Femoston 5/1mg. 28 tab

Femoston 5/1mg. 28 tab

Regular price
$48.00
Sale price
$48.00
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per 

Femoston 5/1 mg.  28 tab. 

Dosage form
Round, biconvex tablets, film-coated in orange-pink color with the engraving "379" - on one side of the tablet and the engraving of the letter "S" over the "Ў" mark - on the other side of the tablet.

Composition
1 film-coated tablet 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; colloidal silicon dioxide - 1.4 mg; magnesium stearate - 0.7 mg. Shell: Mixture for film coating Orange 1 [hypromellose - 2.844 mg, macrogol 400 - 0.284 mg, titanium dioxide (E171) - 0.8 mg, yellow iron dye (E 172) - 0.048 mg, red iron oxide dye (E 172) - 0.024 mg] - 4.0 mg.

Pharmacodynamics
Estradiol, which is part of the drug Femoston® conti, is identical to endogenous human estradiol, which is the most active estrogen. Estradiol replenishes the estrogen deficiency in the female body in menopausal women and reduces menopausal symptoms during the first weeks of treatment. Hormone replacement therapy (HRT) with Femoston® Conti prevents bone loss in the postmenopausal period or after ovariectomy. Dydrogesterone is a progestogen that is effective when administered orally and has activity similar to parenterally administered progesterone. During HRT, the inclusion of dydrogesterone provides a complete secretory transformation of the endometrium, thereby reducing the risk of developing endometrial hyperplasia increased under the influence of estrogen.

Pharmacokinetics
Estradiol Absorption The absorption of estradiol depends on the particle size, micronized estradiol is rapidly absorbed from the gastrointestinal tract. The distribution of estrogen can be detected both in a bound and in a 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 globulin that binds sex hormones (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 may undergo enterohepatic recirculation. Excretion Estron and estradiol are excreted in the conjugated with glucuronic acid state mainly by the kidneys. The half-life (T1 / 2) is 10-16 hours. Estrogens pass into breast milk. Dependence of estradiol concentration on time and dose With daily use of the drug Femoston® Conti, the concentration of estradiol in blood plasma reaches a constant value after about 5 days. Usually this indicator is achieved within 8-11 days after the start of therapy. Dydrogesterone Absorption After oral administration, it is rapidly absorbed and completely metabolized. The values ​​of the time of onset of the maximum concentration (Tmax) for dydrogesterone vary from 30 minutes to 2.5 hours. The absolute bioavailability of dydrogesterone is 28%. Distribution More than 90% of dydrogesterone and DHD bind to plasma proteins. Metabolism The main metabolite of dydrogesterone is 20? -Dihydrohydrogesterone (DGD). The maximum concentration of DHD in blood plasma is reached approximately 1.5 hours after taking the drug. The concentration of DHD in blood plasma significantly exceeds the initial concentration of dydrogesterone, the ratio of the area under the pharmaceutical concentration-time curve (AUC) and the maximum concentration (Cmax) of DGD to dydrogesterone are about 40 and 25, respectively. The half-life for dydrogesterone is 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-dien-3-one of the starting material and the absence of 17β-hydroxylation, which leads to the absence of estrogenic and androgenic activity. Withdrawal Fully dydrogesterone is excreted after 72 hours. On average, 63% of the dose taken is excreted by the kidneys. The total plasma clearance is 6.4 l / min. DGD is determined in the urine mainly in the form of conjugates of glucuronic acid. The dependence of the concentration of dydrogesterone on time and dose. The drug is characterized by linear pharmacokinetics with single and multiple oral administration in a 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 when taking multiple doses. An equilibrium concentration of dydrogesterone is reached 3 days after treatment.