Buy Femoston pills 28 pcs
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Clinical Pharmacology

Pharmacodynamics. Estradiol


Estradiol absorption depends on the size of the particles, micronized estradiol is easily absorbed from the gastrointestinal tract.


Estradiol (as well as other estrogens) can be found both in the bound and in the free state. About 98-99% of the dose of estradiol binds to plasma proteins, of which 30-52% is with albumin and about 46-69% is with the sex hormone-binding globulin (GSPH).


After oral administration, estradiol is actively metabolized in the liver. The main unconjugated and conjugated metabolites are estrone and estrone sulfate, possessing estrogenic activity. Estrone sulfate may be subject to enterohepatic recirculation.


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

The dependence of the concentration of estradiol on time and dose

With daily intake of the drug Femoston ® mini, the concentration of estradiol in the blood plasma reaches a constant value in about 5 days. Usually this indicator is achieved within 8-11 days after the start of therapy.



After oral administration, dydrogesterone is rapidly absorbed. The time of onset of the maximum concentration (T max) for Dydrogesterone varies from 30 minutes to 2.5 hours. The bioavailability of Dydrogesterone is 28%.


More than 90% of dydrogesterone and 20a-dihydrodrodosterone (DHD) are bound to plasma proteins.


After oral administration, dydrogesterone is rapidly metabolized to DHD. The maximum concentration of DHD in the blood plasma is reached approximately 1.5 hours after taking the drug. The plasma DGD concentration significantly exceeds the initial concentration of Dydrogesterone, the ratio of the area under the concentration-time curve (AUC) and the maximum concentration (Cmax) of DHD to Dydrogesterone are about 40 and 25, respectively. The half-life for Dydrogesterone is 5-7 hours, for DGD it is 14-17 hours.

A common characteristic of all metabolites of dydrogesterone is the preservation of the 4,6-dien-3-one configuration of the original substance and the absence of 17α-hydroxylation, which leads to the absence of estrogenic and androgenic activities.


Completely dydrogesterone is eliminated after 72 hours. On average, 63% of the dose taken is excreted by the kidneys. Total plasma clearance - 6.4 l / min. DGD is determined in the urine mainly in the form of a conjugate of glucuronic acid.

The dependence of the concentration of dydrogesterone on time and dose

Comparison of the kinetics of single and multiple doses (from 2.5 to 10 mg) shows that the pharmacokinetic properties of Dydrogesterone and DHD do not change when receiving multiple doses.

The equilibrium concentration of Dydrogesterone was reached 3 days after the start of administration.


Hormone replacement therapy for estrogen deficiency disorders in postmenopausal women (no earlier than 12 months after the last menstruation).


active ingredients: 1 tablet contains didgrogesteron micronized 2.5 mg of estradiol micronized hemihydrate, which is equivalent to 0.5 mg estradiol;

excipients: lactose, monohydrate; hypromellose (HPMC 2910); corn starch; colloidal anhydrous silicon dioxide; magnesium stearate; film shell Yellow 1 (macrogol 3350, polyvinyl alcohol, talc, titanium dioxide (E171), iron yellow oxide (E172)).

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Dosage and Administration

For the purpose of HRT and prevention of osteoporosis: inside in continuous mode, 1 tablet per day (preferably at the same time of day), regardless of the meal. The duration of therapy is determined by the ratio of the benefits and risks to the health of a woman and the severity of estrogen deficiency.

Prevention of postmenopausal osteoporosis It is necessary to carry out taking into account the individual tolerance of the drug and possible effects on bone mass, which are dose-dependent.

Adverse reactions

From the reproductive system: possible pain of the mammary glands, breakthrough bleeding, pain in the pelvic region; sometimes - changes in cervical erosion, changes in secretion, dysmenorrhea; rarely - an increase in the mammary glands, premenstrual syndrome; in some cases - a change in libido.

From the digestive system: nausea, flatulence, abdominal pain; sometimes cholecystitis; rarely (0.01-0.1%) - abnormal liver function, in some cases accompanied by asthenia, malaise, jaundice or abdominal pain; very rarely - vomiting.

From the side of the central nervous system: headache, migraine (1-10%); sometimes (0.1-1%) - dizziness, nervousness, depression; very rarely - chorea.

Since the cardiovascular system: sometimes - venous thromboembolism; very rarely - myocardial infarction.

From the hemopoietic system: very rarely (less than 0.01%) - hemolytic anemia.
Dermatological reactions: sometimes - a rash, itching; very rarely - chloasma, melasma, polymorphic erythema, erythema nodosum, hemorrhagic purpura.

Allergic reactions: sometimes - urticaria; in some cases, angioedema.

Other: change in body weight; sometimes - vaginal candidiasis, breast carcinoma, an increase in the size of the leiomyoma; rarely - peripheral edema, intolerance to contact lenses, increased corneal curvature; in some cases (less than 0.01%) - exacerbation of porphyria.


Carefully and under the supervision of a physician to use in patients receiving HRT and having the following conditions (currently or in history): uterine leiomyoma, endometriosis, thrombosis and their risk factors in history, with the presence of risk factors for estrogen-dependent tumors (for example, breast cancer in mothers of the patient), arterial hypertension, benign liver tumor, diabetes mellitus, cholelithiasis, epilepsy, migraine or intense headache, history of endometrial hyperplasia, systemic lupus erythematosus, bronchial asthma, renal edostatochnost, otosclerosis.

Drug interactions

The estrogenic effect of the drug Femoston is reduced, while taking it with drugs that are inducers of microsomal liver enzymes: anticonvulsant (barbiturates, phenytoin, carbamazepine, oxcarbazepine, topiramate, felbamate), antimicrobial drugs (rifampicin, rifabutin, draw, and nefarmat, felbamate), antimicrobial drugs (rifampicin, rifabutin, nefarbomate). with herbal preparations containing Hypericum perforatum (Hypericum perforatum).
The estrogenic effect of the drug Femoston may be enhanced while taking microsomal liver enzymes (ritonavir, nelfinavir) with inhibitor drugs. The interactions of Dydrogesterone with other drugs are not known. The patient should inform the doctor about the medications that she takes during HRT or took before the appointment of the drug Femoston.

Pregnancy and Lactation

The drug is contraindicated for use during pregnancy and lactation (breastfeeding). If pregnancy occurs during treatment with femoston, therapy should be immediately discontinued.

Special instructions

The drug is prescribed to women who are in postmenopausal, only if there are symptoms that adversely affect the quality of life: "hot flashes", increased sweating, sleep disturbance, increased nervous irritability, dizziness, headache, involution of the skin and mucous membranes, especially mucous urogenital system (dryness and irritation of the vaginal mucosa, pain during intercourse).Therapy should continue as long as the benefits of taking the drug outweigh the risk of side effects, and you should strive to prescribe the minimum therapeutically effective doses of the drug. Should strive to achieve the shortest duration of treatment.
Experience with the use of the drug in women over 65 is limited.
Medical examination: Before the appointment or renewal of HRT, a complete medical and family history should be collected and a general and gynecological examination of the patient should be carried out in order to identify possible contraindications and conditions requiring compliance with precautionary measures. During treatment with Femoston 1/5 Konti, it is recommended to conduct periodic examinations, the frequency and nature of which is determined individually, but not less than 1 time per year, based on the collected history, clinical and laboratory parameters. It is advisable to conduct a study of the mammary glands, incl. mammography. Women should be informed about the possible changes in the mammary glands, which are required to inform the attending physician. The use of estrogen may affect the results of the following laboratory tests: determination of glucose tolerance, the study of the functions of the thyroid gland and liver.
Endometrial hyperplasia: for the purpose of timely diagnosis, it is advisable to conduct an ultrasound (US) screening, if necessary, to conduct a histological (cytological) study.
Bloody issues: Breakthrough bleeding and / or acyclic menstrual bleeding from the vagina may occur during the first months of drug treatment. If such bleeding occurs some time after the start of therapy or continues after cessation of treatment, their cause should be established. An endometrial biopsy may be performed to rule out a malignant neoplasm.
In the presence of thromboembolism in history Patients (including family), as well as with the usual miscarriage in history, it is necessary to conduct a study of hemostasis. Until a thorough assessment of the factors for the possible development of thromboembolism or the start of anticoagulant therapy, HRT is not applied. The risk of thrombosis of the deep veins of the lower extremities may temporarily increase with prolonged immobilization, extensive injuries or surgical interventions. If necessary, long-term immobilization after surgical interventions should stop HRT 4-6 weeks before the operation, the resumption of the drug is possible after the full restoration of the physical activity of the woman. If thrombosis develops after initiation of therapy, HRT should be abolished. You should contact your doctor if any of the symptoms indicate a possible thromboembolism (pain or swelling of the lower extremities, sudden chest pain, dyspnea, visual impairment).
Breast and ovarian cancer: in women who received long-term HRT, the frequency of diagnosis of breast cancer increases, which returns to the initial level within 5 years after discontinuation of therapy. On the background of HRT, an increase in the density of breast tissue during mammography may be observed, which may make it difficult to diagnose breast cancer. The increase in the risk of ovarian cancer with the use of estrogen drugs for HRT has not been proven.
Other states: Estrogens can cause fluid retention, which can adversely affect the condition of patients with impaired cardiac and renal function. In women with triglyceridemia in the background of HRT in very rare cases, there may be a significant increase in plasma triglyceride concentration, which contributes to the development of pancreatitis.Estrogens increase the content of thyroid-binding globulin, which leads to an overall increase in the concentration of circulating thyroid hormones (concentrations of free hormones T C and T 4 usually do not change). Levels of other serum binding proteins (corticoid binding globulin, sex hormone binding globulin) may also increase, leading to an increase in the concentration of circulating corticosteroids and sex hormones. Concentrations of free or biologically active hormones do not change. An increase in the concentration of other plasma proteins (substrate angiotensinogen / renin, a-1-antitrypsin, ceruloplasmin) is possible.


Symptoms: estradiol and didrogesteron - substances with low toxicity. No cases of overdose have been reported. Theoretically, in the case of an overdose, symptoms such as nausea, vomiting, drowsiness, and dizziness may occur.

Treatment: symptomatic.

Studies and clinical trials of Femoston (Click to expand)

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