Estradiol 1mg/day Top Gel Pk
WARNING: All products: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.Skin gel and spray:Do not let another person or a pet touch this drug or the treated part of your skin. If they do, wash their skin with soap and water. If you notice any signs that others may have been in contact with the treated area by accident, call the doctor. This may include signs of unusual sexual development like breast changes in children. @ COMMON USES: It is used to prevent or lower the signs of the change of life (menopause).It may be given to you for other reasons. Talk with the doctor.
Drug Class
Estrogen
Pharmacologic Class
Estrogen receptor agonist
Pregnancy Category
Category X
FDA Approved
Sep 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol gel is a medication containing the hormone estrogen. It is used to relieve symptoms of menopause, such as hot flashes and vaginal dryness. It works by replacing the estrogen that your body no longer makes after menopause. The gel is applied to the skin, allowing the hormone to be absorbed directly into your bloodstream.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to use this medication as directed and follow all instructions carefully.
Application Instructions
Do not take this medication by mouth. It is for use on your skin only.
Avoid getting the medication in your mouth, nose, or eyes, as it may cause burning.
Apply the medication at the same time every day.
Wash your hands before and after applying the medication.
Apply the medication to clean, dry, healthy skin on your thigh.
Certain products are designed for specific areas of the body. Be sure to read the package insert to understand where to apply this medication.
Do not apply the medication to skin with any problems or irritations.
Avoid applying the medication to your face, breast, or vagina.
Special Instructions for Pump or Packet Products
If you are using a pump, you will need to prime it before the first use. Follow the instructions in the package insert to prime the pump correctly.
If you are using a packet, follow the instructions provided.
Safety Precautions
Do not have someone else apply the medication to your skin. If someone else must apply it, they should wear gloves and avoid touching the medication.
Avoid exposure to fire, flames, or smoking until the medication is dry.
Allow the medication to dry completely before covering the treated area with clothing.
Do not wash the treated area for at least 1 hour after applying the medication.
Rotate the application site with each dose to avoid skin irritation.
Storage and Disposal
Store the medication at room temperature in a dry place, away from bathrooms.
Protect the medication from heat or open flames.
Keep all medications in a safe place, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, use it as soon as you remember.
If it is less than 12 hours until your next scheduled dose, skip the missed dose and return to your regular schedule.
* Do not use two doses at the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to use this medication as directed and follow all instructions carefully.
Application Instructions
Do not take this medication by mouth. It is for use on your skin only.
Avoid getting the medication in your mouth, nose, or eyes, as it may cause burning.
Apply the medication at the same time every day.
Wash your hands before and after applying the medication.
Apply the medication to clean, dry, healthy skin on your thigh.
Certain products are designed for specific areas of the body. Be sure to read the package insert to understand where to apply this medication.
Do not apply the medication to skin with any problems or irritations.
Avoid applying the medication to your face, breast, or vagina.
Special Instructions for Pump or Packet Products
If you are using a pump, you will need to prime it before the first use. Follow the instructions in the package insert to prime the pump correctly.
If you are using a packet, follow the instructions provided.
Safety Precautions
Do not have someone else apply the medication to your skin. If someone else must apply it, they should wear gloves and avoid touching the medication.
Avoid exposure to fire, flames, or smoking until the medication is dry.
Allow the medication to dry completely before covering the treated area with clothing.
Do not wash the treated area for at least 1 hour after applying the medication.
Rotate the application site with each dose to avoid skin irritation.
Storage and Disposal
Store the medication at room temperature in a dry place, away from bathrooms.
Protect the medication from heat or open flames.
Keep all medications in a safe place, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, use it as soon as you remember.
If it is less than 12 hours until your next scheduled dose, skip the missed dose and return to your regular schedule.
* Do not use two doses at the same time or take extra doses.
Lifestyle & Tips
- Apply the gel to clean, dry skin on one thigh once daily. Do not apply to breasts or irritated skin.
- Rotate application sites if using daily to avoid irritation.
- Wash hands thoroughly after application.
- Allow the gel to dry completely (usually 2-5 minutes) before dressing or allowing skin-to-skin contact with others.
- Avoid contact with eyes, mouth, or other sensitive areas.
- Do not apply to skin that is broken, irritated, or sunburned.
- Regular exercise and a healthy diet are important for overall health during menopause.
Available Forms & Alternatives
Available Strengths:
- Estradiol 0.05mg Patch (once Wk)
- Estradiol 0.1mg Patch (once Wk)
- Estradiol 1mg Tablets
- Estradiol 2mg Tablets
- Estradiol 0.5mg Tablets
- Estradiol 0.025mg Patch (once Wk)
- Estradiol 0.075mg Patch (once Wk)
- Estradiol Tds 0.0375mg Patches 4s
- Estradiol Tds 0.06mg Patch 4s
- Estradiol 0.025mg Patch (twice Wk)
- Estradiol 0.075mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk)
- Estradiol 0.1mg Patch (twice Wk)
- Estradiol 0.05mg Patch (twice Wk)
- Estradiol 0.0375mg Patch (twice Wk
- Estradiol 10mcg Vaginal Tabs 8s
- Estradiol 10mcg Vaginal Tabs 18s
- Estradiol 0.01% Vag Cream 42.5gm
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol Valerate 40mg/ml Inj, 5ml
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol Val 20mg/ml Inj, 5ml
- Estradiol Valerate 10mg/ml Inj, 5ml
- Estradiol 1.25mg/day Top Gel Pk
- Estradiol 0.75mg/day Top Gel Pk
- Estradiol 1mg/day Top Gel Pk
- Estradiol 0.5mg/day Top Gel Pk
- Estradiol 0.25mg/day Top Gel Pk
- Estradiol 0.06% Gel 37.5gm(pumps)
- Estradiol 0.06% Gel 37.5gm(pumps)
Dosing & Administration
Adult Dosing
Standard Dose:
1 mg estradiol applied once daily to the thigh
Dose Range:
0.25 - 1.5 mg
Condition-Specific Dosing:
vasomotorSymptoms:
Initial dose 0.25 mg or 0.5 mg once daily, titrate up to 1 mg or 1.5 mg once daily based on clinical response and tolerability.
vulvarVaginalAtrophy:
Initial dose 0.25 mg or 0.5 mg once daily, titrate up to 1 mg or 1.5 mg once daily based on clinical response and tolerability.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended
Moderate:
No specific dose adjustment recommended
Severe:
Use with caution; monitor for adverse effects
Dialysis:
Not specifically studied; use with caution
Hepatic Impairment:
Mild:
No specific dose adjustment recommended for topical formulation due to bypass of first-pass metabolism
Moderate:
Use with caution; monitor for adverse effects
Severe:
Contraindicated in severe hepatic dysfunction
Confidence:
Medium
Pharmacology
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, forming a complex that interacts with DNA to regulate gene expression. This leads to the physiological effects of estrogens, including those on the reproductive system, bone, and cardiovascular system.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 10-15% (relative to oral estradiol, but topical bypasses first-pass metabolism, leading to a more favorable estradiol to estrone ratio)
Tmax:
Approximately 2-4 hours
FoodEffect:
Not applicable for topical gel
Distribution:
Vd:
Approximately 1.2 L/kg
ProteinBinding:
Highly protein bound (>95%), primarily to sex hormone-binding globulin (SHBG) and albumin
CnssPenetration:
Limited, but estrogens can cross the blood-brain barrier
Elimination:
HalfLife:
Approximately 1-2 hours (for estradiol itself, but clinical effect is prolonged due to reservoir effect in skin and conversion to estrone)
Clearance:
Not readily quantifiable for topical application due to sustained absorption
ExcretionRoute:
Primarily renal (as glucuronide and sulfate conjugates), with some biliary excretion
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Within days to weeks for symptomatic relief
PeakEffect:
Weeks to months for full therapeutic effect
DurationOfAction:
24 hours (with daily application)
Safety & Warnings
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 (CE 0.625 mg) alone, or in combination with medroxyprogesterone acetate (CE 0.625 mg/MPA 2.5 mg) during 5.6 years of treatment. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older. Estrogens increase the risk of endometrial cancer in a woman with a uterus. Adequate diagnostic measures, including directed endometrial biopsy when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurrent abnormal genital bleeding.
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 liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel
Breast lump, breast pain or soreness, or nipple discharge
Vaginal itching or discharge
Abnormal vaginal bleeding
Depression or other mood changes
Memory problems or loss
Fever
Difficulty urinating or changes in urine output
Pain while urinating
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or breathing difficulties.
Blood Clots and High Calcium Levels
Seek medical attention immediately if you experience:
Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, changes in color, or pain in a leg or arm; or trouble speaking or swallowing
Signs of high calcium levels (more common in people with cancer): weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only mild ones. However, if you notice any of the following side effects or if they persist or bother you, contact your doctor:
Dizziness or headache
Hair loss
Upset stomach or vomiting
Constipation
Stomach pain or cramps
Bloating
Enlarged breasts
Tender breasts
Vaginal bleeding or spotting
Painful periods
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
* Changes in sex interest
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek 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 liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel
Breast lump, breast pain or soreness, or nipple discharge
Vaginal itching or discharge
Abnormal vaginal bleeding
Depression or other mood changes
Memory problems or loss
Fever
Difficulty urinating or changes in urine output
Pain while urinating
This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or breathing difficulties.
Blood Clots and High Calcium Levels
Seek medical attention immediately if you experience:
Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, changes in color, or pain in a leg or arm; or trouble speaking or swallowing
Signs of high calcium levels (more common in people with cancer): weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only mild ones. However, if you notice any of the following side effects or if they persist or bother you, contact your doctor:
Dizziness or headache
Hair loss
Upset stomach or vomiting
Constipation
Stomach pain or cramps
Bloating
Enlarged breasts
Tender breasts
Vaginal bleeding or spotting
Painful periods
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
* Changes in sex interest
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache or migraine
- Sudden partial or complete loss of vision
- Sudden shortness of breath or chest pain
- Pain, swelling, or redness in one or both legs
- Yellowing of the skin or eyes (jaundice)
- Severe abdominal pain
- New breast lump or changes in existing breast lumps
- Unusual vaginal bleeding (especially after menopause)
- Memory loss or confusion (especially in women over 65)
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 developing blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Any instances of unexplained vaginal bleeding
If you are pregnant or think you might be pregnant. Note that this medication should not be taken during pregnancy.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the 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 developing blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Any instances of unexplained vaginal bleeding
If you are pregnant or think you might be pregnant. Note that this medication should not be taken during pregnancy.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
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 inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes, it is crucial to closely monitor your blood sugar levels.
Be aware that medications like this one can cause high blood pressure. Follow your doctor's instructions for regular blood pressure checks. You should also have your blood work and bone density 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. The risk of certain side effects, such as heart attack, stroke, breast cancer, and ovarian cancer, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
High triglyceride levels have been associated with this medication. If you have a history of high triglyceride levels, inform your doctor. This drug may also cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear.
This medication may affect certain laboratory tests, so be sure to 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 recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, and they may require regular growth checks. Consult with your doctor before using any other medications or skin products, including soaps. When using the gel form of this medication, avoid applying sunscreen before or soon after application, and do not use sunscreen on the treated area for 7 consecutive days.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Finally, if you are breastfeeding, consult with your doctor to discuss any potential risks to your baby.
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 inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes, it is crucial to closely monitor your blood sugar levels.
Be aware that medications like this one can cause high blood pressure. Follow your doctor's instructions for regular blood pressure checks. You should also have your blood work and bone density 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. The risk of certain side effects, such as heart attack, stroke, breast cancer, and ovarian cancer, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.
High triglyceride levels have been associated with this medication. If you have a history of high triglyceride levels, inform your doctor. This drug may also cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear.
This medication may affect certain laboratory tests, so be sure to 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 recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, and they may require regular growth checks. Consult with your doctor before using any other medications or skin products, including soaps. When using the gel form of this medication, avoid applying sunscreen before or soon after application, and do not use sunscreen on the treated area for 7 consecutive days.
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Finally, if you are breastfeeding, consult with your doctor to discuss any potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Breast tenderness
- Abdominal pain
- Drowsiness/fatigue
- Withdrawal bleeding (in women)
What to Do:
Seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Treatment is generally supportive; symptoms usually resolve upon discontinuation of the drug.
Drug Interactions
Major Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane) - concurrent use antagonizes effects
- Tamoxifen - concurrent use antagonizes effects
Moderate Interactions
- CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol levels
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may increase estradiol levels
- Thyroid hormone replacement therapy (e.g., levothyroxine) - estrogens may increase thyroid-binding globulin, requiring increased thyroid hormone dose
- Warfarin - estrogens may alter anticoagulant effect (monitor INR)
Minor Interactions
- Corticosteroids - estrogens may decrease clearance of corticosteroids, leading to increased effects
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, leading to increased levels
Monitoring
Baseline Monitoring
Complete medical history and physical examination (including blood pressure, breast exam, pelvic exam)
Rationale: To identify contraindications, risk factors, and establish baseline health status
Timing: Prior to initiation of therapy
Mammography
Rationale: To screen for breast cancer before initiating estrogen therapy
Timing: Prior to initiation, as per screening guidelines
Lipid profile
Rationale: To assess cardiovascular risk factors
Timing: Prior to initiation, if indicated
Liver function tests (LFTs)
Rationale: To assess hepatic function, especially in patients with pre-existing liver conditions
Timing: Prior to initiation, if indicated
Routine Monitoring
Annual physical examination (including blood pressure, breast exam, pelvic exam)
Frequency: Annually
Target: Normal limits
Action Threshold: Abnormal findings require further investigation
Mammography
Frequency: Periodically, as per screening guidelines
Target: Normal
Action Threshold: Abnormal findings require further investigation
Lipid profile
Frequency: Periodically, if indicated by risk factors or clinical judgment
Target: Individualized targets
Action Threshold: Significant changes or out-of-range values require intervention
Symptoms of endometrial hyperplasia/cancer (e.g., abnormal vaginal bleeding)
Frequency: Ongoing
Target: Absence of symptoms
Action Threshold: Any abnormal bleeding requires prompt evaluation
Symptom Monitoring
- Signs and symptoms of thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, stroke, myocardial infarction)
- Signs and symptoms of breast cancer (e.g., new lump, skin changes, nipple discharge)
- Signs and symptoms of endometrial hyperplasia/cancer (e.g., abnormal vaginal bleeding)
- Signs and symptoms of liver dysfunction (e.g., jaundice, abdominal pain)
- Changes in blood pressure
- Headaches (especially new onset or severe)
- Visual disturbances
Special Patient Groups
Pregnancy
Contraindicated during pregnancy. Estrogen use during pregnancy is associated with an increased risk of birth defects and should be avoided. If pregnancy occurs during treatment, discontinue immediately.
Trimester-Specific Risks:
First Trimester:
Potential for adverse effects on fetal development, including genital abnormalities.
Second Trimester:
Not indicated; continued exposure may pose risks.
Third Trimester:
Not indicated; continued exposure may pose risks.
Lactation
Contraindicated during lactation. Estrogens are excreted in breast milk and can reduce the quantity and quality of breast milk. Potential adverse effects on the nursing infant are possible.
Infant Risk:
Risk of adverse effects on infant (e.g., feminization, jaundice) and interference with milk production. Considered L3 (Moderately Safe) to L4 (Potentially Hazardous) depending on source and specific risk assessment.
Pediatric Use
Not indicated for use in pediatric patients. Estrogen therapy in children can cause premature epiphyseal closure and accelerate puberty.
Geriatric Use
Use with caution in women aged 65 years or older. Increased risk of stroke and probable dementia has been observed in women 65 years of age or older receiving estrogen-alone therapy. Consider lowest effective dose and shortest duration.
Clinical Information
Clinical Pearls
- Topical estradiol gel bypasses first-pass hepatic metabolism, leading to a more favorable estradiol to estrone ratio compared to oral estrogens, which may result in a different side effect profile.
- Ensure patients understand proper application technique: apply to clean, dry, intact skin on the thigh, allow to dry, and wash hands thoroughly. Avoid application to breasts or face.
- Advise patients to avoid contact with the application site by others (e.g., children, partners) until the gel is completely dry to prevent secondary exposure.
- Regular monitoring for signs of endometrial hyperplasia/cancer (e.g., abnormal vaginal bleeding) is crucial, especially if the patient has an intact uterus and is not also taking a progestin.
- Emphasize the importance of annual physical exams, including breast and pelvic exams, and mammography as per screening guidelines.
- Discuss the Black Box Warnings regarding cardiovascular events, stroke, breast cancer, and dementia with patients before initiating therapy.
Alternative Therapies
- Other transdermal estradiol formulations (e.g., patches, sprays, emulsions)
- Oral estrogen formulations (e.g., conjugated estrogens, oral estradiol)
- Vaginal estrogen formulations (e.g., creams, rings, tablets) for localized symptoms
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
- Selective Estrogen Receptor Modulators (SERMs) (e.g., ospemifene for dyspareunia, bazedoxifene/conjugated estrogens for VMS and osteoporosis)
Cost & Coverage
Average Cost:
Varies, typically $150-$300 per 30-day supply (30 packets)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for brand), Tier 1 (for generic)
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 is a good idea to consult with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount, and the time it occurred.