Duphaston

General characteristics. Structure:

Active agent: дидрогестерон 10 mg

Excipients: lactoses monohydrate; gipromelloza; starch corn; silicon dioxide colloid; magnesium stearate  

Cover: Opadry white Y-1–7000 (gipromelloza, polyethyleneglycol 400, titanium dioxide (E171).

Pharmacological properties:

Pharmacodynamics. Дюфастон® (дидрогестерон) is a progestogen, active at intake. Didrogesteron on the molecular structure, chemical and pharmacological properties is very close to natural progesterone. Because дидрогестерон testosterone is not derivative, it has no the side effects characteristic of the majority of synthetic progestogens, so-called "androgenic" progestogens. Didrogesteron has no oestrogenic, androgenic, anabolic, glucocorticoid and thermogene activity. Acting as a progestagenny component of the replacement hormonal therapy (RHT) in a menopause, дидрогестерон promotes preservation of favorable effect of estrogen on a blood lipid profile. However, unlike estrogen which usually negatively influences system of a blood coagulation дидрогестерон does not exert impact on coagulation indicators. Does not influence negatively metabolism of carbohydrates and function of a liver. Didrogesteron at oral administration selectively influences an endometria, thereby preventing the increased risk of development of a hyperplasia of an endometria and/or carcinogenesis in the conditions of excess of estrogen. It is shown in all cases of endogenous insufficiency of progesterone. Drug has no contraceptive action. At treatment didrogesterony the therapeutic effect is reached without suppression of an ovulation or disturbance of menstrual function. Didrogesteron does possible conception and preservation of pregnancy during treatment.

Pharmacokinetics. After intake дидрогестерон it is quickly soaked up from a GIT, Cmax in a blood plasma is reached in 2 h. Linkng with proteins of plasma makes 97%. Metabolism in a liver happens by a hydroxylation of ketonic groups of the 20th carbon atom. Along with it also the hydroxylation of methyl groups of the 21st carbon atom and in very insignificant volume — 16-α carbon atom was observed. With urine from 56 to 79% are removed; in 24 h about 85% are removed, in 72 h removal process practically comes to an end. Data on a delay or strengthening of action of a didrogesteron at bounded function of kidneys did not arrive today. Metabolites are found in urine preferential in the form of conjugates of glucuronic acid. Presence at urine of not changed substance is not revealed.

Indications to use:

Progesteronovy insufficiency: endometriosis; the infertility caused by lyuteinovy insufficiency; the usual and menacing abortion against the background of the established deficit of progesterone, a premenstrual syndrome, a dysmenorrhea, irregular periods, a secondary amenorrhea (in combination with therapy by estrogen), dysfunctional uterine bleedings.

ZGT: for neutralization of proliferative effect of estrogen on an endometria within ZGT at women with the frustration caused by a natural or surgical menopause at an intact uterus.

Route of administration and doses:

Inside. Endometriosis: on 10 mg 2–3 times a day from 5 to 25 day of a cycle or are continuous.

The infertility (caused by lyuteinovy insufficiency): 10 mg/day from 14 to 25 day of a cycle, conduct a course continuously during 6 cycles following one after another and more; it is recommended to continue treatment in the first months of pregnancy (as at usual abortion).

The menacing abortion: 40 mg once, then — on 10 mg each 8 h before disappearance of symptoms.

Usual abortion: 10 mg 2 times a day to 20 weeks of pregnancy, with the subsequent gradual reduction of a dose.

Premenstrual syndrome: on 10 mg 2 times a day from 11 to 25 day of a cycle.

Dysmenorrhea: on 10 mg 2 times a day from 5 to 25 day of a cycle.

Irregular periods: on 10 mg 2 times a day from 11 to 25 day of a cycle.

Amenorrhea: estrogen — once a day from 1 to 25 day, Dyufaston® — on 10 mg 2 times a day from 11 to 25 day of a cycle.

Dysfunctional uterine bleedings: for a bleeding stop — on 10 mg 2 times a day within 5–7 days; for prevention of bleeding — on 10 mg 2 times a day from 11 to 25 day of a cycle.

ZGT in combination with estrogen: at the continuous scheme of reception of estrogen — on 10 mg of Dyufastona® once a day within 14 days within a 28-day cycle. At the cyclic scheme of reception of estrogen: Дюфастон® — 10 mg once a day during the last 12–14 days of reception of estrogen. If the biopsy or ultrasonography demonstrate insufficient reaction to progestagenny drug, a daily dose of a didrogesteron it is necessary to increase up to 20 mg.

Features of use:

At some patients breakthrough bleedings which prevent by increase in a dose of drug can be observed. In case of purpose of a didrogesteron in a combination with estrogen (for example, for ZGT) it is necessary to get acquainted with the contraindications and preventions connected using estrogen attentively. Before use of a combination of a didrogesteron and estrogen (for ZGT) the full anamnesis has to be built. During treatment it is recommended to carry out control of individual portability of ZGT periodically. The patient has to be informed about what changes in mammary glands she should report to the doctor or the nurse. The researches including mammography should be conducted according to the standard screening of patients. At the women receiving ZGT, exact assessment of risk and advantage is estimated over time. Sometimes within the first months of treatment developing of breakthrough bleedings is possible. If breakthrough bleedings arise after some period of administration of drug or proceed after a course of treatment, it is necessary to study the reason, to make an endometria biopsy for the purpose of an exception of malignant changes in an endometria.

States at which observation is necessary: patients should be inspected carefully in the presence in the anamnesis of a progesteronzavisimy tumor (for example meningiomas), and also in case of its progressing during pregnancy or during the previous hormonal therapy.

Other states: patients with genetically caused intolerance of a galactose, insufficiency of lactase or a sprue should not accept this drug.

Drug does not influence ability to driving and other mechanisms.

Side effects:

From system of a hemopoiesis: in isolated cases — hemolitic anemia.
From immune system: seldom or never — hypersensitivity reactions.
From TsNS: head pain / migraine.
From gepatobiliarny system: seldom — the insignificant abnormal liver functions which sometimes are followed by weakness or an indisposition, jaundice and pain in a stomach.
From reproductive system: developing of breakthrough bleedings which can be prevented increase in a dose of drug is in rare instances possible; hypersensitivity of mammary glands.
From skin and hypodermic cellulose: seldom — skin rash, an itch, a small tortoiseshell; very seldom — a Quincke's edema.
General frustration: very seldom — peripheral hypostases.

Interaction with other medicines:

Inductors of microsomal enzymes of a liver (phenobarbital, rifampicin) can accelerate metabolism of a didrogesteron and reduce effect.

Contraindications:

Hypersensitivity to a didrogesteron or other components of drug.

With care — a skin itch during the previous pregnancy.
Now patients have no data on negative effect of a didrogesteron with a chronic renal failure.

Use at pregnancy and feeding by a breast
Drug can be used during pregnancy (see the field "Indications"). Didrogesteron is allocated with maternal milk therefore breastfeeding during administration of drug is not recommended.

Overdose:

Messages on symptoms of overdose are not registered. At accidental reception in a dose, is much higher than therapeutic, the gastric lavage is recommended.

Treatment: symptomatic. The specific antidote does not exist.

Storage conditions:

In the dry place, at a temperature not above 30 °C, in original packaging.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In the blister of 20 pieces; in a box the cardboard 1 blister.