Utrozhestan

Active material: Progesterone
When ATH: G03DA04
CCF: Progestogen
ICD-10 codes (testimony): D25, E28, N60, N80, N94.3, N95.1, N95.3, N96, N97, O20.0, Z31.1
When CSF: 15.11.03
Manufacturer: Laboratories BESINS INTERNATIONAL (France)

Pharmaceutical form, composition and packaging

Capsules soft gelatin, round, bright, yellowish; contents of capsules – oil whitish homogeneous suspension without visible phase separation.

Excipients: peanut oil, soy lecithin, gelatin, glycerol, Titanium dioxide.

15 PC. – blisters (2) – packs cardboard.

Capsules soft gelatin, Oval, bright, yellowish; contents of capsules – oil whitish homogeneous suspension without visible phase separation.

Excipients: peanut oil, soy lecithin, gelatin, glycerol, Titanium dioxide.

7 PC. – blisters (2) – packs cardboard.

Pharmacological action

Progestogens drug. Progesterone, the active ingredient of the drug Utrozhestan, It is a hormone of the corpus luteum. By binding to cell-surface receptors of the target organs, enters the nucleus, where activating DNA, It stimulates the synthesis of RNA.

Promotes transition endometrium from proliferative phase, called follicular hormone, the secretory phase. After fertilization, facilitates the transition to the state, necessary for development of the fertilized egg. Reduces excitability and contractility of the muscles of the uterus and fallopian tubes, stimulates the end of breast cancer.

Stimulating proteinlipazu, increases fat stores, increases glucose utilization. By increasing the concentration of basal and stimulated insulin, It contributes to the accumulation of glycogen in the liver, increases the production of pituitary gonadotropins; reduces azotemia, increases the excretion of nitrogen in urine.

It activates the growth of secretory acini of mammary glands department, induces lactation.

It promotes the formation of normal endometrium.

Pharmacokinetics

If ingestion

Absorption

Micronized progesterone is absorbed from the gastrointestinal tract. The concentration of progesterone in blood plasma increases gradually in the first hour, C_max observed after 1-3 h after administration.

The concentration of progesterone in blood plasma increases from 0.13 ng / ml to 4.25 ng / mL in 1 no, to 11.75 ng / ml – through 2 h and is 8.37 ng / mL in 3 no, 2 ng / ml – through 6 and h 1.64 ng / ml – through 8 no.

Metabolism

The main metabolites, are determined in blood plasma, They are 20-alpha-hydroxy-delta-4-alpha-pregnanolon and 5-alpha dihydroprogesterone.

Deduction

Excreted in the urine as metabolites, 95% of them are glyukuronkonyugirovannye metabolites, mainly 3-alpha, 5-beta-pregnanediol (pregnandion).

These metabolites, are determined in plasma and urine, similar substances, formed at physiological secretion of the corpus luteum.

When administered vaginally

Absorption

Absorption occurs quickly, progesterone accumulates in the uterus. High progesterone levels observed in 1 hours after injection. C_max Plasma progesterone levels achieved after 2-6 hours after injection. With the drug at 100 mg 2 times / day average concentration is maintained at 9.7 ng / ml for 24 no.

When administered in a dose 200 mg / day progesterone concentration corresponds to the I trimester of pregnancy.

Metabolism

It is metabolized to form predominantly 3-alpha, 5-beta-pregnanediola. Level 5-beta-pregnanolona plasma does not increase.

Deduction

Excreted in the urine as metabolites, the main part is 3-alpha, 5-beta-pregnanediol (pregnandion). This is confirmed by the constant increase in its concentration (C_max 142 ng / mL in 6 no).

Testimony

States, associated with progesterone deficiency, including:

orally

- Infertility due to luteal insufficiency;

- Premenstrual tension;

- Menstrual disorders due to violation of ovulation or anovulation;

- Fibrocystic breast disease;

- Premenopausal;

- Hormone replacement therapy menopause (in combination with estrogenic agents).

for intravaginal administration

- Hormone replacement therapy with a deficit of progesterone when dormant (Missing) yaychnykah (when egg donation);

- Maintenance of the luteal phase in preparation for in vitro fertilization;

- Maintenance of the luteal phase in spontaneous or induced menstrual cycle;

- Prezhdevremennaya menopause;

- Hormone replacement therapy (in combination with estrogenic agents);

- Infertility due to luteal insufficiency;

- Prevention of habitual or threatened abortion due to lack of progestin;

- Prevention of uterine fibroids;

- Prevention of endometriosis.

Dosage regimen

The duration of therapy is determined individually, depending on the clinical situation.

Orally

The drug is taken orally, drinking water. In most cases, the daily dose of progesterone deficiency is utrozhestan 200-300 mg, razdelennaya of 2 admission (in the morning and in the evening).

At insufficiency of the luteal phase (premenstrual tension syndrome, menstrual irregularities, shotty breast, dysmenorrhoea, Premenopausal) daily dose is 200 or 400 mg for 10 days (usually with 17 to 26-day cycle).

At hormone replacement therapy menopause in patients receiving estrogens used for Utrozhestan 200 mg / day for 10-12 days.

For intravaginal

At complete absence of progesterone in women with nonfunctioning (missing) ovaries (egg donation) the drug is administered vaginally in the background of estrogen therapy 200 mg / day on the 13th and 14th days of the cycle, then – by 100 mg 2 times / day from the 15th to 25th day of the cycle, from the 26th day in the case of determining the dose is increased by pregnancy 100 mg / day every week, reaching a maximum (800 mg / day), razdelennoy of 3 introduction. Such a dose generally used for 60 days.

To maintenance of the luteal phase during the cycle of in vitro fertilization It should enter by intravaginal 400 to 800 mg / day, starting from the day of the injection of human chorionic gonadotropin during the whole period of pregnancy.

To maintenance of the luteal phase in spontaneous or induced menstrual cycle, infertility, associated with impaired function of the corpus luteum, It should enter by intravaginal 200-300 mg / day, starting with a 17-day cycle for 10 days, in case of delay of menstruation and pregnancy diagnosis, treatment should be continued.

At threatened abortion or for prevention of habitual abortion, resulting in deficiency of progesterone, administered vaginally by 200-400 mg daily 2 introduction (in the morning and in the evening) I and II trimesters.

The capsules are injected deep into the vagina.

Side effect

CNS: ingestion – drowsiness, transient dizziness (through 1-3 h after dosing).

On the part of the reproductive system: ingestion rarely – intermenstrual bleeding.

Other: allergic reactions.

Contraindications

- Tendency to thrombosis;

- Acute phlebitis or embolism;

- Bleeding of unknown etiology of genital tract;

- Incomplete abortion;

- Porphyria;

- Established or suspected malignancy of breast;

- Established or suspected malignancy of genitals;

- Expressed human liver (orally);

- Hypersensitivity to the drug.

FROM caution use in patients with diseases of the cardiovascular system, hypertension, chronic renal failure, diabetes, asthma, epilepsy, migraine, depression, hyperlipoproteinemia, in the III trimester of pregnancy and lactation.

Pregnancy and lactation

Utrozhestan indicated for use in the I and II trimesters.

To use caution in the III trimester of pregnancy (due to the risk of liver dysfunction) and lactation.

Cautions

Utrozhestan should not be used for contraception.

Effects on ability to drive vehicles and management mechanisms

When receiving the drug inside should be careful when lesson potentially dangerous activities, require attention and speed of psychomotor reactions.

Overdose

Side effects often indicate overdose and disappear spontaneously at lower dose.

Drug Interactions

In a joint application Utrozhestan enhances the effect of diuretics, antihypertensive drugs, immunosuppressants, antykoahulyantov.

Utrozhestan reduces the lactogenic effect of oxytocin.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.