Zoledronic acid


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Hypercalcaemia of malignancy 4 mg as a single infusion, may repeat if necessary after at least 7 days. Bone metastases associated w/ solid tumours; Osteolytic lesions associated w/ multiple myeloma 4 mg by infusion 3-4 wkly. Paget's disease of bone 5 mg as a single infusion. Osteoporosis in postmenopausal women; Increase bone mass in men w/ osteoporosis; Corticosteroid-induced osteoporosis 5 mg as a single infusion once yrly. Prophylaxis of postmenopausal osteoporosis 5 mg as a single infusion once every 2 yr.
Dosage Details
Intravenous
Hypercalcaemia of malignancy
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.
IV/Parenteral: D
Patient Counseling Information
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.
MonitoringParameters
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

Chemical Structure Image
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.
ATC Classification
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.

Disclaimer: This information is independently developed by MIMS based on Zoledronic acid from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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