Prajisan pills (Progesterone)

Active ingredient :

progesterone 200 mg;

Excipients:

peanut butter,

soy lecithin.

The composition of the capsule shell :

 sorbitol solution 70% (non-crystallized), glycerol, gelatin, titanium dioxide, purified water.

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

By stimulating protein lipase, it 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 it accelerates, and in large doses it suppresses the production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases the excretion of nitrogen in the urine. Activates the growth of the secretory part of the acini of the mammary glands and induces lactation. Promotes the development of normal endometrium.

Pharmacokinetics

When taken orally

Suction

Micronized progesterone is well absorbed from the gastrointestinal tract. The concentration of progesterone in the blood plasma gradually increases during the first hour, C _max  is observed 1-3 hours after ingestion.

Metabolism

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

breeding

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

When administered vaginally

Suction

Absorption is fast; progesterone accumulates in the uterus; a high concentration of progesterone in the blood plasma is observed 1 hour after administration. Cmax _of  progesterone in plasma is reached 2-6 hours after administration. With the introduction of the drug 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 with the formation of predominantly 3-alpha, 5-beta-pregnandiol. The concentration of 5-beta-pregnandiol in plasma does not increase.

breeding

It is excreted in the urine as metabolites, the main part is 3-alpha, 5-beta-pregnandiol (pregnandione).

Progesterone deficiency disorders.

Oral route of administration:

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

Vaginal route of administration:

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

The use of Prajisan during pregnancy is not contraindicated. However, there is a potential risk to the fetus (special male) when using progesterone during 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 cases of fetal anomalies when using progesterone during pregnancy.

Progesterone passes into breast milk. Data on the use of the drug during lactation is not enough to assess the potential risk to the infant.

For oral and vaginal use

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

For oral use (optional)

Severe liver disease at present (including cholestatic jaundice, hepatitis, hepatocellular carcinoma, Dubin-Johnson syndrome, Rotor syndrome) or in history, 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, migraine, depression, hyperlipoproteinemia.

By oral route

Bleeding "breakthrough" 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 drug regimen, or switching to the vaginal route of administration. These effects are usually the first signs of an overdose.

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

For oral and vaginal routes of administration

Allergic reactions (urticaria, anaphylactic shock).

When administered orally

With long-term simultaneous use of barbiturates, carbamazepine, hydantoin or rifampicin may reduce the effectiveness of progesterone.

Despite limited data, it is assumed 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

Interaction with intravaginal use has not been evaluated. The simultaneous administration of other intravaginal drugs should be avoided in order to avoid impaired progesterone release and absorption.

The capsules are inserted deep into the vagina.

Absolute progesterone deficiency in women with non-functioning (absent) 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 is increased 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 of the luteal phase during preparation for in vitro fertilization: it is recommended to take from 200 to 600 mg / day, starting from the day of injection of human chorionic gonadotropin during the first and second trimesters of pregnancy.

Support of the luteal phase in a spontaneous or induced menstrual cycle, with infertility associated with impaired function of the corpus luteum, 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 diagnosis of pregnancy, 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 I and II trimesters of pregnancy.

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 switched to the vaginal route of administration: in case of a 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.

The drug should not be used for contraception.

With prolonged treatment with progesterone, it is necessary to periodically conduct medical examinations (including a study of liver function); treatment should be discontinued if there are abnormal liver function diagnostic tests or if cholestatic jaundice occurs. When using estrogen and / or progestogen-containing drugs, there have been cases of chloasma, especially in patients with a history of chloasma during a previous pregnancy. In women with a tendency to develop chloasma, exposure of the skin to natural or artificial UV radiation can cause or exacerbate chloasma.

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

During treatment with progesterone, fluid retention may occur, which may affect the course of epilepsy, migraine, bronchial asthma, heart or kidney failure; such patients should be closely monitored.

Influence on the ability to drive vehicles and control mechanisms

When taken orally, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.