Proginova tablets 2 mg pack cont cell/pack card x21

Compound

Directions for use and doses

Orally, after meals, without chewing and with a small amount of liquid, 1 tablet daily for 21 days, then a break of 7 days.

If you are menstruating, you should take Proginova on the 5th day of menstrual bleeding.

In any other case, immediate treatment recommended by a doctor is possible.

If the uterus is preserved, it is possible to additionally prescribe another hormone - progesterone. And a doctor’s recommendation is necessary: ​​should the pills be taken continuously (without breaks) or intermittently.

The time of day you take Proginov does not matter. However, if the first tablet is taken at a certain time of the day, you should adhere to this time when taking all subsequent tablets.

Proginova tablets 2 mg pack cont cell/pack card x21

Trade name: Progynova International name: Estradiol Pharmacological group: estrogen Pharmacological group according to ATC: G03CA03. Estradiol Pharmacological action: normalizing menstrual function, preventing genital involution, anti-climacteric, reducing bone resorption of calcium during menopause, estrogenic Pharmacodynamics: The estrogenic drug - 17-beta-estradiol is identical to endogenous estradiol (formed in the body of women, from the first menstruation until menopause), produced by the ovaries. In the cells of the organs to which the action of hormones is directed, estrogens form a complex with specific receptors (found in various organs - in the uterus, vagina, urethra, mammary gland, liver, hypothalamus, pituitary gland), the receptor-ligand complex interacts with estrogen-effector elements genome and specific intracellular proteins that induce the synthesis of mRNA, proteins and the release of cytokines and growth factors. Has a feminizing effect on the body. Stimulates the development of the uterus, fallopian tubes, vagina, stroma and ducts of the mammary glands, pigmentation in the area of ​​the nipples and genitals, the formation of secondary sexual characteristics of the female type, the growth and closure of the epiphyses of long tubular bones. Promotes timely endometrial rejection and regular bleeding, in high concentrations causes endometrial hyperplasia, suppresses lactation, inhibits bone resorption, stimulates the synthesis of a number of transport proteins (thyroxine-binding globulin, transcortin, transferrin, sex hormone binding protein), fibrinogen. It has a procoagulant effect, increases the synthesis of vitamin K-dependent blood coagulation factors (II, VII, IX, X) in the liver, reduces the concentration of antithrombin III. Increases blood concentrations of T4, Fe, Cu2+, etc. Has an anti-atherosclerotic effect, increases the concentration of HDL, reduces LDL and cholesterol (TG concentration increases). Modulates the sensitivity of receptors to progesterone and sympathetic regulation of smooth muscle tone, stimulates the transition of intravascular fluid into tissues and causes compensatory retention of Na+ and water. In large doses, it prevents the degradation of endogenous catecholamines by competing for active catechol-O-methyltransferase receptors. After menopause, only a small amount of estradiol is produced in the body (from estrone found in the liver and adipose tissue). A decrease in the concentration of estradiol produced in the ovaries is accompanied in many women by vasomotor and thermoregulatory instability (“flushes” of blood to the facial skin), sleep disorders, as well as progressive atrophy of the genitourinary system. Osteoporosis (mainly of the spine) develops due to estrogen deficiency. It is known that oral administration of estrogens causes an increase in protein synthesis (including renin), which leads to an increase in blood pressure. Estradiol TTC is a patch that is attached to an area of ​​skin. The control membrane ensures a gradual and continuous release of estradiol from the active substance reservoir through the adhesive layer onto the skin. Due to the lack of a “first pass” effect through the liver, TTC provides high efficacy when using lower doses of the drug. TTS delivers estradiol unchanged into the bloodstream and maintains its concentration in plasma during therapy at a constant level, adequate to the level in the early or middle phase of the follicle.

Pharmacokinetics: After oral administration, it is rapidly and completely absorbed (bioavailability about 100%), a larger amount of estradiol, before entering the bloodstream, is metabolized in the lumen (microflora) and intestinal wall, as well as in the liver (leading to non-physiologically high concentrations of estrone in plasma , and with long-term therapy - to the accumulation of estrone and estrone sulfate). In the blood it is almost completely bound to the carrier protein. It undergoes a “first pass” effect through the liver, where it is metabolized to less active products - estrone and estriol. It is excreted by bile into the lumen of the small intestine and reabsorbed. Finally loses activity as a result of oxidation in the liver. It is excreted mainly by the kidneys in the form of sulfates and glucuronides; small amounts of estradiol, estrone and estriol are also found in the urine.

After application of TTS 25, 50, 75 and 100 mcg, the physiological concentration of estradiol in the blood serum is achieved within 2-4 hours. Its level is directly dependent on the dose. 8 hours after the application of TTS 25, 50 and 100 mcg, the average Cmax of estradiol in plasma is 28, 67 and 130 pg/ml, respectively; subsequently, constant concentration values ​​are established, averaging 23, 40 and 75 pg/ml, respectively. The estradiol/estrone ratio averages 0.9, 1 and 1.35, respectively, which corresponds to the early follicular phase of the reproductive period of life. 24 hours after removal of TTS, the concentration of estradiol in plasma decreases to its original value. The concentration of estradiol metabolites in urine on day 2 after removal of TTC reaches the same values ​​that were measured before application. With repeated application of TTC 50 mcg 2 times a week for 3 weeks (6 applications), the average concentration of estradiol in plasma increases by 30 pg/ml, and estrone by 12 pg/ml. The average estradiol/estrone ratio increases to 0.9. T1/2 of estradiol is about 1 hour. The rate of elimination from plasma is from 500 to 900 l/day/sq.cm. The concentration of estradiol metabolites in urine remains constantly elevated during application and decreases 2-3 days after removal of TTS to the initial value. Gradual release maintains therapeutic plasma concentrations for 3-7 days.

When applying the gel, ethanol quickly evaporates and estradiol penetrates the skin, while most of it enters the systemic circulation immediately, and a certain amount is retained in the subcutaneous fat and is released into the systemic circulation gradually. Cmax is reached within 3-4 hours. Bioavailability is 82%. It is not subject to the “first pass” effect, which to some extent reduces the severity of fluctuations in plasma estrogen concentrations. Metabolism and elimination when using the gel and TTS corresponds to the metabolism and elimination of natural estrogens. Does not accumulate.

Indications for use: Estrogen deficiency during menopause and during surgical menopause for non-malignant neoplasms, after radiation castration, primary and secondary amenorrhea, hypomenorrhea, oligomenorrhea, dysmenorrhea, secondary estrogen deficiency. Hirsutism in polycystic ovary syndrome, vaginitis (in girls and in old age), hypogenitalism, infertility, weakness of labor, post-term pregnancy, to suppress lactation, virile hypertrichosis in women. Postmenopausal osteoporosis. Breast cancer, prostate cancer, urogenital disorders (dyspareunia, atrophic vulvovaginitis, urethritis, trigonitis), alopecia with hyperandrogenemia. As a drug that stimulates hematopoiesis in men with acute radiation injury.

Contraindications: Hypersensitivity, pregnancy, estrogen-dependent malignancies or suspicion of them, unusual or undiagnosed genital or uterine bleeding, thrombophlebitis or thromboembolic diseases in the active phase (except for the treatment of breast and prostate cancer).

Dosage regimen: Orally, without chewing, with a small amount of liquid, 2 mg/day, for 21 days, followed by a break for 7 days, after which treatment is continued. The duration of treatment is up to 6 months, after which an examination is carried out to decide whether it is advisable to continue estrogen replacement therapy. In women with a uterus removed or in menopausal women, treatment can begin on any day. If the menstrual cycle is preserved, the first tablet should be taken on the 5th day of the cycle (1st day of the cycle = 1st day of menstruation).

TTS is attached to a clean, dry and intact area of ​​body skin (lumbar region, abdomen) 2 times a week. Treatment begins with TTC 50 mcg, followed by individual dose selection (the appearance of a feeling of tension in the mammary gland or intermediate bleeding is a sign of an increased dosage that needs to be reduced). If after 2-3 weeks the signs and symptoms of estrogen deficiency do not stop, the dose should be increased. TTC is applied cyclically: after 3 weeks of treatment (6 applications) - an interval of 7 days, during which metrorrhagia is possible. Continuous, non-cyclic therapy is indicated for women following a hysterectomy or in cases where symptoms of estrogen deficiency become severe again during the 7-day interval. Subsequent therapy with gestagens should be carried out according to the following scheme: with continuous use of TTC, it is recommended to additionally prescribe a gestagen (10 mg medroxyprogesterone acetate, 5 mg norethisterone, 5 mg norethisterone acetate or 20 mg dydrogesterone in the first 10-12 days of each month). When using TTC cyclically, it is recommended that in the last 10-12 days of estradiol therapy, additional gestagen be taken so that the fourth week of each cycle remains free from therapy with any hormone. In both cases, after the end of 10-12 days of gestagen therapy, bleeding occurs. The gel is used once a day, in the morning or evening, 1.5 mg (2.5 g of gel or 1-2 doses) - applied in a thin layer to clean skin of the abdomen, lumbar region, shoulders and forearms. The application area should be equal in size to 1-2 palms. The gel should be absorbed in less than 2-3 minutes. If it remains on the surface of the skin for more than 5 minutes, then the drug was applied to too small a surface of the skin. The gel is prescribed continuously or in cycles. Doses and duration of therapy are determined individually.

Side effects: In women: pain, sensitivity and enlargement of the mammary glands, amenorrhea, breakthrough bleeding, menorrhagia, intermenstrual “spotting” vaginal discharge, swelling of the mammary glands, increased libido. In men, pain and sensitivity of the mammary glands, gynecomastia, decreased libido. Peripheral edema, gallbladder obstruction, hepatitis, pancreatitis. Intestinal or biliary colic, flatulence, anorexia, nausea, diarrhea, dizziness, headache (including migraine), intolerance to contact lenses, vomiting (mainly of central origin, mainly when using large doses). In the treatment of breast and prostate cancer (additionally): thromboembolism, thrombosis. When using TTC: skin irritation and hyperemia.

Overdose: Symptoms: nausea, vomiting, in some cases - metrorrhagia. Treatment: drug withdrawal, symptomatic therapy aimed at maintaining vital functions.

Interaction: Increases the effectiveness of lipid-lowering drugs. Weakens the effects of male sex hormones, hypoglycemic, diuretic, antihypertensive drugs and anticoagulants. Reduces glucose tolerance (adjustment of the dosage regimen of hypoglycemic drugs may be required). Barbiturates, anxiolytic drugs (tranquilizers), narcotic analgesics, drugs for general anesthesia, some antiepileptic drugs (carbamazepine, phenytoin), inducers of microsomal liver enzymes accelerate the metabolism of estradiol. Concentration in plasma decreases with the simultaneous use of phenylbutazone and some antibiotics (ampicillin, rifampicin), which is associated with changes in the microflora in the intestine. Folic acid and thyroid medications enhance the effect of estradiol.

Special instructions: Treatment should be preceded by a thorough gynecological examination, which should be repeated at least once a year during long-term therapy. During treatment, systematic monitoring of liver function and blood pressure is necessary, and in patients with diabetes mellitus, the concentration of glucose in the blood. Estradiol therapy must be combined with the use of gestagens. Long-term treatment with estradiol increases the risk of developing breast and endometrial cancer (depending on the duration of treatment and the dose of estrogen). Hyperplasia (atypical or glandular) often precedes endometrial cancer. The combination of estrogens with gestagen has a protective effect on the endometrium. Treatment should be stopped 4-6 weeks before planned surgical treatment. It is not a contraceptive and does not protect against pregnancy. If irregular menstrual flow appears during treatment (in women with an intact uterus), a diagnostic curettage is necessary to exclude a malignant neoplasm of the uterus. The use of estradiol should be stopped immediately in the event of deep vein thrombosis, thromboembolism of other localization, the appearance of jaundice, intensification or appearance of previously non-existing migraine-like pain, sudden visual impairment, or a significant increase in blood pressure. TTS cannot be attached to the skin of the mammary glands and 2 times in a row on the same area of ​​skin. The attached TTS should not be exposed to sunlight. Avoid contact of the gel with the mammary glands and mucous membranes of the vulva and vagina. Carefully. Thrombophlebitis, thrombosis or thromboembolism (with a history of taking estrogen), familial hyperlipoproteinemia, pancreatitis, endometriosis, history of gallbladder disease (especially cholelithiasis), severe liver failure, jaundice (including a history of previous pregnancy), hepatic porphyria, leiomyoma, hypercalcemia associated with bone metastases of breast cancer. For the treatment of breast and prostate cancer only: diseases of the coronary or cerebral vessels, active thrombophlebitis or thromboembolic diseases (high doses of estrogens used for treatment increase the risk of myocardial infarction, pulmonary embolism, thrombophlebitis).

Manufacturer: Delpharm Lille SAS, France Registration certificate holder: Schering SaS subsidiary of Schering AG, France Release form: 2 mg tablets, cellular contour packs Composition: estradiol valerate 2 mg Belongs to the Vital and Essential Drugs Dispensing conditions: by prescription Shelf life: 5 years Information about registration: P N013529/01 dated July 15, 2009 Status of the registration certificate: valid Pharmaceutical article number: ND 42-11637-04