Classes
DEA Class; Rx
Common Brand Names; Reclast, Zometa
- Calcium Metabolism Modifiers;
- Bisphosphonate Derivatives
Description
Potent third-generation intravenous bisphosphonate; carefully select product based on indication for use
Used for hypercalcemia of malignancy and bone metastases (e.g., Zometa); given as a single dose for Paget’s disease (e.g., Reclast)
Given once-yearly for osteoporosis and corticosteroid-induced osteoporosis and prevention in both men and women, and every 2 years for osteoporosis prophylaxis in postmenopausal women (e.g., Reclast)
Indications
Contraindications
Pregnancy
All indications: Hypersensitivity, including rare cases of urticaria, angioedema, and anaphylactic reaction or shock
Nononcologic uses: Hypocalcemia, severe renal impairment (CrCl <35 mL/min or evidence of acute renal impairment)
Adverse Effects
- Bone pain (55%)
- Nausea (29-46%)
- Fever (32-44%)
- Fatigue (39%)
- Anemia (22-33%)
- Vomiting (14-32%)
- Constipation (27-31%)
- Dyspnea (22-27%)
- Diarrhea (17-24%)
- Anorexia (9-22%)
- Arthralgia (5-21%)
- Headache (5-19%)
- Dizziness (18%)
- Insomnia (15-16%)
- Urinary tract infection (UTI; 12-14%)
- Anxiety (11-14%)
- Hypophosphatemia (5-14%)
- Hypokalemia (12%)
- Hypotension (11%)
- Hypomagnesemia (11%)
- Rash (11%)
Warnings
Assess renal function before and after treatment; if renal function is decreased after treatment, withhold additional treatment until it returns to within 10% of baseline
Before each Reclast dose, calculate CrCl on basis of actual body weight, using Cockcroft-Gault formula
Other risks for renal impairment include coadministration of zoledronic acid with nephrotoxic or diuretic medications, severe dehydration before or after zoledronic acid administration, and advanced age
Previous renal insufficiency (serum creatinine >3 mg/dL [265 mmol/L]), hepatic insufficiency, musculoskeletal pain
Infuse over ≥15 minutes; faster infusion increases renal toxicity
May cause significant risk of hypocalcemia (seizures, tetany, and numbness); hypocalcemia must be corrected before initiation of therapy; adequately supplement patients with calcium and vitamin D; monitor serum calcium closely with concomitant administration of other drugs known to cause hypocalcemia to avoid severe or life-threatening hypocalcemia
Use with caution in aspirin-sensitive asthma; may cause bronchoconstriction
Increased risk of osteonecrosis of jaw (advise patients against dental work); reported predominantly in cancer patients treated with IV bisphosphonates, including zoledronic acid; many patients were also receiving chemotherapy and corticosteroids which may be risk factors; risk may increase with duration of exposure to bisphosphonates; perform preventive dental exams before initiating therapy; avoid invasive dental procedures; monitor diabetic patients carefully
Cases of osteonecrosis (primarily involving the jaw but also of other anatomical sites including hip, femur and external auditory canal) reported predominantly in cancer patients
Risk of osteonecrosis of the jaw may increase with duration of exposure to bisphosphonates
Possible increased risk for atypical subtrochanteric and diaphyseal femur fractures; consider periodic reevaluation of need for continued bisphosphonate therapy, particularly if treatment lasts >5 years
If patients are receiving Zometa, they should not receive Reclast
Severe bone, joint, and muscle pain may occur; withhold future doses of zoledronic acid if severe symptoms occur
Pregnancy and Lactation
There are no available data in pregnant women to inform the drug-associated risk
Not known whether drug is present in human milk, or whether it affects milk production, or breastfed child; drug binds to bone long term and may be released over weeks to years
Maximum Dosage
4 mg/dose IV for hypercalcemia/oncology indications; 5 mg/dose IV for Paget’s disease/osteoporosis.
4 mg/dose IV for hypercalcemia/oncology indications; 5 mg/dose IV for Paget’s disease/osteoporosis.
Safety and efficacy have not been established; however, 5 mg IV once yearly or doses up to 0.1 mg/kg/cycle IV every 4 to 6 months have been used off-label for osteogenesis imperfecta.
3 to 12 years: Safety and efficacy have not been established; however, 5 mg IV once yearly or doses up to 0.1 mg/kg/cycle IV every 4 to 6 months have been used off-label for osteogenesis imperfecta.
2 years: Safety and efficacy have not been established; however, 5 mg IV once yearly or doses up to 0.05 mg/kg/cycle IV every 3 months or 0.1 mg/kg/cycle IV every 6 months have been used off-label for osteogenesis imperfecta.
1 year: Safety and efficacy have not been established; however, doses up to 0.05 mg/kg/cycle IV every 3 months or 0.1 mg/kg/cycle IV every 6 months have been used off-label for osteogenesis imperfecta.
Safety and efficacy have not been established; however, doses up to 0.05 mg/kg/cycle IV every 3 months or 0.1 mg/kg/cycle IV every 6 months have been used off-label for osteogenesis imperfecta.
Safety and efficacy have not been established.
How supplied
Zoledronic acid
IV injectable solution
- 4mg/5mL (5mL)
- 5mg/100mL
