pharmacopeia
GET
/api/v1/drug/estradiol

Boxed warning

ENDOMETRIAL CANCER, CARDIOVASCULAR DISORDERS, BREAST CANCER and PROBABLE DEMENTIA Estrogen-Alone Therapy Endometrial Cancer There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adding a progestin to estrogen therapy has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding [see WARNINGS, Malignant Neoplasms, Endometrial Cancer ]. Cardiovascular Disorders and Probable Dementia Estrogen-alone therapy should not be used for the prevention of cardiovascular disease or dementia [see CLINICAL STUDIES and WARNINGS, Cardiovascular Disorders, and Probable Dementia ]. The Women’s Health Initiative (WHI) estrogen-alone substudy reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) during 7.1 years of treatment with daily oral conjugated estrogens (CE) [0.625 mg]-alone, relative to placebo [see CLINICAL STUDIES and WARNINGS, Cardiovascular Disorders ].

2D structure
(8R,9S,13S,14S,17S)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
SMILES C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=C3C=CC(=C4)O
InChIKey VOXZDWNPVJITMN-ZBRFXRBCSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Estrogen Receptor Agonists.

Estrogen Receptor

Indications

Sourced from openFDA
  • Estradiol Vaginal Cream, 0.01% is indicated in the treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.ICD-10: N95.1

Contraindications

Sourced from openFDA
  • Estradiol Vaginal Cream, 0.01% should not be used in women with any of the following conditions: 1. Undiagnosed abnormal genital bleeding.contraindicated

Dosage & administration

Sourced from openFDA

Use of Estradiol Vaginal Cream, 0.01% alone or in combination with a progestin, should be limited to the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women should reevaluate periodically as clinically appropriate to determine if treatment is still necessary. For treatment of vulvar and vaginal atrophy associated with the menopause, the lowest dose and regimen that will control symptoms should be chosen and medication should be discontinued as promptly as possible. For women who have a uterus, adequate diagnostic measures, including directed and random endometrial sampling when indicated, should be undertaken to rule out malignancy in cases of undiagnosed persistent or recurring abnormal genital bleeding. Usual Dosage: The usual dosage range is 2 to 4 g (marked on the applicator) daily for one or two weeks, then gradually reduced to one half initial dosage for a similar period. A maintenance dosage of 1 g, one to three times a week, may be used after restoration of the vaginal mucosa has been achieved. NOTE: The number of doses per tube will vary with dosage requirements and patient handling.

Warnings & precautions

Sourced from openFDA

See BOXED WARNINGS . Systemic absorption may occur with the use of Estradiol Vaginal Cream, 0.01%. The warnings, precautions, and adverse reactions associated with oral estrogen treatment should be taken into account. 1. Cardiovascular Disorders An increased risk of stroke and DVT has been reported with estrogen-alone therapy. An increased risk of PE, DVT, stroke and MI has been reported with estrogen plus progestin therapy. Should any of these occur or be suspected, estrogen with or without progestin therapy should be discontinued immediately. Risk factors for arterial vascular disease (e.g., hypertension, diabetes mellitus, tobacco use, hypercholesterolemia, and obesity) and/or venous thromboembolism (VTE) (e.g., personal history or family history of VTE, obesity, and systemic lupus erythematosus) should be managed appropriately. a. Stroke In the WHI estrogen-alone substudy, a statistically significant increased risk of stroke was reported in women 50 to 79 years of age receiving daily CE (0.625 mg)-alone compared to women in the same age group receiving placebo (45 versus 33 per 10,000 women-years). The increase in risk was demonstrated in year one and persisted [see CLINICAL STUDIES ]. Should a stroke occur or be suspected, estrogen-alone therapy should be discontinued immediately. Subgroup analyses of women 50 to 59 years of age suggest no increased risk of stroke for those women receiving CE (0.625 mg)-alone versus those receiving placebo (18 versus 21 per 10,000 women-years) 3 .

Adverse reactions

Sourced from openFDA

See BOXED WARNINGS, WARNINGS and PRECAUTIONS . Systemic absorption may occur with the use of Estradiol Vaginal Cream, 0.01%. The warnings, precautions, and adverse reactions associated with oral estrogen treatment should be taken into account. The following adverse reactions have been reported with estrogen and/or progestin therapy. 1 . Genitourinary System Abnormal uterine bleeding or spotting; dysmenorrhea or pelvic pain, increase in size of uterine leiomyomata; vaginitis, including vaginal candidiasis; change in cervical secretion; cystitis-like syndrome; application site reactions of vulvovaginal discomfort including burning and irritation; genital pruritus; ovarian cancer; endometrial hyperplasia; endometrial cancer. 2 . Breasts Tenderness, enlargement, pain, nipple discharge, fibrocystic breast changes; breast cancer. 3 . Cardiovascular Deep and superficial venous thrombosis; pulmonary embolism; myocardial infarction; stroke; increase in blood pressure. 4 . Gastrointestinal Nausea, vomiting; abdominal cramps, bloating; increased incidence of gallbladder disease. 5 . Skin Chloasma that may persist when drug is discontinued; loss of scalp hair; hirsutism; rash. 6 . Eyes Retinal vascular thrombosis, intolerance to contact lenses. 7 . Central Nervous System Headache; migraine; dizziness; mental depression; nervousness; mood disturbances; irritability; dementia. 8 . Miscellaneous Increase or decrease in weight; glucose intolerance; edema; arthralgias; leg cramps; changes in libido; urticaria; exacerbation of asthma; increased triglycerides; hypersensitivity.

Use in specific populations

Sourced from openFDA

F. Pregnancy Estradiol Vaginal Cream, 0.01% should not be used during pregnancy [see CONTRAINDICATIONS ]. There appears to be little or no increased risk of birth defects in children born to women who have used estrogens and progestins as an oral contraceptive inadvertently during early pregnancy.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Estrogen drug products are absorbed through the skin, mucous membranes, and the gastrointestinal tract after release from the drug formulation. Distribution The distribution of exogenous estrogens is similar to that of endogenous estrogens.

Overdosage

Sourced from openFDA

Overdosage of estrogen may cause nausea, vomiting, breast tenderness, abdominal pain, drowsiness and fatigue, and withdrawal bleeding may occur in women. Treatment of overdose consists of discontinuation of Estradiol Vaginal Cream, 0.01% therapy together with institution of appropriate symptomatic care.

Approval history

Sourced from openFDA
  • Dec 22, 1994NDANDA020375Bayer Hlthcare
  • Aug 7, 1998NDANDA020870Noven Pharms Inc
  • Nov 18, 1998NDANDA020907Amneal
  • Mar 26, 1999NDANDA020908Novo Nordisk Inc
  • Sep 5, 2003NDANDA021544Teva Branded Pharm
  • Nov 21, 2003NDANDA021258Bayer Hlthcare
  • Mar 16, 2006NDANDA021676Bayer Hlthcare
  • Jun 4, 2007NDANDA022038Vertical Pharms

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
190,010 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Pain19,10610%
  2. 2Pulmonary Embolism14,3567.6%
  3. 3Injury11,7706.2%
  4. 4Deep Vein Thrombosis11,7136.2%
  5. 5Nausea11,4916.0%
  6. 6Drug Ineffective11,3826.0%
  7. 7Anxiety11,2965.9%
  8. 8Headache10,4915.5%
  9. 9Off Label Use9,4034.9%
  10. 10Fatigue8,7854.6%
  11. 11Product Adhesion Issue7,5013.9%
  12. 12Emotional Distress7,0043.7%
  13. 13Dyspnoea6,8833.6%
  14. 14Vomiting6,2133.3%
  15. 15Diarrhoea6,0593.2%

Literature

View JSON

Recent PubMed references pinned to Estradiol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 1,969 ClinicalTrials.gov registrations naming Estradiol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Estradiol work?
Mechanism-of-action class: Estrogen Receptor Agonists.
What is Estradiol used for?
According to FDA labeling, Estradiol carries indications including: Estradiol Vaginal Cream, 0.01% is indicated in the treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Estradiol?
Estradiol is classified as Natural and semisynthetic estrogens, plain, Estrogen, Estrogen Receptor Agonists, Bone Formation Stimulation, Gonadotropin Releasing Hormone Alteration, Hematologic Activity Alteration, Vaginal Function Alteration.
What are the brand names for Estradiol?
Estradiol is marketed under brand names including Alora, Bijuva, Climara, Climara Pro, Combipatch, Compudose, Delestrogen, Depo-estradiol.
What are the contraindications for Estradiol?
Estradiol labeling lists contraindications including: Estradiol Vaginal Cream, 0.01% should not be used in women with any of the following conditions: 1. Undiagnosed abnormal genital bleeding.. Always consult the full prescribing information and a clinician.
Note. Data for estradiol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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