Femoston

Femoston is an anti-climacteric drug of the estrogen-gestagen type, which has a “calendar” regimen for administration.

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Indications Femoston

It is used in HRT to relieve symptoms caused by estrogen deficiency in women in menopause. The drug is prescribed at least 6 months after the last menstruation.

In prophylaxis, the drug is used to prevent osteoporosis during menopause. The drug is used for women who have a high risk of fractures and who cannot take other drugs prescribed to prevent bone loss.

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Release form

The release is carried out in tablets. The form of LS Femoston 1/5 is produced in 28 pieces inside a "calendar" pack.

Femoston 1/10 is packaged in “calendar” packs of 14 tablets of 1 mg + 14 tablets of 1 mg + 10 mg.

Femoston 2/10 is packaged in “calendar” packs of 14 pieces of 2 mg + 14 pieces of 2 mg + 10 mg.

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Pharmacodynamics

Femoston is a complex hormonal drug used to relieve symptoms of estrogen deficiency, and also for the treatment of uterine bleeding of a dysfunctional nature.

Medicinal estradiol is similar to estradiol produced by the body. The drug is used to compensate for the lack of estrogens that develops during menopause, and also eliminates psychoemotional and vegetative disorders that occur during menopause, against the background of which the following problems are noted:

• hyperhidrosis with hot flashes;
• involution of the epidermis with mucous membranes (especially the mucous membranes of the genitourinary tract, including the vaginal mucosa - because of this, a woman feels discomfort during sexual intercourse);
• increased nervous excitability;
• dizziness along with headaches;
• sleep disorders;
• loss of bone mass or osteoporosis (especially if various risk factors are observed, such as recent long-term therapy with GCS, early menopause, smoking, asthenic type of constitution, etc.).

At the same time, estradiol is able to reduce the values of total cholesterol, as well as low-density lipoproteins, while increasing the values of high-density lipoproteins.

The gestagenic element of the drug (dydrogesterone) stimulates the development of the secretory stage of the endometrial cycle, and in addition, reduces the likelihood of carcinogenesis or endometrial hyperplasia, which are associated with the effects of estrogen.

Dydrogesterone does not have estrogenic, androgenic, anabolic or glucocorticosteroid properties.

To ensure the most effective preventive effect of HRT, therapy should be started as soon as possible after the onset of menopause.

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Pharmacokinetics

When the drug is taken orally, estradiol is rapidly absorbed. Its biotransformation process occurs in the liver. Its decay products are estrone, and also estrone in the form of sulfate. Elimination of estrone together with estrone glucuronides occurs mainly with urine.

The substance dydrogesterone is also absorbed from the gastrointestinal tract at high speed after oral administration of the drug. It is completely biotransformed, and the main breakdown product is 20-dihydrodydrogesterone. Excretion of metabolic products occurs mainly with urine.

The half-life of dydrogesterone is about 5-7 hours, and the main decay product is about 14-17 hours. Complete excretion of these elements occurs after 72 hours.

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Dosing and administration

Femoston is often used only on days strictly designated for this by the attending physician, taking into account the individual characteristics of the patient's menstrual cycle. If menstruation is absent, the tablets should be taken on the days when it was expected to appear. If amenorrhea has been observed for 12 months, the use of the drug can be started on any day.

Use of LS in form 1/5.

The medicine should be taken continuously - 1 tablet once a day (it is recommended to do this at the same time), without reference to food intake. One cycle lasts for a full 4 weeks (1 pack of the drug contains 28 tablets). There is no need to take breaks between treatment cycles.

To eliminate the symptoms of menopause, the drug intake begins with the minimum effective dose. Therapy should be started with the use of 1/5 of the drug form. Taking into account the time of the onset of menopause, the degree of severity of the symptoms developing during it and the therapeutic effectiveness, the dosage regimen can be adjusted.

If a switch from another drug containing estrogen-progestogen elements is required, for cyclic use the patient must first complete a full 4-week treatment cycle and only then begin using Femoston (any day will do). No break is needed between courses.

Mode of use of the drug in the form of 1/10.

The drug in the form of 1/10 is taken without reference to the time of food consumption. The estrogen contained in it is intended for daily use during the first 2 weeks of the course. The progestogen element should be added in the last 14 days of each 4-week cycle.

Therapy begins with the following scheme: single intake of 1 (white) tablet per day (at the same time) during the first 14 days of the course. After that, in accordance with the instructions, gray tablets are taken (according to a similar scheme). There is no need to observe breaks between such 4-week cycles.

Sequential combination HRT should be initiated with the 1/10 form, with the dosage then adjusted if necessary (taking into account the clinical efficacy of the treatment).

To switch from a similar medication, you must complete the full course of treatment and then start taking Femoston 1/10. The switch can be made on any day.

Scheme for the use of form LS 2/10.

Estrogen must be taken continuously, and progestogen is taken during the period from day 15 to day 28 of the course. During the first 14 days, pink tablets are taken, one per day, and then, from day 15, following the instructions, yellow tablets are taken.

Often the starting dose of estradiol is 1 mg, which is why sequential complex HRT requires starting with the 1/10 form and then gradually increasing the dose if necessary.

To switch from other medications to the 2/10 formulation, you must first complete a full 28-day treatment cycle (the switch can be made on any day).

Use of the drug in case of accidental missed dose.

If you miss a dose, you must take the pill as quickly as possible. If more than 12 hours have passed since the missed dose, you must continue the course by taking the next dose from the pack (do not take the missed dose).

Taking a double dose to make up for a missed dose is not recommended as it will increase the likelihood of bleeding and vaginal spotting.

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Use Femoston during pregnancy

Femoston is prohibited to use if pregnancy has been definitely established, and in addition, if there is a suspicion of its occurrence. In addition, it cannot be prescribed to women during lactation.

Sometimes the drug is used at the stage of pregnancy planning. Among the indications for such a prescription are:

• conditions caused by a lack of estrogen and developing in the form of stage 1 deficiency (these are conditions during which, at the end of the first stage (follicular) of the menstrual cycle, the thickness of the endometrial layer is a maximum of 7-8 mm);
• infertility caused by hormonal imbalance.

An excessively thin endometrium can be a factor leading to luteal phase disorder, as a result of which the woman is also unable to become pregnant.

Often, when planning, doctors prescribe taking the medicine in a 2/10 form.

The level of estradiol inside the tablets used during the first 2 weeks of the menstrual cycle is such that Femoston does not suppress ovulation (this distinguishes it from other contraceptives), while at the same time simulating the first stage of the menstrual cycle, and also stimulating the growth and proliferation of endometrial cells.

The use of drugs containing estradiol in combination with dydrogesterone helps the secretory transformation of the inner uterine layer, which is required to ensure normal implantation of the fertilized egg with the subsequent onset of pregnancy. This suggests that Femoston 2/10 is able to stabilize the menstrual cycle.

The drug in the form of 2/10 during pregnancy planning should be used from the 1st day of the menstrual cycle - in the amount of 1 tablet / day, during the period of 4 full weeks. Stopping the course before the end of the pack of medicine is prohibited - due to the fact that this can lead to hormonal imbalance, the symptoms of which are bleeding of varying intensity, and preventing the onset of pregnancy.

When using the drug at the planning stage, it is also necessary to additionally increase the activity of the 2nd stage of the cycle (luteal). For this purpose, from the 14th day of the course, the use of the drug in combination with Duphaston (or its analogue) is prescribed.

The gestagenic element in Duphaston is dydrogesterone, which allows potentiating the positive medicinal effect on the woman's body as a whole and on the condition of the endometrium. The medicine should be taken 1 tablet twice a day, for 2 full weeks.

Pregnancy during Femoston administration occurs only in exceptional cases. Usually, a more realistic option is its occurrence after taking the drug for several separate cycles, but in most cases it still occurs after the completion of therapy.

Only occasionally is it permitted to use the drug at the stage of an existing pregnancy - if a woman needs endometrial support. But such a decision can only be made by an experienced and qualified doctor.

Contraindications

Among the contraindications:

• women who have previously been diagnosed with malignant neoplasms of the progestogen- or estrogen-dependent type, or if there is a suspicion of the presence of this pathology;
• suspected or already diagnosed breast cancer;
• vaginal bleeding of unknown origin;
• untreated endometrial hyperplasia (pathological growth of the lesion);
• history of venous thromboembolism or thromboembolism diagnosed during the current period (this includes pulmonary embolism with deep venous thrombosis);
• the presence of various thrombophilic disorders in a woman (this includes thrombophilia associated with a deficiency of antithrombin, as well as coagulation protein type C or protein S, which is its cofactor);
• thromboembolic arterial pathologies, including angina pectoris or myocardial infarction (its active phase or cases where the disease was suffered recently);
• active forms of liver pathologies, and in addition, cases when the patient’s liver biochemical values did not recover after the disease was eliminated;
• hematoporphyria;
• the presence of high sensitivity to estradiol with dydrogesterone or auxiliary elements of the drug;
• teenagers, as well as children who are not yet 18 years old.

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Side effects Femoston

Among the side effects that most often occur due to taking the drug: various pain sensations (abdominal, head, and pelvic), migraine attacks, nausea, bloating, metrorrhagia. In addition, cramps in the legs, severe sensitivity or soreness in the mammary glands, asthenia, the occurrence of bloody vaginal discharge during menopause, as well as weight gain or loss.

Quite often during clinical trials the following manifestations were noted:

• thrush, increase in the size of uterine fibroids, ulcers in the cervix, changes in libido, as well as cervical fluid secretion and dysmenorrhea;
• a state of depression, increased feelings of nervousness and dizziness;
• pain in the back;
• DVT and PE;
• pathologies affecting the functioning of the gallbladder;
• allergy, which manifests itself in the form of hives, itching and rash, and in addition the appearance of peripheral edema.

Occasionally, taking medications can lead to the following disorders:

• increased sensitivity to contact lenses;
• problems with the liver, often manifested in the form of malaise, abdominal pain and asthenia with jaundice;
• increase in the curvature of the cornea;
• enlargement of the mammary glands;
• development of PMS.

Disorders such as stroke, hemolytic anemia, vomiting, choreic hyperkinesis, myocardial infarction or vascular purpura may occur sporadically. In addition, nodular or multiform erythema, melanosis or chloasma (sometimes they persist even after stopping the drug), symptoms of intolerance and Quincke's edema, as well as worsening of hematoporphyria may occur.

At the same time, sometimes therapy with estrogen-progestogen drugs in women leads to the development of tumors (benign and malignant, or of unknown origin), an increase in the size of progestogen-dependent tumors, an increase in plasma triglyceride values and thyroid hormone levels, and in addition to this, to the appearance of fibrocystic lesions in the mammary glands. Blood pressure may also increase, acute blockage in the arteries may occur, varicose veins may develop, peripheral vascular pathology, pancreatitis (accompanies existing hypertriglyceriderma), dyspepsia, SLE, urinary incontinence and cystitis-like syndrome may develop. In addition, symptoms of dementia may appear and existing epilepsy may worsen.

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Overdose

There were no reports of poisoning from the drug.

Both estrogen and progestogen are substances with low toxicity.

In theory, intoxication may increase the intensity of side effects such as vomiting, drowsiness, nausea and dizziness.

In such cases, it is most likely not necessary to prescribe any specific symptomatic procedures (even if the child is intoxicated).

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Interactions with other drugs

Tests for therapeutic interactions of the drug have not been conducted, but there is evidence that certain drugs can affect the effectiveness of progesterones with estrogens.

Anticonvulsants (such as phenobarbital or phenytoin) and antimicrobial drugs (including rifampicin with nevirapine or efavirenz) potentiate the biotransformation of these elements. This effect develops due to the ability to induce enzymes of hemoprotein P450, which participate in the metabolic processes of the drug.

Ritonavir together with nelvinavir are drugs that have a powerful inhibitory effect on the activity of CYP3A4 isoenzymes, as well as A5 with A7. When combined with steroid hormones, they cause activation of the indicated hemoproteins.

Herbal preparations, the main element of which is St. John's wort, are capable of stimulating the process of progestogenic and estrogenic biotransformation by influencing the CYP 3A4 isoenzyme.

There are facts confirming that the activity of metabolic processes of progestogens with estrogens increases due to a decrease in the medicinal effectiveness of these elements, and also affects the profile of uterine bleeding.

At the same time, estrogens are capable of destroying the biotransformation of other components, competitively inhibiting the hemoproteins of the P450 system, which participate in the biotransformation of the active elements of these drugs.

This should be taken into account when prescribing estrogens in combination with drugs that have a narrow drug index (including tacrolimus with cyclosporine and theophylline with fentanyl). Such combinations can lead to an increase in the plasma values of these components to a toxic level. As a result, careful monitoring of the drug over a long period of time may be required, as well as a reduction in the dose of the above drugs.

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Storage conditions

Femoston should be stored in places closed to small children. The temperature level during such storage should be a maximum of 30 ^o C.

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Shelf life

Femoston can be used for 3 years from the date of manufacture of the therapeutic agent.

Analogues

Analogues of the drug are Klimonorm, Trisequens and Kliogest with Divina.

Reviews

Femoston receives many comments on medical forums (they apply to all its forms of release), which have contradictory assessments. Usually, such reviews describe the experience of using the drug at the stage of pregnancy planning or during menopause.

Women who have benefited from the drug highlight good tolerability and low frequency of negative symptoms among its advantages. It is noted that it quickly stabilizes the condition, eliminating unpleasant climacteric manifestations, generally improves well-being, and also has a positive effect on the condition of the epidermis and helps restore the cycle if it has been disrupted. In addition, the drug's ease of use is also noted.

Negative opinions are related to the development of negative symptoms in patients (rashes, swelling, depression, weight gain, decreased activity, joint pain, etc.), and also to the lack of the desired result.

If we consider the reviews of specialists, which are based on clinical test data, we can summarize that the drug has high medicinal effectiveness both in therapy and in the prevention of various conditions that arise due to early depletion of ovarian activity.

At the same time, all patients undergoing treatment showed good tolerance to the drug. Tests showed that the treatment had a positive effect on the well-being of patients (for example, on blood lipid levels).

During the therapy, a significant increase in the values of maximum oxygen consumption was also noted, as well as an increase in the protective effect of estrogen on bones with the help of dydrogesterone.

This allows us to conclude that doctors confirm the need for early initiation and differentiated selection of the type of HRT in women with problems in ovarian function.

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