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Estradiol 0.01% Vag Cream 42.5gm

Manufacturer TEVA Active Ingredient Estradiol Vaginal Cream(es tra DYE ole) Pronunciation ES-tra-dye-ol
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 treat vaginal irritation and dryness caused by menopause.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
Category X
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FDA Approved
Jan 1999
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Estradiol vaginal cream is a medicine that contains the female hormone estrogen. It is used to treat vaginal dryness, itching, and burning that can happen after menopause. It works by replacing the estrogen that your body no longer makes, helping to restore the health of the vaginal tissues.
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How to Use This Medicine

Taking Your Medication Correctly

To use this medication effectively, follow your doctor's instructions and read all the information provided. Before each use, wash your hands thoroughly. Insert the medication into your vagina using the applicator that comes with it, and be sure to wash the applicator after each use. Establish a routine by taking this medication at the same time every day. Note that there may be days when you are not scheduled to take this medication.

Storing and Disposing of Your Medication

Store your medication in its original container at room temperature, away from heat sources. Keep all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion or exposure.

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 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

  • Apply the cream exactly as directed by your doctor, usually at bedtime.
  • Use the applicator provided to measure the correct dose.
  • Wash your hands before and after applying the cream.
  • Do not use this medicine if you are pregnant or breastfeeding.
  • Discuss any unusual vaginal bleeding with your doctor immediately.
  • Regularly discuss the need for continued therapy with your doctor.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Initial: 2-4 grams intravaginally daily for 1-2 weeks. Maintenance: 1 gram intravaginally 2 times per week.
Dose Range: 1 - 4 mg

Condition-Specific Dosing:

vulvarAndVaginalAtrophy: Initial: 2-4 grams intravaginally daily for 1-2 weeks. Maintenance: 1 gram intravaginally 2 times per week. Some patients may require 0.5 grams twice weekly.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended due to low systemic absorption.
Moderate: No specific adjustment recommended due to low systemic absorption.
Severe: Use with caution; monitor for signs of fluid retention. No specific dose adjustment.
Dialysis: Considerations: Use with caution; monitor for signs of fluid retention. No specific dose adjustment.

Hepatic Impairment:

Mild: No specific adjustment recommended due to low systemic absorption.
Moderate: Use with caution; estrogens are extensively metabolized by the liver. Monitor for adverse effects.
Severe: Contraindicated in severe liver disease.
Confidence: Medium

Pharmacology

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Mechanism of Action

Estradiol is a naturally occurring estrogen. It binds to estrogen receptors in target tissues (e.g., vagina, uterus, breast, hypothalamus, pituitary) and forms a complex that interacts with DNA to stimulate gene transcription and protein synthesis. In the vagina, it helps restore the vaginal epithelium, increasing superficial cells and decreasing parabasal cells, and restoring vaginal pH, thereby alleviating symptoms of vulvar and vaginal atrophy.
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Pharmacokinetics

Absorption:

Bioavailability: Variable (low systemic absorption from vaginal application, but sufficient for local effects and some systemic exposure)
Tmax: Variable (systemic absorption peaks within hours, but local effects develop over weeks)
FoodEffect: Not applicable (vaginal administration)

Distribution:

Vd: Not well-defined for vaginal application; systemically, estrogens distribute widely.
ProteinBinding: Approximately 98% (primarily to sex hormone-binding globulin (SHBG) and albumin)
CnssPenetration: Limited (for therapeutic effects on vaginal atrophy)

Elimination:

HalfLife: Systemic half-life of estradiol is approximately 1-2 hours; however, the duration of action from vaginal application is prolonged due to local tissue binding and slow release.
Clearance: Rapid systemic clearance.
ExcretionRoute: Renal (primarily as glucuronide and sulfate conjugates), Biliary (minor)
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Local symptomatic relief may begin within a few weeks; full therapeutic effect typically observed after 8-12 weeks of continuous use.
PeakEffect: Peak symptomatic relief after 8-12 weeks.
DurationOfAction: Effects persist as long as treatment is continued; symptoms may recur upon discontinuation.

Safety & Warnings

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BLACK BOX WARNING

Estrogens and progestins 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 5.6 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) relative to placebo. The WHI study also reported an increased risk of stroke and deep vein thrombosis in postmenopausal women (50-79 years of age) during 7.1 years of treatment with daily oral conjugated estrogens (0.625 mg) alone relative to placebo. The WHI Memory Study (WHIMS), an ancillary study of WHI, reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with daily oral conjugated estrogens (0.625 mg) combined with medroxyprogesterone acetate (2.5 mg) and in postmenopausal women 65 years of age or older during 5.2 years of treatment with daily oral conjugated estrogens (0.625 mg) alone relative to placebo. These risks were not observed in women 50-54 years of age. Because of these risks, estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman. Use of estrogen-alone therapy in women with a uterus is associated with an increased risk of endometrial cancer.
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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 immediately or seek emergency 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, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
 Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, changes in stool, dark urine, yellow skin or eyes, or fever with chills.
Signs of liver problems: dark urine, fatigue, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
 Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
 Weakness on one side of the body, difficulty speaking or thinking, changes in balance, drooping on one side of the face, or blurred vision.
Pelvic pain or pressure.
 Vaginal irritation, itching, or discharge.
Abnormal vaginal bleeding.
 Breast lump, breast pain or soreness, or nipple discharge.
Depression or other mood changes.
 Memory problems or loss.
Changes in vision or loss of vision, bulging eyes, or changes in how contact lenses feel.
 Fluid retention or swelling, which may cause weight gain or difficulty breathing. If you experience swelling, weight gain, or trouble breathing, inform your doctor.

Additional Urgent Side Effects

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 difficulty speaking or swallowing. Seek medical help immediately if you experience any of these symptoms.
 High calcium levels: weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain. If you have cancer and experience any of these symptoms, contact your doctor right away.

Other Possible Side Effects

Not everyone will experience side effects, and many people may only have mild or minor side effects. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical help:

Headache.
 Hair loss.
Tender breasts.
 Diarrhea, upset stomach, or vomiting.
Stomach pain or cramps.
 Bloating.
* Back pain.

Reporting Side Effects

This is not an exhaustive list of possible 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:

  • Unusual vaginal bleeding or spotting
  • New breast lump or changes in breasts
  • Sudden severe headache
  • Sudden vision changes
  • Sudden numbness or weakness on one side of the body
  • Chest pain or heaviness
  • Shortness of breath
  • Pain, swelling, or redness in one leg
  • Yellowing of the skin or eyes (jaundice)
  • Severe abdominal pain
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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 with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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Precautions & 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 have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels. Additionally, have your blood work and other laboratory tests checked as directed by your doctor.

Regular breast exams and gynecology check-ups are vital, and you should also perform breast self-exams as instructed by your doctor.

Be aware that this medication can cause high blood pressure. Ensure that your blood pressure is checked regularly, as advised by your doctor.

Elevated triglyceride levels have been associated with this drug. If you have a history of high triglyceride levels, inform your doctor.

This medication may affect the results of certain laboratory tests. Notify all your healthcare providers and laboratory personnel that you are taking this drug.

Smoking can increase the risk of heart disease. It is recommended that you do not smoke, and discuss this with your doctor if you need help quitting.

If you consume grapefruit juice or eat grapefruit regularly, consult with your doctor to discuss potential interactions.

If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, talk to your doctor. Prolonged immobility may increase the risk of blood clots.

The risk of certain side effects, including heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors such as 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.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

If you are breastfeeding, inform your doctor, as you will need to discuss the potential risks to your baby.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Breast tenderness
  • Abdominal pain
  • Drowsiness/fatigue
  • Withdrawal bleeding in women

What to Do:

There is no specific antidote for estrogen overdose. Treatment is symptomatic and supportive. Contact a poison control center or emergency medical services immediately. Call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Aromatase inhibitors (e.g., anastrozole, exemestane, letrozole) - concurrent use may reduce efficacy of aromatase inhibitors.
  • Tamoxifen - concurrent use may reduce efficacy of tamoxifen.
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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) - may increase estradiol levels.
  • Thyroid hormones (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin, potentially increasing thyroid hormone requirements.
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Minor Interactions

  • Corticosteroids - estrogens may decrease the clearance of corticosteroids, leading to increased effects.

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 endometrial cancer.

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.

Timing: Prior to initiation of therapy (as appropriate for age and risk factors)

Pelvic examination and Pap test

Rationale: To screen for gynecological conditions and cervical cancer.

Timing: Prior to initiation of therapy (as appropriate for age and risk factors)

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Routine Monitoring

Annual physical examination (including breast and pelvic exam)

Frequency: Annually

Target: Normal findings

Action Threshold: Any abnormal findings (e.g., new breast lump, abnormal vaginal bleeding) require immediate investigation.

Blood pressure

Frequency: Annually or as clinically indicated

Target: <130/80 mmHg

Action Threshold: Sustained elevation requires evaluation and management.

Mammography

Frequency: As per national screening guidelines

Target: Normal findings

Action Threshold: Abnormal findings require further diagnostic workup.

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Symptom Monitoring

  • Vaginal bleeding (any new or unusual bleeding)
  • Breast changes (lumps, pain, discharge)
  • Symptoms of deep vein thrombosis (DVT) or pulmonary embolism (PE) (e.g., leg pain/swelling, chest pain, shortness of breath)
  • Symptoms of stroke (e.g., sudden severe headache, vision changes, weakness/numbness on one side of body)
  • Symptoms of myocardial infarction (e.g., chest pain, arm pain, shortness of breath)
  • Symptoms of liver dysfunction (e.g., jaundice, abdominal pain)
  • Changes in mood or cognition

Special Patient Groups

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Pregnancy

Contraindicated in pregnancy. There is no indication for estrogen therapy in pregnancy, and there is evidence of fetal harm.

Trimester-Specific Risks:

First Trimester: Potential for fetal harm, including genital abnormalities in female fetuses.
Second Trimester: Potential for fetal harm.
Third Trimester: Potential for fetal harm.
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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: Moderate risk. Potential for adverse effects on the infant (e.g., feminization, jaundice) and reduction in milk supply.
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Pediatric Use

Not indicated for use in pediatric patients. Safety and efficacy have not been established.

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Geriatric Use

Use with caution. The lowest effective dose should be used for the shortest duration consistent with treatment goals. Women 65 years of age or older may have an increased risk of probable dementia with systemic estrogen therapy. While vaginal cream has lower systemic absorption, caution is still advised.

Clinical Information

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Clinical Pearls

  • Estradiol vaginal cream is primarily for local treatment of vulvar and vaginal atrophy symptoms, with minimal but variable systemic absorption.
  • Patients should be advised to use the lowest effective dose for the shortest duration consistent with treatment goals.
  • Regular re-evaluation (at least annually) is crucial to determine if continued therapy is needed.
  • Despite low systemic absorption, the Black Box Warning for systemic estrogens regarding endometrial cancer, cardiovascular events, breast cancer, and dementia still applies to the class of drugs.
  • Patients with an intact uterus should be monitored for signs of endometrial hyperplasia or cancer, although the risk with low-dose vaginal estradiol is considered lower than with systemic therapy.
  • Non-hormonal options (e.g., vaginal lubricants, moisturizers) should be considered for patients who cannot or prefer not to use estrogen therapy.
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Alternative Therapies

  • Other low-dose vaginal estrogen products (e.g., estradiol vaginal tablets/inserts, conjugated estrogens vaginal cream, estriol vaginal cream (outside US))
  • Ospemifene (oral selective estrogen receptor modulator for dyspareunia)
  • Prasterone (DHEA) vaginal insert
  • Non-hormonal vaginal lubricants and moisturizers (e.g., Replens, K-Y Jelly)
  • Vaginal dilators
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Cost & Coverage

Average Cost: Varies widely, typically $50-$200+ per 42.5gm tube
Generic Available: Yes
Insurance Coverage: Tier 1 or 2 for generic, Tier 3 or higher for brand
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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 this 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 medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.