Indications 

Activella is a combination of estradiol and norethindrone prescribed for women with a uterus for the following purposes: 

• Treating moderate to severe menopause-related vasomotor symptoms 
• Preventing postmenopausal osteoporosis 
• Treating moderate to severe symptoms of vulvar and vaginal atrophy due to menopause 

Estradiol, an estrogen replacement, replaces the body’s depleted estrogen hormone, alleviating symptoms such as hot flashes, night sweats, vaginal dryness and itching, and urinary issues. It also aids in the prevention of bone thinning. 

Norethindrone, a progestin, mimics the natural hormone progesterone produced by the body, thus reducing the risk of estrogen-induced uterine cancer. 

Uses and Dosage 

Before taking Activella, and with each prescription refill, read its medication guide and patient information leaflet thoroughly. If you have any questions or concerns, consult your physician or pharmacist without hesitation. 

The dosage of Activella is determined by the patient’s medical condition and response to the treatment. 

Typically, it is taken once daily as directed by the doctor, with or without food. To avoid stomach discomfort, taking it with food or immediately after a meal is an option. 

Take Activella regularly at the same time every day as prescribed, without increasing or decreasing the dosage or frequency of administration.  

Inform your physician if your condition does not improve or deteriorate. 

Side Effects 

Listed below are the potential side effects of Activella. Notify your physician immediately if any of them persist or worsen. 

Common Side Effects 

• Headache 
• Back pain 
• Hair loss 
• Upset stomach or vomiting 
• Sleep difficulties 
• Cramps 
• Bloating 
• Tender or enlarged breasts 
• Vaginal bleeding or spotting 
• Common cold symptoms 
• Weight gain 

 Serious Side Effects 

• Signs of liver problems such as: 
  • Dark urine 
  • Fatigue 
  • Loss of appetite 
  • Upset stomach 
  • Stomach pain 
  • Light-colored stools 
  • Vomiting 
  • Yellow skin or eyes 
• Signs of gallbladder problems such as: 
  • Upper right belly pain 
  • Right shoulder or shoulder blade pain 
  • Yellow skin or eyes 
  • Fever with chills 
  • Bloating 
  • Severe vomiting 
• Signs of high blood pressure like: 
  • Severe headache or dizziness 
  • Fainting 
  • Changes in vision 
• Signs of pancreas problems (pancreatitis) such as: 
  • Severe stomach pain 
  • Severe back pain 
  • Severe vomiting 
• Weakness on one side of the body, speech or cognitive impairment, balance changes, facial drooping, or blurred vision 
• Changes or loss of eyesight, protruding eyes, or discomfort wearing contact lenses 
• Breast lump, breast soreness or tenderness, or nipple discharge 
• Vaginal discharge or itching 
• Severe or persistent vaginal bleeding or spotting 
• Mood changes, including depression 
• Memory loss or impairment 

Notify your doctor or seek medical assistance if you experience any of the following indications of severe adverse reaction listed above. 

Allergic Reactions 

Activella rarely causes severe allergic reactions, but seek prompt medical assistance if you observe signs of a serious allergic reaction, such as: 

• Rash 
• Hives 
• Itching 
• Redness 
• Swelling 
• Blisters 
• Peeling skin 
• Fever 
• Wheezing 
• Chest or throat tightness 
• Difficulty breathing, swallowing, or talking 
• Unusual hoarseness 
• Swelling of the throat, lips, tongue, face, or mouth 

The adverse effects of Activella listed here are not comprehensive. If you experience any other effects not included above, inform your doctor promptly. 

Cautions 

Before starting treatment with Activella, inform your doctor or pharmacist if you have any known allergies, especially to any ingredients in Activella tablets or any medications. 

To ensure Activella is safe for you, disclose to your physician your medical background, specifically regarding any history of: 

• Vaginal bleeding of unknown cause 
• Certain cancers (such as cancer of the uterus, ovaries, or breast) 
• Blood clots 
• Stroke 
• Heart disease (such as heart attack) 
• Liver disease 
• Kidney disease 
• Family medical history (especially breast lumps, cancer, and blood clots) 
• Family or personal history of angioedema (swelling disorder)  
• Protein C or protein S deficiency (blood clotting disorders) 
• High blood pressure 
• Diabetes 
• High blood cholesterol/triglyceride levels 
• Obesity 
• Lupus 
• Underactive thyroid (hypothyroidism) 
• Mineral imbalance (low or high level of calcium in the blood) 
• A particular hormone problem (hypoparathyroidism) 
• Uterus problems (such as fibroids and endometriosis) 
• Gallbladder disease 
• Asthma 
• Seizures 
• Migraine headaches 
• A particular blood disorder (porphyria) 
• Mental/mood disorders (such as depression and dementia) 

To minimize the risk of drug interactions, inform your healthcare provider of all current medications, including prescription and over-the-counter drugs, vitamins, and herbal products, as many drugs may interact with Activella. 

Some of the products that may interact with Activela include: 

• Aromatase inhibitors lik anastrozole, exemestane, letrozole 
• Fulvestrant 
• Ospemifene 
• Raloxifene 
• Tamoxifen 
• Toremifene 
• Tranexamic acid 
• Certain combination products used to treat chronic hepatitis C like ombitasvir, paritaprevir, ritonavir with or without dasabuvir 

Inform your doctors and the laboratory personnel that you are taking Activella, as it may affect the results of certain tests, including the metyrapone test. 

Inform your doctor if you recently had or will have surgery or will be inactive for an extended period. These circumstances can increase the possibility of blood clots, mainly if you use an estrogen product such as Activella. You may need to discontinue this medication temporarily or take special measures. 

Activella may induce facial hyperpigmentation. Protect your skin from the sun, tanning beds, and sunlamps by using sunscreen, protective clothing, and eyewear. 

If you are nearsighted or wear contact lenses, you may experience vision issues or difficulties wearing contact lenses while taking Activella. Consult your eye doctor if such problems arise. 

Do not use Activella during pregnancy. Inform your doctor immediately if you become pregnant or suspect you are pregnant. 

Activella is not recommended during breastfeeding as it may affect the quantity and quality of breast milk. Consult your doctor before nursing while taking this medication.