How does this medication work? What will it do for me?

Tibolone belongs to the class of medications called hormone replacement therapy. It is used to reduce the symptoms of flushing, hot flashes, and night sweats associated with menopause.  Tibolone is intended for women who are postmenopausal (i.e., who had their last menstrual period more than 12 months ago).

Although tibolone is not a hormone, it breaks down in the body to form 3 substances that behave like the hormones estrogen, progesterone, and testosterone. Due to this activity, many of the concerns that were uncovered with research about hormone replacement therapy with estrogen and estrogen plus progestin may also be concerns with the use of tibolone. Estrogen and progesterone are female hormones that are produced by the ovaries. During menopause, the ovaries produce less estrogen and progesterone and symptoms can occur. Tibolone should only be used by women who have an intact uterus, as this medication produces similar effects as progesterone.

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.

What form(s) does this medication come in?

Each tablet contains 2.5 mg of tibolone. Nonmedicinal ingredients: ascorbyl palmitate, lactose monohydrate, magnesium stearate, mannitol, and potato starch.

How should I use this medication?

The recommended dose of this medication is 2.5 mg (1 tablet) taken by mouth, once daily. It may be taken with or without food and swallowed whole, with some water or other drink. Do not break or chew the tablets.

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 try to take this medication exactly as prescribed by your doctor. Missed doses may cause breakthrough bleeding or spotting.

If you miss a dose, take it as soon as possible and continue with your regular schedule. If it is less than 12 hours until 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 in its original package at room temperature, protect it from light and moisture, and keep it out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Who should NOT take this medication?

Do not take this medication if you:

  • are allergic to tibolone or any ingredients of the medication
  • have abnormal liver test results caused by liver disease or liver problems
  • are breast-feeding
  • are or may be pregnant
  • have a history of known or suspected estrogen-dependent tumours, such as endometrial or uterine cancer
  • have, are suspected to have, or have had breast cancer
  • have active liver disease, with blood tests that have not returned to normal
  • have endometrial hyperplasia (thickening of the inner lining of the uterus)
  • have or have had blood clots (such as deep vein thrombosis or a pulmonary embolism) or active thrombophlebitis (inflammation of the legs)
  • have or have had stroke, heart attack, or coronary heart disease
  • have health conditions that increase the risk of blood clots (such as certain inherited blood clotting disorders)
  • have partial or complete loss of vision from blood vessel disease of the eyes
  • have porphyria
  • have unusual vaginal bleeding that has not been checked by a doctor

What side effects are possible with this medication?

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.

  • acne
  • appetite changes
  • breast pain or discomfort
  • breast swelling
  • changed interest in sexual activity
  • dizziness
  • fatigue
  • hair loss
  • headache
  • irregular menstrual bleeding, spotting
  • itchy skin
  • joint or muscle pain
  • nausea
  • pain during sexual activity
  • rash
  • skin darkening
  • unnatural hair growth
  • upset stomach
  • vomiting
  • weight changes

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:

  • breast changes or breast lumps
  • decreased reflexes
  • fluttering or pounding heartbeat
  • increased blood pressure (e.g., headache, stronger or faster heartbeat, chest pain, dizziness, excessive tiredness, blurred vision)
  • memory loss
  • migraine
  • mood changes (e.g., depression, irritability, nervousness)
  • pain, numbness, or pins-and-needles sensations
  • pain or difficulty urinating
  • signs of a blood clot in the arm or leg (tenderness, pain, swelling, warmth, or redness in the arm or leg) or lungs (difficulty breathing, sharp chest pain that is worst when breathing in, coughing, coughing up blood, sweating, or passing out)
  • 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)
  • stomach, abdominal, or pelvic pain
  • symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
  • urinary tract infection (e.g., increased need to urinate, pain in pelvis or lower back, increased need to urinate at night, blood in urine, burning with urination)
  • unexplained or heavy vaginal bleeding
  • vaginal infections (e.g., discharge, itching, irritation)
  • vision changes, including blurred vision

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of an allergic skin reaction (e.g., red or purple skin patches with blister or crusting, swollen lips, mild itching, or burning)
  • signs of heart attack (e.g., crushing chest pain, chest heaviness, shortness of breath, shoulder or arm pain, unexplained 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)

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.

Are there any other precautions or warnings for 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.

Since tibolone is broken down into estrogen, progesterone, and testosterone, many of the concerns that were uncovered with research about hormone replacement therapy with estrogen and estrogen plus progestin may be concerns with the use of tibolone.

Note the following important information about hormone 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 for 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
  • estrogens with or without progestins should not be used to prevent heart disease, heart attacks, or strokes

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 you are going to have surgery, talk to your doctor about the risk of blood clots and whether you should stop this medication temporarily.

Blood pressure: Women may experience increased blood pressure when using tibolone. Talk to your doctor about how often you should have your blood pressure checked. If you have high blood pressure, 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.

Bone disease: If you have bone disease due to cancer or a metabolic condition causing too much calcium in your body, 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.

Breast and ovarian cancer: Studies indicate an increased risk of breast and ovarian cancer with the use of combined estrogen and progestin therapy. Women who have a history of breast cancer should not use estrogens. Women with a family history of breast cancer or women with a history of breast lumps, breast biopsies, or abnormal mammograms should be closely monitored by their doctor if they use estrogens. Women should have a mammogram before starting hormone replacement therapy. Women taking estrogens should have regular breast examinations and should be taught how to do a breast self-examination.

Cholesterol: This medication may affect levels of cholesterol and triglycerides. If you have high blood cholesterol levels, 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.

Dementia: Women over age 65 receiving combined estrogen and progestin replacement therapy may be at increased risk of developing dementia (loss of memory and intellectual function). If you are over 65, talk to your doctor about whether you should be tested for dementia.

Diabetes: Tibolone 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.

Endometrial cancer: Medications causing estrogen-like effects increase the risk of cancer of the endometrium (lining of the uterus) for women who have had menopause. Breakthrough bleeding or spotting may occur during the first 6 months of taking tibolone, however if any unusual vaginal bleeding continues or occurs after this time, it is important to contact your doctor immediately, to rule out endometrial cancer.

Fibroids: This medication may worsen fibroids by causing sudden enlargement, pain, or tenderness. If you notice these effects, contact your doctor.

Fluid retention: Tibolone may cause fluid retention, and worsen heart disease, high blood pressure, kidney disease, or asthma. Talk to your doctor if you have any concerns. If you experience worsening of these conditions while using this medication, contact your doctor. 

Follow-up examinations: It is important to have a follow-up examination 3 to 6 months after starting this medication to assess the response to treatment. Examinations should be done at least once a year after the first one.

Galactose intolerance/glucose malabsorption:  Tibolone is prepared with lactose. If you have lactose or galactose intolerance you should not take this medication.

Gallbladder: 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.

Heart disease: Studies indicate an increased risk of heart disease with estrogen (with or without progestin) for postmenopausal women. As this medication has estrogen-like activity, it may also increase this risk. If you experience symptoms of a heart attack (chest pain, tightness or pressure, sweating, nausea, feeling of impending doom) while taking this medication, get immediate medical attention.

Liver disease:  If you have liver 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. See your doctor as soon as possible if you develop signs of liver problems such as yellow eyes or skin, abdominal pain, dark urine, pale stools, or itchy skin.

Migraine: People who are at risk of experiencing migraine may have an increased frequency of migraines while taking tibolone. If you have migraines with aura, 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. If you develop severe headaches, usually on one side of the head, with or without visual changes, talk to your doctor as soon as possible.

Seizures: There have been reports of seizures occurring with hormone replacement therapy. If you have a history of epilepsy or medical conditions that increase the risk of seizures, 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.

Stroke: Tibolone increases the risk of stroke caused by reduced blood flow to the brain. The risk of this occurring increases with age. This is consistent with research that demonstrated estrogen and estrogen plus progestin also increase the risk of stroke. If you experience symptoms of stroke (sudden dizziness, headache, loss of speech, changes in vision, weakness or numbness in the arms and legs) while taking this medication, get immediate medical attention.

Systemic lupus erythematosus (Lupus): Women with lupus may find that this medication causes a flare-up of lupus symptoms. If you have been diagnosed with lupus, 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. 

Thyroid disease: This medication may affect how thyroid hormone is used by the body. If you are taking thyroid hormone for an underactive thyroid gland, 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. 

Pregnancy: This medication should not be used during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: Breast-feeding should be avoided while taking this medication.

Children: The safety and effectiveness of using this medication have not been established for children. This medication is not intended for use by children or adolescents.

What other drugs could interact with this medication?

There may be an interaction between tibolone and any of the following:

  • anastrozole
  • anticoagulants (e.g., apixaban, dabigatran, dalteparin, enoxaparin, rivaroxaban, tinzaparin, warfarin)
  • aprepitant
  • ascorbic acid (vitamin C)
  • "azole" antifungals (e.g., fluconazole, itraconazole, ketoconazole, voriconazole)
  • bosentan
  • carbamazepine
  • celecoxib
  • cobicistat
  • conivaptan
  • corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
  • cosyntropin
  • cyclosporine
  • dantrolene
  • deferasirox
  • diabetes medications (e.g., canagliflozin, glyburide, insulin, linagliptin, liraglutide, metformin, rosiglitazone)
  • diltiazem
  • dronedarone
  • efavirenz
  • etravirine
  • exemestane
  • heparin
  • HIV protease inhibitors (e.g., atazanavir, darunavir, lopinavir, ritonavir, saquinavir)
  • hyaluronidase
  • lamotrigine
  • lenalidomide
  • lumacaftor and ivacaftor
  • macrolide antibiotics (e.g., clarithromycin, erythromycin)
  • mifepristone
  • modafinil
  • phenobarbital
  • phenytoin
  • primidone
  • protein kinase inhibitors (e.g., crizotinib, dabrafenib, imatinib, nilotinib, ribociclib)
  • rifabutin
  • rifampin
  • ropinirole
  • St. John's wort
  • sarilumab
  • somatropin
  • thyroid replacements (e.g., desiccated thyroid, levothyroxine)
  • tocilizumab
  • ursodiol
  • verapamil

If you are taking any of these 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.

Medications other than those listed above may interact with this medication. 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.

All material copyright MediResource Inc. 1996 – 2021. Terms and conditions of use. The contents herein are for informational purposes only. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Source: www.medbroadcast.com/drug/getdrug/Tibella