Zoledronic acid

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[edit] BRAND NAMES

[edit] STRUCTURE

Zoledronic acid.jpg

[edit] MECHANISM OF ACTION

Osteoporosis happens when not enough new bone grows to replace the bone that is naturally broken down. Gradually, the bones become thin and fragile, and more likely to break. Osteoporosis is more common in women after the menopause, when the levels of the female hormone estrogen fall, since estrogen helps to keep bones healthy. Approximately 40% of 50-year-old women will experience an osteoporosis-related fracture during their remaining lifetimes.

Osteoblasts make bone, while osteoclasts resorb or take away bone. Zoledronate is a bisphosphonate, it has no direct effect on bone formation, but it stops the action of the osteoclasts, the cells that are involved in breaking down the bone tissue.
Zoledronate is internalized by osteoclasts, causing disruption of osteoclast cytoskeleton, loss of the ruffled border, and the subsequent loss of ability to resorb bone.

In postmenopausal women, Zoledronate reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

By preventing fractures Zoledronate is useful also in cancer patients with bone metastases. Patients with tumours can have high levels of calcium in their blood, released from the bones, Zoledronate helps to reduce hypercalcemia as well.

[edit] INDICATIONS

  • Treatment and prevention of postmenopausal osteoporosis
  • Treatment to increase bone mass in men with osteoporosis
  • Treatment and prevention of glucocorticoid-induced osteoporosis
  • Treatment of Paget’s disease of bone in men and women
  • To reduce hypercalcemia in tumor-induced bone disease
  • Patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy.

[edit] DOSAGE

Zoledronate is given by intravenous infusion lasting at least 15 minutes.

  • Treatment of postmenopausal osteoporosis: 5 mg once a year (Aclasta, Reclast)
  • Prevention of postmenopausal osteoporosis: 5 mg once every 2 years (Aclasta, Reclast)
  • Treatment to increase bone mass in men with osteoporosis: 5 mg once a year (Aclasta, Reclast)
  • Treatment and prevention of glucocorticoid-induced osteoporosis: 5 mg once a year (Aclasta, Reclast)
  • Treatment of Paget’s disease of bone in men and women: a single 5 mg infusion. Patients should receive 1500 mg elemental calcium and 800 international units vitamin D daily (Aclasta, Reclast)
  • To reduce hypercalcemia in tumor-induced bone disease: a single 4 mg infusion and 4 mg as retreatment after a minimum of 7 days (Zometa)
  • Multiple myeloma and bone metastasis from solid tumors: a single 4 mg infusion every 3-4 weeks. An oral calcium supplements of 500 mg and a multiple vitamin containing 400 IU of Vitamin D should be co-administered daily (Zometa)

[edit] DOSAGE FORMS AND STRENGTHS

  • Zometa: 4 mg/100 mL single-use ready-to-use bottle
  • Zometa: 4 mg/5 mL single-use vial of concentrate
  • Reclast and Aclasta: 5 mg in a 100 mL ready-to-infuse solution

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Zoledronic acid
  • Hypocalcemia

[edit] WARNINGS AND PRECAUTIONS

  • Hypocalcemia may worsen during treatment. Patients must be adequately supplemented with calcium and vitamin D
  • Bisphosphonates may cause osteonecrosis of of the jaw. Potential predisposing factors are tooth extractions, poor oral hygiene, corticosteroids use, alcohol abuse, chemotherapy and radiotherapy.
  • Atypical Femur Fractures have been reported. Patients should be advised to report any thigh or groin pain to rule out an incomplete femur fracture.
  • Severe bone, joint, muscle pain may occur. Discontinue use if severe symptoms develop

[edit] INTERACTIONS

  • Loop diuretics like Furosemide may increase risk of hypocalcemia

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). Zoledronate SHOULD NOT BE USED DURING PREGNANCY. If the patient becomes pregnant while taking this drug, the patient should be apprised of the potential harm to the fetus. Women of childbearing potential should be advised to avoid becoming pregnant while receiving
  • Nursing Mothers: It is not known whether zoledronate is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Zoledronate binds to bone long term and may be released over weeks to years.

[edit] SIDE EFFECTS

Side effects can include fever, flu-like symptoms, headache, bone pain, arthralgia, myalgia, fever, fatigue, anemia, nausea and vomiting these symptoms were mild to moderate and usually resolved within a few days.

[edit] RELATED LINKS

How osteoporosis develops

[edit] BIBLIOGRAPHY

[edit] REFERENCES