Estrace 0.5mg Tablets

Estradiol is a naturally occurring estrogen. It binds to estrogen receptors (ERα and ERβ) in target tissues, forming a complex that interacts with estrogen response elements on DNA. This interaction modulates gene transcription, leading to the synthesis of specific proteins responsible for the physiological effects of estrogens. These effects include the development and maintenance of the female reproductive system and secondary sex characteristics, as well as effects on bone density, lipid metabolism, and the cardiovascular system.

Important Side Effects to Report to Your Doctor Immediately

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, seek medical attention right away:

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 people with cancer, high calcium levels have occurred with 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
inform your doctor right away.

Other Possible Side Effects

Most people do not experience severe side effects, and some may not experience any side effects at all. However, if you experience any of the following side effects, consult 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

This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

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 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 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. Do not initiate, stop, or adjust the dosage of any medication without consulting your doctor first.

Important Warnings and 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 instruct you on when to resume taking it after the surgery or procedure.

If you will be immobile for an extended period, 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 tartrazine (FD&C Yellow No. 5) allergy, consult your doctor, as some products contain this ingredient.

If you have diabetes, closely monitor your blood sugar levels. This medication can cause high blood pressure, so have your blood pressure checked regularly as advised by your doctor.

Regularly undergo blood tests and bone density checks as recommended 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.

This medication can cause elevated triglyceride levels, so inform your doctor if you have a history of high triglyceride levels.

Prolonged use of this medication may lead to the development of dark skin patches on your face. Avoid exposure to sunlight, sunlamps, and tanning beds, and use sunscreen and protective clothing and eyewear when going outside.

This medication may affect certain laboratory test results, so inform all your healthcare providers and laboratory personnel that you are taking this medication.

Refrain from smoking, as it increases the risk of heart disease. Limit your alcohol consumption and consult your doctor if you regularly consume grapefruit juice or eat grapefruit.

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

In rare cases, this medication may affect growth in children and adolescents, 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.

• Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane) - concurrent use would counteract the effect of the aromatase inhibitor.

• 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 decreased free thyroid hormone levels and increased thyroid hormone requirements.
• Corticosteroids (e.g., prednisone) - estrogens may decrease the clearance of corticosteroids, leading to increased pharmacologic and toxic effects.

• Anticoagulants (e.g., warfarin) - estrogens may alter the effects of anticoagulants; monitor INR.
• Hypoglycemic agents (e.g., insulin, oral antidiabetics) - estrogens may impair glucose tolerance; dosage adjustment may be needed.
• Cyclosporine - estrogens may inhibit cyclosporine metabolism, increasing its plasma concentrations and risk of toxicity.
• Lamotrigine - estrogens may decrease lamotrigine plasma concentrations, potentially leading to loss of seizure control.

• Folic acid - estrogens may increase folic acid requirements.
• Vitamin B6 - estrogens may increase vitamin B6 requirements.

• Unusual vaginal bleeding or spotting
• Breast lumps or changes
• Leg pain, swelling, or tenderness (signs of DVT)
• Sudden chest pain, shortness of breath, or coughing up blood (signs of PE)
• Sudden severe headache, vision changes, slurred speech, weakness or numbness in an arm or leg (signs of stroke)
• Chest pain or discomfort, pain radiating to arm, back, neck, jaw, or stomach (signs of MI)
• Yellowing of skin or eyes (jaundice)
• Severe abdominal pain
• Memory loss or cognitive decline

Estradiol is contraindicated during pregnancy. There is no indication for estrogen therapy in pregnancy. Exposure to estrogens during pregnancy has been associated with an increased risk of congenital anomalies in the fetus.

Estradiol is not recommended during lactation. Estrogens are excreted in human milk and may decrease the quantity and quality of breast milk. Potential adverse effects on the nursing infant have not been fully established but could include feminization.

Safety and effectiveness in pediatric patients have not been established, except for the treatment of hypoestrogenism in adolescent females with primary ovarian failure or hypogonadism. Use in children should be carefully considered and monitored by a specialist.

In the WHI study, women 65 years and older treated with CEE alone or CEE plus MPA had a higher risk of stroke and probable dementia compared to placebo. Use the lowest effective dose for the shortest duration. Close monitoring for adverse cardiovascular and cognitive events is recommended.

• Always use the lowest effective dose for the shortest duration consistent with treatment goals and risks.
• For women with an intact uterus, a progestin must be added to estrogen therapy to reduce the risk of endometrial hyperplasia and cancer.
• Estrogen therapy should be re-evaluated periodically (e.g., every 3-6 months) to determine if continued treatment is necessary.
• Counsel patients on the Black Box Warnings regarding cardiovascular events, breast cancer, and dementia.
• Patients should be advised to report any signs of blood clots (e.g., leg pain, chest pain, shortness of breath) or abnormal vaginal bleeding immediately.
• Oral estradiol undergoes significant first-pass metabolism, leading to a lower bioavailability compared to transdermal or vaginal formulations.

• Other oral estrogens (e.g., conjugated estrogens, esterified estrogens)
• Transdermal estradiol patches (e.g., Vivelle-Dot, Climara)
• Estradiol gels or sprays (e.g., Divigel, Elestrin, Evamist)
• Vaginal estradiol (creams, rings, tablets) for localized symptoms (e.g., Estrace Vaginal Cream, Vagifem, Estring)
• Selective Estrogen Receptor Modulators (SERMs) for specific indications (e.g., ospemifene for dyspareunia, raloxifene for osteoporosis prevention)
• 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.

If your symptoms or health issues persist or worsen, it is 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 it's a good idea to check with your pharmacist. 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 detailed information about the overdose, including the medication taken, the amount, and the time it occurred.