Estradiol 0.075mg Patch (once Wk)
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 Receptor Agonist
Pregnancy Category
Category X
FDA Approved
Mar 1994
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol 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 bone thinning (osteoporosis) after menopause. The patch is applied 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.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the patch to skin with any problems, such as cuts, wounds, or irritation.
Avoid applying 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 to apply the patch.
Do not apply the patch to your waistline or an area that may cause the patch to come off when sitting.
Do not cut or divide the patches, and do not use damaged patches.
Managing the Patch
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.
After removing a 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.
Dispose of used patches and packaging in a secure location, out of reach of children and pets.
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.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the patch to skin with any problems, such as cuts, wounds, or irritation.
Avoid applying 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 to apply the patch.
Do not apply the patch to your waistline or an area that may cause the patch to come off when sitting.
Do not cut or divide the patches, and do not use damaged patches.
Managing the Patch
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.
After removing a 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.
Dispose of used patches and packaging in a secure location, out of reach of children and pets.
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, as smoking significantly increases the risk of blood clots, heart attack, and stroke, especially when taking estrogen.
- Maintain a healthy diet and engage in regular physical activity to support bone health and cardiovascular health.
- Limit alcohol consumption.
- Apply the patch to a clean, dry, hairless area of skin on your lower abdomen or buttocks. Avoid applying to breasts, waistline, or irritated skin.
- Rotate application sites to prevent skin irritation.
- If a patch falls off, reapply it or apply a new one for the remainder of the 7-day period.
- If you forget to change your patch on the scheduled day, change it as soon as you remember and then resume your regular schedule.
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:
Apply one 0.075 mg/day patch topically to the skin once weekly. Replace the patch every 7 days.
Dose Range:
0.025 - 0.1 mg
Condition-Specific Dosing:
vasomotor_symptoms_of_menopause:
Initial dose typically 0.025 mg/day, titrate based on response. 0.075 mg/day is a common effective dose.
prevention_of_postmenopausal_osteoporosis:
0.025 mg/day to 0.05 mg/day, 0.075 mg/day may be used if higher dose is needed for other symptoms.
vulvar_and_vaginal_atrophy:
Initial dose typically 0.025 mg/day, titrate based on response. 0.075 mg/day may be used if higher dose is needed for other symptoms.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (not indicated for pediatric use)
Dose Adjustments
Renal Impairment:
Mild:
No specific dosage adjustment recommended.
Moderate:
No specific dosage adjustment recommended, but use with caution.
Severe:
Use with caution; monitor for fluid retention and exacerbation of renal disease.
Dialysis:
Considerations: Not specifically studied, but caution due to potential fluid retention and metabolic effects.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function.
Moderate:
Use with caution; monitor liver function. Consider lower doses.
Severe:
Contraindicated in patients with severe liver dysfunction or disease.
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, including the reproductive tract, breast, hypothalamus, pituitary, bone, and liver. This binding leads to gene transcription and protein synthesis, mediating the physiological effects of estrogens, such as the development and maintenance of the female reproductive system and secondary sex characteristics. In menopausal women, it replaces declining endogenous estrogen levels to alleviate symptoms.
Pharmacokinetics
Absorption:
Bioavailability:
Transdermal administration bypasses first-pass hepatic metabolism, resulting in a more favorable estradiol to estrone ratio compared to oral administration. Absolute bioavailability is not precisely quantified but is efficient.
Tmax:
Steady-state estradiol concentrations are generally achieved within 24-48 hours of initial patch application and maintained over the 7-day wear period.
FoodEffect:
Not applicable for transdermal patch.
Distribution:
Vd:
Approximately 1.2 L/kg (for estradiol)
ProteinBinding:
Highly protein bound (approximately 98%), primarily to sex hormone-binding globulin (SHBG) and albumin.
CnssPenetration:
Limited for therapeutic effects, but estrogens can influence CNS function.
Elimination:
HalfLife:
Estradiol: Approximately 1-2 hours (systemic half-life); however, the transdermal patch provides sustained release over 7 days.
Clearance:
Approximately 650-900 mL/min/kg (for estradiol)
ExcretionRoute:
Primarily renal (urine) as glucuronide and sulfate conjugates; some fecal excretion.
Unchanged:
Less than 1% (excreted unchanged in urine)
Pharmacodynamics
OnsetOfAction:
Symptomatic relief may begin within days to weeks; full therapeutic effect for some indications (e.g., osteoporosis prevention) takes longer.
PeakEffect:
Steady-state concentrations achieved within 24-48 hours and maintained over the 7-day wear period.
DurationOfAction:
7 days (due to continuous transdermal delivery).
Safety & Warnings
BLACK BOX WARNING
Estrogens and progestins should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) during 5.2 years of treatment with conjugated equine estrogens (CEE) plus medroxyprogesterone acetate (MPA) relative to placebo. The WHI study also reported an increased risk of stroke and deep vein thrombosis in postmenopausal women (50-79 years of age) during 6.8 years of treatment with CEE alone relative to placebo. The WHI Memory Study (WHIMS), a substudy of WHI, reported an increased risk of probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with CEE plus MPA and during 5.2 years of treatment with CEE alone. 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
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast-related symptoms: lump in the breast, breast pain or soreness, or nipple discharge.
Vaginal symptoms: itching or discharge, or abnormal vaginal bleeding.
Depression or other mood changes, memory problems or loss, or fever.
Urinary problems: inability to pass urine or changes in urine output, or pain while passing urine.
Fluid retention: swelling, weight gain, or trouble breathing.
Blood Clots and High Calcium Levels
If you experience any of the following symptoms, seek medical help right away:
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: weakness, confusion, feeling tired, headache, upset stomach or vomiting, constipation, or bone pain.
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. 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 breasts
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
Reporting Side Effects
If you have questions about side effects or want to report any, contact your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades; yellow skin or eyes; fever with chills; bloating; or severe upset stomach or vomiting.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Breast-related symptoms: lump in the breast, breast pain or soreness, or nipple discharge.
Vaginal symptoms: itching or discharge, or abnormal vaginal bleeding.
Depression or other mood changes, memory problems or loss, or fever.
Urinary problems: inability to pass urine or changes in urine output, or pain while passing urine.
Fluid retention: swelling, weight gain, or trouble breathing.
Blood Clots and High Calcium Levels
If you experience any of the following symptoms, seek medical help right away:
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: weakness, confusion, feeling tired, headache, upset stomach or vomiting, constipation, or bone pain.
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. 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 breasts
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
Reporting Side Effects
If you have questions about side effects or want to report any, contact your doctor or the FDA at 1-800-332-1088. You can also report side effects online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden severe headache or migraine
- 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)
- Yellowing of the skin or eyes (jaundice)
- New breast lump or changes in breasts
- Unusual vaginal bleeding or spotting after menopause
- 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. Be sure to describe the signs and symptoms of your allergic reactions.
A history of certain health conditions, including:
+ Bleeding disorders or blood clots
+ A higher risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack or 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. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the signs and symptoms of your allergic reactions.
A history of certain health conditions, including:
+ Bleeding disorders or blood clots
+ A higher risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack or 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. Never start, stop, or change the dose 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 if so, will instruct you 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 inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), 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, ovarian cancer, and others, 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 to use sunscreen and protective clothing and eyewear when going outside.
This medication may interfere with certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this drug. Smoking can increase your risk of heart disease, so it is recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
To maximize the effectiveness of this medication, use it in conjunction with calcium and vitamin D supplements and engage in weight-bearing exercises, such as walking or physical therapy, as directed by your doctor. Adhere to 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 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 inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), 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, ovarian cancer, and others, 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 to use sunscreen and protective clothing and eyewear when going outside.
This medication may interfere with certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this drug. Smoking can increase your risk of heart disease, so it is recommended that you do not smoke. Limit your alcohol consumption, and if you regularly drink grapefruit juice or eat grapefruit, discuss this with your doctor.
To maximize the effectiveness of this medication, use it in conjunction with calcium and vitamin D supplements and engage in weight-bearing exercises, such as walking or physical therapy, as directed by your doctor. Adhere to 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 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:
Remove the patch immediately. There is no specific antidote. Treatment is symptomatic and supportive. 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, exemestane) - concurrent use is generally contraindicated as estrogens counteract their mechanism of action.
- Dasabuvir/Ombitasvir/Paritaprevir/Ritonavir combination (Viekira Pak) - risk of ALT elevations.
Major Interactions
- CYP3A4 inducers (e.g., Carbamazepine, Phenobarbital, Phenytoin, Rifampin, St. John's Wort) - may significantly decrease estradiol levels, reducing efficacy.
- Thyroid hormone replacement therapy (e.g., Levothyroxine) - estrogens can increase thyroid-binding globulin (TBG), potentially increasing the need for thyroid hormone.
- Warfarin - estrogens may alter the anticoagulant effect of warfarin; monitor INR.
- Flibanserin - increased flibanserin exposure.
Moderate Interactions
- CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Grapefruit juice) - may increase estradiol levels, potentially increasing adverse effects.
- Corticosteroids (e.g., Prednisolone) - estrogens may decrease the clearance of corticosteroids, leading to increased effects.
- Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its levels and toxicity.
- Lamotrigine - estrogens may decrease lamotrigine levels, potentially leading to loss of seizure control.
Minor Interactions
- Not specifically identified for minor interactions with significant clinical impact for transdermal estradiol.
Monitoring
Baseline Monitoring
Complete Medical History and Physical Exam (including blood pressure, breast exam, pelvic exam, Pap test)
Rationale: To identify contraindications, risk factors for adverse events (e.g., cardiovascular disease, breast cancer), and establish baseline health status.
Timing: Prior to initiation of therapy.
Mammography
Rationale: To screen for breast cancer, as estrogen therapy can increase breast cancer risk.
Timing: Prior to initiation of therapy, and periodically thereafter as per guidelines.
Lipid Panel
Rationale: To assess cardiovascular risk factors, as estrogens can affect lipid profiles.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs)
Rationale: To assess hepatic function, especially in patients with a history of liver disease, as estrogens are metabolized by the liver.
Timing: Prior to initiation of therapy.
Routine Monitoring
Blood Pressure
Frequency: Annually, or more frequently if clinically indicated.
Target: <120/80 mmHg
Action Threshold: Sustained elevation (e.g., >140/90 mmHg) warrants investigation and management.
Breast Exam and Mammography
Frequency: Annually (breast exam); Mammography as per national guidelines (e.g., every 1-2 years for women over 40-50).
Target: No new lumps or suspicious findings.
Action Threshold: Any new breast lump, pain, or suspicious mammogram finding requires immediate investigation.
Pelvic Exam and Pap Test
Frequency: Annually (pelvic exam); Pap test as per national guidelines (e.g., every 3-5 years).
Target: Normal findings.
Action Threshold: Abnormal uterine bleeding, pelvic pain, or abnormal Pap test results require investigation.
Symptom Review (e.g., vasomotor symptoms, vaginal dryness)
Frequency: At least annually, or at each follow-up visit.
Target: Adequate symptom control with minimal side effects.
Action Threshold: Persistent or worsening symptoms, or bothersome side effects, warrant dose adjustment or consideration of alternative therapy.
Symptom Monitoring
- Unusual vaginal bleeding or spotting
- New breast lump or changes
- Leg pain, swelling, or tenderness (signs of DVT)
- Sudden chest pain, shortness of breath, or coughing up blood (signs of PE)
- Sudden severe headache, vision changes, slurred speech, weakness or numbness in an arm or leg (signs of stroke)
- Chest pain or discomfort, pain radiating to arm, back, neck, jaw, or stomach (signs of MI)
- Yellowing of skin or eyes (jaundice)
- Severe abdominal pain
- Mood changes, depression
Special Patient Groups
Pregnancy
Estradiol is contraindicated during pregnancy (Pregnancy Category X). There is no indication for estrogen therapy in pregnancy, and there is evidence of fetal harm.
Trimester-Specific Risks:
First Trimester:
Potential for adverse effects on fetal development, including genital abnormalities in female fetuses.
Second Trimester:
Not applicable, as use is contraindicated.
Third Trimester:
Not applicable, as use is contraindicated.
Lactation
Estradiol is not recommended during lactation (Lactation Risk L3). Estrogens can decrease the quantity and quality of breast milk and may be excreted in breast milk, potentially affecting the nursing infant.
Infant Risk:
Low to moderate risk of adverse effects on the infant (e.g., feminization, jaundice) and potential for inhibition of lactation.
Pediatric Use
Estradiol transdermal patches are not indicated for use in pediatric patients. Safety and efficacy have not been established in this population. Estrogen exposure in children can lead to premature epiphyseal closure and other adverse effects.
Geriatric Use
Use with caution in women 65 years of age or older. The WHIMS study showed an increased risk of probable dementia in women 65 years of age or older treated with CEE alone or CEE plus MPA. The lowest effective dose for the shortest duration should be used. Increased risk of stroke and DVT has also been observed in older women.
Clinical Information
Clinical Pearls
- Transdermal estradiol bypasses first-pass hepatic metabolism, leading to a more favorable estradiol to estrone ratio and potentially fewer hepatic side effects (e.g., less impact on clotting factors, triglycerides) compared to oral estrogens.
- Always use the lowest effective dose for the shortest duration consistent with treatment goals and risks.
- For women with an intact uterus, a progestin must be co-administered to reduce the risk of endometrial hyperplasia and cancer.
- Advise patients to apply the patch to a clean, dry, hairless area of the lower abdomen or buttocks. Rotate application sites to avoid irritation.
- Patients should be educated on the signs and symptoms of serious adverse events (e.g., DVT, PE, stroke, MI, breast cancer) and instructed to seek immediate medical attention if they occur.
- Regular follow-up appointments are crucial for monitoring efficacy, side effects, and adherence to screening guidelines (e.g., mammograms, pelvic exams).
Alternative Therapies
- Other estrogen formulations (oral, vaginal cream/tablet/ring, gel, spray)
- Selective Estrogen Receptor Modulators (SERMs) (e.g., Ospemifene for dyspareunia, Raloxifene for osteoporosis prevention)
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
- Non-hormonal therapies for vaginal atrophy (e.g., vaginal moisturizers, lubricants)
Cost & Coverage
Average Cost:
$50 - $200 per 4 patches (1 month supply)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for generic); Tier 3 or Tier 4 (for brand-name)
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. If you have any questions or concerns about this medication, don't 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 details about the medication taken, the amount, and the time it occurred.