Ladybone - Instructions For Use Of The Drug, Reviews, Price, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Ladybone

Ladybone: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. In case of impaired renal function
11. 11. For violations of liver function
12. 12. Use in the elderly
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Ladybon

ATX code: G03CX01

Active ingredient: tibolone (Tibolone)

Manufacturer: Zentiva, c.s. (Zentiva, ks) (Czech Republic)

Description and photo updated: 2018-29-11

Prices in pharmacies: from 520 rubles.

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Ladybone is an anti-climacteric estrogenic drug.

Release form and composition

Dosage form - tablets: round, flat, from white to almost white, on one side with an engraving "e" (in a cardboard box 1 or 3 blisters containing 28 tablets, and instructions for the use of Ladybon).

Composition 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.

Pharmacological properties

Pharmacodynamics

Ladybone is one of the anti-climacteric drugs.

Tibolone - the active substance of Ladybone, 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 contributes to the replenishment of estrogen deficiency in postmenopausal women, while alleviating 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

Tibolone has high absorption. 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 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 that are used to prevent osteoporosis (prevention).

Contraindications

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;
• period less than 12 months after the last menstrual period;
• untreated endometrial hyperplasia;
• bleeding from the vagina of unknown origin;
• arterial / venous thrombosis and thromboembolism, including a burdened anamnesis (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;
• liver failure;
• liver disease in an acute course or a history of liver disease, after which the 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 Ladybone.

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 relapse or exacerbation of these diseases / conditions during the period of therapy with Ladybone.

Ladybone, instructions for use: 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 earlier than the specified period leads to an increase in the likelihood of irregular bleeding / bleeding from the vagina.

Regardless of whether a woman is taking another HRT (hormone replacement therapy) drug or not, before the start of the course, malignant neoplasms of the reproductive system should be excluded, 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 day. The tablet must be swallowed with water.

Blisters with tablets are marked with the days of the week. You need to start using Ladybone with 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: Take the missed dose as soon as possible
• more than 12 hours: the reception is skipped, in the future, the woman should take the pill at the usual time. Do not take two tablets at the same time to replenish the missed dose.

Women who switch from a cyclic regimen of the drug for HRT to Ladybone should begin 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 Ladyibon at any time.

Side effects

Possible adverse reactions reported in 21 placebo-controlled studies (> 10% - very common;> 1% and 0.1% and 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, pain in the mammary glands, 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, weight gain.

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, itchy 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 risk level is determined by the duration of use.

The highest risk of developing endometrial cancer was observed in a randomized, placebo-controlled study that included women who were not initially screened 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 a 2.9-year follow-up, 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 intake or age, but the absolute risk is largely determined by age. The general risk of ischemic stroke in women taking tibolone will be with age.

So, 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. In 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.

There were also other undesirable effects associated with the use of drugs for HRT (combination drugs, estrogen-containing drugs, tibolone), including a slight increase in the risk of 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 Ledibon 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 developing 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, cholelithiasis), dementia when starting therapy in women aged 65 years.

Overdose

The main symptoms are malaise, vaginal bleeding, or nausea.

Therapy: symptomatic.

In case of taking 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, incidence and characteristics of both cancers and stroke in terms of indicators such as cure rate, 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 / 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 taken before starting / when resuming 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, Ladybone is canceled:

• worsening 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 may 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 that lasts longer than 6 months from the start of the drug or begins 6 months after the start of Ladyibon's use and continues even after the drug is discontinued, you need to consult a doctor, since this may be a symptom of endometrial hyperplasia.

From the point of view of evidence-based medicine, the information from different clinical studies on the risk of developing breast cancer against the background of the use of Ladybone is controversial and requires further research.

Breast cancer is much more common than ovarian cancer. Long-term (at least 5–10 years) estrogen replacement monotherapy is associated with a slight increase in the likelihood of ovarian cancer. Several studies, including the Women's Health Initiative, have found that long-term combination drug therapy for HRT may have a similar or slightly lower risk. In a study involving more than a million women, it was proved that the relative likelihood of developing ovarian cancer with Ladyibone is similar to the risk associated with the use of other types of HRT.

Medicines for HRT containing only estrogens or combination medications containing both estrogen and gestagen can increase the risk of VTE (deep vein thrombosis or pulmonary embolism) by 1.3-3 times, especially during the first year of use …

According to the results of an epidemiological study, which took into account the UK database, the likelihood of developing VTE associated with the use of tibolone was lower than the risk due to the use of traditional HRT drugs. However, it should be borne in mind that at that point in time only a small part of women were taking tibolone, therefore, it is impossible to exclude a slight increase in risk compared to women who did not take tibolone.

Patients with known thrombophilic conditions have an increased risk of VTE, and Ladyibon's intake may increase this risk, therefore the drug is contraindicated in this group of women.

Risk factors for VTE:

• the use of estrogens;
• prolonged immobilization;
• extensive surgical intervention;
• obesity (in patients with a body mass index greater than 30 kg / m ²);
• crayfish;
• systemic lupus erythematosus;
• elderly age;
• pregnancy and postpartum period.

After surgical interventions, patients need to pay special attention to preventive measures aimed at preventing VTE in the postoperative period. If it is necessary to immobilize for a long time after the operation, it is recommended to temporarily stop taking Ladyibon 4–6 weeks before the operation. The resumption of therapy is indicated after the restoration of physical activity. Women who do not have a history of VTE but have first-degree relatives with a history of thrombosis at a young age may need screening (it should be borne in mind that only a part of thrombophilic conditions can be detected during screening). When a thrombophilic condition is detected, which is separate from thrombosis in relatives, or a serious disorder (for example,in patients with a deficiency of antithrombin, protein S and C or a combination of disorders), the use of Ladybone is contraindicated.

Women receiving anticoagulants need to carefully assess the balance of benefits and risks before prescribing HRT or tibolone.

In cases where VTE develops after the start of Ladyibon's administration, the drug is canceled. If you experience symptoms of potential thromboembolism (pain and unilateral edema of the lower limb, sudden chest pain, shortness of breath), you should immediately consult a doctor.

When conducting randomized controlled trials, evidence of protection against myocardial infarction in women with / without coronary heart disease receiving HRT with combined agents (estrogen + progestogen) or drugs containing only estrogen was not obtained.

Epidemiological studies using the extensive database of primary care provided to British patients, including a medical record (GPRD), did not provide evidence of protection against myocardial infarction in postmenopausal women receiving tibolone.

When taking Ladyibon, the risk of ischemic stroke increases, starting from the first year of therapy. The absolute risk of developing a stroke is strictly determined by age, and, therefore, this effect of tibolone is greater the older the patient is. If you experience unexplained migraine-like headaches with / without visual impairment, you need to see a doctor as soon as possible. In this case, the drug should not be taken until confirmation of the safety of continuing HRT is obtained (such headaches are early diagnostic signs of a possible stroke).

According to available data, the use of Ladybone led to a significant dose-dependent reduction in HDL cholesterol (high density lipoprotein).

There is also a decrease in the total concentration of triglycerides and VLDL (very low density lipoproteins). Reducing the concentration of total cholesterol and VLDL cholesterol is not dose-dependent. The concentration of LDL cholesterol (low density lipoprotein) does not change. The clinical significance of this information is not yet clear.

In case of already existing hypertriglyceridemia, during the period of Ladyibon's use, careful monitoring of the condition of women should be established. This is due to the fact that rare cases of a significant increase in the plasma concentration of triglycerides in the blood, contributing to the onset of pancreatitis, were observed during the period of use of estrogens in this condition.

Tibolone therapy results in a very slight decrease in TSH (thyroxine-binding globulin) and total T ₄ (thyroxine). The concentration of total T ₃ remains unchanged. Taking Ladyibon helps to reduce the concentration of SHBG (globulin that binds sex hormones), while the drug does not affect the concentration of CSG (corticosteroid binding globulin) and circulating cortisol.

During the period of therapy, there is a possibility of fluid retention, which in women with renal or heart failure requires observation.

It is necessary to take into account the increased risk of dementia if patients over 65 years of age start taking Ladyibon.

Application during pregnancy and lactation

Ladyibon is not prescribed during pregnancy / lactation.

If pregnancy occurs, the drug should be stopped immediately.

With impaired renal function

Women with renal insufficiency should take Ladyibone with caution.

For violations of liver function

Contraindications:

• liver failure;
• liver disease in an acute course or a history of liver disease, after which the liver function indicators did not return to normal;
• benign / malignant liver tumors (including liver adenoma), including a burdened history.

Use in the elderly

Women over 65 should be aware of the increased risk of developing dementia while taking Ladyibon.

Drug interactions

Since tibolone enhances the fibrinolytic activity of the blood, it is possible to enhance the anticoagulant effect of anticoagulants (warfarin). Therefore, the dose of warfarin must be adjusted accordingly based on the MHO (International Normalized Ratio). With the combined use of tibolone and anticoagulants, control is necessary, mainly at the beginning and at the end of treatment with Ladybon.

There is only limited information regarding the pharmacokinetic interaction with the use of tibolone. According to the studies, the combined use with tibolone has an insignificant effect on the pharmacokinetics of the CYP3A4 substrate midazolam. Thus, we can assume the presence of drug interactions with other substrates of CYP3A4.

Medicines - inducers of CYP3A4 (carbamazepine, barbiturates, rifampicin, hydantoins) can increase the metabolism of tibolone, which affects its therapeutic effect. Preparations containing perforated St. John's wort (Hypericum perforatum) can increase the metabolism of gestagens and estrogens by inducing the isoenzyme CYP3A4. That can lead to a decrease in their clinical effect and cause a change in the profile of uterine bleeding.

Analogs

The analogues of Ladybon are Velledien, Livial, Tsimicyclim, etc.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Ladybone

On specialized women's forums and sites, you can find many reviews about Ladyibone. Most women indicate effective relief of symptoms characteristic of the postmenopausal period, and good tolerance of the drug. At the same time, there are responses that indicate the development of side effects of varying severity. It is noted that the cost of Ladybon is lower than that of its counterparts.

Price for Ladybon in pharmacies

Approximate price for Ladybone tablets 2.5 mg:

• 28 pcs. in the package - 889-977 rubles;
• 84 pcs. in the package - 2263-2712 rubles.

Ladybone: prices in online pharmacies

Drug name Price Pharmacy

Ladybone 2.5 mg tablets 28 pcs. RUB 520 Buy

Ladybon tablets 2.5mg 28 pcs. 749 RUB Buy

Ladybone 2.5 mg tablets 84 pcs. 1653 RUB Buy

Ladybon tablets 2.5mg 84 pcs. 1944 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!