Estradiol Tds 0.06mg Patch 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
Estrogen; Hormone Replacement Therapy (HRT)
Pharmacologic Class
Estrogen receptor agonist
Pregnancy Category
Category X
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol transdermal patches are a form of hormone replacement therapy (HRT) that deliver estrogen through your skin. They are used to relieve symptoms of menopause, such as hot flashes and vaginal dryness, and to help prevent osteoporosis (bone thinning) in women after menopause. This specific patch delivers 0.06 milligrams of estradiol per day and is typically changed once 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, avoiding the 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.
Wait at least 7 days before applying a new patch to the same site.
Avoid applying the medication to skin with problems, such as cuts, wounds, or irritated areas.
Do not apply the patch to the 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 for patch application to ensure better adhesion.
Avoid applying the patch near the waistline or on areas that may cause the patch to come off when sitting.
Do not cut or divide the patches, and do not use damaged patches.
Managing Patch Issues
If the patch falls off, reapply it to the same site. If you cannot reapply the patch, apply a new one to a different area.
Wear only one patch at a time to avoid excessive medication.
Disposing of Used Patches
After removing a used patch, fold the sticky sides together and dispose of it in a secure location, out of reach of children and pets.
Storage and Disposal
Store this medication at room temperature in a dry place, avoiding bathrooms and areas with high humidity.
Missed Dose
* If you miss a dose, apply a new patch as soon as possible 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, avoiding the 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.
Wait at least 7 days before applying a new patch to the same site.
Avoid applying the medication to skin with problems, such as cuts, wounds, or irritated areas.
Do not apply the patch to the 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 for patch application to ensure better adhesion.
Avoid applying the patch near the waistline or on areas that may cause the patch to come off when sitting.
Do not cut or divide the patches, and do not use damaged patches.
Managing Patch Issues
If the patch falls off, reapply it to the same site. If you cannot reapply the patch, apply a new one to a different area.
Wear only one patch at a time to avoid excessive medication.
Disposing of Used Patches
After removing a used patch, fold the sticky sides together and dispose of it in a secure location, out of reach of children and pets.
Storage and Disposal
Store this medication at room temperature in a dry place, avoiding bathrooms and areas with high humidity.
Missed Dose
* If you miss a dose, apply a new patch as soon as possible after removing the old one.
Lifestyle & Tips
- Do not smoke: Smoking significantly increases the risk of blood clots, stroke, and heart attack when taking estrogens.
- Maintain a healthy weight and engage in regular physical activity.
- Eat a balanced diet rich in calcium and vitamin D for bone health.
- Limit alcohol intake.
- Apply the patch to a clean, dry, hairless area of the skin on the lower abdomen or buttocks. Avoid the breasts, waistline, or areas that may be rubbed by clothing.
- Rotate application sites to prevent skin irritation.
- If you miss a dose, apply a new patch as soon as you remember, then continue your regular schedule. Do not apply two patches at once.
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:
One 0.06 mg/day patch applied weekly (changed every 7 days)
Dose Range:
0.025 - 0.1 mg
Condition-Specific Dosing:
menopausalSymptoms:
Initial dose typically 0.025 mg/day or 0.0375 mg/day, adjusted based on response and tolerability. 0.06 mg/day is a common maintenance dose.
osteoporosisPrevention:
Typically 0.025 mg/day or 0.0375 mg/day, adjusted to the lowest effective dose.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Estradiol may be used for hypogonadism in adolescents, but specific transdermal patch dosing for this indication would be lower and individualized, not typically 0.06mg/day as an initial dose for HRT).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment required.
Moderate:
No specific adjustment required.
Severe:
No specific adjustment required, but use with caution due to potential fluid retention.
Dialysis:
No specific adjustment required, but monitor for fluid retention.
Hepatic Impairment:
Mild:
Use with caution; monitor for adverse effects.
Moderate:
Use with caution; consider lower doses or alternative therapies. Estrogens are extensively metabolized by the liver.
Severe:
Contraindicated in severe hepatic impairment or liver disease due to impaired metabolism and increased risk of cholestasis and other adverse effects.
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 (e.g., reproductive organs, breast, bone, brain, liver). This binding leads to a cascade of intracellular events, including gene transcription and protein synthesis, mediating the physiological effects of estrogen, such as maintaining female reproductive health, bone density, and modulating lipid metabolism.
Pharmacokinetics
Absorption:
Bioavailability:
High (transdermal bypasses first-pass hepatic metabolism, leading to a more favorable estradiol to estrone ratio compared to oral administration).
Tmax:
Achieves steady-state plasma concentrations within 1-3 days of initial application. Peak concentrations are generally reached within 24-48 hours after patch application.
FoodEffect:
Not applicable for transdermal administration.
Distribution:
Vd:
Approximately 0.9-1.1 L/kg (for estradiol)
ProteinBinding:
Highly protein bound (approximately 98%), primarily to sex hormone-binding globulin (SHBG) and albumin.
CnssPenetration:
Limited (estradiol crosses the blood-brain barrier, but therapeutic effects are primarily peripheral for HRT).
Elimination:
HalfLife:
Approximately 1-2 hours (for circulating estradiol, but the patch provides continuous release, extending the effective half-life for sustained therapeutic levels).
Clearance:
Approximately 650-900 mL/min/mΒ²
ExcretionRoute:
Primarily renal (urine) as glucuronide and sulfate conjugates; some fecal excretion.
Unchanged:
Minimal (less than 1% of estradiol is excreted unchanged in urine).
Pharmacodynamics
OnsetOfAction:
Gradual (therapeutic levels achieved within 1-3 days of patch application).
PeakEffect:
Steady-state concentrations are reached within 1-3 days and maintained throughout the wearing period.
DurationOfAction:
7 days (for weekly patch formulations).
Safety & Warnings
BLACK BOX WARNING
Estrogens and estrogen plus progestin therapies 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) receiving daily oral conjugated estrogens (0.625 mg) alone or in combination with medroxyprogesterone acetate (2.5 mg) compared to placebo. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving daily oral conjugated estrogens alone or in combination with medroxyprogesterone acetate compared to placebo. These risks should be weighed against the benefits of therapy, and estrogens should be prescribed at the lowest effective dose for the shortest duration consistent with treatment goals and risks for the individual woman.
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallbladder problems, such as:
+ Pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
+ Bloating
+ Severe upset stomach or vomiting
Signs of pancreatitis (pancreas problem), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of high blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Blurred eyesight
Eyesight changes or loss
Bulging eyes
Changes in how contact lenses feel
Breast lump, pain, or soreness
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, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, contact your doctor.
Blood Clots and High Calcium Levels
Seek medical attention immediately 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. Contact your doctor right away if you experience signs of high calcium levels, such as:
Weakness
Confusion
Fatigue
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
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
Irritation at the site of administration
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of gallbladder problems, such as:
+ Pain in the upper right belly area, right shoulder area, or between the shoulder blades
+ Yellow skin or eyes
+ Fever with chills
+ Bloating
+ Severe upset stomach or vomiting
Signs of pancreatitis (pancreas problem), including:
+ Severe stomach pain
+ Severe back pain
+ Severe upset stomach or vomiting
Signs of high blood pressure, such as:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Blurred eyesight
Eyesight changes or loss
Bulging eyes
Changes in how contact lenses feel
Breast lump, pain, or soreness
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, leading to swelling or weight gain. If you experience swelling, weight gain, or trouble breathing, contact your doctor.
Blood Clots and High Calcium Levels
Seek medical attention immediately 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. Contact your doctor right away if you experience signs of high calcium levels, such as:
Weakness
Confusion
Fatigue
Headache
Upset stomach or vomiting
Constipation
Bone pain
Other Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or do not go away:
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
Irritation at the site of administration
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache, dizziness, or fainting
- Sudden vision changes (e.g., partial or complete loss of vision)
- Sudden numbness or weakness on one side of the body
- Slurred speech or difficulty speaking
- Sudden chest pain, shortness of breath, or coughing up blood
- Pain, swelling, or redness in one leg (especially the calf)
- New breast lump or changes in the breast (e.g., dimpling, nipple discharge)
- Unusual vaginal bleeding (especially after menopause)
- Yellowing of the skin or eyes (jaundice)
- 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. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note that 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 you experienced, including any symptoms that occurred.
A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note that 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 anticipate being 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.
This medication can cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor. Prolonged use of this drug may lead to the development of dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear.
This medication may interfere with 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, follow a diet and exercise plan that includes calcium and vitamin D supplements, as well as weight-bearing activities like walking or physical therapy, as recommended by your doctor. In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss any concerns 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 any potential risks to your baby.
If you anticipate being 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.
This medication can cause elevated triglyceride levels. If you have a history of high triglyceride levels, inform your doctor. Prolonged use of this drug may lead to the development of dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear.
This medication may interfere with 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, follow a diet and exercise plan that includes calcium and vitamin D supplements, as well as weight-bearing activities like walking or physical therapy, as recommended by your doctor. In some cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Discuss any concerns 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 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:
There is no specific antidote for estrogen overdose. Treatment is symptomatic and supportive. Remove the patch immediately. In case of suspected overdose, contact a poison control center (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use would counteract the effect of the aromatase inhibitor.
- Tranexamic acid (increased risk of thrombosis).
Major Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, phenytoin, St. John's Wort) - may significantly decrease estradiol levels, reducing efficacy.
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may increase estradiol levels, potentially increasing adverse effects.
- Warfarin - estrogens can alter coagulation factors, potentially decreasing the anticoagulant effect of warfarin; monitor INR closely.
- Thyroid hormone replacement (e.g., levothyroxine) - estrogens increase thyroid-binding globulin (TBG), potentially increasing bound thyroid hormone and decreasing free thyroid hormone, requiring an increase in thyroid hormone dose.
- Corticosteroids (e.g., prednisone) - estrogens can decrease the clearance of corticosteroids, leading to increased corticosteroid effects and toxicity.
Moderate Interactions
- Griseofulvin - may reduce estrogen efficacy.
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its levels and toxicity.
- Lamotrigine - estrogens may decrease lamotrigine levels, potentially leading to loss of seizure control.
- Fluvoxamine - may increase estrogen levels.
Minor Interactions
- Not many specific minor interactions commonly cited for transdermal estradiol beyond general considerations.
Monitoring
Baseline Monitoring
Complete medical history and physical examination (including blood pressure, breast exam, pelvic exam)
Rationale: To identify contraindications, risk factors for adverse events (e.g., VTE, breast cancer), and establish baseline health status.
Timing: Prior to initiation of therapy.
Mammogram
Rationale: To screen for breast cancer before initiating estrogen therapy, as estrogens can increase breast cancer risk.
Timing: Prior to initiation of therapy, and periodically thereafter as per screening guidelines.
Lipid profile
Rationale: Estrogens can affect lipid metabolism; establish baseline for cardiovascular risk assessment.
Timing: Prior to initiation of therapy.
Liver function tests (LFTs)
Rationale: To assess hepatic function, as estrogens are metabolized by the liver and contraindicated in severe liver disease.
Timing: Prior to initiation of therapy.
Routine Monitoring
Annual physical examination (including blood pressure, breast exam, pelvic exam)
Frequency: Annually
Target: Normal for age and health status
Action Threshold: Significant changes, new symptoms, or abnormal findings require further investigation.
Mammogram
Frequency: Periodically, as per national screening guidelines (e.g., every 1-2 years)
Target: No suspicious findings
Action Threshold: New lumps, pain, nipple discharge, or abnormal imaging findings require immediate follow-up.
Blood pressure
Frequency: Annually, or more frequently if hypertension is present
Target: <130/80 mmHg
Action Threshold: Sustained elevation (e.g., >140/90 mmHg) requires evaluation and management.
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 (e.g., leg pain/swelling, chest pain, shortness of breath, sudden severe headache, vision changes, breast lump) require immediate medical attention.
Symptom Monitoring
- Leg pain, swelling, tenderness, or redness (signs of DVT)
- Sudden chest pain or shortness of breath (signs of PE)
- Sudden severe headache, vision changes, slurred speech, weakness/numbness on one side of the body (signs of stroke)
- Chest pain, discomfort, pressure, or pain radiating to arm/jaw (signs of MI)
- New breast lump, nipple discharge, or skin changes on the breast
- Abnormal vaginal bleeding (e.g., postmenopausal bleeding, irregular bleeding)
- Severe abdominal pain
- Jaundice or yellowing of skin/eyes
- Mood changes, depression
Special Patient Groups
Pregnancy
Contraindicated. Estradiol is classified as Pregnancy Category X. There is no indication for estrogen therapy during pregnancy, and there is evidence of fetal risk.
Trimester-Specific Risks:
First Trimester:
Potential for adverse effects on fetal development, including genital abnormalities.
Second Trimester:
Not indicated; continued exposure carries risks without benefit.
Third Trimester:
Not indicated; continued exposure carries risks without benefit.
Lactation
Not recommended. Estrogens can decrease the quantity and quality of breast milk and are excreted in breast milk. Potential adverse effects on the infant are possible.
Infant Risk:
L3 (Moderate risk). May cause decreased milk production and potential for adverse effects on the infant (e.g., feminization effects, although unlikely with typical exposure).
Pediatric Use
Not indicated for general use in pediatric populations. While estrogens are used in specific conditions like Turner syndrome or hypogonadism, the 0.06 mg/day dose is typically too high for initial pediatric therapy, and specific dosing regimens are individualized and initiated at much lower doses.
Geriatric Use
Use with caution, especially in women aged 65 years or older. The Women's Health Initiative Memory Study (WHIMS) showed an increased risk of probable dementia in women 65 years of age or older receiving estrogen-alone or estrogen plus progestin therapy. Increased risk of stroke and VTE also observed in older women. Use the lowest effective dose for the shortest duration.
Clinical Information
Clinical Pearls
- Transdermal estradiol bypasses first-pass hepatic metabolism, resulting in a more favorable estradiol to estrone ratio and potentially lower risk of VTE compared to oral estrogens, though VTE 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 educated on the signs and symptoms of serious adverse events (e.g., VTE, stroke, MI, breast cancer) and instructed to seek immediate medical attention if they occur.
- Regular follow-up, including annual physical exams and mammograms, is crucial.
- Adherence to the weekly patch change schedule is important for maintaining consistent hormone levels.
Alternative Therapies
- Selective Estrogen Receptor Modulators (SERMs) (e.g., bazedoxifene/conjugated estrogens, ospemifene, tamoxifen, raloxifene)
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
- Non-hormonal therapies for osteoporosis (e.g., bisphosphonates, denosumab, teriparatide)
- Lifestyle modifications (e.g., diet, exercise, smoking cessation)
Cost & Coverage
Average Cost:
$30 - $150 per 4 patches (1 month supply)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic estradiol patches); Tier 3 or higher for brand-name products.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.