Identification
- Summary
Esterified estrogens is a female hormone used to treat conditions related to estrogen deficiency and moderate to severe vasomotor menopausal symptoms in women.
- Brand Names
- Covaryx, Menest
- Generic Name
- Esterified estrogens
- DrugBank Accession Number
- DB09381
- Background
Esterified estrogens contain a mixture of estrogenic substances; the principle component is estrone. Preparations contain 75% to 85% sodium estrone sulfate and 6% to 15% sodium equilin sulfate such that the total is not <90%. Esterified estrogens are a man-made mixture of estrogens that are used to treat symptoms of menopause such as hot flashes, vaginal dryness, vaginal burning or irritation, or other hormonal changes in the vagina. It is being also for the prevention and treatment of osteoporosis.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Esterified estrogens
- Estrogens, esterified
- Estrogens, Esterified Component of Menrium
- Estrogens,esterified
- Menrium Component Estrogens, Esterified
Pharmacology
- Indication
Esterified estrogens are indicated to replace estrogen in women with ovarian failure or other conditions that cause a lack of natural estrogen in the body. It is also indicated for the treatment of symptoms of breast cancer in both men and women. In men it can be used for the treatment of advanced prostate cancer. It is also indicated for the treatment of menopausal symptoms.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Hypogonadism •••••••••••• Symptomatic treatment of Metastatic breast cancer •••••••••••• Management of Primary ovarian failure •••••••••••• Symptomatic treatment of Advanced prostatic carcinoma •••••••••••• Management of Moderate vulvovaginal atrophy •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Estrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estradiol is the principle intracellular human estrogen and is more potent than estrone and estriol at the receptor level; it is the primary estrogen secreted prior to menopause.
- Mechanism of action
Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle-stimulating hormone through a negative feedback system; estrogen replacement reduces elevated levels of these hormones.
- Absorption
Readily absorbed after oral administration. High concentrations of estrone are achieved with oral administration, whereas higher concentrations of estradiol are generally achieved after percutaneous absorption. Although vaginal products (such as gel, rings, etc.) are administered locally, they achieve high serum concentrations.
- Volume of distribution
The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentration in the sex hormone target organs.
- Protein binding
Approximately 95-98% of estradiol is bound loosely to albumin or tightly to sex hormone binding globulin.
- Metabolism
Hepatic; partial metabolism via CYP3A4 enzymes; estradiol is reversibly converted to estrone and estriol; oral estradiol also undergoes enterohepatic recirculation by conjugation in the liver, followed by excretion of sulfate and glucuronide conjugates into the bile, then hydrolysis in the intestine and estrogen reabsorption. Sulfate conjugates are the primary form found in postmenopausal women.
- Route of elimination
Mainly urinary as estradiol, estrone, estriol, and their glucuronide and sulfate conjugates.
- Half-life
Half-life varies, it is in the range 1-2 hr.
- Clearance
There is variation in the clearance rate depends on each estrogen individual: estradiol-17β: 580 L/day/m2 estrone: 4050 L/day/m2 estriol: 1110 L/day/m2
- Adverse Effects
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LD50 IP 325 mg/Kg (rat). LD50 IV 1740 mg/Kg (mouse). LD50 oral >5000 mg/Kg (rat).
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Esterified estrogens can be increased when it is combined with Abametapir. Abciximab Esterified estrogens may decrease the anticoagulant activities of Abciximab. Aceclofenac Aceclofenac may increase the thrombogenic activities of Esterified estrogens. Acenocoumarol Esterified estrogens may decrease the anticoagulant activities of Acenocoumarol. Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Esterified estrogens. - Food Interactions
- Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of esterified estrogens.
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of esterified estrogens.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Images
- International/Other Brands
- Amnestrogen / Estratab / Evex / Femogen
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Estragyn Tablet 0.3 mg Oral Searchlight Pharma Inc 1980-12-31 Not applicable Canada 
Estragyn Tablet 0.625 mg Oral Searchlight Pharma Inc 1974-12-31 Not applicable Canada Neo Estrone Tab 1.25mg Tablet 1.25 mg Oral Neolab Inc 1974-12-31 2008-04-02 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Menest Tablet 1.25 mg/1 Oral Physicians Total Care, Inc. 2010-12-16 Not applicable US 
Menest Tablet, film coated 0.625 mg/1 Oral Avera McKennan Hospital 2015-11-23 2017-05-24 US Menest Tablet, film coated 0.625 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 1977-09-28 Not applicable US Menest Tablet 0.625 mg/1 Oral Physicians Total Care, Inc. 2008-09-05 Not applicable US Menest Tablet, film coated 2.5 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2018-09-17 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Covaryx Esterified estrogens (1.25 mg/1) + Methyltestosterone (2.5 mg/1) Tablet, coated Oral CENTRIX PHARMACEUTICAL, INC, 2007-04-01 Not applicable US 
Covaryx Hs Esterified estrogens (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, coated Oral CENTRIX PHARMACEUTICAL, INC, 2007-04-01 Not applicable US Eemt Esterified estrogens (1.25 mg/1) + Methyltestosterone (2.5 mg/1) Tablet, coated Oral CREEKWOOD PHARMACEUTICAL, INC, 2011-09-01 Not applicable US Eemt H.S. Esterified estrogens (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, coated Oral Physicians Total Care, Inc. 2006-06-27 2013-01-15 US Eemt Hs Esterified estrogens (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, coated Oral CREEKWOOD PHARMACEUTICAL, INC, 2011-09-01 Not applicable US
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 3ASP8Q3768
- CAS number
- Not Available
References
- General References
- External Links
- PubChem Substance
- 347910451
- 214549
- Wikipedia
- Esterified_estrogens
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Completed Treatment Hot Flushes, Menopause, Postmenopause 1 2 Completed Treatment Menopause 1 2 Terminated Treatment Breast Cancer 1 2 Terminated Treatment Menopause 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, coated Oral Tablet Oral Tablet Oral 0.3 mg Tablet Oral 0.625 mg Tablet Oral 0.3 mg/1 Tablet Oral 0.625 mg/1 Tablet Oral 1.25 mg/1 Tablet, film coated Oral 0.3 mg/1 Tablet, film coated Oral 0.625 mg/1 Tablet, film coated Oral 1.25 mg/1 Tablet, film coated Oral 2.5 mg/1 Tablet Oral 1.25 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Major thyroid hormone transport protein in serum.
- Gene Name
- SERPINA7
- Uniprot ID
- P05543
- Uniprot Name
- Thyroxine-binding globulin
- Molecular Weight
- 46324.12 Da
References
- CYTOMEL (liothyronine) FDA label [File]
Drug created at November 30, 2015 19:10 / Updated at February 20, 2024 23:55