Activelle and Activelle LD are used to treat moderate to severe vasomotor symptoms (uncomfortable feelings of heat, sweating and flushing) that can occur as a result of low estrogen levels associated with menopause. Activelle is also used to treat vulval and vaginal atrophy (changes in the vagina or external genitalia as a result of low estrogen levels associated with menopause) with symptoms such as itching, burning, dryness in or around vagina, difficulty or burning while urination, and pain while having sex. The estrogen hormone is called estradiol (E2) and helps to relieve your menopausal symptoms. Estradiol is identical to the estrogen produced naturally by your body. Activelle replaces the estrogen in your body, which decreases naturally at menopause. The progestin hormone is called norethindrone acetate (NETA) and helps to reduce the risk of endometrial hyperplasia (stimulation of growth of the lining of the uterus), which could lead to cancer of the lining of the uterus (womb). Activelle and Activelle LD should be used only in women with intact uterus. Activelle and Activelle LD should be used only under the supervision of a doctor, with regular follow-up at least once a year to identify side effects associated with its use. Your first follow-up visit should be within 3to 6 months of start of 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 doctor. Your doctor may recommend some blood tests. You should follow the instructions of the doctor who prescribed Activelle to you. Activelle and Activelle LD is supplied in calendar dial packs of 28 white tablets. Take one tablet once daily. Try to take the medication at the same time each day. Once you have finished all the 28 tablets in the pack, start a new pack continuing the treatment without interruption.
Manufacturer Information
Activelle is manufactured by Novo Nordisk and comes from Canada. The active ingredients in Activelle are Estradiol and Norethindrone Acetate. Activelle is available as film-coated tablets in two dosage forms Activelle and Activelle LD. Activelle contains 1 mg estradiol and 0.5 mg norethindrone acetate. Activelle LD contains 0.5 mg estradiol and 0.1 mg norethindrone acetate.
Stop taking Activelle and call your doctor at once if you have one of these serious side effects:
• Swelling of arms and legs
• Depression
• Genital infection with a fungus or vaginal inflammation
• Enlargement of the lining of womb
• Allergic reaction
• Unexpected vaginal bleeding
• Rash with target-shaped reddening or sores
• Heart attack
• Blood clot in legs, lungs and eyes
• Jaundice
• Stroke
• Inflammation of vein
• Increase in blood pressure
• Gallstones or gallbladder disease
• Migraine
Less serious side effects include headache, irregular vaginal bleeding or spotting during the first 6 months of treatment, change in the amount of cervical secretion, vaginal and genital itching, breast pain or tenderness, swelling and enlargement, hot flushes, bloating, uterine fibroids, back or neck pain, involuntary muscle spasms, leg cramps, heartburn, increase or decrease in weight, hair loss or abnormal hairiness, acne, discoloration of the skin especially around the face or neck, known as pregnancy patches, red or purple discolorations of the skin, painful reddish skin nodules, abdominal pain, nausea, vomiting. Please call your doctor if you have any further concerns or questions.
Do not use Activelle if you are allergic to any ingredients in the medication, have liver disease, estrogen-dependent or progestin-dependent malignant neoplasia (e.g. endometrial cancer, excessive thickening of the womb lining, breast cancer, suffer from any unexplained vaginal bleeding, are or think you might be pregnant, are breastfeeding, have had a disease caused by blood clots in the arteries, such as a heart attack, stroke or angina, have a blood clot in a vein such as in the legs or the lungs, partial or complete loss of vision , porphyria, migraine. Activelle may interact with drugs used for the treatment of epilepsy (e.g. phenobarbital, phenytoin and carbamazepine), drugs used for tuberculosis (e.g. rifampicin, rifabutin), drugs used for the treatment of HIV or hepatitis infections (e.g. nevirapine, efavirenz, ritonavir), anticoagulant, antidiabetic and antihypertensive drugs, barbiturates, herbal preparations containing St John’s Wort, ketoconazole (a fungicide). Avoid drinking grapefruit juice while taking this medication as it may increase plasma concentrations of estrogens and result in side effects.
Reference:
1. https://www.novonordisk.ca/content/dam/Canada/AFFILIATE/www-novonordisk-ca/OurProducts/PDF/activelle-product-monograph.pdf
2. https://www.novonordisk.ca/content/dam/Canada/AFFILIATE/www-novonordisk-ca/OurProducts/PDF/activelle-ld-product-monograph.pdf