Raloxifene

Chemical name

[6-Гидрокси-2-(4-гидрокс��фенил)бензо[b]тиен-3-ил ]-[4-[2-(1-пиперидинил)-эт��кси]фенил]метанол (as hydrochloride)

Gross

C28-H27-N-O4-S

Of drugs

The drugs act-mode, ingibirutee bone resorption. Selective Modulator estrogenovykh receptors. Effective as agonist at nereproduguye tissue, as antagonist for reproductive. Selectively targets эстрогенчувствительн ые membranes, participates in the regulation of gene expression. Increases concentration globulinov linking sex hormones, tiroksin, corticosteroids, while increasing their overall content in the blood. Normalizes the bone rezorbtion in postmenopauzne period increased mass bone, reduces the loss of calcium through mochevadelitionuu system. Decreases total cholesterol, cholesterol LPVP, serum fibrinogen and increases subfraktia Lpvp-s_2.bystro absorbed after administration inwards. Bioavailability is about 60%. The "first pass" through the liver under heavy kongugirovaniu with glukuronova acid (absolute bioavailability unmodified product is only 2%). The concentration in the blood is supported by kishechno-pechenocna recycling. In patients with liver failure of the drug in the blood is 2.5 times higher and correlates with the concentration of cium. T_1/2 average 28 hours Renal failure has doubled circulation ralauxifena from such patients for a period of five days to return (with urine), only 6% of the doses.

Indications

Osteoporosis among women postmenopauzne period, and after hysterectomies (prevention).

Contraindications

Hypersensitivity, tromboembolia (incl. history), pulmonary artery disease and pulmonary veins retina, thrombosis of deep veins, liver failure, prolonged immobilization, childbearing women, pregnancy and breast-feeding.

Side-Effects

Thrombosis of deep veins, tromboembolia, pulmonary embolism and venous thrombosis retinal veins, vazodilatation in the first six months of treatment, tides, painful cramps gastrocnemius muscle and peripheral edema.

Patient interaction

Reduces effect coumarin derivatives. Holestiramin reduces bioavailability and blocks kishechno-pechenocnuu circulation. Ampicillin C_max reduced.

Dosing and Administration

Inside, 1 tab. (60 mg) a day, the long-term (can be combined with drugs calcium).

Directory → Hormones and their antagonists → Estrogens, gestagena; Their homologues and antagonists → Raloxifene