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

– Mastodynia.

– Diffuse fibrocystic mastopathy.

Pharmacological effect

Pharmacodynamics.

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

The mechanism of action of Progestogel is based on increasing the concentration of progesterone in breast tissue. The active component of the drug is progesterone.

Progesterone reduces the expression of estrogen receptors in breast tissue, and also reduces the local level of active estrogens by stimulating the production of enzymes (17beta-hydroxysteroid dehydrogenase and estrone sulfotransferase) that oxidize estradiol into the less active estrone, and then bind the latter, converting it into inactive estrone sulfate. Thus, progesterone limits the proliferative effect of estrogens on breast tissue.

Progesterone also has a slight natriuretic effect due to inhibition of tubular reabsorption and increased cellular 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 method of administering gestagen also makes it possible to influence the condition of the glandular epithelium and vascular network, as a result of which capillary permeability decreases, and, consequently, the degree of swelling of the mammary gland tissue decreases and the symptoms of mastalgia disappear.

Pharmacokinetics.

When administered transdermally, Progestogel reaches the mammary gland tissue without being destroyed in the liver and without causing adverse systemic effects on the body. A study of the serum concentrations of prolactin, estradiol and progesterone during treatment with Progestogel showed that an hour after application of the drug, when its maximum absorption into the tissue is observed, the level of hormones remains virtually unchanged.

Absorption of progesterone when applied cutaneously is about 10% of the dose. Cutaneous applications to the area of ​​the mammary glands allow, on the one hand, to reduce the dose of the drug used, and on the other, to create a high concentration in the area of ​​action (10 times higher than in the systemic circulation). The drug is secondarily metabolized in the liver to form conjugates with glucuronic and sulfuric acids. The CYP2C19 isoenzyme is also involved in metabolism. 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 corpus luteum.

Special instructions

Progestogel can be prescribed for mastodynia associated with taking oral contraceptives, puberty, premenopause, and premenstrual syndrome.

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

Avoid exposure to direct sunlight after applying the cream.

Active ingredient

Progesterone

Composition

Composition per 100 g:

Active ingredient:

natural micronized progesterone – 1 g.

Excipients:

octyldodecanol, carbomer 980,

macrogol glyceryl hydroxystearate (polyoxyl hydrogenated castor oil),

trolamine (triethanolamine),

ethanol in terms of absolute ethanol 96% (v/v),

purified water.

Pregnancy

There is not enough experience with the use of Progestogel during pregnancy.

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

Contraindications

– Individual hypersensitivity to any of the components of the drug.

– Nodular forms of fibrocystic mastopathy.

– Tumors (tumor-like formations) of the mammary glands of unknown etiology.

– Pregnancy (II and III trimesters).

– Breast and genital cancer (as monotherapy).

Caution: bleeding from the vagina of unknown etiology; porphyria; epilepsy; migraine; depression; hyperlipoproteinemia; liver failure; renal failure; bronchial asthma; ectopic pregnancy; abortion is in progress; tendency to thrombosis, acute forms of phlebitis or thromboembolic diseases; arterial hypertension; diabetes mellitus

Side Effects

Only extremely rarely: swelling of the lips and neck, fever, headache, nausea, tenderness of the mammary glands, “hot” flushes, metrorrhagia; decreased libido.

In case of hypersensitivity to the components of the drug – erythema at the site of application of the gel.

Interaction

The effect of Progestogel may be enhanced by contraception with combined hormonal drugs.

Overdose

Due to low systemic absorption, overdose is unlikely.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf life

3 years.

Manufacturer

Delpharm Drogenbosch SA, Belgium