Included in the formulation
АТХ:G.03.X.C Selective modulators of estrogen receptors
G.03.X.C.01 Raloxifene
Pharmacodynamics:Selective modulator of estrogen receptors. Raloxifene has estrogenic effect on bone tissue (stimulates estrogen receptors), and on the endometrium and mammary glands - antiestrogenic (block of estrogen receptors). Binding to estrogen receptors leads to the expression of estrogen-regulated genes in various tissues.
Increases the concentration of globulins, binding sex hormones, thyroxine, corticosteroids, with a simultaneous increase in their total content in the blood. Normalizes the processes of bone resorption in the postmenopausal period, increases the mass of bone tissue, reduces calcium loss through the urinary system. Reduces total cholesterol, HDL cholesterol, serum fibrinogen and increases the subfraction of HDL-C.
Unlike tamoxifen and toremifene, it does not increase the risk of hyperplasia and endometrial cancer.
Pharmacokinetics:Quickly absorbed after ingestion. Bioavailability is about 60%. At the first passage through the liver is subjected to intense conjugation with glucuronic acid (absolute bioavailability of unchangedof the drug is only 2%). Concentration in the blood is maintained by intestinal hepaticth recirculation. In patients with hepatic insufficiency, the level of the drug in the blood is 2.5 times higher and correlates with the concentration of bilirubin. The half-life on average is 28 hours. Renal failure significantly prolongs the circulation of raloxifene; in these patients, only 6% of the dose is excreted in urine for 5 days.
Indications:Osteoporosis in postmenopausal women and after hysterectomy (prevention). Prophylaxis of breast cancer in women with osteoporosis in the postmenopausal period.
XIII.M80-M85.M81.1 Osteoporosis after removal of ovaries
XIII.M80-M85.M81.0 Postmenopausal osteoporosis
Contraindications:Thromboembolism, including deep vein thrombosis, pulmonary embolism and retinal vein thrombosis, liver disease (including cholestasis), severe renal dysfunction, uterine bleeding of unclear etiology, breast cancer, endometrial cancer.
Hypersensitivity, premenopause, pregnancy, breast-feeding; expressed violations of the liver.
Long-term immobilization.
Carefully:The potential risk and benefit of using raloxifene in chronic heart failure, malignant tumors, other conditions that increase the risk of thromboembolism, impaired liver function should be correlated (an increase in raloxifene concentration in the blood plasma may be possible, in patients with Child-Pugh class A cirrhosis the drug content was 2.5 times higher than expected and correlated with the concentration of bilirubin, the efficacy and safety of the application for severe violations of the liver were not investigated).
Pregnancy and lactation:Recommendations for FDA - Category X. It is intended only for use in postmenopausal women.
Raloxifene may cause damaging effects on the fetus.
There is no information on the penetration into breast milk. Do not apply!
Dosing and Administration:When you receive inwards the dose is 60 mg per day. Treatment is long.
When used in elderly patients, dose adjustment is not required.
Side effects:From the side blood coagulation system: small thrombocytopenia; rarely - venous thromboembolism (including deep vein thrombosis), pulmonary embolism, retinal vein thrombosis.
From the side circulatory system: vasodilation (sensation of heat).
Other: spasms of the calf muscles, peripheral edema.
Overdose:Symptoms: cramps of the muscles of the lower extremities and dizziness.
Treatment: symptomatic.
Interaction:Ampicillin - reduction of the maximum concentration without affecting absorption and elimination.
Warfarin and others indirect anticoagulants - Decreased efficacy, correction of warfarin dose is necessary.
Kolestyramine - decrease in absorption and intestinal-hepatic recirculation of raloxifene by 60%, simultaneous reception is not recommended.
Estrogens - simultaneous reception is not recommended.
Special instructions:It is not recommended to use in patients with severe impairment of liver function.
If raloxifene is caused by diseases or conditions leading to prolonged immobilization, treatment should be discontinued. Renewal of therapy is possible only after restoration of motor functions.
During the treatment should additionally prescribe calcium preparations. With the development of uterine bleeding, a complete examination is necessary.
Reduces the risk of development and progression of breast cancer and cardiovascular diseases.
Impact on the ability to drive vehicles and manage mechanisms
There are no indications that the drug can have an effect in driving vehicles and engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.