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Zoledronic Acid information from DrugsUpdate  

1
See Available Brands of Zoledronic Acid in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

Zoledronic acid or zoledronate (marketed by Novartis under the trade names Zometa, Zomera, Aclasta and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer, as well as for treating osteoporosis. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of zoledronic acid may also prevent recurring fractures in patients with a previous hip fracture.
Reclast is a single 5 mg infusion for the treatment of Paget's disease of bone.

Pharmacodynamics

Pharmacokinetics

Zoledronic acid, an aminobiphosphonate, is a potent inhibitor of bone resorption. It inhibits osteoclastic activity and skeletal calcium release caused by tumours.

Distribution
Protein binding: Low (22-56%)

Metabolism
Not metabolised.

Excretion
Excreted unchanged in urine (23-55%), the rest sequestered to bone and eliminated very slowly.

Zoledronic Acid Indications / Zoledronic Acid Uses

Information Not Available

Zoledronic Acid Adverse Reactions / Zoledronic Acid Side Effects

Electrolyte disturbances (e.g. hypocalcaemia); GI disturbances; dizziness; hypersensitivity reactions; blood disorders e.g. anaemia; weight loss; dyspnoea; iritis; uveitis; conjunctivitis; influenza-like symptoms; myalgia; arthralgia; fever; rigors; renal impairment; taste disturbance; dry mouth; stomatitis; chest pain; cough; CNS effects; pruritus; rash; sweating; asthenia; peripheral oedema; hypertension; bradycardia.

Precautions

Monitor
Assess serum creatinine before each treatment with zoledronic acid. Monitor serum calcium, phosphorous, magnesium, electrolytes, and renal function.

Special Precautions

Cardiac disease (avoid fluid overload). Renal impairment. Monitor serum electrolytes, calcium, phosphate and magnesium. Assess renal function before each dose. Withhold treatment if there is worsening of renal function (increase of 44 micromoles/l in patients with normal baseline creatinine or increase in 88 micromoles/l in those with abnormal baseline creatinine); restart treatment at precious dose when creatinine return to within 10% of baseline. Ensure adequate hydration throughout therapy and maintain urinary output of 2 L/day. Increased risk of renal impairment with small infusion volume and rapid infusion. Increased risk of bronchoconstriction in aspirin-sensitive patients. Consider dental examination with appropriate corrective action before initiating treatment in patients at risk of osteomyelitis and osteonecrosis of the jaws (e.g. infection, anaemia, pre-existing viral disease, trauma, coagulation disorders). Hard and soft tissue oral assessment to be carried out every 3-4 months and avoid invasive dental procedures while on treatment.

Other Drug Interactions

Increased risk of hypocalcaemia with aminoglycosides and loop diuretics. Increased risk renal dysfunction with nephrotoxic agents.

Other Interactions

Information Not Available

Dosage

Intravenous
Hypercalcaemia of malignancy
Adult: 4 mg as a single dose by infusion over at least 15 minutes. Retreatment in patients who relapse or who are refractory to initial treatment: 4 mg as an infusion over at least 15 minutes, after at least 1 week from initial dose.
Renal impairment: Serum creatinine >400 micromol/L: Avoid.

Intravenous
Bone metastases associated with solid tumours
Adult: 4 mg infusion over at least 15 minutes every 3-4 weeks, in conjunction with 500 mg calcium and 400 IU vitamin D oral supplement.
CrCl (ml/min)    Dosage Recommendation
50-60               3.5 mg every 3-4 weeks
40-49               3.3 mg every 3-4 weeks
30-39               3 mg every 3-4 weeks
<30                  Not recommended.

Intravenous
Osteolytic lesions associated with multiple myeloma
Adult: 4 mg infusion over at least 15 minutes every 3-4 weeks, in conjunction with 500 mg calcium and 400 IU vitamin D oral supplement.
CrCl (ml/min)    Dosage Recommendation
50-60               3.5 mg every 3-4 weeks
40-49               3.3 mg every 3-4 weeks
30-39               3 mg every 3-4 weeks
<30                  Not recommended.

Intravenous
Paget's disease of bone
Adult: Single 5 mg IV infusion over 15 minutes, in conjunction with 1500 mg elemental calcium daily in divided doses and 800 IU vitamin D daily, especially in the 2 weeks following zoledronic acid admin.
CrCl (ml/min)    Dosage Recommendation
<40                  Not recommended.

Intravenous
Osteoporosis in postmenopausal women
Adult: Single 5 mg IV infusion over at least 15 minutes, once a year.
CrCl (ml/min)    Dosage Recommendation
<40                  Not recommended.


Reconstitution
Dilute the required amount in 100 ml of 0.9% sodium chloride or 5% dextrose.

Incompatibility
Incompatible with calcium containing solutions (e.g. lactated Ringer's solution) and other divalent cation containing solutions.

Food(before/after)

Information Not Available

List of Contraindications

Zoledronic Acid and Pregnancy

Contraindicated in pregnancy

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Zoledronic Acid and Lactation

Contraindicated in lactation

Zoledronic Acid and Children

Safety and efficacy not established

Zoledronic Acid and Geriatic

Because decreased renal function occurs more commonly in elderly patients, take special care to monitor renal function.

Zoledronic Acid and Other Contraindications

Pregnancy; lactation; children.

Storage

Intravenous
Store at 15-30°C(59-86°F).

Lab interference

Intravenous
Store at 15-30°C(59-86°F).

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