Zoledronic acid


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Suy thận
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.
Hướng dẫn pha thuốc
Dilute the required amount in 100 mL of NaCl 0.9% or dextrose 5%.
Tương kỵ
Ca- or other divalent cation-containing infusion soln (e.g. lactated Ringer's soln).
Chống chỉ định
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.
Thận trọng
Patient w/ aspirin-sensitive asthma. Mild to moderate renal impairment. Pregnancy.
Tác dụng không mong muốn
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.
Thông tin tư vấn bệnh nhân
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.
Chỉ số theo dõi
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.
Quá liều
Symptoms: Renal impairment, hypocalcaemia, hypophosphatemia, hypomagnesaemia. Management: Admin IV Ca gluconate, K or Na phosphate, and Mg sulfate, respectively.
Tương tác
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.
Ảnh hưởng đến kết quả xét nghiệm
May interfere w/ diagnostic imaging agents (e.g. technetium-99m-diphosphonate) in bone scans.
Tác dụng
Description:
Mechanism of Action: 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.
Đặc tính

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)

Bảo quản
Store between 15-30°C. After opening, stable for 24 hr at 2-8°C. Allow refrigerated soln to reach room temp before admin.
Phân loại MIMS
Thuốc ảnh hưởng chuyển hóa xương / Trị liệu chăm sóc nâng đỡ
Phân loại ATC
M05BA08 - zoledronic acid ; Belongs to the class of bisphosphonates. Used in the treatment of bone diseases.
Tài liệu tham khảo
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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