Instructions for Ladybone (Tibolone) 2,5 mg
Ladybone is an anti-climacteric estrogenic drug.
Release form and composition Ladybone:
Dosage form - tablets:
round, flat, from white to almost white, on one side with engraving "e" (in a cardboard box 1 or 3 blisters containing 28 tablets, and instructions for the use of Ladybone).
Composition Ladybone of 1 tablet:
active substance: tibolone - 2.5 mg; additional components: potato starch - 9.5 mg; lactose monohydrate (direct compression lactose) - 74.5 mg; lactose monohydrate (micronized) - 12.5 mg; ascorbyl palmitate - 0.5 mg; magnesium stearate - 0.5 mg.
Pharmacodynamics Ladybone:
Ladybone is one of the anti-climacteric drugs.
Ladybone is the active substance of Ladybone, which, due to oral administration, is rapidly metabolized, with the formation of three compounds that determine the pharmacodynamic characteristics of the drug. Two of them (3α- and 3β-hydroxytybolone) have estrogen-like activity, the Δ4-isomer of tibolone (the third metabolite) - exhibits androgen-like and gestagen-like effects. Ladybone helps to replenish the estrogen deficiency in postmenopausal women, while alleviating the symptoms associated with their deficiency, including vasomotor disorders (increased sweating at night, hot flashes), discomfort and dryness in the vagina, irritability, decreased libido, deterioration of mood, etc. The therapy prevents bone loss after ovarian removal or menopause.
Pharmacokinetics Ladybone:
Tibolone is highly absorbed.
Metabolism occurs in the liver with the subsequent formation of hydrophilic products, some of which exhibit pharmacological activity. Excretion of the substance and metabolites is carried out by the kidneys and through the intestines.
Indications Ladybone:
for use Ladybone is prescribed for postmenopausal women in the following cases: estrogen deficiency (treating symptoms); osteoporosis in the presence of a high risk of fractures and intolerance to other groups of drugs Ladybone that are used to prevent osteoporosis (prophylaxis).
Contraindications Ladybone:
Absolute: diagnosed malignant estrogen-dependent tumors, including a burdened history, or suspicion of them; diagnosed breast cancer, including a burdened history, or suspicion of it; a period less than 12 months after the last menstrual period; untreated endometrial hyperplasia; vaginal bleeding of unknown origin; arterial / venous thrombosis and thromboembolism, including a burdened history (including pulmonary embolism, deep vein thrombosis / thrombophlebitis, myocardial infarction, ischemic / hemorrhagic cerebrovascular disorders); diagnosed thrombophlebic conditions.
including protein C, antithrombin III or protein S deficiency; conditions preceding thrombosis, including a burdened history (including angina pectoris, transient ischemic attacks); numerous or pronounced risk factors for arterial / venous thrombosis (including uncontrolled arterial hypertension, atrial fibrillation, complicated lesions of the valvular apparatus of the heart and subacute bacterial endocarditis, extensive trauma, extended surgery, which requires prolonged immobilization, obesity with mass index body more than 30 kg / m 2 ), smoking over the age of 35; Ladybone liver failure; liver disease in an acute course or a history of liver disease, after which liver function indicators did not return to normal; cardiovascular failure in the stage of decompensation; benign / malignant liver tumors (including liver adenoma), including a burdened history; porphyria; otosclerosis that occurred during a previous pregnancy or against the background of the use of hormonal contraceptive drugs in history;
rare hereditary diseases, including Lapp lactase deficiency, galactose intolerance, glucose-galactose malabsorption; pregnancy and lactation; individual intolerance to the components of Ladybon. Relative (Ladyibon is prescribed under medical supervision in cases where any of the following diseases / conditions was observed earlier, is present and / or aggravated during pregnancy or previous hormone therapy):
controlled arterial hypertension; cardiovascular failure without signs of decompensation; increased concentration of cholesterol in the blood; the presence of risk factors for the development of estrogen-dependent tumors (for example, a burdened family history); disorders of carbohydrate metabolism, diabetes mellitus with / without complications; severe headache or migraine; otosclerosis, which is not associated with pregnancy or previous use of hormonal contraceptive drugs; cholelithiasis; a history of endometrial hyperplasia; systemic lupus erythematosus; bronchial asthma; epilepsy; renal failure. Women should take into account the likelihood of recurrence or exacerbation of these diseases / conditions during the period of therapy with.
method and dosage Ladybone:
tablets are intended for oral administration. It is recommended to start treatment 12 months after the last natural period. The use of the drug Ladybone earlier than the specified period leads to an increase in the likelihood of irregular spotting / bleeding from the vagina. Regardless of whether a woman is taking another HRT (hormone replacement therapy) drug or not, malignant neoplasms of the reproductive system should be excluded before the start of the course, especially when bloody discharge from the genital tract appears.
There is no need for additional use of gestagen-containing drugs while taking Ladyibon. The recommended daily dose is 1 tablet. It is advisable to take Ladyibone at the same time of the day. The tablet must be swallowed with water. Blisters with tablets are marked with the days of the week. You need to start using Ladyibon by taking the pill, which is marked by the current day. In the future, the tablets are taken according to the days of the week.
The drug is intended for continuous administration. If you miss taking a pill, you must be guided by the following recommendations (depending on the time that has passed after the pass): less than 12 hours: you need to take the missed dose as soon as possible; more than 12 hours: the reception is skipped, in the future, the woman must take the pill at the usual time. To replenish the missed dose, do not take two tablets at the same time. Women who switch from a cyclic regimen of the drug for HRT to Ladybone should start therapy the next day after the end of the previous treatment regimen. When switching from a continuous mode of use of the combined preparation for HRT, you can start taking Ladyibone at any time.
Side effects Ladybone:
Possible adverse reactions reported in 21 placebo-controlled studies (> 10% - very common;> 1% and <10% - often;> 0.1% and <1% - infrequently;> 0.01% and <0 , 1% - rarely; <0.01% - very rare): digestive system: often - pain in the lower abdomen; reproductive system and mammary gland: often - genital itching, endometrial thickening, vaginal discharge, bleeding / spotting from the vagina, breast pain, pelvic pain, vulvovaginal candidiasis, vulvovaginitis, cervical dysplasia; infrequently - soreness of the nipples, engorgement of the mammary glands, mycosis; skin and subcutaneous tissue: often - increased hair growth, including on the face; infrequently - acne; laboratory / instrumental data: often - deviations in the results of a smear from the cervix, an increase in body weight. In most cases, side effects are mild. The number of cases of cervical pathology (cervical cancer) with the use of Ladybon does not increase in comparison with placebo. Other possible disorders (with an unknown frequency): gastrointestinal disorders (in the form of diarrhea, flatulence), dizziness, headache, migraine, depression, skin rashes, itching of the skin, seborrheic dermatitis, visual disturbances (including blurred vision) , peripheral edema, fluid retention in the body, hepatic dysfunction (including increased transaminase activity), muscle and joint pain. With therapy with combined drugs (estrogen + progestogen) for more than 5 years, there is a twofold increase in the frequency of diagnosing breast cancer. The presence of any increased risk in patients receiving only estrogen or tibolone is significantly lower than the degree of risk observed in women receiving combination drug therapy.
The level of risk is determined by the duration of use. The highest risk of developing endometrial cancer was observed in a randomized, placebo-controlled study, which included women who were not initially scheduled for examination for endometrial pathology. The study design is thus close to the clinical setting. There were no cases of endometrial cancer diagnosed in the placebo group after follow-up for 2.9 years, compared with four cases of endometrial cancer in the tibolone group. This corresponds to a diagnosis of 0.8 additional cases of endometrial cancer per 1000 women who received tibolone for one year in this study.
The relative risk of ischemic stroke does not depend on the duration of Ladybone's administration or age, but the absolute risk is largely determined by age. The overall risk of ischemic stroke in women taking tibolone will be with age. Thus, over a period of five years, the absolute risk is (per 1000 women): age 50–59 years - 3 cases, age 60–69 years - 11 cases. For women taking tibolone during the same period, the following changes can be expected (per 1000 women): age 50–59 years - 4 additional cases, age 60–69 years - 13 additional cases. Other undesirable effects were also noted that are associated with the use of drugs for HRT (combination drugs, estrogen-containing drugs, tibolone), including a slight increase in the risk of developing ovarian cancer.
The relative risk of developing ovarian cancer during the use of tibolone is similar to that with the use of other drugs for HRT. The use of Ladybone is associated with an increase in the relative risk of VTE (venous thromboembolism), ie, deep vein thrombosis and pulmonary embolism, by 1.3–3 times. Most often, this disorder is noted during the first year of tibolone therapy. There is evidence of a slight increase in the risk of coronary heart disease in patients over 60 years of age receiving combined HRT. It is believed that the same violation can be observed with the use of Ladybone. Other possible deterioration in health: increased blood pressure, chloasma, vascular purpura, skin diseases, erythema nodosum, erythema multiforme, pancreatitis, gallbladder disease (cholecystitis, gallstone disease), dementia when starting therapy in women aged 65 years.
Overdose Ladybone:
The main symptoms are malaise, vaginal bleeding, or nausea.
Therapy: symptomatic.
If you take a large number of tablets at the same time, you should consult a doctor.
special instructions Ladybone:
does not protect against unwanted pregnancy; it is not intended for use as a contraceptive. The decision to initiate therapy is made on the basis of an assessment of the balance of benefits and risks, while all individual risk factors must be taken into account, and women over 60 years old also need to take into account the increased risk of stroke. For the treatment of postmenopausal symptoms, Ladybone should only be prescribed for symptoms that have an adverse effect on quality of life. All women, without exception, need to carefully assess the benefits of therapy and the risk at least once a year. Every woman with an intact uterus should be assessed for the likelihood of developing stroke, breast and endometrial cancer, taking into account all individual risk factors, the incidence and characteristics of both cancers and stroke in terms of indicators such as curability, morbidity and mortality. There is limited evidence regarding the risks associated with HRT or the use of tibolone in the treatment of premature menopause. However, the benefit-to-risk ratio in women with premature menopause is likely to be more favorable than in older women, due to the lower absolute level of risk in younger women.
A medical history (individual and family) must be collected before / upon resumption of treatment. Physical examination (including examination of the mammary glands and pelvic organs) must be carried out taking into account the anamnestic data and available both absolute and relative contraindications. During the period of therapy, repeated preventive examinations are recommended, their frequency and nature are determined depending on the individual characteristics of the patient, however, they should be held at least once every six months. A woman should inform her doctor about any changes in the mammary glands. Examinations that include appropriate imaging techniques (in particular mammography) should be carried out in accordance with the accepted scheme, which is adapted to the clinical needs of each patient, but at least once every six months. In the event of the appearance of the following diseases / conditions, is canceled: deterioration in liver function or jaundice; a sudden increase in blood pressure, which differs from the usual indicators characteristic of the patient; the appearance of a migraine-type headache. Despite the fact that the information obtained as a result of randomized controlled clinical trials is controversial, observational data indicate an increased risk of developing endometrial hyperplasia or cancer in women taking Ladybon.
Their results show that the risk of developing endometrial cancer increases with the duration of drug use. Tibolone can increase the thickness of the endometrium, as measured by transvaginal ultrasound. During the first months of using Ladybone, spotting and breakthrough bleeding may occur. In the event of bloody discharge / bleeding during tibolone therapy, which lasts longer than 6 months from the start of the drug
