Femostone 1,28 pcs.

Pharmacodynamics

Estradiol, the estrogen in Femoston, is identical to endogenous human estradiol. Estradiol replenishes estrogen deficiency in women after menopause and provides effective treatment of psychoemotional and vegetative menopausal symptoms: “hot flashes”, increased sweating, sleep disorders, increased nervous irritability, dizziness, headache, involution of skin and mucous membranes, especially of mucous membranes of urogenital system (dryness and irritation of vaginal mucosa, painfulness during intercourse). Hormone replacement therapy (HRT) with Femostone prevents loss of bone mass in the postmenopausal period caused by estrogen deficiency. Femostone leads to changes in lipid profile toward a decrease in total cholesterol and LDL and an increase in HDL.

Didrogesterone is a progestagen effective when taken orally which completely provides the onset of endometrial secretion phase, thereby reducing the risk of endometrial hyperplasia and/or carcinogenesis increased with estrogen. Didrogesterone has no estrogenic, androgenic, anabolic or glucocorticosteroid activity.

The combination of 1 mg of estradiol with didrogesterone is a modern low-dose ZGT regimen.

Pharmacokinetics

Micronized estradiol is easily absorbed after oral administration. It is metabolized in the liver to estrone and estrone sulfate, which also undergoes hepatic biotransformation. Glucuronides of estrone and estradiol are excreted mainly with the urine.

Dydrogesterone after oral administration is quickly absorbed from the gastrointestinal tract. It is completely metabolized. The main metabolite is 20-dihydrodihydrogesterone, which is present in the urine mainly in the form of glucuronic acid conjugate. Complete excretion of didrogesterone occurs after 72 hours.

Indications

Climax, Osteoporosis

• Hormone replacement therapy for disorders due to estrogen deficiency in perimenopausal women (not earlier than 6 months after last menstruation) or in postmenopausal women;
• Postmenopausal osteoporosis prophylaxis in women at high risk of fractures when other medications are intolerant or contraindicated.

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Active ingredient

Dydrogesterone, Estradiol

Composition

1 tablet contains:

the active ingredient:

estradiol 1 mg;

excipients:

Lactose monohydrate,

Hypromellose,

Corn starch,

colloidal silicon dioxide,

magnesium stearate

Composition of the shell:

Opadry OY-1-7000 white.

The tablets are gray, round, biconvex, with “S” embossed above the “dlt” symbol on one side, “379” – on the other side; the core of the tablet is white (14 pieces in a blister).

1 tablet contains:

the active ingredients:

estradiol 1 mg,

didrogesterone 10 mg;

excipients:

Lactose monohydrate,

Hypromellose,

corn starch,

silicon dioxide colloid,

magnesium stearate.

Composition of the shell:

Opadry OY-8243 gray.

How to take, the dosage

Actually, preferably at the same time of the day, regardless of meals, 1 tablet a day without interruption. Femostone 1/10 is taken according to the following regimen: in the first 14 days of a 28-day cycle, take 1 white tablet daily (from half of the package with an arrow marked “1”) containing 1 mg of estradiol, and in the remaining 14 days, take 1 gray tablet daily (from half of the package with an arrow marked “2”) containing 1 mg of estradiol and 10 mg of didrogesterone.

Patients whose menstruation has not stopped are advised to start treatment on the first day of their menstrual cycle (day 1 of the start of their period).

Patients with irregular menstrual cycles are advised to start treatment after 10-14 days of progestagen monotherapy.

Patients whose last menstrual period was more than 1 year ago can begin treatment at any time.

Interaction

Drugs that are inducers of microsomal liver enzymes (barbiturates, phenytoin, rifampicin, rifabutin, carbamazepine) may weaken the estrogenic effect of Femostone.

Ritonavir and nelfinavir, although known as inhibitors of microsomal metabolism, may act as inducers when taken simultaneously with steroid hormones. Herbal preparations containing St. John’s wort can stimulate estrogen and progestagen metabolism.

The interactions of didrogesterone with other drugs are unknown.

The patient should tell her doctor about any medications she is currently taking or was taking before Femostone was prescribed.

Special Instructions

Before prescribing or renewing ZGT, a complete medical and family history should be taken and a general and gynecologic exam should be performed to identify possible contraindications and conditions that require precautionary measures. During treatment with the drug it is recommended to periodically examine women (frequency and nature of examinations shall be determined individually). In addition, it is reasonable to conduct a breast examination and/or mammography in accordance with the accepted norms, taking into account clinical indications. The use of estrogens may affect the results of the following laboratory tests: determination of glucose tolerance, thyroid and liver function tests.

Publicly recognized risk factors for thrombosis and thromboembolism on ZGT are thromboembolic complications in the history, severe forms of obesity (body mass index over 30 kg/m2) and systemic lupus erythematosus. There is no generally accepted opinion about the role of varicose veins in the development of thromboembolism.

The risk of developing deep vein thrombosis of the lower extremities may temporarily increase with prolonged immobilization, extensive trauma or surgery. If prolonged immobilization is necessary after surgery, consideration should be given to temporarily discontinuing MHT 4 to 6 weeks prior to surgery.

The benefits and risks of MHT should be carefully evaluated when considering MHT in patients with recurrent deep vein thrombosis or thromboembolism treated with anticoagulants.

If thrombosis develops after starting MHT, the drug should be discontinued. Patients should be advised to consult a physician if they experience the following symptoms: painful swelling of the lower extremities, sudden loss of consciousness, dyspnea, visual disturbances.

There is data showing a slight increase in the rate of breast cancer detection in women who have been on ZHT for a long time (more than 10 years). The likelihood of being diagnosed with breast cancer increases with duration of treatment and returns to normal 5 years after discontinuing MHT.

Patients who were previously on estrogen-only MHT should be particularly carefully screened before starting treatment to detect possible endometrial hyperstimulation. Breakthrough uterine bleeding and mild menstrual-like bleeding may occur during the first months of treatment with the drug. If, despite dose adjustments, such bleeding does not stop, the drug should be discontinued until the cause of bleeding is determined. If bleeding recurs after a period of amenorrhea or continues after treatment withdrawal, its etiology should be established. This may require an endometrial biopsy.

Femostone is not a contraceptive. Patients in perimenopause are advised to use a non-hormonal contraceptive.

There is no effect on the ability to drive or operate machinery.

Synopsis

Two kinds of film-coated tablets.

White film-coated tablets, round, biconvex, engraved “379” on one side; white rugged surface on the fracture.

Gray film-coated tablets, round, biconvex, engraved “379” on one side; at fracture – white rugged surface.

Contraindications

• established or suspected pregnancy;
• breastfeeding period;
• diagnosed or suspected breast cancer, breast cancer history;
• diagnosed or suspected oestrogen-dependent malignancies;
• vaginal bleeding of unclear etiology;
• active or recent arterial thromboembolism;
• acute liver disease or history of liver disease (until normalization of liver function tests);
• untreated endometrial hyperplasia;
• high sensitivity to any of the components of the drug;
• porphyria.

With caution–Patients receiving ZGT who have the following conditions (current or past) should be under close medical supervision:

• leiomyoma of the uterus, endometriosis;
• thrombosis or their risk factors in a history;
• arterial hypertension;
• doble liver tumor;

diabetes mellitus;

• cholletiasis;
• epilepsy;
• migraine or severe headache;
• hyperplasia endometrium in anamnesis;
• systemic lupus erythematosus;
• bronchial asthma;
• renal failure;
• otosclerosis.
• After consultation with a physician, the drug should be discontinued in cases such as:
• appearance of jaundice or worsening of liver function;
• serious rise in BP;
• pregnancy;
• manifestation of any contraindication.

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Side effects

Blood and lymphatic system disorders: very rarely (

Nervous system disorders: headache, migraine (in 1-10%); sometimes (in 0.1-1%) – dizziness, nervousness, depression, change in libido; very rarely – chorea.

Cardiovascular system: sometimes – venous thromboembolism; very rare – myocardial infarction.

Gastrointestinal disorders: nausea, abdominal pain, flatulence; very rare – vomiting.

Liver and biliary tract: sometimes – cholecystitis; rare (0.01-0.1%) – liver dysfunction, sometimes accompanied by asthenia, malaise, jaundice or abdominal pain.

Skin and subcutaneous fat: sometimes – allergic reactions, rash, urticaria, pruritus, peripheral edema; very rarely – chloasma, melasma, erythema multiforme, erythema nodosa, hemorrhagic purpura, angioedema.

Reproductive system and mammary glands: mammary gland pain, breakthrough bleeding, pelvic pain; sometimes – changes in cervical erosion, changes in secretion, dysmenorrhea; rarely – breast enlargement, premenstrual-like syndrome.

Others: changes in body weight; sometimes – vaginal candidiasis, breast carcinoma, increased size of leiomyoma; rarely – contact lens intolerance, increased corneal curvature; very rarely – exacerbation of porphyria.

Overdose

In case of overdose, symptoms such as: nausea, vomiting, mammary gland tension, dizziness, abdominal pain, drowsiness/weakness and bleeding “withdrawal” may develop.

Treatment is symptomatic

Pregnancy use

The drug is contraindicated in pregnancy and during breast-feeding. If pregnancy occurs during treatment with the drug, therapy should be stopped immediately.

Similarities

Femoston 1/5, Femoston 2/10, Femoston mini