Evista (Tablets) Instructions for Use

Marketing Authorization Holder

Lilly, S.A. (Spain)

ATC Code

G03XC01 (Raloxifene)

Active Substance

Raloxifene (Rec.INN registered by WHO)

Dosage Form

Evista

Film-coated tablets, 60 mg: 14, 28, or 84 pcs.

Dosage Form, Packaging, and Composition

14 pcs. – blister packs (1) – cardboard packs
14 pcs. – blister packs (2) – cardboard packs
14 pcs. – blister packs (6) – cardboard packs.

Clinical-Pharmacological Group

Selective estrogen receptor modulator for the prevention of postmenopausal osteoporosis

Pharmacotherapeutic Group

Bone resorption inhibitor

Pharmacological Action

Selective estrogen receptor modulator. Acts as an agonist on non-reproductive body tissues and as an antagonist on reproductive tissues. The action is due to high-affinity binding to estrogen receptors and regulation of gene expression.

It reduces the process of bone resorption and normalizes calcium balance in the body, primarily by reducing calcium loss in the urine.

It does not cause endometrial proliferation, uterine enlargement, spotting, or bleeding in the postmenopausal period. No cases of de novo endometrial cancer have been described. It does not cause hyperplasia of breast tissue. It reduces breast swelling and tenderness.

It reduces total cholesterol and LDL levels. HDL and triglyceride levels do not change significantly. It reduces plasma fibrinogen levels.

Pharmacokinetics

After oral administration, Raloxifene is rapidly absorbed from the gastrointestinal tract. It undergoes intensive metabolism by glucuronidation during the first pass through the liver. Three conjugated metabolites are detected in blood plasma. The absolute bioavailability of raloxifene is 2%.

It is widely distributed in the body. The V_d is dose-independent. Plasma protein binding is 98-99%.

The level of raloxifene is maintained due to enterohepatic recirculation. The T_1/2 is 27.7 hours.

Most of the dose is excreted within 5 days, mainly in the feces as the unchanged substance and metabolites, with less than 5% excreted in the urine.

Indications

Prevention of osteoporosis in postmenopausal women.

ICD codes

Dosage Regimen

Take one 60 mg tablet orally once daily.

Administer the tablet at any time of day, with or without food.

Swallow the tablet whole; do not crush or chew it.

Continue treatment on a long-term basis for the prevention of postmenopausal osteoporosis.

No dose adjustment is necessary for elderly patients.

Discontinue therapy in the event of an immobilizing illness; resume only after full mobility is restored.

Ensure adequate calcium and vitamin D intake during treatment.

Conduct a gynecological examination if unexplained uterine bleeding occurs.

Adverse Reactions

From the blood coagulation system mild thrombocytopenia; rarely – venous thromboembolism (including deep vein thrombosis), pulmonary embolism, retinal vein thrombosis.

From the circulatory system vasodilation (hot flashes).

Other leg cramps, peripheral edema.

Contraindications

Thromboembolism, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis, liver disease (including cholestasis), severe renal impairment, uterine bleeding of unknown etiology, breast cancer, endometrial cancer, hypersensitivity to raloxifene.

Use in Pregnancy and Lactation

Intended for use only in postmenopausal women.

Raloxifene may have a damaging effect on the fetus.

It is not known whether Raloxifene is excreted in breast milk. When used during lactation, it may have a negative impact on child development.

Use in Hepatic Impairment

Contraindicated in liver disease (including cholestasis).

Use in Renal Impairment

Contraindicated in severe renal impairment.

Geriatric Use

No dose adjustment is required when used in elderly patients.

Special Precautions

Use in patients with severe hepatic impairment is not recommended.

If diseases or conditions leading to prolonged immobilization occur during the use of raloxifene, treatment must be discontinued. Therapy can be resumed only after motor functions are restored.

Calcium supplements should be additionally prescribed during treatment. If uterine bleeding develops, a complete examination is necessary.

Drug Interactions

When used concomitantly with coumarin derivatives, a slight decrease in prothrombin time is possible.

Cholestyramine significantly reduces the absorption and enterohepatic circulation of raloxifene.

When used concomitantly with ampicillin, the maximum plasma concentration of raloxifene decreases; however, the extent of absorption and the elimination rate of raloxifene do not change.

Combination therapy with raloxifene and estrogens is not recommended due to the lack of clinical data on the safety of their simultaneous use.

During the use of raloxifene, the concentration of hormone-binding globulins, including sex hormone-binding globulin, thyroxine-binding globulin, and corticosteroid-binding globulin, slightly increases, with a simultaneous increase in the total concentration of hormones. These changes do not affect the concentration of free hormones.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.