Active substanceProgesteroneProgesterone
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  • Dosage form: & nbspgel for external use
    Composition:

    100 g of the preparation contain:

    active substance: progesterone natural micronized 1 g;

    Excipients: octyl dodecanol, carbomer 980, macrogol glyceryl hydroxy stearate (castor oil polyoxyl hydrogenated), trolamine (triethanolamine), ethanol in terms of ethanol absolute 96% (v / v), purified water

    Description:

    Colorless translucent slightly opalescent gel with a smell of alcohol without visible particles.

    Pharmacotherapeutic group:gestagen
    ATX: & nbsp

    G.03.D.A   Derivative derivatives

    G.03.D.A.04   Progesterone

    Pharmacodynamics:

    The action of progesterone, on the one hand, is based on blockages of estrogen receptors,as a result of which the absorption of fluid from the tissues improves, the compression of the milk ducts decreases; on the other - blocking the prolactin receptors in the breast tissue, which leads to a decrease in lactopoiesis. Thus, the local use of the drug, creating a high concentration of progesterone in the area of ​​application, does not have a systemic effect and avoids undesirable side effects.

    The mechanism of action of the Projug is based on an increase in the concentration of progesterone in the tissues of the breast. The active component of the drug is progesterone. Progesterone reduces the expression of estrogen receptors in the tissues of the mammary gland, and also reduces the local level of active estrogens by stimulating the production of enzymes (17β-hydroxysteroid dehydrogenase and estrone sulfotransferase), oxidizing estradiol in a less active estrone, and then, binding the latter, turning it into an inactive estrone sulfate. In this way, progesterone limits the proliferative effect of estrogens on breast tissue. Also progesterone has a small sodium diuretic effect due to inhibition of tubular reabsorption and increased cell filtration,thereby preventing fluid retention in secretory transformations of the glandular component of the mammary glands and, as a consequence, the development of pain syndrome (mastalgia or mastodynia). Along with this, the transdermal way of introducing gestagens also allows to influence the condition of the glandular epithelium and the vasculature, as a result of which the capillary permeability decreases, and, consequently, the degree of edema of the breast tissue decreases and the symptoms of mastalgia disappear.

    Pharmacokinetics:

    In the transdermal mode of application, the Progestogen reaches the breast tissue without breaking down in the liver and without adversely affecting systemic effects on the body. The study of the serum concentration of prolactin, estradiol and progesterone in the treatment with Progestogen showed that an hour after application, when its maximum absorption in the tissue is observed, the level of hormones practically does not change. Absorption of progesterone for dermal application is about 10% of the dose. Nappy applications on the area of ​​the mammary glands allow, on the one hand, to reduce the applied dose of the drug, and on the other - to create a high concentration in the area of ​​action (10 times higher than in the systemic bloodstream).

    The drug is re-metabolized in the liver with the formation of conjugates with glucuronic and sulfuric acids. Also, isozyme participates in the metabolism CYP2C19.

    It is excreted by the kidneys - 50-60%, with bile - more than 10%. The amount of metabolites excreted by the kidneys varies depending on the phase of the yellow body.

    Indications:

    - Mastodonia;

    diffuse fibrocystic mastopathy.
    Contraindications:

    - Nodular forms of fibrocystic mastopathy;

    - tumors (tumorous formations) of the mammary glands of an obscure etiology;

    - individual hypersensitivity to any of the components of the drug;

    - breast and genital cancers (as monotherapy);

    - pregnancy (II and III trimesters).

    Carefully:

    - Liver failure;

    - kidney failure;

    - bronchial asthma;

    - epilepsy;

    - Migraine;

    - Depression;

    - hyperlipoproteinemia;

    - ectopic pregnancy;

    - abortion in the course;

    - propensity to thrombosis, acute forms of phlebitis or thromboembolic diseases;

    bleeding from the vagina of an unclear etiology;

    - porphyria;

    - arterial hypertension;

    - diabetes.

    Pregnancy and lactation:

    There is insufficient experience in the use of the Progestogen during pregnancy.The use of the drug during pregnancy and during lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby.

    Dosing and Administration:

    1 application (2.5 g of gel), containing 0.025 g of progesterone, is applied to the skin of the mammary glands by the applicator-dispenser until complete absorption of 1-2 times daily, or in the 2-phase (from 16 to 25 days) of the menstrual cycle.

    The course of treatment is up to 3 cycles.

    Repeated treatment may be prescribed only after consultation with a doctor.

    Side effects:

    Rarely: soreness of the mammary glands, hot hot flushes, metrorrhagia, decreased libido. With increased sensitivity to the components of the drug - erythema in the place of application of the gel, swelling of the lips and neck, fever, headache, nausea.

    Overdose:

    Due to low systemic absorption, an overdose is unlikely.

    Interaction:

    The action of the Progestogen can be intensified against a background of contraception by combined hormonal preparations.

    Special instructions:

    The progestogen can be prescribed for mastodynia associated with taking oral contraceptives, pubertal period, premenopause, premenstrual syndrome.

    The drug should be applied to the skin of the breast with the applicator-doser, without rubbing or massaging the mammary glands.

    Avoid direct sunlight after applying cream.

    Effect on the ability to drive transp. cf. and fur:

    No studies have been conducted to identify the possible effects of the drug on the ability to drive a car or on the ability to control working mechanisms.

    Form release / dosage:Gel for external use, 1%.
    Packaging:

    For 80 g of the drug in an aluminum tube, ukuporennuyu screw cap.

    The tube is placed in a cardboard box together with the applicator-dispenser and instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013765 / 01
    Date of registration:09.10.2008
    The owner of the registration certificate:Bezen Helskea SABezen Helskea SA Belgium
    Manufacturer: & nbsp
    Representation: & nbspBEZEN HELSKEA ENG LLCBEZEN HELSKEA ENG LLCRussia
    Information update date: & nbsp01.09.2015
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