Estrace 1mg Tablets
Overview
What is this medicine?
How to Use This Medicine
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication at the same time every day. Note that there may be days when you are not scheduled to take your medication.
You can take your medication with or without food. If it causes stomach upset, taking it with food may help.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When your medication is no longer needed or has expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Do not smoke while taking this medication, as smoking significantly increases the risk of blood clots, stroke, and heart attack.
- Maintain a healthy diet and engage in regular physical activity.
- Discuss any history of blood clots, heart disease, stroke, or cancer with your doctor before starting this medication.
- Report any unusual vaginal bleeding immediately to your doctor.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Condition-Specific Dosing:
Pediatric Dosing
Dose Adjustments
Renal Impairment:
Hepatic Impairment:
Pharmacology
Mechanism of Action
Pharmacokinetics
Absorption:
Distribution:
Elimination:
Pharmacodynamics
Safety & Warnings
BLACK BOX WARNING
Side Effects
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 immediately or seek emergency medical attention:
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, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach pain or upset, light-colored stools, vomiting, or yellow skin and eyes
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, yellow skin and eyes, fever with chills, bloating, or severe stomach upset or vomiting
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe stomach upset or vomiting
Signs of high blood pressure: severe headache or dizziness, fainting, or changes in vision
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision
Changes in vision or loss of vision, bulging eyes, or changes in how contact lenses feel
Breast lump, breast pain or tenderness, or 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
Swelling or fluid retention in the body (tell your doctor if you experience swelling, weight gain, or breathing difficulties)
Additional Serious Side Effects
Blood clots: chest pain or pressure, coughing up blood, shortness of breath, swelling, warmth, numbness, color changes, or pain in a leg or arm, or difficulty speaking or swallowing
High calcium levels (more common in people with cancer): weakness, confusion, fatigue, headache, stomach upset or vomiting, constipation, or bone pain
Common Side Effects
Most people do not experience severe side effects, but some may have mild or moderate side effects. If you experience any of the following, contact your doctor if they bother you or do not go away:
Dizziness or headache
Hair loss
Stomach upset 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 drive
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden chest pain or shortness of breath
- Sudden severe headache or migraine
- Sudden vision changes (e.g., partial or complete loss of vision)
- Numbness or weakness in an arm or leg, especially on one side of the body
- Slurred speech
- Severe pain, swelling, or redness in your leg (especially calf)
- Yellowing of your skin or eyes (jaundice)
- Lump in your breast
- Unusual vaginal bleeding or spotting after menopause
Before Using This Medicine
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 estrogen-dependent
Unexplained vaginal bleeding
Pregnancy or potential pregnancy. Note: This medication is contraindicated during pregnancy and should not be taken if you are pregnant.
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. Do not initiate, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Your doctor may advise you to stop taking this drug before certain surgical procedures, and will provide guidance on when to resume taking it after the surgery or procedure.
If you 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 a known allergy to tartrazine (FD&C Yellow No. 5), consult your doctor, as some products contain this ingredient.
If you have diabetes, it is crucial to closely monitor your blood sugar levels. This medication may cause high blood pressure, so regular blood pressure checks are necessary, as advised by your doctor.
Regular blood tests and bone density checks are also recommended, as directed by your doctor. Additionally, schedule regular breast exams and gynecology check-ups, and 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, so inform your doctor if you have a history of elevated triglyceride levels.
This medication may cause dark skin patches on the 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. Consult your doctor for guidance on quitting.
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. Follow the diet and exercise plan recommended by your doctor.
In rare cases, this medication may affect growth in children and teenagers, so regular growth checks may be necessary. Consult your doctor if you have concerns.
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:
There is no specific antidote. Treatment is symptomatic and supportive. In case of suspected overdose, contact a poison control center (1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Contraindicated Interactions
- Aromatase inhibitors (e.g., anastrozole, letrozole) - concurrent use would counteract the effect of the aromatase inhibitor.
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, potentially increasing thyroid hormone requirements.
- Warfarin - estrogens may alter the effects of anticoagulants; monitor INR closely.
Moderate Interactions
- Corticosteroids (e.g., prednisone) - 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.
- Fluvoxamine - may increase estradiol levels.
Minor Interactions
- Not readily available for minor interactions with significant clinical impact.
Monitoring
Baseline Monitoring
Rationale: To identify contraindications, risk factors for cardiovascular disease, breast cancer, and endometrial cancer.
Timing: Prior to initiation of therapy.
Rationale: Estrogens can affect lipid metabolism; baseline assessment is important.
Timing: Prior to initiation of therapy.
Rationale: To assess hepatic function, as estradiol is extensively metabolized by the liver.
Timing: Prior to initiation of therapy.
Routine Monitoring
Frequency: Annually, or as clinically indicated.
Target: Normal for age and health status.
Action Threshold: Abnormal findings (e.g., new breast lump, abnormal bleeding) require immediate investigation.
Frequency: As recommended by national guidelines (e.g., annually or biennially for women over 40-50).
Target: Normal findings.
Action Threshold: Suspicious findings require further diagnostic evaluation.
Frequency: Regularly, at least annually.
Target: <130/80 mmHg (or as per individual goals).
Action Threshold: Sustained elevation requires evaluation and management.
Frequency: Ongoing patient education and self-monitoring.
Target: Absence of symptoms.
Action Threshold: New onset of leg pain/swelling, chest pain, shortness of breath, sudden severe headache, visual disturbances, or speech changes require immediate medical attention.
Symptom Monitoring
- Unusual vaginal bleeding or spotting
- Breast lumps or changes
- Calf pain, swelling, or tenderness (signs of DVT)
- Sudden severe headache
- Chest pain or shortness of breath
- Sudden vision changes
- Slurred speech or weakness/numbness on one side of the body
- Yellowing of skin or eyes (jaundice)
- Severe abdominal pain
Special Patient Groups
Pregnancy
Contraindicated during pregnancy. There is no indication for estrogen therapy during pregnancy, and there is evidence of potential harm to the fetus (e.g., genital abnormalities in female fetuses exposed to diethylstilbestrol (DES)).
Trimester-Specific Risks:
Lactation
Not recommended during lactation. Estrogens are excreted in breast milk and may reduce the quantity and quality of breast milk. Potential adverse effects on the breastfed infant are not fully established but include possible effects on infant development.
Pediatric Use
Generally not indicated for pediatric use, except in specific cases of hypoestrogenism due to primary ovarian failure or hypogonadism, where dosing is carefully individualized by a specialist. Safety and efficacy in prepubertal children for other indications have not been established.
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 conjugated estrogens plus medroxyprogesterone acetate or conjugated estrogens alone. Increased risk of stroke and VTE also observed. Use the lowest effective dose for the shortest duration consistent with treatment goals and risks.
Clinical Information
Clinical Pearls
- Always use the lowest effective dose for the shortest duration consistent with treatment goals and risks, especially for menopausal symptom management.
- For women with an intact uterus, estradiol must be prescribed with a progestin to reduce the risk of endometrial hyperplasia and cancer.
- Patients should be advised to report any unusual vaginal bleeding, breast lumps, or symptoms of blood clots (e.g., leg pain, chest pain, sudden shortness of breath) immediately.
- Regular follow-up appointments, including annual physical exams and mammograms, are crucial during estrogen therapy.
- Smoking is a major contraindication due to significantly increased cardiovascular risks.
- Oral estradiol undergoes significant first-pass metabolism; transdermal or vaginal formulations may be preferred in some cases to avoid this.
Alternative Therapies
- Other estrogen formulations (transdermal patch, gel, spray, vaginal ring, vaginal cream, vaginal tablet)
- Selective Estrogen Receptor Modulators (SERMs) (e.g., ospemifene for dyspareunia, bazedoxifene/conjugated estrogens for vasomotor symptoms and osteoporosis)
- 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)