PROZHESTOZHEL

Active material: Progesterone
When ATH: G03DA04
CCF: Progestogen for outdoor use in mastodynia
ICD-10 codes (testimony): N60, N64.4
Manufacturer: BESINS Laboratories INTERNATIONAL (France)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Gel for external use 1% colorless, translucent, slightly opalescent, no visible particles, with the smell of alcohol.

Excipients: octyidodecanol, karʙomer 980, Macrogols glicerilgidroksistearat (Castor oil polioksilgidrogenizirovannoe), trolamin (triethanolamine), ethanol, water distillirovannaya.

80 g (32 dose on 2.5 g gel) – aluminum tuba (1) complete with applikatorom-dropper – packs cardboard.

Pharmacological action

Progestogen for external use. The active ingredient of the drug is progesterone.

Effect of progesterone receptor blocking based on estrogen, as a result of which improves the absorption of fluid from the tissues and reduces the compression of the lactiferous ducts, as well as blocking receptors of prolactin in breast tissue, resulting in lower laktopoèza.

Local use medication, creating a high concentration of progesterone in the zone of application of the, It has no systemic action and avoids unwanted side effects.

The mechanism of action of Prožestoželâ is based on the concentration of progesterone in breast tissue. Progesterone reduces the expression of estrogen receptors in breast tissue, as well as local level Active estrogen through the stimulation of production of enzymes (17-Beta-hydroxysteroid dehydrogenase deficiency and èstronsul′fotransferazy), oxidizing estradiol in less active estrone (tying the last, enzymes make it inactive estrone sulfate).

Thus, progesterone restricts proliferativnoe action of estrogen on breast tissue.

Progesterone also assists small natriyureticescoe effect through oppression and increase kanalzeva reabsorbtion cell filtering, preventing fluid retention in secretory transformation of ferrous component of mammary glands and, Consequently, development of pain (mastalgii or mastodinii).

Along with the transdermal route of Administration also allows progestogen affect the State of the glandular epithelium and vascular network, resulting in a reduced capillary permeability, reducing the swelling of breast tissue, fade the symptoms mastalgii.

Pharmacokinetics

Absorption

When dermal use Projestojel reaches breast tissue, not collapsing in the liver and without adverse systemic effects on the body.

Absorption of progesterone nakozhnom application is about 10% dose. Study on serum concentration of prolactin, estradiol and progesterone in the treatment of Prožestoželem revealed, that through 1 h after preparation, When there is maximum absorption in tissue, hormone levels virtually unchanged.

Distribution

Cutaneous application on the breast area allow you to create a high concentration in the range (in 10 times higher, than in the systemic blood) at the same time reducing the dose applied medication.

Metabolism

The drug again metabolised in the liver with the formation of conjugates with glukuronova and sulphuric acids. Also involved in the metabolism of CYP CYP2S19.

Deduction

Excreted in the urine – 50-60%, the bile – more 10%. The number of metabolites, excreted with urine, varies depending on the phase of the corpus luteum.

Testimony

- Mastodinija;

-diffuse fibrocystic breast disease.

Dosage regimen

Should be applied 1 application of gel (2.5 g gel; It contains 0.025 g progesterone) on the skin of the breast applicator-dropper until intake 1-2 times per day every day or in 2 phase (from the 16th to 25th day) menstrual cycle. A course of treatment – up to 3 's cycles.

A second course of treatment can be appointed only after consultation with the doctor.

Side effect

On the part of the reproductive system: rarely – breast tenderness, tides, metrorragija, decreased libido.

Allergic reactions: Erythema in the application of the gel, swelling of the lips and neck, fever, headache, nausea.

Contraindications

— anchor form fibrocystic mastopathy;

-tumors (tumour-education) mammary glands unclear etiology;

-monotherapy for breast cancer;

-monotherapy genital cancer;

— II and III trimenon of pregnancy;

- Hypersensitivity to the drug.

FROM caution use in patients with hepatic insufficiency, renal failure, asthma, epilepsy, migraine, depression, hyperlipoproteinemia, ectopic pregnancy, abortion in the go, the inclination to trombozam, in acute forms of phlebitis or thromboembolic diseases, bleeding unclear etiology of vagina; porfirii, hypertension, diabetes.

Pregnancy and lactation

There is insufficient experience of the drug Projestojel in pregnancy.

Use of the drug during pregnancy and lactation is possible only if, when the intended benefits to the mother outweighs the potential risk to the fetus and child.

Cautions

Projestojel can be used in mastodinii, associated with the intake of oral contraceptives, pubertatnym period, premenopauzoj, premenstrual syndrome.

The preparation should be applied on the skin breast applicator-dropper, No rubbing and not massaging breasts.

After applying the cream should avoid direct sunlight.

Effects on ability to drive vehicles and management mechanisms

Study on the identification of possible influence on the ability to drive a car or the ability to management mechanisms have not been conducted.

Overdose

Due to the low systemic absorption overdose is unlikely.

Drug Interactions

The drug may increase together with the use of combined hormonal contraceptives.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 2 year.