Clinical and pharmacological group: & nbsp

"Estrogens, gestagens, their homologues and antagonists"

Included in the formulation
  • Cyclo-Proginova®
    pills inwards 
    Bayer Pharma AG     Germany
  • АТХ:

    G.03.A.A.06   Norgestrel and ethinylestradiol

    Pharmacodynamics:

    Estradiol, which is a part of the drug, in the human body is transformed into a natural 17β-Extradiol and acts similarly.

    The estrogen component - estradiol is a substance of natural origin and, upon admission into the body, rapidly turns into estradiol, identical to the hormone produced by the ovaries and exerts its own effects: it activates the proliferation of the epithelium of the organs of the reproductive system, including the regeneration and growth of the endometrium in the first phase of the menstrual cycle, the preparation of the endometrium to the action of progesterone, the increase in libido in the middle of the cycle, affects the exchange of fats, proteins, carbohydrates and electrolytes, stimulates the production of liver globulins, binding sex hormones, renin, triglycerides and coagulation factors. Through participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system estradiol It can also cause moderate central effects. It plays an important role in the development of bone tissue and the formation of bone structure.

    Another component is the active synthetic gestagen - norgestrel, superior in strength to the action of the natural hormone of the yellow body progesterone. Promotes the transition of the mucous membrane of the uterus from the stage of proliferation into the secretory phase. Reduces excitability and contractility of the musculature of the uterus and fallopian tubes, stimulates the development of the end elements of the mammary glands. It blocks the secretion of hypothalamic release factors luteinizing hormone and follicle-stimulating hormone, inhibits the formation of gonadotropic hormones, inhibits ovulation, has minor androgenic properties.

    Estradiol replenishes the estrogen deficiency in the female body after the onset of menopause and provides effective treatment of psychoemotional and vegetative climacteric symptoms (such as "hot flashes", increased sweating, sleep disturbances, increased nervous excitability, irritability, palpitations, cardialgia, dizziness, headache, decreased libido, muscle and joint pain); involution of the skin and mucous membranes, especially the mucosal genitourinary system (urinary incontinence, dryness and irritation of the vaginal mucosa,soreness with sexual intercourse).

    Estradiol prevents bone loss caused by estrogen deficiency. This is mainly due to the suppression of osteoclast function and the shift of the bone remodeling process towards bone formation. It has been proven that prolonged use of hormone replacement therapy reduces the risk of fractures of peripheral bones in women after menopause.

    Hormone replacement therapy also has a beneficial effect on the content of collagen in the skin, as well as on its density, and can also slow the process of wrinkle formation.

    Hormone replacement therapy leads to a reduction in total cholesterol, low-density lipoprotein cholesterol and high-density lipoprotein cholesterol, and an increase in triglyceride levels. The gestagen contained in the combined preparation, to a certain extent, prevents the effect of estradiol on the metabolism of lipids.

    Observational studies suggest that, among postmenopausal women, the use of hormone replacement therapy reduces the incidence of colon cancer.

    Pharmacokinetics:

    Estradiol is rapidly and completely absorbed in the gastrointestinal tract, metabolized in the liver with the formation of estrone and 17β-estradiol. After oral administration, the bioavailability of estradiol is about 3%. Eating does not affect the bioavailability of estradiol. The maximum concentration of estradiol in the serum is usually achieved 4-9 hours after taking the pills. Excreted in the form of metabolites mainly by the kidneys.

    Norgestrel is completely and rapidly absorbed in the gastrointestinal tract. The maximum concentration of levonorgestrel in the serum is usually achieved after 1-1.5 hours after taking the pills. Metabolised in the liver. Half-life is 1 day, excreted in urine and bile.

    Indications:

    - prevention of osteoporosis during the postmenopause;

    - primary / secondary amenorrhea;

    - irregular menstrual cycle;

    - estrogen insufficiency (after ovariectomy for non-malignant diseases or after radiation castration);

    - hormone replacement therapy for menopausal disorders, involutional changes in the skin and genitourinary tract, depressive conditions in the climacteric period,as well as symptoms of estrogen deficiency due to natural menopause or hypogonadism, sterilization or primary ovarian dysfunction in women with an unrefined uterus.

    XIII.M80-M85.M81.0   Postmenopausal osteoporosis

    XIII.M80-M85.M81.1   Osteoporosis after removal of ovaries

    XIV.N80-N98.N91   Absence of menstruation, meager and rare menstruation

    XIV.N80-N98.N95.1   Menopause and menopause in women

    XIV.N80-N98.N95.3   Conditions associated with artificially induced menopause

    Contraindications:

    - pregnancy and lactation;

    - heavyliver ablation;

    - breast cancer (confirmed or suspected);

    - liver tumors, including in the anamnesis;

    - bleeding of the vagina of an unclear etiology;

    - severe hypertriglyceridemia;

    - hypersensitivity;

    - acute arterial thrombosis / thromboembolism;

    - deep vein thrombosis in the acute stage, thromboembolism now or in the anamnesis;

    - hormone-dependent tumor / hormone-dependent precancerous disease (identified or suspected).

    Carefully:

    - congenital hyperbilirubinemia;

    - uterine myoma;

    - endometriosis;

    - arterial hypertension;

    - diabetes;

    - Cholestatic jaundice / cholestatic itching during pregnancy.

    Pregnancy and lactation:

    Category FDA - X. Do not use when pregnant and breast-feeding.

    Dosing and Administration:

    If the patient has menstruation, the drug is taken on the 5th day of the cycle, with amenorrhea, very rare menstruation or postmenopause, the drug can be taken any day. The drug is taken daily 21 days according to the instructions, then make a 7-day break, after a break, the drug is resumed according to the same scheme. The duration of treatment is determined by the attending physician.

    Dragee swallowed whole, squeezed a small amount of liquid. The time of day when a woman takes the drug does not matter, however, if she starts taking the pills at any particular time, she should stick to this time and on. If the woman forgot to take the pills, she can take it within the next 12-24 hours. If treatment is interrupted for a longer time, vaginal bleeding may occur.

    Side effects:

    From the gastrointestinal tract: bloating, dyspepsia, recurrence of cholestatic jaundice, vomiting, abdominal pain, nausea.

    From the nervous system: Migraine, headache, fatigue, agitation, depression.

    From the skin: itching, rash, chloasma, erythema nodosum.

    On the part of the reproductive system: breakthrough bleeding, changes in the intensity and frequency of uterine bleeding, soreness / tension / enlargement of the mammary glands, dysmenorrhea, conditions similar to premenstrual syndrome, changes in vaginal discharge, intermenstrual bleeding.

    Overdose:

    Vomiting and nausea, vaginal bleeding. There is no specific antidote, treatment is symptomatic.

    Interaction:

    Do not allow simultaneous reception with hormonal contraceptives.

    Medicines that induce liver enzymes (eg, hydantoins, barbiturates, primidon, carbamazepine and rifampicin, topiramate, felbamate, griseofulvin), can reduce the clinical effectiveness of the drug and increase the clearance of sex hormones.

    Some antibiotics, such as penicillins and tetracyclines, can reduce the concentration of estradiol.

    With hormone replacement therapy, glucose tolerance can change,in some cases, the need for oral antidiabetics or insulin may change.

    Alcohol can increase the concentration of circulating estradiol.

    Preparations undergoing conjugation (for example, paracetamol) can significantly increase the bioavailability of estradiol due to competitive inhibition of the conjugation system in the absorption process.

    Special instructions:

    If contraception is necessary, non-hormonal contraceptives should be used while taking the drug.

    Treatment should be preceded by a thorough gynecological examination, which should be repeated at least once a year with prolonged therapy.

    In the treatment process, systematic monitoring of liver function and arterial pressure, and in patients with diabetes mellitus - for the concentration of glucose in the blood. Therapy with estradiol must necessarily be combined with the use of progestogens. Prolonged treatment with estradiol at high doses increases the risk of developing breast cancer and endometrial cancer (depending on the duration of treatment and the dose of estrogen used). Hyperplasia (atypical or glandular) often precedes endometrial cancer.The combination of estrogens with gestagen has a protective effect on the endometrium.

    Treatment should be discontinued in 4-6 weeks before the planned surgical intervention.

    It is not a contraceptive and does not protect against pregnancy.

    When there are altered or irregular menstrual flow on the background of treatment (in women with a healthy uterus), diagnostic scraping is necessary to exclude malignant uterine formation.

    Impact on the ability to drive vehicles and manage mechanisms

    Not influences.

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