Prajisun, 200mg capsules, 10pcs

Composition

Active ingredient:

progesterone 200 mg;

Auxiliary substances:

peanut butter,

soy lecithin.

Capsule shell composition:

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

Pharmacological action

Prajisun is a progestogen, a yellow body hormone. Binding to receptors on the surface of target organ cells, it penetrates into the nucleus, where it activates DNA and stimulates RNA synthesis. 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 a fertilized egg. Reduces excitability and contractility of the uterine and fallopian tube muscles, stimulates the development of the terminal elements of the breast.

Stimulating protein lipase, increases fat reserves, increases glucose utilization, increases 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 doses – suppresses the production of pituitary gonadotropins; reduces azotemia, increases the excretion of nitrogen in the urine. Activates the growth of the secretory part of the acinuses of the mammary glands and induces lactation. Promotes the development of a normal endometrium.

Pharmacokinetics

When taken orally

Suction

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

Metabolism

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

Deduction

It is excreted in the urine as metabolites. 95% of them are glucuronconjugated metabolites, mainly 3-alpha,5-beta-pregnanediol (pregnanedione). These metabolites, which are detected in blood plasma and urine, are similar to substances formed during physiological secretion of the corpus luteum.

When administered vaginally

Suction

Absorption is rapid; progesterone accumulates in the uterus; a high concentration of progesterone in the blood plasma is observed 1 h after use. _{Cmax of}progesterone in blood plasma is reached 2-6 hours after use. When the drug is administered at 100 mg 3 times/day, the average concentration is maintained for 24 hours. When administered in doses of more than 200 mg/day, the concentration of progesterone corresponds to the first trimester of pregnancy.

Metabolism

It is metabolized to form mainly 3-alpha,5-beta-pregnanediol. The concentration of 5-beta-pregnanediol in plasma does not increase.

Deduction

It is excreted in the urine in the form of metabolites, the main part is 3-alpha,5-beta-pregnanediol (pregnandion).

Indications

Disorders associated with progesterone deficiency.

Oral route of use:

• infertility due to luteal insufficiency;
• premenstrual syndrome;
• menstrual disorders due to ovulation or anovulation disorders;
• fibrocystic mastopathy;
• premenopause;
• peri – and postmenopausal hormone replacement therapy (in combination with estrogen-containing drugs).

Vaginal route of use:

• hormone replacement therapy in case of deficiency of progesterone in non-functioning (missing) ovaries (egg donation);
• support the luteal phase in preparation for in vitro fertilization;
• support the luteal phase in spontaneous or induced menstrual cycle;
• premature menopause;
• hormone replacement therapy (in combination with estrogen therapy);
• infertility due to luteal failure;
• prevention of habitual and threatened abortion due to progestin-only failure;
• prevention of uterine fibroids;
• prevention of endometriosis.

Use during pregnancy and lactation

The use of Prajisun during pregnancy is not contraindicated. However, there is a potential risk to the fetus (especially males) when using progesterone in the first 4 months of pregnancy. The use of micronized progesterone in the II-III trimesters of pregnancy can lead to the development of liver diseases in pregnant women. Numerous epidemiological studies have not revealed any cases of fetal malformation when using progesterone during pregnancy.

Progesterone passes into breast milk. Data on the use of the drug during lactation are insufficient to assess the potential risk to the infant.

Contraindications

For oral and vaginal use

• , thrombophlebitis, thromboembolic disorders, intracranial hemorrhage or the presence of these conditions in the anamnesis;
• bleeding from the genital tract of unknown origin;
• incomplete abortion;
• porphyria;
• established or suspected malignant neoplasms of the mammary glands or genitals;
• hypersensitivity to the components of the drug, including peanut butter, soy.

For oral use (optional)

Severe liver diseases at present (including cholestatic jaundice, hepatitis, hepatic cell carcinoma, Dubin-Johnson and Rotor syndromes) or in the anamnesis, if liver function indicators have not returned to normal values.

With caution, the drug should be prescribed for diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraines, depression, hyperlipoproteinemia.

Side effects

With an oral route of use

Breakthrough bleeding or shortening of the normal menstrual cycle, tightness of the mammary glands (usually in the first month of treatment).

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

Feeling tired, migraines, headache, skin rash, itching, jaundice, fluid retention.

For oral and vaginal use

Allergic reactions (urticaria, anaphylactic shock).

Interaction

For oral use

Long-term concomitant use of barbiturates, carbamazepine, hydantoin, or rifampicin may reduce the effectiveness of progesterone.

Despite limited data, it is suggested that activated charcoal and griseofulvin may also reduce the effectiveness of the drug.

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

For vaginal use

Interactions with intravaginal use were not evaluated. Concomitant use of other intravaginal medications should be avoided to avoid disrupting progesterone release and absorption.

How to take, course of use and dosage

Capsules are inserted deep into the vagina.

Absolute progesterone deficiency in women with non-functioning (missing) ovaries (egg donation):  against the background of estrogen therapy,200 mg/day on the 13th and 14th days of the cycle, then 100 mg 2 times/day from the 15th to the 25th day of the cycle, from the 26th day, and in case of pregnancy, the dose increases by 100 mg/day every week, reaching a maximum of 600 mg / day, divided into 3 doses. This dose can be used for 60 days.

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

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

In cases of threatened abortion or in order to prevent habitual abortions that occur against the background of progesterone deficiency: 200-400 mg daily in 2 doses in the first and second trimesters of pregnancy.

Overdose

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

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

Special instructions

The drug should not be used for the purpose of contraception.

With long-term progesterone treatment, periodic medical examinations (including liver function tests) should be performed; treatment should be discontinued if there are deviations in diagnostic tests of liver function or cholestatic jaundice occurs. When using estrogen and / or progestogen-containing drugs, cases of chloasma have been reported, especially in patients with a history of chloasma during previous pregnancy. In women with a tendency to develop chloasma, exposure of the skin to natural or artificial UV radiation can cause or worsen the course of chloasma.

Patients with a history of depression should be monitored, and if severe depression develops, the drug should be discontinued. Patients with concomitant cardiovascular diseases or a history of them should also be monitored periodically by a doctor.

When treated with progesterone, fluid retention may occur, which may affect the course of epilepsy, migraines, bronchial asthma, heart or kidney failure; such patients should be carefully monitored.

Influence on the ability to drive motor vehicles and manage mechanisms

When taken orally, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Capsules

Storage conditions

At temperatures below 25 °C

Shelf life

2 years

Active ingredient

Progesterone

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For menopausal women, For postmenopausal women, For women of childbearing age, For women planning pregnancy, For women, For adults as prescribed by a doctor

Indications

Menopause, Premenstrual syndrome, Menstrual Disorders, Mastopathy