Active Ingredient and Formulation

Evista contains the active ingredient raloxifene hydrochloride. It is formulated as a tablet for oral administration. Each tablet is white, elliptical, and imprinted with the manufacturer’s mark and a code. The medication is available in 60 mg strength.

Pharmacological Classification

Evista is classified as a selective estrogen receptor modulator (SERM). It exhibits estrogen-agonistic effects on bones and lipid metabolism while having estrogen-antagonistic effects on uterine and breast tissues. This dual action helps in maintaining bone density and reducing the risk of vertebral fractures.

Indications for Use

Evista is primarily indicated for the treatment and prevention of osteoporosis in postmenopausal women. Additionally, it is indicated to reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis or those at high risk for invasive breast cancer.

Pharmacodynamics Details

Raloxifene binds to estrogen receptors, resulting in differential expression of multiple estrogen-regulated genes across various tissues. It reduces bone resorption and turnover, leading to an increase in bone mineral density. The medication also modifies lipid profiles by decreasing total and LDL cholesterol levels.

Pharmacokinetics Properties

After oral administration, raloxifene is rapidly absorbed. The drug undergoes extensive first-pass metabolism, with an absolute bioavailability of approximately 2%. It exhibits a half-life of approximately 27.7 hours due to enterohepatic recycling. Raloxifene is highly bound to plasma proteins, primarily albumin.

Mechanism of Action

Evista exerts its effects predominantly through selective modulation of estrogen receptors. By acting as an estrogen agonist on bone and lipids, it helps maintain bone mass and reduces the risk of vertebral fractures. Its antagonistic effects on uterine and breast tissue decrease estrogen stimulation, reducing the risk of cancer in estrogen-sensitive tissues.

Dosing and Administration

Evista is prescribed as one 60 mg tablet taken once daily by mouth. It can be administered with or without food. Consistency in timing of dosage each day ensures optimal therapeutic outcomes and assists in establishing a routine for the patient.

Storage Recommendations

Store Evista tablets at room temperature, between 68°F to 77°F (20°C to 25°C). The medication should be kept in a tightly closed container away from moisture and heat. Protect the tablets from light by keeping them in their original packaging.

Drug Interactions Overview

Evista may interact with various drugs affecting its metabolism. Concurrent use with cholestyramine significantly reduces raloxifene absorption. Caution should be exercised when combining with highly protein-bound drugs, as displacement interactions may occur. Raloxifene may also alter the effects of warfarin, requiring monitoring of INR levels.

Contraindications Specification

Evista is contraindicated in patients with active or past deep vein thrombosis, pulmonary embolism, or retinal vein thrombosis. It should not be used in women who are or may become pregnant. Not suitable for individuals with a known hypersensitivity to raloxifene.

Adverse Effects Potential

Common adverse effects include hot flashes, leg cramps, and peripheral edema. Less commonly, patients may experience flu-like symptoms, arthralgia, and sweating. Rare but severe side effects involve venous thromboembolism and retinal vein thrombosis, requiring immediate medical attention.

Therapeutic Monitoring Criteria

Patients on Evista should undergo regular bone mineral density measurements to assess efficacy in preventing osteoporosis. Lipid profiles may also be monitored as part of therapy. Regular checks for signs of venous thromboembolism are essential due to the increased risk associated with treatment.

Patient Counseling Information

Patients should be informed about the purpose of therapy and expected outcomes, including bone health improvement and breast cancer risk reduction. It’s essential to educate on signs of potential side effects, especially thromboembolic events. The importance of lifestyle modifications, including dietary calcium and vitamin D intake, should be emphasized alongside pharmacotherapy.

Clinical Studies References

Multiple clinical trials have established the efficacy of Evista in reducing vertebral fracture risk and its role in breast cancer risk mitigation. Studies show an increase in bone mineral density and favorable changes in lipid metabolism. Data suggest a generally safe profile with adherence to recommended guidelines.