Prozhestozhel

General characteristics. Structure:

Active agent: 1 dose contains progesterone natural micronized 25 mg; 800 mg in 1 tuba.

Excipients: octyllauryl alcohol, carbomer 980, a macrogoal глицерилгидроксистеарат (polioksilgidrogenizirovanny castor oil), троламин (trietanolamine), ethanol, water cleared.

Pharmacological properties:

Gestagen for external use. Active component of drug is progesterone.
Effect of progesterone is based on blocking of receptors of estrogen as a result of which absorption of liquid from fabrics improves and the prelum of lacteal channels, and also on blocking of receptors of prolactin in tissue of a mammary gland decreases that leads to decrease in a laktopoez.
Local use of drug, creating high concentration of progesterone in a use zone, has no systemic action and allows to avoid undesirable side effects.
The mechanism of action of Prozhestozhel is based on increase in concentration of progesterone in tissues of a mammary gland. Progesterone reduces an expression of receptors of estrogen in tissues of a mammary gland, and also reduces the local level of active estrogen by means of stimulation of products of the enzymes (17 - beta гидроксистероиддегидрогеназы and estronsulfotransferaza) oxidizing oestradiol in less active estrone (connecting the last, enzymes turn it into inactive sulfate of estrone).
Thus, progesterone limits proliferative effect of estrogen on tissue of a mammary gland.
Also progesterone has small natriydiuretichesky effect due to oppression of a canalicular reabsorption and increase in cellular filtering, preventing a liquid delay at secretory transformations of a ferruterous component of mammary glands and, as a result, development of a pain syndrome (a mastalgiya or a mastodynia).
Along with it the transdermalny way of introduction of a gestagen allows to influence also a condition of a ferruterous epithelium and vascular network therefore permeability of capillaries decreases, degree of hypostasis of tissues of mammary gland decreases, mastalgiya symptoms disappear.

Pharmacokinetics. Absorption. At a transdermalny route of administration of Prozhestozhel® reaches tissue of mammary glands, without collapsing in a liver and without rendering adverse system effects on an organism.
Absorption of progesterone at cutaneous use makes about 10% of a dose. The research of serumal concentration of prolactin, oestradiol and progesterone at treatment by Prozhestozhel showed that in 1 h after putting drug when the maximum absorption in fabric is observed, the level of hormones practically does not change.

Distribution. Cutaneous applications on area of mammary glands allow to create high concentration in an area of coverage (10 times higher, than in a system blood-groove) drug at reduction of the applied dose.

Metabolism. Drug for the second time is metabolized in a liver with formation of conjugates with glucuronic and sulfuric acids. Also CYP2C19 isoenzyme participates in metabolism.

Removal. It is removed by kidneys - 50-60%, with bile - more than 10%. The quantity of the metabolites removed by kidneys fluctuates depending on a phase of a yellow body.

Indications to use:

— mastodynia;
— diffusion fibrous and cystous mastopathy.

Route of administration and doses:

It is necessary to put 1 application of gel (2.5 g of gel; contains 0.025 g of progesterone) on skin of mammary glands the applicator doser before full absorption of 1-2 times/days daily or in the 2nd phase (from the 16th to the 25th day) a menstrual cycle. A course of treatment - to 3 cycles.
The repeated course of treatment can be appointed only after consultation with the doctor.

Features of use:

Прожестожель® it can be applied at the mastodynia connected with reception of oral contraceptives, the pubertal period premenopauzy, a syndrome of premenstrual tension.

Drug should be applied on skin of a mammary gland with the applicator doser, without rubbing and without massing mammary glands.

After putting cream it is necessary to avoid direct sunshine.

Influence on ability to driving of motor transport and to control of mechanisms
Researches on identification of possible influence of drug on ability to driving of the car or on ability to control of mechanisms were not conducted.

Side effects:

From a reproductive system: extremely seldom - morbidity of mammary glands, hot rushes of blood, a metrorrhagia, decrease in a libido.
Allergic reactions: an erythema in the place of application of gel, hypostasis of lips and a neck, fever, a headache, nausea.

Interaction with other medicines:

Effect of drug can amplify at simultaneous use with the combined hormonal contraceptives.

Contraindications:

— nodal forms of a fibrous and cystous mastopathy;
— tumors (tumorous educations) of mammary glands of not clear etiology;
— monotherapy of a breast cancer;
— monotherapy of cancer of generative organs;
— II and III trimesters of pregnancy;
— individual hypersensitivity to drug components.

With care it is necessary to use drug at a liver failure, a renal failure, bronchial asthma, epilepsy, migraine, a depression, a giperlipoproteinemiya, an extrauterine pregnancy, abortion in the course, tendency to fibrinferments, at acute forms of phlebitis or thromboembolic diseases, bleedings of not clear etiology from a vagina; porphyrias, arterial hypertension, diabetes mellitus.

Use of the drug PROZHESTOZHEL® at pregnancy and feeding by a breast
There is no sufficient experience of use of the drug Prozhestozhel® at pregnancy.
Use of drug at pregnancy and in the period of a lactation perhaps only in that case when the estimated advantage for mother exceeds potential risk for a fruit and the child.

Use at abnormal liver functions
With care it is necessary to use drug at a liver failure.

Use at renal failures
With care it is necessary to use drug at a renal failure.

Overdose:

Due to the low system absorption the overdose is improbable.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

80 g - tubas aluminum (1) complete with the applicator doser - packs cardboard.