Chemical: Drug
conjugated estrogens

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

List of all variant annotations for conjugated estrogens

Gene ? Variant?
(147)
Alternate Names ? Chemicals ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA SLCO1B1 *1A N/A N/A N/A
No VIP available CA VA SLCO1B1 *12 N/A N/A N/A
No VIP available CA VA SLCO1B1 *13 N/A N/A N/A
No VIP available CA VA
rs1544410 NC_000012.11:g.48239835C>T, NC_000012.12:g.47846052C>T, NG_008731.1:g.63980G>A, NM_000376.2:c.1024+283G>A, NM_001017535.1:c.1024+283G>A, NM_001017536.1:c.1174+283G>A, XM_006719587.2:c.1024+283G>A, XM_011538720.1:c.1024+283G>A, XR_944903.1:n.-763C>T, rs386536760, rs56495123, rs56911380
C > T
SNP
No VIP available No Clinical Annotations available VA
rs35529209 NC_000016.10:g.16111468G>A, NC_000016.9:g.16205325G>A, NG_028268.1:g.166892G>A, NM_004996.3:c.2965G>A, NP_004987.2:p.Ala989Thr, NT_187607.1:g.1769332G>A, XM_005255326.1:c.2995G>A, XM_005255327.1:c.2839G>A, XM_005255328.1:c.2827G>A, XM_005255329.1:c.2788G>A, XM_011522497.1:c.2941G>A, XM_011522498.1:c.2872G>A, XP_005255383.1:p.Ala999Thr, XP_005255384.1:p.Ala947Thr, XP_005255385.1:p.Ala943Thr, XP_005255386.1:p.Ala930Thr, XP_011520799.1:p.Ala981Thr, XP_011520800.1:p.Ala958Thr, rs45620940
G > A
SNP
A989T
No VIP available No Clinical Annotations available VA
rs4148356 NC_000016.10:g.16083418G>A, NC_000016.9:g.16177275G>A, NG_028268.1:g.138842G>A, NM_004996.3:c.2168G>A, NP_004987.2:p.Arg723Gln, NT_187607.1:g.1741275G>A, XM_005255326.1:c.2168G>A, XM_005255327.1:c.2042G>A, XM_005255328.1:c.2030G>A, XM_005255329.1:c.2116-3406G>A, XM_011522497.1:c.2144G>A, XM_011522498.1:c.2075G>A, XP_005255383.1:p.Arg723Gln, XP_005255384.1:p.Arg681Gln, XP_005255385.1:p.Arg677Gln, XP_011520799.1:p.Arg715Gln, XP_011520800.1:p.Arg692Gln, rs52805887, rs587779731, rs60989413
G > A
SNP
R723Q
No VIP available CA VA
rs9282861 NC_000016.10:g.28606193C>T, NC_000016.9:g.28617514C>T, NG_028128.1:g.22353G>A, NM_001055.3:c.638G>A, NM_001310136.1:c.121-139291G>A, NM_177529.2:c.638G>A, NM_177530.2:c.638G>A, NM_177534.2:c.638G>A, NM_177536.3:c.404G>A, NP_001046.2:p.Arg213His, NP_803565.1:p.Arg213His, NP_803566.1:p.Arg213His, NP_803878.1:p.Arg213His, NP_803880.1:p.Arg135His, XM_005255522.1:c.638G>A, XP_005255579.1:p.Arg213His, rs17844870, rs17857585
C > T
SNP
R213H
No VIP available CA VA
rs9340799 NC_000006.11:g.152163381A>G, NC_000006.12:g.151842246A>G, NG_008493.1:g.156751A>G, NM_000125.3:c.453-351A>G, NM_001122740.1:c.453-351A>G, NM_001122741.1:c.453-351A>G, NM_001122742.1:c.453-351A>G, NM_001291230.1:c.453-351A>G, NM_001291241.1:c.453-351A>G, XM_005266856.1:c.453-351A>G, XM_005266857.1:c.453-351A>G, XM_006715374.2:c.453-351A>G, XM_006715375.2:c.-67-351A>G, XM_011535543.1:c.453-351A>G, XM_011535544.1:c.453-351A>G, XM_011535545.1:c.453-351A>G, XM_011535546.1:c.453-351A>G, XM_011535547.1:c.453-351A>G, XM_011535548.1:c.-67-351A>G, rs17208058, rs59875577
A > G
SNP
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 147

Overview

Generic Names
  • Estrogens
  • Estrone Estrone Hydrogen Sulfate
  • Estrone Hydrogen Sulfate
  • Estrone Sodium Sulfate
  • Estrone Sulfate
  • Estrone Sulfate Sodium
  • Estrone Sulphate
  • Estrone-sulfate
  • Oestrone Sulphate
  • Sodium Estrone Sulfate
Trade Names
  • Conestoral
  • Evex
  • Hyhorin
  • Morestin
  • Par Estro
  • Premarin
  • Premarin Vaginal
  • Premarin tabs
  • Prempro
  • Prempro/Premphase
Brand Mixture Names
  • Prempro (conjugated estrogens + medroxyprogesteron)

PharmGKB Accession Id

PA164754789

Type(s):

Drug

Description

Conjugated estrogens, a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 alpha-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics.

Source: Drug Bank

Indication

For the treatment of moderate to severe vasomotor symptoms associated with the menopause, atrophic vaginitis, osteoporosis, hypoestrogenism due to hypogonadism, castration, primary ovarian failure, breast cancer (for palliation only), and Advanced androgen-dependent carcinoma of the prostate (for palliation only)

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Estrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. Estrogens decrease the secretion of gonadotropin-releasing hormone by the hypothalamus, reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary.

Source: Drug Bank

Pharmacology

Conjugated estrogens, a mixture of the water soluble salts of sulfate esters from estrone, equilin, 17 alpha-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics. They promote growth and development of the vagina, uterus, and fallopian tubes, and enlargement of the breasts. Indirectly, they contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones that allow for the pubertal growth spurt and its termination, growth of axillary and pubic hair, and pigmentation of the nipples and genitals. Decline of estrogenic activity at the end of the menstrual cycle can bring on menstruation, although the cessation of progesterone secretion is the most important factor in the mature ovulatory cycle. However, in the preovulatory or nonovulatory cycle, estrogen is the primary determinant in the onset of menstruation. Estrogens also affect the release of pituitary gonadotropins. The pharmacologic effects of conjugated estrogens are similar to those of endogenous estrogens.

Source: Drug Bank

Food Interaction

Take with food to reduce nausea.|Avoid alcohol.|Avoid excessive quantities of coffee or tea (Caffeine).

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

90% bound to plasma proteins

Source: Drug Bank

Absorption

Well absorbed

Source: Drug Bank

Half-Life

7.4 hours

Source: Drug Bank

Toxicity

Nausea and vomiting

Source: Drug Bank

Route of Elimination

Estradiol, estrone, and estriol are excreted in the urine, along with glucuronide and sulfate conjugates. Exogenous estrogens are metabolized in the same manner as endogenous estrogens.

Source: Drug Bank

Chemical Properties

Chemical Formula

C18H21NaO5S

Source: Drug Bank

Canonical SMILES

[Na+].C[C@]

Source: Drug Bank

Average Molecular Weight

372.411

Source: Drug Bank

Monoisotopic Molecular Weight

372.100739147

Source: Drug Bank

SMILES

[Na+].[H][C@@]12CCC(=O)[C@@]1(C)CC[C@]1([H])C3=CC=C(OS([O-])(=O)=O)C=C3CC[C@@]21[H]

Source: Drug Bank

InChI String

InChI=1S/C18H22O5S.Na/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19;/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22);/q;+1/p-1/t14-,15-,16+,18+;/m1./s1

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ESR1 (source: Drug Bank)

Drug Interactions

Interaction Description
fosphenytoin - conjugated estrogens The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
griseofulvin - conjugated estrogens The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
phenobarbital - conjugated estrogens The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
phenytoin - conjugated estrogens The enzyme inducer decreases the effect of the hormones (source: Drug Bank)
phenytoin - conjugated estrogens The enzyme inducer, phenytoin, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
prednisolone - conjugated estrogens The estrogenic agent may increase the effect of the corticosteroid, prednisolone. (source: Drug Bank)
prednisone - conjugated estrogens The estrogenic agent may increase the effect of corticosteroid, prednisone. (source: Drug Bank)
primidone - conjugated estrogens The enzyme inducer, primidone, decreases the effect of the hormone agent, conjugated estrogens. (source: Drug Bank)
raloxifene - conjugated estrogens Association not recommended (source: Drug Bank)
tipranavir - conjugated estrogens Conjugated estrogens may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Conjugated estrogens. Monitor for estrogen deficiency during concomitant therapy. (source: Drug Bank)

Curated Information ?

Publications related to conjugated estrogens: 8

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Polymorphisms of caffeine metabolism and estrogen receptor genes and risk of Parkinson's disease in men and women. Parkinsonism & related disorders. 2010. Palacios N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Variation in anastrozole metabolism and pharmacodynamics in women with early breast cancer. Cancer research. 2010. Ingle James N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Identification and characterization of single nucleotide polymorphisms of SLC22A11 (hOAT4) in Korean women osteoporosis patients. Molecules and cells. 2008. Lee Woon Kyu, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Estrogen sulfation genes, hormone replacement therapy, and endometrial cancer risk. Journal of the National Cancer Institute. 2006. Rebbeck Timothy R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Ontogeny of expression of organic anion transporters 1 and 3 in ovine fetal and neonatal kidney. Experimental biology and medicine (Maywood, N.J.). 2005. Wood Charles E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
Functional characterization of non-synonymous single nucleotide polymorphisms in the gene encoding human multidrug resistance protein 1 (MRP1/ABCC1). Pharmacogenetics and genomics. 2005. L├ętourneau Isabelle J, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans. The Journal of biological chemistry. 2001. Tirona R G, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Change of bone mass in postmenopausal Caucasian women with and without hormone replacement therapy is associated with vitamin D receptor and estrogen receptor genotypes. Human genetics. 1998. Deng H W, et al. PubMed

LinkOuts

National Drug Code Directory:
0046-0872-93
DrugBank:
DB00286
ChEBI:
16469
KEGG Drug:
D00312
PubChem Compound:
23667301
PubChem Substance:
46505680
7847378
Drugs Product Database (DPD):
2239655
ChemSpider:
9532
Therapeutic Targets Database:
DNC001150
FDA Drug Label at DailyMed:
96609623-528e-4aba-cabe-7254aed816d5

Clinical Trials

These are trials that mention conjugated estrogens and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

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Sources for PharmGKB drug information: DrugBank, PubChem.