Elestrin 0.06% Gel Pump 2 X 26gm

Manufacturer MYLAN SPECIALTY L.P. Active Ingredient Estradiol Gel (Elestrin)(es tra DYE ole) Pronunciation ES-tra-DYE-ole
WARNING: All products: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.Skin gel and spray:Do not let another person or a pet touch this drug or the treated part of your skin. If they do, wash their skin with soap and water. If you notice any signs that others may have been in contact with the treated area by accident, call the doctor. This may include signs of unusual sexual development like breast changes in children. @ COMMON USES: It is used to prevent or lower the signs of the change of life (menopause).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
Dec 2006
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Elestrin gel is a form of estrogen hormone that you apply to your skin. It's used to help relieve symptoms of menopause, such as hot flashes and vaginal dryness. If you still have your uterus, your doctor will also prescribe a progestin to protect your uterus.
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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 accompanying information carefully. It is essential to use this medication as directed.

Application Instructions

Apply this medication only to your skin, as directed. Do not ingest it.
Avoid getting the medication in your mouth, nose, or eyes, as it may cause irritation or 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.
Apply the medication to clean, dry, and healthy skin on your upper arm and shoulder. Some products may have specific application areas, so be sure to follow the package insert instructions for guidance.
Do not apply the medication to skin with any problems, such as cuts, wounds, or irritations.
Avoid applying the medication to your face, breast, or vagina.

Precautions and Safety Measures

Before using the pump for the first time, prime it according to the manufacturer's instructions.
Avoid exposure to fire, flames, or smoking until the medication is completely dry on your skin.
Allow the medication to dry completely before covering the area with clothing.
Do not bathe, shower, or swim for at least 2 hours after applying the medication.

Storage and Disposal

Store the medication at room temperature in a dry place, away from bathrooms and heat sources.
Protect the medication from heat and open flames.
If using a pump, discard any unused medication after the labeled number of doses has been reached.

Missed Dose Instructions

If you miss a dose, apply it as soon as you remember.
However, if it is almost time for your next scheduled dose (less than 12 hours), skip the missed dose and resume your regular application schedule.
* Do not apply two doses at once or use extra doses to make up for a missed dose.
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Lifestyle & Tips

  • Apply the gel to clean, dry skin on one arm from the wrist to the shoulder. Do not apply to breasts or irritated skin.
  • Allow the gel to dry for at least 5 minutes before dressing.
  • Avoid contact with the application site by others for at least one hour after application.
  • Wash hands thoroughly after application.
  • Do not apply to skin that is broken or irritated.
  • Avoid smoking, as it increases the risk of serious side effects like blood clots.
  • Maintain a healthy diet and regular exercise.
  • Attend all scheduled doctor appointments and screenings (e.g., mammograms, pelvic exams).
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: 1 pump actuation (0.75 mg estradiol) applied once daily to the skin of one arm from the wrist to the shoulder.
Dose Range: 0.75 - 1.5 mg

Condition-Specific Dosing:

vasomotorSymptoms: Initial dose: 0.75 mg (1 pump actuation) once daily. May be adjusted to 1.5 mg (2 pump actuations) once daily based on clinical response. For women with a uterus, a progestin should be added to reduce the risk of endometrial cancer.
vulvarAndVaginalAtrophy: Initial dose: 0.75 mg (1 pump actuation) once daily. May be adjusted to 1.5 mg (2 pump actuations) once daily based on clinical response. For women with a uterus, a progestin should be added to reduce the risk of endometrial cancer.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established
Adolescent: Not established (Not indicated for pediatric use for hormone replacement therapy)
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Dose Adjustments

Renal Impairment:

Mild: No specific dosage adjustment recommended, but use with caution.
Moderate: No specific dosage adjustment recommended, but use with caution.
Severe: No specific dosage adjustment recommended, but use with caution. Monitor for adverse effects.
Dialysis: Not specifically studied. Use with caution and monitor for adverse effects.

Hepatic Impairment:

Mild: Use with caution. Estrogens are extensively metabolized by the liver.
Moderate: Use with caution. Estrogens are extensively metabolized by the liver. Consider lower starting dose and close monitoring.
Severe: Contraindicated in severe hepatic impairment due to impaired metabolism and increased risk of adverse effects.
Confidence: Medium

Pharmacology

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Mechanism of Action

Estradiol is the primary estrogen produced by the human ovary. It binds to and activates estrogen receptors (ERΞ± and ERΞ²) in target tissues, forming a complex that interacts with DNA to regulate gene expression. This leads to the physiological effects of estrogens, including effects on the reproductive system, bone, cardiovascular system, and central nervous system. In menopausal women, it replaces declining endogenous estrogen levels to alleviate symptoms.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 80% (transdermal, relative to oral), avoids first-pass metabolism.
Tmax: Approximately 2-4 hours after transdermal application.
FoodEffect: Not applicable for transdermal gel.

Distribution:

Vd: Approximately 1.2 L/kg (for estradiol)
ProteinBinding: Approximately 98% (primarily to sex hormone-binding globulin [SHBG] and albumin).
CnssPenetration: Yes, estradiol crosses the blood-brain barrier.

Elimination:

HalfLife: Approximately 1-2 hours (for estradiol itself, but effective half-life for transdermal is longer due to reservoir effect in skin, leading to sustained release).
Clearance: High systemic clearance.
ExcretionRoute: Primarily renal (as glucuronide and sulfate conjugates), with some biliary excretion.
Unchanged: Very small percentage.
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Pharmacodynamics

OnsetOfAction: Symptomatic relief may begin within weeks.
PeakEffect: Full therapeutic effect may take several weeks to months.
DurationOfAction: Sustained release over 24 hours with daily application.

Safety & Warnings

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BLACK BOX WARNING

Estrogens and estrogen plus progestin therapies should not be used for the prevention of cardiovascular disease or dementia. The Women's Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50-79 years of age) 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 relative to placebo. 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. There is an increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens. Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurrent abnormal vaginal bleeding.
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Side Effects

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, yellow skin or eyes, fever with chills, bloating, or severe upset stomach or vomiting
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting
Signs of high blood pressure: severe headache or dizziness, passing out, or changes in eyesight
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight
Eyesight changes or loss, bulging eyes, or changes in how contact lenses feel
Breast lump, breast pain or soreness, or nipple discharge
Vaginal itching or discharge
Abnormal vaginal bleeding
Depression or other mood changes
Memory problems or loss
Fever
Difficulty urinating or changes in urine output
Pain while urinating

This medication may cause fluid retention or swelling in the body. Inform your doctor if you experience swelling, weight gain, or trouble breathing.

Blood Clots and High Calcium Levels

Seek medical attention immediately if you experience:

Signs of a blood clot: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, changes in color, or pain in a leg or arm, or trouble speaking or swallowing
Signs of high calcium levels: weakness, confusion, fatigue, headache, upset stomach or vomiting, constipation, or bone pain (especially in people with cancer)

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people may not experience any side effects or only mild ones. However, if you notice any of the following side effects or if they persist or bother you, contact your doctor:

Dizziness or headache
Hair loss
Upset stomach or vomiting
Constipation
Stomach pain or cramps
Bloating
Enlarged breasts
Tender breasts
Vaginal bleeding or spotting
Painful periods
Common cold symptoms
Nose or throat irritation
Weight gain or loss
Joint pain
Leg cramps
* Changes in sex interest

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Sudden severe headache, dizziness, or fainting
  • Sudden vision changes (e.g., partial or complete loss of vision)
  • Chest pain or heaviness, pain spreading to arm or shoulder, nausea, sweating, general ill feeling
  • Sudden cough, wheezing, rapid breathing, coughing up blood
  • Pain, swelling, warmth, or redness in one or both legs
  • Unusual vaginal bleeding or spotting after menopause
  • Lump in your breast
  • Yellowing of your skin or eyes (jaundice)
  • Severe stomach pain
  • Memory problems or confusion (especially if over 65)
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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, such as foods or drugs. Be sure to describe the allergic reaction you experienced.
A history of certain health conditions, including:
+ Bleeding disorders
+ Blood clots or an increased risk of blood clots
+ Breast cancer
+ Liver problems or liver tumors
+ Heart attack
+ Stroke
+ Tumors that are sensitive to estrogen
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: 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 consulting your doctor first.
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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, consult with your doctor, as this may increase your risk of developing blood clots. Additionally, if you have diabetes, it is crucial to closely monitor your blood sugar levels.

This medication may cause high blood pressure, so it is essential to have your blood pressure checked regularly, as advised by your doctor. 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, 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, so inform your doctor if you have a history of elevated triglyceride levels. This drug may also 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 interfere with certain laboratory tests, so inform all your healthcare providers and lab personnel that you are taking this drug. Smoking increases the 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, consult with your doctor.

In some cases, this medication may affect growth in children and teenagers, so they may require regular growth checks. Consult with your doctor before using other medications or skin products, including soaps. When using the gel form of this medication, avoid applying sunscreen before or soon after application, and do not use sunscreen on the treated area for 7 consecutive days.

If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. If you are breastfeeding, discuss the potential risks to your baby with your doctor.
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Overdose Information

Overdose Symptoms:

  • Nausea
  • Vomiting
  • Breast tenderness
  • Abdominal pain
  • Drowsiness/fatigue
  • Withdrawal bleeding in women

What to Do:

Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is generally supportive; there is no specific antidote.

Drug Interactions

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Contraindicated Interactions

  • Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use would counteract their mechanism of action in breast cancer treatment.
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Major Interactions

  • CYP3A4 inducers (e.g., carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) - may decrease estradiol levels, reducing efficacy.
  • CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir, grapefruit juice) - may increase estradiol levels, increasing risk of adverse effects.
  • Thyroid hormone replacement therapy (e.g., levothyroxine) - estrogens can increase thyroid-binding globulin (TBG), leading to increased thyroid hormone requirements.
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Moderate Interactions

  • Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased effects.
  • Warfarin - estrogens may decrease the anticoagulant effect of warfarin; monitor INR.
  • Folic acid - estrogens may increase folic acid requirements.
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Minor Interactions

  • Not specifically noted for minor interactions with significant clinical impact for transdermal estradiol.

Monitoring

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Baseline Monitoring

Complete medical history and physical examination (including blood pressure, breast exam, pelvic exam, Pap test)

Rationale: To identify contraindications, risk factors for cardiovascular disease, breast cancer, and endometrial cancer.

Timing: Prior to initiation of therapy.

Lipid profile

Rationale: Estrogens can affect lipid metabolism.

Timing: Prior to initiation of therapy.

Liver function tests

Rationale: Estrogens are metabolized by the liver; assess baseline hepatic function.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Annual physical examination (including blood pressure, breast exam, pelvic exam)

Frequency: Annually

Target: Normal for age and health status

Action Threshold: Abnormal findings require further investigation (e.g., new breast lump, abnormal bleeding, significant BP elevation).

Mammography

Frequency: As clinically indicated, based on age and risk factors (e.g., every 1-2 years)

Target: No suspicious findings

Action Threshold: Suspicious findings require further diagnostic workup.

Blood pressure

Frequency: Regularly (e.g., every 3-6 months or as clinically indicated)

Target: <130/80 mmHg

Action Threshold: Sustained elevation (e.g., >140/90 mmHg) may require dose adjustment or discontinuation.

Symptoms of VTE, stroke, MI, endometrial cancer

Frequency: Ongoing patient education and inquiry at each visit

Target: Absence of symptoms

Action Threshold: Presence of symptoms requires immediate medical evaluation.

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Symptom Monitoring

  • Unusual vaginal bleeding or spotting
  • Breast lumps or changes
  • Chest pain, shortness of breath, sudden severe headache
  • Sudden vision changes
  • Pain, swelling, or tenderness in one leg
  • Yellowing of skin or eyes (jaundice)
  • Severe abdominal pain
  • Memory loss or confusion (in older women)

Special Patient Groups

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Pregnancy

Contraindicated during 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 indicated; continued exposure may pose risks.
Third Trimester: Not indicated; continued exposure may pose risks.
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Lactation

Contraindicated during lactation. Estrogens are excreted in breast milk and can reduce the quantity and quality of breast milk. Potential adverse effects on the nursing infant are also a concern.

Infant Risk: High (L4 - Possibly hazardous; L5 - Contraindicated by some sources due to milk suppression and potential infant exposure).
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Pediatric Use

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

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Geriatric Use

Increased risk of probable dementia in women 65 years of age or older. Use the lowest effective dose for the shortest duration. Close monitoring for cardiovascular events and dementia is recommended.

Clinical Information

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Clinical Pearls

  • Elestrin gel should be applied to a clean, dry, intact area of skin on one arm from the wrist to the shoulder. Do not apply to breasts or face.
  • Ensure the gel is completely dry before dressing or allowing skin-to-skin contact with others to prevent transfer.
  • For women with a uterus, a progestin must be co-administered to reduce the risk of endometrial hyperplasia and cancer.
  • Patients should be educated on the signs and symptoms of serious adverse events, particularly blood clots (DVT, PE, stroke, MI), and instructed to seek immediate medical attention if they occur.
  • Regular follow-up, including annual physical exams and mammograms, is crucial for women on HRT.
  • Consider the patient's individual risk factors for cardiovascular disease, breast cancer, and VTE before initiating and during therapy.
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Alternative Therapies

  • Other hormone replacement therapies (e.g., conjugated estrogens, synthetic estrogens)
  • Non-hormonal therapies for vasomotor symptoms (e.g., SSRIs/SNRIs like paroxetine, venlafaxine; gabapentin; clonidine)
  • Lifestyle modifications (e.g., diet, exercise, avoiding triggers for hot flashes)
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Cost & Coverage

Average Cost: Varies widely, typically $100-$300+ per 2 x 26gm pump
Generic Available: Yes
Insurance Coverage: Tier 2 or 3 (Brand), Tier 1 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.