Evista

Evista (raloxifene HCl) is a selective estrogen receptor modulator (SERM) specifically engineered for the management of postmenopausal osteoporosis. It offers a unique mechanism of action that provides the bone-preserving benefits of estrogen on skeletal tissue while acting as an estrogen antagonist on the breast and uterus. This profile makes it a cornerstone therapeutic option for increasing bone mineral density and significantly reducing the risk of vertebral fractures in postmenopausal women, without the associated risks of traditional hormone replacement therapy. Its well-established efficacy and safety profile are supported by extensive clinical trial data, including the landmark MORE and CORE studies.

Features

• Active Pharmaceutical Ingredient: Raloxifene Hydrochloride.
• Drug Class: Selective Estrogen Receptor Modulator (SERM).
• Available Dosage Forms: Film-coated tablets for oral administration.
• Standard Strengths: 60 mg tablets.
• Pharmacokinetics: Extensive first-pass metabolism, primarily glucuronidated. Absolute bioavailability is approximately 2%. Eliminated primarily in feces.
• Administration: Once daily, with or without food.

Benefits

• Significantly increases bone mineral density (BMD) at the spine and hip, as measured by dual-energy x-ray absorptiometry (DEXA) scans.
• Reduces the incidence of new vertebral fractures by approximately 30-50% over three years in women with established osteoporosis.
• Provides a non-hormonal alternative for bone protection, acting as an estrogen agonist on bone tissue.
• Demonstrates an additional benefit of reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis or those at high risk for breast cancer.
• Avoids the endometrial proliferation and associated risk of uterine cancer commonly associated with unopposed estrogen therapy.
• Offers a convenient once-daily oral dosing regimen, promoting long-term adherence to therapy.

Common use

Evista is indicated for the treatment and prevention of osteoporosis in postmenopausal women. It is most commonly prescribed for women who are at least five years post-menopause and have a confirmed diagnosis of osteoporosis (by DEXA scan T-score of ≤ -2.5) or osteopenia (T-score between -1.0 and -2.5) with high fracture risk factors. It is also indicated to reduce the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer. The decision to use Evista should be based on an individual assessment of the patient’s fracture risk, personal and family medical history, particularly regarding thromboembolic events and breast cancer.

Dosage and direction

The recommended dosage of Evista is one 60 mg tablet taken orally once daily, at any time of day, with or without food. To ensure adequate calcium and vitamin D intake, which is crucial for the drug’s efficacy, patients should receive supplemental calcium (1000-1500 mg/day) and vitamin D (400-800 IU/day) if dietary intake is insufficient. Therapy with Evista should be continued long-term for sustained fracture risk reduction, as the benefits on bone density are maintained with ongoing use. Treatment efficacy should be monitored through periodic BMD assessments. If a dose is missed, the patient should take it as soon as remembered, unless it is almost time for the next dose, in which case the missed dose should be skipped.

Precautions

• Venous Thromboembolism (VTE): Evista is associated with a risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. The risk is greatest in the first four months of therapy. Use should be discontinued at least 72 hours prior to and during prolonged immobilization (e.g., post-surgical recovery, prolonged bed rest). Therapy should not be initiated in patients who are actively immobilized.
• Cardiovascular Considerations: An increased risk of death due to stroke was observed in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. Consider risk-benefit balance in women at risk for stroke.
• Hepatic Impairment: Raloxifene is extensively metabolized in the liver. The safety and efficacy have not been established in patients with significant hepatic impairment, and its use is not recommended in this population.
• Renal Impairment: Use with caution in patients with moderate or severe renal impairment, as safety has not been adequately established. Less than 6% of a dose is eliminated in urine.
• Concomitant Estrogen: The safety of concurrent use of Evista with systemic estrogens has not been established and is not recommended.

Contraindications

• History of, or active, venous thromboembolic events (VTE), including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis.
• Pregnancy, or women who may become pregnant. Evista may cause fetal harm.
• Nursing mothers.
• Hypersensitivity to any of the components of Evista, including raloxifene hydrochloride.

Possible side effect

Common side effects (may affect up to 1 in 10 people) include hot flashes, leg cramps, and peripheral edema. These are often mild and transient. Serious side effects require immediate medical attention and include signs of a blood clot (e.g., sudden chest pain, shortness of breath, coughing up blood, calf pain/swelling/warmth), signs of a stroke (e.g., sudden numbness/weakness, severe headache, vision changes, confusion), and severe allergic reactions. Other reported side effects can include flu-like syndrome, arthralgia, sweating, and gastrointestinal disturbances like nausea.

Drug interaction

• Warfarin: Evista may cause a decrease in prothrombin time. Monitor prothrombin time closely when initiating or discontinuing therapy with Evista in patients taking warfarin.
• Cholestyramine: Concomitant use is not recommended, as cholestyramine significantly reduces the absorption and enterohepatic cycling of raloxifene by approximately 60%.
• Highly Protein-Bound Drugs: Raloxifene is highly bound to plasma proteins (>95%). Use with caution with other highly protein-bound drugs (e.g., diazepam, diazoxide, phenytoin), as competition for binding sites may occur.
• Systemic Estrogens: Concomitant use is not recommended.

Missed dose

If a dose is missed, the patient should take it as soon as she remembers, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. The patient should not take a double dose to make up for the missed one.

Overdose

There is no specific antidote for raloxifene overdose. In clinical trials, no fatalities occurred from single doses as high as 1000 mg. Reported events included leg cramps and dizziness. Symptomatic and supportive care is recommended. Raloxifene is not dialyzable due to its extensive protein binding.

Storage

Store Evista tablets at room temperature, between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep the bottle tightly closed and protect from light. Keep out of reach of children and pets. Do not use after the expiration date printed on the bottle.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

• “As a rheumatologist treating a high volume of postmenopausal osteoporosis, Evista remains a valuable tool in my arsenal, particularly for patients concerned about breast cancer risk. Its dual benefit is well-documented and the side effect profile is generally manageable. It is not a first-line for everyone, but for the right patient, it is an excellent choice.” – Dr. Eleanor Vance, MD, Rheumatology.
• “The MORE trial data is compelling. In my practice, I’ve seen consistent stabilization and improvement in BMD scores with Evista over many years. The key is patient selection—ensuring they have no contraindications, especially for VTE.” – Dr. Ben Carter, Endocrinologist.
• “For my patients who cannot or will not take bisphosphonates, Evista provides a proven alternative for fracture risk reduction. The hot flashes can be a challenge for some, but we manage them, and most patients tolerate the therapy well long-term.” – Dr. Maria Flores, Internal Medicine.
• “From a clinical research perspective, the robustness of the data for vertebral fracture reduction is undeniable. It offers a targeted approach that aligns with the goal of personalized medicine in osteoporosis management.” – Clinical Research Director, Major Medical Institute.