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Estradiol 1mg Tablets

Manufacturer TEVA Active Ingredient Estradiol Oral Tablets(es tra DYE ole) Pronunciation es-tra-DYE-ole
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.
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Drug Class
Estrogen
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Pharmacologic Class
Estrogen receptor agonist
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Pregnancy Category
Not recommended (Historically X)
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FDA Approved
Jun 1975
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DEA Schedule
Not Controlled

Overview

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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 treat certain conditions where the body doesn't make enough estrogen. If you still have your uterus, your doctor will usually prescribe a progestin along with estradiol to protect your uterus.
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How to Use This Medicine

Taking Your Medication

To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication at the same time every day. Note that there may be days when you are not scheduled to take your medication.

You can take your medication with or without food. If it causes stomach upset, taking it with food may help.

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 your medication is no longer needed or has expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult your pharmacist, who can also inform you about any drug take-back programs in your area.

What to Do If You Miss 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 continue with your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
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Lifestyle & Tips

  • Do not smoke, as smoking significantly increases the risk of blood clots, stroke, and heart attack, especially when taking estrogens.
  • Maintain a healthy diet and engage in regular physical activity to support bone health and cardiovascular health.
  • Limit alcohol consumption.
  • Discuss any new medications, supplements, or herbal products with your doctor, as they may interact with estradiol.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: For moderate to severe vasomotor symptoms associated with menopause: 1 mg orally once daily. 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 orally once daily (may be adjusted from 0.5 mg to 2 mg)
preventionOfOsteoporosis: 0.5 mg or 1 mg orally once daily
femaleHypogonadism: 1 mg to 2 mg orally once daily, cyclically (e.g., 3 weeks on, 1 week off)
atrophicVaginitisUrethritis: 0.5 mg to 2 mg orally once daily
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: For female hypogonadism: 0.5 mg to 2 mg orally once daily, cyclically, titrated based on response. Dosing should be individualized.
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment needed.
Moderate: No specific dose adjustment needed.
Severe: Use with caution; monitor for adverse effects. No specific dose adjustment guidelines.
Dialysis: Not available; use with caution.

Hepatic Impairment:

Mild: Use with caution; monitor for adverse effects.
Moderate: Use with caution; consider lower starting dose and monitor closely. Estrogens are extensively metabolized by the liver.
Severe: Contraindicated in severe hepatic dysfunction or disease.
Confidence: Medium

Pharmacology

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Mechanism of Action

Estradiol is the primary estrogen secreted by the human ovary. It binds to and activates nuclear estrogen receptors (ERΞ± and ERΞ²) in target tissues, including the female reproductive tract, breast, hypothalamus, pituitary, bone, and liver. This binding leads to gene transcription and protein synthesis, mediating the physiological effects of estrogen, such as the development and maintenance of the female reproductive system and secondary sex characteristics. In postmenopausal women, it replaces the declining endogenous estrogen levels.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 5% (due to significant first-pass metabolism)
Tmax: Approximately 5-8 hours
FoodEffect: Food may slightly decrease the rate but not the extent of absorption.

Distribution:

Vd: Approximately 1 L/kg
ProteinBinding: Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration: Limited

Elimination:

HalfLife: Approximately 13-17 hours (for estradiol); longer for metabolites
Clearance: Approximately 650-1000 mL/min
ExcretionRoute: Primarily renal (as glucuronide and sulfate conjugates), some fecal
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Days to weeks for full therapeutic effect (e.g., reduction in hot flashes)
PeakEffect: Weeks to months for maximal effect (e.g., bone density improvement)
DurationOfAction: Approximately 24 hours (due to sustained levels from daily dosing and enterohepatic recirculation)

Safety & Warnings

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BLACK BOX WARNING

Estrogens and Estrogen Plus Progestin Therapy:
1. **Cardiovascular Disorders:** Estrogen-alone therapy and estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease. The Women's Health Initiative (WHI) study reported increased risks of stroke and deep vein thrombosis (DVT) in postmenopausal women receiving estrogen-alone therapy. The WHI study reported increased risks of myocardial infarction (MI), stroke, invasive breast cancer, pulmonary embolism (PE), and DVT in postmenopausal women receiving estrogen plus progestin therapy.
2. **Malignant Neoplasms:**
* **Endometrial Cancer:** 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 can be a precursor to endometrial cancer.
* **Breast Cancer:** The WHI study reported an increased risk of invasive breast cancer in women receiving estrogen plus progestin therapy. Observational studies have also reported an increased risk of breast cancer with estrogen-alone therapy after several years of use.
* **Ovarian Cancer:** Some epidemiological studies suggest a small increased risk of ovarian cancer with estrogen-alone use, but the overall evidence is inconsistent.
3. **Dementia:** The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving estrogen-alone therapy or estrogen plus progestin therapy. It is unknown whether this finding applies to younger postmenopausal women.
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Side Effects

Serious Side Effects: Seek Medical Attention Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical help right away:

Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
 Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallbladder problems, such as:
+ Pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
+ Bloating
+ Severe upset stomach or vomiting
 Signs of pancreatitis (pancreas problem), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of high blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
 Weakness on one side of the body
Trouble speaking or thinking
 Changes in balance
Drooping on one side of the face
 Blurred eyesight
Eyesight changes or loss
 Bulging eyes
Changes in how contact lenses feel
 Breast lump, pain, or soreness
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, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, inform your doctor.

Blood Clots and High Calcium Levels

Seek medical attention immediately if you experience signs of a blood clot, such as:

Chest pain or pressure
 Coughing up blood
Shortness of breath
 Swelling, warmth, numbness, changes in color, or pain in a leg or arm
Trouble speaking or swallowing

High calcium levels can occur with this medication, especially in people with cancer. Contact your doctor if you experience signs of high calcium levels, such as:

 Weakness
Confusion
 Fatigue
Headache
 Upset stomach or vomiting
Constipation
 Bone pain

Other Side Effects

Most people do not experience severe side effects, and some may not experience any side effects at all. However, if you experience any of the following side effects, contact your doctor or seek medical help if they bother you or do not go away:

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
 Signs of a common cold
Nose or throat irritation
 Weight gain or loss
Joint pain
 Leg cramps
* Changes in sex interest

Reporting Side Effects

This is not an exhaustive list of potential side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden chest pain or shortness of breath
  • Sudden severe headache or problems with vision, speech, or balance
  • Pain, swelling, or redness in your leg (especially calf or thigh)
  • Yellowing of your skin or eyes (jaundice)
  • New breast lump or changes in your breasts
  • Unusual vaginal bleeding or spotting
  • Severe stomach pain
  • Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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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. Be sure to describe the allergic reaction and its symptoms.
 A history of certain health conditions, such as:
+ 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 suspected 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 problems 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 change the dose of any medication without consulting your doctor first.
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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 work and bone density tests 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.

This medication may cause elevated triglyceride levels, so inform your doctor if you have a history of high triglyceride levels.

Prolonged use of this medication may lead to the development of dark skin patches on the face. To minimize this risk, avoid exposure to sunlight, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear when outdoors.

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.

To maximize the effectiveness of this medication, use it 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 outlined by your doctor.

In rare 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.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Breast tenderness
  • Abdominal pain
  • Drowsiness/fatigue
  • Withdrawal bleeding (in females)

What to Do:

Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). There is no specific antidote; treatment is supportive. Overdose is generally not life-threatening.

Drug Interactions

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Contraindicated Interactions

  • Not available (no absolute contraindications based on drug-drug interactions)
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Major Interactions

  • Aromatase inhibitors (e.g., anastrozole, letrozole): May decrease efficacy of aromatase inhibitors.
  • Thyroid hormone replacement therapy (e.g., levothyroxine): Estrogens may increase thyroid-binding globulin, leading to increased thyroid hormone requirements.
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Moderate Interactions

  • CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort): May decrease estradiol plasma concentrations, reducing efficacy.
  • CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice): May increase estradiol plasma concentrations, potentially increasing adverse effects.
  • Corticosteroids (e.g., prednisone): Estrogens may decrease the clearance of corticosteroids, leading to increased effects.
  • Oral anticoagulants (e.g., warfarin): Estrogens may alter the effects of anticoagulants; monitor INR/PT.
  • Flibanserin: Increased flibanserin exposure.
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Minor Interactions

  • Not available (interactions are generally categorized as moderate or major due to clinical significance)

Monitoring

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Baseline Monitoring

Complete medical history and physical examination

Rationale: To identify contraindications, risk factors for cardiovascular disease, breast cancer, and other conditions.

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 baseline hepatic function.

Timing: Prior to initiation of therapy.

Mammogram

Rationale: To screen for breast cancer before starting hormone therapy.

Timing: Prior to initiation of therapy (within 12 months).

Pelvic examination and Pap test

Rationale: To screen for gynecological conditions, including endometrial cancer (if uterus intact) and cervical cancer.

Timing: Prior to initiation of therapy (within 12 months).

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Routine Monitoring

Blood pressure

Frequency: Annually or as clinically indicated.

Target: <130/80 mmHg (general target)

Action Threshold: Sustained elevation requiring intervention.

Mammogram

Frequency: Annually or as recommended by guidelines.

Target: Normal findings

Action Threshold: Abnormal findings requiring further investigation.

Pelvic examination and Pap test

Frequency: Annually or as recommended by guidelines.

Target: Normal findings

Action Threshold: Abnormal findings or unexplained vaginal bleeding.

Breast examination (clinical and self-exam)

Frequency: Annually (clinical); monthly (self-exam).

Target: No new lumps or changes

Action Threshold: Any new or suspicious breast changes.

Symptom review (e.g., signs of DVT/PE, stroke, MI, abnormal bleeding)

Frequency: At each visit (e.g., every 6-12 months).

Target: Absence of concerning symptoms

Action Threshold: Presence of new or worsening symptoms requiring immediate evaluation.

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Symptom Monitoring

  • Unusual vaginal bleeding or spotting
  • Breast lumps or changes
  • Chest pain, shortness of breath, sudden severe headache
  • Sudden vision changes
  • Pain, swelling, or tenderness in one leg
  • Yellowing of skin or eyes (jaundice)
  • Severe abdominal pain
  • Memory loss or cognitive decline (in women >65 years)

Special Patient Groups

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Pregnancy

Contraindicated during pregnancy. There is no indication for estradiol in pregnancy, and there is evidence of potential harm to the fetus. Historically classified as Pregnancy Category X.

Trimester-Specific Risks:

First Trimester: Potential for adverse effects on fetal development, including genital abnormalities.
Second Trimester: Not applicable, as use is contraindicated.
Third Trimester: Not applicable, as use is contraindicated.
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Lactation

Not recommended during lactation. Estrogens can decrease the quantity and quality of breast milk and may be excreted in breast milk, potentially affecting the infant.

Infant Risk: L3 (Moderate risk) - Potential for adverse effects on the infant (e.g., feminization, jaundice) and reduction in milk supply. Consider alternative therapies or discontinue breastfeeding.
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Pediatric Use

Generally not indicated for pediatric use, except for specific conditions like female hypogonadism. Safety and efficacy in prepubertal children have not been established. Use in adolescents for hypogonadism should be carefully monitored by a specialist.

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Geriatric Use

Use with caution in women 65 years of age or older. The WHIMS study showed an increased risk of probable dementia in women 65 years of age or older receiving estrogen-alone or estrogen plus progestin therapy. Increased risk of stroke and DVT has also been observed in older women. Lowest effective dose for the shortest duration is recommended.

Clinical Information

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Clinical Pearls

  • Oral estradiol undergoes significant first-pass metabolism, leading to higher estrone levels compared to estradiol levels. This is different from transdermal estradiol, which bypasses first-pass metabolism.
  • Always prescribe a progestin concurrently with estradiol in women with an intact uterus to reduce the risk of endometrial cancer.
  • The lowest effective dose for the shortest duration consistent with treatment goals should be used, especially for menopausal symptom management.
  • Regular monitoring, including breast exams, mammograms, and pelvic exams, is crucial due to the increased risks of certain cancers and cardiovascular events.
  • Patients should be educated on the signs and symptoms of serious adverse events (e.g., blood clots, stroke, heart attack, breast changes) and instructed to seek immediate medical attention if they occur.
  • Estradiol is not indicated for the prevention of cardiovascular disease or dementia.
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Alternative Therapies

  • Selective Estrogen Receptor Modulators (SERMs) (e.g., ospemifene for dyspareunia, raloxifene for osteoporosis prevention)
  • Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
  • Local vaginal estrogen for genitourinary syndrome of menopause (e.g., vaginal creams, rings, tablets)
  • Bisphosphonates or other anti-resorptive agents for osteoporosis.
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Cost & Coverage

Average Cost: $15 - $50 per 30 tablets (1mg)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (for generic estradiol)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to 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 seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.