjugated estrogens.
Aspartame The excretion of Conjugated estrogens can be decreased when combined with Aspartame.
Succinic acid The excretion of Succinic acid can be decreased when combined with Conjugated estrogens.
Citrulline The excretion of Citrulline can be decreased when combined with Conjugated estrogens.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Conjugated estrogens.
Cefdinir The excretion of Cefdinir can be decreased when combined with Conjugated estrogens.
Leucovorin The excretion of Leucovorin can be decreased when combined with Conjugated estrogens.
Fluorescein The excretion of Fluorescein can be decreased when combined with Conjugated estrogens.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Conjugated estrogens.
Famotidine The excretion of Famotidine can be decreased when combined with Conjugated estrogens.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Conjugated estrogens.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Conjugated estrogens.
Tazobactam The excretion of Tazobactam can be decreased when combined with Conjugated estrogens.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Conjugated estrogens.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Conjugated estrogens.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Conjugated estrogens.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Conjugated estrogens.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Conjugated estrogens.
Avibactam The excretion of Avibactam can be decreased when combined with Conjugated estrogens.
Silibinin The excretion of Silibinin can be decreased when combined with Conjugated estrogens.
Relebactam The excretion of Relebactam can be decreased when combined with Conjugated estrogens.
Guanidine The excretion of Conjugated estrogens can be decreased when combined with Guanidine.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Conjugated estrogens.
Minocycline The excretion of Conjugated estrogens can be decreased when combined with Minocycline.
Probenecid The excretion of Conjugated estrogens can be decreased when combined with Probenecid.
Ouabain The excretion of Conjugated estrogens can be decreased when combined with Ouabain.
Cilastatin The excretion of Conjugated estrogens can be decreased when combined with Cilastatin.
trans-2-hydroxycinnamic acid The excretion of Conjugated estrogens can be decreased when combined with trans-2-hydroxycinnamic acid.
Benzoic acid The excretion of Conjugated estrogens can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Conjugated estrogens can be decreased when combined with Caprylic acid.
Ataluren The excretion of Conjugated estrogens can be decreased when combined with Ataluren.
Cabotegravir The excretion of Conjugated estrogens can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Conjugated estrogens can be decreased when combined with Pradigastat.
Cefotiam The excretion of Conjugated estrogens can be decreased when combined with Cefotiam.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Conjugated estrogens.
Cefalotin The excretion of Conjugated estrogens can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Conjugated estrogens can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Conjugated estrogens can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Conjugated estrogens can be decreased when combined with Piroxicam.
Methotrexate The excretion of Methotrexate can be decreased when combined with Conjugated estrogens.
Cephalexin The excretion of Cephalexin can be decreased when combined with Conjugated estrogens.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Conjugated estrogens.
Diclofenac The excretion of Conjugated estrogens can be decreased when combined with Diclofenac.
Acyclovir The excretion of Acyclovir can be decreased when combined with Conjugated estrogens.
Phenylbutazone The excretion of Conjugated estrogens can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Cefaclor can be decreased when combined with Conjugated estrogens.
Salicylic acid The excretion of Conjugated estrogens can be decreased when combined with Salicylic acid.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Conjugated estrogens.
Ketoprofen The excretion of Conjugated estrogens can be decreased when combined with Ketoprofen.
Cefadroxil The excretion of Conjugated estrogens can be decreased when combined with Cefadroxil.
Cefamandole The excretion of Conjugated estrogens can be decreased when combined with Cefamandole.
Cefazolin The excretion of Cefazolin can be decreased when combined with Conjugated estrogens.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Conjugated estrogens.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Conjugated estrogens.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Conjugated estrogens.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Conjugated estrogens.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Conjugated estrogens.
Tenofovir The excretion of Tenofovir can be decreased when combined with Conjugated estrogens.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Conjugated estrogens.
Piperacillin The excretion of Piperacillin can be decreased when combined with Conjugated estrogens.
Trifluridine The excretion of Trifluridine can be decreased when combined with Conjugated estrogens.
Allopurinol The excretion of Allopurinol can be decreased when combined with Conjugated estrogens.
Cimetidine The excretion of Cimetidine can be decreased when combined with Conjugated estrogens.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Conjugated estrogens.
Ganciclovir The excretion of Conjugated estrogens can be decreased when combined with Ganciclovir.
Doripenem The excretion of Doripenem can be decreased when combined with Conjugated estrogens.
Indomethacin The excretion of Indomethacin can be decreased when combined with Conjugated estrogens.
Dronedarone The excretion of Conjugated estrogens can be decreased when combined with Dronedarone.
Pantoprazole The excretion of Conjugated estrogens can be decreased when combined with Pantoprazole.
Zidovudine The excretion of Zidovudine can be decreased when combined with Conjugated estrogens.
Tetracycline The excretion of Tetracycline can be decreased when combined with Conjugated estrogens.
Ranitidine The excretion of Ranitidine can be decreased when combined with Conjugated estrogens.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Conjugated estrogens.
Captopril The excretion of Captopril can be decreased when combined with Conjugated estrogens.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Conjugated estrogens.
Lansoprazole The excretion of Conjugated estrogens can be decreased when combined with Lansoprazole.
Esomeprazole The excretion of Conjugated estrogens can be decreased when combined with Esomeprazole.
Ibuprofen The excretion of Conjugated estrogens can be decreased when combined with Ibuprofen.
Ceftriaxone The excretion of Conjugated estrogens can be decreased when combined with Ceftriaxone.
Cefoperazone The excretion of Conjugated estrogens can be decreased when combined with Cefoperazone.
Dolutegravir The excretion of Conjugated estrogens can be decreased when combined with Dolutegravir.
Letermovir The excretion of Letermovir can be decreased when combined with Conjugated estrogens.
Rucaparib Rucaparib may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.
Ivosidenib The metabolism of Conjugated estrogens can be increased when combined with Ivosidenib.
Favipiravir The excretion of Conjugated estrogens can be decreased when combined with Favipiravir.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Conjugated estrogens.
Lenvatinib The excretion of Conjugated estrogens can be decreased when combined with Lenvatinib.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Conjugated estrogens.
Acetylsalicylic acid The excretion of Conjugated estrogens can be decreased when combined with Acetylsalicylic acid.
Linezolid The excretion of Conjugated estrogens can be decreased when combined with Linezolid.
Prasterone The risk or severity of adverse effects can be increased when Prasterone is combined with Conjugated estrogens.
Exemestane The therapeutic efficacy of Exemestane can be decreased when used in combination with Conjugated estrogens.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Conjugated estrogens.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Conjugated estrogens.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Conjugated estrogens.

Target Protein

Estrogen receptor beta ESR2
Estrogen receptor ESR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28798519
    Authors unspecified: Conjugated oestrogens/bazedoxifene. Aust Prescr. 2017 Jun;40(3):114-115. doi: 10.18773/austprescr.2017.039. Epub 2017 May 10.
  • PMID: 24715748
    Cada DJ, Baker DE: Conjugated estrogens and bazedoxifene. Hosp Pharm. 2014 Mar;49(3):273-83. doi: 10.1310/hpj4903-273.
  • PMID: 9421201
    Bhavnani BR: Pharmacokinetics and pharmacodynamics of conjugated equine estrogens: chemistry and metabolism. Proc Soc Exp Biol Med. 1998 Jan;217(1):6-16.
  • PMID: 16112947
    Kuhl H: Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. 2005 Aug;8 Suppl 1:3-63. doi: 10.1080/13697130500148875.
  • PMID: 17443713
    Cline JM: Assessing the mammary gland of nonhuman primates: effects of endogenous hormones and exogenous hormonal agents and growth factors. Birth Defects Res B Dev Reprod Toxicol. 2007 Apr;80(2):126-46. doi: 10.1002/bdrb.20112.
  • PMID: 5822587
    Hembree WC, Bardin CW, Lipsett MB: A study of estrogen metabolic clearance rates and transfer factors. J Clin Invest. 1969 Oct;48(10):1809-19. doi: 10.1172/JCI106147.
Textbook
  • ISBN: 0-203-62272-3
    Lauritzen C. and Studd J. (2005). Current management of the menopause. Taylor and Francis.
  • ISBN: 9780323511216
    Arthur H. Jeske (2017). Mosby's Dental Drug Reference - E-Book. Elsevier Health Sciences.
  • Kelsey J. and Marcus R. (2000). Menopause. Academic Press.

Contoh Produk & Brand

Produk: 105 • International brands: 0
Produk
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    Tablet • 0.9 mg • Oral • Canada • Generic • Approved
  • Apo-conest Tab 1.25mg
    Tablet • 1.25 mg • Oral • Canada • Generic • Approved
  • Apo-conest Tab 2.5mg
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • C.E.S.
    Tablet • 0.625 mg • Oral • Canada • Approved
  • C.E.S. Tablets
    Tablet • 1.25 mg • Oral • Canada • Approved
  • C.E.S. Tablets
    Tablet • 0.3 mg • Oral • Canada • Approved
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