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How to take Tibolone during menopause - instructions for use

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Menopausal syndrome is a common name for a number of interrelated health disorders that occur in women during menopause. In the absence of adequate treatment, menopausal syndrome can lead to such serious diseases as coronary heart disease, dementia, type 2 diabetes mellitus, and osteoporosis. Hormone therapy has long been used to treat menopausal disorders, but often gives unwanted side effects. The use of drugs STEAR (including tibolone) is a new approach to the treatment of menopausal disorders. For drugs of this group is characterized by selective effects on various organs and tissues of the female body. The report on conference "Reproductive health of women: from abortion to contraception"held on September 15, 2011 in Samara, the highest category doctor, gynecologist and endocrinologist Marina Vladimirovna Glukhova substantiated the need for the widespread use of tibolone (including its equivalent, generic Ledibon) in the treatment of menopausal disorders.

At the beginning of his speech head. Department of Gynecology "JSC SDTs", gynecologist-endocrinologist of the highest category, because M. Sc. Mv Glukhova reported alarming statistics.

In the world, 25 million women come to menopause every year, and only 10% of them have no pathological manifestations. According to WHO forecasts, by 2015, 46% of women in the world will experience menopausal disorders of varying severity. In Russia, almost 40 million women have already reached menopause. And, as reported by the highest category gynecologist-endocrinologist, by 2020, demographers expect an increase of this figure by another 20 million. At the same time, Russia lags far behind countries with a high standard of living (Japan, Australia, Sweden, etc.). The climacteric period is a natural biological process of transition from the reproductive period to old age. It is time-consuming and includes the gradual extinction of ovarian function, the last independent menstruation (menopause), a decrease in the level of estrogen. But the climacteric syndrome should be distinguished from the climacteric period - a complex of pathological symptoms accompanying the menopausal period. “What are we afraid of in the 21st century?” - asked the rhetorical question of M.V. Glukhov. “We fear cardiovascular disease, dementia, type 2 diabetes and osteoporosis.” All these diseases can occur as complications of menopausal syndrome. In the modern world, the social and economic well-being of a woman largely depends on her health and physical fitness. “That is why we must choose this type of therapy in order to ensure the safety and optimal quality of life for our women,” she said. Glukhov.

Menopause and menopausal syndrome

For menopause is characterized by a decrease in the level of estrogen. It begins after 45 years, and by 52-53 years, the estrogen content is reduced to a minimum level that persists in the future. Meanwhile, the physiological effects of estrogen are extremely diverse. They affect the central nervous system, the heart and blood vessels, the state of the bone tissue, skin, mucous membranes and hair, the urogenital system and the mammary glands, and the metabolism of lipids in the body. Thus, a sharp decrease in estrogen production has a significant impact on many organs and systems. The climacteric period includes several phases. Premenopause usually occurs between the ages of 45 and 47, from the appearance of the first symptoms of menopause to the cessation of independent menstruation. Menopause is considered premature if it occurs between the ages of 37-39 years, and early if it occurs in 40-45 years. The normal age of menopause is about 50 years. Natural and artificial menopause is distinguished, the latter may be associated with surgery, exposure to radiation, cytostatics and other causes. Perimenopause is a period that chronologically combines premenopause and the first year of postmenopause. The selection of this period is due to the fact that regular menstruation can sometimes appear after a considerable period of time (up to 1-1.5 years) from the moment of their termination. Climacteric syndrome begins with neuro-vegetative and psychoemotional disorders, and in the long run it can lead to osteoporosis, cardiovascular disease and Alzheimer's disease. To prevent such unfortunate consequences, it is necessary to begin to deal with the menopausal syndrome at the onset of its first symptoms, which include hot flushes. During tides, body temperature can rise by 5 ° C in just a few minutes. The duration of the "tide" ranges from 30 seconds to 3 minutes, and their frequency can reach up to 30 times a day. "Tides" are accompanied by profuse sweating. Often there are sympathoadrenal crises, fluctuations in blood pressure. According to the speaker, 75% of women suffer from "hot flashes" and other disorders within 3-5 years after the cessation of menstruation, about 10% - more than 5 years, and in 5% of women "hot flashes" continue until the end of life.

There are a number of other symptoms of menopausal syndrome. The blood supply to the mucous membranes deteriorates, sexual intercourse can become painful, urinary incontinence, frequent urination, and urgent urges can occur. More rare symptoms include numbness and tingling in the limbs or their tremors, crawling on the skin, muscle pain, shortness of breath and feeling of lack of air, bronchospasm, dryness or burning sensation in the mouth, various unpleasant taste, as well as "dry" conjunctivitis, stomatitis and laryngitis.

In the future, we can expect more serious consequences: the development of osteoporosis, dyslipidemia and atherosclerosis, increase in weight and redistribution of male-type fat, decrease in cognitive abilities.

Hormone therapy and its evolution

Mv Glukhova sees hormone replacement therapy (HRT) as a very effective method for treating climacteric disorders. It simultaneously eliminates all the symptoms of menopausal syndrome, and the effectiveness of the prevention of osteoporosis by this method has been proven in randomized studies. HRT eliminates vasomotor manifestations, symptoms of depression, insomnia, and prevents the development of urogenital atrophy. This method of therapy has a positive effect on connective tissue, which allows you to remove joint and muscle pain in the back, cure "dry" conjunctivitis, and has a positive effect on the skin. Prevention of osteoporosis can not only reduce the frequency of spinal and hip fractures, but also reduce the periodontal disease and the associated loss of teeth. It has also been proven to reduce the incidence of colorectal cancer under the influence of HRT.

The speaker described the evolution of treatment methods for menopausal disorders. In the 1920s. Phytoestrogens were first used; in the 1940s, “pure” estrogens; in the 1970s, combination therapy with estrogens and progestogens appeared, and in the 1990s, drugs of the STEAR group.

The principle of modern HRT is to reduce the possible risks of treatment, therefore only natural estrogens (17- (3-estradiol) are used in minimal effective doses, while the patient’s hormone dose decreases with age. In women with an intact uterus, estrogens are combined with progestogens (combination therapy) The drug is selected individually. Before the appointment of therapy, a special examination is carried out, during therapy - annual monitoring. In addition to women with menopausal disorders, HRT is recommended for patients, I have risk factors for osteoporosis or decreased bone density, women with premature menopause, women after removal of the ovaries and / or uterus. HRT is not indicated for women over 65 years of age, and also solely for the prevention of cardiovascular disease or Alzheimer's disease in the absence climacteric disorders. There are a number of contraindications for hormone replacement therapy. It is not prescribed for a history of breast cancer, currently or if it is suspected, for estrogen-dependent cancers. nnyh tumors (cancer of the endometrium or suspicion of this pathology), bleeding from the genital tract of unknown etiology, if untreated endometrial hyperplasia. HRT is also contraindicated in cases of deep vein thrombosis, pulmonary embolism, angina pectoris, myocardial infarction (all of these diseases, both at the time of treatment, and in history, are contraindicated for HRT), uncompensated arterial hypertension, liver diseases in the acute stage, allergies to active substances in the acute stage, active substances, active substances that are active substances, liver disease in the acute stage, allergies to active substances. to any of the fillers of the drug, skin porphyria. Indications for the use of HRT are vegetative-vascular symptoms and psycho-emotional disorders of mild and moderate in the period of pre- and post-menopause: "hot flashes", excessive sweating, dizziness, headaches, insomnia, hyperexcitability. Premenopause and early postmenopause (no later than 5-7 years after the last menstruation) is the “window” of the therapeutic possibilities of HRT. There are various types of hormonal therapy: parenteral drugs - estradiol (patch) and estradiol (gel), topical preparations (for example, vaginal cream), but most commonly used oral drugs are combinations of estradiol with didrogesterone (Femoston), estradiol with levonorgestrel (Klimonorm) , estradiol with drospirenone (Angelique), as well as tibolone.

STEAR - a new approach to treatment

The main part of his report is a gynecologist-endocrinologist of the highest category M.V. Glukhova devoted precisely tibolone to the drug, including its generic equivalent Ledibon. Earlier, since 2003, he was included in the group of drugs “other sex hormones”, and later, since 2009, he was transferred to the group “other estrogenic drugs.” Tibolone is a member of the STEAR (Selective Tissue Estrogenic Activity Regulator) group of drugs. The use of drugs STEAR is a fundamentally new approach to the treatment of menopausal disorders. The goal of this approach is not the total replacement of deficient hormones, but the selective regulation of estrogenic activity in tissues. Tibolone is an estrogen stimulant.

The principle of action of STEAR preparations is that estradiol or its analogs stimulate estrogen receptors (receptor level), and at the pre-receptor level, tissue enzymes activate or inhibit the synthesis of active forms of estrogen directly in the tissue. Tibolone metabolism provides the effect of the drug on the body sulphatase-sulfotransferase system. “In young women, this system is in balance, but in women of mature, menopausal age, the activity of the enzyme sulfatase predominates,” said M.V. Glukhov. Metabolites block sulfatase and activate the sulfotransferase system. The clinical effects of the drug tibolone are diverse. These include treatment of symptoms of menopausal disorders, a beneficial effect on the cardiovascular system, elimination of the symptoms of urogenital atrophy, and prevention of postmenopausal osteoporosis. An important effect of tibolone is improved mood and libido. Unlike some other drugs, it does not stimulate the mammary glands, does not increase the mammographic density 1, does not stimulate the proliferation of the endometrium 2. If two of the three metabolites of tibolone are stimulators of estrogenic activity, the third metabolite (delta-4-isomer), which is formed in the endometrium, has an exclusively progestogenic effect. At the same time, there are no tibolone metabolites in the endometrium that bind to estrogen receptors, which is explained by the activity of enzymes already described at the pre-receptor level. In this regard, an important advantage of Tibolone is the absence of bleeding.

Advantages of the drug Tibolone (Ledibon)

The main advantage of the STEAR group of drugs (including tibolone) is that they have a selective effect on estrogenic activity in the tissues (the fundamental difference between the drugs of this group). As a result, favorable estrogenic effects are achieved in the central nervous system, bone tissue and the urogenital tract and there is no undesirable estrogenic effect in the endometrium and mammary glands, which avoids the risk of developing tumors (traditional HRT is widely criticized for its ability to increase the incidence of breast cancer glands), as well as engorgement and tenderness of the mammary glands. With fibrocystic mastopathy and mastalgia, tibolone not only does not interfere with the treatment, but also contributes to it.

Hormone therapy for climacteric disorders improves the quality of life for women. “Of course, for women, a good mood and a positive effect of therapy on appearance are important,” said M.V. Glukhov. In terms of the quality of life of patients, treatment with tibolone is comparable to combined HRT. Reception of tibolone improves the emotional background of patients who have undergone a long course of treatment (10-12 months) with this drug 3, there is an increase in the level (3-endorphins ("joy hormones"). The positive effect of this drug on the sexual life of a woman has also been established, and its effect increases both the frequency of initiative and satisfaction. In this regard, tibolone is more effective than traditional HRT 4. In addition, the drug has a positive effect on the appearance of patients. Tibolon increases the mass of braids This tissue is very important because fat accumulation contributes to the development of various diseases in women who have reached menopause. Tibolone improves the hydration of the body. Tibolone is indicated for the use of vegetative-vascular and psycho-emotional disorders typical of for menopausal syndrome mild to moderate: hot flashes, excessive sweating, dizziness, headaches, sleep disturbances, increased excitability.

The positive effect of the drug on the hormonal status of women after hysterectomy was also noted. Tibolon is recommended to apply already in the early postoperative period - in the first three days after surgery. Therapy for 3 months after surgery resulted in a decrease in FSH by 1.31.6 times and an increase in E2 by 2.0-2.2 times. If you begin therapy in the long term after surgery, the effectiveness of Tibolone decreases. In this case, significant changes in hormonal markers are achieved only after 6-12 months of therapy.

One of the main advantages of the drug tibolone is a positive effect on bone tissue. According to a British study, over 10 years, bone mineral density (BMD) in tibolone-treated patients has not only not decreased, but even increased (both in the lumbar region and in the femoral neck area). In contrast, in the control group, the IPC steadily and significantly decreased with age 5.

Conclusion

Summing up his speech, M.V. Glukhova noted: a comparison of the use of tibolone and combined HRT suggests that these two types of therapy are equally effective in treating menopausal syndromes and preventing osteoporosis. Tibolone is more effective for improving mood and libido, for obtaining sexual satisfaction. Unlike combined HRT, this drug does not stimulate endometrial proliferation, does not cause bleeding. Thibolon also does not stimulate breast tissue, does not increase mammographic density, does not contribute to breast engorgement. When taking tibolone, the patient's failure rate for therapy due to side effects is much lower than when using combined HRT. The use of drugs STEAR (in particular Tibolone) is the most physiological, and therefore the safest means of treating menopausal disorders.
Responding to questions from the audience, the speaker noted the complete equivalence of tibolone and generic drug Ledibon, which has a similar therapeutic effect.

Tibolon action

The drug has estrogenic, progestin, androgenic activity, stimulates the pituitary gland, the hypothalamus. What it is? Combined medication containing hormones of the first and second phases of the menstrual cycle. Despite the fact that during menopause only estrogen is lacking. The cumulative combined effect causes the body to produce the required amount of hormones of the first phase, reduces the amount of progesterone. The hormonal background is restored, the symptoms of menopause are eliminated. The presence in the preparation of the hormone of the second phase prevents the development of cancer cells with prolonged use.

Tibolon is designed to eliminate, prevent the symptoms of menopause, osteoporosis. It is necessary to begin treatment after consultation with a specialist. The basis for therapy are:

  • tides
  • excessive sweating
  • headache,

  • fainting
  • nervousness,
  • insomnia,
  • weakness,
  • unstable emotional state
  • decreased libido
  • vaginal dryness
  • pain during intercourse.

Application

Тиболон выпускается в форме таблеток. They must be taken once a day, preferably at the same time, before going to bed. Wash down with plenty of water. The treatment is long with short breaks or cyclical. During therapy, it is recommended to be examined every six months. One course of treatment is 3 months. Immediately stop treatment if:

  • vaginal bleeding appears,
  • severe headache
  • pressure jumps

  • there are clear signs of impaired liver, kidney, heart.

Overdose is determined by the disorder of the gastrointestinal tract - nausea, vomiting, diarrhea, abdominal pain, etc. As well as an allergic reaction on the skin. Symptomatic treatment. Stop taking the drug for a while, reduce the dose or replace it with another.

Tibolon should be started on treatment after 1 month after menstruation. Otherwise, bleeding occurs. The same situation may occur when skipping several pills at once. If you forgot to drink 1, the actions are as follows:

  • take as soon as possible the next pill to drink on schedule,
  • if more than 24 hours have passed, skip, drink the next one at the scheduled time.

Tibolon is not addictive. However, a break in treatment is necessary. Periodically, you should check the work of the pancreas, liver, kidneys.

Contraindications

Substitution treatment can not be taken in some cases:

  • in the presence or suspicion of breast cancer,
  • cancer or developmental tendency,
  • with vaginal bleeding of unclear etymology,

  • hypersensitivity to the drug,
  • thrombosis, thrombophlebitis,
  • otosclerosis,
  • porphyrias,
  • endometrial hyperplasia in the present, past,
  • liver disease.

The treatment is carried out under the supervision of a physician in patients with problems in the work of the heart, kidneys, gastrointestinal tract.

Side effects

Mainly manifested in the first months of therapy:

  • nausea,
  • anorexia,
  • drowsiness or insomnia,
  • loose stools
  • abdominal pain,
  • dizziness,
  • weakness,

  • bad taste in the mouth
  • headache,
  • irritability,
  • excitability of the nervous system
  • puffiness
  • blurred vision
  • joint pain,
  • depression,
  • weight gain.

Reviews of women indicate the disappearance of symptoms without discontinuing therapy for 3 months of treatment. If the side effects are too pronounced, you must contact your doctor.

Drug cost

The tool can be purchased at the pharmacy by prescription. Price depends on the location of the pharmacy. The average cost of a package with 28 tablets for 1 month of treatment is 2500 rubles.

The drug is quite expensive, many women prefer to buy an analog. It is advisable to immediately discuss this issue with your doctor. Tibolone counterparts include:

  • Velledien,

  • Ledibon,
  • Livial.

Mechanism of action

It is a drug with androgenic, gestogennoe and estrogenic activity. It stimulates the pituitary and hypothalamus. The medication contains hormones produced in the body during the first and second phases of the cycle.

Closer to the approach of menopause in women there is a decrease in the concentration of estrogen only. The combined effect makes it possible to begin the forced synthesis of hormones of the first phase and suppress the production of progesterone. Due to this, the hormonal background is normalized and the severity of menopausal symptoms decreases. The drug can also prevent the onset of a malignant process, but only in the case of prolonged treatment.

Composition and release form

The active ingredient of the drug is tibolone. In addition, it contains the following components:

  • lactose,
  • potato starch,
  • ascorbyl palmitate,
  • magnesium stearate.

The drug is available in the form of white round flat tablets. Their edges are slightly sloping.

Indications for use

Reception of Tibolon is made in order to prevent or eliminate the clinical manifestations of menopause, as well as for the treatment and prevention of osteoporosis. The use of the drug is shown in the following cases:

  • tides
  • excessive sweating
  • mood swings
  • decrease in sexual desire
  • weakness,
  • vaginal dryness,
  • the appearance of pain during intimacy.

Dosage and administration

Tablets need to be taken once a day. It is recommended to perform this procedure at the same time, closer to going to bed, and drink plenty of water. Therapy is long, cyclical or with minor interruptions. The course of treatment involves taking the medication for three months.

The use of the drug should be immediately abandoned in the event of the following changes:

  • severe headaches
  • vaginal bleeding of unknown etiology,
  • malfunction of the heart, kidneys and liver.

In case of overdose, a violation of the gastrointestinal tract is noted. At the same time, vomiting, nausea, diarrhea and pain in the abdomen are noted. In addition, there are manifestations of allergies on the skin. Therapy in this case completely stop or reduce the dosage.

Begin taking the medication a year after the end of menstruation. Earlier therapy may lead to the onset of bleeding. Similar changes are also observed with unsystematic use of the drug. Therefore, in cases where a woman forgot to take a pill, you need to take it as soon as possible. If the day has passed, then just take the next schedule.

The medication is not addictive, but the break between courses is done without fail. The effect of Tibolon on bone tissue is noted. In addition, in the process of therapy you need to monitor the activity of the kidneys, pancreas and liver.

Interaction with other drugs

The instructions for the drug does not say that it can not be taken in combination with other drugs. Nevertheless, it is noted that Tibolon enhances fibrinolytic blood activity and thereby potentiates the effect that coagulants have. In addition, the drug contributes to a decrease in glucose tolerance and thereby increases the need for medicines of the hypoglycemic group.

It is noted that the activity of the drug decreases when it is taken in combination with the following drugs:

The effect of Tibolon on Midazolam pharmacokinetics was revealed.

Analogs means

Among the analogues of the drug Tibolon are the following:

As many reviews indicate, their use also manages to achieve the desired result. At the same time, it is strictly prohibited to replace one medicine with another without the consent of the doctor. The drug is selected on an individual basis after a comprehensive examination.

Tibolon is an effective drug that can eliminate the unpleasant symptoms characteristic of menopause. With its systematic use marked a significant improvement. Menopause occurs with the smallest number of clinical manifestations. The main thing is not to resort to self-treatment and agree on the tactics of therapy with a gynecologist.

What is a drug?

Armed with the physicians is Tibolon, a synthetic drug that is indispensable in the period of natural and surgical menopause. This drug is very effective as a prophylactic against osteoporosis in case of estrogen deficiency.

The drug perfectly stimulates the vaginal mucosa, reduces the severity of symptoms caused by menopause, eliminates the irritability and anxiety that often accompany menopause, prevents osteoporosis from developing.

Tablets are packaged in 28 pieces, each - 2.5 mg.

How to take medication?

Taking the pills during the course of treatment differs in that, as recommended by Tibolon's instructions for use, they must be used in a strict sequence:

  1. The treatment begins with a pill taken from the top row marked with a frame. A pill is taken, labeled exactly on the day when the course of therapy began.
  2. The following tablets should be used one per day, taking from the package only in the direction indicated by the arrow. So one needs to drink until the pills run out.
  3. It is necessary to take inside without chewing, and to make it a rule - at the same time every day.

Women note that the condition is much improved in a few weeks. But you can not stop treatment, because only prolonged treatment can really help, and this period is not less than 3 months. This recommended dose can be used for a longer period.

Climax occurs when hormones are not produced by the body in the proper amount, so scientists are looking for a way out using hormone replacement therapy. Tibolone in this case is the most reliable and safe drug. This synthetic steroid has the following properties:

The drug appeared on the market more than 20 years ago and is actively sold in more than 70 countries around the world. At first it was prescribed for the treatment of osteoporosis, but then it was noticed that women over the age of 50 who used the medicine felt much better. Therefore, relying on such pharmacological properties, the medicine has been translated and registered as a drug that helps in the treatment of menopausal syndrome.

Climacteric symptoms of varying severity can occur in almost 75% of women, and 25% of them very difficult to endure this period, suffering from various manifestations.

This difficult period includes several stages:

  1. Premenopause, which originates a few years before the last menstruation occurs, and its termination occurs in postmenopausal women.
  2. Menopause. That time when the last menstruation occurred.
  3. Postmenopause. Comes after a year, its duration - until the end of life.

The first stage occurs at about 46 years old, when the production of sex hormones begins to fall gradually, and ovulation becomes impossible. First of all, the level of gestagens, which regulate menses, decreases. Because menstruation is broken. When the body stops grabbing estrogen, hot flushes, excessive sweating, frequent and severe headaches, poor sleep, irritability can occur. At the same time begin problems with the heart, blood vessels, digestive tract. Many are beginning to rapidly gain weight.

The second stage begins at an average of 52-53 years. This is the time when the level of follicle-stimulating hormone starts moving upwards. The ovaries begin to shrink, shrink. In 60-year-old women, the ovaries weigh 2 times less than young ones.

All of these symptoms usually last after menopause for 5 years and then disappear. They are replaced by dryness and discomfort in the vagina, with urination there is pain.

Pathologies begin in the bones and vessels, atherosclerosis, heart attack, hypertension can develop. More often at this time there is a stroke and diabetes. The bones at this age are more fragile, and therefore fractures occur more often. If the changes occur in the muscles of the pelvic floor, then there may be a prolapse, and then loss of both the uterus and the vagina, and this leads to incontinence of urine with a sharp strain.

The most striking manifestations of menopause that most disturb a woman are:

  • hot flashes: during this short but very unpleasant time, the sensation of heat occurs, the skin in the area of ​​the face, neck, chest may blush,
  • heartbeat, in which there are interruptions in heart rhythm, shortness of breath,
  • perspiration, especially at night,
  • change in the mucous membrane of the vagina, it becomes thin and dry, which is reflected in the absence of sexual desire, pain occurs during sexual intercourse,
  • the appearance of weakness and chills,
  • changeable mood, especially irritation, anxiety,
  • poor sleep at night, daytime sleepiness.

This is where Tibolon comes to the rescue thanks to its metabolites, which affect a wide variety of organs and tissues. Once inside the body of a woman, it forms metabolites that resemble steroid receptors, such as estrogen, progesterone and, in a weaker form, androgen.

Different types of metabolites in each organ and in tissues are concentrated in the right quantities. And the bone tissue and the vagina get a positive effect equal to the estrogenic one. In the endometrium tablets show their properties as a gestagen.

Often during menopause chest pain may occur. But in the mammary gland, Tibolone is able to produce a powerful inhibition of sulfatase and some other positive effects, which will make the process of turning estrone sulfate into estrone, and then into estradiol, impossible.

These unique qualities of Tibolon allowed him to be distinguished into a special class of medicines that successfully regulate estrogenic activity.

Tibolon perfectly extinguishes hot flashes or effectively weakens them, relieves anxiety, eliminates headache, psychological instability in behavior.

Hot flashes become less, and therefore the mood improves, sleep becomes more sound. This is due to the fact that the active ingredient of the drug affects the beta-endorphins, increasing their concentration.

Tibolon affects the state of the vagina due to its estrogenic effect. The drug helps cell maturation, which reduces vaginal dryness, and female sexuality begins to rise along with sexual fantasies and orgasms. The drug changes the level of hormones, thereby improving the quality of life in all aspects, improves mood.

During this period, uterine bleeding may occur in women, but Tibolon causes bleeding twice as much as other drugs, and mostly in the early postmenopausal period, and for this reason, the drug should not be taken for patients who experience menopause for less than a year.

The bone tissue medication affects due to estrogenic activity, which increases the bone mineral density in the femoral neck and lumbar spine.

Opinion of experts

Reviews of doctors about Tibolon treatment come down to one thing - treatment should be carried out under the supervision of specialists. Every six months you need to explore the hormones, periodically take a break.

With prolonged use of the drug increases the risk of cancer education, thrombosis, hypertension.

Given the feedback from doctors, we can say that it is advisable to start treatment when the symptoms of menopause are pronounced, significantly spoils the quality of life.

pharmachologic effect

The drug for the treatment of menopausal syndrome, does not cause regular withdrawal bleeding. Stabilizes the work of the hypothalamic-pituitary system in menopause, which is achieved due to estrogenic, progestogenic and weak androgenic properties of the drug.

In postmenopausal women, tibolone at a daily dose of 2.5 mg inhibits the secretion of gonadotropins without stimulating the proliferation of the endometrium, prevents bone loss in the postmenopausal period, reduces the degree of vasomotor disorders (tides, increases sweating), has a positive effect on libido and mood, and stimulating effect on the vaginal mucosa. In fertile women, the drug inhibits ovulation.

Interaction with other drugs

While taking tibolone with anticoagulants at the same time, it is possible to enhance the effects of the latter (a decrease in the content of fibrinogen, an increase in the concentration of antithrombin III, plasminogen, and an increase in plasma fibrinolytic activity). Tibolone metabolism can be accelerated and, therefore, its activity can be reduced while taking drugs that induce enzymatic systems.

TIBOLON, tibolone - instructions for use of the medicine


Anabolic steroid. It has estrogenic, progestogenic and weak androgenic activity, stabilizes the hypothalamic-pituitary system after the ovarian function stops, causes a decrease in the secretion of gonadotropic hormones.

Inhibits bone resorption in the postmenopausal period, alleviates such manifestations of menopausal syndrome, such as blood flushes to the skin of the face, increased sweating, and headaches. A positive effect on libido and mood (increases the concentration of central and peripheral opioids).

It has a stimulating effect on the mucous membrane of the vagina without stimulating the proliferation of the endometrium. In fertile women suppresses ovulation.

It prevents the development of osteoporosis, reduces the concentration of phosphates and calcium in the serum.

Climax (natural or due to oophorectomy).

Prevention of climacteric osteoporosis.

Inside at a dose of 2.5 mg / day (at the same time), the minimum duration of treatment is 3 months. The drug is started 1 year after the last menstruation or immediately after surgical menopause.

From the side of the central nervous system: dizziness, headache.

From the digestive system: diarrhea, increased liver transaminase activity, change in body weight.

On the part of the endocrine system: increased facial hair growth, metrorrhage, endometrial proliferation.

Other: swelling of the legs, seborrheic dermatosis, pain in the back, arms and legs.

Pregnancy, hormone-dependent tumors (including suspicion of them), thrombophlebitis, thromboembolism (includinghistory), vaginal bleeding of unknown etiology, liver failure, cardiovascular failure, cerebrovascular disorders, otosclerosis, arising from pregnancy or with steroids, a period of less than 1 year after the last menstruation.

Contraindicated in pregnancy.

Contraindicated in liver failure.

Use caution in renal failure.

Use caution with renal failure, carbohydrate metabolism, hypercholesterolemia, epilepsy.

Not intended for use as a contraceptive. In the course of treatment, it is possible to increase the sensitivity of patients to anticoagulants due to increased fibrinolytic activity of the blood.

When symptoms of thromboembolism, jaundice, or persistent pathological changes in liver function tests occur, treatment is stopped.

During the period of treatment, regular monitoring of appropriate laboratory parameters in patients with hypercholesterolemia, renal failure, and diabetes mellitus is necessary. The treatment may reduce the concentrations of total and free T4 and thyroxin-binding globulin.

Enhances the effect of anticoagulants.

Tibolon - instructions for use, dose, side effects, contraindications


Clinico-pharmacological group:

Hormones of the hypothalamus, pituitary, gonadotropins and their antagonists

Included in the list (Order of the Government of the Russian Federation No. 2782-p dated December 30, 2014): ATC: Pharmacodynamics:

Tissue-specific estrogen receptor agonist-antagonist. As an agonist, tibolone acts on lipid metabolism and bone tissue, in relation to the endometrium and mammary glands acts as an antagonist.

In the endometrium has a progestogenic effect, and in the brain - estrogenic and androgenic.

Thus, it eliminates vasomotor symptoms, without having a proliferative effect on the mammary glands and endometrium.

Inhibits bone resorption in the postmenopausal period, reduces the concentration of phosphates and calcium in the blood serum, in the blood plasma - prevents the development of osteoporosis, softens the manifestations of menopausal syndrome - blood flushes to the skin of the face, headaches, increased sweating. Increasing the concentration of central and peripheral opioids has a positive effect on libido and mood.

It has a stimulating effect on the cells of the vaginal mucosa, without causing proliferation of the endometrium. Reduces the concentration of calcium and phosphate.

Does not cause menstrual bleeding.

After ingestion, the stomach is completely absorbed in the gastrointestinal tract. The maximum plasma concentration of tibolone metabolites is reached after 1 hour.

Metabolism in the liver.

The elimination half-life makes 7 h. Elimination with excrements and partially kidneys. Indications:

It is used to treat menopausal disorders caused by natural or surgical menopause, and is used to prevent osteoporosis associated with estrogen deficiency.

Hepatic failure, thrombophlebitis, hormone-dependent tumors, a period of less than 1 year from the last menstruation.

Pregnancy and lactation:

Recommendations for the FDA - category C. Contraindicated in pregnancy and lactation.

Dosage and administration:

Inside 2.5 mg / day at the same time of day.

The highest daily dose: 2.5 mg.

The highest single dose: 2.5 mg.

Central and peripheral nervous system: headache, dizziness.

Cardiovascular system: swelling of the legs.

Digestive system: dyspepsia, diarrhea.

Dermatological manifestations: seborrheic rash, increased facial hair growth.

Dysfunction of the gastrointestinal tract.

Enhances the effect of anticoagulants, reduces glucose tolerance.

The simultaneous use of liver microsomal enzymes with inducers reduces the activity of the drug by accelerating its metabolism.

The drug has no contraceptive effect.

Tibolone (Tibolone) instructions, the use of the drug


Pharmacotherapeutic group G03DC05 - hormones of the sex glands and the means used in the pathology of the genital sphere. Progestin

Basic pharmacological action:

  • Stabilizes the hypothalamic-pituitary system during menopause, when the functioning of the ovaries stops,
  • The central effect is due to a combination of hormonal properties of the drug (estrogenic, progestogenic and weak androgenic) Tibolone at a daily dose of 2.5 mg inhibits the secretion of gonadotropins in postmenopausal women and inhibits ovulation in fertile women, in this dose, tibolone does not stimulate endometrium in postmenopausal women,
  • Only a few patients showed a slight proliferation of the endometrium, the extent of which did not grow with an increase in the duration of the drug intake, a stimulating effect on the vaginal mucosa was also observed,
  • It has been proven that this dose of tibolone prevents bone mass loss in the postmenopausal period,
  • Menopausal disorders and especially vasomotor disturbances, such as hot flashes and sweating, are also suppressed.
  • Tibolon has a positive effect on libido and mood.

INDICATIONS: menopausal sm (syndrome).

Dosage and administration:

  • Tibolon is desirable to take at the same time of day,
  • The dose is 1 tbl / day of BNF (recommendation for the use of drugs in the British National Formulary, 60th edition) improvement is achieved within a few weeks, but the best results are observed with treatment for at least 3 months at the recommended dose Tibolone can last longer.

Side effects when using drugs: change in body weight, dizziness, seborrheic dermatosis, vaginal bleeding, headache, upset stomach, changes in liver function, increased facial hair growth, swelling of the legs.

Contraindications to the use of drugs:

  • Pregnancy and Lactation,
  • A hormone-dependent tumor or suspicion of its presence (breast cancer, endometrial cancer) is diagnosed as SS (cardiovascular) or cerebrovascular disorders (thrombophlebitis, thromboembolic disorders at the moment or in anamnesis),
  • Vaginal bleeding of unknown etiology of the occurrence or complication of the course of otosclerosis during pregnancy or steroids, impaired liver function,
  • Hypersensitivity to lactose and other components of the drug.

Drug release forms: tab. (Tablets) 2.5 mg

Visa-mode with other drugs

When taking tibolone, patients may become more sensitive to anticoagulants h / by increased blood fibrinolytic activity (decreased fibrinogen level, increased concentration of antithrombin III, plasminogen, and increased plasma fibrinolytic activity. Changes in these parameters are caused by steroids with hormonal activity, these parameters return to their original level after canceling drug.

Features of use in case of insufficiency of internal organs

Dysfunction of the certzovascular system: Contraindicated in SS (cardiovascular) disorders.
Violation of the function Pechinky: Contraindicated.
Renal dysfunction No special recommendations.
Dysfunction of the respiratory system: No special recommendations.

Features of use in children and the elderly

Children, 12 years: No special recommendations.
Elderly and senile age: No special precautions for rozdrukuvati


A remedy for the treatment of menopausal syndrome, does not cause regular withdrawal bleeding. Stabilizes the work of the hypothalamic-pituitary system during menopause, which is achieved due to estrogenic, progestogenic and weak androgenic properties of tibolone.

Tibolone is rapidly metabolized to form three compounds that provide its pharmacotherapeutic effect.

Two metabolites, 3α-OH-tibolone and 3β-OH-tibolone, have predominantly estrogenic activity, and the third, the delta-4-isomer, has progestogenic and weak androgenic activity.

After ingestion, tibolone is rapidly and completely absorbed. Due to rapid metabolism, Tibolone plasma levels are very low. The maximum plasma concentrations of tibolone metabolites are reached 1–1.5 hours after administration.

Excretion of tibolone occurs mainly in the form of metabolites. A small amount is excreted in the urine, and most of it in the bile and feces. The half-life of metabolites is approximately 7 hours without subsequent accumulation.

Symptoms of natural or surgical menopause, prevention of osteoporosis with estrogen deficiency.

Inside 2.5 mg / day, preferably at the same time of the day. Improvement occurs within a few weeks, but the best results are observed with continued treatment for at least 3 months. At the recommended dose, tibolone can be continued for a long time.

special instructions

Tibolon is not a contraceptive. Tibolon should be prescribed immediately after the onset of surgical menopause and no earlier than 1 year after natural menopause (last menstruation).

It is not recommended to exceed the recommended daily dose due to the possibility of bloody discharge from the vagina.

While taking tibolone, it is necessary to carry out medical monitoring of patients with migraine, epilepsy, diabetes, renal dysfunction and hypercholesterolemia, as well as in the presence of these diseases in history.

Interactions

While taking tibolone with anticoagulants, it is possible to enhance the effect of the latter (a decrease in fibrinogen level, an increase in the concentration of antithrombin III, plasminogen, and an increase in plasma fibrinolytic activity). Tibolone metabolism can be accelerated, and, consequently, its activity can be reduced while taking inductors of microsomal liver enzymes.

The phenomena of acute tibolone poisoning are mild, usually with a slight overdose of toxic manifestations is not observed. Possible violations of the digestive tract. No specific treatment is required.

Description and use of the drug


Tibolon Tibolon: instruction and application
Russian nameTibolon

Latin substance name Tibolon

Chemical name

Gross formulaC21H28O2

Pharmacological group of substances Tibolon

Estrogens, gestagens, their homologs and antagonists

Nosological classification (ICD-10)M82.1 Osteoporosis with endocrine disorders (E00-E34 +)

N95.1 Menopausal and menopausal status in women

CAS code5630-53-5

Pharmacology

Pharmacological action - estrogen-progestin. It also has mild androgenic and anabolic activity. It eliminates climacteric changes in the hypothalamic-pituitary system. Reduces FSH and LH in menopausal women. In fertile women, it inhibits ovulation. It has a stimulating effect on the vaginal mucosa.

Prevents osteoporosis, reduces the level of phosphate and calcium in serum. Reduces the severity of climacteric autonomic dysfunction (hot flashes, increased sweating, headaches), improves libido and psycho-emotional state (increases the level of central and peripheral opioids).

After ingestion is rapidly and completely absorbed from the gastrointestinal tract.

Biotransformed to form three pharmacologically active metabolites: 3-alpha-OH-tibolone and 3-beta-OH-tibolone possess predominantly estrogenic activity, the delta4-isomer of tibolone has progestogenic and weak androgenic activity. Cmax of 3-alpha-OH- and 3-beta-OH-metabolites are reached in 1–1.5 h, T1 / 2 - about 7 h, do not accumulate.

It is displayed mainly in the form of metabolites, mainly with feces, a small amount - with urine.

Application of the substance Tibolon
Menopause (natural and surgical), osteoporosis with estrogen deficiency (prevention).

The drug is contraindicated in:

  • Hypersensitivity, hormone-dependent tumors (or suspicion of them), vaginal bleeding of unknown etiology, thrombophlebitis and thromboembolism (including in history), severe impairment of liver function, cardiovascular insufficiency, cerebrovascular disorders,
  • Otosclerosis, arising during pregnancy or with steroids,
  • In the period of less than 1 year after the last menstruation, untreated endometrial hyperplasia, porphyria, pregnancy, breast-feeding.

Restrictions on the use of
Leiomyoma, endometriosis, history of endometrial hyperplasia, renal failure, carbohydrate metabolism, hypercholesterolemia, epilepsy, migraine or severe headaches, systemic lupus erythematosus, bronchial asthma.

Use during pregnancy and lactation

Use during pregnancy is contraindicated. In the event of pregnancy during the use of the drug treatment should be stopped immediately.

Use during breastfeeding is not recommended.

Side effects of TibolonFrom the nervous system and sensory organs: headache, dizziness, blurred vision, depression. For the digestive tract: nausea, diarrhea, increased activity of hepatic transaminases. From the urogenital system: metrorrhagia, endometrial proliferation.

Other: swelling of the legs, pain in the back, arms and legs, change in body weight, increased growth of hair on the face, skin itching, rash, seborrheic dermatitis.

The drug enhances the effect of anticoagulants, increases the need for hypoglycemic agents (reduces glucose tolerance). Activity decreases with simultaneous use of rifampicin, carbamazepine.

Overdose

Symptoms: dysfunction of the gastrointestinal tract.

Dosage and administration
Inside, without chewing, on 2.5 mg once a day (at the same time of day).

The first is taken a tablet from the top, circled in the frame of the row, which is marked by the day corresponding to the day of the start of reception, the next - in the direction indicated by the arrow.

Do not take a double dose to replace the missed. Improvement is achieved within a few weeks, the optimal course of treatment is 3 months or more.

Precautions substances Tibolone

Do not take the drug in the period before the expiration of 12 months after the last natural menstruation.

If you start taking the drug before the specified time, then the likelihood of irregular bleeding / bleeding from the vagina increases.

Regular monitoring of appropriate laboratory parameters in patients with hypercholesterolemia, impaired renal function and diabetes mellitus is necessary. It should be borne in mind that against the background of tibolone may decrease levels of total and free thyroxin and thyroxin-binding globulin.

When symptoms of thromboembolism, jaundice, or persistent pathological changes in liver function tests occur, treatment is stopped.

Year of last adjustment: 2010

Instructions farm group, which includes


Tibolone Estrogens, gestagens, their homologs and antagonists

Russian name: Tibolon.
English name: Tibolone.

Estrogens, gestagens, their homologs and antagonists.

M82.1 Osteoporosis with endocrine disorders (E00-E34 +).
N95.1 Menopausal and menopausal status in women.

Pharmacological action - estrogen-gestagennoe. It also has a mild androgenic and anabolic activity. It reduces menopausal changes in the hypothalamic-pituitary system. It reduces the level of FSH and PH in menopausal women. In fertile women it inhibits ovulation. It has a stimulating effect on the mucous membrane of the vagina. Prevents osteoporosis, reduces the level of phosphates and calcium in the blood serum. Reduces the severity of climacteric autonomic dysfunction (hot flushes, increased sweating, headaches), improves libido and psycho-emotional state (increases the level of central and peripheral areas, and increases the central and peripheral levels of peripherals and peripherals.

After ingestion is rapidly and completely absorbed from the gastrointestinal tract.

Biotransformed to form three pharmacologically active metabolites: 3-alpha-OH-tibolone and 3-beta-OH-tibolone possess predominantly estrogenic activity, the delta-4 isomer of tibolone has progestogenic and weak androgenic activity.

Cmax of 3-alpha-OH- and 3-beta-OH-metabolites are reached in 1–1.5 h, T1 / 2 - about 7 h, do not accumulate. They are eliminated mainly as metabolites, mainly with faeces, a small amount - with urine.

Menopause (natural and surgical), osteoporosis with estrogen deficiency (prevention).

Hypersensitivity. Hormone-dependent tumors (or suspicion of them). Vaginal bleeding of unknown etiology. Thrombophlebitis and thromboembolism (including history). Severe violation of the functions of the liver.

Cardiovascular insufficiency. Cerebrovascular disorders, otosclerosis. Occurred during pregnancy or when treated with steroids, in a period less than 1 year after the last menstrual period. Untreated endometrial hyperplasia. Porphyria.

Leiomyoma, endometriosis, history of endometrial hyperplasia, renal failure, carbohydrate metabolism, hypercholesterolemia, epilepsy, migraine or severe headaches, systemic lupus erythematosus, bronchial asthma.

Use during pregnancy is contraindicated. In case of pregnancy during the use of the drug, treatment should be stopped immediately.
Use during breastfeeding is not recommended.

From the nervous system and sensory organs: headache, dizziness, blurred vision, depression. On the part of the digestive tract: nausea, diarrhea, increased activity of hepatic transaminases. From the genitourinary system: metrorrhagia, endometrial proliferation.

Other: swelling of the legs, pain in the back, arms and legs, change in body weight, increased growth of hair on the face, skin itching, rash, seborrheic dermatitis.

Enhances the effect of anticoagulants, increases the need for hypoglycemic agents (reduces glucose tolerance). The activity decreases with the simultaneous use of rifampicin, carbamazepine.

Symptoms: dysfunction of the gastrointestinal tract.
Treatment: symptomatic.

You should not take the drug in the period before the expiration of 12 months after the last natural menstruation. If you start taking the drug earlier than the specified period, then the likelihood of irregular bleeding / bleeding from the vagina increases. Regular monitoring of appropriate laboratory parameters in patients with hypercholesterolemia, impaired renal function and diabetes mellitus is necessary. It should be borne in mind that, against the background of tibolone, a decrease in the levels of total and free thyroxin and thyroxin binding globulin is possible.

When symptoms of thromboembolism, jaundice, or persistent pathological changes in liver function tests occur, treatment is stopped.


Ladybon

From white to almost white, flat, round tablets, engraved with “e” on one side.

Pharmacological action - estrogen.

When taken orally, tibolone is rapidly metabolized to form 3 compounds that determine the pharmacodynamic characteristics of Ledibon®. Two metabolites of tibolone (3α-hydroxytibolone and 3β-hydroxytibolone) possess estrogen-like activity, while the third metabolite, δ4-isomer of tibolone, has gestagen-like and androgen-like activity.

Ledibon® supplements estrogen deficiency in postmenopausal women by alleviating symptoms associated with their deficiency, such as vasomotor disorders (hot flashes, increased sweating at night), irritability, dryness and vaginal discomfort, decreased mood, and libido. Ledibon® prevents bone loss after menopause or removal of the ovaries.

After oral administration, Tibolone is rapidly absorbed. As a result of rapid metabolism, plasma concentrations of tibolone are very low. Cmax in plasma of metabolites of 3α-hydroxy-tibolone and 3β-hydroxy-tibolone is higher, but accumulation does not occur. The concentration of δ4-isomer in plasma is very low. Therefore, a number of pharmacokinetic parameters cannot be determined.

The removal of tibolone occurs in the form of conjugated metabolites (mainly sulfated). Part of the drug is excreted by the kidneys, the majority is excreted through the intestines. Eating does not have noticeable effects on the degree of absorption. The pharmacokinetic parameters of tibolone and its metabolites do not depend on renal function.

  • Treatment of symptoms of estrogen deficiency in postmenopausal women,
  • Prevention of osteoporosis in postmenopausal women with a high risk of fractures and intolerance to other groups of drugs used to prevent osteoporosis.
  • Installed hypersensitivity to the active substance or any excipient of the drug,
  • Period less than a year after the last menstruation,
  • Diagnosed (including a history of) breast cancer or suspicion of it,
  • Diagnosed (including in history) malignant estrogen-dependent tumors (for example endometrial cancer) or suspicion of them,
  • Bleeding from the vagina of unknown etiology,
  • Untreated endometrial hyperplasia,
  • Thrombosis (venous or arterial) and thromboembolism at present or in history (including thrombosis and deep vein thrombophlebitis, deep pulmonary thromboembolism, myocardial infarction, ischemic or hemorrhagic cerebrovascular disorders),
  • Diagnosed thrombophilic conditions (for example, deficiency of protein C, protein S, or antithrombin III) (see "Special Instructions"),
  • The states preceding thrombosis (including transient ischemic attacks, angina), now or in history,
  • Severe or multiple risk factors for venous or arterial thrombosis (including
  • Atrial fibrillation, complicated valvular heart disease and subacute bacterial endocarditis, uncontrolled arterial hypertension,
  • Extended surgical intervention, accompanied by prolonged immobilization, extensive trauma, obesity (body mass index> 30 kg / m2), smoking over the age of 35)
  • Cardiovascular insufficiency in the stage of decompensation,
  • A history of acute liver disease or liver disease, after which the liver function indicators did not return to normal,
  • Liver failure,
  • Malignant or benign liver tumors (including liver adenoma) at present or in history,
  • Porphyria,
  • Otosclerosis, which occurred during a previous pregnancy or when using hormonal contraceptive drugs in history,
  • Rare hereditary diseases: galactose intolerance, Lapp's lactase deficiency or glucose-galactose malabsorption,
  • Pregnancy,
  • Breastfeeding period.

If any of the conditions / diseases listed below are present, observed previously and / or exacerbated during pregnancy or previous hormone therapy, the patient should be under the close supervision of a physician. These conditions / diseases include:

  • Leiomyoma (uterine fibroma) and / or endometriosis,
  • Cardiovascular failure without signs of decompensation,
  • The presence of risk factors for estrogen-dependent tumors (for example, the presence of breast cancer in the immediate family (mother, sister),
  • Controlled arterial hypertension,
  • Increasing the concentration of cholesterol in the blood,
  • Disorders of carbohydrate metabolism, diabetes mellitus, both in the presence and in the absence of complications,
  • Cholelithiasis,
  • Migraine or severe headache
  • Systemic lupus erythematosus,
  • Endometrial hyperplasia in history
  • Epilepsy,
  • Bronchial asthma,
  • Renal failure
  • Otosclerosis, not associated with pregnancy or previous use of hormonal contraceptive drugs.

It should be appreciated that these conditions / diseases may recur or worsen during tibolone treatment.

Use of the drug Ledibon® during pregnancy and breastfeeding is contraindicated. In the event of pregnancy, treatment with Ledibon® should be stopped immediately.

This section describes the undesirable effects that were recorded during 21 placebo-controlled studies (including the study “Assessing the effect of Tibolone on the incidence of new vertebral fractures in postmenopausal women with osteoporosis” ([Long Term Intervention on Tibolone (LIFT) with the participation of 4079 women who received therapeutic doses (1.25 or 2.5 mg) of tibolone, and 3476 women who received a placebo. The duration of treatment in these studies ranged from 2 months to 4.5 years. The following are undesirable effects that were statistically significantly more frequent with tibolone than with placebo.

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