Progestogel gel for external use 1%, 80g

Composition

Composition per 100 g:

Active ingredient:  

natural micronized progesterone – 1 g.

Auxiliary substances:  

octyldodecanol, carbomer 980,

macrogol glycerylhydroxystearate (polyoxylhydrogenated castor oil),

trollamine (triethanolamine),

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

purified water.

Pharmacological action

Pharmacodynamic.

The effect of progesterone, on the one hand, is based on blocking estrogen prescriptions, as a result of which fluid absorption from tissues improves, compression of the milk ducts decreases; on the other, it blocks 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 undesirable side effects.

The mechanism of action of Progestogel is based on an increase in the concentration of progesterone in breast tissues. The active ingredient of the drug is progesterone.

Progesterone reduces the expression of estrogen receptors in breast tissues, and also reduces 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 by binding compounds that convert it to inactive estrone sulfate. Thus, progesterone limits the proliferative effect of estrogens on breast tissue.

Progesterone also has a small natridiuretic 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, as a result, the development of pain syndrome (mastalgia or mastodynia). Along with this, the transdermal method of introducing progestogen also allows you to affect the condition of the glandular epithelium and vascular network, 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.

With the transdermal method of application, Progestogel reaches the breast tissue without being destroyed in the liver and without having adverse systemic effects on the body. A study of the serum concentrations of prolactin, estradiol and progesterone during the treatment with Progestogel showed that an hour after applying the drug, when its maximum absorption in the tissues is observed, the level of hormones practically does not change.

The absorption of progesterone by cutaneous use is about 10% of the dose. Cutaneous applications to the mammary gland area 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 circulation). The drug is secondarily metabolized in the liver to form conjugates with glucuronic and sulfuric acids. The isoenzyme CYP2C19 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.

Indications

– Mastodynia. – Diffuse fibrocystic mastopathy.

Use during pregnancy and lactation

There is not enough experience of using Progestogel during pregnancy.

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

Contraindications

-Individual hypersensitivity to any of the components of the drug. – Nodular forms of fibrocystic mastopathy. – Tumours (tumour-like formations) of the mammary glands of unclear etiology. – Pregnancy (II and III trimesters). – Breast and genital cancer (as monotherapy). Caution: vaginal bleeding of unknown etiology; porphyria; epilepsy; migraine; depression; hyperlipoproteinemia; liver failure; renal failure; bronchial asthma;ectopic pregnancy; abortion in progress; tendency to thrombosis, acute forms of phlebitis or thromboembolic diseases; arterial hypertension; diabetes mellitus.

Side effects

Only extremely rare: swelling of the lips and neck, fever, headache, nausea, tenderness of the mammary glands, ” hot ” flushes of blood, metrorrhagia; decreased libido. With hypersensitivity to the components of the drug-erythema at the site of application of the gel.

Interaction

The effect of Progestogel can be enhanced against the background of conraception with combined hormonal drugs.

How to take, course of use and dosage

Apply 1 application of Progestogel 1% gel (2.5 g of gel; contains 0.025 g of progesterone) to the skin of the mammary glands with a dispenser applicator until complete absorption 1-2 times daily, or in the 2nd phase (from day 16 to day 25) of the menstrual cycle.

The course of treatment is up to 3 cycles.

A second course of treatment can be prescribed only after consulting a doctor.

Overdose

Due to low systemic arbsorption, overdose is unlikely.

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 breast with a dispenser applicator, without rubbing or massaging the mammary glands.

Avoid direct sunlight after applying the cream.

Form of production

Gel for external use.

Storage conditions

At a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Progesterone

Conditions of release from pharmacies

By prescription

Dosage form

gel for external use

Description

For women, Nursing mothers as prescribed by a doctor, Pregnant women in the first trimester as prescribed by a doctor, For adults as prescribed by a doctor

Indications

Mastopathy