Activella

Name: Activella

What should I avoid while using Activella (estradiol and norethindrone)?

Grapefruit and grapefruit juice may interact with estradiol and lead to unwanted side effects. Discuss the use of grapefruit products with your doctor.

What other drugs will affect Activella (estradiol and norethindrone)?

Other drugs may interact with estradiol and norethindrone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Before Using Activella

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group 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.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of estrogens and progestins in the elderly with use in other age groups.

Pregnancy

Estrogens and progestins are not recommended for use during pregnancy or right after giving birth. Becoming pregnant or maintaining a pregnancy is not likely to occur around the time of menopause.

Breast Feeding

Estrogens and progestins pass into the breast milk and can change the content or lower the amount of breast milk. Use of this medicine is not recommended in nursing mothers.

Interactions with 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 any of these medicines, 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 medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

  • Boceprevir
  • Dasabuvir
  • Ombitasvir
  • Paritaprevir
  • Ritonavir
  • Tranexamic Acid

Using medicines in this class 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.

  • Anagrelide
  • Aprepitant
  • Boceprevir
  • Bosentan
  • Bupropion
  • Carbamazepine
  • Ceritinib
  • Conivaptan
  • Dabrafenib
  • Darunavir
  • Dasabuvir
  • Dexamethasone
  • Donepezil
  • Efavirenz
  • Eliglustat
  • Enzalutamide
  • Fosphenytoin
  • Griseofulvin
  • Idelalisib
  • Isotretinoin
  • Lesinurad
  • Lixisenatide
  • Lumacaftor
  • Mitotane
  • Modafinil
  • Netupitant
  • Oxcarbazepine
  • Paclitaxel
  • Paclitaxel Protein-Bound
  • Phenytoin
  • Piperaquine
  • Pitolisant
  • Pixantrone
  • Prednisone
  • Rifabutin
  • Rifampin
  • St John's Wort
  • Sugammadex
  • Theophylline
  • Tizanidine
  • Topiramate
  • Ulipristal
  • Valproic Acid

Interactions with Food/Tobacco/Alcohol

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. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

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

  • Asthma or
  • Calcium, too much or too little in blood or
  • Diabetes mellitus (sugar diabetes)
  • Epilepsy (seizures) or
  • Heart problems or
  • Kidney problems or
  • Liver tumors, benign or
  • Lupus erythematosus, systemic or
  • Migraine headaches or
  • Porphyria—Estrogens may worsen these conditions.
  • Blood clotting problems (or history of during previous estrogen therapy)—Estrogens usually are not used until blood clotting problems stop; using estrogens is not a problem for most patients without a history of blood clotting problems due to estrogen use.
  • Breast cancer or
  • Bone cancer or
  • Cancer of the uterus or
  • Fibroid tumors of the uterus—Estrogens may interfere with the treatment of breast or bone cancer or worsen cancer of the uterus when these conditions are present.
  • Changes in genital or vaginal bleeding of unknown causes—Use of estrogens may delay diagnosis or worsen condition. The reason for the bleeding should be determined before estrogens are used.
  • Endometriosis or
  • Gallbladder disease or gallstones (or history of) or
  • High cholesterol or triglycerides (or history of) or
  • Liver disease or
  • Pancreatitis (inflammation of pancreas)—Estrogens may worsen these conditions; while estrogens can improve blood cholesterol, they may worsen blood triglycerides for some people.
  • Hypothyroid (too little thyroid hormone)—Dose of thyroid medicine may need to be increased.
  • Vision changes, sudden onset including
  • Bulging eyes or
  • Double vision or
  • Migraine headache or
  • Vision loss, partial or complete—Estrogens may cause these problems. Tell your doctor if you have had any of these problems, especially while taking estrogen or oral contraceptives (“birth control pills”).

Precautions While Using Activella

It is very important that your doctor check your progress at regular visits to make sure this medicine does not cause unwanted effects. These visits will usually be every year, but some doctors require them more often.

It is not yet known whether the use of estrogens increases the risk of breast cancer in women. Therefore, it is very important that you regularly check your breasts for any unusual lumps or discharge. Report any problems to your doctor. You should also have a mammogram (x-ray pictures of the breasts) done if your doctor recommends it. Because breast cancer has occurred in men taking estrogens, regular breast self-exams and exams by your doctor for any unusual lumps or discharge should be done.

Tell the doctor in charge that you are taking this medicine before having any laboratory test because some results may be affected.

Activella Side Effects

Women rarely have severe side effects from taking estrogens to replace estrogen. Discuss these possible effects with your doctor:

The prolonged use of estrogens has been reported to increase the risk of endometrial cancer (cancer of the lining of the uterus) in women after menopause. This risk seems to increase as the dose and the length of use increase. When estrogens are used in low doses for less than 1 year, there is less risk. The risk is also reduced if a progestin (another female hormone) is added to, or replaces part of, your estrogen dose. If the uterus has been removed by surgery (total hysterectomy), there is no risk of endometrial cancer, and no need to take an estrogen and progestin combination.

It is not yet known whether the use of estrogens increases the risk of breast cancer in women. Although some large studies show an increased risk, most studies and information gathered to date do not support this idea.

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

Check with your doctor as soon as possible if any of the following side effects occur:

More common
  • Breast pain or tenderness
  • dizziness or light-headedness
  • headache
  • rapid weight gain
  • swelling of feet and lower legs
  • vaginal bleeding
Rare
  • Breast lumps
  • change in vaginal discharge
  • discharge from nipple
  • nausea and vomiting
  • pains in chest, groin, or leg, especially calf
  • pains in stomach, side, or abdomen
  • pain or feeling of pressure in pelvis
  • severe or sudden headache
  • sudden and unexplained shortness of breath
  • sudden loss of coordination
  • sudden slurred speech
  • sudden vision changes
  • weakness or numbness in arm or leg
  • yellow eyes or skin

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
  • bloating or gas
  • dizziness
  • general feeling of tiredness
  • flu-like symptoms
  • mental depression
  • muscle aches
  • nausea—taking tablet with food may decrease
  • vaginitis

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.

What are some things I need to know or do while I take Activella?

  • Tell all of your health care providers that you take Activella. This includes your doctors, nurses, pharmacists, and dentists.
  • If you have high blood sugar (diabetes), talk with your doctor. This medicine may raise blood sugar.
  • Check your blood sugar as you have been told by your doctor.
  • Have your blood pressure checked often. Talk with your doctor.
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • Have a bone density test as you have been told by your doctor. Talk with your doctor.
  • Be sure to have regular breast exams and gynecology check-ups. Your doctor will tell you how often to have these. You will also need to do breast self-exams as your doctor has told you. Talk with your doctor.
  • This medicine may affect certain lab tests. Tell all of your health care providers and lab workers that you take this medicine.
  • Limit your drinking of alcohol.
  • Avoid cigarette smoking. Smoking raises the chance of heart disease. Talk with your doctor.
  • If you drink grapefruit juice or eat grapefruit often, talk with your doctor.
  • This medicine may raise the chance of blood clots, a stroke, or a heart attack. Talk with the doctor.
  • Talk with your doctor if you will need to be still for long periods of time like long trips, bedrest after surgery, or illness. Not moving for long periods may raise your chance of blood clots.
  • If you are 65 or older, use Activella with care. You could have more side effects.
  • This medicine is not approved for use in children. Talk with the doctor.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

Soft, brittle bones (osteoporosis):

  • This medicine works best when used with calcium/vitamin D and weight-bearing workouts like walking or PT (physical therapy).
  • Follow the diet and workout plan that your doctor told you about.

How is this medicine (Activella) best taken?

Use this medicine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

  • Take Activella at the same time of day.
  • Take with or without food. Take with food if it causes an upset stomach.

What do I do if I miss a dose?

  • Use a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not use 2 doses or extra doses.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Activella or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Activella. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Activella Dosage and Administration

Use of estrogen-alone, or in combination with a progestin, should be with the lowest effective dose and for the shortest duration consistent with treatment goals and risks for the individual woman. Postmenopausal women should be re-evaluated periodically as clinically appropriate to determine if treatment is still necessary.

Treatment of Moderate to Severe Vasomotor Symptoms due to Menopause

Activella therapy consists of a single tablet to be taken once daily for the treatment of moderate to severe vasomotor symptoms due to menopause.

  • Activella 1 mg/0.5 mg
  • Activella 0.5 mg/0.1 mg

Treatment of Moderate to Severe Symptoms of Vulvar and Vaginal Atrophy due to Menopause

Activella therapy consists of a single tablet to be taken once daily for the treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.

  • Activella 1 mg/0.5 mg

Prevention of Postmenopausal Osteoporosis

Activella therapy consists of a single tablet to be taken once daily for the prevention of postmenopausal osteoporosis.

  • Activella 1 mg/0.5 mg
  • Activella 0.5 mg/0.1 mg

Dosage Forms and Strengths

Activella tablets are available in two strengths:

  • Each tablet of Activella 1 mg/ 0.5 mg contains 1 mg of estradiol and 0.5 mg of norethindrone acetate. The tablets are white, round, bi-convex, film-coated tablets engraved with NOVO 288 on one side and the APIS bull on the other.
  • Each tablet of Activella 0.5 mg/ 0.1 mg contains 0.5 mg of estradiol and 0.1 mg of norethindrone acetate. The tablets are white, round, bi-convex, film-coated tablets engraved with NOVO 291 on one side and the APIS bull on the other.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Long-term continuous administration of natural and synthetic estrogens in certain animal species increases the frequency of carcinomas of the breast, uterus, cervix, vagina, testis, and liver.

Activella Usage

Take Activella exactly as your healthcare provider tells you to take it.

Take 1 Activella at the same time each day.

You and your healthcare provider should talk regularly (every 3 to 6 months) about the dose you are taking and whether you still need treatment with Activella.

If you miss a dose, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take your next dose at the regular time. Do not take two doses of Activella at the same time.

In Summary

Commonly reported side effects of conjugated estrogens/medroxyprogesterone include: depression, headache, nausea, and mastalgia. Other side effects include: dizziness, and peripheral edema. See below for a comprehensive list of adverse effects.

Usual Adult Dose for Primary Ovarian Failure

Regimen 1 (Cyclic Combined Estrogen-Progestin Therapy): Conjugated estrogens 0.625 mg orally once a day AND Medroxyprogesterone acetate 5 mg orally once a day for 14 days per month.

-or-

Regimen 2 (Continuous Combined Estrogen-Progestin Therapy): Conjugated estrogens 0.45 mg orally once a day AND Medroxyprogesterone acetate 1.5 mg orally once a day or conjugated estrogens 0.625 mg orally once a day AND Medroxyprogesterone acetate 2.5 mg or 5 mg orally once a day.

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