Instruction for use: Evista

Active substance Raloxifene

ATX code G03XC01 Raloxifene

Pharmacological groups

Estrogens, gestagens; Their homologues and antagonists

Nosological classification (ICD-10)

M81.0 Postmenopausal osteoporosis

Menopause osteoporosis, Osteoporosis in menopause, Osteoporosis in menopause, Osteoporosis in postmenopausal women, Osteoporosis in the postmenopausal period, Postmenopausal osteoporosis, Osteoporosis in postmenopausal women, Perimenopausal osteoporosis, Postmenopausal osteoporosis, Post-menopausal osteoporosis, Postmenopausal osteoporosis, Postmenopausal demineralization of bones, Osteoporosis with estrogen deficiency, Osteoporosis in postmenopausal women, Osteoporosis in postmenopausal women and after hysterectomy

Composition and form of release

1 tablet, coated, contains raloxifene hydrochloride 60 mg; In the outline cell box 14, 28 or 84 pcs.

pharmachologic effect

Pharmacological action - inhibiting bone resorption.

Selective modulator of estrogen receptors. As an agonist affects non-productive tissues and as an antagonist - on the reproductive. Increases the concentration of globulins, binding hormones (sex, thyroxine, corticosteroids) with a simultaneous increase in their total content in the blood without increasing the level of free fraction.

Pharmacodynamics

Normalizes the processes of bone resorption in the postmenopausal period (increases the mass of bone tissue), reduces the loss of calcium through the urinary system. Reduces total cholesterol, cholesterol in the LDL fraction (low density lipoprotein), serum fibrinogen, Lp (a) and increases the concentration of HDL sub-fraction (high-density lipoproteins) -C2. Does not stimulate the proliferation of the endometrium, breast tissue, reduces the risk of developing breast cancer.

Pharmacokinetics

Quickly absorbed after oral administration by approximately 60%. Before entering the systemic blood stream is subjected to intensive formation of glucuronides. Absolute availability is only 2%. The time to reach the mean maximum plasma concentration and bioavailability depends on the interconversions in systemic circulation and the conversions of raloxifene and its glucuronide metabolites in the intestine and liver. In patients with hepatic insufficiency, the plasma concentration is about 2.5 times higher than in healthy ones and correlates with the concentration of bilirubin. Has a large volume of distribution (does not depend on the dose). T1 / 2 in plasma - 27.7 hours. Most of the drug and its metabolites are excreted for 5 days and is found mainly in feces (less than 6% excreted in urine).

Indications

Prevention of osteoporosis in postmenopausal women.

Contraindications

Hypersensitivity, thromboembolism (including in the anamnesis), pulmonary embolism and retinal vein thrombosis, deep vein thrombosis, hepatic insufficiency, osteoporosis in men, childbearing age (in women).

pregnancy and lactation

Not recommended.

Side effects

Thrombosis of veins, thromboembolism, hot flushes, painful spasms of calf muscles, peripheral edema.

Interaction

With simultaneous administration with warfarin or other derivatives of coumarin, prothrombin time may decrease. Cholestyramine decreases absorption.

Dosing and Administration

Inside, 1 tab. (60 mg) per day (at any time of the day, regardless of food intake). The course of treatment is long. Women can be combined with calcium supplements.

Precautionary measures

It is not recommended to use in combination with estrogens.

storage Conditions

In a dry, the dark place at a temperature of no higher than 30 ° C. Do not freeze or expose to excessive heat or sunlight.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiry date printed on the package.