Expiration date: 03/2025

Structure and Composition:

Dragee of white color. 1 tablet contains:

2 mg estradiol valerate

Dragee of pink color. 1 tablet contains:

2 mg estradiol valerate

1 mg cyproterone acetate

in a blister pack with a calendar scale of 21 pcs. (11 pills white and 10 pink pills) in a cardboard box 1 blister

Pharmachologic effect:

Fills in a woman's sex hormones deficiency eliminates the symptoms of menopausal disorders, has a preventive effect against the development of osteoporosis, endometrial hyperplasia, lowers the level of LDL cholesterol in the blood serum. Hormone replacement therapy reduces the risk of cardiovascular disease.

Pharmacokinetics:

Estradiol valerate.

Once inside quickly and completely absorbed. At the "first pass" through the liver steroid ester is cleaved to valeric acid and estradiol, which is further metabolized to estrone, estriol and estrone sulfate. Bioavailability of estradiol is 3% (a meal does not affect bioavailability). Cmax 30 pg / ml, achieved after 4-9 hours during the day reduced serum and 15 pg / ml. Associated 30-40% albumin and globulin, sex hormone binding (SHBG). The volume of distribution following single on / in the - 1 l / kg. Estradiol is mainly metabolised in the liver and intestine, skeletal muscle and target organs to form estrone, estriol, kateholestrogenov, sulfate and glucuronide conjugates of these substances. Cl estradiol after a single on / in the 10-30 ml / min / kg, the final metabolites are excreted in the urine. The equilibrium concentration of estradiol 30-60 pg / L. After discontinuation of estradiol and estrone levels are restored in 2-3 days.

Cyproterone acetate.

Once inside quickly and completely absorbed. The absolute bioavailability - 88%. Cmax (8 pg / ml) was achieved in 1-2 hours after oral administration of 1 mg of drug. T1 / 2 biphasic - 0.8 hours and 2.3 days. Almost completely binds serum albumin, 3.5-4% of the total is in the free state. Total speed Cl - 3,6 ml / min / kg. It is metabolized to form derivatives, which are then excreted in the urine and bile in a ratio of 3: 7 and T1 / 2 - 1.9 days.

Testimony:

Climacteric disorder (hormone replacement therapy): psycho-vegetative disorders, symptoms of skin involution, dry mucous membranes of the urinary organs, a phenomenon androgenization estrogen deficiency of postmenopausal osteoporosis prevention (oophorectomy about non-malignant neoplasms), menstrual disorders - primary and secondary amenorrhea, and others.

Contraindications:

Hypersensitivity to the drug, severe hepatic dysfunction, liver tumors (including in history), thromboembolic processes and active deep vein thrombosis (including history), breast cancer, severe hypertriglyceridemia, uterine bleeding unclear etiology , pregnancy, breastfeeding.

Application of pregnancy and breastfeeding:

Contraindicated during pregnancy. At the time of treatment should stop breastfeeding.

Side effect:

In rare cases:

• With the genitourinary system: menstrual disorders (breakthrough, spotting), dysmenorrhea, change in vaginal secretions.
  
• From the digestive tract: dyspepsia, loss of appetite, nausea, vomiting, abdominal pain, flatulence.
  
• For the skin: polymorphic rash.
  
• From the nervous system and sensory organs: headache, dizziness, migraine, anxiety, depression, fatigue, seizures, vision disorders.
  
• Miscellaneous: palpitations, edema, change in body weight, bloating, pain and breast enlargement, changes in libido, hypersensitivity reactions, intolerance to contact lenses.
  

Drug Interactions:

PM inducing liver enzymes (anticonvulsants, antimicrobial and other drugs), steroid hormones increase metabolism and reduce clinical efficacy. Antibiotics (penicillins, tetracyclines) lower effective concentration. PM undergoing conjugation (including paracetamol), increase the bioavailability of estradiol by competitive inhibition of conjugation in the intestinal absorption. When concomitant administration may require dose adjustment of hypoglycemic agents. Ethanol increases the level of estradiol in the blood.

Dosage and administration:

The inside is not liquid, squeezed small amounts of liquid, at about the same time, 1 tablet per day, starting from 5th day of the cycle. After completion of the ingestion of one calendar packaging make a 7-day interval, during which 2-4 days after the last drops, bleeding menstrualnopodobnoe begins. If the doctor does not prescribe a different treatment, after a 7-day break starting to take the drug from the next calendar packaging. In the absence of a 7-day break bleeding, treatment should be continued only after the exclusion of pregnancy.

Precautionary measures:

Before treatment is necessary to conduct general medical and gynecological examination, including breast examination, cytology cervical mucus, the exclusion of pregnancy, diseases of the blood coagulation system. Please note that Climen not be used as a contraceptive agent.

Special instructions:

You can change the biochemical parameters of liver, thyroid, adrenal, kidney, level of transportation of plasma proteins (including corticosteroid-binding globulin and lipid / lipoprotein fractions, parameters of carbohydrate metabolism, coagulation and fibrinolysis).