Estradiol: Uses, Side Effects and Dosage

What is ESTRADIOL used for?

ESTRADIOL is used to provide adults with:

• Relief of menopausal symptoms such as hot flushes, dryness, itching and burning in and around the vagina.
• help to prevent osteoporosis. When you have osteoporosis, your bones are weaker and break more easily. ESTRADIOL is used to prevent naturally occurring osteoporosis or osteoporosis resulting from low levels of estrogen after surgery. ESTRADIOL is used in combination with other important therapies such as proper diet, calcium and vitamin D intake, ending smoking habits and regular physical exercises.

How does ESTRADIOL work?

ESTRADIOL is a hormone replacement therapy. It contains 17β-estradiol. 17β-estradiol is similar to the female hormone estrogen produced by the body. During menopause, the amount of the estrogen produced by a woman’s body drops. This can cause menopausal symptoms such as hot flushes. Low estrogen levels in menopause can also cause osteoporosis, which is a thinning of the bones that makes them weaker and easier to break. ESTRADIOL replaces lower levels of estrogen in your body

Serious Warnings and Precautions

• If you are taking ESTRADIOL with progestin medication (another female hormone), there is an increased risk of developing serious problems. This includes breast cancer, heart attack, stroke and blood clots in both lungs and large veins.
• If you are taking ESTRADIOL alone, there is an increased risk of developing serious problems such as stroke and blood clots in the large veins.

• Estrogens, including ESTRADIOL, should:

  • not be used for the prevention of heart disease or stroke.

  • be used at the lowest effective dose and for the shortest period of time possible.

    Regular medical follow up is recommended.

What are the ingredients in ESTRADIOL?

Medicinal ingredients: 17β-estradiol

Non-medicinal ingredients: Acacia, cornstarch, dibasic calcium phosphate, lactose, magnesium stearate, silicon dioxide, talc and colour dyes [FD&C Blue #1 aluminum lake and D&C Red #27 aluminum lake (1 mg tablet); FD&C Blue #1 aluminum lake and FD&C Yellow #5 aluminum lake (tartrazine) (2 mg tablet)]

ESTRADIOL comes in the following dosage forms:

Tablets: 0.5 mg, 1 mg and 2 mg

Do not use ESTRADIOL if:

• you have liver disease
• you have (or have had) a history of known or suspected estrogen-dependent cancer. An example is cancer of the uterus (endometrial cancer)
• you have excessive thickening of the womb lining (endometrial hyperplasia)
• you have (or have had) a history of known or suspected breast cancer
• you have unusual or unexplained vaginal bleeding

• you may be pregnant or are breastfeeding

• you have (or have had) a disease caused by blood clots in the arteries, such as a heart attack, stroke or angina.
• you have migraines
• you have (or have had) blood clot disorders. This includes blood clots in the legs, lungs or veins.
• you have partial or complete loss of vision due to blood vessel disease in the eye
• you are allergic to estradiol or any of the other ingredients in ESTRADIOL

To help avoid side effects and ensure proper use, talk to your healthcare professional before you take ESTRADIOL. Talk about any health conditions or problems you may have, including if you:

• Have a history of allergy or intolerance to any medications or other substances

• Have a personal history of breast disease (including breast lumps), abnormal mammograms

  (breast x-rays), and/or breast biopsies, or a family history of breast cancer. Estrogens, including ESTRADIOL, should not be given to women who have breast cancer or to those who have a history of breast disease.

• Have experienced any unusual or undiagnosed vaginal bleeding

• Have a history of fibroids inside your womb or growth of womb lining outside your womb

  (endometriosis).

• Have a history of liver disease, jaundice (yellowing of the eyes and/or skin). Your healthcare professional will monitor your liver by conducting liver function tests during treatment.
• Have a history of itching related to estrogen use or during pregnancy
• Have a history of migraine headache
• Have a history of high blood pressure. Taking hormone replacement therapy, like ESTRADIOL, may cause your blood pressure to rise. Your healthcare professional will monitor your blood pressure while on treatment.
• Have a personal or family history of blood clots, or a personal history of heart disease or stroke
• Have a history of kidney disease
• Have history of asthma
• Have history of epilepsy (seizures)
• Have a history of bone disease. This includes certain conditions or cancers that can affect the levels of calcium or phosphorus in your blood
• Have been diagnosed with diabetes or at risk of developing diabetes.
• Have been diagnosed with porphyria (a blood disease)
• Have a history of high cholesterol or high triglycerides (fats). Your healthcare professional will test your blood during and before treatment. Your healthcare professional may need to lower the levels of fat in your blood before you start your treatment.
• Are taking thyroid replacement therapy
• Are pregnant or may be pregnant
• Have had a hysterectomy (surgical removal of the uterus)
• Smoke
• Had surgery recently or are planning to have surgery in the future

Other warnings you should know about:

ESTRADIOL can cause serious side effects, including:

• Overgrowth of the lining of the uterus and cancer of the uterus: Taking estrogen-only HRT

  (hormone replacement therapy) will increase your risk of excessive thickening of the lining of the womb (endometrial hyperplasia) and cancer of the womb (endometrial cancer). If you still have your uterus, your healthcare professional will prescribe a progestin (another hormone drug) for a certain number of days of each month to reduce the risk of endometrial hyperplasia (abnormal growth of the lining of the uterus). This will reduce the risk of developing these side effects. You should discuss progestin therapy and risk factors for endometrial hyperplasia and endometrial cancer with your healthcare professional. You should also report any unexpected or unusual vaginal bleeding to your healthcare professional.

  • If you have had your uterus removed, you are not at risk of developing endometrial hyperplasia or endometrial cancer. Progestin therapy is not generally required in women who have had a hysterectomy (surgical removal of the uterus).
• Ovarian Cancer: Taking hormone replacement therapy [HRT] for five years or more may increase your risk of developing ovarian cancer. Ovarian cancer may develop when using HRT with estrogen alone or estrogen in combination with progestin.

• Abnormal Blood Clotting: Taking estrogen can increase your risk of developing blood clots. You should discuss risk factors for blood clots with your healthcare professional since blood clots can be life threatening or cause serious disability. Consult your healthcare professional if:

  • you or a family member have a history of blood clots
  • you smoke
  • you are severely overweight
  • you have lupus

The risk of blood clots also can temporarily increase:

• if you are inactive for long periods of time
• following major surgery.
• Dementia: Your risk of developing dementia (memory loss) is increased if you are a woman aged 65 and over taking estrogen with progestin.
• Gallbladder Disease: Your risk of developing gallbladder disease that requires surgery is increased when taking estrogens.

Check-ups and testing: You will have regular visits with your healthcare profession, before and during your treatment. They will:

• Complete a physical examination on you before you begin treatment. Your visit may include a blood pressure check, a breast exam, a Pap smear and pelvic exam. You should have a mammogram before starting treatment and at regular intervals as recommended by your healthcare professional. Your healthcare professional may recommend some blood tests
• Conduct regular follow-up examinations at least once a year to identify side effects associated with the use of ESTRADIOL. Your first follow-up visit should be within 3 to 6 months of starting treatment.
• Advise you to regularly check your own breasts. Speak to your healthcare professional if you are uncertain on the technique to perform a breast self-examination

Tell your healthcare professional about all the medicines you take, including any drugs, vitamins, minerals, natural supplements or alternative medicines.

The following may interact with ESTRADIOL:

• Drugs that are used to:

  • prevent blood clots
  • control diabetes
  • control high blood pressure
  • prevent inflammation (containing phenylbutazone)
  • control epilepsy (for example, phenobarbital, phenytoin, or carbamazepine)
  • control anxiety (for example, meprobamate)
  • treat fungal infection (for example , ketoconazole, itraconazole)
  • treat viral infections such as HIV (for example, ritonavir)
  • treat bacterial infection such as antibiotics containing rifampicin (also called rifampin)

• Grapefruit juice

• some herbal products (for example, St. John’s Wort) obtained without a prescription from a healthcare professional.

If you are taking a blood test, tell your healthcare professional that you are taking ESTRADIOL, because this medicine can affect the results of some tests.

How to take ESTRADIOL:

• Your healthcare professional will give the lowest dose of ESTRADIOL to treat you.
• Take exactly as your healthcare professional has told you. Check with your healthcare professional if you are not sure.
• Take one tablet of ESTRADIOL at the same time each day.

• Estrogen is usually administered for the first 21 days to 25 days of each month. If you:

  • have had your uterus removed (hysterectomy): you will take ESTRADIOL every day of the month.
  • have a uterus: you will take ESTRADIOL on certain days of the month as directed by your healthcare professional. You will also take a progestin on certain days of the month to prevent excessive thickening of the lining of the womb.

Usual dose:

• Treatment of menopausal symptoms: At the start of treatment, take a 1 mg tablet each day.

  Every 3 to 6 months, speak to your healthcare professional on whether you should reduce your dose or end your treatment.

• Prevention of osteoporosis: At the start of treatment, take a 0.5 mg tablet each day as soon as possible after menopause. Your healthcare professional may change your dose depending on the status of your condition.

Overdose:

In women, overdosage of ESTRADIOL may cause nausea, breast discomfort, fluid retention, bloating, and vaginal bleeding.

If you think you, or a person you are caring for, have taken too much ESTRADIOL, contact a healthcare professional, hospital emergency department, or regional poison control centre immediately, even if there are no symptoms.

Missed Dose:

If you missed a dose, take it as soon as you remember. But if it is almost time to take your next dose, skip the missed dose and continue with your next schedule dose. Go back to the regular dosing schedule. Do not take two doses at the same time.

What are possible side effects from using ESTRADIOL?

These are not all the possible side effects you may have when taking ESTRADIOL. If you experience any side effects not listed here, tell your healthcare professional.

These side effects go away during treatment as your body adjusts to the medicine. However, check with your healthcare professional if they continue or become bothersome:

• Acne
• Allergic reaction and rash
• Bloating
• Breast pain and swelling
• Change in blood pressure
• Change in cholesterol and/or triglyceride levels
• Change in sex drive
• Change in weight or appetite
• Constipation
• Dark skin patches on face
• Dizziness (mild)
• Hair loss or abnormal hair growth
• Headaches (mild)
• Increased blood sugar levels
• Irritation when wearing contact lenses
• Nervousness, and/or irritability
• Stomach cramps
• Tired or lack of energy
• Vaginal bleeding/ spotting
• Vaginal itching/discharge or pain

Many women who are taking estrogens with a progestin will start having monthly vaginal bleeding, similar to menstrual periods again. This effect will continue for as long as the medicine is taken. However, monthly bleeding should not occur in women who have had their uterus removed by surgery (hysterectomy).

Serious side effects and what to do about them

Serious side effects and what to do about them

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough to interfere with your daily activities, tell your healthcare professional.

Reporting Side Effects

You can report any suspected side effects associated with the use of health products to Health Canada by:

• Visiting the Web page on Adverse Reaction Reporting (https://www.canada.ca/en/health-canada/services/drugs-health-products/medeffect-canada.html) for information on how to report online, by mail or by fax; or
• Calling toll-free at 1-866-234-2345.

NOTE: Contact your health professional if you need information about how to manage your side effects. The Canada Vigilance Program does not provide medical advice.

Storage:

Store the bottle at room temperature (15-30°C). Keep container tightly closed and protect from light.

Keep out of reach and sight of children.

If you want more information about ESTRADIOL:

• Talk to your healthcare professional

• Find the full product monograph that is prepared for healthcare professionals and includes this

  Patient Medication Information by visiting the Health Canada website:

  (https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/drug-product-database.html; or by calling Pharmascience Inc. at 1-888-550-6060.

Last Revised: OCT 25, 2022