Estradiol 0.5mg/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
Jun 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol gel is a medication containing the female hormone estrogen. It is applied to the skin to help relieve symptoms of menopause, such as hot flashes and night sweats. It works by replacing the estrogen that your body no longer makes after menopause.
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 topical 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 to maintain a consistent routine.
Before and after applying the medication, wash your hands thoroughly.
Apply the medication to clean, dry, and healthy skin on your thigh.
Be sure to apply the medication to the correct area of the body, as specified in the package insert.
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 Certain Products
If you are using a pump, prime it before the first use, following the instructions in the package insert.
If you are using packets, follow the instructions provided.
Do not have someone else apply the medication to your skin. If someone must assist you, ensure they wear gloves and avoid touching the medication.
Precautions and Safety Measures
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 minimize skin irritation.
Storage and Disposal
Store the medication at room temperature in a dry place, away from bathrooms and heat sources.
Protect the medication from heat, open flames, and sparks.
Keep all medications in a safe and secure location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, apply it as soon as you remember.
If it is less than 12 hours until your next scheduled dose, skip the missed dose and resume your regular schedule.
* Do not apply two doses at the same time or use extra doses to make up for a missed dose.
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 topical 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 to maintain a consistent routine.
Before and after applying the medication, wash your hands thoroughly.
Apply the medication to clean, dry, and healthy skin on your thigh.
Be sure to apply the medication to the correct area of the body, as specified in the package insert.
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 Certain Products
If you are using a pump, prime it before the first use, following the instructions in the package insert.
If you are using packets, follow the instructions provided.
Do not have someone else apply the medication to your skin. If someone must assist you, ensure they wear gloves and avoid touching the medication.
Precautions and Safety Measures
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 minimize skin irritation.
Storage and Disposal
Store the medication at room temperature in a dry place, away from bathrooms and heat sources.
Protect the medication from heat, open flames, and sparks.
Keep all medications in a safe and secure location, out of the reach of children and pets.
Missed Dose Instructions
If you miss a dose, apply it as soon as you remember.
If it is less than 12 hours until your next scheduled dose, skip the missed dose and resume your regular schedule.
* Do not apply two doses at the same time or use extra doses to make up for a missed dose.
Lifestyle & Tips
- Apply the gel to clean, dry, unbroken skin on the thigh or calf once daily. Do not apply to breasts or face.
- Allow the gel to dry for at least 5 minutes before dressing.
- Wash hands thoroughly after application.
- Avoid contact with eyes and mouth.
- Avoid applying to areas that will be covered by clothing immediately, or areas that will be washed soon after application.
- Avoid transferring the gel to others, especially children or pets, by ensuring the application site is dry and covered if necessary.
- If you have a uterus, your doctor will likely prescribe a progestin along with estradiol to protect against uterine cancer.
- Regularly perform breast self-exams and get routine mammograms and pelvic exams as advised by your doctor.
- Report any unusual vaginal bleeding immediately.
- Discuss any history of blood clots, stroke, heart attack, or cancer with your doctor before starting this medication.
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:
0.5 mg estradiol applied topically once daily to the thigh or calf
Dose Range:
0.25 - 1.5 mg
Condition-Specific Dosing:
vasomotorSymptoms:
Initial dose 0.25 mg or 0.5 mg once daily; adjust based on clinical response to 0.25 mg, 0.5 mg, 0.75 mg, 1.0 mg, or 1.25 mg, or 1.5 mg per day. The lowest effective dose should be used.
vulvarAndVaginalAtrophy:
Not the primary indication for systemic gel, but may provide relief. Localized vaginal preparations are preferred.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (unless for specific conditions like Turner Syndrome, but not typically with this formulation/dose)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended
Moderate:
No specific dose adjustment recommended
Severe:
Use with caution; monitor for adverse effects. Estrogens are primarily metabolized by the liver.
Dialysis:
Not available
Hepatic Impairment:
Mild:
Use with caution; monitor for adverse effects. Estrogens are extensively metabolized by the liver.
Moderate:
Contraindicated due to impaired estrogen metabolism and increased risk of cholestasis.
Severe:
Contraindicated due to impaired estrogen metabolism and increased risk of cholestasis.
Pharmacology
Mechanism of Action
Estradiol is the primary estrogen secreted by the human ovary. It binds to and activates estrogen receptors (ERΞ± and ERΞ²) in target tissues, including the hypothalamus, pituitary, reproductive organs, bone, and cardiovascular system. This binding leads to gene transcription and protein synthesis, mediating the physiological effects of estrogen, such as reducing vasomotor symptoms and preventing bone loss.
Pharmacokinetics
Absorption:
Bioavailability:
Variable, but transdermal application avoids first-pass metabolism, leading to a more favorable estradiol to estrone ratio compared to oral administration.
Tmax:
Approximately 2-4 hours after topical application.
FoodEffect:
Not applicable for topical gel.
Distribution:
Vd:
Approximately 1.2 L/kg (for estradiol)
ProteinBinding:
Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration:
Limited, but estrogen receptors are present in the CNS.
Elimination:
HalfLife:
Approximately 10-16 hours (for estradiol after transdermal application)
Clearance:
Not readily quantifiable for topical application due to continuous absorption.
ExcretionRoute:
Primarily renal (as glucuronide and sulfate conjugates), with some biliary excretion.
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Symptomatic relief may begin within weeks.
PeakEffect:
Full therapeutic effect may take several weeks to months.
DurationOfAction:
Maintained with daily application.
Safety & Warnings
BLACK BOX WARNING
Estrogen-alone therapy: Increased risk of endometrial cancer in women with a uterus. Increased risk of stroke and deep vein thrombosis (DVT) in postmenopausal women. Estrogen plus progestin therapy: Increased risk of stroke, DVT, pulmonary embolism (PE), and breast cancer. Increased risk of probable dementia in postmenopausal women 65 years of age or older.
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, 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-related symptoms: lump in the breast, breast pain or soreness, or nipple discharge
Vaginal symptoms: itching, discharge, or abnormal bleeding
Depression or other mood changes
Memory problems or loss
Fever
Urinary problems: inability to pass urine or changes in urine output, pain while passing urine
This medication may cause fluid retention, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, inform your doctor.
Blood Clots and High Calcium Levels
Seek immediate medical attention 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. If you experience any of the following symptoms, contact your doctor right away:
Weakness
Confusion
Feeling tired
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Side Effects
Most people taking this medication do not experience severe side effects, and some may not have any side effects at all. However, if you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or persist:
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 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.
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, 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-related symptoms: lump in the breast, breast pain or soreness, or nipple discharge
Vaginal symptoms: itching, discharge, or abnormal bleeding
Depression or other mood changes
Memory problems or loss
Fever
Urinary problems: inability to pass urine or changes in urine output, pain while passing urine
This medication may cause fluid retention, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, inform your doctor.
Blood Clots and High Calcium Levels
Seek immediate medical attention 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. If you experience any of the following symptoms, contact your doctor right away:
Weakness
Confusion
Feeling tired
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Side Effects
Most people taking this medication do not experience severe side effects, and some may not have any side effects at all. However, if you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or persist:
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 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.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache
- Sudden vision changes
- Numbness or weakness on one side of the body
- Slurred speech
- Sudden chest pain or shortness of breath
- Pain, swelling, or redness in your leg
- Yellowing of the skin or eyes (jaundice)
- New breast lump or nipple discharge
- Unusual vaginal bleeding or spotting (if you have a uterus)
- Severe abdominal pain
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. Describe the allergic reaction you experienced, including the 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
Unexplained vaginal bleeding
Pregnancy or suspected pregnancy. Do not take this medication if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the 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. Describe the allergic reaction you experienced, including the 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
Unexplained vaginal bleeding
Pregnancy or suspected pregnancy. Do not take this medication if you are pregnant.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the 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 drug, so inform your doctor if you have a history of elevated triglyceride levels. This medication may cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and to 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. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, so they may require regular growth checks. Consult with your doctor before using 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 drug, so inform your doctor if you have a history of elevated triglyceride levels. This medication may cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and to 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. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor.
In some cases, this medication may affect growth in children and teenagers, so they may require regular growth checks. Consult with your doctor before using 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. There is no specific antidote. Treatment is symptomatic and supportive. Call 1-800-222-1222 (Poison Control Center).
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use would counteract their mechanism of action in breast cancer treatment.
- Fulvestrant - concurrent use would counteract its mechanism of action in breast cancer treatment.
Major Interactions
- CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol levels, reducing efficacy.
- CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice) - may increase estradiol levels, increasing risk of adverse effects.
- Thyroid hormones (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin, potentially increasing thyroid hormone requirements.
- Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased effects.
Moderate Interactions
- Anticoagulants (e.g., warfarin) - estrogens may alter the effects of anticoagulants; monitor INR.
- Hypoglycemic agents (e.g., insulin, oral antidiabetics) - estrogens may impair glucose tolerance; adjust dose if necessary.
- Lamotrigine - estrogens may decrease lamotrigine levels, potentially leading to loss of seizure control.
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its levels and toxicity.
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Complete medical history and physical examination
Rationale: To identify contraindications, risk factors (e.g., VTE, breast cancer, cardiovascular disease), and establish baseline health status.
Timing: Prior to initiation of therapy.
Blood pressure
Rationale: Estrogens can affect blood pressure.
Timing: Prior to initiation.
Breast examination and mammography
Rationale: To screen for breast cancer, as estrogen therapy can increase risk.
Timing: Prior to initiation and as clinically indicated.
Pelvic examination and Pap test
Rationale: To screen for gynecological conditions, especially if the patient has a uterus (risk of endometrial hyperplasia/cancer).
Timing: Prior to initiation and as clinically indicated.
Lipid profile
Rationale: Estrogens can affect lipid metabolism.
Timing: Prior to initiation.
Routine Monitoring
Blood pressure
Frequency: Annually or as clinically indicated.
Target: Normal limits
Action Threshold: Significant increase or hypertension development.
Breast examination and mammography
Frequency: Annually or as per national guidelines.
Target: No suspicious findings
Action Threshold: New lumps, pain, or abnormal mammogram results.
Pelvic examination and Pap test
Frequency: Annually or as per national guidelines.
Target: Normal findings
Action Threshold: Abnormal bleeding, pain, or abnormal Pap test results.
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 requiring immediate medical attention.
Symptom Monitoring
- Persistent or recurrent vaginal bleeding (if uterus present)
- Breast lumps or changes
- Unusual vaginal discharge
- Severe headache or migraine
- Sudden partial or complete loss of vision
- Sudden onset of proptosis, diplopia, or migraine
- Swelling, redness, or pain in an arm or leg (DVT)
- Sudden chest pain, shortness of breath (PE)
- Weakness or numbness of face, arm, or leg, especially on one side of the body (stroke)
- Speech difficulties (stroke)
- Yellowing of skin or eyes (jaundice)
- Abdominal pain, especially right upper quadrant (liver issues)
- Mood changes, depression
Special Patient Groups
Pregnancy
Contraindicated in pregnancy. Estrogen therapy during pregnancy is associated with an increased risk of birth defects in the fetus.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital anomalies, particularly cardiovascular and limb defects, if used during the first trimester.
Second Trimester:
Not indicated; potential for adverse effects on fetal development.
Third Trimester:
Not indicated; potential for adverse effects on fetal development.
Lactation
Contraindicated during lactation. Estrogens are excreted in breast milk and can decrease the quantity and quality of breast milk. Potential for adverse effects on the nursing infant (e.g., feminization).
Infant Risk:
L5 - Contraindicated. Significant risk of adverse effects on milk production and potential for adverse effects on the infant.
Pediatric Use
Not indicated for pediatric use, except in specific conditions like Turner Syndrome, where lower doses and different formulations may be used under specialist supervision. Safety and efficacy not established for general pediatric use.
Geriatric Use
Use with caution in women 65 years of age or older. The Women's Health Initiative (WHI) study showed an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving estrogen plus progestin or estrogen-alone therapy. The lowest effective dose for the shortest duration consistent with treatment goals should be used.
Clinical Information
Clinical Pearls
- Transdermal estradiol avoids first-pass hepatic metabolism, potentially leading to a more favorable safety profile regarding VTE risk compared to oral estrogens, though risk is still present.
- 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 educated on proper application technique to ensure consistent dosing and minimize transfer to others.
- Regularly reassess the need for continued therapy, especially for vasomotor symptoms, and use the lowest effective dose for the shortest duration.
- Consider alternative non-hormonal therapies for menopausal symptoms if contraindications or significant risk factors exist.
Alternative Therapies
- Other hormone therapies (e.g., conjugated estrogens, synthetic estrogens)
- Selective Estrogen Receptor Modulators (SERMs) (e.g., ospemifene for dyspareunia)
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
- Lifestyle modifications (e.g., diet, exercise, stress reduction)
Cost & Coverage
Average Cost:
$150 - $300 per 30-day supply (e.g., 30 packets)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 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's a good idea to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.