Estrace Vaginal Cream 42.5gm

Estradiol is the primary estrogen secreted by the human ovary. It binds to estrogen receptors (ERα and ERβ) in target tissues, including the vagina, uterus, breast, hypothalamus, and pituitary. This binding forms a complex that interacts with DNA, regulating gene expression and protein synthesis. In the vagina, it helps restore the integrity of the vaginal epithelium, increasing superficial cells, reducing parabasal cells, and improving vaginal pH, thereby alleviating symptoms of vulvar and vaginal atrophy.

Urgent 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 notice any of the following symptoms, contact your doctor or seek immediate 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, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of gallbladder problems: pain in the upper right belly area, right shoulder area, or between the shoulder blades, change in stools, dark urine, yellow skin or eyes, or fever with chills.
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 high blood pressure: severe headache or dizziness, passing out, or changes in eyesight.
Signs of pancreatitis (pancreas problem): severe stomach pain, severe back pain, or severe upset stomach or vomiting.
Weakness on one side of the body, trouble speaking or thinking, changes in balance, drooping on one side of the face, or blurred eyesight.
Pelvic pain or pressure, vaginal irritation, vaginal itching or discharge, or abnormal vaginal bleeding.
Breast changes: lump, pain, soreness, or nipple discharge.
Depression or other mood changes, memory problems or loss, eyesight changes or loss, bulging eyes, or changes in how contact lenses feel.
Fluid retention: swelling, weight gain, or trouble breathing.
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.
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 minor ones. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical help:

Headache
Hair loss
Tender breasts
Diarrhea, upset stomach, or vomiting
Stomach pain or cramps
Bloating
* Back pain

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.

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
Any instances of unexplained vaginal bleeding
If you are pregnant or think you may be pregnant. Note that 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 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 have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels. Additionally, follow your doctor's instructions for regular blood work and other laboratory tests.

Regular breast exams and gynecology check-ups are vital, and you should also perform breast self-exams as directed by your doctor.

Be aware that this medication can cause high blood pressure. Your doctor will advise you on how often to have your blood pressure checked.

Elevated triglyceride levels have been associated with this drug. If you have a history of high triglyceride levels, inform your doctor.

This medication may affect the results of certain laboratory tests. Be sure to inform all your healthcare providers and laboratory personnel that you are taking this drug.

Smoking can increase the risk of heart disease, so it is recommended that you do not smoke. Discuss this with your doctor if you need help quitting.

If you consume grapefruit juice or eat grapefruit regularly, consult with your doctor about potential interactions.

If you will be immobile for extended periods, such as during long trips, bedrest after surgery, or illness, discuss this with your doctor, as it may increase your risk of blood clots.

The risk of certain side effects, including heart attack, stroke, breast cancer, ovarian cancer, and others, may vary depending on factors such as 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.

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

If you are breastfeeding, consult with your doctor to discuss any potential risks to your baby.

• None specifically for drug-drug interactions with vaginal cream, but general contraindications for estrogen therapy apply (e.g., undiagnosed abnormal genital bleeding, active DVT/PE, estrogen-dependent neoplasia).

• Aromatase inhibitors (e.g., anastrozole, letrozole, exemestane): May antagonize the effects of estradiol.
• CYP3A4 inducers (e.g., rifampin, carbamazepine, phenobarbital, St. John's Wort): May decrease systemic estradiol levels, potentially reducing efficacy (though less relevant for local action).
• CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin): May increase systemic estradiol levels, potentially increasing systemic side effects (though less relevant for local action).

• Thyroid hormones (e.g., levothyroxine): Estrogens can increase thyroid-binding globulin (TBG), potentially increasing the need for thyroid hormone replacement.
• Corticosteroids (e.g., prednisone): Estrogens may decrease the clearance of corticosteroids, leading to increased pharmacologic effects.
• Warfarin: Estrogens may alter the effects of anticoagulants; monitor INR.

• Not well-defined for estradiol vaginal cream due to low systemic absorption.

• Unusual vaginal bleeding or spotting
• New breast lump or changes in breasts
• Severe headache or migraine
• Vision changes (e.g., sudden partial or complete loss of vision)
• Chest pain, shortness of breath, or coughing up blood
• Pain, swelling, or tenderness in one or both legs (suggestive of DVT)
• Yellowing of skin or eyes (jaundice)
• Severe abdominal pain

Contraindicated during pregnancy (Pregnancy Category X). There is no indication for estrogen therapy in pregnancy, and there is evidence of fetal harm.

Not recommended during lactation (Lactation Risk L4). Estrogens can decrease the quantity and quality of breast milk and may be excreted in breast milk, potentially affecting the nursing infant.

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

Use with caution. Women 65 years of age or older may have an increased risk of stroke and DVT/PE with systemic estrogen therapy. While systemic absorption from vaginal cream is low, the lowest effective dose for the shortest duration should be used. Close monitoring for adverse events is recommended.

• Estrace Vaginal Cream is intended for local treatment of vaginal symptoms of menopause. While systemic absorption is low, it's important to be aware of the Black Box Warnings associated with systemic estrogen therapy.
• Apply the cream at bedtime to allow for maximum absorption and to minimize leakage.
• Use the calibrated applicator provided to ensure accurate dosing.
• Patients should be advised to report any unusual vaginal bleeding, breast changes, or symptoms of blood clots immediately.
• Regular follow-up with a healthcare provider, including annual physical exams and mammograms, is crucial during therapy.

• Non-hormonal vaginal lubricants and moisturizers (e.g., Replens, K-Y Jelly) for symptomatic relief of dryness and dyspareunia.
• Ospemifene (Osphena) - an oral selective estrogen receptor modulator (SERM) for moderate to severe dyspareunia.
• Prasterone (Intrarosa) - a vaginal insert containing DHEA, converted to estrogens and androgens locally.
• Laser therapy (e.g., MonaLisa Touch) for vaginal atrophy (off-label use).

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's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't 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 reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.