Zoledronic acid
Last updated: October 29, 2014
Trade Names: Reclast
Drug Class: Bisphosphonate
Preparations: 5 mg in 100 mL i.v. preparation
Dose/Administration
Osteoporosis: for treatment 5 mg i.v. once a year; for prevention 5 mg i.v. every 2 years
Paget’s disease: 5 mg i.v., consider retreatment for relapse
Indications: Treatment and prevention of osteoporosis and glucocorticoid-induced osteoporosis; treatment of Paget’s disease, hypercalcemia of malignancy, multiple myeloma and metastases from solid tumors
Mechanism of Action: Antiresorptive; localizes to areas of bone resorption and inhibits osteoclast activity without any effect on bone formation; increases bone mineral density and significantly reduces fracture rates.
Contraindications: Hypersensitivity, hypocalcemia, not recommended for patients with severe renal insufficiency (creatinine clearance <35 mL/min)
Precautions: A dental exam and preventive dental work should be performed before starting chronic bisphosphonate therapy.
Pregnancy Risk: D
Adverse Effect
Common: 44% of patients have arthralgia, fever and flu-like symptoms in the first 3 days (can be reduced by administering acetaminophen for 3 days after the infusion), fatigue, headache, dizziness, edema, nausea, vomiting, diarrhea, hypocalcemia
Uncommon: Infusion reaction, atypical subtrochanteric femur fractures, osteonecrosis of the jaw, severe musculoskeletal pain, uveitis, altered taste, urticaria, angioedema, atrial fibrillation, rash, severe hypocalcemia
Drug Interactions: Do not use Reclast and Zometa together – they are the same drug – zoledronic acid
Patient Instructions: Supplement calcium and vitamin D intake if needed.
Comments: Supplemental calcium and vitamin D are co-administered, particularly if treating myeloma or Paget’s. IV bisphosphonates have a higher risk of osteonecrosis of the jaw. The optimal duration of treatment for osteoporosis is uncertain. A temporary discontinuation may be considered after 3-5 years of therapy in patients at low risk of fracture with monitoring of bone density 2-3 years after discontinuation.
Clinical Pharmacology: Renally excreted and not metabolized. Elimination from body over months or years indicating localization and slow release from bone.
Cost: $$$$
BIBLIOGRAPHY
McClung M, Harris ST, Miller PD et al. Bisphosphonate therapy for osteoporosis: benefits, risks and drug holiday. Am J Med 2013;126:13-20.PMID: 23177553
Lyles KW, Colón-Emeric CS, Magaziner JS, et al.Zoledronic acid and clinical fractures and mortality after hip fracture. N Engl J Med 2007;357:1799-809. PMID: 17878149.
