Utrogestan

The progesterone drug Utrozhestan is a representative of hormonal medications based on sex gland hormones, which are used in obstetrics and gynecology.

Indications Utrogestan

Utrozhestan is indicated for the correction of disorders related to progesterone deficiency in the body.

• Internal use of Utrozhestan is indicated for the following diseases or conditions:
  • severe PMS associated with progesterone deficiency;
  • dysovulatory, anovulatory monthly cycle;
  • various forms of fibrocystic mastopathy;
  • premenopause;
  • substitution treatment during menopause (gestagens in combination with estrogens);
  • diagnosed luteal phase deficiency, infertility;
  • prevention of the risk of miscarriage during pregnancy if there is luteal insufficiency;
  • high risk of premature birth.
• Intravaginal use of Utrozhestan is indicated:
  • in case of primary or secondary etiology of infertility with relative or absolute luteal deficiency (dysovulatory cycles, strengthening of the corpus luteum phase during the IVF protocol, egg donation program);
  • to prevent habitual miscarriage or the threat of termination of pregnancy due to insufficient luteal phase;
  • to prevent premature onset of labor in patients with a shortened cervix, or in patients with a history of premature birth;
  • in case of difficulties with internal administration of Utrozhestan (for example, in case of severe vomiting).

Release form

You can buy the encapsulated drug Utrozhestan in the pharmacy chain:

• 100 mg dosage – round, elastic gelatin capsules, white-yellowish in color;
• 200 mg dosage – oval, elastic gelatin capsules, white-yellowish in color.

The active ingredient is progesterone (100 or 200 mg, respectively).

A soft cardboard box may contain 30 capsules of 100 mg or 14 capsules of 200 mg.

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Pharmacodynamics

The therapeutic effect of Utrozhestan is associated with the presence of progesterone in the drug, the leading hormone of the corpus luteum, which promotes the growth of a high-quality endometrial layer in women.

Utrozhestan normalizes the transformation of the mucous tissues of the uterus from the proliferative phase to the secretory phase, and after successful fertilization helps the uterus to acquire a state that is optimal for the strengthening and development of the fertilized egg.

Utrozhestan reduces the level of excitability and smoothes out contractions of the muscles of the uterus and tubes, without demonstrating androgenic activity.

Utrozhestan blocks the release of luteinizing and follicle-stimulating hormone releasing factors in the hypothalamus, inhibits the synthesis of gonadotropic hormones and inhibits ovulation.

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Pharmacokinetics

Oral administration.

An increase in serum progesterone levels is observed within an hour after Utrozhestan is absorbed from the digestive system. The maximum possible level is reached within 1-3 hours after oral administration of Utrozhestan: after 60 minutes - 4.25 ng per ml, after 120 minutes - 11.75 ng per ml, after 4 hours - 8.37 ng per ml, after six hours - 2 ng per ml, after eight hours - 1.64 ng per ml.

The main products of progesterone metabolism are 20α-hydroxy, σ4α-pregnanolone and 5α-dihydroprogesterone.

Utrozhestan is excreted with urine fluid as glucuronic metabolic products (the main product is 3α,5β-pregnanediol). These products are completely equivalent to those formed during the natural production of the corpus luteum.

Intravaginal use.

After intravaginal administration, Utrozhestan is well absorbed through the mucous tissues.

An increase in serum progesterone levels begins to be observed within the first hour. The highest possible level is detected 1-3 hours after intravaginal administration.

At a standard dosage (100 mg Utrozhestan before bedtime), it is possible to approximate and maintain a natural and stable level of serum progesterone, which is approximately 9.7 ng per ml. This level is close to the progesterone indicators in the corpus luteum phase of the monthly cycle during normal ovulation. Utrozhestan corrects the correct maturation of the endometrium, helps the embryo to implant.

Vaginal administration of large daily amounts of Utrozhestan (more than 200 mg) results in an increase in progesterone levels to levels usually recorded in pregnant women in the first trimester.

The metabolites in serum and urine are identical to those found in the natural secretory activity of the corpus luteum of the ovary. First of all, we are talking about such products as 20α-hydroxy, σ4α-pregnanolone and 5α-dihydroprogesterone.

Excretion with urine occurs in 95% in the form of glucuronic metabolic products, which include 3α, 5β-pregnanediol.

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Dosing and administration

Oral administration of Utrozhestan.

The standard daily dose of Utrozhestan can be 200-300 mg in one or two doses (for example, 200 mg at night and 100 mg in the morning).

• In case of insufficient corpus luteum phase, Utrozhestan is taken for ten days (usually from the 17th to the 26th day of the cycle).
• When conducting replacement therapy during the premenopausal period, Utrozhestan is used against the background of estrogen therapy, during the last two weeks of each treatment course.
• To eliminate the threat of premature labor, 400 mg of Utrozhestan is prescribed every 6-8 hours until the threat is eliminated. After the symptoms have been relieved, the dosage is reduced slowly until it is fixed at the maintenance amounts of Utrozhestan - for example, 200 mg three times a day. This dosage is acceptable for a woman to take up to 36 weeks of gestation.

It is not advisable to use Utrozhestan after 36 weeks.

Intravaginal administration of Utrozhestan.

The drug is inserted as deeply as possible into the vagina. Before inserting the capsule, it is necessary to wash your hands thoroughly.

The average daily dosage of Utrozhestan is 200 mg, but this amount can be changed at the discretion of the doctor.

• For dysovulatory cycles or other menstrual irregularities, 200 mg of Utrozhestan is prescribed for ten days (most often from the 17th to the 26th day of the cycle).
• In case of absolute insufficiency of the corpus luteum phase (for example, in case of egg donation), Utrozhestan is prescribed at 100 mg on the 13th and 14th day of the required cycle. Starting from the 15th day and up to the 25th day, the amount of Utrozhestan will be 100 mg in the morning and at night. If pregnancy occurs, from the 26th day of the cycle, the amount of the drug is gradually increased (weekly), until reaching 600 mg per day (in three doses). This regimen is followed until the 60th day of the cycle.
• Maintenance of the corpus luteum phase during IVF involves taking Utrozhestan in the evening after embryo transfer, at a daily dosage of 600 mg in three doses (200 mg every eight hours).
• To prevent threatened miscarriage due to luteal deficiency, 200-400 mg per day is prescribed up to the twelfth week of gestation.
• To prevent premature onset of labor in patients with a shortened cervix, or in women with previously diagnosed premature birth, a daily dose of Utrozhestan 200 mg is prescribed, at night, starting from the 22nd to 36th week of gestation.

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Use Utrogestan during pregnancy

The use of Utrozhestan during pregnancy is permissible, both in the first and subsequent weeks.

To date, there is no information on cases of negative effects of Utrozhestan on fetal development.

If Utrozhestan is used in the second half of pregnancy, it is necessary to regularly monitor the level of liver functionality.

The possibility of the drug getting into breast milk has not been studied, so experts do not recommend prescribing Utrozhestan to nursing patients.

There is information about an increased risk of developing hypospadias - a congenital anomaly of the urethra in boys - if

Utrozhestan is used during pregnancy to prevent habitual miscarriage or the threat of miscarriage due to luteal deficiency. The doctor must warn the patient about this.

Contraindications

You should not start treatment with the drug Utrozhestan:

• if you are prone to allergic reactions after taking medications containing progesterone;
• in severe liver pathologies;
• in case of probable or diagnosed neoplasia of the mammary glands or reproductive organs;
• for vaginal bleeding of unknown etiology;
• in case of failed or partial abortion;
• in thrombosis, thromboembolism;
• in case of cerebral hemorrhage;
• in porphyria disease (pigment formation pathology).

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Side effects Utrogestan

When taking Utrozhestan capsules internally, the following side effects are possible:

• common: menstrual irregularities, amenorrhea, irregular vaginal bleeding, headache;
• uncommon: discomfort in the mammary glands, drowsiness, short-term episodes of dizziness, dyspepsia, cholestasis, skin itching;
• rare: depressive state, skin rashes such as urticaria, chloasma.

In addition, other side effects may be observed, such as changes in libido, PMS, increased body temperature, sleep disorders, venous thrombosis, edema, weight fluctuations, digestive disorders, allergic reactions.

Dizziness or drowsiness may be signs of concomitant decreased estrogen levels. The condition of patients improves significantly after reducing the amount of Utrozhestan taken, or after increasing the dosage of estrogens.

If the course of treatment with Utrozhestan was started in the first days of a new monthly cycle, a decrease in the duration of the cycle or the appearance of non-cyclic bleeding may be observed.

With intravaginal administration, allergic reactions may develop, which manifest as a burning sensation, itching, swelling and redness of the skin and mucous membranes.

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Overdose

Signs of taking excessive amounts of Utrozhestan include increased side effects, as well as the appearance of dysmenorrhea, metrorrhagia, and euphoric states.

In case of overdose, the following measures should be taken:

• if drowsiness or dizziness occurs, reduce the daily amount of Utrozhestan, or take it only at night for 10 days per cycle;
• if bleeding or hemorrhages occur, adjust the treatment regimen and move the intake of Utrozhestan to a later date (for example, on the nineteenth day instead of the seventeenth);
• In case of overdose during replacement therapy of premenopause, monitor the woman's estrogen levels.

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Interactions with other drugs

When taking estrogens during premenopause, Utrozhestan is prescribed no later than day 12 of the cycle.

The combination of Utrozhestan with β-adrenergic agonists may require a reduction in the dosage of the latter.

Increased metabolism of Utrozhestan can be caused by such medications as sleeping pills, anticonvulsants, Griseofulvin, Rifampicin, etc.

Certain antibiotics (for example, tetracycline series) can alter the balance of microflora in the intestine, which, in turn, can lead to disruption of the intestinal-hepatic steroid cycle.

The bioavailability of Utrozhestan may change with regular smoking and alcohol consumption.

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Storage conditions

Utrozhestan can be stored at temperatures ranging from +18 to +25°C, out of reach of children, in dark, dry places.

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Shelf life

Utrozhestan is stored for up to 3 years.

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