Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):ONLS
Pharmacodynamics: Tissue-specific agonist-antagonist of estrogen receptors. As an agonist tibolone affects the lipid metabolism and bone tissue, with respect to the endometrium and mammary glands acts as an antagonist. In the endometrium has a progestogen effect, and in the brain - estrogenic and androgenic. Thus, it alleviates the vasomotor symptoms, without exerting a proliferative effect on the mammary glands and endometrium.
It inhibits the resorption of bone tissue in the postmenopausal period, reduces the concentration of phosphates and calcium in the blood serum, in blood plasma - prevents the development of osteoporosis, softens manifestations of climacteric syndrome - "tides" of blood to the skin of the face, headaches, increased sweating. Increasing the concentration of central and peripheral opioids positively affects libido and mood.
Has a stimulating effect on the cells of the mucous membrane of the vagina, without causing proliferation of the endometrium. Reduces the concentration of calcium and phosphate.
Does not cause menstrual bleeding.
Pharmacokinetics:After oral administration, the empty stomach is completely absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma of metabolites of tibolone is reached after 1 hour.
Metabolism in the liver.
The elimination half-life is 7 hours. Elimination with feces and partial kidneys.
Indications:Used to treat menopausal disorders caused by natural or surgical menopause, it is used to prevent osteoporosis associated with estrogen deficiency.
XIII.M80-M85.M81.1 Osteoporosis after removal of ovaries
XIII.M80-M85.M81.0 Postmenopausal osteoporosis
XIV.N80-N98.N95.1 Menopause and menopause in women
Contraindications:Hepatic insufficiency, thrombophlebitis, hormone-dependent tumors, period less than 1 year from the last menses.
Individual intolerance.
Pregnancy and lactation:Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside for 2.5 mg / day at the same time of day.
The highest daily dose: 2.5 mg.
The highest single dose: 2.5 mg.
Side effects:Central and peripheral nervous system: headache, dizziness.
Cardiovascular system: edema of the shins.
Digestive system: dyspeptic disorders, diarrhea.
Dermatological manifestations: seborrhea rash, increased hair growth on the face.
Allergic reactions.
Overdose:Violation of the functions of the gastrointestinal tract.
Treatment is symptomatic.
Interaction:Strengthens the effect of anticoagulants, reduces glucose tolerance.
Simultaneous use with inductors of microsomal liver enzymes reduces the activity of the drug due to the acceleration of its metabolism.
Special instructions:The drug does not have a contraceptive effect.