This combination medication contains 3 medications: relugolix, estradiol, and norethindrone acetate. Together, these medications are used to reduce symptoms of uterine fibroids and endometriosis.

Estrogens and progestins are female hormones. They are produced by the body and are needed for normal female sexual development and for regulating the menstrual cycle during childbearing years. They are also responsible for the symptoms associated with endometriosis and uterine fibroids.

Endometriosis is a painful condition where tissue that normally forms the lining of the uterus grows outside of the uterus. This tissue goes through the same changes during the menstrual cycle as the tissue in the uterus. These changes are caused by the hormone estrogen.

Progesterone is responsible for the development and growth of fibroids, and by reducing the amount of progesterone produced by the body, fibroids often shrink and become less painful.

Relugolix belongs to the group of medications known as gonadotropin-hormone releasing hormone (GnRH) receptor antagonists. Relugolix works by blocking GnRH and thereby reducing the amount of estrogen and progesterone produced by the body.

Estradiol belongs to the class of medications called estrogens, while norethindrone acetate belongs to the class of medications known as progestins. Including a specific amount of these female hormones in this medication helps to reduce the menopause-like effects caused by reducing the amount of estrogen and progesterone in the body.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

The recommended dose of relugolix - estradiol - norethindrone is 1 tablet, taken by mouth, once a day, at approximately the same time each day. It may be taken with or without food, and should be swallowed whole with some liquid, as needed.

This medication is usually started as soon as possible after menstrual bleeding has started, but no later than the fifth day of bleeding. This helps to regulate the frequency and amount of bleeding that occurs in the first month of taking the medication. This medication should not be used for more than 24 months to reduce the risk of bone loss.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor. If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Each light-yellow-to-yellow, round, film-coated tablet, debossed with "MVT" on one side and "415" on the other side contains 40 mg of relugolix, 1 mg of estradiol, and 0.5 mg of norethindrone acetate. Nonmedicinal ingredients: hydroxypropyl cellulose (E463), hypromellose type 2910 (E464), iron oxide yellow (E172), lactose monohydrate, mannitol (E421), magnesium stearate (E572), sodium starch glycolate, titanium dioxide (E171), and triacetin (E1518).

Do not take this medication if you:

• are allergic to relugolix, estradiol, norethindrone acetate, or any ingredients of this medication
• are breast-feeding
• are or may be pregnant
• are over 35 years of age and have migraine headaches with aura
• are over 35 years of age and smoke
• are using a hormonal form of birth control
• have an increased risk for developing hormone-sensitive cancer
• have or have had any blood clotting disorders (e.g., thrombophlebitis, deep vein thrombosis, or pulmonary embolism)
• have or have had cerebrovascular disorders (e.g., stroke)
• have or have had a heart attack, coronary artery disease, or angina
• have uncontrolled high blood pressure
• have osteoporosis
• have, have had, or may have breast cancer or endometrial cancer
• have or have had liver tumours, decreased liver function or liver disease
• have undiagnosed vaginal bleeding
• have eye damage resulting from blood vessel disease of the eye, such as a partial or complete loss of vision
• have an inherited blood clotting problem
• have a thickened lining of the uterus (endometrial hyperplasia)

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• back pain
• decreased interest in sexual activity
• hair loss or thinning
• headache
• heartburn or indigestion
• hot flushes
• increased sweating
• irritability
• joint pain
• night sweats
• unusual or abnormal vaginal bleeding

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

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

• anxiety
• breast changes (e.g., pain and tenderness, lumps, nipple discharge)
• high blood pressure
• mood or mental changes
• signs of a blood clot in the arm or leg (e.g., tenderness, pain, swelling, warmth, or redness in the arm or leg)
• signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
• signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
• sudden, heavy vaginal cramping and bleeding
• symptoms of gall bladder problems (e.g., yellowing of the eyes and skin, dark urine, light-coloured stools)

if any of the following occur:

• signs of a severe allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• signs of a blood clot in the eye (e.g., sudden unexplained partial or complete loss of vision or double vision)
• signs of a blood clot in the lungs (difficulty breathing, sharp chest pain that is worst when breathing in, coughing, coughing up blood, sweating, or passing out)
• signs of a heart attack (e.g., chest pain or pressure, pain extending through shoulder and arm, nausea and vomiting, sweating)
• signs of stroke (e.g., sudden or severe headache; sudden loss of coordination; vision changes; sudden slurring of speech; or unexplained weakness, numbness, or pain in arm or leg)
• thoughts of self-harm or suicide

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Note the following important information about estrogen replacement therapy:

The Women's Health Initiative (WHI) study results indicated an increased risk of heart attack, stroke, breast cancer, blood clots in the lungs, and blood clots in the leg veins in postmenopausal women during 5 years of treatment with 0.625 mg conjugated equine estrogens and 2.5 mg medroxyprogesterone compared to women receiving sugar tablets. Other combinations of estrogen and progestins were not studied. However, until additional data are available, the risks should be assumed to be similar for other hormone replacement products. Therefore,

• estrogens with or without progestins should be used at the lowest dose that relieves your menopausal symptoms for the shortest time period possible, as directed by your doctor; and
• estrogens with or without progestins should not be used to prevent heart disease, heart attacks, or strokes.

Birth control: This medication should not be taken while using hormonal birth control such as birth control pills or implants. It is important to use a non-hormonal method of birth control, such as condoms, while taking this medication and for at least 1 week after the last dose.

Blood clotting disorders: Estrogens with or without progestins are associated with an increased risk of blood clots in the lungs and legs. This risk also increases with age, a personal or family history of blood clots, smoking, and obesity. The risk of blood clots is also increased if you are immobilized for prolonged periods and with major surgery. If possible, this medication should be stopped 4 weeks before major surgery. Talk about the risk of blood clots with your doctor.

Blood pressure: You may experience increased blood pressure when using this medication. Your doctor may want to monitor your blood pressure more frequently while you are using relugolix-estradiol-norethindrone. Ask your doctor how often you should have your blood pressure checked.

Bone health: This medication can cause a decrease in the density of bones that may be permanent. Long-term use is likely to increase the amount of bone lost. If you have risk factors for osteoporosis, such as previous use of other medications that decrease bone density, metabolic bone disease, anorexia, long term use of alcohol or tobacco, or family history of osteoporosis, discuss with your doctor whether any special monitoring is needed.

Depression and suicidal behaviour: This medication can cause mood swings and symptoms of depression. People taking this medication may feel agitated (restless, anxious, aggressive, emotional, and feeling not like themselves), or they may want to hurt themselves or others. Symptoms of depression such as poor concentration, changes in weight, changes in sleep, and decreased interest in activities may also occur. If you experience these side effects or notice them in a family member who is taking this medication, contact your doctor immediately. Your doctor should closely monitor your emotional and behavioural changes while taking this medication. 

If you have depression or a history of depression, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Diabetes: Hormone changes, including hormone replacement therapy, may cause an increase in blood sugar levels (may cause a loss of blood glucose control) and glucose tolerance may change. People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication.

If you have diabetes or are at risk for developing diabetes, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Gallbladder disease: This medication can aggravate gallbladder disease or increase the risk of developing it. If you have gallbladder disease, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Hair changes: This medication can cause hair thinning and hair loss. It is unknown whether these changes are permanent. If you experience hair thinning or hair loss, talk to your doctor.

Heart disease and stroke: Studies indicate an increased risk of heart disease and stroke with estrogen (with or without progestin) replacement. Get immediate medical attention if you experience symptoms of a heart attack (chest pain, tightness or pressure, sweating, nausea, feeling of impending doom) or stroke (sudden dizziness, headache, loss of speech, changes in vision, weakness or numbness in the arms and legs).

High cholesterol or triglycerides: Estrogen may increase triglyceride levels in those who already have high levels. Your doctor will monitor your cholesterol and triglyceride levels while you are taking this medication. If you have a condition known as familial hypertriglyceridemia (a disorder leading to high levels of fats known as triglycerides in the blood), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver disease: People with active liver disease or liver tumours should not use relugolix - estradiol - norethindrone. If you have or have had liver problems, you may require special monitoring by your doctor while you use this medication. Make sure to tell your doctor if you have ever had liver problems. Your doctor may do blood work to monitor your liver function while you are using relugolix-estradiol-norethindrone.

If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Menstrual changes: This medication is likely to cause changes to menstrual bleeding patterns. Many people stop experiencing menstrual bleeding, while others experience predictable menses with lighter bleeding. This can make identifying a pregnancy difficult. If you suspect you may be pregnant, contact your doctor immediately.

If you experience unusual pain or bleeding that is much heavier than usual or is unexpected, you should also contact your doctor immediately.

Surgery: Certain situations such as long-term bed confinement may make blood clots more likely. Discuss with your doctor the risks and benefits of temporarily stopping this medication. If you are scheduled for surgery, let all doctors involved in your care know that you are taking this medication.

Pregnancy: This medication should not be used during pregnancy as it may harm the developing baby. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: This medication may pass into breast milk. Breast-feeding is not recommended while taking relugolix - estradiol - norethindrone and for 2 weeks after the last dose.

Children: The safety and effectiveness of using this medication have not been established for children.

For a full list of interactions, use the Drug Interaction Checker available on the Drugs.com website.

If you are taking other medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.