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Estradiol 0.5mg 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; Hormone Replacement Therapy (HRT)
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Pharmacologic Class
Estrogen receptor agonist
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Pregnancy Category
Category X
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FDA Approved
Aug 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, and to help prevent bone thinning (osteoporosis) after menopause. It works by replacing the estrogen your body no longer makes enough of.
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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 location, avoiding the bathroom. Keep all medications in a safe place, 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, consult your pharmacist for guidance on proper disposal. You may also want to check if there are drug take-back programs available in your area.

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.
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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 estrogen.
  • Maintain a healthy weight and engage in regular physical activity to support cardiovascular health and bone density.
  • Discuss any new medications, supplements, or herbal products with your doctor, as they may interact with estradiol.
  • Report any unusual vaginal bleeding, breast lumps, or symptoms of blood clots (e.g., chest pain, shortness of breath, leg pain/swelling) immediately.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: 0.5 mg orally once daily (for specific indications like vasomotor symptoms or vulvar and vaginal atrophy)
Dose Range: 0.5 - 2 mg

Condition-Specific Dosing:

vasomotorSymptomsOfMenopause: 0.5 mg to 1 mg orally once daily, may be adjusted based on response and tolerability. Cyclical or continuous regimen.
vulvarAndVaginalAtrophy: 0.5 mg to 1 mg orally once daily, may be adjusted based on response and tolerability. Cyclical or continuous regimen.
preventionOfPostmenopausalOsteoporosis: 0.5 mg orally once daily, typically as part of a continuous regimen.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Estradiol is not indicated for pediatric use for HRT; specific uses for hypogonadism in adolescents would involve different dosing and formulations)
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended, use with caution.
Moderate: No specific dose adjustment recommended, use with caution.
Severe: No specific dose adjustment recommended, use with caution, monitor for adverse effects.
Dialysis: Not specifically studied, use with caution.

Hepatic Impairment:

Mild: Use with caution, monitor for adverse effects.
Moderate: Generally not recommended due to extensive hepatic metabolism and potential for exacerbation of liver dysfunction.
Severe: Contraindicated in patients with severe liver dysfunction or disease.

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, leading to gene transcription and protein synthesis. This results in the expression of estrogen-specific effects, including those on the reproductive system, bone, cardiovascular system, and central nervous system.
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Pharmacokinetics

Absorption:

Bioavailability: Low (approx. 5% for oral estradiol due to extensive first-pass metabolism)
Tmax: Oral: 5-8 hours
FoodEffect: Food may slightly delay absorption but does not significantly alter bioavailability.

Distribution:

Vd: Not precisely quantified for oral estradiol, but widely distributed throughout the body.
ProteinBinding: Approximately 98% bound to sex hormone-binding globulin (SHBG) and albumin.
CnssPenetration: Limited (crosses the blood-brain barrier, but therapeutic effects are primarily peripheral for HRT indications).

Elimination:

HalfLife: Oral: 13-17 hours (for estradiol, but estrone and other metabolites have longer half-lives)
Clearance: Not precisely quantified for oral estradiol.
ExcretionRoute: Primarily renal (urine) as glucuronide and sulfate conjugates; some fecal excretion.
Unchanged: <1% (due to extensive metabolism)
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Pharmacodynamics

OnsetOfAction: Days to weeks for symptomatic relief (e.g., hot flashes), longer for bone density effects.
PeakEffect: Weeks to months for full therapeutic effect.
DurationOfAction: Effects persist as long as therapy is continued; related to half-life and receptor binding kinetics.

Safety & Warnings

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BLACK BOX WARNING

Estrogens and estrogen plus progestin therapies should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5.2 years of treatment with conjugated equine estrogens (CEE) alone or CEE plus medroxyprogesterone acetate (MPA). The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older. These risks should be weighed against the benefits of therapy, and estrogens should be prescribed at the lowest effective dose for the shortest duration consistent with treatment goals and risks for the individual woman.
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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: 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 changes: lump in the breast, breast pain or soreness, or nipple discharge
Vaginal changes: itching or discharge, or abnormal vaginal bleeding
 Depression or other mood changes
Memory problems or loss
 Fever
Urination problems: inability to pass urine or changes in urine output, or pain while passing urine

Fluid Retention and Swelling

This medication may cause fluid retention and swelling in the body. If you experience swelling, weight gain, or trouble breathing, contact 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 in some people with cancer taking this medication. Contact your doctor if you experience:
Weakness
 Confusion
Feeling tired
 Headache
Upset stomach or vomiting
 Constipation
Bone pain

Other Side Effects

Most people do not experience serious side effects, but some may occur. 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

If you have questions 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 severe headache or migraine
  • Sudden partial or complete loss of vision
  • Sudden numbness or weakness in an arm or leg, especially on one side of the body
  • Chest pain or heaviness, pain spreading to arm or shoulder, nausea, sweating, general ill feeling
  • Shortness of breath, sudden cough, rapid breathing
  • Pain, swelling, warmth, or redness in one or both legs
  • Yellowing of the skin or eyes (jaundice)
  • Dark urine, light-colored stools
  • New breast lump or nipple discharge
  • Unusual vaginal bleeding or spotting after menopause
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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, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
 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 in conjunction with your other treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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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 it may increase your risk of developing blood clots.

If you have a tartrazine (FD&C Yellow No. 5) allergy, consult your doctor, as some products contain this ingredient.

If you have diabetes (high blood sugar), closely monitor your blood sugar levels. This medication can cause high blood pressure, so have your blood pressure checked as directed by your doctor.

Regularly have your blood work and bone density checked as advised by your doctor. It is also crucial to have regular breast exams and gynecology check-ups, and to perform breast self-exams as instructed.

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 can 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 your face. To minimize this risk, avoid sun exposure, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear.

This medication may affect certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug.

Smoking can increase 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 it may interact with this 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 directed by your doctor. Follow the diet and exercise plan recommended 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:

There is no specific antidote. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center immediately (Call 1-800-222-1222 in the US).

Drug Interactions

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Contraindicated Interactions

  • Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use would counteract their mechanism of action.
  • Fulvestrant - concurrent use would counteract its mechanism of action.
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Major Interactions

  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, phenytoin, St. John's Wort) - may decrease estradiol levels, reducing efficacy.
  • CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) - may increase estradiol levels, increasing risk of adverse effects.
  • Thyroid hormone replacement therapy (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin, potentially increasing thyroid hormone requirements.
  • Anticoagulants (e.g., warfarin) - estrogens may alter the effects of anticoagulants; monitor INR/PT.
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Moderate Interactions

  • Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased effects.
  • Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing cyclosporine levels and toxicity.
  • Lamotrigine - estrogens may decrease lamotrigine levels, potentially leading to loss of seizure control.
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Minor Interactions

  • Not many specific minor interactions are clinically significant enough to warrant specific listing beyond general caution with drugs affecting liver enzymes.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination

Rationale: To identify contraindications, risk factors (e.g., cardiovascular disease, breast cancer), and establish baseline health status.

Timing: Prior to initiation of therapy

Blood pressure

Rationale: Estrogens can affect blood pressure.

Timing: Prior to initiation of therapy

Breast examination and mammography

Rationale: To screen for breast cancer, as estrogen therapy can increase risk.

Timing: Prior to initiation of therapy (as per age-appropriate screening guidelines)

Pelvic examination and Pap test

Rationale: To screen for gynecological conditions and cervical cancer.

Timing: Prior to initiation of therapy (as per age-appropriate screening guidelines)

Lipid profile

Rationale: Estrogens can affect lipid metabolism.

Timing: Prior to initiation of therapy

Liver function tests (LFTs)

Rationale: Estradiol is extensively metabolized by the liver; to assess baseline liver function.

Timing: Prior to initiation of therapy (if clinically indicated)

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Routine Monitoring

Blood pressure

Frequency: Annually or as clinically indicated

Target: Normal range for age and comorbidities

Action Threshold: Significant increase or sustained hypertension; consider dose adjustment or discontinuation.

Breast examination and mammography

Frequency: Annually (breast exam); mammography as per age-appropriate screening guidelines (e.g., every 1-2 years)

Target: No new masses or suspicious findings

Action Threshold: New breast lump, nipple discharge, or suspicious mammogram findings; prompt referral for evaluation.

Pelvic examination and Pap test

Frequency: Annually (pelvic exam); Pap test as per age-appropriate screening guidelines

Target: Normal findings

Action Threshold: Abnormal bleeding, pelvic pain, or abnormal Pap test; prompt referral for evaluation.

Lipid profile

Frequency: Periodically (e.g., every 1-2 years) or as clinically indicated

Target: Optimal lipid levels for cardiovascular health

Action Threshold: Significant adverse changes in lipid profile; consider alternative therapy or lipid-lowering agents.

Symptoms of VTE, stroke, MI, or breast cancer

Frequency: Ongoing patient education and self-monitoring

Target: Absence of symptoms

Action Threshold: Any new or worsening symptoms suggestive of these conditions; immediate medical attention.

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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 redness in one leg
  • Yellowing of skin or eyes (jaundice)
  • Severe abdominal pain
  • Memory loss or cognitive decline (in older women)

Special Patient Groups

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Pregnancy

Contraindicated during pregnancy. There is no indication for estrogen therapy in pregnancy, and there is evidence of fetal harm (e.g., genital abnormalities in female fetuses exposed to diethylstilbestrol, a synthetic estrogen).

Trimester-Specific Risks:

First Trimester: Potential for fetal harm, including genital abnormalities.
Second Trimester: Potential for fetal harm.
Third Trimester: Potential for fetal harm.
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Lactation

Not recommended during lactation. Estrogens are excreted in breast milk and may decrease the quantity and quality of breast milk. Potential adverse effects on the breastfed infant are unknown but possible.

Infant Risk: L3 (Moderate risk) - Potential for decreased milk supply and possible effects on infant development (e.g., feminization in male infants), though data are limited.
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Pediatric Use

Not indicated for pediatric use. Safety and efficacy have not been established in pediatric patients for hormone replacement therapy. Use in specific conditions like hypogonadism would involve different formulations and expert guidance.

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Geriatric Use

Use with caution in women 65 years of age or older. Increased risk of stroke, deep vein thrombosis, and probable dementia has been reported in women 65 years of age or older receiving estrogen-alone or estrogen plus progestin therapy. Use the lowest effective dose for the shortest duration consistent with treatment goals.

Clinical Information

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Clinical Pearls

  • Estradiol 0.5mg is a low dose often used for initial therapy or maintenance in women with mild menopausal symptoms or for osteoporosis prevention.
  • Always co-administer a progestin with estradiol in women with an intact uterus to reduce the risk of endometrial hyperplasia and cancer.
  • Patients should be advised to report any unusual vaginal bleeding immediately, as it may be a sign of endometrial cancer.
  • The decision to initiate or continue estrogen therapy should be individualized, weighing the benefits for symptom relief against the potential risks of cardiovascular events, breast cancer, and dementia.
  • Regular follow-up appointments are crucial for monitoring efficacy and safety, including breast exams, mammograms, and pelvic exams.
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Alternative Therapies

  • Other routes of estrogen administration (transdermal patch, gel, spray, vaginal ring, vaginal cream/tablet)
  • Selective Estrogen Receptor Modulators (SERMs) for specific indications (e.g., ospemifene for dyspareunia, raloxifene for osteoporosis prevention)
  • Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
  • Lifestyle modifications (e.g., diet, exercise, stress reduction) for menopausal symptoms.
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Cost & Coverage

Average Cost: $15 - $50 per 30 tablets (0.5mg)
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 is essential to contact your doctor promptly. To ensure safe and effective treatment, 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 for more information. 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 seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.