Selective estrogen receptor modulator. Acts as agonist on body tissues not related to reproduction, and the antagonist in reproductive tissues. Effect due to high-affinity binding to estrogen receptors and regulation of gene expression.
Process reduces bone resorption and normalizes the balance of calcium in the body, primarily by reducing losses of calcium in the urine.
Does not cause endometrial proliferation, increase of uterine size, bleeding or bleeding in the postmenopausal period. Not described the incidence of endometrial cancer de novo. Does not cause hyperplasia of mammary tissue. Reduces swelling and breast tenderness.
Reduces levels of total cholesterol and LDL. Levels of HDL and triglycerides were not significantly changed. Reduces the level of fibrinogen of blood plasma.
Once inside the raloxifene is rapidly absorbed from the gastrointestinal tract. Subjected to intensive metabolism by glucuronidation in the “first pass” through the liver. In plasma be determined 3 conjugated metabolite. Absolute bioavailability of raloxifene is 2%.
Widely distributed in the body. Vd does not depend on the dose. Linking plasma protein is 98-99%.
The level of raloxifene maintained by enterohepatic recirculation. T1/2 is 27.7 h.
Most of the dose in the form of unchanged substance and metabolites was excreted within 5 days mainly with faeces, less than 5% excreted in the urine.
Not recommended for use in patients with severe liver dysfunction.
If the use of raloxifene experiencing the disease or condition leading to prolonged immobilization, treatment should be discontinued. Restoration therapy is possible only after recovery of motor function.
During the period of treatment should appoint preparations of calcium. With the development of uterine bleeding need a full examination.
Together with the use of coumarin derivatives may be a small decrease in prothrombin time.
Kolestiramin reduces absorption and enterohepatic circulation of raloxifene.
Together with the use of ampicillin decreased the maximum concentration of raloxifene in the plasma, however, extent of absorption and the elimination rate of raloxifene are not changed.
Not recommended combined therapy with raloxifene and estrogens due to the lack of clinical data on the safety of their simultaneous use.
With the use of raloxifene slightly increases the concentration of globulins that bind hormones, including globulin, linking sex hormones, thyroxine-binding globulin and globulin, corticosteroid binding, with a simultaneous increase in the total concentration of hormones. These changes do not affect the concentration of free hormones.