Estradiol Tds 0.0375mg Patches 4s
WARNING: Do not use this drug to prevent heart disease or dementia. A study of women taking an estrogen with a progestin showed a raised chance of heart attack, stroke, blood clot, breast cancer, and dementia. The chance of stroke, blood clot, and dementia was also raised when the estrogen was taken alone. Not all products and doses were studied. It is not known if the same effects may happen with this drug.The chance of endometrial cancer may be raised with the use of estrogen alone in patients with a uterus. Use of a progestin along with estrogen may lower the risk. Call your doctor right away if you have unexplained or long-lasting vaginal bleeding.Use this drug for the shortest time needed at the lowest useful dose. Your doctor will talk with you on a regular basis to see if you need to keep taking this drug. @ COMMON USES: It is used to prevent soft, brittle bones (osteoporosis) after menopause.It is used to prevent or lower the signs of the change of life (menopause).It is used to add estrogen to the body when the ovaries have been taken out or do not work the right way.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Hormone Replacement Therapy (HRT)
Pharmacologic Class
Estrogen
Pregnancy Category
Category X
FDA Approved
Aug 1986
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol transdermal patches are a form of hormone therapy that delivers estrogen through your skin. They are used to relieve symptoms of menopause, such as hot flashes and vaginal dryness, and to help prevent bone thinning (osteoporosis) after menopause. The patch releases a steady amount of estrogen into your bloodstream over a week.
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's essential to use this medication as directed.
Application Instructions
Apply this medication only to your skin, as directed. Do not take it by mouth.
Keep the medication away from your mouth, nose, and eyes, as it may cause burning.
Use the medication at the same time every day to maintain a consistent routine.
Before and after applying the medication, wash your hands thoroughly.
Choose a clean, dry, and healthy area of skin on your lower belly or upper buttocks to apply the patch. Rotate the application site with each new patch to avoid skin irritation.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the medication to skin with any problems, such as cuts, wounds, or irritated areas.
Avoid applying the patch to your breast or skin where you have recently used creams, oils, lotions, powder, or other skin products, as this may affect the patch's adhesion.
Select a hair-free area of skin to apply the patch.
Avoid applying the patch to your waistline or areas where sitting may cause it to come off.
Patch Handling and Disposal
Do not cut or divide the patches.
Do not use damaged patches.
If a patch falls off, try to reapply it. If you cannot reapply the patch, apply a new one to a different area.
Wear only one patch at a time.
After removing a used patch, fold the sticky sides together and dispose of it in a secure location where children and pets cannot access it.
Storage and Disposal
Store this medication at room temperature in a dry place, away from bathrooms.
Keep used patches out of reach of children and pets.
Missed Dose
If you miss a dose, apply a new patch as soon as you remember, after removing the old one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It's essential to use this medication as directed.
Application Instructions
Apply this medication only to your skin, as directed. Do not take it by mouth.
Keep the medication away from your mouth, nose, and eyes, as it may cause burning.
Use the medication at the same time every day to maintain a consistent routine.
Before and after applying the medication, wash your hands thoroughly.
Choose a clean, dry, and healthy area of skin on your lower belly or upper buttocks to apply the patch. Rotate the application site with each new patch to avoid skin irritation.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the medication to skin with any problems, such as cuts, wounds, or irritated areas.
Avoid applying the patch to your breast or skin where you have recently used creams, oils, lotions, powder, or other skin products, as this may affect the patch's adhesion.
Select a hair-free area of skin to apply the patch.
Avoid applying the patch to your waistline or areas where sitting may cause it to come off.
Patch Handling and Disposal
Do not cut or divide the patches.
Do not use damaged patches.
If a patch falls off, try to reapply it. If you cannot reapply the patch, apply a new one to a different area.
Wear only one patch at a time.
After removing a used patch, fold the sticky sides together and dispose of it in a secure location where children and pets cannot access it.
Storage and Disposal
Store this medication at room temperature in a dry place, away from bathrooms.
Keep used patches out of reach of children and pets.
Missed Dose
If you miss a dose, apply a new patch as soon as you remember, after removing the old one.
Lifestyle & Tips
- Apply the patch to a clean, dry area of skin on your lower abdomen or buttocks. Avoid breasts, waistline, or areas that may be rubbed by clothing.
- Rotate application sites to prevent skin irritation. Do not apply to the same spot twice in a row.
- If a patch falls off, try to reapply it. If it doesn't stick, apply a new patch and continue your regular schedule.
- Avoid applying lotions, oils, or powders to the skin area where you plan to apply the patch, as this can prevent it from sticking properly.
- Discuss any concerns about diet, exercise, or smoking with your doctor, as these can impact your overall health and the effectiveness/safety of HRT.
- Regularly perform breast self-exams and attend scheduled mammograms and pelvic exams.
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:
0.0375 mg/day applied transdermally once weekly. Patch is replaced every 7 days.
Dose Range:
0.025 - 0.1 mg
Condition-Specific Dosing:
vasomotorSymptoms:
Initial dose typically 0.025 mg/day or 0.0375 mg/day, adjusted based on response and tolerability. For 0.0375 mg/day, apply one patch once weekly.
preventionOfOsteoporosis:
0.025 mg/day or 0.0375 mg/day applied once weekly. Lowest effective dose should be used.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Estradiol transdermal patches are not indicated for pediatric use. However, oral estradiol may be used for certain conditions like Turner Syndrome, but transdermal is not standard for this age group.)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
Use with caution. Estrogens are primarily metabolized by the liver, but renal excretion of metabolites occurs. No specific dose adjustment guidelines.
Dialysis:
No specific recommendations. Use with caution.
Hepatic Impairment:
Mild:
Use with caution.
Moderate:
Use with caution. Estrogens are extensively metabolized by the liver. Impaired hepatic function may lead to increased systemic exposure.
Severe:
Contraindicated in patients with severe liver dysfunction or disease.
Confidence:
Medium
Pharmacology
Mechanism of Action
Estradiol is the primary estrogen secreted by the human ovary. It binds to 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 the development and maintenance of the female reproductive system and secondary sex characteristics. In menopausal women, it replaces the declining endogenous estrogen, alleviating vasomotor symptoms and preventing bone loss.
Pharmacokinetics
Absorption:
Bioavailability:
High (avoids first-pass hepatic metabolism compared to oral forms)
Tmax:
Approximately 2-4 hours after patch application (for initial rise), steady-state levels typically reached within 24-48 hours.
FoodEffect:
Not applicable for transdermal patch.
Distribution:
Vd:
Not readily available for transdermal, but generally large for estrogens due to lipophilicity.
ProteinBinding:
Approximately 98% (primarily to sex hormone-binding globulin (SHBG) and albumin).
CnssPenetration:
Yes (estrogen receptors are present in the CNS).
Elimination:
HalfLife:
Approximately 1-2 hours (for estradiol itself, but the patch provides continuous release, leading to sustained levels). Effective half-life from patch is longer due to reservoir effect.
Clearance:
Not readily available for transdermal, but rapid for estradiol.
ExcretionRoute:
Renal (primarily as glucuronide and sulfate conjugates), some biliary excretion.
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Within hours to days for symptomatic relief.
PeakEffect:
Within weeks to months for full therapeutic effect (e.g., bone density, sustained symptom relief).
DurationOfAction:
7 days (for weekly patch) due to continuous transdermal delivery.
Safety & Warnings
BLACK BOX WARNING
Estrogens and Estrogen Plus Progestin Therapy:
1. Estrogen-Alone Therapy: There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. 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 vaginal bleeding. There is an increased risk of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) receiving estrogen-alone therapy.
2. Estrogen Plus Progestin Therapy: Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported an increased risk of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women (50 to 79 years of age) receiving daily conjugated equine estrogens (CEE) plus medroxyprogesterone acetate (MPA). The WHI study also reported an increased risk of invasive breast cancer. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving CEE plus MPA or CEE alone.
3. Other risks: Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. The WHI and WHIMS studies were conducted in generally healthy postmenopausal women. 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.
1. Estrogen-Alone Therapy: There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. 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 vaginal bleeding. There is an increased risk of stroke and deep vein thrombosis (DVT) in postmenopausal women (50 to 79 years of age) receiving estrogen-alone therapy.
2. Estrogen Plus Progestin Therapy: Estrogen plus progestin therapy should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported an increased risk of DVT, pulmonary embolism (PE), stroke, and myocardial infarction (MI) in postmenopausal women (50 to 79 years of age) receiving daily conjugated equine estrogens (CEE) plus medroxyprogesterone acetate (MPA). The WHI study also reported an increased risk of invasive breast cancer. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving CEE plus MPA or CEE alone.
3. Other risks: Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. The WHI and WHIMS studies were conducted in generally healthy postmenopausal women. 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.
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 immediate 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 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 trouble breathing.
Blood Clots and High Calcium Levels
Seek immediate medical attention 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 any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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
Irritation at the site of administration
Reporting Side Effects
This list is not exhaustive, and you may experience other 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 or seek immediate 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 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 trouble breathing.
Blood Clots and High Calcium Levels
Seek immediate medical attention 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 any other symptoms that bother you or do not go away, contact your doctor or seek medical help:
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
Irritation at the site of administration
Reporting Side Effects
This list is not exhaustive, and you may experience other 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, dizziness, or fainting
- Sudden vision changes (e.g., partial or complete loss of vision)
- Numbness or weakness in an arm or leg, especially on one side of the body
- Slurred speech or difficulty speaking
- Sudden chest pain, shortness of breath, or coughing up blood
- Pain, swelling, or tenderness in one or both legs (especially calf)
- Yellowing of the skin or eyes (jaundice)
- Severe abdominal pain
- New breast lump or changes in breasts
- Unusual or abnormal vaginal bleeding (especially after menopause)
- Signs of an allergic reaction (rash, itching, swelling, severe dizziness, trouble breathing)
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 suspected 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. Do not initiate, 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. 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 suspected 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. Do not initiate, 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 immobility may increase your risk of developing blood clots. 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. Additionally, adhere to your doctor's recommendations for regular blood work and bone density tests.
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 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 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.
To maximize the effectiveness of this medication, use it in conjunction with calcium and vitamin D supplements, and engage in weight-bearing exercises like walking or physical therapy. Follow the diet and exercise plan recommended by your doctor.
In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss this with your doctor. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, consult your doctor to discuss 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 immobility may increase your risk of developing blood clots. 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. Additionally, adhere to your doctor's recommendations for regular blood work and bone density tests.
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 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 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.
To maximize the effectiveness of this medication, use it in conjunction with calcium and vitamin D supplements, and engage in weight-bearing exercises like walking or physical therapy. Follow the diet and exercise plan recommended by your doctor.
In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss this with your doctor. If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, consult your doctor to discuss potential risks to your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Breast tenderness
- Abdominal pain
- Drowsiness/fatigue
- Withdrawal bleeding (in women with a uterus)
What to Do:
Remove the patch immediately. There is no specific antidote. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center or seek emergency medical attention. Call 1-800-222-1222.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., Anastrozole, Letrozole, Exemestane) - concurrent use would counteract their mechanism of action in breast cancer treatment.
- Tranexamic acid (increased risk of thrombosis)
Major Interactions
- CYP3A4 inducers (e.g., Carbamazepine, Phenobarbital, Phenytoin, Rifampin, St. John's Wort) - may decrease estradiol levels, reducing efficacy.
- CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Ritonavir, Clarithromycin, Grapefruit juice) - may increase estradiol levels, increasing risk of adverse effects.
- Thyroid hormone replacement (e.g., Levothyroxine) - estrogens can increase thyroid-binding globulin (TBG), potentially increasing thyroid hormone requirements.
- Warfarin - estrogens may decrease anticoagulant effects of warfarin; monitor INR.
Moderate Interactions
- Corticosteroids (e.g., Prednisone) - estrogens may decrease corticosteroid clearance, increasing their effects.
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its levels and toxicity.
- Lamotrigine - estrogens may decrease lamotrigine levels, reducing seizure control.
- Folic acid supplements - may reduce efficacy of estradiol in some contexts (less common for HRT).
Minor Interactions
- Ascorbic acid (Vitamin C) - may increase estrogen levels slightly by inhibiting sulfate conjugation.
Monitoring
Baseline Monitoring
Complete medical history and physical examination (including blood pressure, breast and pelvic examination)
Rationale: To identify contraindications, risk factors, and establish baseline health status.
Timing: Prior to initiation of therapy.
Mammography
Rationale: To screen for breast cancer prior to initiating estrogen therapy.
Timing: Prior to initiation, and periodically thereafter as per guidelines.
Lipid profile
Rationale: Estrogens can affect lipid metabolism; establish baseline.
Timing: Prior to initiation.
Liver function tests (LFTs)
Rationale: To assess hepatic function, as estrogens are metabolized by the liver.
Timing: Prior to initiation, especially if history of liver disease.
Routine Monitoring
Blood pressure
Frequency: Annually, or more frequently if clinically indicated.
Target: <130/80 mmHg (general target)
Action Threshold: Sustained elevation requiring intervention.
Breast examination
Frequency: Annually by healthcare provider; monthly self-examination.
Target: Normal findings
Action Threshold: New lumps, pain, or discharge requiring further investigation.
Pelvic examination and Pap test
Frequency: Annually, or as per national screening guidelines.
Target: Normal findings
Action Threshold: Abnormal findings requiring further investigation.
Mammography
Frequency: Periodically, as per national screening guidelines (e.g., every 1-2 years for women over 40-50).
Target: Normal findings
Action Threshold: Suspicious findings requiring further investigation.
Endometrial biopsy (if indicated)
Frequency: If abnormal uterine bleeding occurs in women with an intact uterus.
Target: Normal endometrial histology
Action Threshold: Abnormal bleeding or endometrial thickening on ultrasound.
Symptom Monitoring
- Resolution of vasomotor symptoms (hot flashes, night sweats)
- Improvement in vaginal dryness or atrophy
- Mood changes
- Breast tenderness or swelling
- Fluid retention/bloating
- Headaches
- Nausea
- Leg pain, swelling, or redness (signs of DVT)
- Chest pain or shortness of breath (signs of PE)
- Sudden severe headache, vision changes, weakness/numbness (signs of stroke)
- Abnormal vaginal bleeding
Special Patient Groups
Pregnancy
Contraindicated. Estradiol transdermal patches are not indicated for use in pregnant women. There is no indication for estrogen therapy during pregnancy, and there is evidence of fetal harm.
Trimester-Specific Risks:
First Trimester:
Known to cause virilization of female fetuses and other congenital anomalies if administered 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. Estrogens are excreted in human milk and may decrease the quantity and quality of breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Potential for adverse effects on the nursing infant (e.g., feminization, decreased milk supply).
Pediatric Use
Not indicated for pediatric use. Safety and effectiveness have not been established in pediatric patients.
Geriatric Use
Use with caution in women 65 years of age or older. The Women's Health Initiative Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving estrogen plus progestin or estrogen alone. The lowest effective dose for the shortest duration should be used. Close monitoring for adverse effects is recommended.
Clinical Information
Clinical Pearls
- Transdermal estradiol avoids first-pass hepatic metabolism, which may result in a more favorable lipid profile and lower risk of venous thromboembolism compared to oral estrogens, though risk is still present.
- Always use the lowest effective dose for the shortest duration consistent with treatment goals.
- For women with an intact uterus, a progestin must be co-administered to reduce the risk of endometrial hyperplasia and cancer.
- Patients should be instructed on proper patch application and rotation to minimize skin irritation and ensure consistent drug delivery.
- Counsel patients on the importance of regular follow-up appointments, including breast exams and mammograms.
- Inform patients about the signs and symptoms of serious adverse events (e.g., blood clots, stroke, heart attack, breast cancer) and when to seek immediate medical attention.
Alternative Therapies
- Selective Serotonin Reuptake Inhibitors (SSRIs) or Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) for vasomotor symptoms (e.g., Paroxetine, Venlafaxine)
- Gabapentin for vasomotor symptoms
- Clonidine for vasomotor symptoms
- Non-hormonal vaginal moisturizers/lubricants for vaginal atrophy
- Bisphosphonates, Denosumab, Raloxifene for osteoporosis prevention (if HRT is contraindicated or not preferred)
Cost & Coverage
Average Cost:
$50 - $200 per 4 patches (1 month supply)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic versions; Tier 3 or higher for brand names. Coverage varies by insurance plan.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may have additional patient information leaflets, 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.