Pragisan, 200 mg capsules 10 pcs

Pragisan is a gestagen, a corpus luteum hormone. Binding to receptors on the surface of target organ cells, it penetrates the nucleus where, by activating DNA, it stimulates RNA synthesis. It promotes the transition of the uterine mucosa from the proliferation phase caused by follicular hormone to the secretory phase, and after fertilization to the state necessary for the development of the fertilized egg. It reduces the excitability and contractility of the uterine muscles and fallopian tubes and stimulates the development of mammary gland terminal elements.

Stimulating protein lipase, increases fat stores, increases glucose utilization by increasing the concentration of basal and stimulated insulin, promotes the accumulation of glycogen in the liver, increases the production of aldosterone; In small doses accelerates, and in large – suppresses production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases excretion of nitrogen in the urine. Activates the growth of the secretory division of mammary gland acini and induces lactation. Promotes the development of normal endometrium.

Pharmacokinetics

In oral administration

p> Absorption

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

Metabolism

Metabolized in the liver with the participation of the CYP 2C19 isoenzyme. The main metabolites that are determined in blood plasma are 20-alpha-hydroxy-delta-4-alpha-pregnanolone and 5-alpha-dihydroprogesterone.

Excretion

Extracted in the urine as metabolites. 95% of these are glucuronconjugated metabolites, mainly 3-alpha, 5-beta-pregnandiol (pregnandione). These metabolites, which are determined in plasma and urine, are similar to substances produced during physiological corpus luteum secretion.

In vaginal administration

Intake

Absorption is rapid; progesterone accumulates in utero; high plasma concentrations of progesterone are observed 1 h after administration. C_max progesterone in blood plasma is reached 2-6 hours after administration. When administered in doses of 100 mg 3 times/day, the average concentration is maintained for 24 hours. When administered in doses greater than 200 mg/day, the progesterone concentration corresponds to the first trimester of pregnancy.

Metabolism

Metabolized with the formation of predominantly 3-alpha, 5-beta-pregnandiol. The plasma concentration of 5-beta-pregnandiol is not increased.

Elimination

Extracted in the urine as metabolites, the main part is 3-alpha, 5-beta-pregnandiol (pregnandion).

Indications

Progesterone deficiency disorders.

The oral route of administration:

Vaginal route of administration:

Active ingredient

Composition

Active ingredient:

Progesterone 200 mg;

Associates:

Peanut butter,

soy lecithin.

Capsule shell composition:

sorbitol solution 70% (uncrystallized), glycerol, gelatin, titanium dioxide, purified water.

How to take, the dosage

The capsules are inserted deep into the vagina.

The absolute deficiency of progesterone in women with non-functioning (absent) ovaries (egg donation): on estrogen therapy at 200 mg/day on days 13 and 14 of the cycle, then 100 mg 2 times/day from days 15 to 25 of the cycle, from day 26, and if pregnancy is established, the dose increases by 100 mg/day each week, reaching a maximum of 600 mg/day, divided into 3 doses. This dose can be used for 60 days.

Luteal phase support during preparation for in vitro fertilization: It is recommended to take 200 to 600 mg/day starting from the day of chorionic gonadotropin injection during the first and second trimesters of pregnancy.

Luteal phase support in spontaneous or induced menstrual cycle, in infertility associated with impaired corpus luteum function, it is recommended to take 200-300 mg/day starting on day 17 of the cycle for 10 days, in case of delayed menstruation and pregnancy diagnosis, treatment should be continued.

In cases of threatened abortion or to prevent recurrent abortions due to progesterone insufficiency: 200-400 mg daily in 2 doses in I and II trimesters of pregnancy.

Interaction

In oral administration

In prolonged concomitant use, barbiturates, carbamazepine, guidantoin or rifampicin may decrease the effectiveness of progesterone.

Despite limited data, it has been suggested that activated charcoal and griseofulvin may also decrease the effectiveness of the drug.

Progesterone may increase the therapeutic, pharmacological or toxic effects of cyclosporine, theophylline and troleandomycin.

In vaginal use

Interactions with intravaginal use have not been evaluated. Concomitant administration of other intravaginal medications should be avoided to avoid impairing the release and absorption of progesterone.

Special Instructions

The drug should not be used for contraceptive purposes.

Long-term treatment with progesterone requires periodic medical examinations (including liver function tests); treatment should be discontinued if there are abnormal diagnostic tests of liver function or if cholestatic jaundice occurs. Chloasma has been reported with estrogen and/or progestogen-containing medications, especially in patients with a history of chloasma during a previous pregnancy. In women who are prone to developing chloasma, exposure of the skin to natural or artificial UV irradiation may cause or exacerbate the course of chloasma.

Patients with a history of depression should be monitored, and if severe depression develops, the drug should be withdrawn. Patients with a history or concomitant cardiovascular disease should also be monitored periodically by a physician.

The treatment with progesterone may cause fluid retention, which may affect the course of epilepsy, migraine, bronchial asthma, heart, or renal failure; these patients should be monitored closely.

Impact on driving and operating machinery

When taken orally, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

For oral and vaginal use

For oral use (optional)

Severe liver disease at present (including Cholestatic jaundice, hepatitis, hepatic cell carcinoma, Dubin-Johnson syndrome, Rotor syndrome) or a history if liver function has not returned to normal values.

The drug should be used with caution in cardiovascular diseases, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression, hyperlipoproteinemia.

Side effects

In the oral route of administration

Bleeding “breakthrough” or shortening of the normal menstrual cycle, mammary gland tightness (usually in the first month of treatment).

Drowsiness, transient dizziness (usually 1 to 3 h after administration), nausea. These side effects can be reduced by reducing the dose, changing the regimen of the drug, or switching to the vaginal route of administration. These effects are usually the first signs of overdose.

Sensation of fatigue, migraine, headache, skin rash, itching, jaundice, fluid retention.

In oral and vaginal routes of administration

Allergic reactions (urticaria, anaphylactic shock).

Overdose

Symptoms: drowsiness, transient dizziness, shortening of normal menstrual cycle.

Treatment: dose reduction or correction of the mode of administration, for example, in case of drowsiness and dizziness – 200 mg taken before bedtime from the 12th to the 14th day of the cycle or switch to vaginal route of administration: in case of shortening of menstrual cycle – start treatment later in the cycle, for example from the 19th day, instead of the 17th. If necessary, symptomatic treatment is carried out.

Pregnancy use

The use of Prajisan in pregnancy is not contraindicated. However, there is a potential risk to the fetus (especially males) when progesterone is used in the first 4 months of pregnancy. Micronized progesterone use in the second and third trimesters of pregnancy can lead to the development of liver disease in pregnant women. Numerous epidemiologic studies have found no cases of fetal abnormal development when progesterone is used in pregnancy.

Progesterone penetrates into breast milk. There is insufficient data on the use of the drug during lactation to assess the potential risk to the infant.

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