How does this medication work? What will it do for me?

Estradiol vaginal tablets belong to the class of medications known as local estrogen replacement therapy. Estradiol is a type of estrogen, a hormone that is produced by the ovaries. This medication is used to treat vaginal atrophy (shrinkage and dryness of tissues in the vagina) caused by low estrogen levels in the body (due to menopause).

At menopause, the amount of estrogen made by the ovaries declines and symptoms such as vaginal atrophy can occur. When an estradiol vaginal tablet is inserted into the vagina, it releases estradiol, which helps to make vaginal tissues thicker and more supple. An improvement in symptoms usually occurs after 2 to 3 weeks of treatment.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are using this medication, speak to your doctor. Do not stop using this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

What form(s) does this medication come in?

10 µg
Each small, white, film-coated vaginal tablet contains 10 µg of estradiol. Nonmedicinal ingredients: hypromellose, lactose monohydrate, maize starch, magnesium stearate, and polyethylene glycol 6000.

How should I use this medication?

The usual dose is 1 tablet inserted into the vagina once daily for 2 weeks, then 1 tablet twice weekly after the first 2 weeks.

Using the applicator supplied, insert estradiol vaginal tablets gently into the vagina as follows:

  • Remove the plastic wrap from the applicator.
  • Insert the end of the applicator with the vaginal tablet as high into the vagina as it can comfortably go without forcing it.
  • Gently press the plunger until you hear a click. This means the tablet has been released from the applicator.
  • Remove the applicator from the vagina and discard it. Applicators are intended for a single use only.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are using the medication without consulting your doctor.

It is important to use this medication exactly as prescribed by your doctor. If you miss a dose, use it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not use a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature in a dry place, protect it from light and moisture, and keep it out of the reach of children. Store the medication in its original package.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take this medication if you:

  • are allergic to estradiol or any ingredients of this medication
  • are breast-feeding
  • are or may be pregnant
  • have a metabolic condition known as porphyria
  • have active liver disease or liver dysfunction, with abnormal liver function test results
  • have active thrombophlebitis (inflammation of a vein leading to a blood clot)
  • have had blood clotting problems caused by the use of estrogen
  • have known or suspected estrogen-dependent cancer such as breast or endometrial cancer or a history of any of these cancers
  • have or has had blood clots in the legs, lungs, heart, or brain
  • have overgrowth of the lining of the uterus (endometrial hyperplasia)
  • have partial or complete loss of vision due to blood vessel disease of the eyes
  • have unusual vaginal bleeding that has not been checked by a doctor

What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who uses this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people using this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • breast tenderness, pain, enlargement
  • flu symptoms
  • headache
  • nausea
  • vaginal discharge
  • vaginal discomfort
  • vaginal itching
  • vaginal spotting (small amounts of vaginal bleeding)
  • vaginal yeast infection (itching, discomfort, and discharge)
  • weight gain

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • abdominal pain, nausea or vomiting
  • allergic reaction (redness, itching, or irritation of the vaginal tissues)
  • back pain
  • breast lump
  • signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
  • signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
  • swelling of the arms or legs
  • unusual or unexpected vaginal bleeding

Stop using the medication and seek immediate medical attention if any of the following occur:

  • pain or swelling in the leg
  • sharp pain in the chest, coughing blood, or sudden shortness of breath
  • signs of heart attack (e.g., sudden chest pain or pain radiating to back, down arm, jaw; sensation of fullness of the chest; nausea; vomiting; sweating; anxiety)
  • signs of stroke (e.g., sudden or severe headache; sudden loss of coordination; vision changes; sudden slurring of speech; or unexplained weakness, numbness, or pain in arm or leg)
  • symptoms of a serious allergic reaction (such as shortness of breath, hives, or swelling of the face or throat)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Note the following important information about estrogen:

  • Estrogen should be used at the lowest dose that relieves your menopausal symptoms for the shortest time period possible, as directed by your doctor.
  • Estrogens with or without progestins should not be used to prevent heart disease, heart attacks, or strokes.

Allergy: Contact allergy (such as itching and redness) may occur when estrogen is applied to the skin or inside the vagina. Although this allergy is extremely rare, people who develop skin reactions or contact sensitization to any ingredient of the medication are at risk of developing a severe allergic reaction with continued use. Contact your doctor if you experience itching and redness of the skin while using this medication.

Applicator use: Women who have a very dry vagina or those who have some shrinkage in the vaginal area should be careful when inserting the applicator. If it becomes uncomfortable, do not force it. Women who have recently had surgery in the vaginal area or the reproductive system should talk to their doctor before using this medication.

Blood clotting disorders: Estrogens with or without progestins are associated with an increased risk of blood clots in the lungs and legs. This risk also increases with age, a personal or family history of blood clots, smoking, and obesity. The risk of blood clots is also increased if you are immobilized for prolonged periods and with major surgery. If possible, this medication should be stopped 4 weeks before major surgery. Talk about the risk of blood clots with your doctor.

Blood pressure: Women may experience increased blood pressure when using estrogen replacement therapy. Blood pressure should be monitored, especially if high doses of estrogen are used. With estradiol vaginal tablets, an increase in blood pressure is less likely because less estrogen is absorbed into the blood, compared with estrogen oral tablets, patches, or gel. Ask your doctor how often you should have your blood pressure checked.

Bone disease: If you have bone disease due to cancer or a metabolic condition causing too much calcium in your body, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Breast and ovarian cancer: Studies indicate an increased risk of breast and ovarian cancer with long-term use of estrogen replacement therapy. Women who have breast nodules, fibrocystic disease, abnormal mammograms, or a strong family history of breast cancer should be closely monitored by their doctor if they use estrogens. Women taking estrogens should have regular breast examinations and should be taught how to do breast self-examination. This medication must not be applied to the breasts, as it may have harmful effects on the breast tissue.

Dementia: Women over age 65 receiving combined hormone replacement therapy may be at increased risk of developing dementia (loss of memory and intellectual function). If you are over 65, talk to your doctor about whether you should be tested for dementia.

Diabetes: Estrogens can cause changes to glucose tolerance for people with diabetes. Well-controlled diabetes may not be affected by the use of estradiol vaginal tablets, because less estrogen is absorbed into the blood, compared with estrogen oral tablets, patches, or gel. If your diabetes is not well controlled, your doctor should closely monitor your condition while you are using this medication.

Endometrial cancer: There is evidence that estrogen replacement therapy can increase the risk of cancer of the endometrium (lining of the uterus). Taking a progestin at the right time along with the estrogen reduces this risk of endometrial cancer to the same level as that of a woman who does not take estrogen. A progestin is not usually needed for women using estradiol vaginal tablets. This is because very little estrogen from the estradiol vaginal tablet is absorbed into the blood, compared with estrogen oral tablets, patches, or gel. For further information, check with your doctor.

Endometriosis: Estrogen replacement therapy can cause endometriosis to reappear or get worse. If you have or have had endometriosis, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Fibroids: This medication may worsen fibroids, causing sudden enlargement, pain, or tenderness. If you notice these effects, contact your doctor.

Fluid retention: Estrogen may cause fluid retention. Fluid retention can increase symptoms of heart or kidney problems, epilepsy, or asthma. If you have any of these conditions, you should be closely monitored by your doctor while taking this medication.

Follow-up examinations: It is important to have a follow-up examination 3 to 6 months after starting this medication to assess the response to treatment. Examinations should be done at least once a year after the first one.

Gallbladder: This medication can aggravate gallbladder disease or increase the risk of developing it. If you have gallbladder disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

High cholesterol or triglycerides: Estrogen may increase levels of triglycerides (a type of fat found in the blood) in those who already have high levels of triglycerides. This has been observed particularly when estrogen is taken orally (by mouth). The risk is reduced with use of the vaginal tablets. Ask your doctor to monitor your levels of triglycerides.

Liver disease: If you have or have had liver problems, you may require special monitoring by your doctor while you use this medication. If you have ever had liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Migraine headaches: For some people, estrogen can aggravate migraine headaches. Talk to your doctor if you notice any change in your migraine pattern while using estrogen.

Pregnancy: Estradiol vaginal tablets should not be used during pregnancy. If you become pregnant while using this medication, contact your doctor immediately.

Breast-feeding: Estrogen passes into breast milk. If you are a breast-feeding mother and are using estradiol vaginal tablets, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of this medication have not been established for use by children. This medication is not intended to be used by children.

What other drugs could interact with this medication?

There may be an interaction between estradiol vaginal tablets and any of the following:

  • anastrozole
  • "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • carbamazepine
  • celecoxib
  • clarithromycin
  • clozapine
  • cobicistat
  • corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
  • diabetes medications (e.g. acarbose, canagliflozin, glyburide, insulin, linagliptin, lixisenatide, metformin, rosiglitazone)
  • efavirenz
  • HIV protease inhibitors (e.g., atazanavir, darunavir, ritonavir)
  • HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., efavirenz, etravirine, nevirapine)
  • lenalidomide
  • melatonin
  • mifepristone
  • modafinil
  • rifabutin
  • rifampin
  • St. John's wort
  • seizure medications (e.g., carbamazepine, lamotrigine, phenobarbital, phenytoin)
  • tacrolimus
  • theophylline
  • thyroid replacements (e.g., desiccated thyroid, levothyroxine)
  • tizanidine
  • tranexamic acid
  • ursodiol

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. In many cases, interactions are intended or are managed by close monitoring. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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