Progestogel, gel 1% 80 g

Pharmacodynamic.

The action of progesterone, on the one hand, is based on blocking estrogen receptors, resulting in improved absorption of fluid from tissues, reducing compression of the milk ducts; on the other – blocking prolactin receptors in breast tissue, which leads to decreased lactopoiesis. Thus, local application of the drug, by creating a high concentration of progesterone in the zone of application, has no systemic action and allows to avoid undesirable side effects.

The mechanism of action of Progestozhel is based on increasing the concentration of progesterone in mammary gland tissues. Progesterone is the active ingredient of the drug.

Progesterone reduces the expression of estrogen receptors in the breast tissue and also reduces the local level of active estrogen by stimulating the production of enzymes (17beta-hydroxysteroid dehydrogenase and estronsulfotransferase) which oxidize estradiol to less active estrone and then, by binding the ambassador, turn it into inactive estronsulfate. In this way, progesterone limits the proliferative effect of estrogen on breast tissue.

Progesterone also has a small sodium diuretic effect by inhibiting tubular reabsorption and increasing cellular filtration, thereby preventing fluid retention during secretory transformations of the glandular component of the mammary glands and, consequently, the development of pain syndrome (mastalgia or mastodynia). At the same time, the transdermal method of gestagen administration also allows to influence the condition of the glandular epithelium and the vascular network which results in a decrease of capillary permeability and, consequently, reduction of the degree of mammary gland tissue edema and disappearance of mastalgia symptoms.

Pharmacokinetics.

In transdermal administration Progestozhel reaches the breast tissue without being destroyed in the liver and with no adverse systemic effects on the body. The study of serum concentration of prolactin, estradiol and progesterone during Prozhestozhel treatment showed that one hour after application of the preparation, when its maximum absorption into the tissue is observed, the level of hormones remains practically unchanged.

The absorption of progesterone by topical application is about 10% of the dose. Topical application to the mammary glands allows reducing the applied dose of the drug, on the one hand, and creating a high concentration in the area of action (10 times higher than in the systemic blood flow). The drug is secondary metabolized in the liver with the formation of conjugates with glucuronic and sulfuric acids. CYP2C19 isoenzyme is also involved in metabolism. It is excreted by kidneys – 50-60%, with bile – more than 10%. The amount of metabolites excreted by the kidneys varies depending on the phase of the corpus luteum.

Indications

Active ingredient

Composition

Composition per 100 g:

Active ingredient:

Progesterone natural micronized – 1 g.

Associates:

Octyldodecanol, carbomer 980,

Macrogoal glyceryl hydroxystearate (polyoxylhydrogenated castor oil),

trolamine (triethanolamine),

ethanol equivalent to 96% absolute ethanol (o/o),

purified water.

How to take, the dosage

Pregestozhel 1% gel 1 application (2.5 g of gel; contains 0.025 g of progesterone) should be applied by dosage applicator to the mammary gland skin until full absorption 1-2 times daily or during the 2nd phase (from the 16th-25th day) of the menstrual cycle.

The course of treatment is up to 3 cycles.

The repeated course of treatment can be prescribed only after consultation with the doctor.

Interaction

The effects of Progestojele may be enhanced when combined hormonal drugs are contraceptive.

Special Instructions

Progestozhel may be prescribed for mastodynia associated with taking oral contraceptives, puberty, premenopause, premenstrual syndrome.

The drug should be applied to the mammary gland skin using a dosage applicator without rubbing or massaging the mammary glands.

Please avoid direct sunlight after applying the cream.

Contraindications

Side effects

Overdose

Due to low systemic absorption, overdose is unlikely.

Pregnancy use

There is insufficient experience with the use of Progestogel during pregnancy.

The use of the drug during pregnancy and lactation is possible only when the expected benefit to the mother outweighs the potential risk to the fetus and child.

Similarities