Estradiol and norethindrone

Estradiol/norethindrone is a prescription medication used after menopause to reduce moderate to severe hot flashes, treat moderate to severe menopausal changes in and around the vagina, and help reduce your chances of getting osteoporosis (thin weak bones). It is also used to treat certain conditions in women before menopause if their ovaries do not make enough estrogens naturally. 

This medication contains two hormones, estradiol and norethindrone, and belongs to a group of drugs called estrogen and progestin combinations. Together these work as a hormone replacement to relieve issues caused by hormonal changes. 

This medication comes in a tablet form and is usually taken once daily, with or without food. 

It is also available as a patch and is usually applied 2 times each week or every 3 to 4 days.

Common side effects of this medication include headache, breast pain, and irregular vaginal bleeding or spotting. 

Do not use if you are pregnant.

You should not use estradiol and norethindrone if you have had a hysterectomy, or if you have any of the following conditions: liver disease, unusual vaginal bleeding, a history of breast or uterine cancer, or if you have recently had a heart attack, stroke, or a blood clot.

Estradiol and norethindrone 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 of this medicine may increase your risk of breast cancer, uterine cancer, heart attack, stroke, or blood clot. Talk with your doctor about your individual risk.

Do not take this medicine in larger amounts or for longer than recommended.

You should not use estradiol and norethindrone if you are allergic to it, or if you have:

• a recent history of heart attack, stroke, or blood clots;

• liver disease;

• abnormal vaginal bleeding that a doctor has not checked;

• a history of breast, uterine, or hormone-related cancer;

• if you have had a hysterectomy; or

• if you are pregnant.

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

• heart disease;

• risk factors for coronary artery disease (such as diabetes, 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);

• asthma;

• diabetes;

• epilepsy or other seizure disorder;

• migraines;

• porphyria;

• lupus;

• kidney disease;

• gallbladder disease;

• endometriosis or uterine fibroid tumors;

• a thyroid disorder; or

• high levels of calcium in your blood.

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

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

FDA pregnancy category X: Do not use estradiol and norethindrone if you are pregnant. Tell your doctor right away if you become pregnant during treatment.

Estradiol and norethindrone can pass into breast milk. This medication may slow breast milk production. Do not use if you are breast-feeding a baby.

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

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

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 a mammogram every year while using estradiol and norethindrone.

Store at room temperature away from moisture, heat, and light.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• chest pain or heavy feeling, pain spreading to the jaw or shoulder, sweating, feeling short of breath, fainting;

• sudden numbness or weakness (especially on one side of the body), sudden severe headache, slurred speech, problems with vision or balance;

• sudden cough, wheezing, rapid breathing, coughing up blood;

• pain, swelling, warmth, or redness in one or both legs;

• vomiting, jaundice (yellowing of the skin or eyes);

• unusual vaginal bleeding; or

• a lump in your breast.

Common side effects may include:

• nausea, bloating, stomach cramps;

• headache, depressed mood;

• breast pain, back pain;

• sleep problems (insomnia);

• hair loss, weight changes, acne; or

• vaginal itching or discharge, breakthrough bleeding.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In the U.S.

• Activella
• Lopreeza
• Mimvey

Available Dosage Forms:

• Tablet

Therapeutic Class: Estrogen/Progestin Combination

Pharmacologic Class: Estrogen

It is very important that you use estradiol and norethindrone exactly as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects.

estradiol and norethindrone comes with a patient information leaflet. Read and follow the instructions carefully. Ask your doctor if you have any questions.

estradiol and norethindrone sometimes comes in a special dispenser pack with a calendar reminder dial.

To use:

• To use this dispenser, first turn the inner disc so the current day of the week is lined up with the plastic tab. Pull the plastic tab up and break if off. Tip out the first tablet.
• To get the next tablet out (on the next day), turn the outer transparent dial one space clockwise as shown by the arrow.
• The transparent dial can be turned only after the tablet in the opening has been removed. This will help you to remember to take one tablet every day.

Dosing

The dose of estradiol and norethindrone will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of estradiol and norethindrone. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  • For hot flashes and other symptoms caused by menopause:
    • Adults—One tablet once a day. One tablet contains 1 milligram (mg) of estradiol and 0.5 mg of norethindrone, or 0.5 mg of estradiol and 0.1 mg of norethindrone.
    • Children—Use is not recommended.
  • For treatment of changes in and around the vagina (such as vaginal dryness, itching, and burning) caused by low estrogen levels or menopause.
    • Adults—One tablet once a day. One tablet contains 1 milligram (mg) of estradiol and 0.5 mg of norethindrone.
    • Children—Use is not recommended.
  • For prevention of osteoporosis after menopause:
    • Adults—One tablet once a day. One tablet contains 1 milligram (mg) of estradiol and 0.5 mg of norethindrone, or 0.5 mg of estradiol and 0.1 mg of norethindrone.
    • Children—Use is not recommended.

Missed Dose

If you miss a dose of estradiol and norethindrone, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

• Estradiol/Norethindrone Acet
• Norethindrone and Estradiol

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): Known, suspected, or history of estrogen-dependent or progestin-dependent malignant neoplasm (eg, endometrial cancer); endometrial hyperplasia; porphyria; partial or complete loss of vision associated with ophthalmic vascular disease; active thrombophlebitis; classical migraine; breast-feeding

Refer to adult dosing.