ESTROJEL

Active material: Estradiol
When ATH: G03CA03
CCF: Protivoklimakterichesky estrogenic drugs
ICD-10 codes (testimony): M81.0, M81.1, N95.1, N95.3
When CSF: 15.11.01
Manufacturer: BESINS Laboratories INTERNATIONAL (France)

Pharmaceutical form, composition and packaging

Transdermal gel colorless, clear, with the smell of ethanol.

Excipients: karʙomer (Carbopol 980), trolamin (triethanolamine), ethanol, Purified water.

80 g – Plastic bottles with a dosing device (1) – packs cardboard.

Transdermal gel colorless, clear, with the smell of ethanol.

Excipients: karʙomer (Carbopol 980), trolamin (triethanolamine), ethanol, Purified water.

80 g – aluminum tuba (1) complete with spatula-dropper – packs cardboard.

Pharmacological action

Estrogenic drug for external use. Estradiol, the active substance of the preparation Estrojel, is estrogen.

Èstroželem treatment significantly reduced the severity of menopausal syndrome (incl. tides, increased sweating, vaginal dryness, reduced mood). Clinical efficacy of Èstroželâ in the treatment of symptoms of postmenopauznogo period is comparable with such when taking estrogenic drugs inside.

The drug helps reduce total cholesterol concentrations without changing the ratio of cholesterol/HDL.

The drug inhibits the reduction of bone density in menopausal.

Pharmacokinetics

Absorption and distribution

When applying a gel ethanol evaporates quickly penetrates the skin and estradiol. While most of it gets into the bloodstream immediately, and some amount of estradiol is delayed in the subcutaneous fat tissue and is released into the bloodstream gradually.

C_max blood estradiol reaches through 3-4 no. Bioavailability is 82%.

Metabolism and excretion

When an external application estradiol is not subject to the effect of “first pass”, that provides a more physiological concentrations of estrogen in the blood plasma.

Metabolism and excretion of estradiol in applying Èstroželâ biotransformation and excretion matches the natural estrogen.

Testimony

-addressing the symptoms of menopause (incl. in Artificial menopause);

— postmenopauznogo prevention and treatment of osteoporosis.

Dosage regimen

Estrojel appoint external, continuous or cyclical mode. Dose and duration of therapy is determined individually.

1 dose (bottle) matches 1.25 g gel and contains 750 micrograms of estradiol.

1 dose (tuba) matches 2.5 g gel and contains 1.5 mg estradiol.

Should be applied 1 dose (2.5 g gel) (tuba) or 2 dose (2.5 g gel) (bottle) a thin layer on the skin of the abdomen, the lumbar region or forearms until intake 1 time / day.

Drawing is considered correct and efficient, If the gel is absorbed completely within 2-3 m. If a sticky consistency remains more 5 minutes after application, means the gel covered too small surface area of the skin. Coating area shall be not less than two square Palms.

Application of Estrojel should be the woman, in the morning or evening, preferably on clean skin.

Side effect

CNS: headache, migraine, mood lability, dizziness.

Reproductive system: soreness and sensitivity of the breast, amenorrhea, irregular menstruation, changes in libido, spotting from your vagina with frequent use of drugs.

From the digestive system: rarely (There is no effect “first pass” through the liver and stomach) – dyspeptic symptoms, cramps smooth muscles stomach, epigastric pain, cholestatic jaundice, cholelithiasis, flatulence, anorexia, nausea, vomiting (mainly central origin, mainly in the application of high doses).

Allergic reactions: hives, itching, contact dermatitis.

Other: peripheral edema, weight change, increased blood pressure, thromboembolism.

Side effects, usually, weakly expressed, celebrated mainly in the first few months of therapy and very rarely lead to withdrawal.

Contraindications

-hemorrhagic or ischemic stroke;

-embolism or acute thrombophlebitis;

- Uterine bleeding of unknown etiology;

— estrogenzawisimy breast cancer;

— estrogenzawisimy ovarian cancer;

— estrogenzawisimy uterine cancer;

— malignant pituitary tumors;

-benign tumors of the pituitary gland;

-severe liver disease in the acute period;

- Liver tumors;

- Jaundice;

- Renal failure;

-Johnson Syndrome;

Rotor syndrome;

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

FROM caution use in patients with coronary artery disease, circulatory failure, diabetes, migraine, asthma, inflammatory diseases of female genital organs, epilepsy, severe hypertension, hepatic dysfunction, guidance in history on thrombophlebitis, thrombosis, thromboembolism during treatment with estrogens in history, family hyperlipoproteinemia, pancreato, эndometrioze, gallbladder disease in history (especially cholelithiasis), jaundice (incl. a history of previous pregnancy during), hepatic porphyria, LM.

Pregnancy and lactation

Estrojel is contraindicated for use in pregnancy and lactation.

Cautions

Before treatment to conduct gynecological examination, and if long-term therapy should visit the gynecologist at least 1 per year.

Estradiol treatment it is advisable to combine with the use of gestagennah drugs.

Avoid getting gel on the breast and the mucous membranes of the vulva and vagina.

Should be systematically monitored liver and hell, blood glucose in diabetes mellitus.

Estrojel does not stain.

Overdose

Symptoms: nausea, vomiting, in some cases – metrorragija.

Treatment: removal of the drug, simptomaticheskaya therapy, aimed at maintaining vital functions.

Drug Interactions

Together with the use of estrogens may reduce proximity effect anticoagulants, antihypertensive and hypoglycemic drugs (You may need a correction mode of hypoglycemic drugs).

Together with the use of estrogens increase the efficacy of lipid-lowering drugs.

Together with the use of estrogen and drugs, inducing liver enzymes (incl. barbiturates, Carbamazepine, griseofulvin, rifampicin), may reduce the concentration of estradiol in plasma.

Together with the use of estrogens weakening effect of male sex hormones, diuretic medicines.

Together with the application anksioliticaskie estrogenami medicines (trankvilizatorы), opioid analgesics, drugs for general anesthesia accelerates the metabolism of estradiol.

Together with the use of estrogens with fenilbutazonom and some antibiotics (incl. ampicillin, rifampicin) decreases the concentration of estradiol in plasma, due to changes in the gut microflora.

Together with the use of folic acid and estrogen drugs thyroid hormones increase the effect of estradiol.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.