Progesterone

General characteristics. Structure:

The operating veshchstvo: 10 mg or 25 mg of progesterone in 1 ml of Solutio oleosa.

Drug with the expressed progestagenny action.

Pharmacological properties:

Pharmacodynamics. Is hormone of a yellow body. Contacting receptors on a surface of cells of target organs, gets into a kernel, activates DNA and stimulates RNA synthesis.

Promotes transition of a mucous membrane of a uterus from proliferative in a secretory phase, creates necessary conditions for implantation of an oospore, reduces sensitivity of a uterus to oxytocin and relaxes her muscles (tokolitichesky effect). Stimulates lipoprotein lipases, increases fat reserves, increases levels of the basal and induced insulin, glucose utilization, accumulation in a glycogen liver, development of Aldosteronum, causes a hypoazotemia and a hyperazoturia; suppresses products of hypothalamic release factors of LG and FSG and, respectively, biosynthesis of gonadotropic hormones of a hypophysis.

In tissues of a mammary gland reduces permeability of capillaries, reduces the hypostasis of a connective tissue stroma dependent on a phase of a menstrual cycle slows down proliferation and mitotic activity of an epithelium of channels (at application in the form of gel).

Pharmacokinetics. At intake, intravaginalny (capsules), п / to and introduction in oil it is quickly absorbed. Cmax  at intake is reached in 1–3 h, at intravaginalny application — in 2–6 h. Linkng with proteins — 96–99%, is preferential with albumine (50–54%) and transcortinum (43–48%). In a liver turns mainly into pregnandiol and прегнанолон which then are exposed to conjugation with formation of glucuronides and sulfates. It is removed by kidneys (50–60%) and with bile (more than 10%); the progesterone metabolites which are excreted with bile are removed with excrements and can be exposed to enterogepatichesky recirculation.

At application on skin in the form of gel for external use it is practically not soaked up and does not get to a system blood stream.

Efficiency of use in the form of vaginal gel is shown at treatment of the secondary amenorrhea caused by a lack of progesterone and also in reproductive technologies for completion of a lack of progesterone at donorship of ova.

Indications to use:

Capsules: for intake — a premenstrual syndrome, a fibrous and cystous mastopathy; a premenopauza, a menopause, including premature, a postmenopause — as a gestagenny component of the replacement hormonal therapy (RHT) in combination with estrogen; intravaginalno — ZGT at nonfunctioning ovaries in case of lack of progesterone (donorship of ova), support of a lyuteinovy phase during preparation for extracorporal fertilization, support of a lyuteinovy phase in the spontaneous or induced menstrual cycle, prevention of the usual and menacing abortion owing to gestagenny insufficiency, endocrine infertility, prevention of a hysteromyoma, endometriosis.

Solution in oil: an amenorrhea, an oligomenorrhea, альгодисменорея (because of a hypogenitalism), an anovulatory metrorrhagia, endocrine infertility (including insufficiency of a yellow body), threat of abortion, diagnosis of secretion of estrogen.

Gel for external use: mastodynia, mastopathy.

Route of administration and doses:

Inside, intravaginalno, in oil, locally. The mode of dosing and the choice of a dosage form depend on indications. Duration of treatment is defined by character and features of a disease.

Features of use:

During treatment concentration of attention is weakened (it is necessary to be careful at control of vehicles and occupations other potentially dangerous types of activity demanding speed of psychomotor reactions).

Side effects:

Allergic reactions.

Capsules: drowsiness, passing dizziness (in 1–3 h after reception), frustration of a menstrual cycle (reduction, intermediate bleeding).

Solution in oil: thromboembolism (including pulmonary artery and vessels of a brain), thrombophlebitis, retina vein thrombosis, increase in the ABP, hypostases, calculous cholecystitis, cholestatic hepatitis, drowsiness, headache, depression, apathy, dysphoria, vision disorder, nausea, vomiting, loss of appetite, galactorrhoea, change of body weight, hirsutism, alopecia; increase, pain and tension of mammary glands; decrease in a libido, frustration of a menstrual cycle (reduction, intermediate bleeding); morbidity in an injection site.

Interaction with other medicines:

Reduces efficiency of action of the HP stimulating unstriated muscles of a uterus, anabolic steroids. At simultaneous use with barbiturates effect of progesterone decreases.

Contraindications:

Hypersensitivity. Capsules: the expressed abnormal liver functions, tendency to fibrinferments, acute forms of phlebitis or thromboembolic diseases, vaginal bleedings of unspecified genesis, incomplete abortion, a porphyria.

Solution in oil: a breast cancer and generative organs (for monotherapy), the expressed abnormal liver functions, pregnancy (II and the III trimester), tendency to fibrinferments, acute forms of phlebitis or thromboembolic diseases, vaginal bleedings of unspecified genesis, a cancelled abortion, a porphyria.

Restrictions to use. Capsules: diseases of cardiovascular system, including arterial hypertension, bronchial asthma, the expressed renal failures; TsNS diseases, including depression, epilepsy, migraine; diabetes mellitus; pregnancy (II and III trimester), feeding by a breast.

Solution in oil: diseases of cardiovascular system, including arterial hypertension, bronchial asthma, the expressed renal failures, TsNS diseases, including a depression, epilepsy, migraine; diabetes mellitus, extrauterine pregnancy, feeding by a breast.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solutio oleosa for injections of 10 mg/ml and 25 mg/ml, on 1 ml in an ampoule. On 1, 5 or on 10 ampoules, in cardboard packaging.