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Estradiol 10mcg Vaginal Tabs 18s

Manufacturer TEVA Active Ingredient Estradiol Vaginal 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 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
Mar 1999
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Estradiol vaginal tablets are a low-dose estrogen medicine inserted into the vagina. They work locally to treat vaginal dryness, itching, and burning, and painful intercourse caused by menopause. It helps restore the natural 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 accompanying information carefully. Before each use, wash your hands thoroughly. Insert the medication into your vagina using the provided applicator, and then wash the applicator after 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

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

What to Do If You Miss a Dose

If you forget to take a dose, use it as soon as you remember. However, if it is 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 dose.
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Lifestyle & Tips

  • Continue regular gynecological exams, including breast exams and mammograms, as recommended by your doctor.
  • Report any unusual vaginal bleeding, breast lumps, or other concerning symptoms to your doctor immediately.
  • Discuss any concerns about long-term use with your healthcare provider.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: One 10 mcg tablet vaginally once daily for 2 weeks, then one 10 mcg tablet vaginally twice weekly.
Dose Range: 10 - 10 mg

Condition-Specific Dosing:

vaginalatrophy: One 10 mcg tablet vaginally once daily for 2 weeks, then one 10 mcg tablet vaginally 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; systemic exposure may be increased in severe renal impairment, though data for vaginal route is limited.
Dialysis: Not available

Hepatic 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; estrogens are extensively metabolized by the liver. Systemic exposure may be increased in severe hepatic impairment, though data for vaginal route is limited.

Pharmacology

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Mechanism of Action

Estradiol is an estrogen, a primary female sex hormone. It binds to estrogen receptors (ERΞ± and ERΞ²) in target tissues, including the vagina, uterus, breast, hypothalamus, and pituitary. This binding leads to gene transcription and protein synthesis, resulting in the physiological effects of estrogens. In the vagina, it helps restore the vaginal mucosa, increase superficial cells, decrease parabasal cells, and lower vaginal pH, alleviating symptoms of vulvovaginal atrophy.
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Pharmacokinetics

Absorption:

Bioavailability: Low systemic bioavailability (primarily local action); systemic absorption is variable but generally low with 10 mcg vaginal tablets.
Tmax: Systemic Tmax for estradiol is approximately 5-10 hours after vaginal administration.
FoodEffect: Not applicable for vaginal administration.

Distribution:

Vd: Not precisely quantified for vaginal administration, but estradiol distributes widely.
ProteinBinding: Approximately 98% bound to plasma proteins, primarily sex hormone-binding globulin (SHBG) and albumin.
CnssPenetration: Limited

Elimination:

HalfLife: Systemic half-life of estradiol is approximately 1-2 hours, but effective half-life considering enterohepatic recirculation is longer (13-17 hours).
Clearance: Not precisely quantified for vaginal administration.
ExcretionRoute: Renal (primarily as glucuronide and sulfate conjugates), biliary.
Unchanged: <1%
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Pharmacodynamics

OnsetOfAction: Symptomatic relief may begin within a few weeks; full effect on vaginal cytology and pH may take 8-12 weeks.
PeakEffect: Not applicable for local effect; systemic peak levels occur within hours.
DurationOfAction: Effects persist as long as treatment is continued; twice-weekly dosing maintains therapeutic levels.

Safety & Warnings

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BLACK BOX WARNING

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 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 6.8 years of treatment with daily oral conjugated estrogens (0.625 mg) alone relative to placebo. The WHI Memory Study (WHIMS), an ancillary study of the 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) alone or in combination with medroxyprogesterone acetate (2.5 mg) relative to placebo. These risks are for systemic estrogen therapy. While systemic absorption of estradiol from vaginal tablets is low, the potential for systemic effects, particularly with long-term use, cannot be entirely excluded. Therefore, the lowest effective dose should be used for the shortest duration consistent with treatment goals and risks.
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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 or seek medical attention immediately:

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 gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, change in stools, dark urine, yellow skin or eyes, or fever with chills.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.
 Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or throwing up.
 Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Pelvic pain or pressure, vaginal irritation, vaginal itching or discharge, or abnormal vaginal bleeding.
 Breast changes: lump, pain, soreness, or nipple discharge.
Depression or other mood changes, memory problems or loss, eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
 Fluid retention: swelling, weight gain, or trouble breathing.
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.
 High calcium levels: weakness, confusion, feeling tired, headache, upset stomach or throwing up, constipation, or bone pain.

Common Side Effects

Most people experience few or no side effects while taking this medication. However, some common side effects may occur, including:

Headache
 Hair loss
Tender breasts
 Diarrhea, upset stomach, or throwing up
Stomach pain or cramps
 Bloating
Back pain

If any of these side effects or other symptoms bother you or do not go away, contact your doctor for advice.

Reporting Side Effects

If you have questions about side effects or want to report any, you can:

 Call your doctor for medical advice
Contact the FDA at 1-800-332-1088
 Report side effects 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 or migraine
  • Sudden vision changes
  • Chest pain or heaviness, pain radiating to arm or jaw
  • Shortness of breath
  • Pain, swelling, or tenderness in one leg (especially calf)
  • Yellowing of 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. 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 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 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 adjust the dose of any medication without consulting your doctor first.
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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, it is crucial to closely monitor your blood sugar levels. Follow your doctor's instructions for regular blood work and other laboratory tests.

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

Be aware that this medication can cause high blood pressure. Your doctor will advise you on how often to have your blood pressure checked.

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. Be sure to notify all your healthcare providers and laboratory personnel that you are taking this drug.

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

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

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

If you are breastfeeding, consult with 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:

Overdose with vaginal estradiol is unlikely due to the low dose and local administration. If suspected, contact a poison control center (Call 1-800-222-1222) or seek emergency medical attention. Treatment is symptomatic and supportive.

Drug Interactions

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Moderate Interactions

  • CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, St. John's Wort): May decrease systemic estradiol levels, potentially reducing efficacy, though less relevant for low-dose vaginal products.
  • CYP3A4 inhibitors (e.g., erythromycin, clarithromycin, ketoconazole, ritonavir): May increase systemic estradiol levels, though less relevant for low-dose vaginal products.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination (including blood pressure, breast, abdomen, and pelvic organs)

Rationale: To identify contraindications, risk factors for estrogen-related adverse events, and establish baseline health status.

Timing: Prior to initiation of therapy.

Mammogram

Rationale: To screen for breast cancer before initiating estrogen therapy.

Timing: As appropriate, based on patient age and risk factors, prior to initiation.

Pap test

Rationale: To screen for cervical abnormalities.

Timing: As appropriate, based on patient age and risk factors, prior to initiation.

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Routine Monitoring

Annual physical examination (including blood pressure, breast, abdomen, and pelvic organs)

Frequency: Annually or as clinically indicated.

Target: Not applicable

Action Threshold: Any significant changes or new findings should prompt further investigation.

Mammogram

Frequency: Periodically, as appropriate for age and risk factors.

Target: Not applicable

Action Threshold: Abnormal findings require further diagnostic evaluation.

Assessment of symptoms of vulvovaginal atrophy

Frequency: Regularly, at follow-up visits.

Target: Improvement or resolution of symptoms.

Action Threshold: Lack of improvement or worsening symptoms may require re-evaluation of therapy.

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Symptom Monitoring

  • Abnormal 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

Special Patient Groups

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Pregnancy

Contraindicated in pregnancy. There is no indication for estrogen therapy in pregnancy. Estrogens may cause severe fetal harm, including congenital anomalies of the reproductive organs in female fetuses.

Trimester-Specific Risks:

First Trimester: Potential for feminization of male fetuses and virilization of female fetuses.
Second Trimester: Potential for feminization of male fetuses and virilization of female fetuses.
Third Trimester: Potential for feminization of male fetuses and virilization of female fetuses.
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Lactation

Not recommended during lactation. Estrogens are excreted in human 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 production, unknown effects on infant).
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Pediatric Use

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

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Geriatric Use

No specific dose adjustment is necessary based on age. However, women 65 years of age or older may be at increased risk for stroke and probable dementia with systemic estrogen therapy. While systemic absorption from vaginal tablets is low, the lowest effective dose should be used for the shortest duration consistent with treatment goals and risks.

Clinical Information

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Clinical Pearls

  • Estradiol 10 mcg vaginal tablets are designed for local treatment of vulvovaginal atrophy symptoms, with minimal systemic absorption compared to oral or transdermal estrogens.
  • Patients should be instructed on the correct insertion technique for the vaginal tablet.
  • The initial daily dosing for 2 weeks helps to rapidly restore vaginal tissue health, followed by a maintenance dose of twice weekly.
  • Despite low systemic absorption, the FDA label carries the Black Box Warning for systemic estrogens, emphasizing the importance of using the lowest effective dose for the shortest duration.
  • Regular follow-up is crucial to assess symptom relief and monitor for any potential adverse effects, including abnormal vaginal bleeding.
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Alternative Therapies

  • Other low-dose vaginal estrogens (e.g., estradiol vaginal cream, estradiol vaginal ring, conjugated estrogens vaginal cream, prasterone vaginal insert)
  • Systemic hormone therapy (oral or transdermal estrogens, with or without progestin, for moderate to severe vasomotor symptoms and/or vulvovaginal atrophy)
  • Non-hormonal lubricants and moisturizers for vaginal dryness
  • Ospemifene (oral SERM for dyspareunia due to vulvovaginal atrophy)
  • Lasofoxifene (oral SERM for dyspareunia due to vulvovaginal atrophy)
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Cost & Coverage

Average Cost: $200 - $500 per 18 tablets
Generic Available: Yes
Insurance Coverage: Tier 2 or Tier 3 (depending on specific plan and formulary)
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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 emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.