Instruction for use: Progestogel

Active substance Progesterone

ATX code G03DA04 Progesterone

Pharmacological groups

Estrogens, gestagens; Their homologues and antagonists

Nosological classification (ICD-10)

N60.1 Diffuse cystic mastopathy

Benign cystic change in mammary glands, Cystic fibrosis mastopathy, Fibrous-cystic mastopathy, Pre-cancerous condition of mammary glands, Benign mammary gland disease, Benign breast tumor

N64.4 Mastodinia

Mastalgia, Soreness of the mammary glands, Cooper's disease

Composition

Gel for external use 100 g

active substance:

Progesterone natural micronized 1 g

Auxiliary substances: octyldodecanol; Carbomer 980; Macrogol glyceryl hydroxy stearate (castor oil polyoxyl hydrogenated); Trolamine (triethanolamine); Ethanol in terms of ethanol absolute 96% (vol.%); purified water

Description of dosage form

Gel: colorless, translucent, slightly opalescent, with the smell of alcohol without visible particles.

pharmachologic effect

The pharmacological action is gestagenic.

Pharmacodynamics

The effect of progesterone on the one hand is based on blocking the receptors of estrogens, which improves the absorption of fluid from the tissues, reduces the compression of the milk ducts; On the other - on the blocking of 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 Progestogen is based on increasing 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 breast tissue, and also decreases the local level of active estrogens by stimulating the production of enzymes (17-beta-hydroxysteroid dehydrogenase and estrone sulfotransferase) that oxidize estradiol to less active estrone, and then bind the latter to inactive estrone sulfate. Thus, progesterone limits the proliferative effect of estrogens on breast tissue. Progesterone also has a small sodium diuretic effect due to oppression of tubular reabsorption and increased cell filtration, thereby preventing fluid retention during 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 vascular network, as a result of which the permeability of capillaries decreases, and consequently the degree of edema of the mammary gland tissue decreases and the symptoms of mastalgia disappear.

Pharmacokinetics

With the transdermal route of use, 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 after 1 h 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, the isozyme CYP2C19 (cytochrome P450 isoenzyme) participates in the metabolism. 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

mammalgia;

Diffuse fibrocystic mastopathy.

Contraindications

Individual hypersensitivity to any of the components of the drug;

Nodal forms of fibrocystic mastopathy;

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

Breast and genital cancers (monotherapy);

Pregnancy (II and III trimesters).

With caution: 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

Adequate experience in the use of Progestogen during pregnancy is absent.

The use of the drug during pregnancy and lactation is possible only if the intended benefit for the mother exceeds the potential risk to the fetus and the baby.

Side effects

It is extremely rare - soreness of the mammary glands, "hot" flushes of blood, metrorrhagia; Decreased libido.

With increased sensitivity to the components of the drug - erythema in the place of gel application, edema of the lips and neck, fever, headache, nausea.

Interaction

The effect of the drug Progestogen can intensify against a background of contraception by combined hormonal preparations.

Dosing and Administration

Outwardly.

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-doser until it is fully absorbed 1-2 times daily or in the 2 nd phase (from the 16th to the 25th day) of the menstrual cycle .

The course of treatment up to 3 cycles. A second course of treatment can be prescribed only after consulting a doctor.

Overdose

Due to low systemic absorption, an overdose is unlikely.

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 the cream.

Influence on the ability to drive vehicles and work with machinery. No studies have been conducted to identify the possible effects of the drug on the ability to drive a car or control working mechanisms.

Form of issue

Gel for external use, 1%. In an aluminum tube, sealed with a screw cap, 80 g. The tube is placed in a cardboard box together with the applicator-dispenser.

Terms of leave from pharmacies

On prescription.

storage Conditions

At a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use after the expiry date printed on the package.