Patient Medication Information: uses, side effects, how to take - Activelle
Serious Warnings and Precautions
In postmenopausal women taking estrogen-alone, who had surgery to remove the uterus (called a hysterectomy), there is an increased risk of:
Estrogens with progestin, like Activelle®, should:
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What is Activelle® used for?
Activelle® is used only in women who still have a uterus. It is used to treat the following conditions that can occur as a result of lower estrogen levels associated with menopause:
- moderate to severe vasomotor symptoms of menopause (such as hot flashes).
- changes in the vagina and/or external genitalia (vulva).
How does Activelle® work?
After menopause, your body makes less estrogen.
Activelle® is a Hormone Replacement Therapy (HRT) that contains 2 ingredients that have different functions. The estradiol (a type of estrogen) in Activelle® replaces the estrogen that some women are missing. This may help relieve your menopausal symptoms such as hot flashes. Since estrogen may also stimulate the lining of the uterus to grow Activelle® also contains the progestin hormone called norethindrone acetate (NETA). NETA helps to reduce the risk of overgrowth of the lining of the uterus (a condition called endometrial hyperplasia), which could lead to cancer of the lining of the uterus (womb).
What are the ingredients in Activelle®?
Medicinal ingredients: Estradiol, and norethindrone acetate.
Non-medicinal ingredients: Copovidone, hypromellose, lactose monohydrate, magnesium stearate, maize starch, talc, and triacetin.
Activelle® comes in the following dosage form(s):
Film-coated tablets: 1 mg estradiol (as estradiol hemihydrate) and 0.5 mg norethindrone acetate.
Do not use Activelle® if:
- you are allergic to estradiol, norethindrone acetate or to any of the ingredients in Activelle®,
- you have or have had liver problems, and the blood tests to measure how your liver is working have not returned to normal.
- you have or have had estrogen-dependent or progestin-dependent cancer (e.g. endometrial cancer).
- you have thickening of the lining of the uterus (endometrial hyperplasia).
- you have or have had breast cancer.
- you have unexpected or unusual vaginal bleeding.
you are pregnant or think you might be pregnant.
- you are breast-feeding
- you have, or have had a heart attack, stroke, angina or heart disease
you have or have had blood clotting problems such as:
- deep vein thrombosis (where a blood clot forms in a deep vein);
- pulmonary embolism (where a blood clot forms in the lung);
- Thromboembolism (where a blood clot blocks the flow of blood through your veins).
- you have partial or complete loss of vision due to blood vessel disease of the eye (called ophthalmic vascular disease)
- you have porphyria (a disease caused by how your body makes heme – a component of your blood).
- you have migraine headaches.
To help avoid side effects and ensure proper use, talk to your healthcare professional before you take Activelle®. 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) and/or breast biopsies, or a family history of breast cancer.
- have experienced any unusual or undiagnosed vaginal bleeding.
have or had:
- a history of uterine fibroids (growths) inside of your uterus;
- endometriosis (growth of the uterine lining outside your uterus); and/or
- a history of overgrowth of the lining of the uterus (endometrial hyperplasia)
- have a history of liver disease or liver tumors, jaundice (yellowing of the eyes and/or skin).
- have a history of itching related to estrogen use or during pregnancy.
- have a history of migraine headaches.
- have a history of high blood pressure.
- 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 asthma.
- have seizures (epilepsy).
- have gallbladder disease.
- have a history of bone disease (this includes certain metabolic conditions or cancers that can affect the calcium and phosphorus levels in your blood).
- have a condition where your thyroid gland fails to produce enough thyroid hormone (hypothyroidism) and you are being treated with thyroid hormone replacement therapy.
- have a condition called hereditary angioedema, or if you have had episodes of rapid swelling of the hands, feet, face, lips, eyes, tongue, throat (airway blockage) or digestive tract.
- have been diagnosed with lupus.
- have been diagnosed with diabetes.
- have or had high levels of fat in your blood (cholesterol, triglycerides).
- have been diagnosed with depression.
- will have to lie in bed for an extended period of time (prolonged bed rest).
- are pregnant or may be pregnant.
- are breastfeeding.
- have been diagnosed with hearing loss due to abnormal bone growth in your ear (otosclerosis).
- have an intolerance to lactose. Activelle® contains lactose.
- have eye problems.
- smoke.
- are having surgery.
Other warnings you should know about:
Breast cancer:
There is a higher risk of breast cancer in postmenopausal women taking combined
estrogen plus progestin.
Estrogens with or without progestins should not be taken by women who have a
personal history of breast cancer.
Talk to your healthcare professional before starting HRT if you have:
- a family history of breast cancer or breast lumps, breast biopsies or abnormal mammograms (breast x-rays)
- never had a baby before or had your first full-term pregnancy at an older age
- you are overweight
- you started menstruating at an early age
Overgrowth of the lining of the uterus and cancer of the uterus:
- Taking estrogen-only therapy by postmenopausal women who still have a uterus increases your risk of excessive thickening of the lining of the womb (endometrial hyperplasia) and cancer of the lining of the womb (endometrial cancer).
- Talk to your healthcare professional about progestin therapy and risk factors for endometrial hyperplasia and endometrial cancer. 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 HRT for 5 years or more increases 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 Activelle® can increase your risk of developing blood clots in your large veins. You should discuss risk factors for blood clots with your healthcare professional since blood clots can be life-threatening or cause serious disability. Talk to your healthcare professional if:
- you or a family member has had blood clots.
- you smoke.
- you are overweight.
The risk of blood clots is increased as you get older. It is also temporarily increased:
- if you are inactive for long periods of time.
- following major surgery.
If you are going to have surgery, your healthcare professional may recommend you temporarily stop take Activelle® about 4 to 6 weeks before the procedure to reduce the risk of blood clots.
Gallbladder Disease: Your risk of developing gallbladder disease that requires surgery is increased when taking estrogens.
Dementia: Your risk of developing dementia (memory loss) is increased if you are a woman aged 65 and over taking estrogen with progestin.
Check-ups and testing: You will have regular visits with your healthcare professional, before and during your treatment. They will:
- Do a physical exam and blood work (which may include a pregnancy test) 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.
- Do regular follow-up exams including a breast exam and blood pressure check at least once a year to identify side effects associated with the use of Activelle®. Your first follow-up visit should be within 3 to 6 months of starting treatment.
- Advise you to regularly check your own breasts. Talk to your healthcare professional if you are unsure on the technique to use.
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 Activelle®:
- medicines used for the treatment of epilepsy (e.g. phenobarbital, hydantoin, phenytoin and carbamazepine).
- medicines used for tuberculosis (e.g. rifampicin, rifabutin).
- medicines used for the treatment of HIV or hepatitis infections (e.g. nevirapine, efavirenz, ritonavir, telaprevir and nelfinavir).
- medicines used for the prevention or treatment of blood clots (anticoagulant).
- medicines used to treat diabetes.
- medicines used to treat high blood pressure (antihypertensive).
- medicines used to help you relax such as barbiturates.
- herbal treatments to treat depression containing St. John’s Wort (Hypericum perforatum).
- medicines used to treat fungal infection such as ketoconazole.
Grapefruit juice.
How to take Activelle®:
- You may begin taking Activelle® on any day of the week that is convenient. If you are switching from another Hormone Replacement Therapy product, start Activelle® right after withdrawal bleeding (menstrual period) has ended.
- Your healthcare professional will prescribe the lowest dose to treat your symptoms for as short amount of time as necessary. Speak to your healthcare professional if you think your dose is too strong or not strong enough.
- Activelle® is not a contraceptive. If it is less than 12 months since your last menstrual period or you are under 50 years old, you may still need to use additional contraception to prevent pregnancy. Talk to your healthcare professional.
Usual dose:
Take 1 tablet once daily, at around the same time each day. Once you have finished all the 28 tablets in the pack, start a new pack without interruption.
How to use the dial pack:
Activelle® is supplied in calendar dial packs of 28 white tablets. Follow the steps below on how to use the calendar dial pack.
- 1.
Set the day reminder
Turn the inner disc to set the day of the week for the first tablet (see image 1). The day of the week should be aligned with the little plastic tab.
Image 1:
- 2.
How to take the first tablet
The first tablet to be taken is under the sealed opening in the transparent outer rim of the dial-pack. Break the plastic tab and tip out the first tablet (see image 2).
Image 2:
- 3.
Following days
Move the outer transparent dial clockwise one space to the next day as indicated by the arrow (see image 3). Tip out the next tablet.
Image 3:
The transparent dial can only be turned after the tablet in the opening has been removed.
Overdose:
Signs of an overdose may include nausea, vomiting, breast discomfort, fluid retention (swelling), bloating, vaginal bleeding, depressed mood, tiredness, acne, and growth of body or facial hair.
| If you think you, or a person you are caring for, have taken too much Activelle®, contact a healthcare professional, hospital emergency department, regional poison control centre or Health Canada's toll-free number, 1-844 POISON-X (1-844-764-7669) immediately, even if there are no signs or symptoms. |
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Missed Dose:
If you forget to take a tablet and it’s within 12 hours of the time you should have taken it, take it as soon as you remember. If it has been more than 12 hours do not take this dose. The next dose should be taken at the normal time. Do not take two tablets to make up for the missed dose.
Forgetting a dose may increase the likelihood of breakthrough bleeding and spotting.
What are possible side effects from using Activelle®?
These are not all the possible side effects you may have when taking Activelle®. If you experience any side effects not listed here, tell your healthcare professional.
- Nausea, vomiting.
- Abdominal cramps, pressure, pain, and bloating.
- Feeling tired (fatigue), inability to sleep or stay awake.
- Changes in appetite, and body weight.
- Change in sex drive.
- Muscle aches and pains, including in the legs, abdominal, back, chest, and pelvic.
- Headache, dizziness.
- Anxiety, feeling nervous.
- Vaginal itching, discharge, discomfort, and odour.
- Pain during or after sex.
- Breast tenderness, pain, swelling.
- Skin darkening on the face (chloasma).
- Acne, itchy skin.
- Hair loss or abnormal hairiness.
- Hot flushes.
- Flu-like symptoms.
- Tingling sensation of the skin.
- Passing gas (flatulence).
- Diarrhea, constipation.
- Joint stiffness.
Activelle® can cause abnormal blood and positive cervical smear test results. Your healthcare professional will decide when to do these tests and will interpret the results.
Serious side effects and what to do about them
| Symptom / effect | Talk to your healthcare professional | Stop taking drug and get immediate medical help | ||
|---|---|---|---|---|
| Only if severe | In all cases | |||
| COMMON | ||||
Serious side effects and what to do about them
| Symptom / effect | Talk to your healthcare professional | Stop taking drug and get immediate medical help | |||||
|---|---|---|---|---|---|---|---|
| Only if severe | In all cases | ||||||
| Peripheral edema: Swelling of arms and legs | ✓ | ||||||
| Depression (sad mood that won’t go away): difficulty sleeping or sleeping too much, changes in appetite or weight, feelings of worthlessness, guilt, regret, helplessness or hopelessness, withdrawal from social situations, family, gatherings and activities with friends, reduced libido (sex drive) and thoughts of death or suicide | ✓ | ||||||
| Vaginitis: Genital infection with a fungus, vaginal inflammation, discharge, itching, and pain | ✓ | ||||||
| UNCOMMON | |||||||
| Allergic reaction: difficulty swallowing or breathing, wheezing; drop in blood pressure; feeling sick to your stomach and throwing up; hives or rash; swelling of the face, lips, tongue or throat. | ✓ | ||||||
| Erythema multiforme (an allergic skin reaction): raised red or purple skin patches, possibly with blister or crust in the center; possibly swollen lips, mild itching or burning | ✓ | ||||||
| Erythema nodosum (swelling of the fat cells under the skin): tender red lumps usually on both shins | ✓ | ||||||
| Vaginal bleeding changes: increased or decreased menstrual bleeding, spotting, infrequent periods or absence of bleeding, severe vaginal bleeding | ✓ | ||||||
| Deep Vein Thrombosis (blood clot in the legs or arms): pain or swelling in the leg or arm | ✓ | ||||||
| Thromboembolism (blood clot in a vein or artery): pain or tenderness or swelling in your arm or leg, skin that is red or warm, coldness, tingling or numbness, pale skin, muscle pain or spasms, weakness | ✓ | ||||||
| Pulmonary Embolism (blood clot in the lungs): Sharp pain in the chest, coughing blood, sudden shortness of breath | ✓ | ||||||
Serious side effects and what to do about them
| Symptom / effect | Talk to your healthcare professional | Stop taking drug and get immediate medical help | |||||
|---|---|---|---|---|---|---|---|
| Only if severe | In all cases | ||||||
| Eye disorders: blurred vision, loss of vision in eye, increased sensitivity of the eyes to light, eye pain or redness, swelling and itching of the eyelids, decreased sharpness of vision, eye irritation, blocked eye veins | ✓ | ||||||
| Stroke (bleeding or blood clot in the brain): sudden severe headache or worsening of headache, vomiting, dizziness, fainting, problems with your vision or speech, weakness or numbness in face, arm or leg | ✓ | ||||||
| Hypertension (high blood pressure): shortness of breath, fatigue, dizziness or fainting, chest pain or pressure, swelling in your ankles and legs, bluish colour to your lips and skin, racing pulse or heart palpitations. | ✓ | ||||||
| Migraine: severe headache often accompanied by nausea, vomiting and sensitivity to light | ✓ | ||||||
| RARE | |||||||
| Breast abnormalities (including breast cancer): dimpling or sinking of the skin, changes in the nipple, or any lumps you see or feel, discharge from breasts, enlarged breasts, swelling | ✓ | ||||||
| Coronary thrombosis (blocked heart arteries): chest pain and pressure, shortness of breath | ✓ | ||||||
| Cystitis (bladder infection): increased need to urinate, pain in the pelvis or lower back, frequent urination during the night, cloudy urine that may contain blood, burning sensation when passing urine | ✓ | ||||||
| Endometrial hyperplasia (abnormal growth of the lining of the uterus): menstrual bleeding that is heavier or lasts longer than normal, bleeding after menopause, menstrual cycles that are shorter than 21 days | ✓ | ||||||
| Endometrial cancer (cancer of the lining of the uterus): vaginal bleeding not associated with a period or after menopause; abnormal blood-tinged discharge from the vagina; pain in the pelvis | ✓ | ||||||
Serious side effects and what to do about them
| Symptom / effect | Talk to your healthcare professional | Stop taking drug and get immediate medical help | |||||
|---|---|---|---|---|---|---|---|
| Only if severe | In all cases | ||||||
| Gallbladder problems: fever, nausea, pain that radiates to your shoulder or back, severe pain in your upper right abdomen, vomiting | ✓ | ||||||
| Liver problems: yellowing of your skin and eyes (jaundice), right upper stomach area pain or swelling, nausea or vomiting, unusual dark urine, light coloured stool, unusual tiredness | ✓ | ||||||
| Neuritis (inflammation of the nerve): pain, feeling of pins-and needles, numbness, loss of reflexes | ✓ | ||||||
| Palpitations (fast-beating, fluttering or pounding heart): heart skipping beats, beating too fast, pounding, fluttering rapidly | ✓ | ||||||
| Urinary tract disorders: difficulty and pain when passing urine, blood in urine | ✓ | ||||||
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:
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 at room temperature between 15°C - 25°C.
- Store in a dry place. Do not refrigerate.
- Protect from light by keeping the dial-pack inside the outer carton.
- Keep out of the reach and sight of children
If you want more information about Activelle®:
- Talk to your healthcare professional.
- Find the full product monograph that is prepared for health professionals and includes the Patient Medication Information by visiting the Health Canada Drug Product Database website (https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/drug-product-database.html); the manufacturer’s website http://www.novonordisk.ca; or by calling 1-800-465-4334.
Last Revised: FEB 17, 2025
Activelle® is a registered trademark of Novo Nordisk Health Care AG and is used under license by Novo Nordisk Canada Inc.
© Novo Nordisk Canada Inc. 2025