Zoledronic Acid

Indications
 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 wk 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 wk, in conjunction with 500 mg calcium and 400 IU vitamin D oral supplement.
CrCl (ml/min)Dosage Recommendation
50-603.5 mg every 3-4 wk
40-493.3 mg every 3-4 wk
30-393 mg every 3-4 wk
<30Not recommended.

Intravenous
Osteolytic lesions associated with multiple myeloma
Adult: 4 mg infusion over at least 15 minutes every 3-4 wk, in conjunction with 500 mg calcium and 400 IU vitamin D oral supplement.
CrCl (ml/min)Dosage Recommendation
50-603.5 mg every 3-4 wk
40-493.3 mg every 3-4 wk
30-393 mg every 3-4 wk
<30Not 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 wk following zoledronic acid admin.
CrCl (ml/min)Dosage Recommendation
<40Not 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
<40Not 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.
Contraindications
 Pregnancy; lactation; children.
Warnings / 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 mth and avoid invasive dental procedures while on treatment.
Adverse Reactions
 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.
Drug Interactions
 Increased risk of hypocalcaemia with aminoglycosides and loop diuretics. Increased risk renal dysfunction with nephrotoxic agents.
See Below for More zoledronic acid Drug Interactions
Mechanism of Actions
 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.
Storage Conditions
 Intravenous: Store at 15-30°C(59-86°F).
ATC Classification
 M05BA08 - zoledronic acid ; Belongs to the class of bisphosphonates. Used in the treatment of bone diseases.
Storage
 Intravenous: Store at 15-30°C(59-86°F).
Available As
  • Zoledronic Acid 4 mg

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