Estradiol (Topical)

Estradiol is a form of estrogen, a female sex hormone that regulates many processes in the body.

Some estradiol products placed directly into the vagina are used for "local" treatment of vaginal menopause symptoms involving the secretions and surrounding tissues of the vagina. Other vaginal estradiol products are used for treating menopause symptoms affecting the vagina as well as other parts of the body (such as hot flashes). This type of vaginal estradiol has "systemic" effects, meaning that it can affect parts of the body other than where the medicine is placed or applied.

The information in this leaflet is specific to estradiol vaginal products that are used for local treatment of symptoms. Estradiol vaginal (local) is used to treat vaginal symptoms of menopause such as dryness, burning, and itching.

Estradiol vaginal (local) may also be used for purposes not listed in this medication guide.

You should not use estradiol if you have: liver disease, a bleeding disorder, unusual vaginal bleeding, history of a hormone-dependent cancer (such as breast, uterine, ovarian, or thyroid cancer), or if you have ever had a heart attack, stroke, or a blood clot.

Do not use if you are pregnant.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Call your doctor at once if you have any unusual vaginal bleeding while using this medicine.

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions. Long-term use may also increase your risk of breast cancer or blood clot.

Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment.

You should not use this medicine if you are allergic to estradiol, if you are pregnant, or if you have:

• unusual vaginal bleeding that a doctor has not checked;
• liver disease;
• a bleeding or blood-clotting disorder;
• a recent history of heart attack or stroke;
• a history of hormone-dependent cancer (such as breast, uterine, ovarian, or thyroid cancer); or
• if you have ever had a blood clot (especially in your lung or your lower body).

Estradiol should not be used to prevent heart disease, stroke, or dementia, because this medicine may actually increase your risk of developing these conditions.

To make sure estradiol is safe for you, tell your doctor if you have:

• heart disease;
• risk factors for coronary artery disease (such as diabetes, lupus, smoking, being overweight, having high blood pressure or high cholesterol, having a family history of coronary artery disease, or if you have had a hysterectomy);
• a history of jaundice caused by pregnancy or birth control pills;
• hereditary angioedema (an immune system disorder);
• a thyroid disorder;
• kidney disease;
• asthma;
• epilepsy or other seizure disorder;
• migraines;
• porphyria (a genetic enzyme disorder that causes symptoms affecting the skin or nervous system);
• endometriosis or uterine fibroid tumors;
• gallbladder disease;
• high or low levels of calcium in your blood; or
• if you have had your uterus removed (hysterectomy).

Long-term use of estradiol may increase your risk of breast cancer, heart attack, stroke, or blood clot. Talk with your doctor about your individual risks before using estradiol vaginal long term.

FDA pregnancy category X. Estradiol can harm an unborn baby or cause birth defects. Do not use if you are pregnant. Tell your doctor right away if you become pregnant during treatment. Use effective birth control while you are using this medication.

Estradiol can pass into breast milk. This medication may slow breast milk production. Tell your doctor if you are breast-feeding a baby.

Follow all directions on your prescription label. Do not take this medicine in larger or smaller amounts or for longer than recommended.

Estradiol may increase your risk of developing a condition that may lead to uterine cancer. Your doctor may prescribe a progestin to take while you are using estradiol, to help lower this risk. Report any unusual vaginal bleeding right away.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Wash your hands before and after inserting estradiol vaginal.

You should not be able to feel the vaginal ring once it is in place. Leave the vaginal ring in place for 90 days, then remove it. Your doctor may want you to replace it with a new ring.

Use the applicator provided to measure the prescribed dose of estradiol vaginal cream. Take apart the cream applicator and wash it with mild soap and warm water after each use.

Each estradiol vaginal tablet is supplied in a single-use disposable applicator. Throw the tablet applicator away after one use.

Your doctor should check your progress on a regular basis (every 3 to 6 months) to determine whether you should continue this treatment. Self-examine your breasts for lumps on a monthly basis, and have regular mammograms while using estradiol transdermal.

If you need surgery or medical tests or if you will be on bed rest, you may need to stop using this medicine for a short time. Any doctor or surgeon who treats you should know that you are using estradiol.

Store at room temperature away from moisture and heat. Keep the vaginal ring in its protective pouch until you are ready to use it.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Overdose symptoms may include nausea, vomiting, and vaginal bleeding.

Use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose. Remove the vaginal ring and insert a new one as soon as you remember. Do not use an extra vaginal ring to make up the missed wearing time.

• Estrace
• Estring
• Vagifem
• Yuvafem

• Estrogen Derivative

Angioedema, anaphylactic reaction, or hypersensitivity to estradiol or any component of the formulation; undiagnosed abnormal genital bleeding; DVT or PE (current or history of); active or history of arterial thromboembolic disease (eg, stroke, MI); breast cancer (known, suspected, or history of); estrogen-dependent tumor (known or suspected); hepatic impairment or disease; known protein C, protein S, antithrombin deficiency, or other known thrombophilic disorders; pregnancy.

Canadian labeling: Additional contraindications (not in US labeling): Endometrial hyperplasia; partial or complete loss of vision due to ophthalmic vascular disease; breastfeeding; porphyria.

Documentation of allergenic cross-reactivity for estrogens is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Vaginal cream: Gently insert applicator filled with vaginal cream deeply into vagina. Cleanse applicator after use with warm water and mild soap (do not boil or use hot water).

Vaginal ring: Insert as deeply as possible into the upper one-third of the vagina; exact positioning is not critical for efficacy; however, patient should not feel anything once inserted. In case of discomfort, ring should be gently pushed further into vagina. Straining at defecation may make the ring move down in the lower part of the vagina; if this occurs, push up ring with finger. If ring is expelled prior to 90 days, it may be rinsed in lukewarm water and reinserted. Ensure proper vaginal placement of the ring to avoid inadvertent urinary bladder insertion. If vaginal infection, ulceration, erosion, or adherence to vaginal wall develops, remove ring and reinsert only after healing is complete.

Vaginal tablet: Insert tablet with supplied applicator at the same time each day. Once inserted, press plunger until fully depressed, then remove applicator and discard. If tablet comes out of applicator prior to insertion, do not replace; use a new tablet filled applicator instead. (If the tablet has fallen out of applicator but still remains in the package, it can be reinserted in the applicator for use.)

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience hair loss, cramps, bloating, or dark patches on face. Have patient report immediately to prescriber signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of gallstones (pain in the upper right abdominal area, right shoulder area, or between the shoulder blades; jaundice; or fever with chills), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), angina, shortness of breath, coughing up blood, severe headache, severe dizziness, passing out, severe nausea, vomiting, severe abdominal pain, pelvic pain, severe vaginal irritation, vaginal bleeding, vaginitis, lump in breast, breast soreness or pain, nipple discharge, depression, mood changes, memory impairment, bulging eyes, contact lens discomfort, vision changes, edema, blindness, or signs of toxic shock syndrome (diarrhea, dizziness, passing out, severe muscle pain, nausea, vomiting, or sunburn like rash) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

Commonly reported side effects of estradiol topical include: headache. Other side effects include: limb pain. See below for a comprehensive list of adverse effects.

Vaginal cream:
Initial dose: 2 to 4 grams intravaginally per day for 1 to 2 weeks
Maintenance dose: 1 gram intravaginally 1 to 3 times a week

Vaginal ring:
One vaginal ring should be inserted into the upper third of the vagina

Vaginal tablet:
Initial dose: One tablet inserted into the vagina once a day for two weeks
Maintenance dose: One tablet inserted into the vagina twice weekly

Comments:
-Vaginal cream: The initial dosage should be reduced to 1 to 2 grams intravaginally per day for 1 to 2 weeks.
-Vaginal cream: The number of doses per tube will vary with dosage requirements and patient handling.
-Vaginal ring: The ring should remain continuously in place for 3 months.
-Vaginal ring: If expulsion or removal occurs during a 90 day treatment period, the ring should be rinsed in lukewarm water prior to reinsertion.
-Vaginal ring: Retention of the ring beyond 90 days results in underdosage and loss of efficacy.
-Vaginal tablet: Patients should be started at the 10 mcg dose strength.

Uses:
-Treatment of atrophic vaginitis due to menopause
-Treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause

Data not available