estradiol and norethindrone

Generic Name: estradiol and norethindrone (ess tra DYE ole and nor ETH in drone)

Brand Names: Activella

What are estradiol and norethindrone?

Estradiol is a form of estrogen. Estrogen is a female sex hormone that is involved in the development and maintenance of the female reproductive system.

Norethindrone is a form of progesterone. Progesterone is a female hormone important for the regulation of ovulation and menstruation.

Together, estradiol and norethindrone are used to treat the symptoms of menopause such as feelings of warmth in the face, neck and chest, or sudden intense spells of heat and sweating ("hot flashes" or "hot flushes"); to treat vulvar and vaginal changes (itching, burning, dryness in or around the vagina, difficulty or burning with urination) caused by menopause; and to replace estrogen in conditions such as hypogonadism, removal of the ovaries, or primary ovarian failure that result in a lack of estrogen. Estradiol and norethindrone is also used to prevent thinning of the bones (osteoporosis).

Estradiol and norethindrone may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about estradiol and norethindrone?

Estradiol increases the risk of developing endometrial hyperplasia, a condition that may lead to cancer of the lining of the uterus. Using a progestin, such as norethindrone, with estradiol lowers the risk of developing this condition. Visit your doctor regularly and report any unusual vaginal bleeding right away.

Have yearly physical exams and examine your breasts for lumps on a monthly basis while taking estradiol and norethindrone.

What should I discuss with my healthcare provider before taking estradiol and norethindrone?

Do not take estradiol and norethindrone without first talking to your doctor if you have

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  a circulation, bleeding, or blood-clotting disorder;

  
  


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  undiagnosed, abnormal vaginal bleeding;

  
  


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  any type of breast, uterine, or hormone-dependent cancer; or

  
  


• liver disease.

Taking estradiol and norethindrone may be dangerous in some cases if you have any of the conditions listed above.

Before taking estradiol and norethindrone, tell your doctor if you have

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  high blood pressure, angina, or heart disease;

  
  


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  high levels of cholesterol or triglycerides in your blood;

  
  


• kidney disease;


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  asthma;

  
  


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  epilepsy;

  
  


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  migraines;

  
  


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  depression;

  
  


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  diabetes;

  
  


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  gallbladder disease;

  
  


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  uterine fibroids; or

  
  


• 
  

  had a hysterectomy (uterus removed).

  
  

You may not be able to take estradiol and norethindrone, or you may need a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Estradiol and norethindrone is in the FDA pregnancy category X. This means that estradiol and norethindrone is known to cause birth defects in an unborn baby. Do not take estradiol and norethindrone if you are pregnant or could become pregnant during treatment. Estradiol and norethindrone may decrease milk flow and have other effects on milk composition. Do not take estradiol and norethindrone without first talking to your doctor if you are breast-feeding a baby.

How should I take estradiol and norethindrone?

Take estradiol and norethindrone exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a glass of water.

Try to take each dose at the same time every day.

Have yearly physical exams and examine your breasts for lumps on a monthly basis while taking estradiol and norethindrone.

Store ethinyl estradiol and norethindrone tablets at room temperature away from moisture, heat, and direct light.

See also: Estradiol and norethindrone dosage (in more detail)

What happens if I miss a dose?

Take the missed dose as soon as you remember. However, if it is almost time for the next dose, skip the dose you missed and take only the next regularly scheduled dose. Do not take a double dose of this medication.

What happens if I overdose?

Contact an emergency room or poison control center for advice if an overdose is suspected.

Symptoms of a estradiol and norethindrone overdose may include nausea, vomiting, and withdrawal bleeding may occur in females.

What should I avoid while using estradiol and norethindrone?

There are no restrictions on food, beverages, or activity while taking estradiol and norethindrone unless otherwise directed by your doctor.

Estradiol and norethindrone side effects

If you experience any of the following serious side effects, stop taking estradiol and norethindrone and seek emergency medical attention or notify your doctor immediately:

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  an allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives);

  
  


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  shortness of breath or pain in the chest;

  
  


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  a painful, red, swollen leg;

  
  


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  abnormal vaginal bleeding;

  
  


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  pain, swelling, or tenderness in the abdomen;

  
  


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  severe headache or vomiting, dizziness, faintness or changes in vision or speech;

  
  


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  yellowing of the skin or eyes; or

  
  


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  a lump in a breast.

  
  

Other, less serious side effects may be more likely to occur. Continue to take estradiol and norethindrone and talk to your doctor if you experience

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  nausea and vomiting;

  
  


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  tenderness or enlargement of the breasts;

  
  


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  weakness;

  
  


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  swelling of the hands or feet;

  
  


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  spotty darkening of the skin, particularly on the face;

  
  


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  difficulty in wearing contact lenses;

  
  


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  vaginal irritation or discomfort; or

  
  


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  changes in menstrual cycle, painful menstruation, or break-through bleeding.

  
  

Estradiol increases the risk of developing endometrial hyperplasia, a condition that may lead to cancer of the lining of the uterus. Using a progestin, such as norethindrone, with estradiol lowers the risk of developing this condition. Visit your doctor regularly and report any unusual vaginal bleeding right away.

It is unclear to what extent estrogen and progesterone treatments may affect the risk of breast cancer.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

Estradiol and norethindrone Dosing Information

Usual Adult Dose for Atrophic Urethritis:

One (1 mg estradiol/0.5 mg norethindrone or 0.5 estradiol/ 0.1 mg norethindrone) tablet orally once a day.

-or-

One (0.05 mg-0.14 mg) patch applied twice weekly. If a greater progestin dose is desired, a single (0.05 mg-0.25 mg) patch may be applied twice weekly.

Alternatively, either patch may be applied as a continuation to an initial 14-day application of an estradiol-only transdermal patch within a 28-day cycle.

The patch should not be applied to, or near, the breasts. The application site should be smooth, clean, dry, fold-free, without damage or irritation, and be rotated with an interval of at least one week allowed to pass between applications to the same site.

If a patch dislodges, it may be reapplied to another area of the lower abdomen, or a new patch may be applied, in which case, the original treatment schedule resumes. However, only one patch should be worn at any given time during the three to four day dosing interval.

Usual Adult Dose for Atrophic Vaginitis:

One (1 mg estradiol/0.5 mg norethindrone or 0.5 estradiol/ 0.1 mg norethindrone) tablet orally once a day.

-or-

One (0.05 mg-0.14 mg) patch applied twice weekly. If a greater progestin dose is desired, a single (0.05 mg-0.25 mg) patch may be applied twice weekly.

Alternatively, either patch may be applied as a continuation to an initial 14-day application of an estradiol-only transdermal patch within a 28-day cycle.

The patch should not be applied to, or near, the breasts. The application site should be smooth, clean, dry, fold-free, without damage or irritation, and be rotated with an interval of at least one week allowed to pass between applications to the same site.

If a patch dislodges, it may be reapplied to another area of the lower abdomen, or a new patch may be applied, in which case, the original treatment schedule resumes. However, only one patch should be worn at any given time during the three to four day dosing interval.

Usual Adult Dose for Hypoestrogenism:

One (1 mg estradiol/0.5 mg norethindrone or 0.5 estradiol/ 0.1 mg norethindrone) tablet orally once a day.

-or-

One (0.05 mg-0.14 mg) patch applied twice weekly. If a greater progestin dose is desired, a single (0.05 mg-0.25 mg) patch may be applied twice weekly.

Alternatively, either patch may be applied as a continuation to an initial 14-day application of an estradiol-only transdermal patch within a 28-day cycle.

The patch should not be applied to, or near, the breasts. The application site should be smooth, clean, dry, fold-free, without damage or irritation, and be rotated with an interval of at least one week allowed to pass between applications to the same site.

If a patch dislodges, it may be reapplied to another area of the lower abdomen, or a new patch may be applied, in which case, the original treatment schedule resumes. However, only one patch should be worn at any given time during the three to four day dosing interval.

Usual Adult Dose for Postmenopausal Symptoms:

One (1 mg estradiol/0.5 mg norethindrone or 0.5 estradiol/ 0.1 mg norethindrone) tablet orally once a day.

-or-

One (0.05 mg-0.14 mg) patch applied twice weekly. If a greater progestin dose is desired, a single (0.05 mg-0.25 mg) patch may be applied twice weekly.

Alternatively, either patch may be applied as a continuation to an initial 14-day application of an estradiol-only transdermal patch within a 28-day cycle.

The patch should not be applied to, or near, the breasts. The application site should be smooth, clean, dry, fold-free, without damage or irritation, and be rotated with an interval of at least one week allowed to pass between applications to the same site.

If a patch dislodges, it may be reapplied to another area of the lower abdomen, or a new patch may be applied, in which case, the original treatment schedule resumes. However, only one patch should be worn at any given time during the three to four day dosing interval.

What other drugs will affect estradiol and norethindrone?

Before taking estradiol and norethindrone, tell your doctor if you are taking an anticoagulant (blood thinner) such as warfarin (Coumadin). You may not be able to take estradiol and norethindrone, or you may require a dosage adjustment or special monitoring during treatment.

Drugs other than those listed here may also interact with estradiol and norethindrone. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including vitamins, minerals, and herbal products.

More estradiol and norethindrone resources

• Estradiol and norethindrone Dosage
• Estradiol and norethindrone Use in Pregnancy & Breastfeeding
• Estradiol and norethindrone Drug Interactions
• Estradiol and norethindrone Support Group
• 4 Reviews for Estradiol and norethindrone - Add your own review/rating

Compare estradiol and norethindrone with other medications

• Atrophic Urethritis
• Atrophic Vaginitis
• Hypoestrogenism
• Postmenopausal Symptoms

Where can I get more information?

• Your pharmacist has additional information about estradiol and norethindrone written for health professionals that you may read.