Femoston® 2/10 (Femoston® 2/10)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDydrogesterone + EstradiolDydrogesterone + Estradiol
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    • Dosage form: & nbspFilm coated tablets.
    Composition:

    1 a tablet covered with a film shell, pink color contains:

    Active substance: Estradiol hemihydrate - 2.06 mg (in terms of estradiol -2.0 mg).

    Excipients: lactose monohydrate - 118.2 mg; hypromellose - 2,8 mg; starch corn - 14.9 mg; silicon dioxide colloidal - 1.4 mg; magnesium stearate-0.7 mg.

    Film sheath: Opadney OY-6957 pink (hypromellose - 2.5056 mg, talc 0.6 mg, titanium dioxide (E171) - 0.6 mg, macrogol 400 - 0.248 mg, iron oxide red - 0.04632 mg, iron oxide black - 0.00004 mg, iron oxide yellow - 0.00004 mg) - 4.0 mg.


    1 tablet, film-coated, light yellow color contains:

    Active substances: Estradiol hemihydrate - 2.06 mg in terms of estradiol -2.0 mg and dydrogesterone 10 mg.

    Excipients: lactose monohydrate - 109.4 mg; hypromellose - 2,8 mg; corn starch - 13.7 mg; silicon dioxide colloidal - 1.4 mg; magnesium stearate - 0.7 mg.

    Film Sheath: Opadry OY-02B22764 yellow (hypromellose - 2.5 mg, talc - 0.6244 mg, titanium dioxide (E 171) - 0.6116 mg, macrogol 400 - 0.25 mg, iron oxide yellow - 0.014 mg) - 4.0 mg.

    Description:
    Tablets 2 mg of estradiol:

    Round, biconvex tablets covered with a pink film shell, with engraving "379" - on one side of the tablet.
    Type of tablet on the break: white rough surface.

    Tablets 2 mg estradiol / 10 mg dydrogesterone:

    Round, biconvex tablets, covered with a film coating of light yellow color, with engraving "379" - on one side of the tablet.
    Type of tablet on the break: white rough surface.
    Pharmacotherapeutic group: Anti-climacteric combined (estrogen + gestagen).
    ATX: & nbsp

    G.03.F.A.14   Dydrogesterone and estrogen

    Pharmacodynamics:
    Estradiol, which is part of the preparation Femoston ® 2/10, is identical to the endogenous estradiol of a human being, which is the most active estrogen.
    Estradiol replenishes the deficiency of estrogen in the female body in women at menopausal age and reduces menopausal symptoms during the first weeks of treatment. Hormone replacement therapy (HRT) with Femoston® 2/10 prevents bone loss in the postmenopausal period or after ovariectomy. Dydrogesterone - Progestogen, effective at ingestion and having parenteral progesterone-like activity.
    When carrying out HRT, the inclusion of dydrogesterone provides a full secretory transformation of the endometrium, thereby reducing the increased risk of endometrial hyperplasia under the influence of estrogen.
    Pharmacokinetics:

    Estradiol

    Suction

    The absorption of estradiol depends on the particle size, micronized estradiol easily absorbed from the gastrointestinal tract.

    Distribution

    Estrogen can be detected both in bound and free state. About 98-99% of the dose of estradiol binds to plasma proteins, of which 30-52% with albumin and about 46- 69% with sex hormone binding globulin (GSHG).

    Metabolism

    Estradiol is metabolized in the liver to estrone and estrone sulfate, which have estrogenic activity. Estrone sulfate can undergo intestinal hepatic recirculation.

    Excretion

    Estrone and estradiol are excreted in conjugated glucuronic acid state mainly by the kidneys. The half-life (T1 /2) is 10-16 hours. Estrogens penetrate into breast milk.

    Dependence of time and dose of cointritional and estradiol

    With daily intake of the drug Femoston® 2/10, the concentration of estradiol in the blood plasma reaches a constant value after about 5 days.

    Dydrogesterone

    Suction

    After oral administration, it is rapidly absorbed and completely metabolized. The time values ​​of the maximum concentration (TmOh) for dydrogesterone vary from 30 minutes to 2.5 hours. Bioavailability of dydrogesterone - 28%.

    Distribution

    More than 90% of dydrogesterone and DGD bind to plasma proteins.

    Metabolism

    The main metabolite of dydrogesterone is 20α-dihydrodydrogesterone (DHD). The maximum concentration of DGD in the blood plasma is reached approximately 1.5 hours after the administration of the drug. The concentration of DGD in blood plasma significantly exceeds the initial concentration of dydrogesterone, the ratio of the area values ​​under the curve "concentration-time" (AUC) and the maximum concentration (CmOh) DGD to dydrogesterone is about 40 and 25, respectively. The half-life is for dydrogesterone 5-7 hours, for DGD 14-17 hours.

    A common characteristic feature of all metabolites of dydrogesterone is the preservation of the configuration of 4,6-diene-3-one of the starting material and the lack of 17α-hydroxylation,which causes the absence of estrogenic and androgenic activity.

    Excretion

    Completely dydrogesterone is excreted after 72 hours. On average, 63% of the dose is excreted by the kidneys. The total plasma clearance is 6.4 l / min. DGD is defined in the urine advantageously in the form of a glucuronic acid conjugate.

    Dependence of dydrogesterone concentration on time and dose

    A comparison of the kinetics of single and multiple doses shows that the pharmacokinetic the properties of dydrogesterone and DGD do not change when receiving multiple doses.

    The equilibrium concentration of dydrogesterone was achieved 3 days after treatment.

    Indications:
    - Hormone replacement therapy due to estrogen deficiency in women in the perimenopause (no earlier than 6 months after the last menstrual period) or in postmenopausal women.

    - Prevention of postmenopausal osteoporosis in women with a high risk of fractures with intolerance or contraindications to the use of other medications.
    Contraindications:
    - Pregnancy and the period of breastfeeding.

    - Diagnosed or suspected breast cancer.

    - Diagnosed or suspected estrogen-dependent malignant neoplasms (eg, endometrial cancer).

    - Diagnosed or suspected progestogen-dependent neoplasms (eg, meningioma).

    - Bleeding from the vagina of an unclear etiology.

    - Untreated hyperplasia of the endometrium.

    - Thrombosis (arterial and venous) and thromboembolism now or in the anamnesis (including thrombosis, deep vein thrombosis, pulmonary embolism, myocardial infarction, ischemic or hemorrhagic cerebrovascular disorders).

    - Multiple or expressed factors of arterial or venous thrombosis associated with congenital or acquired predisposition, for example, protein C deficiency, protein S deficiency, antithrombin III deficiency, antibodies to phospholipids (antibodies to cardiolipin, lupus anticoagulant), angina pectoris, prolonged immobilization, severe forms obesity (body mass index more than 30 kg / m), cerebrovascular or coronary artery disease, transient ischemic attacks, complicated valve lesions cardiac apparatus, atrial fibrillation.

    - Acute or chronic liver disease at present or in the anamnesis (before the normalization of indicators of functional liver tests), including malignant liver tumors.

    - Porphyria.

    - Hypersensitivity to the components of the drug.

    - Intolerance to galactose, insufficiency of lactase, glucose-galactose malabsorption syndrome.

    Taking Femoston® 2/10 should be discontinued if there are any contraindications and / or when the following conditions occur:

    - jaundice and / or liver dysfunction;

    - uncontrolled arterial hypertension;

    - The first to appear on the background of the use of drugs for HRT is migraine headache.
    Carefully:
    HRT is prescribed for women if, at the present time or in a history, they have been diagnosed with:

    - Leiomyoma of the uterus, endometriosis.

    - The presence of risk factors for the occurrence of estrogen-dependent tumors (for example, relatives of the first degree of kinship with breast cancer).

    - Arterial hypertension.

    - Benign tumors of the liver.

    - Diabetes mellitus, both in the presence of vascular complications, and in the absence of them.

    - Chololithiasis.

    - Migraine or severe headache.

    - Systemic lupus erythematosus.

    - Hyperplasia of the endometrium in the anamnesis.

    - Epilepsy.

    - Bronchial asthma.

    - Otosclerosis.

    Pregnancy and lactation:
    The drug is contraindicated in pregnancy and during breastfeeding.
    If pregnancy occurs, the therapy should be stopped immediately after treatment with Femoston® 2/10.
    Dosing and Administration:
    The drug is taken orally daily, in continuous mode, 1 tablet per day (preferably at the same time of day), regardless of food intake.
    Each package is designed for a 28-day drug intake. In the first 14 days, 1 tablet of pink color is taken daily (from the half of the package with the arrow marked with the number "1") containing 2 mg of estradiol, and for the remaining 14 days - 1 light-yellow tablet daily (from the half of the package with the arrow, labeled "2") containing 2 mg of estradiol and 10 mg of dydrogesterone.
    Usually, treatment should begin with the preparation of Femoston® 1/10. Depending on the clinical effectiveness, the doses of the active substances can be adjusted according to the individual need. If complaints related to estrogen deficiency persist, the dosage can be increased using Femoston ® 2/10.Patients making the transition from another continuous sequential or cyclic regimen should complete the current cycle, and then switch to Femoston® 2/10. Patients making the transition from a continuous combination regimen can begin taking Femoston® 2/10 any day.
    If the patient missed the pill, it should be taken within 12 hours after the usual time of admission; otherwise, the missed tablet should not be taken, and the next day it is necessary to take the pill at the usual time. Skipping the drug may increase the likelihood of "breakthrough" uterine bleeding.
    Side effects:
    In clinical studies, the most common cases of patients receiving estradiol / dydrogesterone combination therapy were headache, abdominal pain, mammary tension / tenderness, and back pain.
    In clinical studies (n = 4929), the following adverse events were observed with a developmental frequency indicated below (number of reported cases / number of patients):

    Often - from 1 to 10 cases;

    often - from 1 to 100 to 1 for 10 cases;

    infrequently - from 1 per 1000 to 1 per 100 cases;

    rarely - from 1 per 10,000 to 1 per 1000 cases;

    rarely - less than 1 per 10,000 cases.

    From the nervous system:

    Very often - a headache.

    Often - a migraine, dizziness.

    Mental disorders:

    Often - depression, nervousness.

    Infrequently, a change in the libido.

    From the cardiovascular system:

    Infrequent - venous thromboembolism, increased blood pressure.

    Rarely, myocardial infarction.

    From the gastrointestinal tract:

    Very often - a pain in the abdomen.

    Often - nausea, vomiting, flatulence.

    From the hepatobiliary system:

    Infrequently - a disease of the gallbladder, a violation of the liver, sometimes in combination with jaundice, asthenia, malaise, abdominal pain.

    On the part of the reproductive system and mammary glands:

    Very often - the tension / soreness of the mammary glands.

    Often - "smearing" spotting in postmenopause, metrorrhagia, copious menstrual like bleeding, meager or no menstrual like bleeding, acyclic spotting, painful menstrual bloody discharge, pain in the abdomen, change in vaginal secretion, candidiasis of the vagina.

    Infrequently - an increase in the size of leiomyoma, an increase in mammary glands, premenstrual like syndrome.

    From the immune system:

    Infrequent - hypersensitivity to the drug or any of the components of the drug.

    From the side of skeletal musculature and connective tissue:

    Very often - pain in the back (waist).

    From the skin and subcutaneous fat:

    Often - allergic reactions, such as urticaria, skin rash and itching.

    Rarely - vascular purpura, angioedema.

    Infectious diseases:

    Infrequently - a cystitis.

    General disorders:

    Often - asthenic conditions (weakness, malaise, fatigue), peripheral edema.

    Other:

    Often - an increase in body weight.

    Infrequent is the decrease in body weight.

    Other side effects caused by the treatment of a combination of estrogen and progestogen

    (including estradiol / dydrogesterone):

    - Benign, malignant and unspecified neoplasms (eg, endometrial cancer, ovarian cancer, meningioma).

    - From the hemopoietic system: hemolytic anemia.

    - On the part of the immune system: systemic lupus erythematosus.

    - From the nervous system: the risk of developing dementia in women starting to use drugs for HRT, over the age of 65, chorea, provoking epileptic seizures.

    - On the part of the organs of vision: intolerance of contact lenses, increased curvature of the cornea.

    - From the skin and subcutaneous fat: chloasma and / or melasma, which can persist after discontinuation, erythema multiforme, erythema nodosum.

    - From the skeletal musculature and connective tissue: convulsions in the muscles of the lower limbs.

    - From the cardiovascular system: arterial thromboembolism.

    - From the genitourinary system: urinary incontinence.

    - On the part of the reproductive system and mammary glands: fibrocystic mastopathy, erosion of the cervix.

    - Congenital and hereditary disorders: worsening of the course of concomitant porphyria.

    - Metabolic disorders: hypertriglyceridemia.

    - Disorders from the gastrointestinal tract: pancreatitis (in patients with hypertriglyceridemia).

    - Diagnosis: elevated thyroid hormone levels.

    Overdose:
    Estradiol and dydrogesterone - substances with low toxicity.
    In case of an overdose, symptoms such as nausea, vomiting, mammary gland tension, dizziness, abdominal pain, drowsiness / weakness and bleeding can be developed.Treatment is symptomatic.
    Interaction:

    The estrogenic and progestational effect of the preparation Femoston® 2/10 can be reduced in the following cases:

    Metabolism of estrogens and gestagens can be enhanced by simultaneous reception with induction drugs of microsomal liver enzymes (P450 2B6, ZA4, ZA5, ZA7): anticonvulsant (phenobarbital, carbamazepine, phenytoin) and antimicrobial agents (rifampicin, rifabutin, nevirapine, efavirenz).

    - Herbal preparations containing St. John's wort (Hypericum perforatum), can enhance the metabolism of estrogens and gestagens through CYP 450 AP4.

    - Ritonavir and nelfinavir, although they are known as strong inhibitors CYP 450 SA4, A5, A7, with simultaneous application with sex hormones can enhance their metabolism.

    - An increase in the metabolism of estrogens and gestagens can be clinically manifested by a decrease in the effect of the drug and a change in the intensity of bleeding from the vagina.

    Estrogens can affect the metabolism of other medicines:

    Estrogens can affect the metabolism of other drugs through competitive binding to enzymes (CYP 450) involved in their splitting. This should be taken into account for drugs with a narrow breadth of therapeutic effect, such as tacrolimus and ciclosporin A (CYP 450 ЗА4, ЗАЗ), fentanyl (CYP 450 SA4) and theophylline (CYP 450 1A2), since this type of interaction can lead to an increase in the concentration in the blood plasma of the above drugs to a toxic level. In this regard, careful monitoring of medication intake over a long period of time and possibly a reduction in the dose of tacrolimus, fentanyl, cyclosporin A, and theophylline may be required.

    Studies on the interaction with other drugs have not been conducted.

    Special instructions:

    The drug is prescribed only in the presence of symptoms adversely affecting the quality of life. Therapy should be continued until the benefit of taking the drug exceeds the risk of side effects. The experience of using the drug in women over 65 is limited.

    Medical examination

    Before the appointment or resumption of therapy with the drug Femoston® 2/10, it is necessary to collect a complete medical and family history and conduct a general and gynecological examination (including the mammary glands) of the patient in order to identify possible contraindications and conditions,requiring precautions. During

    treatment with the drug Femoston ® 2/10 is recommended to conduct periodic examinations, the frequency and nature of which are determined individually, but at least 1 time in 6 months. It is advisable to conduct mammography for additional examination of the mammary glands. Women should be informed of any possible changes in the mammary glands that are required to inform the attending physician.

    The use of estrogens can affect the results of the following laboratory tests: the determination of glucose tolerance, the study of the functions of the thyroid and liver. Endometrial hyperplasia

    The risk of developing hyperplasia and endometrial cancer in patients with estrogen alone depends on the dose and duration of treatment and is increased 2 to 12 times compared to the absence of treatment; the risk may remain elevated for 10 years after discontinuation of therapy.

    The cyclic use of progestogen (at least for 12 days of a 28-day cycle), or the use of a continuous combined HRT regime in women with a preserved uterus, can prevent estrogen-induced risk of hyperplasia and endometrial cancer.

    For the purpose of timely diagnosis, it is advisable to perform ultrasound (ultrasound) screening, if necessary - to conduct a histological (cytological) study.

    Bloody discharge from the vagina

    In the first months of treatment, the drug may be marked by "breakthrough" bleeding and / or meager spotting from the vagina. If such bleeding occurs some time after the initiation of therapy or continues after the cessation of treatment, their cause should be established. It is possible to conduct an endometrial biopsy to exclude a malignant neoplasm.

    Venous thromboembolism

    HRT is associated with a 1.3-3-fold risk of venous thromboembolism (VTE), i.e. deep vein thrombosis or pulmonary embolism. This phenomenon is most likely during the first year of HRT.

    In the presence of thromboembolic complications in relatives of the first degree of kinship at a young age, as well as with a habitual miscarriage of a pregnancy in an anamnesis,

    it is necessary to conduct a study of hemostasis. If the patient is taking anticoagulants,

    It is necessary to carefully consider the appointment of the drug Femoston® 2/10 in terms of the "benefit / risk" ratio.Before the completion of a thorough assessment of the possible development of thromboembolism or the initiation of anticoagulant therapy, the preparation of Femoston® 2/10 is not prescribed.

    If a member of the family is diagnosed with a thrombophilic condition and / or in the case of severity or severity of the defect (eg, insufficiency of antithrombin III, protein S or C, as well as a combination of defects), the preparation Femoston® 2/10 is contraindicated.

    Since patients with diagnosed thrombophilic conditions have an increased risk of developing venous thromboembolism, the appointment of the drug Femoston® 2/10, which increases this risk, is contraindicated.

    In most cases, risk factors for VTE include: estrogen use, advanced age, extensive surgical interventions, prolonged immobilization, obesity (body mass index> 30 kg / m2), pregnancy or the postpartum period, systemic lupus erythematosus and cancer. There is no consensus on the possible role of varicose veins in the development of VTE.

    To prevent VTE after surgical intervention in all postoperative patients, it is necessary to consider the issue of preventive measures.

    In case of prolonged immobilization after surgery, 4-6 weeks before this is recommended to stop taking the drug Femoston® 2/10, and the treatment should not be resumed until the woman completely regains mobility. If VTE develops after the initiation of therapy, the drug should be discontinued and the patients should be informed that they should immediately consult their doctor if they have any potentially thromboembolic symptoms (eg, tenderness or swelling of the lower limbs, sudden pain in the chest, shortness of breath).

    Breast Cancer and Ovarian Cancer

    In women who have received HRT for a long time with the use of estrogen alone or the estrogen-progestagen complex, the frequency of breast cancer diagnosis increases, which returns to baseline within 5 years after discontinuation of therapy. The increase in risk depends on the duration of HRT use. In women taking combined estrogen-progestogen HRT for more than 5 years, the risk of developing breast cancer may increase up to 2-fold.

    Against the background of taking drugs for HRT, there may be an increase in tissue densitybreast cancer during mammography, which can make it difficult to diagnose breast cancer.

    Ovarian cancer is much less common than breast cancer. Long-term use (at least 5-10 years) of estrogen in monotherapy with HRT is associated with a slight increase in the risk of ovarian cancer. Data from some studies, including WHI, indicate that a long combined HRT can

    in the same or slightly lesser degree, increase the risk of developing this pathology.

    The risk of ischemic stroke

    Combined therapy with estrogen and progestogen or estrogen alone is associated with an increase in the relative risk of ischemic stroke by a factor of 1.5. The risk of hemorrhagic stroke when HRT is not increased.

    The relative risk does not depend on the age or duration of therapy, but the baseline risk depends heavily on age, so the overall risk of stroke in women receiving HRT will increase with age.

    Ischemic heart disease (CHD)

    The relative risk of coronary heart disease during the use of combined HRT

    estrogen + progestogen slightly increased. Due to the fact that the absolute risk

    CHD strongly depends on age, the number of additional cases of IHD due to the use of combined HRT in healthy women of premenopausal age is very small, but it increases with age.

    Other states

    Estrogens can cause fluid retention, which can adversely affect the condition of patients with impaired renal and cardiac function.

    In women with hypertriglyceridemia, when taking drugs for HRT in very rare cases, the plasma concentration of triglycerides can significantly increase, which contributes to the development of pancreatitis.

    Estrogens increase the concentration of thyroid-binding globulin, which leads to a general increase in the concentration of circulating thyroid hormones (the concentration of free hormones T3 (triiodothyronine) and T4 (thyroxine) usually do not change). Concentrations of other binding proteins in the blood plasma (transcortin, globulin, binding sex hormones) can also increase, which leads to an increase in the concentration of circulating glucocorticosteroids and sex hormones. Concentrations of free or biologically active hormones do not change.It is possible to increase the concentration of other plasma proteins (angiotensinogen / renin system, a-1 antitrypsin, ceruloplasmin).

    The use of HRT does not improve cognitive function. There are reports of an increased risk of developing dementia in women who started using HRT (combined or estrogen-only) after 65 years.

    The drug Femoston® 2/10 is not a contraceptive.

    Effect on the ability to drive transp. cf. and fur:
    Care should be taken when controlling vehicles and mechanisms, taking into account the risk of adverse reactions from the nervous system.
    Form release / dosage:
    Film-coated tablets.

    Packaging:
    For 14 tablets 2 mg of estradiol and 14 tablets of 2 mg of estradiol / 10 mg of dydrogesterone in a blister of PVC / PVDC / Al foil.
    For 1, 3 or 10 blisters in a cardboard box together with instructions for use.
    Storage conditions:Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011361 / 02
    Date of registration:02.11.2009
    The owner of the registration certificate:Abbott Helskea Products BVAbbott Helskea Products BV Netherlands
    Manufacturer: & nbsp
    Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia
    Information update date: & nbsp28.01.2016
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