Velledien Tab 2.5 mg 28 pcs

Description

Composition
Active substance:
1 tablet contains: Tibolone – 2.50 mg ;.
Excipients:
Lactose monohydrate – 69.44 mg, Microcrystalline Cellulose – 17.36 mg, ascorbyl palmitate – 0.20 mg maize starch – 10.00 mg Magnesium 0.50 mg stearat-.
Description:
Round, Valium white pills.
Product form:
Tablets of 2.5 mg. 28 tablets in a blister of PVC / Al foil. 1 blister together with instructions for use placed into cardboard pack.
Contraindications
Pregnancy and lactation; Diagnosed (including a history of) breast cancer or suspected it and diagnosed (including history) estrogen-dependent cancers (e.g., cancer of the endometrium) or suspicion of them; vaginal bleeding of unknown etiology; Thrombosis (venous and arterial) and thromboembolism present or in history (including thrombosis and deep vein thrombophlebitis, pulmonary embolism), ischemic heart disease, myocardial infarction, ischemic and hemorrhagic cerebrovascular disorders; state prior thrombosis (including transient ischemic attack, angina, now or in history); detection of predisposition to venous or arterial thrombosis, including resistance to activated protein C, protein C deficiency, protein S deficiency or antithrombin III, phospholipids antibodies (antibodies to cardiolipin, lupus anticoagulant); multiple or severe venous or arterial thrombosis risk factors, including complicated lesions valvular atrial fibrillation, cerebrovascular disease, or coronary artery; uncontrolled hypertension; extended surgery with prolonged immobilization, major trauma, smoking at the age of 35 years, obesity with a body mass index> 30 kg / m2; malignant or benign tumors (including – liver adenoma); now or in history; liver failure, acute liver disease or a history of liver disease, after which the indicators are not normalized liver function tests; hypersensitivity to the drug or any of its components; porphyria; otosclerosis, occurred during a previous pregnancy or use of hormonal contraceptive pills in history; Chronic heart failure (III-IV FC), cerebrovascular disorder; period of at least 1 year after the last menstrual period; untreated endometrial hyperplasia; rare hereditary disease: galactose intolerance, 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. It will be appreciated that these conditions / diseases may recur or deteriorate during treatment with Velledien, in particular: leiomyoma (uterine fibroids), or endometriosis; cardiovascular failure decompensation without signs; the presence of risk factors, estrogen dependent tumors (e.g., breast cancer in first-degree relatives); controlled hypertension; hypercholesterolemia; 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.
Dosage
2.5 mg
Indications
Treatment of estrogen deficiency symptoms in postmenopausal women (not earlier than 1 year after the onset of the last menstrual period at natural menopause or after surgical menopause); prevention of postmenopausal osteoporosis in women at high risk of fracture in case of intolerance or contraindication to the use of other drugs for the treatment 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 the INR (international normalized ratio). The simultaneous use of tibolone and anticoagulants must be controlled, especially at the beginning and end of treatment tibolone. 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 (barbiturates, carbamazepine, hydantoin derivatives, rifampicin), while the application may increase the metabolism of tibolone and therefore affect its therapeutic effect. Preparations containing St. John’s wort (Hypericum perforatum) may enhance the metabolism estrogen and progestogen through induction of isoenzyme CYP3A4. Increased metabolism of estrogen and progestogen can lead to a decrease in their clinical effect and change in the profile of uterine bleeding.
Overdose
you can not expect the acute toxicity of tibolone in animals is very low, so the toxic symptoms, even if the patient has taken several tablets at a time. In cases of acute overdose may develop nausea, vomiting, and vaginal bleeding. Antidote is unknown. Recommended symptomatic therapy.
pharmachologic effect
Pharmacological group:
Other estrogens.
Pharmacodynamics:
The drug selectively regulates estrogen-like activity in the tissues and is a tissue selective control. Its pharmacodynamic properties are determined by the action of three pharmacologically-active metabolites of tibolone: ​​gidroksitibolon 3-alpha- and beta-3-gidroksitibolon possess estrogen-like activity, delta-4 isomer progestagenopodobnaya characteristic and weak androgen activity. The drug makes up for deficiency of estrogen in postmenopausal women, facilitating related to their deficiency symptoms – “tides”, depression, sweating at night, headache. Positive effect on the libido and mood (increases the concentration of the central and peripheral opioid). It has a trophic effect on the mucous membrane of the vagina without causing endometrial proliferation. Prevents bone loss following menopause or ovariectomy. Reduces the concentration of calcium and phosphate in blood plasma.
Pharmacokinetics:
After oral administration, tibolone is rapidly and extensively absorbed. Food intake did not significantly affect the absorption of the drug. As a result of the rapid metabolism of tibolone, its concentration in blood plasma is very low. The concentration of delta 4 isomer in plasma is also very low, so a series of pharmacokinetic parameters can not be determined. Maximum plasma concentrations of metabolites 3alpha-gidroksitibolona (3alpha-OH) and 3beta-gidroksitibolona (3beta-OH) above but no accumulation occurs.
Tibolone excretion occurs mainly in the form of conjugated metabolites (mainly sulfated). Portion of the received tibolone excreted by the kidneys, a large part, through the intestines. Pharmacokinetic parameters of tibolone are independent of renal function.
Pregnancy and breast-feeding
The drug is contraindicated in pregnancy and during breastfeeding.
Conditions of supply of pharmacies
Prescription.
side effects
To determine the incidence of side effects of the drug following classification is used:
Very common (> 1/10)
Often (> 1/100 and
special instructions
Velledien The drug is not intended for use as a contraceptive and does not protect against pregnancy. The decision to start taking the drug Velledien should be based on 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. For the treatment of postmenopausal symptoms Velledien drug should be administered only on the symptoms that adversely affect quality of life. In all cases, at least once a year to carry out a thorough risk assessment and therapeutic use, and should continue taking the drug Velledien only when the benefits of therapy outweigh the risks. It is necessary to carefully assess the risk of stroke, the risk of breast and endometrial cancer in every 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 examination / observation
Before starting or restarting reception Vellediena 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 treatment recommended preventive repeated examinations, 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 currently accepted inspection circuit adapted to clinical needs of each patient, but not less than 1 time in 6months.
Reasons for the immediate abolition of the drug and immediate treatment to the doctor
The drug should be stopped in case of contraindications and / or under the following conditions / diseases: jaundice or deterioration of liver function; a sudden increase in blood pressure, characterized by normal blood pressure parameters characteristic of the patient; the occurrence of headache such as migraine.
Hyperplasia and endometrial cancer
These observational studies have shown an increased risk of endometrial hyperplasia or cancer in women taking tibolone. Risk of endometrial cancer increases with the duration of drug application. Tibolone may increase endometrial thickness, measured by transvaginal ultrasonography. During the first months of taking tibolone may experience “breakthrough” bleeding and spotting. When the bleeding / hemorrhage in patients receiving Velledien drug that – lasted for more than 6 months from the start of drug administration – starting 6 months after starting the drug and continue even after its cancellation, a woman should see a doctor – this may be a sign of hyperplasia endometrial
Mammary cancer
These various clinical studies in terms of evidence-based medicine in relation to breast cancer risk when taking tibolone controversial and require further research. According to “Research million women” it revealed a significant increase in breast cancer risk when applying tibolone 2.5 mg (see. The section “Side effect”). This risk became apparent within a few years of the drug and increases with duration of application, returning to baseline within a few years (usually 5 years) after discontinuation of the drug. These results were confirmed in a study using data from a common base (medical) practice (GPRD).
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) suggest that chronic 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 a combination of drugs for hormone replacement therapy containing an estrogen and progestogen may increase the risk of VTE (deep vein thrombosis or pulmonary embolism) 1.3 – 3 times, especially during the first year of application of HRT (see. section “Side effects”). These increase the risk of developing VTE when using tibolone insufficient, but we can not exclude a small increase in risk compared with women not taking tibolone. Patients with known thrombophilic states have an increased risk of VTE and reception Velledien drug can increase this risk, however this population of patients contraindicated drug application (see. The section “Contra ‘). 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. Particular attention should be paid to preventive measures, preventing thrombosis, venous thromboembolism in the postoperative period. Recommended cessation of therapy with Velledien 4-6 weeks prior to surgery, if it is subsequently assumed long-term compliance with bed rest. Treatment should not be resumed until a woman has not recovered motor activity. 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., deficiency of antithrombin III, S protein, protein C or a combination of disorders), the drug Velledien contraindicated. Before the appointment of tibolone women receiving anticoagulants, the physician should carefully evaluate the benefit / risk of HRT or tibolone. If, after the start of treatment is developed VTE receiving the drug should be discontinued. The woman should be informed about the need for immediate treatment to the doctor, if the symptoms appear a potential thromboembolic (unilateral pain and swelling of the lower limb, sudden chest pain, shortness of breath).
Coronary artery disease
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 for hormone replacement therapy containing an estrogen only. Epidemiological studies using GPRD database was not obtained evidence of protection against myocardial infarction in postmenopausal women who received tibolone. Velledien or any other drugs for HRT should not be used for the prevention of cardiovascular diseases.
Ischemic stroke
Admission tibolone increases the risk of ischemic stroke from the first year of application (see. “Side effects” section). 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 use of tibolone resulted in a significant dose-dependent reduction in HDL (high density lipoprotein) (from 16.7% at a dose of 1.25 mg to 21.8% at 2.5 mg after two years of use). Decreased total concentration of triglycerides and lipoproteins. 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) was not changed. The clinical implications of these findings is still unknown.
Estrogens may cause fluid retention, therefore, patients with cardiac or renal failure should be under close medical supervision.
Женщины с уже имеющейся гипертриглицеридемией должны находиться под тщательным наблюдением врача во время терапии тиболоном, так как редкие случаи значительного повышения концентрации триглицеридов в плазме крови, способствующие развитию панкреатита, отмечались во время терапии эстрогенами при данном состоянии.
Прием тиболона может вызвать незначительное снижение концентрации в плазме крови тироксинсвязывающего глобулина (ТСГ) и общего Т4. Концентрация общего Т3 не изменяется. Тиболон снижает концентрацию глобулина, связывающего половыегормоны (ГСПГ), но не влияет на концентрацию кортикостероидсвязывающего глобулина (КГС) и свободного кортизола.
Применение препаратов для ЗГТ не улучшает когнитивную функцию. Имеются данные о повышенном риске возможного развития деменции у женщин при начале непрерывной терапии препаратами для ЗГТ, содержащими только эстрогены, в возрасте после 65 лет (см. раздел «Побочное действие»).
Влияние на способность управления транспортными средствами, механизмами
Не отмечено какого-либо действия тиболона на концентрацию внимания и способность управлять транспортными средствами и другими механизмами.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Препарат Велледиен принимают внутрь по 1 таблетке в сутки, не разжевывая, запивая водой, желательно в одно и то же время, непрерывно. Первой принимается таблетка из ячейки верхнего ряда, отмеченной днем недели, соответствующим дню начала приема. Все остальные таблетки принимаются последовательно из ячеек в направлении стрелки на календарной упаковке, до тех пор, пока не будут приняты все таблетки.
Начало приема препарата Велледиен
Для лечения постменопаузальных симптомов препарат Велледиен необходимо применять только в отношении симптомов, неблагоприятно влияющих на качество жизни женщины. Прием препарата Велледиен начинают не ранее, чем через 12 месяцев после последней менструации при наступлении естественной менопаузы. Пациентки с менопаузой, обусловленной оперативным вмешательством, могут начинать прием препарата сразу же. Во всех случаях, не менее 1 раза в 6 месяцев необходимо проводить тщательную оценку риска и пользы лечения и продолжать применение препарата в период времени, когда польза от терапии превышает риск.
Переход на прием препарата Велледиен после другого препарата для заместительной гормональной терапии (ЗГТ)
Женщинам с интактной маткой, при переходе на прием препарата Велледиен после применения другого препарата ЗГТ, содержащего только эстрогены, рекомендуется сначала вызвать менструальноподобное кровотечение «отмены» путем применения прогестагена для устранения вероятно существующей гиперплазии эндометрия
При переходе с препарата для ЗГТ с циклическим режимом приема, прием препарата Велледиен должен быть начат на следующий день после завершения применения прогестагена. Если переход осуществляется с комбинированного препарата ЗГТ с непрерывным режимом приема, прием препарата Велледиен можно начинать в любое время
Нарушение схемы приема препарата
Пропущенную таблетку, если с момента пропуска прошло менее 12 ч, женщина должна принять как можно скорее в тот же день. Следующая таблетка принимается в обычное время суток. Если опоздание в приеме таблетки составило более 12 ч (интервал с момента приема последней таблетки более 36 ч), принимать пропущенную таблетку не нужно, а следующую таблетку необходимо выпить в обычное 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