Utrozhestan

Progesterone - Utrozhestan - is a representative of hormonal medications based on hormones of the gonads, which are used in obstetrics and gynecology.

Indications of the utrozhestan

The appointment of Utrozestan is indicated for the correction of disorders related to a deficiency in the body of progesterone.

• Internal reception of Utrozhestan is indicated in such diseases or conditions:
  • expressed PMS, associated with a deficiency of progesterone;
  • anovulatory month cycle;
  • various forms of fibrocystic mastopathy;
  • preclimate;
  • substitution treatment in the menopausal period (gestagens in combination with estrogens);
  • diagnosed deficiency of the luteal phase, infertility;
  • prevention of miscarriage in pregnancy if there is luteal insufficiency;
  • a high risk of premature birth.
• Intravaginal application of Utroshestan is shown:
  • at the primary or secondary etiology of infertility with relative or absolute luteal deficiency (dysovulatory cycles, strengthening of the phase of the yellow body with the maintenance of the IVF protocol, maintenance of the egg donation program);
  • to prevent a habitual miscarriage, or threat of abortion in case of insufficient luteal phase;
  • to prevent the premature onset of labor in patients with shortened cervix, or in patients with pre-existing births;
  • with complexities with internal administration of Utrozhestan (for example, with severe vomiting).

Release form

In the pharmacy network you can buy encapsulated medication Utrozhestan:

• dosage of 100 mg - round, elastic capsules of gelatin, white-yellowish shade;
• dosage of 200 mg - oval, elastic capsules made of gelatin, white-yellowish shade.

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

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

[1], [2], [3], [4]

Pharmacodynamics

The therapeutic effect of Utrozhestan is associated with the presence in the medication of progesterone - the leading hormone of the yellow body, which contributes to the development of a qualitative endometrial layer in women.

Utrozhestan normalizes the transformation of the uterine mucous tissues from the proliferative phase to the secretion phase, and after successful fertilization the uterus helps to restore the condition optimal for strengthening and development of the fertilized egg.

Utrozhestan lowers the degree of excitability and smooths contractions in the muscles of the uterus and tubes, without demonstrating androgenic activity.

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

[5], [6], [7], [8]

Pharmacokinetics

Oral reception.

The increase in the content of progesterone in the serum is observed within an hour after assimilation of Utrozestan from the digestive system. The highest possible level is reached within 1-3 hours after oral administration. 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 basic products of progesterone metabolism are 20α-hydroxy, σ4α-pregnanolone and 5α-dihydroprogesterone.

Utrozhestan is excreted with urinary fluid, as glucuronic exchange products (the main product is 3α, 5β-pregnanene diol). These products are completely equivalent to those that are formed with the natural production of the yellow body.

Intra-vaginal use.

After intravaginal administration, Utrozestan is well absorbed through mucous tissues.

The increase in the content of progesterone in the serum begins to be noted already during the first hour. The highest possible level is found 1-3 hours after intra-vaginal administration.

At a standard dosage (100 mg of Utrozestan 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 that of progesterone in the phase of the yellow body of the monthly cycle with normal ovulation. Utrozestan corrects the correct maturation of the endometrium and helps the embryo to be implanted.

Vaginal administration of large daily amounts of Utrozestan (more than 200 mg) leads to an increase in the progesterone level to those that are usually recorded in pregnant women in the first trimester.

The products of metabolism in serum and urine are identical to those that are found with the natural secretory activity of the ovarian yellow body. First of all, we are talking about such products as 20α-hydroxy, σ4α-pregnanolone and 5α-dihydroprogesterone.

Excretion with urinary fluid occurs in 95% in the form of glucuronic metabolic products, which include 3α, 5β-pregnanene diol.

[9], [10]

Dosing and administration

Oral reception.

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

• With insufficient phase of the yellow body, Utrozhestan is drunk for ten days (usually from the 17th to the 26th day of the cycle).
• When conducting substitution treatment in the period of premenopause, Utrozestan is used against estrogen therapy, during the last two weeks of each treatment course.
• To eliminate the threat of the onset of premature labor, 400 mg of Utrozestan is administered every 6-8 hours, until the threat is eliminated. After relief of the symptoms, the dosage drops slowly until it fixes on the supporting amounts of Utrozestan - for example, 200 mg three times a day. This dosage is acceptable for a woman until the 36th week of gestation.

Use of Utrozestan after 36 weeks is undesirable.

Intravaginal introduction Utrozhestan.

The drug is injected as deep as possible into the vagina. Before you insert the capsule, you should wash your hands well.

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

• With disovulant cycles, or other violations of menstruation, 200 mg of Utrozestan is administered for ten days (most often from 17 to 26 d).
• With absolute insufficiency of the phase of the yellow body (for example, in the case of egg donation), Utrozhestan is prescribed 100 mg on the 13th and 14th days of the required cycle. Starting at day 15 and day 25, the amount of Utrozestan will be 100 mg in the morning and overnight. At the onset of pregnancy from the 26th day of the cycle, the amount of the drug is gradually increased (weekly), to 600 mg per day (three times). Such a scheme is followed up to 60 d.
• Maintaining the phase of the yellow body with IVF involves taking Utrozestan from the evening after embryo transfer, at a daily dosage of 600 mg for three doses (200 mg every eight hours).
• To prevent a threatening miscarriage due to luteal shortage, 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 amount of Utrozestan 200 mg is prescribed, at night, from 22 to 36 weeks of gestation.

[14], [15], [16]

Use of the utrozhestan during pregnancy

The appointment of Utrozestan during pregnancy is acceptable, both in the first and in the following weeks.

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

If Utrozestan is used in the second half of pregnancy, then it is necessary to regularly monitor the degree of liver function.

The possibility of getting a medication in breast milk has not been investigated, therefore, experts do not advise to appoint Utrozestan to nursing patients.

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

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

Contraindications

Utrozhestan should not be treated with medication:

• with an inclination to the allergic process after taking medications with progesterone;
• with severe liver pathologies;
• with probable or diagnosed neoplasia of mammary glands or reproductive organs;
• with vaginal bleeding of unexplained etiology;
• with a failed or partial abortion;
• with thrombosis, thromboembolism;
• with cerebral hemorrhage;
• with porphyrin disease (pathology of pigmentation).

[11], [12]

Side effects of the utrozhestan

With internal use of capsules of Utrozestan, there are possible side effects:

• often: malfunctions of the monthly cycle, amenorrhea, irregular vaginal bleeding, headache;
• infrequent: unpleasant sensations in the mammary glands, drowsiness, short episodes of dizziness, dyspepsia, cholestasis, itchy skin;
• rarely: a depressive state, skin rashes like hives, chloasma.

In addition, there may be other side effects, such as changes in libido, PMS, fever, sleep disorders, venous thrombosis, swelling, weight fluctuations, digestive disorders, allergic reactions.

Dizziness or drowsiness may be signs of a concomitant lowered level of estrogen. The condition of patients is significantly improved after a decrease in the amount of taking Utrozhestan, or after an increase in the dosage of estrogens.

If the course of treatment of Utrozestan was started in the first days of a new monthly cycle, there may be a decrease in the duration of the cycle or the occurrence of non-cyclic bleeding.

With intravaginal administration, it is possible to develop allergic reactions, which are manifested as a sensation of burning, itching, swelling and redness of the skin and mucous membranes.

[13],

Overdose

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

In case of an overdose, it is necessary to take such measures:

• When there is drowsiness or dizziness, reduce the daily amount of Utrozhestan, or take it only at night for 10 days per cycle;
• when there is bleeding or bleeding, correct the treatment regimen and move the method of Utrozhestan to a later term (for example, on the nineteenth day instead of the seventeenth);
• In case of an overdose during the replacement therapy of the premenopause, check the estrogen content of the woman.

[17], [18], [19], [20]

Interactions with other drugs

When taking estrogens with pre-menopause, Utrozestan is prescribed no later than 12 days of the cycle.

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

Strengthening the metabolism of Utrozestan can cause such medications as hypnotics, anticonvulsants, Griseofulvin, Rifampicin, etc.

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

Biological accessibility Utrozhestan can change against the background of regular smoking and drinking.

[21], [22], [23]

Storage conditions

It is possible to store in the temperature range from +18 to + 25 ° C, far from children's access, in darkened dry places.

[24]

Shelf life

Store Utrozestan up to 3 years.

[25]