Estradiol 0.05mg Patch (twice 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
Estrogen
Pharmacologic Class
Estrogen receptor agonist
Pregnancy Category
Category X
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Estradiol patches are a form of hormone replacement therapy that deliver estrogen through your skin. They are used to relieve symptoms of menopause, such as hot flashes and vaginal dryness, and to prevent bone loss. This patch replaces the estrogen your body no longer makes after menopause.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It's essential to use this medication as directed.
Application Instructions
Do not take this medication by mouth. It is for skin use only. Avoid getting it in your mouth, nose, or eyes, as it may cause burning.
Apply the patch at the same time every day to maintain a consistent routine.
Before and after applying the patch, wash your hands thoroughly.
Place the patch on clean, dry, and healthy skin on your lower belly or upper buttocks. With each new patch, move the application site to a different area.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the patch to skin with any problems or irritations.
Do not place the patch on your breast or on skin where you have recently used creams, oils, lotions, powder, or other skin products, as this may affect the patch's adhesion.
Choose a hair-free site for the patch to ensure better adhesion.
Avoid placing the patch on your waistline or on an area that may cause it 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, try to reapply it. If you cannot reapply the old patch, apply a new one to a different area.
Wear only one patch at a time.
Disposing of Used Patches
After removing a used patch, fold the sticky sides together to prevent accidental exposure.
Dispose of used patches in a secure location where children and pets cannot access them.
Storage and Disposal
Store this medication at room temperature in a dry place, avoiding bathrooms.
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
Do not take this medication by mouth. It is for skin use only. Avoid getting it in your mouth, nose, or eyes, as it may cause burning.
Apply the patch at the same time every day to maintain a consistent routine.
Before and after applying the patch, wash your hands thoroughly.
Place the patch on clean, dry, and healthy skin on your lower belly or upper buttocks. With each new patch, move the application site to a different area.
Avoid applying a patch to the same site for at least 7 days.
Do not apply the patch to skin with any problems or irritations.
Do not place the patch on your breast or on skin where you have recently used creams, oils, lotions, powder, or other skin products, as this may affect the patch's adhesion.
Choose a hair-free site for the patch to ensure better adhesion.
Avoid placing the patch on your waistline or on an area that may cause it 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, try to reapply it. If you cannot reapply the old patch, apply a new one to a different area.
Wear only one patch at a time.
Disposing of Used Patches
After removing a used patch, fold the sticky sides together to prevent accidental exposure.
Dispose of used patches in a secure location where children and pets cannot access them.
Storage and Disposal
Store this medication at room temperature in a dry place, avoiding bathrooms.
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, hairless area of skin on your lower abdomen or buttocks. Avoid the 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.
- Press the patch firmly in place for about 10 seconds to ensure good adhesion.
- If a patch falls off, reapply it or apply a new one. If it's close to your next scheduled application, just wait and apply the new patch then.
- Avoid applying lotions, oils, or powders to the skin area where you plan to place the patch.
- Avoid exposing the patch to direct sunlight or excessive heat (e.g., hot tubs, saunas) as this can affect drug release.
- Maintain a healthy lifestyle, including regular exercise and a balanced diet, to support overall health and bone density.
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 0.05 mg/day patch transdermally twice weekly (e.g., replace every 3-4 days).
Dose Range:
0.025 - 0.1 mg
Condition-Specific Dosing:
vasomotorSymptomsOfMenopause:
Initial dose typically 0.025 mg/day, titrated based on response. 0.05 mg/day is a common maintenance dose.
vulvarAndVaginalAtrophy:
Often treated with lower doses or local therapy, but systemic 0.05 mg/day can be used.
hypoestrogenism:
Dose individualized based on clinical response and symptom severity.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (except for specific conditions like Turner syndrome, where dosing is individualized and typically initiated at lower doses and titrated up)
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed.
Moderate:
No specific adjustment needed, but use with caution.
Severe:
Use with caution; monitor for fluid retention and adverse effects.
Dialysis:
Considerations: Not well studied, but generally not removed by dialysis. Use with caution due to potential for fluid retention and electrolyte imbalance.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function.
Moderate:
Use with caution; consider lower doses or alternative therapies. Estrogens are extensively metabolized by the liver.
Severe:
Contraindicated due to impaired metabolism and increased risk of cholestasis and other liver complications.
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 conformational changes in the receptor, allowing it to dimerize and bind to estrogen response elements (EREs) on DNA, thereby regulating gene transcription and protein synthesis. This action mediates the physiological effects of estrogen, including the development and maintenance of female reproductive system and secondary sex characteristics, and effects on bone density, lipid metabolism, and the cardiovascular system.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80% (transdermal, bypasses first-pass hepatic metabolism compared to oral)
Tmax:
Approximately 1-2 days (for sustained release from patch)
FoodEffect:
Not applicable for transdermal patch.
Distribution:
Vd:
Approximately 1.2 L/kg
ProteinBinding:
Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin)
CnssPenetration:
Limited for therapeutic effects, but estrogens do cross the blood-brain barrier and have effects on CNS function.
Elimination:
HalfLife:
Approximately 1-2 hours (for circulating estradiol, but sustained release from patch provides continuous delivery)
Clearance:
Approximately 650-900 mL/min/mΒ²
ExcretionRoute:
Primarily renal (as glucuronide and sulfate conjugates), with some biliary excretion.
Unchanged:
<1% (in urine)
Pharmacodynamics
OnsetOfAction:
Within hours for initial systemic levels; symptomatic relief may take days to weeks.
PeakEffect:
Sustained therapeutic levels achieved within 24-48 hours of patch application and maintained throughout the wear period.
DurationOfAction:
Maintained for the duration of patch application (3-4 days for twice-weekly patches).
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 receiving daily oral conjugated estrogens (CE) alone or in combination with medroxyprogesterone acetate (MPA). The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older receiving CE plus MPA or CE alone. These risks should be weighed against the benefits of therapy, especially for long-term use.
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 experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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 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, inform your doctor.
Seek immediate medical attention if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, color changes, or pain in a leg or arm
Trouble speaking or swallowing
In some cases, high calcium levels have occurred in people with cancer taking medications like this one. If you experience signs of high calcium levels, such as:
Weakness
Confusion
Fatigue
Headache
Upset stomach or vomiting
Constipation
Bone pain
contact your doctor right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or may only have mild ones. If you experience any of the following side effects, or if they bother you or do not go away, contact your doctor:
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
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
Changes in sex interest
Irritation at the injection site
This is not an exhaustive list of all 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 immediately:
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 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, inform your doctor.
Seek immediate medical attention if you experience signs of a blood clot, such as:
Chest pain or pressure
Coughing up blood
Shortness of breath
Swelling, warmth, numbness, color changes, or pain in a leg or arm
Trouble speaking or swallowing
In some cases, high calcium levels have occurred in people with cancer taking medications like this one. If you experience signs of high calcium levels, such as:
Weakness
Confusion
Fatigue
Headache
Upset stomach or vomiting
Constipation
Bone pain
contact your doctor right away.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or may only have mild ones. If you experience any of the following side effects, or if they bother you or do not go away, contact your doctor:
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
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
Changes in sex interest
Irritation at the injection site
This is not an exhaustive list of all 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 or migraine
- Sudden vision changes (e.g., partial or complete loss of vision)
- Chest pain, shortness of breath, or coughing up blood
- Pain, swelling, or tenderness in your leg(s)
- Weakness or numbness in your arm or leg, or trouble speaking
- Yellowing of your skin or eyes (jaundice)
- New breast lump or changes in your 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 allergic reaction you experienced, including any symptoms that occurred.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of developing blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential 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 issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of developing blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential 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 issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and if so, they will instruct you on when to resume taking it after the surgery or procedure.
If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), you will need 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 crucial, 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.
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 to use sunscreen and protective clothing and eyewear when outdoors.
This medication may affect certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this drug. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly 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 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 they may require regular growth checks. 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 will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged inactivity may increase your risk of developing blood clots. Additionally, if you have diabetes (high blood sugar), you will need 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 crucial, 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.
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 to use sunscreen and protective clothing and eyewear when outdoors.
This medication may affect certain laboratory tests, so be sure to inform all your healthcare providers and lab personnel that you are taking this drug. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly 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 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 they may require regular growth checks. 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 females)
What to Do:
Remove the patch immediately. Seek medical attention. For severe symptoms or concerns, call Poison Control at 1-800-222-1222.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., Anastrozole, Letrozole, Exemestane) - concurrent use would counteract the effect of the aromatase inhibitor.
- Dasabuvir/Ombitasvir/Paritaprevir/Ritonavir (Viekira Pak) - increased risk of ALT elevations.
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 hormones (e.g., Levothyroxine) - Estrogens can increase thyroid-binding globulin (TBG), potentially increasing thyroid hormone requirements.
- Corticosteroids (e.g., Prednisone) - Estrogens may decrease corticosteroid clearance, leading to increased effects and toxicity.
Moderate Interactions
- Anticoagulants (e.g., Warfarin) - Estrogens may alter the effects of anticoagulants; monitor INR.
- Antidiabetic agents (e.g., Insulin, Metformin) - Estrogens may decrease glucose tolerance; monitor blood glucose.
- Tricyclic antidepressants (e.g., Imipramine) - Estrogens may increase plasma concentrations of TCAs.
- Cyclosporine - Estrogens may increase cyclosporine levels, increasing risk of toxicity.
Minor Interactions
- Not many specific minor interactions with significant clinical impact are consistently reported for transdermal estradiol.
Monitoring
Baseline Monitoring
Complete medical history and physical examination (including blood pressure, breast exam, pelvic exam, Pap test)
Rationale: To identify contraindications, risk factors, and establish baseline health status.
Timing: Prior to initiation of therapy.
Mammogram
Rationale: To screen for breast cancer before starting estrogen therapy.
Timing: Prior to initiation, as per screening guidelines.
Lipid profile
Rationale: Estrogens can affect lipid metabolism; establish baseline.
Timing: Prior to initiation.
Liver function tests (LFTs)
Rationale: To assess hepatic function, especially given hepatic metabolism of estrogens.
Timing: Prior to initiation, especially if hepatic impairment is suspected.
Routine Monitoring
Blood pressure
Frequency: Annually, or more frequently if clinically indicated.
Target: <130/80 mmHg (general target)
Action Threshold: Sustained elevation requiring intervention or discontinuation.
Breast examination
Frequency: Annually by a healthcare provider; monthly self-exam.
Target: Normal findings
Action Threshold: New lumps, pain, nipple discharge, or skin changes warrant immediate investigation.
Mammogram
Frequency: As per national screening guidelines (e.g., annually or biennially for women over 40-50).
Target: Normal findings
Action Threshold: Abnormal findings require further diagnostic workup.
Pelvic examination and Pap test
Frequency: Annually, or as per screening guidelines.
Target: Normal findings
Action Threshold: Abnormal bleeding, pain, or Pap results require investigation.
Symptom assessment (e.g., vasomotor symptoms, vaginal dryness)
Frequency: Regularly (e.g., every 3-6 months initially, then annually).
Target: Improved or resolved symptoms with minimal side effects.
Action Threshold: Persistent or worsening symptoms, or intolerable side effects, warrant dose adjustment or alternative therapy.
Symptom Monitoring
- Unusual vaginal bleeding or spotting (especially postmenopausal)
- New breast lumps or changes
- Severe headache or migraine
- Sudden partial or complete loss of vision
- Sudden onset of severe chest pain, shortness of breath, or coughing up blood (signs of pulmonary embolism)
- Pain, swelling, or tenderness in one or both legs (signs of deep vein thrombosis)
- Weakness or numbness in an arm or leg, slurred speech, sudden confusion (signs of stroke)
- Yellowing of skin or eyes (jaundice), dark urine, light-colored stools (signs of liver problems)
- Severe abdominal pain
Special Patient Groups
Pregnancy
Contraindicated. Estrogen therapy during pregnancy is associated with an increased risk of birth defects and should not be used.
Trimester-Specific Risks:
First Trimester:
Increased risk of congenital anomalies, particularly cardiovascular and limb defects, if used during early pregnancy.
Second Trimester:
Not indicated; continued exposure could lead to adverse fetal effects.
Third Trimester:
Not indicated; continued exposure could lead to adverse fetal effects.
Lactation
Not recommended. Estradiol is excreted in breast milk and may reduce the quantity and quality of breast milk. Potential adverse effects on the breastfed infant are possible.
Infant Risk:
Low to moderate risk. Potential for effects on infant's endocrine system; may cause breast enlargement or feminization in male infants. Primary concern is reduction in milk supply.
Pediatric Use
Not indicated for routine use in pediatric populations. Estrogen therapy in children is reserved for specific conditions (e.g., Turner syndrome, primary ovarian failure) and requires specialized dosing and monitoring by an endocrinologist.
Geriatric Use
Use with caution. Women aged 65 years and older may be at increased risk for stroke, deep vein thrombosis, and probable dementia, especially with long-term use. The lowest effective dose for the shortest duration consistent with treatment goals should be used. Close monitoring for adverse cardiovascular and cognitive events is essential.
Clinical Information
Clinical Pearls
- Transdermal estradiol bypasses first-pass hepatic metabolism, potentially leading to a more favorable lipid profile and lower risk of venous thromboembolism compared to oral estrogens, especially in women with certain risk factors.
- Always co-administer a progestin with estradiol in women with an intact uterus to reduce the risk of endometrial hyperplasia and cancer.
- Patients should be instructed on proper patch application and rotation to maximize absorption and minimize skin irritation.
- Regularly assess the need for continued therapy. Estrogen therapy should be used for the shortest duration consistent with treatment goals.
- Counsel patients on the Black Box Warning regarding cardiovascular events, stroke, breast cancer, and dementia, and discuss individual risks and benefits.
Alternative Therapies
- Other systemic estrogen formulations (oral tablets, gels, sprays, vaginal rings)
- Local vaginal estrogen products (creams, tablets, rings) for isolated vaginal symptoms
- Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like Paroxetine, Venlafaxine; Gabapentin; Clonidine)
- Lifestyle modifications (e.g., diet, exercise, stress reduction) for menopausal symptoms
Cost & Coverage
Average Cost:
Variable, typically $30 - $150 per 8 patches (4-week supply)
Generic Available:
Yes
Insurance Coverage:
Tier 1 (generic) or Tier 2/3 (brand) on most commercial and Medicare Part D plans.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to check with your pharmacist for more information. If you have any questions or concerns about your 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 seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.