Adult: 4 mg as a single infusion over at least 15 min. Re-treatment: 4 mg after at least 7 days if necessary. Co-admin oral Ca 500 mg and vit D 400 IU daily.
Intravenous Bone metastases associated with solid tumours, Osteolytic lesions associated with multiple myeloma
Adult: 4 mg by infusion over at least 15 min 3-4 wkly. Co-admin oral Ca 500 mg and vit D 400 IU daily.
Intravenous Corticosteroid-induced osteoporosis, Increase bone mass in men with osteoporosis, Osteoporosis in postmenopausal women
Adult: 5 mg as a single infusion over at least 15 min, once yrly, w/ adequate Ca and vit D intake. Patients w/ low-trauma hip fracture: Start 2 or more wk after hip fracture repair w/ a loading dose of vit D 50,000-125,000 IU given orally or by IM route prior to 1st infusion.
Intravenous Paget's disease of bone
Adult: 5 mg as a single infusion over 15 min. Patients should receive elemental Ca 1,500 mg and vit D 800 IU daily particularly w/in 2 wk after admin. Patients who have relapsed: May be given an additional infusion of 5 mg after an interval of at least 1 yr from the initial dose.
Intravenous Prophylaxis of postmenopausal osteoporosis
Adult: 5 mg as a single infusion once every 2 yr.
Renal Impairment
Bone metastases associated w/ solid tumours, Osteolytic lesions associated with multiple myeloma:
CrCl (mL/min)
Dosage
<30
Not recommended.
30-39
3 mg 3-4 wkly.
40-49
3.3 mg 3-4 wkly.
50-60
3.5 mg 3-4 wkly.
Hypercalcaemia of malignancy: Serum creatinine >400 μmol/L or >4.5 mg/dL: Evaluate risk versus benefit. Osteoporosis in postmenopausal women, Increase bone mass in men with osteoporosis, Corticosteroid-induced osteoporosis, Paget's disease of bone, Prophylaxis of postmenopausal osteoporosis:
CrCl (mL/min)
Dosage
<35
Contraindicated.
Reconstitution
Dilute the required amount in 100 mL of NaCl 0.9% or dextrose 5%.
Incompatibility
Ca- or other divalent cation-containing infusion soln (e.g. lactated Ringer's soln).
Contraindications
Hypocalcaemia, severe renal impairment (CrCl <35 mL/min) and those w/ evidence of acute renal impairment due to an increased risk of renal failure. Lactation.
Special Precautions
Patient w/ aspirin-sensitive asthma. Mild to moderate renal impairment. Pregnancy.
Adverse Reactions
Arthralgia, fever, flu-like symptoms, myalgia, headache, pain in extremity, nausea, vomiting, diarrhoea, eye inflammation; alopecia, hyperhidrosis, bone/joint/muscle pain, osteonecrosis of the jaw, femoral fracture, hypersensitivity reactions (e.g. urticaria, angioedema), Stevens-Johnson syndrome, toxic epidermal necrolysis, hypotension. Potentially Fatal: Severe hypocalcaemia, severe kidney problems.
This drug may cause dizziness, if affected, do not drive or operate machinery. Adequately hydrate patients prior to admin. Ensure adequate Ca and vit D intake.
Monitoring Parameters
Monitor serum Ca, Mg, phosphate and electrolytes; haematocrit/Hb (oncology use); biochemical markers of bone turnover (non-oncology use). Prior to therapy, perform dental exam and preventive dentistry in patients at risk of osteonecrosis.
Overdosage
Symptoms: Renal impairment, hypocalcaemia, hypophosphatemia, hypomagnesaemia. Management: Admin IV Ca gluconate, K or Na phosphate, and Mg sulfate, respectively.
Drug Interactions
Increased exposure of concomitant drugs eliminated by renal excretion (e.g. digoxin). Increased risk of hypocalcaemia w/ loop diuretics. Lowered serum Ca concentrations for prolonged periods w/ aminoglycosides. Increased risk of renal dysfunction w/ nephrotoxic agents.
Lab Interference
May interfere w/ diagnostic imaging agents (e.g. technetium-99m-diphosphonate) in bone scans.
Action
Description: Zoledronic acid inhibits osteoclast activity and skeletal Ca release induced by tumours. It decreases serum Ca and phosphorus, and increases their elimination. In osteoporosis, it inhibits osteoclast-mediated resorption, thus reducing bone turnover. Pharmacokinetics: Distribution: Plasma protein binding: 28-56%. Metabolism: Not metabolised. Excretion: Via urine (approx 23-55% of the dose) as unchanged drug. Terminal elimination half-life: Approx 146 hr.
Chemical Structure
Zoledronic acid Source: National Center for Biotechnology Information. PubChem Database. Zoledronic acid, CID=68740, https://pubchem.ncbi.nlm.nih.gov/compound/Zoledronic-acid (accessed on Jan. 24, 2020)
Storage
Store between 15-30°C. After opening, stable for 24 hr at 2-8°C. Allow refrigerated soln to reach room temp before admin.
M05BA08 - zoledronic acid ; Belongs to the class of bisphosphonates. Used in the treatment of bone diseases.
References
Anon. Zoledronic acid. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/09/2015.Buckingham R (ed). Zoledronate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/09/2015.McEvoy GK, Snow EK, Miller J et al (eds). Zoledronic Acid. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/09/2015.Zoledronic Acid Injection, Solution (Dr. Reddy’s Laboratories Ltd). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/09/2015.Zoledronic Acid Injection, Solution Concentrate (Actavis Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/09/2015.
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