Utrozhestan

General characteristics. Structure:

Active agent: progesterone natural micronized 100 mg; 200 mg.

Excipients: peanut butter, lecithin soy, gelatin, глицерол, titanium dioxide.

Pharmacological properties:

Gestagenny drug. Progesterone, active agent of the drug Utrozhestan®, is hormone of a yellow body. Contacting receptors on a surface of cells of target organs, gets into a kernel where activating DNA, stimulates RNA synthesis.
Promotes transition of a mucous membrane of a uterus from a phase of the proliferation caused by follicular hormone in a secretory phase. After fertilization promotes transition to a state necessary for development of an oospore. Reduces excitability and contractility of muscles of a uterus and uterine tubes, stimulates development of trailer elements of a mammary gland.
Stimulating a proteinlipaza, increases fat reserves, increases glucose utilization. Increasing concentration of basal and stimulated insulin, promotes accumulation in a glycogen liver, increases production of gonadotropic hormones of a hypophysis; reduces an azotemia, increases removal of nitrogen with urine.
Activates growth of secretory department of an acinus of mammary glands, induces a lactation.
Promotes formation of a normal endometria.

Pharmacokinetics. At intake. Absorption. The micronized progesterone is absorbed from a GIT. Concentration of progesterone in a blood plasma gradually increases within the first hour, Cmax is noted in 1-3 h after reception.
Concentration of progesterone in a blood plasma increases from 0:13 ng/ml to 4:25 ng/ml in 1 h, to 11.75 ng/ml - in 2 h and makes 8.37 ng/ml in 3 h, 2 ng/ml - in 6 h and 1.64 ng/ml - in 8 h after reception.

Metabolism. The main metabolites which are defined in a blood plasma are 20-альфа-гидрокси-дельта-4-альфа-прегнанолон and 5 - alpha dihydroprogesterone.

Removal. It is removed with urine in the form of metabolites, 95% from them are made by glyukuronkonjyugirovanny metabolites, generally 3 alpha, 5 - beta прегнанедиол (прегнандион).
The specified metabolites which are defined in a blood plasma and in urine are similar to the substances which are formed at physiological secretion of a yellow body.

At intravaginalny introduction. Absorption. Absorption happens quickly, progesterone collects in a uterus. High level of progesterone is observed in 1 h after introduction. Cmax of progesterone in a blood plasma is reached in 2-6 h after introduction. At administration of drug on 100 mg of 2 times/days average concentration remains at the level of 9.7 ng/ml during 24 h.
At introduction in doses more than 200 mg/days concentration of progesterone corresponds to the I trimester of pregnancy.

Metabolism. 3 alpha, 5 - beta прегнанедиола are metabolized with education preferential. Level 5 - beta прегнанолона in plasma does not increase.

Removal. It is removed with urine in the form of metabolites, the main part is made by 3 alpha, 5 - beta прегнанедиол (прегнандион). It is confirmed by continuous increase in its concentration (Cmax of 142 ng/ml in 6 h).

Indications to use:

Progesterone-scarce states at women, including:
for intake
— infertility owing to lyuteinovy insufficiency;
— syndrome of premenstrual tension;
— disturbances of a menstrual cycle owing to disturbance of an ovulation or anovulation;
— fibrous and cystous mastopathy;
— premenopauza;
— replaceable hormonal therapy of a menopause (in combination with oestrogenic drugs).

for intravaginalny introduction
— replaceable hormonal therapy at deficit of progesterone at the nonfunctioning (absent) ovaries (at donorship of ova);
— support of a lyuteinovy phase during preparation for extracorporal fertilization;
— support of a lyuteinovy phase in the spontaneous or induced menstrual cycle;
— premature menopause;
— replaceable hormonal therapy (in combination with oestrogenic drugs);
— infertility owing to lyuteinovy insufficiency;
— prevention of the usual or menacing abortion owing to progestinovy insufficiency;
— prevention of a hysteromyoma;
— prevention of endometriosis.

Route of administration and doses:

Duration of therapy is established individually, depending on a clinical situation.
For intake
Drug should be accepted inside, washing down with water. In most cases at insufficiency of progesterone the daily dose of Utrozhestan makes 200-400 mg, divided into 2 receptions (in the morning and in the evening).
At insufficiency of a lyuteinovy phase (a syndrome of premenstrual tension, disturbance of a menstrual cycle, a fibrous and cystous mastopathy, a dysmenorrhea, a premenopauza) the daily dose of drug makes 200 or 400 mg within 10 days (usually from the 17th to the 26th day of a cycle).

At replaceable hormonal therapy in peri-and a postmenopause against the background of reception of Utrozhestan® estrogen about 200 mg/days within 10-12 days are applied.

For intravaginalny introduction
At total absence of progesterone at women with the nonfunctioning (absent) ovaries (donorship of ova) the drug is administered intravaginalno against the background of oestrogenic therapy on 200 mg/days for the 13th and 14th days of a cycle, then - on 100 mg of 2 times/days from the 15th to the 25th day of a cycle, from the 26th day and in case of pregnancy definition the dose increases on 100 mg/days every week, reaching maximum (600 mg/days), divided into 3 introductions. Such dose is usually applied for 60 days.
For maintenance of a lyuteinovy phase during a cycle of extracorporal fertilization it is recommended to enter intravaginalno from 200 to 600 mg/days, since day of an injection of a chorionic gonadotrophin during I and II trimesters of pregnancy.

For maintenance of a lyuteinovy phase in the spontaneous or induced menstrual cycle, at the infertility connected with dysfunction of a yellow body about 200-300 mg/days, since 17th day of a cycle for 10 days are recommended to enter intravaginalno, in case of a delay of periods and diagnosis of pregnancy treatment has to be continued.

In cases of threat of abortion or for prevention of the usual abortions arising against the background of insufficiency of progesterone appoint intravaginalno 200-400 mg daily in 2 receptions (in the morning and in the evening) in I and II trimesters of pregnancy. Capsules enter deeply into a vagina.

Features of use:

Утрожестан® it is impossible to apply for the purpose of contraception.

Influence on ability to driving of motor transport and to control of mechanisms
At administration of drug inside it is necessary to be careful at occupation potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Side effects:

Allergic reactions.
At intake - drowsiness, passing dizziness (in 1-3 h after administration of drug), it is extremely rare - intermenstrual bleeding.

Interaction with other medicines:

At combined use of Utrozhestan® strengthens effect of diuretics, hypotensive medicines, immunodepressants, anticoagulants. Reduces lactogenic effect of oxytocin.

Contraindications:

— hypersensitivity to drug components, including to peanut butter, soy;
— tendency to fibrinferments;
— acute phlebitis or thromboembolisms;
— bleeding of not clear etiology from a genital tract;
— incomplete abortion;
— porphyria;
— the established or suspected malignant new growths of mammary glands and generative organs;
— the expressed abnormal liver functions (for intake).

With care it is necessary to use drug at diseases of cardiovascular system, arterial hypertension, a chronic renal failure, a diabetes mellitus, bronchial asthma, epilepsy, migraine, a depression, a giperlipoproteinemiya, in the period of a lactation.

Use of the drug UTROZHESTAN® at pregnancy and feeding by a breast
Утрожестан® it is shown to use in I and II trimesters of pregnancy.
With care it is necessary to apply at pregnancy (because of risk of emergence of abnormal liver functions) and in the period of a lactation.

Use at abnormal liver functions
Use of drug at a porphyria, the expressed abnormal liver functions is contraindicated (for intake).

Use at renal failures
With care use drug at a chronic renal failure.

Overdose:

Side effects most often demonstrate overdose and disappear spontaneously at a drug dose decline.

Storage conditions:

List B. Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Capsules on 100 mg – 30 pieces in the blister.
Capsules on 200 mg – 14 pieces in the blister. Capsules of an oval form, with a brilliant surface, yellowish color. In capsules – homogeneous oily suspension of white color without visible division of phases. The blister is packed into a cardboard box.