Index of drugs

Treatment and prevention of osteoporosis in postmenopausal women. A significant reduction in the incidence of vertebral fractures has been demonstrated, but there has been no reduction in the incidence of hip fractures. The postmenopausal symptoms, the effect of the product on the uterus and nipple, and the risks and benefits of cardiovascular effects should be considered in postmenopausal women prior to the decision to use the preparation as well as other therapies, including the administration of estrogen. vascular.

1 tabl powl. contains 60 mg of raloxifene hydrochloride. The preparation contains lactose.

Selective estrogen receptor modulator (SERM). It has selective agonistic or antagonistic activity in relation to estrogen-sensitive tissues. As an agonist, it acts on the bones and partly on the metabolism of cholesterol (reduction of total cholesterol and LDL cholesterol). However, it does not show any agonist effects on the hypothalamus, uterus or breast tissue. The biological activity of raloxifene, like estrogens, depends on binding, with high affinity, to estrogen receptors and regulation of gene expression. This binding induces different expression of estrogen-regulated genes in various tissues. Raloxifene is rapidly absorbed after oral administration. Approximately 60% of the administered dose is absorbed. It undergoes the first-pass effect to a significant extent due to increased conjugation with glucuronic acid. Absolute bioavailability is 2%. Raloxifene is extensively bound to plasma proteins (98-99%). It is highly coupled to glucuronic acid in the first pass process, forming 4'-glucuronate, 6-glucuronate, and raloxifene 6, 6'-diglucuronate. In the total concentration of raloxifene and its glucuronides in the blood, the parent compound is only 1%. The concentration of raloxifene is maintained thanks to the hepatic-enteric circulation. T_0,5 raloxifene in plasma is 27.7 hours. Most of the dose of raloxifene administered and its glucuronide metabolites are excreted within 5 days, mainly in faeces. Less than 6% is excreted in the urine.

Hypersensitivity to the active substance or to any of the excipients. Do not use in women of childbearing age. Current or previous thromboembolism, including deep vein thrombosis, pulmonary embolism, retinal vein thrombosis. Hepatic impairment, including cholestasis. Severe kidney problems. Bleeding from the genital tract with an undetermined cause. The drug should not be used in patients with signs or symptoms of endometrial cancer, because the safety of use in this group of patients has not been adequately tested.

The use of raloxifene increases the risk of thrombotic changes in the venous system, in a similar degree to the reported risk associated with the use of HRT. In patients with risk factors for thrombotic changes in the venous system, regardless of etiology, the benefit-risk ratio should always be considered. In any case of a disease or condition requiring prolonged immobilization, the preparation should be discontinued. Discontinuation of use should be as soon as possible in case of disease causing immobility or 3 days before planned immobilization. Do not restart the preparation until the cause of immobilization persists and the patient is not fully functional. An increased risk of stroke should be considered when taking raloxifene in postmenopausal women with a history of stroke or other significant risk factors for stroke, such as transient ischemic attacks or atrial fibrillation. No proliferation of the endometrium was observed. During the use of the drug, any uterine bleeding is unexpected and requires careful examination by a specialist. The two most commonly diagnosed causes of genital tract bleeding during raloxifene use are endometrial atrophy and benign endometrial polyps. It is not recommended to use the drug in patients with hepatic impairment.Serum concentrations of bilirubin, GGT, alkaline phosphatase, ALT and AST should be closely monitored if increases in serum concentrations have been observed with raloxifene. Caution should be exercised in patients with moderate and mild renal impairment. Limited clinical data indicate that in patients who have undergone hypertriglyceridemia (> 5.6 mmol / l) after oral estrogen treatment, the use of raloxifene may result in a significant increase in serum triglycerides. When using raloxifene in these patients, serum triglyceride levels should be monitored. The safety of the medicine has not been studied in patients with breast cancer. There are no data on co-administration of raloxifene and preparations used to treat early and advanced forms of breast cancer. Therefore, the drug should be used in the treatment and prevention of osteoporosis, only after the treatment of breast cancer, including after the completion of adjuvant therapy. The concomitant use of raloxifene and estrogens given in general due to limited data on the safety of this combination is not recommended. The drug does not reduce vasomotor symptoms (hot flushes) or other symptoms of menopause associated with estrogen deficiency. The product should not be used in children. The preparation contains lactose - should not be used in patients with rare inherited disorders associated with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

The drug is intended only for use in postmenopausal women. It must not be used in women of childbearing age. The use of raloxifene in pregnant women can cause fetal damage. Do not use in breast-feeding women.

Very common: vasodilatation (hot flushes), gastrointestinal symptoms (such as nausea, vomiting, abdominal pain, indigestion), flu-like symptoms, increased blood pressure. Common: headaches (including migraine headaches), rash, cramps in the lower limbs, benign breast ailments (such as pain, enlargement and tenderness), peripheral edema. Uncommon: thrombocytopenia, fatal stroke, venous thromboembolic events (including deep vein thrombosis, pulmonary embolism, retinal vein thrombosis, superficial thrombophlebitis), thromboembolic reactions in the arterial system.

Orally. Adults: 1 tabl. daily at any time of the day, regardless of meals. The preparation is intended for long-term use. A small amount of Calcium and vitamin D in the diet should be supplemented with calcium and vitamin D supplements. There is no need to adjust the dose in the elderly.