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Estradiol and norethindrone (Oral route)

Pronunciation:

es-tra-DYE-ol, nor-ETH-in-drone AS-e-tate

Brand Names:

  • Activella
  • Mimvey

Dosage Forms:

  • Tablet

Warnings:

Oral route(Tablet)

Estrogens with or without progestins should not be used for the prevention of cardiovascular disease or dementia. Increased risks of DVT, pulmonary embolism, stroke, myocardial infarction, and invasive breast cancer have been reported. An increased risk of probable dementia in postmenopausal women 65 years of age or older has also been reported. There is an increased risk of endometrial cancer in women with a uterus who use unopposed estrogens. Estrogens with or without progestins should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman .

Classifications:

Therapeutic—

Estrogen/Progestin Combination

Pharmacologic—

Estrogen

Uses of This Medicine:

Estradiol and norethindrone combination is used to treat moderate to severe hot flashes and other symptoms of menopause. It is also used to treat changes in and around the vagina (such as vaginal dryness, itching, and burning) caused by low estrogen levels or menopause. This medicine is also used to treat certain conditions in women before menopause if their ovaries do not make enough estrogens naturally, and prevent osteoporosis after menopause.

This medicine is a combination of two hormones: an estrogen hormone (estradiol) and a progestin hormone (norethindrone). It works by preventing symptoms, such as feelings of warmth in the face, neck, and chest, or sudden strong feelings of heat and sweating (hot flashes) in women during menopause.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Use of Activella® is not indicated in children.

Older adults—

Although appropriate studies on the relationship of age to the effects of Activella® have not been performed in the geriatric population, no geriatric-specific problems have been documented to date. However, elderly patients are more likely to have breast cancer, strokes, or dementia, which may require caution in patients receiving this medicine.

Pregnancy—

Pregnancy CategoryExplanation
All TrimestersXStudies in animals or pregnant women have demonstrated positive evidence of fetal abnormalities. This drug should not be used in women who are or may become pregnant because the risk clearly outweighs any possible benefit.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Tranexamic Acid

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Acrivastine
  • Aripiprazole
  • Bupropion
  • Carbamazepine
  • Ceritinib
  • Crizotinib
  • Dabrafenib
  • Eliglustat
  • Eslicarbazepine Acetate
  • Fentanyl
  • Idelalisib
  • Isotretinoin
  • Mitotane
  • Piperaquine
  • Pixantrone
  • Primidone
  • Siltuximab
  • Theophylline
  • Tizanidine
  • Topotecan

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Alprazolam
  • Amprenavir
  • Aprepitant
  • Atazanavir
  • Bacampicillin
  • Betamethasone
  • Bexarotene
  • Bosentan
  • Clarithromycin
  • Colesevelam
  • Cyclosporine
  • Darunavir
  • Delavirdine
  • Efavirenz
  • Etravirine
  • Fosamprenavir
  • Fosaprepitant
  • Fosphenytoin
  • Ginseng
  • Griseofulvin
  • Itraconazole
  • Ketoconazole
  • Lamotrigine
  • Levothyroxine
  • Licorice
  • Modafinil
  • Mycophenolate Mofetil
  • Mycophenolic Acid
  • Nelfinavir
  • Oxcarbazepine
  • Phenobarbital
  • Phenytoin
  • Pioglitazone
  • Prednisolone
  • Primidone
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rosuvastatin
  • Rufinamide
  • Selegiline
  • St John's Wort
  • Tacrine
  • Telaprevir
  • Tipranavir
  • Topiramate
  • Troglitazone
  • Troleandomycin
  • Valdecoxib
  • Voriconazole
  • Warfarin

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Caffeine

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Abnormal or unusual vaginal bleeding or
  • Blood clots (eg, deep vein thrombosis, pulmonary embolism), active or history of or
  • Breast cancer, known or suspected, or a history of or
  • Heart attack, history of or
  • Liver disease or
  • Protein C, protein S, or other known blood clotting disorders or
  • Stroke, history of or
  • Tumors (estrogen-dependent), known or suspected—Should not be used in patients with these conditions.
  • Asthma or
  • Bone problems or
  • Diabetes or
  • Edema (fluid retention or body swelling) or
  • Endometriosis or
  • Epilepsy (seizures) or
  • Gallbladder disease or
  • Hereditary angioedema (swelling of the face, lips, tongue, or throat) or
  • Hypercalcemia (high calcium in the blood) or
  • Hypocalcemia (low calcium in the blood) or
  • Hypothyroidism (an underactive thyroid) or
  • Jaundice during pregnancy or from using hormonal therapy in the past or
  • Liver tumors or
  • Migraine headache or
  • Porphyria (an enzyme problem) or
  • Systemic lupus erythematosus (SLE)—Use with caution. May make these conditions worse.
  • Heart disease or
  • Hypercholesterolemia (high cholesterol or fats in the blood) or
  • Hypertension (high blood pressure) or
  • Hypertriglyceridemia (high triglycerides or fats in the blood) or
  • Obesity, or history of or
  • Prolonged periods of immobilization—Use with caution. These conditions may increase risk for more serious side effects.

Proper Use of This Medicine:

It is very important that you use this medicine 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.

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

This medicine 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 this medicine 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 this medicine. 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 this medicine, 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.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and does not cause unwanted effects. Pelvic exam, breast exam, and mammogram (breast x-ray) may be needed to check for unwanted effects, unless your doctor tells you otherwise. Be sure to keep all appointments.

It is unlikely that a postmenopausal woman may become pregnant. But, you should know that using this medicine while you are pregnant could harm your unborn baby. If you think you have become pregnant while using the medicine, tell your doctor right away.

Using this medicine may increase your risk for having blood clots, strokes, or heart attacks. This risk may continue even after you stop using the medicine. Your risk for these serious problems is even greater if you have high blood pressure, high cholesterol in your blood, diabetes or are overweight or smoke cigarettes. Contact your doctor immediately if you experience chest pain, confusion, difficulty speaking, double vision, headaches, an inability to move arms, legs or facial muscle, or an inability to speak.

Using this medicine may increase your risk of endometrial cancer, breast cancer, or uterine cancer. Talk with your doctor about this risk. Check with your doctor immediately if your experience abnormal vaginal bleeding.

Do not use this medicine if you have had your uterus (womb) removed (hysterectomy).

Using this medicine may increase your risk of dementia, especially in women 65 years of age and older.

Check with your doctor immediately if severe headache or sudden loss of vision or any other change in vision occurs while you are using this medicine. Your doctor may want you to have your eyes checked by an ophthalmologist (eye doctor).

Make sure any doctor or dentist who treats you knows that you are using this medicine. You may need to stop using this medicine before you have surgery or if you need to stay in bed for an extended time. This medicine may affect the results of certain medical tests.

Do not eat grapefruit or drink grapefruit juice while you are using this medicine. Grapefruit and grapefruit juice may change the amount of this medicine that is absorbed in the body.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common
Body aches or pain
chills or fever
cold or flu-like symptoms
difficulty breathing
headache
itching of the vagina or genital area
nonmenstrual vaginal bleeding
pain during sexual intercourse
thick, white vaginal discharge with no odor or with a mild odor
unusual tiredness or weakness
Incidence not known
Abdominal or stomach pain
blistering, peeling, or loosening of the skin
change in vaginal discharge
chest pain, discomfort, or tightness in chest
clay-colored stools
clear or bloody discharge from the nipple
confusion
dark urine
difficulty speaking
difficulty swallowing
dizziness or lightheadedness
double vision
fainting
fast heartbeat
inability to move the arms, legs, or facial muscles
inability to speak
joint or muscle pain
loss of appetite
lump in the breast or under the arm
nausea and vomiting
noisy breathing
pain in the ankles or knees
pain or discomfort in the arms, jaw, back, or neck
pain or feeling of pressure in the pelvis
pain, redness, or swelling in the arm or leg
painful, red lumps under the skin, mostly on the legs
pains in the stomach, side, or abdomen, possibly radiating to the back
problems with memory or speech
puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
red, irritated eyes
redness or swelling of the breast
skin rash, hives, or itching
sores, ulcers, or white spots in the mouth or on the lips
sudden shortness of breath or troubled breathing
sweating
trouble recognizing objects
trouble thinking and planning
trouble walking

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
Back pain
breast pain
cramps
crying
euphoria
mental depression
paranoia
quick to react or overreact emotionally
rapidly changing moods
trouble sleeping
weakness
weight gain
Incidence not known
Changes in appetite
changes in sexual ability, desire, drive, or performance
excess air or gas in the stomach or intestines
increased hair growth, especially on the face
patchy brown or dark brown discoloration of the skin
trouble wearing contact lenses

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.


Last Updated: 11/4/2014

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