What is Activelle?
Activelle is a medication that combines both estradiol (identical to the natural hormone estrogen) and progestin in a single tablet.
It’s used as a treatment for:
- Moderate to severe vasomotor symptoms (hot flashes, flushing, sweating), which are associated with lower estrogen levels brought on by menopause
- Vulval and vaginal atrophy and associated symptoms occurring due to menopause
Activelle should only be used in women that have an intact uterus.
For more resources, including a full list of the risks and benefits of Activelle, please review the product monograph.
How does Activelle work?
As the female body enters the menopausal and postmenopausal life stages, it begins producing less estrogen. This is a natural, universal transition.
However, reduced levels of estrogen can lead to unpleasant symptoms in some women (i.e., heart palpitations, mood changes, hot flashes, etc.).
Activelle works by providing estradiol to the body (virtually identical to the naturally produced hormone estrogen). This reduces the severity of certain vasomotor menopause/postmenopause symptoms (i.e., hot flashes, night sweats, excessive sweating, etc.).
The progestin hormone that is also in an Activelle dosage works in combination with the estradiol to help prevent endometrial hyperplasia (overgrowth of the lining of the uterus), as well as cancer of the lining of the uterus (endometrial carcinoma), if left untreated.
What is Activelle used to treat?
Activelle is used to treat women that have intact uteri, who are experiencing moderate to severe vasomotor symptoms associated with menopause and postmenopause, or vulvar or vaginal atrophy associated with menopause.
These symptoms relate specifically to temperature regulation within the body, leading to things like hot flashes, night sweats, feeling uncomfortably hot, or excessive sweating.
Because Activelle also contains the progestin hormone, it also helps reduce the chances of endometrial hyperplasia (overgrowth of the lining of the uterus) occurring.
How do you take Activelle?
Activelle tablets are to be taken orally, once a day. It can be taken with or without food.
It’s a good idea to try and take your Activelle doses around the same time each day, so that the medication maintains the highest possible level of efficacy throughout your treatment cycle.
There are 28 pills in each Activelle dial pack, and you should follow the instructions closely on the package, so that you can use the pack to help track your Activelle doses (and avoid missing any).
How long does Activelle last after you take it?
What are the common side effects of Activelle?
Some potential side effects of Activelle that could occur include:
- Headaches
- Irregular vaginal bleeding or spotting, during first 3-6 months of treatment
- Changes in amount of cervical secretion
- Vaginal and genital itching
- Breast pain, tenderness, swelling, or enlargement
- Hot flashes
- Bloating
- Uterine fibroid
- Back or neck pain
- Involuntary muscle spasms
- Leg cramps
- Heartburn
- Increase or decrease in weight
- Hair loss or growth
- Acne
- Skin discoloration (i.e., chloasma or vascular purpura)
- Painful, red skin nodules
If any of these side effects of Activelle start to become severe, be sure to talk to your healthcare practitioner. They may be able to suggest an alternative medication that will work better for you.
MHT is the most effective treatment for menopausal symptoms and has been shown to prevent bone loss.
In menopausal women who start appropriately-dosed MHT prior to age 60 OR within 10 years of their last period, the health benefits outweigh the risks.
Risks of MHT are considered very rare (~1 case per 1000 to 10,000 women on MHT per year) and may include:
- risks of stroke or blood clots in legs or lungs with oral estrogen (much lower risk with estrogen gel or patch)
- risks of dementia in women older than 65 years,
- risk of breast cancer (less than ~1 case per 1000 women on MHT per year)
These conditions are all rare, but they highlight the importance of having a full discussion with your healthcare practitioner; especially if you’re experiencing moderate to severe side effects.
Individualization is key, and your MHT treatment plan should be reassessed (at least) once a year to monitor your health, as well as ensure that you are on the correct dosage and formulation. Your practitioner can help you find balance between treating your symptoms safely, and avoiding increased risks.
Who shouldn't take Activelle?
There are certain people that shouldn’t use Activelle, including:
- If you have a known hypersensitivity to this drug or any of its ingredients, or to components of its container
- If you have liver disease or liver function issues
- If you have known or suspected estrogen- or progestin-dependent cancer, or any history of this
- If you have or have had breast cancer
- You have any unexplained vaginal bleeding
- If you are or think you may be pregnant
- If you’re breastfeeding
- If you have or have had any blood clotting diseases, of have experienced any blood clots in a vein before
- If you have vision issues resulting from ophthalmic vascular disease (a blood vessel disease in the eye)
- If you experience migraines
- If you have porphyria (a blood pigment disease)
In addition to these people, there are others that should be extra cautious about taking Activelle. Be sure to talk to your healthcare practitioner before starting Activelle if you:
- Have a history of allergies or intolerances to other medications or substances
- Have a history of breast disease, breast biopsies, or a family history of breast cancer
- Have experienced any unusual or undiagnosed vaginal bleeding
- Have a history of uterine fibroids or endometriosis
- Have a history of endometrial hyperplasia (an overgrowth of the lining of the uterus)
- Have a history of liver disease, liver tumours, or jaundice
- Have a history of itching related to estrogen use or during pregnancy
- Have a history of migraines
- Have a history of high blood pressure
- Have a history of heart disease, heart attacks, or strokes
- Have a personal or family history of blood clots
- Have a history of kidney disease, asthma, or epilepsy
- Have gallbladder disease
- Have a history of bone disease
- Have hypothyroidism, and you’re taking thyroid hormone replacement therapy
- Have hereditary angioedema, or have had episodes of rapid swelling of the feet, face, lips, eyes, tongue, throat, or digestive tract
- Have lupus
- Have diabetes
- Have been diagnosed with porphyria (a disease of blood pigment)
- Have a history of high triglycerides or high cholesterol
- Have very low calcium levels
- Have depression
- Are on prolonged bed rest
- Are pregnant or may be pregnant
- Are breastfeeding
- Have had a hysterectomy
- Have otosclerosis (a disease that affects the eardrum and hearing)
- Have lactose intolerance
- Smoke
Drugs that may interact with Activelle include:
- Drugs used for the treatment of epilepsy (i.e., phenobarbital, hydantoin, phenytoin, and carbamazepine)
- Drugs used for tuberculosis (i.e., rifampicin, rifabutin)
- Drugs used for the treatment of HIV or hepatitis infections (i.e., nevirapine, efavirenz, ritonavir, telaprevir, and nelfinavir)
- Anticoagulant, antidiabetic, and antihypertensive drugs
- Barbiturates
- Herbal preparations containing St John’s Wort (Hypericum perforatum)
- Ketoconazole (a fungicide)
Grapefruit juice may increase the effect of Activelle.
If any of these conditions apply to you, your practitioner may want to suggest an alternative medication that could work better for you.
Further reading
