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Estradiol 0.025mg Patch (once Wk)

Manufacturer MYLAN Active Ingredient Estradiol Transdermal Weekly Patch(es tra DYE ole) Pronunciation es-tra-DYE-ole
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.
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Drug Class
Estrogen
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Pharmacologic Class
Estrogen receptor agonist
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Pregnancy Category
Category X
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Estradiol is a type of estrogen, a female hormone. This patch is used to replace the estrogen your body no longer makes after menopause. It helps relieve symptoms like hot flashes and vaginal dryness, and can help prevent bone thinning (osteoporosis). The patch is applied to your skin and changed once a week.
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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.

Administration

Do not take this medication by mouth. It is for skin use only.
 Avoid getting the medication 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.

Preparation and Application

 Wash your hands before and after handling the patch to ensure cleanliness.
Choose a clean, dry, and healthy area of skin on your lower belly or upper buttocks for patch application.
 Rotate the patch site with each new application to avoid skin irritation.
Wait at least 7 days before applying a new patch to the same site.
 Avoid applying the patch to skin with problems, such as cuts, wounds, or irritation.
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 to the waistline or areas that may cause the patch to come off when sitting.

Patch Handling and Disposal

 Do not cut or divide patches, as this may affect their efficacy.
Do not use damaged patches, as they may not work properly.
 If the patch falls off, reapply it to the same site. If it cannot be reapplied, attach a new patch to a different area.
Wear only one patch at a time to avoid overdose.
 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 the 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.
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Lifestyle & Tips

  • Apply the patch to a clean, dry, hairless area of skin on your lower abdomen or buttocks. Do not apply to breasts or waistline.
  • Rotate application sites to avoid skin irritation. Allow at least one week between applications to the same site.
  • Avoid applying lotions, oils, or powders to the skin area where the patch will be applied.
  • If the patch falls off, reapply it or apply a new patch. If it's close to your next scheduled change, wait and apply a new patch at that time.
  • Do not use this medication to prevent heart disease, stroke, or dementia.
  • Discuss with your doctor if you have a uterus, as you may need to take another hormone (progestin) to protect your uterus.
  • Maintain a healthy lifestyle, including regular exercise and a balanced diet.
  • Quit smoking, as smoking increases the risk of serious cardiovascular side effects with estrogen therapy.
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Available Forms & Alternatives

Available Strengths:

Dosing & Administration

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Adult Dosing

Standard Dose: Apply one 0.025 mg/day patch transdermally once weekly. Replace the patch every 7 days.
Dose Range: 0.025 - 0.1 mg

Condition-Specific Dosing:

vasomotorSymptoms: Initial dose often 0.025 mg/day, adjusted based on response and tolerability. If uterus intact, progestin must be co-administered.
preventionOfPostmenopausalOsteoporosis: 0.025 mg/day is the lowest effective dose for this indication. If uterus intact, progestin must be co-administered.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (not indicated for pediatric use)
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Dose Adjustments

Renal Impairment:

Mild: No specific dose adjustment recommended.
Moderate: No specific dose adjustment recommended.
Severe: Use with caution; monitor for adverse effects. No specific dose adjustment recommended.
Dialysis: Not available

Hepatic Impairment:

Mild: Use with caution; monitor for adverse effects. No specific dose adjustment recommended.
Moderate: Use with caution; monitor for adverse effects. Consider lower doses or alternative therapies.
Severe: Contraindicated in severe hepatic dysfunction or disease.
Confidence: Medium

Pharmacology

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Mechanism of Action

Estradiol is the primary estrogen secreted by the human ovary. It binds to nuclear estrogen receptors in estrogen-responsive tissues (e.g., female genital tract, breast, hypothalamus, pituitary), forming a complex that interacts with DNA to modulate gene expression. This leads to the physiological effects of estrogens, including the alleviation of menopausal symptoms and maintenance of bone density.
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Pharmacokinetics

Absorption:

Bioavailability: Variable, generally good transdermal absorption, bypassing first-pass hepatic metabolism.
Tmax: Approximately 1-2 days (for steady-state plasma concentrations after patch application).
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 (therapeutic effects are primarily peripheral, though some central effects related to vasomotor symptoms occur).

Elimination:

HalfLife: Approximately 1-2 days (for transdermal estradiol, reflecting sustained release from patch).
Clearance: Not readily quantifiable for transdermal due to continuous absorption.
ExcretionRoute: Primarily renal (as glucuronide and sulfate conjugates); small amount via bile/feces.
Unchanged: Negligible amount excreted unchanged.
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Pharmacodynamics

OnsetOfAction: Days to weeks for symptomatic relief (e.g., hot flashes).
PeakEffect: Steady-state plasma concentrations typically achieved within 1-2 days of patch application, with clinical peak effect for symptom relief often observed within a few weeks.
DurationOfAction: Maintained for 7 days while the patch is worn.

Safety & Warnings

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BLACK BOX WARNING

Estrogen-alone therapy and Estrogen plus Progestin therapy should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported increased risks of stroke, deep vein thrombosis (DVT), pulmonary embolism (PE), and myocardial infarction (MI) with estrogen plus progestin therapy. The WHI study also reported an increased risk of invasive breast cancer with estrogen plus progestin therapy. The WHI Memory Study (WHIMS) reported an increased risk of probable dementia in postmenopausal women 65 years of age or older. Estrogen-alone therapy has been associated with an increased risk of endometrial cancer in women with a uterus.
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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 or pain
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, 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. Contact your doctor 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 few or no side effects. 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

Reporting Side Effects

If you have questions about side effects or experience any side effects not listed here, 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.
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Seek Immediate Medical Attention If You Experience:

  • Sudden chest pain or shortness of breath
  • Sudden severe headache or dizziness
  • Sudden vision changes (e.g., partial or complete loss of vision)
  • Pain, swelling, or redness in one leg
  • Yellowing of skin or eyes (jaundice)
  • Undiagnosed abnormal vaginal bleeding
  • Lump in your breast
  • Severe abdominal pain
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
 A history of certain health conditions, such as:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
 Pregnancy or suspected pregnancy. Note: This medication should not be taken during pregnancy.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.

If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as prolonged immobility may increase your risk of developing blood clots. If you have diabetes, it is crucial to closely monitor your blood sugar levels.

Be aware that medications like this one can cause high blood pressure. Follow your doctor's instructions for regular blood pressure checks. Additionally, have your blood work and bone density checked as recommended by your doctor.

Regular breast exams, gynecology check-ups, and breast self-exams, as instructed by your doctor, are vital. The risk of certain side effects, such as heart attack, stroke, breast cancer, and ovarian cancer, may vary depending on factors like the duration of estrogen use, whether it is taken with or without a progestin, and other individual factors. Discuss the benefits and risks of using this medication with your doctor.

High triglyceride levels have been associated with this medication. If you have a history of high triglyceride levels, inform your doctor. This drug may cause dark skin patches on your face, so it is essential to avoid sun exposure, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear.

This medication may affect certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug. Avoid smoking, as it increases the risk of heart disease, and limit your alcohol consumption. If you regularly consume grapefruit juice or eat grapefruit, discuss this with your doctor.

For optimal effectiveness, use this medication in conjunction with calcium and vitamin D supplements and engage in weight-bearing exercises, such as walking or physical therapy, as recommended by your doctor. Adhere to the diet and exercise plan prescribed 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.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Breast tenderness
  • Abdominal pain
  • Drowsiness/fatigue
  • Withdrawal bleeding (in women with a uterus)

What to Do:

Remove the patch. There is no specific antidote. Treatment is symptomatic and supportive. Contact your poison control center (1-800-222-1222) or seek immediate medical attention.

Drug Interactions

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Contraindicated Interactions

  • Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use is generally contraindicated as estrogens counteract their effect.
  • Drugs that induce severe hepatic impairment (if patient has pre-existing liver disease).
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Major Interactions

  • CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol plasma concentrations, reducing therapeutic effect.
  • CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may increase estradiol plasma concentrations, potentially increasing adverse effects.
  • Thyroid hormone replacement therapy (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin (TBG), potentially increasing thyroid hormone requirements.
  • Anticoagulants (e.g., warfarin) - estrogens may affect coagulation factors, potentially altering anticoagulant effect. Close monitoring of INR is recommended.
  • Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased corticosteroid levels and effects.
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Moderate Interactions

  • Cyclosporine - estrogens may inhibit the metabolism of cyclosporine, leading to increased cyclosporine plasma concentrations and potential toxicity.
  • Theophylline - estrogens may decrease the clearance of theophylline, leading to increased theophylline levels and potential toxicity.
  • Folic acid - high doses of folic acid may reduce estrogen levels (less significant for transdermal).
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Minor Interactions

  • Not many specific minor interactions are clinically significant for transdermal estradiol.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination

Rationale: To identify contraindications, risk factors (e.g., cardiovascular disease, breast cancer), and establish baseline health status.

Timing: Prior to initiation of therapy.

Blood pressure

Rationale: Estrogens can cause fluid retention and may affect blood pressure.

Timing: Prior to initiation of therapy.

Breast examination and mammography

Rationale: To screen for breast cancer, as estrogen therapy can increase breast cancer risk.

Timing: Prior to initiation of therapy, as per established guidelines.

Pelvic examination (including Pap test if indicated)

Rationale: To screen for gynecological conditions and establish baseline endometrial status (if uterus intact).

Timing: Prior to initiation of therapy.

Lipid profile

Rationale: Estrogens can affect lipid metabolism.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Annual physical examination

Frequency: Annually

Target: Normal

Action Threshold: Any significant changes or new symptoms warrant further investigation.

Blood pressure

Frequency: Annually or more frequently if clinically indicated.

Target: Normal for patient

Action Threshold: Sustained elevation or significant changes.

Breast examination and mammography

Frequency: Annually (breast exam); mammography as per national guidelines (e.g., every 1-2 years for women over 40-50).

Target: Normal

Action Threshold: New lumps, pain, discharge, or abnormal mammogram findings.

Pelvic examination

Frequency: Annually or as clinically indicated.

Target: Normal

Action Threshold: Abnormal findings, new symptoms.

Endometrial monitoring (if uterus intact)

Frequency: As clinically indicated (e.g., if abnormal vaginal bleeding occurs).

Target: Normal endometrial stripe

Action Threshold: Undiagnosed persistent or recurrent abnormal genital bleeding requires evaluation to rule out endometrial malignancy.

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Symptom Monitoring

  • Resolution of menopausal symptoms (e.g., hot flashes, night sweats, vaginal dryness)
  • Signs of thromboembolic events (e.g., chest pain, shortness of breath, sudden severe headache, leg pain/swelling)
  • Breast changes (e.g., lumps, tenderness, discharge)
  • Abnormal vaginal bleeding
  • Signs of liver dysfunction (e.g., jaundice, abdominal pain)
  • Mood changes or depression

Special Patient Groups

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Pregnancy

Contraindicated in pregnancy. 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.
Second Trimester: Not applicable, contraindicated.
Third Trimester: Not applicable, contraindicated.
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Lactation

Not recommended during lactation. Estrogens can decrease the quantity and quality of breast milk and are excreted in breast milk, potentially affecting the infant.

Infant Risk: Low risk of direct harm to infant from small amounts excreted, but potential for decreased milk supply and possible effects on infant's endocrine system. Use generally avoided.
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Pediatric Use

Not indicated for use in pediatric patients. Safety and efficacy have not been established.

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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 receiving estrogen plus progestin therapy. Use the lowest effective dose for the shortest duration. Monitor closely for adverse cardiovascular events.

Clinical Information

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Clinical Pearls

  • Transdermal estradiol bypasses first-pass hepatic metabolism, potentially leading to a more favorable lipid profile and less impact on clotting factors compared to oral estrogens.
  • Always co-administer a progestin with estradiol therapy if the patient has an intact uterus to reduce the risk of endometrial hyperplasia and cancer.
  • Advise patients to apply the patch to a clean, dry, hairless area of the trunk (lower abdomen or buttocks) and to rotate sites to prevent skin irritation.
  • Emphasize the importance of regular follow-up appointments, including breast exams and mammograms, due to the black box warnings.
  • Educate patients on the signs and symptoms of serious adverse events, such as blood clots, stroke, and heart attack, and when to seek immediate medical attention.
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Alternative Therapies

  • Other forms of estrogen therapy (oral tablets, vaginal rings, gels, sprays)
  • Selective Estrogen Receptor Modulators (SERMs) for specific indications (e.g., ospemifene for dyspareunia, bazedoxifene/conjugated estrogens for vasomotor symptoms and osteoporosis prevention)
  • Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
  • Bisphosphonates or other anti-resorptive agents for osteoporosis prevention.
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Cost & Coverage

Average Cost: $50 - $200+ per 4 patches (1 month supply)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (generics often Tier 1, brands Tier 2 or 3)
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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 consult with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.