Femoston® continent (Femoston® conti)

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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  • Femoston® 1/10
    pills inwards 
    Abbott Helskea Products BV     Netherlands
  • Femoston® 2/10
    pills inwards 
    Abbott Helskea Products BV     Netherlands
  • Femoston® continent
    pills inwards 
    Abbott Helskea Products BV     Netherlands
  • Femoston® mini
    pills inwards 
    Abbott Helskea Products BV     Netherlands
    • Dosage form: & nbspTfilm-covered abeys.
    Composition:

    1 tablet, film-coated, contains:

    Active substance: Estradiol hemihydrate - 1.03 mg (in terms of estradiol - 1.0 mg) and dydrogesterone - 5.0 mg.

    Excipients: lactose monohydrate - 114.7 mg; hypromellose - 2,8 mg; corn starch - 14.4 mg; silicon dioxide colloidal - 1.4 mg; magnesium stearate - 0.7 mg.

    Sheath: A mixture for film coating of Orange 1 [hypromellose - 2,844 mg, macrogol 400 - 0.284 mg, titanium dioxide (E171) - 0.8 mg, iron dye oxide yellow (E 172) - 0.048 mg, iron oxide red (E 172) 0.024 mg] 4.0 mg.

    Description:

    Round, biconvex tablets, covered with a film shell of orange-pink color with engraving "379" - on one side of the tablet and engraved with the letter "S"above the" ▼ "icon on the other side of the tablet.

    Pharmacotherapeutic group:antimycotics combined (estrogen + progestogen)
    ATX: & nbsp

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

    Pharmacodynamics:

    Estradiol, which is part of the drug Femoston® contin, 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 the drug Femoston® contin prevents the loss of bone mass 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 quickly 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 blood plasma proteins, of which 30-52% with albumin and about 46-69% with sex hormone binding globulin (SHBG).

    Metabolism

    After oral administration estradiol is actively metabolized in the liver. The main unconjugated and conjugated metabolites are 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 the concentration of estradiol on time and dose

    With the daily administration of the drug Femoston® the concentration of estradiol in the blood plasma reaches a constant value after about 5 days. Usually this indicator is reached within 8-11 days after initiation of therapy.

    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.Absolute bioavailability dydrogesterone - 28%.

    Distribution

    More than 90% of dydrogesterone and DGD bind to blood 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 plasma significantly exceeds the initial concentration of dydrogesterone, the ratio of the area under the pharmaceutical curve "concentration-time" (AUC) and maximum concentration (CmOh) DGD to dydrogesterone is about 40 and 25, respectively. The half-life is 5-7 hours for dydrogesterone, 14-17 hours for DGD.

    A common characteristic feature of all metabolites of dydrogesterone is the preservation of the configuration of 4,6-dien-3-one of the starting material and the absence 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 accepted dose is excreted by the kidneys. The total plasma clearance is 6.4 l / min. DGD is determined in urine mainly in the form of conjugates of glucuronic acid.

    Dependence of dydrogesterone concentration on time and dose

    The drug is characterized by linear pharmacokinetics with single and multiple oral administration in the dose range from 2.5 mg to 10 mg.

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

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

    Indications:

    - Replacement hormone therapy for estrogen deficiency disorders 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:

    - Prescribed or anticipated pregnancy and lactation period;

    - diagnosed or suspected breast cancer, history of breast cancer;

    - diagnosed or suspected progestogen-dependent neoplasms;

    - diagnosed or suspected estrogen-dependent malignant neoplasms, including endometrial cancer, incl. in the anamnesis;

    - bleeding from the vagina of an unclear etiology;

    - thromboembolic diseases at present or in the anamnesis (for example: myocardial infarction, deep vein thrombosis, pulmonary embolism);

    - impaired cerebral circulation;

    - acute or chronic liver diseases at present or in the anamnesis (before normalization of laboratory parameters of liver function);

    - untreated endometrial hyperplasia;

    - porphyria;

    - hypersensitivity to the components of the drug;

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

    Carefully:

    HRT in postmenopausal women is prescribed to women if they have been diagnosed or have anamnesis at the moment:

    - uterine leiomyoma, endometriosis;

    - the presence of risk factors for the occurrence of estrogen-dependent tumors (for example, the first degree of heredity of breast cancer);

    - adenoma of the liver;

    - cholelithiasis;

    - migraine or an intense headache;

    - kidney failure;

    - bronchial asthma;

    - endometrial hyperplasia in the anamnesis;

    - epilepsy;

    - otosclerosis;

    - multiple sclerosis;

    - hemoglobinopathy;

    - risk factors for the development of thromboembolic conditions, incl.stenocardia, prolonged immobilization, severe forms of obesity (body mass index more than 30 kg / m2 );

    - arterial hypertension;

    - diabetes mellitus, both in the presence of vascular complications, and in cases of their absence;

    - systemic lupus erythematosus.

    Pregnancy and lactation:

    The drug is contraindicated in pregnancy and during lactation.

    If a pregnancy occurs, the therapy should be stopped immediately after the treatment with Femoston®.

    Dosing and Administration:

    The drug is taken orally daily, in continuous 1 tablet per day (preferably at the same time of day), regardless of food intake.

    Treatment should continue without interruption, immediately after the end of the 28-day cycle, the next treatment cycle should begin.

    To start and continue treatment for postmenopausal disorders, the lowest effective dose should be administered for the shortest period of time. Depending on the clinical response in the future, the dose can be adjusted.

    Patients making the transition from another continuous sequential or of the cyclic regimen of the drug, must complete the current cycle, and then switch to the preparation of Femoston® contin.

    Patients who make the transition from a continuous combination regimen can start taking Femoston® contin on any given day.

    If the patient misses the pill, it must be taken within 12 hours after the usual reception time. If more than 12 hours pass the missed pill should not be taken, and the next day you need to take the pill at the usual time. Skipping the drug may increase the probability of breakthrough uterine bleeding or spotting spotting.

    Side effects:

    Classification of adverse reactions according to the frequency of development (number of reported cases / number of patients):

    Often - more than 1 for 10 cases;

    often - from 1 to 10 to 1 per 100 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:

    Often - headache, migraine;

    Infrequent - dizziness;

    Very rarely - chorea.

    Mental disorders:

    Infrequently - depression, change of libido, nervousness.

    From the side of the cardiovascular system:

    Very rarely - increased blood pressure, venous thromboembolism, stroke, myocardial infarction.

    From the gastrointestinal tract:

    Often - nausea, pain in the abdomen, flatulence;

    Very rarely - vomiting.

    From the hepatobiliary system:

    Infrequent - cholecystitis;

    Rarely - a violation of the liver, sometimes in combination with asthenia, malaise and pain in the abdomen, jaundice (cholestatic).

    From the side of the reproductive system and mammary glands:

    Often - the tension / tenderness of the mammary glands, metrorrhagia in the first months of treatment, smearing spotting from the vagina, pain in the lower abdomen;

    Infrequent changes in cervical epithelium during cervical erosion, changes in cervical secretion, dysmenorrhea, increased size of leiomyoma, candidiasis of the vagina;

    Rarely - an increase in mammary glands, premenstrual like syndrome.

    Congenital and hereditary disorders:

    Very rarely - clinical manifestations of previously undiagnosed porphyria.

    On the part of the hematopoiesis system:

    Very rarely - hemolytic anemia;

    From the side of skeletal musculature and connective tissue:

    Often - cramps in the muscles of the lower limbs;

    Infrequent pain in the back (waist).

    Skin and subcutaneous fatty tissue:

    Infrequently, allergic reactions, such as urticaria, skin rash and itching;

    Very rarely - chloasma and / or melasma, which can persist after discontinuation, erythema multiforme, erythema nodosum, vascular purpura, angioedema.

    General disorders:

    Often - asthenia;

    Infrequent edema is infrequent.

    Other:

    Often - increase or decrease in body weight;

    Rarely - intolerance of contact lenses, increased curvature of the cornea;

    Very rarely, hypersensitivity reactions.

    Overdose:

    Estradiol and dydrogesterone - substances with low toxicity. No cases of overdose have been reported.

    Theoretically, in case of an overdose, symptoms such as nausea, vomiting, drowsiness, dizziness may occur.

    Treatment - symptomatic.

    Interaction:

    - The estrogenic effect of the drug Femoston® contin is reduced by simultaneous reception with induction drugs of microsomal liver enzymes: anticonvulsants (barbiturates, carbamazepine, phenytoin, oxcarbazepine, topiramate, felbamate), antimicrobial agents (rifampicin, rifabutin, nevirapine, efavirenz); with preparations of vegetable origin containing St. John's Wort (perforated)Hypericum perforatum).

    - The estrogenic effect of the drug Femoston® contin can be enhanced by simultaneous administration with inhibitor preparations of microsomal liver enzymesritonavir, nelfinavir).

    - Interactions of dydrogesterone with other drugs are not known.

    The patient should inform the doctor about the medications that she takes while taking HRT, or took it before the appointment of the drug Femoston® contin.

    Special instructions:

    The drug is prescribed only in the presence of symptoms adversely affecting the quality of life.

    All patients receiving HRT at least once a year require an assessment of the benefit / risk ratio. 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.

    Information on the risks associated with HRT in case of premature menopause are limited.

    Because of the low level of absolute risk in women of younger age, the benefit / risk ratio among them may be in favor of HRT compared to older women.

    Medical examination

    Before the appointment or resumption of therapy with Femoston® Continent should collect a complete medical and family history and conduct a general and gynecological examination (including the breast) of the patient in order to identify possible contraindications and conditions requiring compliance with precautionary measures. During treatment with the drug Femoston® Continu it is recommended to conduct periodic examinations, the frequency and nature of which are determined individually, but not less than 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 patients not receiving therapy; the risk may remain elevated for 10 years after discontinuation of therapy.

    In women with a preserved uterus, HRT is not recommended for estrogen alone because of an increased risk of endometrial cancer. 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.

    In women, the use of combined HRT for 5 years did not lead to an increased risk of 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 with the drug, breakthrough bleeding and / or scanty spotting from the vagina may be noted. 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. The development of 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 in a history, it is necessary to carry out a study of hemostasis (during screening, only a part of the disorders of the blood coagulation system is detected).

    If the patient is taking anticoagulants, you should carefully consider the appointment of the drug Femoston® continent in terms of benefit / risk ratio. Before the completion of a thorough assessment of the possible development of thromboembolism or the initiation of anticoagulant therapy, the drug Femoston® contin is not assigned.

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

    Since patients with diagnosed thrombophilic conditions have an increased risk of developing venous thromboembolism, the appointment of the drug Femoston® contin, 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, it is recommended to stop taking Femoston® the drug 4-6 weeks before, and the treatment should not be resumed until the woman fully 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).

    Mammary cancer

    In women who have been on HRT for a long time with estrogen alone or in combination with estrogen and progestogen, the incidence of breast cancer diagnosis is increasing, which returns to baseline within 5 years after cessation of therapy.

    The increase in risk depends on the duration of HRT use. In women taking combined HRT for more than 5 years, the risk of developing breast cancer may increase up to 2-fold.

    Combined therapy with estrogen and progestogen

    The results of a randomized placebo-controlled study (the Women's Health Initiative (WHI)) and epidemiological studies showed an increased risk of developing breast cancer in women taking combined HRT with estrogen and progestogen. This increase becomes noticeable after about three years of therapy.

    Therapy with estrogen alone

    According to the results of the WHI study, there was no increase in the risk of developing breast cancer in women with previous hysterectomy who received HRT only with estrogen.

    Most observational studies have shown a slight increase in the risk of breast cancer, and this risk was significantly lower in women taking combination therapy with estrogen and progestogen.

    The increase in risk becomes noticeable after several years of HRT use, and after cessation of therapy it returns to baseline within a few (maximum five) years.

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

    Ovarian Cancer

    Ovarian cancer is much less common than breast cancer. Epidemiological data from a large-scale meta-analysis indicate a slight increase in the risk of ovarian cancer for women receiving HRT in the form of estrogen monotherapy or combined therapy with estrogens and progestogens.

    These studies (increased risk) become more evident with a duration of therapy of more than five years, and after its termination, the risk gradually decreases with time. The results of a number of other studies, including WHI, indicate that combined HRT is associated with a similar or slightly lower risk of ovarian cancer.

    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, timing of the onset of menopause or the duration of therapy. However, the initial risk depends heavily on age, so the overall risk of stroke in women receiving HRT will increase with age.

    Ischemic heart disease (CHD)

    In randomized controlled clinical trials, no evidence of the protective effect of HRT against myocardial infarction was found in women with / without IHD who received combined HRT with estrogen and progestogen or estrogen monotherapy.

    Combined therapy with estrogen and progestogen

    The relative risk of coronary artery disease during the use of combined HRT with estrogen and progestogen slightly increases. Due to the fact that the absolute risk of coronary heart disease 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.The risk is slightly higher for women over the age of 60 years.

    Therapy with estrogen alone

    Based on data from randomized controlled trials, there was no increased risk of CHD in women with previous hysterectomy who received estrogen alone.

    Other states

    Estrogens can cause fluid retention, which can adversely affect the condition of patients with impaired renal and cardiac function. This group of patients should be under medical supervision.

    Patients with hypertriglyceridemia when taking drugs for HRT should also be under medical supervision, there are reports of very rare cases of a significant increase in the concentration of triglycerides in the blood plasma, which contributes to the development of pancreatitis.

    Estrogens increase the concentration of thyroxine-binding globulin, which leads to a general increase in the concentration of circulating thyroid hormones, as measured by the determination of iodine bound to plasma proteins, the concentration of thyroxine (T4) - chromatographic or radioimmunoassay or triiodothyronine (T3) - radioimmune analysis.The capture test of labeled triiodothyronine shows an elevated level of thyroxin-binding globulin. Concentrations of free hormones T3 and T4 usually do not change.

    Concentrations of other binding proteins in the blood plasma (eg, transcortin and 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, α-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.

    Femoston ® the drug 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:

    Tablets, film-coated, 5 mg + 1 mg.

    Packaging:

    For 28 tablets in a blister of PVC / PVDC / Al foil.

    For 1 or 3 blisters are placed with instructions for use in a cardboard box.

    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 N014320 / 01
    Date of registration:13.04.2009 / 20.05.2016
    Expiration Date:Unlimited
    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: & nbsp06.01.2017
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