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

Estradiol vaginal inserts 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 moderate to severe pain during sexual intercourse that is caused by low estrogen levels in the body during menopause.

At menopause, the amount of estrogen made by the ovaries declines and symptoms such as vaginal atrophy can occur. When an estradiol vaginal insert is placed inside the vagina, it releases estradiol, which helps to make vaginal tissues thicker and more supple. An improvement in symptoms usually occurs after 12 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 taking this medication, speak to your doctor. Do not stop taking 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?

Each small, light pink, tear-shaped, soft gel insert contains either 4 mg or 10 mg of estradiol. Nonmedicinal ingredients: ethylene glycol palmitostearate, FD&C Red #40, gelatin, glycerin, hydrolyzed gelatin, lecithin, mannitol, medium chain triglycerides, pharmaceutical ink, polyethylene glycol stearates, purified water, sorbitan, sorbitol, and titanium dioxide.

How should I use this medication?

The usual starting dose of this medication is one 4 mg vaginal insert placed inside the vagina once daily for 2 weeks. After 2 weeks, 1 vaginal insert is used twice a week, typically every 3 to 4 days.

This medication is used intravaginally (inside of the vagina). Insert the smaller end into the vaginal canal to a depth of about 2 inches. From this placement, the insert melts, releasing the estradiol into the vagina.

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 taking the medication without consulting 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 take 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, protect it from light and moisture, and keep it out of the reach of children.

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 or may be pregnant
  • have a known thrombophilic condition (deficiencies in certain proteins involved in preventing blood clots)
  • 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 takes 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 taking 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.

  • abdominal, back, or pelvic pain
  • acne
  • appetite changes
  • body odour
  • breast tenderness, pain, or swelling
  • change in body weight
  • decreased appetite
  • diarrhea
  • dizziness
  • feeling bloated
  • hair growth on face, chest, abdomen, or legs
  • hair loss on head
  • headache
  • increased frequency of cold- or flu-like symptoms (e.g., runny or stuffy nose, sore throat, cough, sinus discomfort, body aches, headache, fever, general feeling of being unwell)
  • increased sweating
  • itchy skin
  • migraine
  • nausea
  • pain with sexual activity
  • rash
  • tender red lumps on the shins
  • tiredness or fatigue
  • vaginal discharge, discomfort or odour
  • vomiting

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:

  • anxiety or nervousness
  • breast changes (e.g., dimpling or sinking of the skin, changes in the nipple, lumps that you can see or feel)
  • changed vaginal bleeding (e.g., increased or decreased bleeding or frequency, spotting, severe bleeding)
  • fast or pounding heartbeat
  • memory loss
  • symptoms of nerve inflammation (e.g., pins and needles feeling, decreased reflexes, pain or numbness)
  • signs of a blood clot in the leg or inflammation of blood vessels (e.g., sudden swelling or pain, redness, warmth, tenderness in the affected area)
  • signs of depression (e.g., poor concentration, weight changes, sleep changes, decreased interest in activities, thoughts of suicide)
  • signs of high blood pressure (e.g., shortness of breath, fatigue, dizziness or fainting, chest pain or pressure, swelling in the ankles and legs, bluish colour to lips and skin)
  • signs of liver problems (e.g., yellowing of skin and eyes, swelling or pain in the right upper abdomen, dark urine, light coloured stool)
  • swelling of the legs, hands
  • symptoms of a vaginal yeast infection (e.g., itching, burning, or discharge from the vagina)
  • symptoms of endometrial cancer (e.g., vaginal bleeding that occurs other than during menstruation, bleeding after menopause, blood-tinged vaginal discharge, pelvic pain)
  • symptoms of ovarian cancer (e.g., abdominal pain or bloating, quickly feeling full after eating, weight loss, pelvic pain, frequent urination, changes in bowel habits)
  • symptoms of urinary tract infection (e.g., pain or burning sensation when urinating, frequent need to urinate, pelvic pain, blood in urine, strong smelling or cloudy urine)
  • vision changes (e.g., blurred vision, increased sensitivity to light, eye pain, swelling or itching of eyelids, vision loss)

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

  • signs of a blood clot in the lungs (e.g., sharp pain in the chest, coughing up blood, sudden shortness of breath)
  • signs of a heart attack or blocked heart arteries (e.g., chest pain and pressure, shortness of breath)
  • signs of a stroke (e.g., sudden or severe headache, sudden loss of coordination, vision changes, sudden slurring of speech, unexplained weakness, numbness or pain in an arm or leg)
  • symptoms of gastrointestinal (stomach or intestine) bleeding (such as blood in the stools; black, tarry stools; coughing or vomiting up of blood or material that looks like coffee grounds; abdominal pain; shortness of breath; and weakness or fatigue)

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.

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: People 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 inserts, 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. People 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. People 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: People 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 inserts, 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 person who does not take estrogen. A progestin is not usually needed for people using estradiol vaginal inserts. This is because very little estrogen from the estradiol vaginal insert 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 inserts. 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.

Seizures: Estrogens may cause an increase in the frequency of seizures for people who experience seizures or have a history of seizures. If you have a history of seizures, 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.

Thyroid disease: Estrogens can affect how well the thyroid gland works. If you have thyroid disease such as hypothyroidism (low thyroid levels), 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.

Pregnancy: Estradiol vaginal inserts 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 breast-feeding and using estradiol vaginal inserts, 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?

For a full list of interactions, use the Drug Interaction Checker available on the website.

If you are taking other 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. Speak to your doctor about how any drug interactions are being managed or should be managed.

Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications 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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