Estradiol 2mg Tablets
WARNING: Do not use this drug to prevent heart disease or dementia. A study of women taking an estrogen with a progestin showed a raised chance of heart attack, stroke, blood clot, breast cancer, and dementia. The chance of stroke, blood clot, and dementia was also raised when the estrogen was taken alone. Not all products and doses were studied. It is not known if the same effects may happen with this drug.The chance of endometrial cancer may be raised with the use of estrogen alone in patients with a uterus. Use of a progestin along with estrogen may lower the risk. Call your doctor right away if you have unexplained or long-lasting vaginal bleeding.Use this drug for the shortest time needed at the lowest useful dose. Your doctor will talk with you on a regular basis to see if you need to keep taking this drug. @ COMMON USES: It is used to prevent soft, brittle bones (osteoporosis) after menopause.It is used to prevent or lower the signs of the change of life (menopause).It is used to add estrogen to the body when the ovaries have been taken out or do not work the right way.Rarely, it is used to treat breast or prostate cancers.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Estrogen; Hormone Replacement Therapy (HRT)
Pharmacologic Class
Estrogen receptor agonist
Pregnancy Category
Category X
FDA Approved
Jun 1975
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol is a type of estrogen, a female hormone. It's used to treat symptoms of menopause like hot flashes and vaginal dryness, to prevent bone loss (osteoporosis) after menopause, and to replace hormones in women whose bodies don't make enough estrogen. It works by acting like the natural estrogen in your body.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication at the same time every day. Note that there may be days when you are not scheduled to take this medication. You can take it with or without food, but if it causes stomach upset, take it with food.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also have access to local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication at the same time every day. Note that there may be days when you are not scheduled to take this medication. You can take it with or without food, but if it causes stomach upset, take it with food.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also have access to local drug take-back programs.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Do not smoke while taking this medication, as smoking significantly increases the risk of blood clots, stroke, and heart attack.
- Maintain a healthy diet and engage in regular exercise to support overall health and bone density.
- Discuss any new or worsening symptoms with your doctor promptly.
- Attend all scheduled follow-up appointments and screenings (e.g., mammograms, pelvic exams).
Available Forms & Alternatives
Available Strengths:
- Estradiol 0.05mg Patch (once Wk)
- Estradiol 0.1mg Patch (once Wk)
- Estradiol 1mg Tablets
- Estradiol 2mg Tablets
- Estradiol 0.5mg Tablets
- Estradiol 0.025mg Patch (once Wk)
- Estradiol 0.075mg Patch (once Wk)
- Estradiol Tds 0.0375mg Patches 4s
- Estradiol Tds 0.06mg Patch 4s
- Estradiol 0.025mg Patch (twice Wk)
- Estradiol 0.075mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk)
- Estradiol 0.1mg Patch (twice Wk)
- Estradiol 0.05mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk
- Estradiol 10mcg Vaginal Tabs 8s
- Estradiol 10mcg Vaginal Tabs 18s
- Estradiol 0.01% Vag Cream 42.5gm
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.06% Gel 37.5gm(pumps)
- Estradiol 0.06% Gel 37.5gm(pumps)
Dosing & Administration
Adult Dosing
Standard Dose:
Dosage varies by indication. For moderate to severe vasomotor symptoms associated with menopause: 1 mg or 2 mg orally once daily. For vulvar and vaginal atrophy: 1 mg or 2 mg orally once daily. For female hypogonadism: 1 mg or 2 mg orally once daily, adjusted based on response. For prevention of postmenopausal osteoporosis: 0.5 mg or 1 mg orally once daily.
Dose Range:
0.5 - 2 mg
Condition-Specific Dosing:
vasomotorSymptoms:
1 mg or 2 mg orally once daily
vulvarVaginalAtrophy:
1 mg or 2 mg orally once daily
femaleHypogonadism:
1 mg or 2 mg orally once daily, adjusted based on response
postmenopausalOsteoporosisPrevention:
0.5 mg or 1 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
For female hypogonadism, initial dose typically 0.5 mg orally once daily, gradually increased to 1 mg or 2 mg daily over 1-2 years to mimic pubertal development.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment generally required.
Moderate:
No specific dose adjustment generally required, but use with caution.
Severe:
No specific dose adjustment generally required, but use with caution and monitor for adverse effects.
Dialysis:
Considerations: Not extensively studied, use with caution.
Hepatic Impairment:
Mild:
Use with caution; monitor for adverse effects.
Moderate:
Use with caution; consider lower doses. Estrogens are extensively metabolized by the liver.
Severe:
Contraindicated in severe hepatic impairment due to impaired metabolism and increased risk of adverse effects.
Pharmacology
Mechanism of Action
Estradiol is the primary and most potent estrogen produced by the human ovary. It binds to and activates nuclear estrogen receptors (ERΞ± and ERΞ²) in target tissues, leading to gene transcription and protein synthesis. This results in the expression of estrogen-specific effects, including the development and maintenance of female reproductive organs and secondary sex characteristics, and effects on bone, cardiovascular system, and central nervous system.
Pharmacokinetics
Absorption:
Bioavailability:
3-5% (oral, due to extensive first-pass metabolism)
Tmax:
4-6 hours (oral)
FoodEffect:
Food may slightly delay absorption but does not significantly alter bioavailability.
Distribution:
Vd:
Approximately 1 L/kg
ProteinBinding:
Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration:
Limited, but active in CNS for certain effects (e.g., vasomotor symptoms).
Elimination:
HalfLife:
1-2 hours (estradiol itself); 10-16 hours (estrone, estriol)
Clearance:
High hepatic clearance
ExcretionRoute:
Mainly renal (urine) as glucuronide and sulfate conjugates; some fecal excretion.
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Varies by effect; symptomatic relief (e.g., hot flashes) may begin within weeks.
PeakEffect:
Symptomatic relief may peak within 4-8 weeks.
DurationOfAction:
Effects persist as long as therapy is continued; hormonal effects last for the dosing interval.
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
WARNING: ESTROGENS AND PROGESTINS
CARDIOVASCULAR DISORDERS AND PROBABLE DEMENTIA
Estrogens and progestins should not be used for the prevention of cardiovascular disease or dementia.
Estrogen-alone therapy:
β’ The Womenβs Health Initiative (WHI) estrogen-alone substudy reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women aged 50-79 years during 7.1 years of treatment with daily oral conjugated estrogens (CE) [0.625 mg].
β’ The WHI Memory Study (WHIMS) estrogen-alone ancillary study of the WHI study reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 5.2 years of treatment with daily oral CE [0.625 mg].
Estrogen plus progestin therapy:
β’ The WHI estrogen plus progestin substudy reported increased risks of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women aged 50-79 years during 5.6 years of treatment with daily oral CE [0.625 mg] combined with medroxyprogesterone acetate (MPA) [2.5 mg].
β’ The WHIMS estrogen plus progestin ancillary study of the WHI study reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily oral CE [0.625 mg] combined with MPA [2.5 mg].
ENDOMETRIAL CANCER
β’ The use of estrogen-alone therapy in women with a uterus is associated with an increased risk of endometrial cancer. 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 all cases of undiagnosed persistent or recurrent abnormal genital bleeding.
BREAST CANCER
β’ The WHI estrogen plus progestin substudy reported an increased risk of invasive breast cancer in women receiving daily oral CE [0.625 mg] combined with MPA [2.5 mg] for 5.6 years. Observational studies also suggest an increased risk of breast cancer with estrogen-alone therapy after several years of use. The most important randomized clinical trial to date providing information about estrogen-alone and estrogen plus progestin therapy and breast cancer is the WHI study. See WARNINGS section for additional information.
CARDIOVASCULAR DISORDERS AND PROBABLE DEMENTIA
Estrogens and progestins should not be used for the prevention of cardiovascular disease or dementia.
Estrogen-alone therapy:
β’ The Womenβs Health Initiative (WHI) estrogen-alone substudy reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women aged 50-79 years during 7.1 years of treatment with daily oral conjugated estrogens (CE) [0.625 mg].
β’ The WHI Memory Study (WHIMS) estrogen-alone ancillary study of the WHI study reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 5.2 years of treatment with daily oral CE [0.625 mg].
Estrogen plus progestin therapy:
β’ The WHI estrogen plus progestin substudy reported increased risks of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women aged 50-79 years during 5.6 years of treatment with daily oral CE [0.625 mg] combined with medroxyprogesterone acetate (MPA) [2.5 mg].
β’ The WHIMS estrogen plus progestin ancillary study of the WHI study reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily oral CE [0.625 mg] combined with MPA [2.5 mg].
ENDOMETRIAL CANCER
β’ The use of estrogen-alone therapy in women with a uterus is associated with an increased risk of endometrial cancer. 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 all cases of undiagnosed persistent or recurrent abnormal genital bleeding.
BREAST CANCER
β’ The WHI estrogen plus progestin substudy reported an increased risk of invasive breast cancer in women receiving daily oral CE [0.625 mg] combined with MPA [2.5 mg] for 5.6 years. Observational studies also suggest an increased risk of breast cancer with estrogen-alone therapy after several years of use. The most important randomized clinical trial to date providing information about estrogen-alone and estrogen plus progestin therapy and breast cancer is the WHI study. See WARNINGS section for additional information.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or soreness, or nipple discharge.
Vaginal itching or discharge.
Abnormal vaginal bleeding.
Depression or other mood changes.
Memory problems or loss.
Fever.
Difficulty urinating or changes in urine output.
Pain while urinating.
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or breathing difficulties.
Blood Clots and High Calcium Levels
Seek immediate medical attention if you experience:
Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, changes in color, or pain in a leg or arm; or trouble speaking or swallowing.
Signs of high calcium levels (more common in people with cancer): weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only mild ones. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Dizziness or headache.
Hair loss.
Upset stomach or vomiting.
Constipation.
Stomach pain or cramps.
Bloating.
Enlarged or tender breasts.
Vaginal bleeding or spotting.
Painful periods.
Common cold symptoms.
Nose or throat irritation.
Weight gain or loss.
Joint pain.
Leg cramps.
Changes in sex interest.
This is not an exhaustive list of possible side effects. If you have concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast lump, breast pain or soreness, or nipple discharge.
Vaginal itching or discharge.
Abnormal vaginal bleeding.
Depression or other mood changes.
Memory problems or loss.
Fever.
Difficulty urinating or changes in urine output.
Pain while urinating.
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or breathing difficulties.
Blood Clots and High Calcium Levels
Seek immediate medical attention if you experience:
Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, changes in color, or pain in a leg or arm; or trouble speaking or swallowing.
Signs of high calcium levels (more common in people with cancer): weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only mild ones. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:
Dizziness or headache.
Hair loss.
Upset stomach or vomiting.
Constipation.
Stomach pain or cramps.
Bloating.
Enlarged or tender breasts.
Vaginal bleeding or spotting.
Painful periods.
Common cold symptoms.
Nose or throat irritation.
Weight gain or loss.
Joint pain.
Leg cramps.
Changes in sex interest.
This is not an exhaustive list of possible side effects. If you have concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache or migraine.
- Sudden vision changes (e.g., partial or complete loss of vision).
- Sudden numbness or weakness on one side of the body.
- Slurred speech or difficulty speaking.
- Sudden chest pain, shortness of breath, or coughing up blood.
- Pain, swelling, or redness in one leg.
- Yellowing of the skin or eyes (jaundice).
- New breast lump, breast pain, or nipple discharge.
- Unusual vaginal bleeding (e.g., spotting, breakthrough bleeding, prolonged bleeding).
- Severe abdominal pain.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the signs and symptoms you experienced.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication should not be taken during pregnancy.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the signs and symptoms you experienced.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication should not be taken during pregnancy.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.
If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged immobility may increase your risk of developing blood clots.
If you have a known allergy to tartrazine (FD&C Yellow No. 5), consult your doctor, as some products contain this ingredient.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. This medication may cause high blood pressure, so regular blood pressure checks are necessary, as advised by your doctor.
Regular blood tests and bone density checks are also recommended, as directed by your doctor. Additionally, schedule regular breast exams and gynecology check-ups, and perform breast self-exams as instructed by your doctor.
The risk of certain side effects, such as heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
High triglyceride levels have been associated with this medication, so inform your doctor if you have a history of elevated triglyceride levels.
This medication may cause dark skin patches on the face, so avoid sun exposure, sunlamps, and tanning beds. Use sunscreen and protective clothing and eyewear to minimize sun exposure.
This medication may interfere with certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug.
Smoking increases the risk of heart disease, so it is essential to avoid smoking. Limit your alcohol consumption and discuss any concerns with your doctor.
If you regularly consume grapefruit juice or eat grapefruit, consult your doctor, as this may interact with the medication.
For optimal effectiveness, use this medication in conjunction with calcium and vitamin D supplements and engage in weight-bearing exercises, such as walking or physical therapy, as recommended by your doctor. Adhere to the diet and exercise plan prescribed by your doctor.
In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss any concerns with your doctor.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.
If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged immobility may increase your risk of developing blood clots.
If you have a known allergy to tartrazine (FD&C Yellow No. 5), consult your doctor, as some products contain this ingredient.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. This medication may cause high blood pressure, so regular blood pressure checks are necessary, as advised by your doctor.
Regular blood tests and bone density checks are also recommended, as directed by your doctor. Additionally, schedule regular breast exams and gynecology check-ups, and perform breast self-exams as instructed by your doctor.
The risk of certain side effects, such as heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
High triglyceride levels have been associated with this medication, so inform your doctor if you have a history of elevated triglyceride levels.
This medication may cause dark skin patches on the face, so avoid sun exposure, sunlamps, and tanning beds. Use sunscreen and protective clothing and eyewear to minimize sun exposure.
This medication may interfere with certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug.
Smoking increases the risk of heart disease, so it is essential to avoid smoking. Limit your alcohol consumption and discuss any concerns with your doctor.
If you regularly consume grapefruit juice or eat grapefruit, consult your doctor, as this may interact with the medication.
For optimal effectiveness, use this medication in conjunction with calcium and vitamin D supplements and engage in weight-bearing exercises, such as walking or physical therapy, as recommended by your doctor. Adhere to the diet and exercise plan prescribed by your doctor.
In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss any concerns with your doctor.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects.
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Breast tenderness
- Abdominal pain
- Drowsiness/fatigue
- Withdrawal bleeding (in females)
What to Do:
There is no specific antidote for estrogen overdose. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Major Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane) - concurrent use would counteract their effect.
- Tranexamic acid - increased risk of thrombosis.
Moderate Interactions
- CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol levels.
- CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice) - may increase estradiol levels.
- Thyroid hormones (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin, potentially increasing thyroid hormone requirements.
- Corticosteroids - estrogens may decrease corticosteroid clearance, leading to increased effects.
- Anticoagulants (e.g., warfarin) - estrogens may alter anticoagulant effects; monitor INR.
Minor Interactions
- Folic acid - may reduce efficacy of folic acid.
- Vitamin B6 - may reduce efficacy of vitamin B6.
Monitoring
Baseline Monitoring
Complete medical history and physical examination
Rationale: To identify contraindications, risk factors (e.g., VTE, breast cancer, cardiovascular disease), and establish baseline health.
Timing: Prior to initiation of therapy.
Blood pressure
Rationale: Estrogens can affect blood pressure.
Timing: Prior to initiation of therapy.
Lipid profile
Rationale: Estrogens can affect lipid metabolism.
Timing: Prior to initiation of therapy.
Liver function tests (LFTs)
Rationale: Estrogens are metabolized by the liver; assess hepatic function.
Timing: Prior to initiation of therapy, especially if history of liver disease.
Breast examination and mammogram
Rationale: To screen for breast cancer, as estrogen therapy can increase risk.
Timing: Prior to initiation of therapy, and as clinically indicated.
Pelvic examination and Pap test
Rationale: To screen for gynecological conditions, including endometrial cancer (if unopposed estrogen).
Timing: Prior to initiation of therapy, and as clinically indicated.
Routine Monitoring
Annual physical examination, including blood pressure
Frequency: Annually
Target: Normal for age and health status
Action Threshold: Significant changes or sustained hypertension require evaluation.
Annual breast examination and mammogram
Frequency: Annually (or as per national guidelines)
Target: No suspicious findings
Action Threshold: New lumps, pain, nipple discharge, or abnormal mammogram findings require immediate investigation.
Annual pelvic examination and Pap test
Frequency: Annually (or as per national guidelines)
Target: No suspicious findings
Action Threshold: Abnormal bleeding, pain, or Pap test results require investigation.
Lipid profile
Frequency: Periodically, as clinically indicated
Target: Individualized based on cardiovascular risk
Action Threshold: Significant adverse changes require evaluation and management.
Symptom Monitoring
- Signs of deep vein thrombosis (DVT) or pulmonary embolism (PE): leg pain, swelling, redness, shortness of breath, chest pain.
- Signs of stroke: sudden severe headache, vision changes, weakness or numbness on one side of the body, slurred speech.
- Signs of myocardial infarction (MI): chest pain, discomfort in arms/back/neck/jaw/stomach, shortness of breath, cold sweat, nausea, lightheadedness.
- Abnormal vaginal bleeding (spotting, breakthrough bleeding, prolonged bleeding).
- Breast lumps, pain, or nipple discharge.
- Severe headache or migraine.
- Jaundice or signs of liver dysfunction (e.g., dark urine, pale stools, persistent nausea/vomiting).
Special Patient Groups
Pregnancy
Contraindicated during pregnancy. There is no indication for estrogen therapy in pregnancy, and there is evidence of potential harm to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal abnormalities (e.g., cardiovascular, limb defects) if exposed during critical periods of organogenesis.
Second Trimester:
No established benefit; continued exposure may pose risks.
Third Trimester:
No established benefit; continued exposure may pose risks.
Lactation
Not recommended during lactation. Estradiol is excreted into breast milk and may decrease the quantity and quality of breast milk. Potential adverse effects on the infant are not well-established but cannot be ruled out.
Infant Risk:
Low to moderate risk of direct adverse effects on the infant; however, significant risk of reducing milk supply.
Pediatric Use
Generally not indicated for children, except for specific conditions like female hypogonadism where it is used to induce puberty. Use in pediatric patients should be carefully monitored by a specialist.
Geriatric Use
Increased risks of stroke, deep vein thrombosis, pulmonary embolism, and probable dementia in women 65 years of age or older. Use the lowest effective dose for the shortest duration consistent with treatment goals. Regular re-evaluation of the need for continued therapy is crucial.
Clinical Information
Clinical Pearls
- Always use the lowest effective dose for the shortest duration consistent with treatment goals, especially for postmenopausal hormone therapy.
- For women with an intact uterus, estradiol must be prescribed with a progestin to reduce the risk of endometrial cancer.
- Counsel patients on the importance of regular follow-up appointments, including breast exams and mammograms.
- Emphasize the increased risk of blood clots, stroke, and heart attack, particularly in smokers and older women.
- Patients should be advised to report any unusual vaginal bleeding immediately.
- Oral estradiol undergoes significant first-pass metabolism, leading to a higher estrone-to-estradiol ratio compared to transdermal formulations.
Alternative Therapies
- Selective Estrogen Receptor Modulators (SERMs) for osteoporosis (e.g., raloxifene) or vasomotor symptoms (e.g., bazedoxifene/conjugated estrogens combination).
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine).
- Bisphosphonates or other anti-resorptive agents for osteoporosis.
- Ospemifene for vulvar and vaginal atrophy.
- Local vaginal moisturizers and lubricants for vaginal atrophy.
Cost & Coverage
Average Cost:
$15 - $50 per 30 tablets (generic 2mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic formulations) on most commercial and Medicare Part D plans.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.