Ledibon Tab 2.5 mg 28 shtx3

Description

Composition
Active substance:
1 tablet contains: 2.5 mg tibolone.
Excipients:
Lactose monohydrate (micronized) – 12.5 mg, lactose monohydrate (direct compression lactose) – 74.5 mg potato starch – 9.5 mg ascorbyl palmitate – 0.5 mg magnesium stearate – 0.5 mg.
Description:
White to off-white flat round tablets, engraved with “e” on one side.
Product form:
Tablets of 2.5 mg. 28 tablets in a blister of PVC / PVDC / AI. 1 or 3 blisters are placed in a cardboard box, together with instructions for medical use.
Contraindications
Pregnancy and breast-feeding.
Period of less than a year after the last menstrual period.
Diagnosed (including history) of breast cancer or suspected it.
Diagnosed (including history) estrogen-dependent malignant tumors (eg endometrial cancer) or suspicion on them.
Vaginal bleeding of unknown etiology.
Untreated endometrial hyperplasia.
Thrombosis (venous or arterial) and thromboembolism present or in history (including thrombosis and deep vein thrombophlebitis, pulmonary embolism, myocardial infarction, ischemic or hemorrhagic cerebrovascular accident).
Diagnosed thrombophilic state (e.g., a deficiency in protein C, S or antithrombin III protein) (see. The “Special instructions”).
State prior thrombosis (including transient ischemic attack, angina pectoris), at present or in history.
Expressed or multiple risk factors for venous or arterial thrombosis (including atrial fibrillation, complicated lesions valvular and subacute bacterial endocarditis; uncontrolled hypertension; advanced surgery, accompanied by prolonged immobilization, major trauma, obesity (body mass index> 30 kg / m2), smoking at the age of 35 years).
Cardiovascular failure decompensation.
Acute liver disease or a history of liver disease, after which no liver function returned to normal.
Liver failure.
Malignant or benign tumor of the liver (including liver adenoma) currently or history.
Porphyria.
Otosclerosis, occurred during a previous pregnancy or use of hormonal contraceptive pills in history.
Mounted hypersensitivity to the active substance or auxiliary substance any drug.
Rare hereditary disease: galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption
Carefully
If any of the following conditions / diseases has now been observed previously and / or exacerbate during pregnancy or previous hormone therapy, the patient should be under close medical supervision. Such conditions / diseases include: leiomyomas (uterine fibroids) and / or endometriosis; cardiovascular failure decompensation without signs; the presence of risk factors, estrogen dependent tumors (e.g., the presence of breast cancer in the immediate family (mother, sister)); controlled hypertension; increasing the concentration of cholesterol in the blood; disorders of carbohydrate metabolism, diabetes, both in the presence and 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 preparations.
It should be taken into account that these conditions / diseases may recur or worsen during treatment with tibolone.
Dosage
2.5 mg
Indications
Treatment of estrogen deficiency symptoms in postmenopausal women; Prevention of osteoporosis in postmenopausal women at high risk of fractures and intolerance of other groups of drugs used for the prevention of osteoporosis.
Interaction with other drugs
Tibolone enhances fibrinolytic activity of blood that can lead to increased anticoagulant action of anticoagulants, particularly warfarin, the warfarin dose should therefore be appropriately adjusted by
INR (international normalized ratio). The simultaneous use of tibolone and anticoagulants must be controlled, particularly at the beginning and end of drug treatment Ledibon®. There is limited information regarding pharmacokinetic interactions with tibolone treatment. In vivo study demonstrated that the combined use of tibolone in a small degree affects the pharmacokinetics of a substrate of cytochrome P450 3A4 Midazolam.
Accordingly, the possible presence of drug interactions with other substrates of CYP3A4. Medications Inductors CYP3A4, such as barbiturates, carbamazepine, hydantoins and rifampicin, can increase the metabolism of tibolone and thus affect its therapeutic effect. Preparations containing St. John’s wort (Hypericum perforatum), may enhance the metabolism estrogen and progestin by induction of isoenzyme CYP3A4.
Increased metabolism of estrogens and progestins may reduce their clinical effect and change in the profile of uterine bleeding.
Overdose
At the same time taking a large number of Ledibon® tablets, seek medical advice.
Main symptoms: malaise, nausea or vaginal bleeding.
Treatment: symptomatic.
pharmachologic effect
Pharmacological group:
Estrogen.
Pharmacodynamics:
pharmacodynamics
For oral reception tibolone is rapidly metabolized to form three compounds that determine the pharmacodynamic characteristics of the drug
Ledibon®. Two metabolites of tibolone (3 alpha gidroksitibolon and Zbeta-gidroksitibolon) possess estrogen-like activity, whereas the third metabolite – delta 4 isomer of tibolone has gestagenopodobnoy and androgen activity.
The drug restores Ledibon® estrogen deficiency in postmenopausal women, facilitating related to their lack of symptoms, such as vasomotor disturbances ( “tides”, increased sweating at night), irritability, dryness and discomfort in the vagina, mood and libido decrease, etc..). Ledibon® prevents bone loss after menopause or ovariectomy.
Pharmacokinetics:
After receiving oral tibolone is rapidly absorbed. As a result, rapid metabolism, tibolone plasma concentrations are very low. Maximum plasma concentrations of metabolites 3alpha-gidroksitibolona and 3beta-gidroksitibolona higher but accumulation does not occur. The concentration of delta-4 isomer is very low in plasma.
Therefore, a series of pharmacokinetic parameters can not be determined.
Tibolone excretion occurs mainly in the form of conjugated metabolites (mainly sulfated). Part of the drug is excreted by the kidneys, most of the output through the intestines. Food intake has no significant effects on the extent of absorption. Pharmacokinetic parameters of tibolone and its metabolites are not dependent on renal function.
Pregnancy and breast-feeding
Use of the drug Ledibon® during pregnancy and breast-feeding is contraindicated. In case of pregnancy, treatment with Ledibon® should be discontinued immediately.
Conditions of supply of pharmacies
On prescription.
side effects
* CNS: dizziness, headache, visual disturbances, depression. From the digestive system: diarrhea, increase in liver transaminases, part of the endocrine system: changes in body weight, edema, increased hair growth on the face. On the part of the reproductive system: metrorrhagia, endometrial proliferation. Dermatological reactions: seborrheic dermatosis, rash, itching. On the part of the musculoskeletal system: pain in the back, arms and legs, arthralgia * A list of all side effects presented in the medical instructions.
special instructions
Ledibon® The drug is not intended for use as a contraceptive and does not protect against pregnancy. The decision to start taking the drug Ledibon® should be based on an assessment of the ratio of “risk / benefit” with all the individual risk factors, and in women older than 60 years should also take into account the increased risk of stroke.
It should be prescribed only on the symptoms that adversely affect quality of life for the treatment of postmenopausal symptoms drug Ledibon®. In all cases, at least once a year to carry out a thorough risk assessment and therapeutic use, and should continue therapy with Ledibon® only in the period of time when the benefits of therapy outweigh the risks. It is necessary to carefully assess the risk of stroke, breast cancer and endometrial cancer risk of cancer for each woman with an intact uterus (see. Section “Side effects”), taking into account all the individual risk factors, the incidence and characteristics of both cancers and stroke, in terms of izlechivaemosti , morbidity and mortality.
Evidence of the relative risks associated with hormone replacement therapy (HRT) or the use of tibolone for the treatment of premature menopause, limited. However, the benefit / risk ratio in women with premature menopause may be more favorable than in older women, due to the low level of absolute risk in younger women.
Medical inspection / observation
Before starting or resuming therapy with Ledibon® should collect a personal and family medical history.
Physical exam (including pelvic examination and mammary glands) must take into account anamnesis data, the absolute and relative contraindications. During therapy, preventive repeated examinations are recommended, the frequency and nature of which are determined by the individual characteristics of the patient, but at least 1 time in 6 months. In particular, women should be informed of the need to doctor message on changes in the mammary glands. Surveys, including the corresponding imaging techniques, such as mammography, be carried out in accordance with the current time of the received inspection circuit adapted to clinical needs of each patient, but at least 1 every 6 months.
Reasons for immediate discontinuation and immediate treatment to the doctor
Therapy should stop in case of contraindications and / or under the following conditions / diseases: -zheltuha or impairment of liver function; -vnezapnoe increase in blood pressure, characterized by normal blood pressure exponent characteristic of the patient; -vozniknovenie headaches such as migraines.
Hyperplasia and endometrial cancer
Data from randomized controlled clinical trials are contradictory, but these observational studies have shown an increased risk of endometrial hyperplasia or cancer in women taking tibolone (see. Also section “Side effects”). These studies showed that the risk of endometrial cancer increases with increasing duration of use of the drug. tibolone can increase the endometrial thickness, measured by transvaginal ultrasonography.
During the first months of treatment may experience “breakthrough” bleeding and spotting.
When bleeding / bleeding during treatment Ledibon® drug that ‘continued longer than 6 months from the start of dosing, -nachinayutsya 6 months after the beginning of the preparation and use Ledibon® continue even after the patient has stopped the use of the drug Ledibon® necessary consult your doctor – this may be a sign of endometrial hyperplasia.
Mammary cancer
These various clinical studies in terms of evidence-based medicine in relation to breast cancer risk when taking tibolone contradictory, and further research is needed.
ovarian cancer
Ovarian cancer is much less common than breast cancer. Long-term (at least 5-10 years) estrogen substitution monotherapy was associated with a small increased risk of developing ovarian cancer.
Some studies, including the study on “Women’s Health Initiative» (WHI) [Women’s Health Initiative], suggest that prolonged treatment with combination therapy for hormone replacement therapy may have the same or a slightly lower risk.
In “explore the millions of women,” it has been shown that the relative risk of developing ovarian cancer when used tibolone was similar to the risk associated with the use of other types of HRT.
venous thromboembolism
Formulations for HRT containing only estrogen or combined preparations containing estrogen and progestogen may increase the risk of venous thromboembolism (VTE) (i.e., deep vein thrombosis or pulmonary embolism) in 1.3-3 times and especially during the first year of application (see. section “Side effects”).
According to epidemiological studies using databases Britain the risk of VTE associated with taking tibolone was lower than the risk associated with conventional HRT, but due to the fact that at that time only a small proportion of women taking tibolone, should not be eliminate the slight increase in risk compared with women not taking tibolone. Patients with known thrombophilic states have an increased risk of VTE and receiving tibolone this risk may increase, however the use of the population of the drug contraindicated patients (see. The section “Contraindications”).
Risk factors for VTE are the use of estrogens, older age, major surgery, prolonged immobilisation, obesity (body mass index (BMI)> 30 kg / m2), pregnancy and the postpartum period, systemic lupus erythematosus, and cancer. Patients after surgery is necessary to pay special attention to preventive measures for VTE prevention in the postoperative period. If necessary, prolonged immobilisation after surgery recommended Ledibon® temporary discontinuation of the drug for 4-6 weeks prior to surgery. Treatment should not be reopened as long as women are not motor activity recovers. Women who have a history of venous thromboembolism is absent, but which are first-degree relatives with a history of thrombosis at a young age, it may be provided a screening (must inform the woman that only part of thrombophilic state is detected at screening). If detected thrombophilic state which is separated from relatives thrombosis or severe disorder (e.g., a deficiency in antithrombin III, protein S, protein C or a combination of disorders) drug contraindicated reception Ledibon® For women who are already receiving anticoagulant therapy requires careful consideration the benefit / risk of HRT or tibolone. If, after the start of treatment is developed VTE, should stop taking the drug.
Patients should be informed about the need for immediate treatment to the doctor if symptoms appear potential thromboembolism (eg, pain and unilateral lower limb edema, sudden chest pain, shortness of breath).
Coronary heart disease (CHD)
In a randomized, controlled trials have not produced evidence of protection against myocardial infarction in women with or without coronary artery disease who were receiving combination therapy HRT (estrogen / gestagen) or preparations containing estrogen only.
Epidemiological studies using GPRD database was not obtained evidence of protection against myocardial infarction in postmenopausal women who received tibolone.
Ischemic stroke
Therapy Tibolone increases the risk of ischemic stroke from the first year of application (see. Section “Side effects”). The absolute risk of stroke is strongly dependent on age, and, therefore, the effect of tibolone is greater, the greater the age. If you have any unexplained migraine headaches with or without visual impairment, you must immediately consult a doctor. In this case, you can not take the drug as long as doctor does not confirm the safety of continuation of HRT, such as headaches may be an early diagnostic sign of a possible stroke.
other conditions
According to reports, the reception tibolone resulted in a significant dose-dependent reduction in HDL cholesterol (high-density lipoprotein) (-16.7% at a dose of 1.25 mg to -21.8% at 2.5 mg after 2 years of use).
Also decreased the total concentration of triglycerides and VLDL. Reducing the concentration of total cholesterol and VLDL cholesterol (very low density lipoproteins) was not dose-dependent. The concentration of LDL cholesterol (low density lipoprotein) remained unchanged. The clinical implications of these findings is still unknown.
Women with pre-existing hypertriglyceridemia should be under close medical supervision while receiving Ledibon® drug, as rare cases of a significant increase in plasma concentrations of triglycerides, contributing to the development of pancreatitis observed during estrogen therapy for a given condition.
tibolone treatment leads to a very small reduction thyroxine binding globulin (TBG) and total T4. Концентрация общего Т3 не изменяется. Ледибон® снижает концентрацию глобулина, связывающего половые гормоны (ГСПГ), тогда как уровни кортикостероидсвязывающего глобулина (КСГ) и циркулирующего кортизола не изменяются.
Следует учитывать повышенный риск развития деменции в случае начала терапии тиболоном у женщин в возрасте старше 65 лет. На фоне приема препарата Ледибон® существует вероятность задержки жидкости. В связи с этим необходимо тщательное наблюдение за пациентками с сердечной или почечной недостаточностью.
ВЛИЯНИЕ НА СПОСОБНОСТЬ УПРАВЛЕНИЯ ТРАНСПОРТНЫМИ СРЕДСТВАМИ И МЕХАНИЗМАМИ
Не отмечено какого-либо отрицательного действия препарата на концентрацию внимания и реакцию, способность управлять транспортными средствами и другими механизмами.
Storage conditions
At temperatures above 25 C, in the original package.
Keep out of the reach of children!.
Dosing and Administration
Препарат Ледибон® следует принимать по истечении 12 месяцев после последней естественной менструации. Если препарат Ледибон® начать принимать раньше указанного срока, то увеличивается вероятность нерегулярных кровянистых выделений/кровотечений из влагалища. Перед началом приема препарата Ледибон® следует исключить злокачественные новообразования органов репродуктивной системы, независимо от того, принимает женщина другой препарат ЗГТ или нет, особенно в случае появления кровянистых выделений из половых путей.
Доза препарата – одна таблетка в сутки.
Коррекции дозы с учетом возраста не требуется. Таблетки необходимо проглатывать, запивая водой, предпочтительно в одно и то же суток.
Блистеры с препаратом Ледибон® маркированы днями недели. Начните приём препарата с приёма таблетки, отмеченной текущим днём. Например, если день приема совпадает с понедельником, то необходимо принять таблетку, отмеченную понедельником, из верхнего ряда блистера. Далее принимайте таблетки, согласно дням недели. Из следующего блистера таблетки принимаются без пропусков и перерывов. Не допускайте пропуска в приёме препарата при смене блистера или упаковки.
При лечении препаратом Ледибон® нет необходимости добавлять гестагенсодержащие препараты.
Если пропущен прием очередной таблетки, дальнейшая тактика зависит от времени опоздания от запланированного времени приема. Если с момента пропуска таблетки прошло меньше 12 часов, необходимо принять пропущенную таблетку, как можно скорее. Если опоздание в приеме таблеток составило более 12 часов, следует пропустить прием, и принять следующую таблетку в обычное время.
Не рекомендуется принимать две таблетки одновременно для восполнения пропущенной дозы!
Переход с циклического или непрерывного режима приема препарата для заместительной гормональной терапии (ЗГТ) на тиболон
При переходе с циклического режима приема препарата для ЗГТ лечение препаратом
Ледибон® необходимо начинать на следующий день после завершения предыдущей схемы лечения. В случае перехода с непрерывного режима приёма комбинированного препарата для ЗГТ лечение можно начинать в любое время.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist