Trade Names:Reclast- Injection, solution 5 mg per 100 mL
Trade Names:Zometa- Injection, solution, concentrate 4 mg per 5 mLAclasta (Canada)
Inhibition of osteoclastic bone resorption.
In vitro protein binding ranges from 28% to 53%.
Does not undergo biotransformation.
Excreted unchanged by the kidney (less than 3% in feces). The 0- to 24-h renal Cl is about 3.7 L/h. The half-life is 146 h.
Mild renal function impairment increased AUC by an average of 15%. Moderate renal function impairment increased AUC by an average of 43%. The risk of renal deterioration appears to increase with AUC, which doubled at a CrCl of 10 mL/min.Hepatic Function Impairment
No pharmacokinetic studies have been conducted.
Treatment of osteoporosis in postmenopausal women; treatment to increase bone mass in men with osteoporosis; treatment of Paget disease of bone in men and women.Zometa
Treatment of hypercalcemia of malignancy; treatment of patients with multiple myeloma and bone metastases from solid tumors in conjunction with standard antineoplastic therapy.
Hypersensitivity to zoledronic acid or any component of the product; hypocalcemia.
IV 4 mg max dose given as single infusion over no less than 15 min. Retreatment with 4 mg may be considered if serum calcium does not return to normal or does not remain normal after initial treatment. To allow a full response, it is recommended that a minimum of 7 days elapse before retreatment.Multiple Myeloma and Metastatic Bone Lesions From Solid TumorsAdults
IV 4 mg max dose infused over no less than 15 min every 3 to 4 wk in patients with CrCl more than 60 mL/min. Reduce dose in patients with renal function impairment as follows: CrCl 50 to 60 mL/min: 3.5 mg/dose; CrCl 40 to 49 mL/min: 3.3 mg/dose; CrCl 30 to 39 mL/min: 3 mg/dose.Paget DiseaseAdults
IV 5 mg at a constant infusion rate over no less than 15 min. Retreatment may be considered in patients who have relapsed, based on increases in serum alkaline phosphatase, in patients who failed to achieve normalization of their serum alkaline phosphatase, or in those with symptoms, as dictated by medical practice. All patients with Paget disease should receive elemental calcium 750 mg twice daily or 500 mg 3 times daily and vitamin D 800 units daily, particularly in the 2 wk following Reclast administration.Postmenopausal Osteoporosis, Osteoporosis in MenAdults
IV 5 mg infusion once a year given over no less than 15 minutes. If dietary intake is insufficient, supplement with calcium 1,200 mg daily and vitamin D 800 to 1,000 units daily.
Store unopened vials at room temperature (59° to 86°F). If not used immediately, Zometa diluted solution for infusion may be stored in refrigerator (36° to 46°F) and then equilibrated to room temperature before administration. Total time between dilution, storage in refrigerator, and end of administration must not exceed 24 h. After opening, Reclast is stable for 24 h at 36° to 46°F. If refrigerated, allow solution to reach room temperature before administration.
Increased risk of hypocalcemia. Avoid loop diuretics until patient is rehydrated.Nephrotoxic drugs (eg, NSAIDs)
Increased risk of nephrotoxicity; use with caution.Thalidomide
Increased risk of renal function impairment.
None well documented.
Hypertension (13%); hypotension (11%); atrial fibrillation, palpitations (3%); bradycardia (postmarketing).
Fatigue (39%); pyrexia (32%); weakness (24%); headache (19%); dizziness (18%); insomnia (16%); paresthesia (15%); anxiety, depression (14%); agitation, confusion (13%); hypoesthesia (12%); somnolence (less than 10%); malaise (7%); lethargy (5%); hyperesthesia, taste disturbance, tremor (postmarketing).
Alopecia (12%); dermatitis (11%); hyperhidrosis, rash (3%); urticaria (postmarketing).
Sore throat (8%); vertigo (4%); eye pain (2%); blurred vision, episclerosis, scleritis, uveitis (postmarketing).
Nausea (46%); vomiting (32%); constipation (31%); diarrhea (24%); abdominal pain (16%); dyspepsia (10%); dysphagia (less than 10%); stomatitis (8%); upper abdominal pain (5%); abdominal distension (2%); dry mouth (postmarketing).
UTI (14%); hematuria, proteinuria, renal deterioration progressing to renal failure and dialysis (postmarketing).
Anemia (33%); neutropenia (12%); thrombocytopenia (10%); granulocytopenia, pancytopenia (less than 10%).
Anaphylactic reaction/shock, angioedema, hypersensitivity reaction (postmarketing).
Hypophosphatemia (13%); hypokalemia (12%); hypomagnesemia (11%); hypocalcemia (less than 10%); increased blood creatinine (2%); hyperkalemia, hypernatremia (postmarketing).
Local-site reactions (3%).
Anorexia (22%); decreased weight (16%); dehydration (14%); decreased appetite (13%); musculoskeletal stiffness (5%); weight increase (postmarketing).
Bone pain (55%); arthralgia (24%); myalgia (23%); back pain (15%); limb pain (14%); musculoskeletal pain, skeletal pain (12%); pain in extremity, rigors (11%); shoulder pain (7%); musculoskeletal stiffness (5%); muscle spasm, neck pain (4%); incapacitating bone, joint, and/or muscle pain, muscle cramps, osteonecrosis primarily of the jaw (postmarketing).
Dyspnea (27%); cough (22%); upper respiratory tract infection (10%); bronchoconstriction (postmarketing).
Fever (44%); acute phase reaction (25%); lower limb edema (21%); malignant neoplasm aggravated (20%); progression of cancer (16%); moniliasis, pain (12%); influenza-like illness (11%); chills (10%); asthenia, chest pain, leg edema, mucositis, nonspecific infection (less than 10%); influenza (7%); peripheral edema (6%); increased C-reactive protein (5%); hyperthermia (2%).
Assess serum creatinine before each treatment with zoledronic acid. Monitor serum calcium, phosphorous, magnesium, electrolytes, and renal function.
Category D .
Safety and efficacy not established.
Because decreased renal function occurs more commonly in elderly patients, take special care to monitor renal function.
Has been reported following administration of zoledronic acid, especially in patients with preexisting renal compromise or additional risk factors. Reclast is not recommended in patients with severe renal function impairment (CrCl less than 35 mL/min). Zometa treatment is not recommended in patients with bone metastases with severe renal function impairment.
No clinical data available.
Use with caution in patients with aspirin-sensitive asthma.
Because hypocalcemia may occur, preexisting hypocalcemia must be treated by adequate calcium and vitamin D before initiating therapy.
Severe and occasionally incapacitating bone, joint, and/or muscle pain, starting 1 day to several months after starting therapy, has been reported in patients taking bisphosphonates. Symptoms usually resolve following discontinuation of therapy and may recur with rechallenge with the same or different bisphosphonate.
Has been reported in patients receiving treatment regimens that include bisphosphonates. Risk factors include cancer chemotherapy, corticosteroid administration, and dental procedures. Consider a dental examination with appropriate preventive dentistry prior to treatment with zoledronic acid in patients with concomitant risk factors.
Hypocalcemia, hypomagnesemia, hypophosphatemia, renal function impairment.
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