Estrozhel

General characteristics. Structure:

Acting substances: oestradiol гемигидрат (in terms of oestradiol) 1 g 600 mkg;

Excipients: carbomer (карбопол 980), троламин (trietanolamine), ethanol, water cleared.

Pharmacological properties:

Oestrogenic drug for external use. Oestradiol, active agent of the drug Estrozhel®, is estrogen.
Against the background of treatment by Estrozhel expressiveness of a menopausal syndrome considerably decreases (including inflows, the increased sweating, dryness of a vagina, reduced mood). Clinical performance of Estrozhel at treatment of symptoms of the postmenopauzny period is comparable with that at reception of oestrogenic drugs inside.
Use of drug promotes decrease in concentration of the general cholesterol without change of a ratio of cholesterol/LPVP.
Use of drug slows down reduction of density of a bone tissue in the period of a menopause.
Has procoagulant effect, increases synthesis in a liver vitamin of K-dependent blood-coagulation factors (II, VII, IX, X), reduces concentration of antithrombin III.

Pharmacokinetics. Absorption and distribution. When putting gel ethanol quickly evaporates and oestradiol gets through skin. At the same time its most part gets to a system blood stream at once, and a quantity of oestradiol is late in a hypodermic fatty tissue and is released in a system blood stream gradually.
Cmax in blood reaches oestradiol in 3-4 h. Bioavailability makes 82%.

Metabolism and removal. At external use oestradiol is not exposed to effect of "the first passing" that provides higher concentration of oestradiol in a blood plasma in comparison with peroral forms.
Metabolism and removal of oestradiol at Estrozhel's use corresponds to biotransformation and removal of natural estrogen.

Indications to use:

— elimination of symptoms of a menopausal syndrome (including at an artificial menopause);
— prevention and treatment of postmenopauzny osteoporosis.

Route of administration and doses:

Эстрожель® appoint outwardly, it is continuous or in the cyclic mode. Doses and duration of therapy establish individually.
1 dose of the applicator corresponds to 2.5 g of gel and contains 1.5 mg of oestradiol.
1 dose of the applicator (or 2.5 g of gel) is applied with a thin layer on skin of a stomach, lumbar area, shoulders or forearms before full absorption of 1 times/days. The area of drawing has to make not less than the area of two palms.
Drawing is considered correct and effective if gel is soaked up completely within 2-3 min. If the sticky consistence remains more than 5 min. after drawing, means gel too small surface area of skin is covered.
Use of the drug Estrozhel® has to be carried out by the woman, in the morning or in the evening, it is preferable on clean skin. Эстрожель® does not leave spots.

Features of use:

Before an initiation of treatment it is necessary to conduct gynecologic examination, and at long therapy it is necessary to carry out it not less than 1 time a year.

Oestradiol it is reasonable to combine treatment with gestagena according to the recommendation of the doctor.

It is necessary to avoid hit of gel on mammary glands and mucous membranes of a vulva and a vagina.

Prolonged treatment by oestradiol increases risk of development of a breast cancer and an endometria (depends on duration of treatment and a dose of estrogen).

The hyperplasia (atipichesky or ferruterous) often precedes endometrial cancer. The combination of estrogen with gestageny has protective action on an endometria. Treatment should be stopped for 4-6 weeks before the planned surgical treatment.

Is not a contraceptive and does not protect from pregnancy.

At emergence of irregular menstrual allocations against the background of treatment (at women with an intact uterus) carrying out a diagnostic scraping is necessary for an exception of a malignant new growth of a uterus.

Use of oestradiol should be stopped immediately in case of a deep vein thrombosis, a thromboembolism of other localization, emergence of jaundice, strengthening or emergence of earlier not existing migrenepodobny pains, a sudden vision disorder, substantial increase of the ABP.

It is necessary to carry out systematically control of function of a liver and the ABP, concentration of glucose to blood at a diabetes mellitus.

Side effects:

From TsNS: headache, migraine, changes of mood, dizziness.
From a reproductive system: morbidity, sensitivity and increase in the sizes of mammary glands, an amenorrhea, bleedings of "break", a menorrhagia, the intermenstrual "smearing" vulval allocations, a tumor of mammary glands, increase in a libido.
From the alimentary system: extremely seldom (since there is no effect of "the first passing" through a liver) - dyspepsia, spasms of smooth muscles of a GIT (including intestinal or bilious colic), pain in epigastriums, cholestatic jaundice, a cholelithiasis, a meteorism, anorexia, nausea, vomiting (mainly the central genesis, generally at use of high doses), diarrhea, obstruction of a gall bladder, hepatitis, pancreatitis.
Local reactions: irritation and dermahemia.
Others: peripheral hypostases, change of body weight, increase in the ABP, allergic skin reactions (urticaria, skin itch), thrombembolia, contact dermatitis, intolerance of contact lenses.
Side effects are, as a rule, expressed poorly, are noted preferential in the first months of therapy and very seldom lead to drug withdrawal.

Interaction with other medicines:

At simultaneous use estrogen can reduce effect of indirect anticoagulants, hypotensive and hypoglycemic drugs (correction of the mode of dosing of hypoglycemic medicines can be required).

At simultaneous use estrogen increases efficiency of hypolipidemic medicines.

At simultaneous use of the estrogen and medicines inducing microsomal enzymes of a liver (including barbiturates, carbamazepine, griseofulvin, rifampicin), decrease in concentration of oestradiol in a blood plasma is possible.

At simultaneous use estrogen weakens effect of male sex hormones, diuretic medicines.

At simultaneous use with estrogen anxiolytic medicines (tranquilizers), opioid analgetics, medicines for the general anesthesia accelerate oestradiol metabolism.

At simultaneous use of estrogen with phenylbutazone and some antibiotics (including ampicillin, rifampicin) concentration of oestradiol in a blood plasma decreases that is connected with change of microflora in intestines.

At simultaneous use with estrogen folic acid and drugs of hormones of a thyroid gland strengthen effect of oestradiol.

Contraindications:

— hemorrhagic or ischemic stroke;
— thromboembolisms or acute thrombophlebitis;
— uterine bleedings of not clear etiology;
— estrogenzavisimy malignant new growths or suspicion on them;
— malignant and benign tumors of a hypophysis;
— a serious illness of a liver during the acute period, liver tumors, jaundice;
— renal failure;
— syndrome Cudgel Johnson;
— Rotor syndrome;
— pregnancy;
— breastfeeding period;
— hypersensitivity to drug components.

With care it is necessary to use drug at an ischemic heart disease, a circulatory unefficiency, a diabetes mellitus, migraine, bronchial asthma, inflammatory diseases of female generative organs, epilepsy, a severe form of arterial hypertension, abnormal liver functions, instructions in the anamnesis on thrombophlebitises, thromboses or thromboembolisms against the background of use of estrogen, a family giperlipoproteinemiya, pancreatitis, endometriosis, diseases of a gall bladder in the anamnesis (especially a cholelithiasis), jaundice in the anamnesis (including during the previous pregnancy), a hepatic porphyria, a leiomyoma, the hypercalcemia associated with bone metastasises of a breast cancer.

Use of the drug ESTROZHEL® at pregnancy and feeding by a breast
Эстрожель® it is contraindicated to use at pregnancy and during breastfeeding.

Use at abnormal liver functions
Use of drug at a serious illness of a liver during the acute period is contraindicated, liver tumors, jaundice.
With care it is necessary to use drug at abnormal liver functions, diseases of a gall bladder in the anamnesis (especially a cholelithiasis), jaundice (including in the anamnesis during the previous pregnancy), a hepatic porphyria.

Use at renal failures
Use of drug at a renal failure is contraindicated.

Overdose:

Symptoms: nausea, vomiting, in certain cases - a metrorrhagia.
Treatment: drug withdrawal, symptomatic therapy.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Gel of transdermalny 600 mkg/g: tubas of 80 g in set. with the applicator.