Utrojestan (progesterone) capsules 200 mg. №14

Description

Utrojestan (progesterone) capsules 200 mg. №14

Composition

active substance: progesterone;
1 capsule contains micronized progesterone 200 mg;
Excipients: sunflower oil, soy lecithin, gelatin, glycerin, titanium dioxide (E 171), purified water.

Dosage form
Capsules.

Basic physical and chemical properties:
200 mg capsules: Oval, soft, slightly yellowish gelatin capsules containing a whitish oil suspension.

Pharmacotherapeutic group

Gonadal hormones. Progestogens.

ATX code G03D A04.

Pharmacological properties

The pharmacological properties of the drug are due to progesterone – one of the hormones of the corpus luteum, which promotes the formation of a normal secretory endometrium in women. Causes the transition of the uterine mucosa from the proliferation phase to the secretory phase, and after fertilization promotes its transition to the state necessary for the development of the fertilized egg. Reduces the excitability and contractility of the muscles of the uterus and fallopian tubes. Has no androgenic activity. Has a blocking effect on the secretion of hypothalamic factors releasing LH and FSH, inhibits the formation of gonadotropic hormones by the pituitary gland and ovulation.

Oral use
The level of increase in progesterone in plasma is observed from the first hour after absorption of the drug in the digestive tract. The highest level of progesterone in blood plasma is observed in 1-3 hours after drug administration (after 1 hour – 4,25 ng / ml, after 2 hours – 11,75 ng / ml, after 4 hours – 8,37 ng / ml, after 6 hours – 2 ng / ml and 1.64 ng / ml after 8 hours). The major metabolites of plasma progesterone are 20α-hydroxy, δ4α-pregnanolone and 5α-dihydroprogesterone. The drug is excreted in the urine in the form of glucuronide metabolites, the main of which is 3α, 5β-pregnanenediol (pregnandiol). These metabolites are identical to the metabolites formed by the physiological secretion of the corpus luteum.

Intravaginal use
After insertion into the vagina, progesterone is rapidly absorbed by the mucous membrane.
The increase in plasma progesterone levels begins in the first hour, the highest level in blood plasma is reached in 1-3 hours after application.
At the average prescribed dose (100 mg of progesterone per night) Utrozhestan allows to achieve and maintain physiological and stable levels of plasma progesterone (on average at the level of 9.7 ng / ml), similar to that in the luteal phase of the menstrual cycle with normal ovulation. Thus, Utrozhestan stimulates adequate maturation of the endometrium, promotes embryo implantation.
At higher doses (above 200 mg per day), increasing gradually, the vaginal method of administration allows to achieve plasma progesterone levels similar to those during the first trimester of pregnancy.
Metabolism: Plasma and urine metabolites are identical to those found during physiological secretion of the ovarian corpus luteum: plasma is mainly 20α-hydroxy, δ4α-pregnanolone and 5α-dihydroprogesterone. Urinary excretion is 95% in the form of glucuronide metabolites, the main component of which is 3α, 5β-pregnanenediol (pregnandiol).

Indication

Disorders associated with progesterone deficiency.

Oral use
Gynecological:
disorders associated with progesterone deficiency, namely:

• premenstrual syndrome,
•  menstrual disorders (disovulation, anovulation),
• fibrocystic mastopathy,
• premenopausal period;
• hormone replacement therapy in menopause (in combination with estrogen therapy);
• infertility in lutein deficiency.

Obstetric:
prevention of habitual miscarriage or threat of miscarriage on the background of lutein deficiency;
threat of premature birth.

Intravaginal use
Decreased ability to fertilize in primary or secondary infertility in partial or complete luteal insufficiency (disovulation, maintenance of the luteal phase during preparation for in vitro fertilization, egg donation program). Prevention of habitual miscarriage or threat of miscarriage in luteal insufficiency.
Prevention of preterm birth in women with a short cervix or in women with a history of premature birth.
Impossibility or restriction of oral administration of the drug.

Contraindication:

• hypersensitivity to any component of the drug;
• severe liver dysfunction;
• suspected or confirmed neoplasia of the breast or genitals;
• undiagnosed vaginal bleeding;
• unsuccessful or incomplete abortion;
• thrombophlebitis. Thromboembolic disorders;
• hemorrhage in the brain;
• porphyria.

Use during pregnancy or breastfeeding.

Utrozhestan is not contraindicated during pregnancy, including in the first weeks.
During the period of drug use, no case of adverse effects of the drug on the fetus was observed.
Liver function should be monitored during the second and third trimesters of pregnancy.
The intake of progesterone in breast milk has not been studied in detail. Therefore, its use should be avoided during breastfeeding.
There is evidence of the possible development of hypospadias, the use of progestogens during pregnancy to prevent miscarriage, or the risk of miscarriage due to lutein deficiency, which should be reported to the patient.

Method of application and dosage

The duration of treatment depends on the nature of the disease.

Oral use
In most cases, the average daily dose is 200-300 mg in 1 or 2 doses (200 mg in the evening, at bedtime, and 100 mg in the morning, if necessary).
In case of luteal phase insufficiency (premenstrual syndrome, menstrual disorders, premenopause, fibrocystic mastopathy): take for 10 days (usually from the 17th to the 26th day of the cycle inclusive).
With hormone replacement therapy for menopause: As estrogen therapy alone is not recommended, progesterone should be used as an adjunct to the last 2 weeks of each course of therapy, followed by one week of support for any replacement therapy during which withdrawal bleeding may occur.
At the risk of premature birth: take 400 mg of Utrozhestan every 6-8 hours until the symptoms disappear. The effective dose and frequency of application are selected individually depending on the clinical manifestations of the threat of premature birth. After the symptoms disappear, the dose of Utrozhestan is gradually reduced to maintenance (for example, 200 mg 3 times a day). At this dose, the drug can be used up to 36 weeks of pregnancy.
The use of progesterone after 36 weeks of pregnancy is not recommended.

Intravaginal use
The capsules are inserted deep into the vagina in a supine position.
Wash your hands thoroughly before each use so that no detergent remains on your hands.
The average dose is 200 mg of progesterone per day (1 capsule of 200 mg or 2 capsules of 100 mg, divided into 2 doses, morning and evening, which are injected deep into the vagina, if necessary with an applicator). The dose can be increased depending on the patient’s response.

With partial insufficiency of the luteal phase (disovulation, menstrual irregularities), the daily dose is 200 mg for 10 days (usually from the 17th to the 26th day of the cycle).
In case of complete luteal phase insufficiency [complete absence of progesterone in women with non-functioning (absent) ovaries (egg donation)]: the dose of progesterone is 100 mg on the 13th and 14th day of the transfer cycle. From the 15th to the 25th day of the cycle, the dose of progesterone is 200 mg, divided into two doses (morning and evening). From the 26th day, in the case of early diagnosis of pregnancy, the dose is increased, gradually (every week) by 100 mg of progesterone per day, reaching a maximum of 600 mg of progesterone per day, divided into three doses. This dosage should be followed until the 60th day.
Maintenance of the luteal phase during the cycle of in vitro fertilization: treatment is carried out starting in the evening of the day of embryo transfer, at the rate of 600 mg per day in 3 doses (200 mg once every 8 hours).
In case of risk of miscarriage or for the prevention of habitual miscarriage due to lutein deficiency: 200-400 mg per day (100-200 mg per dose every 12 hours) up to 12 weeks of pregnancy.
Prevention of preterm birth in women with a short cervix or in women with a history of premature birth: the dose is 200 mg per day and is used in the evening before bedtime from the 22nd to the 36th week of pregnancy.
Children There are no clinical data on the use of the drug in children.

Children

There are no clinical data on the use of the drug in children.

Overdose

Symptoms of an overdose may be manifested by symptoms of adverse reactions, including drowsiness, dizziness, euphoria, dysmenorrhea, a decrease in the duration of the cycle, metrorrhagia.

In some individuals, the usual dose may be excessive due to the existing or secondary occurrence of unstable endogenous progesterone secretion, hypersensitivity to the drug, or a very low concomitant blood level of estradiol.

In such cases, it is enough:

• reduce the dose of progesterone or prescribe progesterone in the evening before bedtime for 10 days per cycle in case of drowsiness or transient dizziness;
• postpone the start of treatment to a later date in the cycle (for example, the nineteenth day instead of the 17th) in case of its reduction or bleeding;
• check whether the level of estradiol is sufficient in a patient receiving premenopausal hormone replacement therapy.

Side effects:

• disorders of the reproductive system and mammary glands: changes in menstruation, amenorrhea, intermenstrual bleeding;
• violation of the central nervous system: headaches, drowsiness, short-term feeling of dizziness;
• hepatobiliary system: cholestatic jaundice.