Pharmacological action Evista 60 mg
Selective estrogen receptor modulator. It acts as an agonist on body tissues, not associated with reproduction, and as an antagonist – the reproductive tissue. Effect due to high-affinity binding to estrogen receptors and the regulation of gene expression.
Process reduces bone resorption and normalizes the balance of calcium in the body, primarily by reducing the loss of calcium in the urine.
It does not cause endometrial proliferation, increasing the size of the uterus, bleeding, or bleeding in the postmenopausal period. Does not describe the incidence of endometrial cancer de novo. It does not cause hyperplasia of mammary tissue. Reduces swelling and breast tenderness.
Reduces the levels of total cholesterol and LDL cholesterol. HDL cholesterol and triglyceride levels were not significantly altered. Reduces plasma fibrinogen levels.
Pharmacokinetics Evista 60 mg
After oral administration, raloxifene is rapidly absorbed from the gastrointestinal tract. Subjected to intensive metabolism by glucuronidation in the “first pass” through the liver. In blood plasma determined by three conjugated metabolites. Absolute bioavailability of raloxifene is 2%.
Widely distributed in the body. Vd does not depend on the dose. Plasma protein binding is 98-99%.
The level of raloxifene is maintained by enterohepatic recirculation. T1 / 2 at 7.27 pm
Most of the dose as unchanged substance and metabolites are excreted within 5 days mainly in feces, less than 5% excreted in urine.
Indications for use of the drug Evista 60 mg
Prevention of osteoporosis in women postmenopauznom period.
Dosage regimen Evista 60 mg
When administered dose is Evista 60 mg / day. Treatment of long-term.
When applying for elderly patients dose adjustment is required.
Side effectEvista 60 mg
With the blood coagulation system: a small thrombocytopenia, rare – venous thromboembolism (including deep vein thrombosis), pulmonary embolism, thrombosis, retinal vein.
On the part of the circulatory system: vasodilation (hot flashes).
Other: calf muscle cramps, peripheral edema.
Contraindications to the use of the drug Evista 60 mg
Thromboembolism, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis, liver disease (including cholestasis), severe renal dysfunction, uterine bleeding of unknown etiology, breast cancer, endometrial cancer, increased sensitivity to raloxifene.
Pregnancy and lactation Evista 60 mg
Designed for use in women in postmenopauznom period.
Raloxifene may have a damaging effect on the fetus.
Is not known whether raloxifene in breast milk. When used in lactation may have a negative impact on child development.
Cautions Evista 60 mg
We do not recommend use in patients with severe hepatic impairment.
If during treatment with raloxifene having a disease or condition, leading to prolonged immobilization, treatment should be stopped. Resumption of therapy only after recovery of motor functions.
In the period of treatment should prescribe additional calcium. With the development of uterine bleeding should be a complete examination.
Drug Interactions Evista 60 mg
With the simultaneous use of coumarin derivatives may slight decrease in prothrombin time.
Kolestiramin significantly reduces the absorption and enterohepatic circulation of raloxifene.
In an application with ampicillin reduced the maximum concentration in plasma raloxifene, however, the extent of absorption and elimination rate of raloxifene did not change.
We do not recommend combination therapy with estrogen and raloxifene, for lack of clinical data on the safety of their simultaneous application.
Against the background of raloxifene significantly increases the concentration of globulins that bind hormones, including binding globulin sex hormone, thyroxine-binding globulin and binding globulin corticosteroid, with a simultaneous increase in the total concentration of hormones. These changes do not affect the concentration of free hormones.
