Conjugated estrogen

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Estrone sulfate, the main active agent of conjugated estrogen formulations.
Not to be confused with Estrogen conjugate.

Conjugated estrogens, or conjugated equine estrogens (CEEs), are blended equine estrogens,[1] which may include estrone sulfate, equilin sulfate, and equilenin sulfate.[1] CEEs are used clinically in hormone replacement therapy, with marketed products including both natural preparations isolated from the urine of pregnant mares (brand names Premarin) as well as fully synthetic replications of the natural preparations (brand names Cenestin, Enjuvia, Congest, and C.E.S.).[2][3] Prempro and Premphase are combination formulations of natural CEEs with medroxyprogesterone acetate.[4]

The exact composition of Premarin specifically is as follows: sodium estrone sulfate (49.3%), sodium equilin sulfate (22.4%), sodium 17α-dihydroequilin sulfate (13.8%), sodium 17α-estradiol sulfate (4.5%), sodium 8,9-dehydroestrone sulfate (3.5%), sodium equilenin sulfate (2.2%), sodium 17β-dihydroequilin sulfate (1.7%), sodium 17α-dihydroequilenin sulfate (1.2%), sodium 17β-estradiol sulfate (0.9%), sodium 17β-dihydroequilenin sulfate (0.5%), and sodium 8,9-dehydroestradiol sulfate (small amounts).[1][5]

17β-Dihydroequilenin has unexpectedly shown a selective estrogen receptor modulator-like profile of estrogenic activity in studies with monkeys, in which beneficial effects on bone and the cardiovascular system were noted but proliferative responses in breast or endometrium were not observed.[6]

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References[edit]

  1. ^ a b c Marc A. Fritz; Leon Speroff (28 March 2012). Clinical Gynecologic Endocrinology and Infertility. Lippincott Williams & Wilkins. pp. 751–. ISBN 978-1-4511-4847-3. 
  2. ^ Kathy Moscou; Karen Snipe (1 December 2012). Pharmacology for Pharmacy Technicians Pageburst E-Book on VitalSource2: Pharmacology for Pharmacy Technicians Pageburst E-Book on VitalSource. Elsevier Health Sciences. pp. 573–. ISBN 0-323-08578-4. 
  3. ^ IARC Working Group on the Evaluation of Carcinogenic Risks to Humans; World Health Organization; International Agency for Research on Cancer (2007). Combined Estrogen-progestogen Contraceptives and Combined Estrogen-progestogen Menopausal Therapy. World Health Organization. pp. 378–. ISBN 978-92-832-1291-1. 
  4. ^ MaryAnne Hochadel; Jerry Avorn (1 January 2007). The AARP Guide to Pills: Essential Information on More Than 1,200 Prescription and Nonprescription Medications, Including Generics. Sterling Publishing Company Incorporated. pp. 235–. ISBN 978-1-4027-4446-4. 
  5. ^ Kuhl H (2005). "Pharmacology of estrogens and progestogens: influence of different routes of administration". Climacteric. 8 Suppl 1: 3–63. doi:10.1080/13697130500148875. PMID 16112947. 
  6. ^ Cline JM (2007). "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. 80 (2): 126–46. doi:10.1002/bdrb.20112. PMID 17443713.