Prajisan: instructions for use, reviews on forums and price. Use during pregnancy

Compound

One tablet of Prajisan contains 100 or 200 mg of the active ingredient progesterone + excipients (soy lecithin, glycerol , peanut oil, water, sorbitol , gelatin, titanium dioxide).
Vaginal gel contains 80 mg of progesterone per 1 gram of the drug + sorbic acid, guar gum, liquid paraffin, hypromellose K100M, hydrogenated palm oil glyceride, water.

Pharmacodynamics and pharmacokinetics

The drug is a hormone of the corpus luteum . The hormone is able to penetrate into the nucleus of target organs and stimulate RNA and activate DNA .

Prajisan transfers the uterine mucosa to the secretion phase from the proliferative phase . Thus, specific conditions are created for the implantation of a fertilized egg to occur. The muscles of the uterus relax, the organ becomes less sensitive to the action of Oxytocin .

The active substance stimulates lipoprotein lipases , increases fat reserves, and activates the process of inducing Insulin Aldosterone production .

When the gel is applied to the mammary gland, there is a decrease in the proliferation and mitotic activity of the epithelium in the ducts. When taken orally, the permeability of the capillaries of the mammary gland tissue decreases, and the swelling of the connective stroma subsides.

The medicine is quickly and almost completely absorbed. Maximum concentration is achieved within two hours. The degree of binding of the hormone to blood plasma . The drug undergoes metabolic in liver tissue. The drug is excreted with bile and kidneys, with feces.

When using the drug vaginally, the active component accumulates in the uterus; an hour after administration, the maximum concentration of the substance is already blood

Prajisan capsules 200 mg No. 10

Compound

Active substance: progesterone (micronized) - 200 mg.
Excipients: peanut oil - 295 mg, soy lecithin - 5 mg. Composition of the capsule shell: 70% sorbitol solution (uncrystallized) - 12.8 mg, glycerol - 63.84 mg, gelatin - 121.6 mg, titanium dioxide - 1.5 mg, purified water - 120.26 mg.

Pharmacokinetics

When taken orally

Suction and distribution

Micronized progesterone is well absorbed from the gastrointestinal tract (GIT). The concentration of progesterone in the blood plasma gradually increases during the first hour, the maximum concentration in the blood (Cmax) is observed 1-3 hours after administration. After taking 200 mg, the concentration of progesterone in plasma increases from 0.13 ng/ml to 4.25 ng/ml after 1 hour and is 11.75 ng/ml after 2 hours. 8.37 ng/ml after 3 hours, 2 ng/ml after 6 hours, 1.64 ng/ml - after 8 hours.

Metabolism

Metabolized in the liver with the participation of the CYP2C19 isoenzyme. The main metabolites that are detected in blood plasma are 20-alpha-hydroxy-delta-4-alpha-pregnanolone and 5-alpha-dihydroprogesterone.

Removal

Excreted by the kidneys in the form of metabolites. 95% of these are glucurone-conjugated metabolites, mainly 3-alpha. 5-beta-pregnanediol (pregnandione). These metabolites, which are determined in blood plasma and urine, are similar to substances formed during the physiological secretion of the corpus luteum.

With intravaginal administration

Suction and distribution

Absorption occurs quickly; a high concentration of progesterone in the blood plasma is observed 1 hour after administration. Cmax of progesterone in blood plasma is achieved 2-6 hours after administration. When the drug is administered at a dose of 100 mg 2 times a day, the average concentration of 9.7 ng/ml is maintained for 24 hours. When administered in doses of more than 200 mg/day. progesterone concentration corresponds to the first trimester of pregnancy. Progesterone accumulates in the uterus.

Metabolism

Metabolized to form predominantly 3-alpha. 5-beta-pregnanediol. Plasma concentrations of 5-beta-pregnanediol do not increase.

Removal

It is excreted by the kidneys in the form of metabolites, the main part being 3-alpha, 5-beta-pregnanediol (pregnandione). This is confirmed by a constant increase in its concentration (Cmax 142 ng/ml after 6 hours).

Indications for use

Disorders associated with progesterone deficiency.

Oral route of administration:

infertility due to luteal insufficiency;
premenstrual syndrome;
menstrual irregularities due to ovulation or anovulation disorders;
fibrocystic mastopathy;
premenopause;
hormone replacement therapy for 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);
prevention (prophylaxis) of premature birth in women at risk (with shortening of the cervix and/or anamnestic data of premature birth and/or premature rupture of membranes);
luteal phase support during preparation for in vitro fertilization;
luteal phase support in spontaneous or induced menstrual cycle;
premature menopause;
hormone replacement therapy (in combination with estrogen drugs);
infertility due to luteal insufficiency;
prevention of habitual and threatened abortion due to progestin deficiency.

Contraindications

For oral and vaginal use

deep vein thrombosis, thrombophlebitis;
thromboembolic disorders (pulmonary embolism, myocardial infarction, stroke), intracranial hemorrhage or a history of these conditions/diseases;
bleeding from the vagina of unknown origin;
incomplete abortion;
porphyria;
established or suspected malignant neoplasms of the mammary glands and genital organs;
age under 18 years (efficacy and safety have not been established);
lactation period (breastfeeding);
hypersensitivity to progesterone or any of the auxiliary components of the drug.

For oral use (optional)

severe liver diseases (including cholestatic jaundice, hepatitis, Dubin-Johnson syndrome, Rotor syndrome, malignant liver tumors) currently or in history;

The drug should be used with caution in diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression, and in the second trimester of pregnancy.

Directions for use and doses

Oral route of administration

The drug is taken orally in the evening before bedtime with water.

In most cases, with progesterone deficiency, the daily dose of Prajisan® is 200-300 mg, divided into 2 doses (200 mg in the evening before bed and 100 mg in the morning, if necessary).

In case of threatened abortion or in order to prevent habitual abortion due to progesterone deficiency. 200-600 mg per day daily in the first and second trimesters of pregnancy. Further use of the drug is possible as prescribed by the attending physician based on an assessment of the clinical data of the pregnant woman.

For luteal phase deficiency (premenstrual syndrome, fibrocystic mastopathy, dysmenorrhea, menopausal transition), the daily dose is 200 mg or 400 mg, taken for 10 days (usually from the 17th to the 26th day of the cycle).

For MHT in perimenopause while taking estrogen, Prajisan® is used at a dose of 200 mg per day for 12 days.

For MHT in postmenopause in a continuous mode, the drug Prajisan® is used in a dose of 100-200 mg from the first day of taking estrogen. Dose selection is carried out individually.

Intravaginal route of administration

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, 100 mg per day on the 13th and 14th days of the cycle, then 100 mg 2 times a day from the 15th to the 25th day of the cycle, from the 26th day. and if pregnancy is diagnosed, the dose increases by 100 mg per day every week, reaching a maximum of 600 mg per day, divided into 3 doses. This dose can be used for 60 days. Prevention (prophylaxis) of preterm birth in women at risk (with shortening of the cervix and/or history of preterm labor and/or premature rupture of membranes): the usual dose is 200 mg at bedtime, from the 22nd to the 34th week pregnancy.

Support of the luteal phase during the in vitro fertilization cycle: it is recommended to administer from 200 mg to 600 mg per day, starting from the day of human chorionic gonadotropin injection during the 1st and 2nd trimester of pregnancy. Support of the luteal phase in a spontaneous or induced menstrual cycle, in case of infertility associated with dysfunction of the corpus luteum, it is recommended to administer 200-300 mg per day, starting from the 1st 7th day of the cycle for 10 days, in case of delayed menstruation and diagnosis of pregnancy, treatment should to be continued.

In the case of a threatened abortion or in order to prevent a habitual abortion that occurs against the background of progesterone deficiency: 200-400 mg per day in 2 divided doses daily in the first and second trimesters of pregnancy.

Storage conditions

In a place protected from light, at a temperature not exceeding 25°C.
Keep out of the reach of children.

Best before date

2 years. Do not use after the expiration date.

special instructions

Prajisan® should not be used for contraception.
The drug should not be taken with food, since food intake increases the bioavailability of progesterone.

The drug Prajisan® should be taken with caution in patients with diseases and conditions that may be aggravated by fluid retention (arterial hypertension, cardiovascular disease, chronic renal failure, epilepsy, migraine, bronchial asthma); in patients with diabetes mellitus, mild to moderate liver dysfunction, and photosensitivity.

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 periodically observed by a doctor.

The use of Prajisan® after the first trimester of pregnancy may cause the development of cholestasis.

During long-term treatment with progesterone, regular medical examinations (including liver function tests) are necessary; Treatment should be discontinued if abnormal liver function tests or cholestatic jaundice are present.

When using progesterone, it is possible to reduce glucose tolerance and increase the need for insulin and other hypoglycemic drugs in patients with diabetes mellitus.

If amenorrhea occurs during treatment, pregnancy must be excluded. If the course of treatment begins very early in the menstrual cycle, especially before the 15th day of the cycle, a shortening of the menstrual cycle and/or acyclic bleeding is possible. In case of acyclic bleeding, the drug should not be used until the cause is determined, including a histological examination of the endometrium.

If there is a history of chloasma or a tendency to develop it, patients are advised to avoid UV irradiation.

More than 50% of spontaneous abortions in early pregnancy are caused by genetic disorders. In addition, the cause of spontaneous abortions in early pregnancy can be infectious processes and mechanical damage. The use of the drug Prajisan® in these cases can only lead to a delay in rejection and evacuation of a non-viable ovum. The prescription of Prajisan® for the purpose of preventing and/or treating the threat of miscarriage is justified only in cases of progesterone deficiency.

The drug contains soy lecithin, which can cause hypersensitivity reactions (urticaria and anaphylactic shock).

When conducting MHT with estrogen during perimenopause, it is recommended to use Prajisan® for at least 12 days of the menstrual cycle.

With a continuous MHT regimen in postmenopause, it is recommended to use the drug from the first day of taking estrogen.

When conducting MHT, the risk of developing venous thromboembolism (deep vein thrombosis or pulmonary embolism), the risk of developing ischemic stroke, and coronary heart disease increases.

Due to the risk of developing thromboembolic complications, you should stop using the drug if: visual disturbances such as vision loss, exophthalmos, double vision, vascular lesions of the retina: migraine; venous thromboembolism or thrombotic complications, regardless of their location.

If there is a history of thrombophlebitis, the patient should be closely monitored.

When using Prajisan® with estrogen-containing drugs, you should refer to the instructions for their use regarding the risks of venous thromboembolism.

The results of the Women Health Initiative Study (WHI) clinical study indicate a slight increase in the risk of breast cancer with long-term, more than 5 years, combined use of estrogen-containing drugs with synthetic gestagens. It is unknown whether there is an increased risk of breast cancer in postmenopausal women when undergoing MHT with estrogen-containing drugs in combination with progesterone.

The WHI study also found an increased risk of dementia when starting MHT after age 65 years.

Before starting MHT and regularly during it, a woman should be examined to identify contraindications to its implementation. If clinically indicated, a breast examination and gynecological examination should be performed.

The use of progesterone may affect the results of some laboratory tests, including liver and thyroid function tests; coagulation parameters; pregnanediol concentration.

Description

Gestagen.

Dosage form

Soft gelatin capsules, oval, light yellow in color; the contents of the capsules are an oily suspension of almost white color.

Use in children

Contraindication: age under 18 years (efficacy and safety have not been established).

Pharmacodynamics

The active ingredient of Prajisan® is progesterone, which is identical to the natural hormone of the corpus luteum of the ovary. By binding to receptors on the surface of cells of target organs, it penetrates into the nucleus, where. activating DNA. stimulates RNA synthesis. Promotes the transition of the uterine mucosa from the proliferation phase caused by the follicular hormone estradiol 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. Promotes the formation of normal endometrium. Stimulates the development of the end elements of the mammary gland and induces lactation, stimulating protein lipase, increases fat reserves; increases glucose utilization; increasing 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 nitrogen excretion by the kidneys.

Side effects

By oral route of administration

The following adverse events noted during oral administration of the drug are distributed according to the frequency of occurrence in accordance with the following gradation: often (>1/100, <1/10), infrequently (>1/1000, <1/100), rarely (> 1/10,000, <1/1000), very rare (<1/10,000).

From the genital organs and mammary gland: often - amenorrhea, menstrual irregularities, acyclic bleeding; infrequently - mastodynia.

From the mental side: very rarely - depression.

From the nervous system: often - headache; infrequently - drowsiness, transient dizziness.

From the gastrointestinal tract: often - bloating; uncommon - vomiting, diarrhea, constipation; rarely - nausea.

From the liver and biliary tract: infrequently - cholestatic jaundice.

From the immune system: very rarely - urticaria.

From the skin and subcutaneous tissues: infrequently - itching, acne; very rarely - chloasma.

Drowsiness and transient dizziness are possible, as a rule, 1-3 hours after taking the drug. These side effects can be reduced by reducing the dose, using the drug at bedtime, or switching to the intravaginal route of administration.

These unwanted effects are usually the first signs of an overdose. Drowsiness and/or transient dizziness are observed, in particular, in the case of concomitant hypoestrogenism. Reducing the dose or restoring higher estrogenization immediately eliminates these effects without reducing the therapeutic effect of progesterone.

If the course of treatment begins too early (in the first half of the menstrual cycle, especially before the 15th day of the cycle), a shortening of the menstrual cycle or acyclic bleeding is possible.

Recorded changes in the menstrual cycle, amenorrhea or acyclic bleeding are characteristic of all progestogens.

Application in clinical practice

During post-marketing use, the following adverse events were noted with oral use of progesterone: insomnia; premenstrual syndrome, tension in the mammary glands, vaginal discharge; joint pain; hyperthermia; increased sweating at night; fluid retention; change in body weight; acute pancreatitis; alopecia, hirsutism; changes in libido; thrombosis and thromboembolic complications (when carrying out HRT in combination with estrogen-containing drugs); increase in blood pressure.

The drug contains soy lecithin, which can cause hypersensitivity reactions (urticaria and anaphylactic shock).

For vaginal route of administration

Isolated cases of local intolerance reactions to the components of the drug (in particular, soy lecithin) have been reported in the form of hyperemia of the vaginal mucosa, burning, itching, and oily discharge.

Systemic side effects with intravaginal use of the drug in recommended doses, in particular drowsiness or dizziness (observed with oral administration of the drug), were not observed.

Use during pregnancy and breastfeeding

The drug should be used with caution in the second and third trimesters of pregnancy due to the risk of developing cholestasis.

Progesterone passes into breast milk, so the use of the drug is contraindicated during breastfeeding.

Interaction

When administered orally

Progesterone enhances the effect of diuretics, antihypertensive drugs, immunosuppressants, and anticoagulants. Reduces the lactogenic effect of oxytocin.

Concomitant use with drugs that induce microsomal liver enzymes CYP3A4, such as barbiturates, antiepileptic drugs (phenytoin), rifampicin, phenylbutazone, spironolactone, griseofulvin, is accompanied by an acceleration of progesterone metabolism in the liver.

Simultaneous use of progesterone with some antibiotics (penicillins, tetracyclines) can lead to a decrease in its effectiveness due to disruption of the enterohepatic recirculation of sex hormones due to changes in the intestinal microflora.

The severity of these interactions may vary in different patients, so predicting the clinical effects of these interactions is difficult.

Ketoconazole may increase the bioavailability of progesterone. Progesterone may increase the concentration of ketoconazole and cyclosporine.

Progesterone may reduce the effectiveness of bromocriptine.

Progesterone can cause a decrease in glucose tolerance, resulting in an increase in the need for insulin or other hypoglycemic drugs in patients with diabetes.

The bioavailability of progesterone may be reduced in patients who smoke and with excessive alcohol consumption.

For intravaginal use

Interaction with intravaginal use has not been assessed. The simultaneous use of other intravaginal drugs should be avoided to avoid interfering with the release and absorption of progesterone.

Overdose

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

In some patients, the average therapeutic dose may be excessive due to existing or emerging unstable endogenous secretion of progesterone, special sensitivity to the drug, or too low concentration of estradiol.

Treatment:

in case of drowsiness and dizziness, it is necessary to reduce the dose or prescribe the drug before bedtime for 10 days of the menstrual cycle:
in case of a shortening of the menstrual cycle or spotting, it is recommended to postpone the start of treatment to a later day of the cycle (for example, on the 19th day instead of the 17th);
in perimenopause and with MHT in postmenopause, you need to make sure. that the concentration of estradiol is optimal.

If necessary, carry out symptomatic treatment.

Impact on the ability to drive vehicles and operate machinery

When taken orally, caution must be exercised when driving vehicles, using machinery and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Indications for use

The drug is prescribed for various disorders associated with a lack of the hormone progesterone in the body.

Capsules taken:

for premenstrual syndrome ;
if there is a disturbance in the menstrual cycle due to anovulation and ovulation ;
for fibrocystic myopathy ;
during perimenopause ;
when using hormone replacement therapy for perimenopause and postmenopause .

The medicine is prescribed locally:

as hormone replacement therapy for progesterone ;
during preparation for in vitro fertilization to prolong the luteal phase ;
upon the onset of early menopause ;
for the treatment of infertility due to failure to enter the luteal phase ;
to prevent abortion due to hormonal imbalance;
as a prophylactic for uterine fibroids or endometriosis .

PRAGISAN CAPS 200MG N10

Prajisan® should not be used for contraception.

The drug should not be taken with food, since food intake increases the bioavailability of progesterone.

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 periodically observed by a doctor.

The use of Prajisan® after the first trimester of pregnancy may cause the development of cholestasis.

When using progesterone, it is possible to reduce glucose tolerance and increase the need for insulin and other hypoglycemic drugs in patients with diabetes mellitus.

If there is a history of chloasma or a tendency to develop it, patients are advised to avoid UV irradiation.

The drug contains soy lecithin, which can cause hypersensitivity reactions (urticaria and anaphylactic shock).

When carrying out HRT with estrogens during perimenopause, it is recommended to use Prajisan® for at least 12 days of the menstrual cycle.

With a continuous HRT regimen in postmenopause, it is recommended to use the drug from the first day of taking estrogen.

When carrying out hormone replacement therapy (HRT), the risk of developing venous thromboembolism (deep vein thrombosis or pulmonary embolism), the risk of developing ischemic stroke, and coronary heart disease increases.

Due to the risk of developing thromboembolic complications, the use of the drug should be discontinued if: visual disturbances such as loss of vision, exophthalmos, double vision, vascular lesions of the retina occur; migraine; venous thromboembolism or thrombotic complications, regardless of their location.

If there is a history of thrombophlebitis, the patient should be closely monitored.

When using Prajisan® with estrogen-containing drugs, you should refer to the instructions for their use regarding the risks of venous thromboembolism.

The results of the Women Health Initiative Study (WHI) clinical study indicate a slight increase in the risk of breast cancer with long-term, more than 5 years, combined use of estrogen-containing drugs with synthetic gestagens. It is not known whether there is an increased risk of breast cancer in postmenopausal women when undergoing HRT with estrogen-containing drugs in combination with progesterone.

The WHI study also found an increased risk of dementia when starting HRT after age 65 years.

Before starting HRT and regularly during it, a woman should be examined to identify contraindications to its implementation. If clinically indicated, a breast examination and gynecological examination should be performed.

The use of progesterone may affect the results of some laboratory tests, including liver and thyroid function tests; coagulation parameters; pregnanediol concentration.

Impact on the ability to drive vehicles and machinery

Contraindications

The medicine is not prescribed:

patients with disturbances in the blood circulation of the brain, thromboembolic disorders, including a history;
with thrombophlebitis ;
patients with porphyria ;
persons suffering from liver or kidney diseases;
if you suspect or have malignant neoplasms of the mammary glands or genital organs;
persons with allergies to the components of the product;
with bleeding from the genitals of unknown origin;
after an incomplete abortion .

The solution in oil is not prescribed in the 2nd and 3rd trimester of pregnancy , as there is a tendency to form blood clots .

Prajisan, 200 mg, capsules, 10 pcs.