Zoledron 100 ml Solution for Infusion: Each vial with 100 ml of Solution contains 5 mg Zoledronic Acid INN equivalent to 5.331 mg Zoledronic Acid Monohydrate.
Pharmacology:
The active ingredient in Zoledron is Zoledronic Acid, which belongs to a group of medicines called bisphosphonates. It is an inhibitor of osteoclast mediated bone resorption. The action of bisphosphonates on bone is based on their high affinity for mineralized bone. Intravenously administered Zoledronic Acid is rapidly distributed to bone. Zoledronic Acid is not metabolized and is excreted unchanged via the kidney.
Osteoporosis: Osteoporosis is a disease which causes bones to become less dense, gradually making them weaker, more brittle and likely to break. This is common in women after menopause, when a woman s ovaries stop producing the female hormone, oestrogen, which keeps bones healthy. Osteoporosis also occurs in men and women with increasing age. Broken bones may result from injury or simple falls. Breaks may occur during normal everyday activity such as lifting or from minor injury that would not ordinarily fracture normal bone. Fractures in people with osteoporosis usually occur at the hip, spine or wrist. These can lead not only to pain but also to considerable deformity and disability such as stooped posture from curvature of the spine and loss of mobility.
How does it work: Zoledronic Acid works by slowing down bone resorption, which allows the bone-forming cells time to rebuild normal bone. This is achieved by slowing down bone resorption and protects the bones from being weakened.
Preparation: Zoledronic Acid is a single intravenous infusion of 5 mg Zoledronic Acid administered once a year. Adequate supplemental Calcium and Vitamin-D intake is important in women with osteoporosis if dietary intake is inadequate.
Prevention of clinical fractures after a hip fracture:
Recommended dose is a single intravenous infusion of 5 mg Zoledronic Acid. Re-treatment with Zoledronic Acid may be considered in patients who have relapsed, based on increases in serum alkaline phosphatase, in patients who have had a active remission of serum alkaline phosphatase or in patients with osteoporosis, as dictated by medical practice 12 months after the initial dose.
In patients with Paget’s disease, adequate Vitamin-D intake is recommended.
in association with Zoledronic Acid administration. In addition, it is strongly advised that adequate supplemental Calcium corresponding to at least 500 mg elemental Calcium daily was to be ensured in patients with Paget’s disease for a least 10 days following Zoledronic Acid administration.
Special dosage instruction: Patients with renal impairment. The use of Zoledronic Acid in patients with creatinine clearance <35 ml/min is not recommended due to limited clinical safety data in such patients. No dose adjustment is necessary in patients with creatinine clearance <35 ml/min. Patients with hepatic impairment. No dose adjustment is required. However because decreased renal function occurs more common in the elderly, special care should be taken for monitor renal function.
Method of administration: Follow all directions given to you by your doctor carefully.
Zoledronic Acid should be administered intravenously via an infusion line, given at a constant infusion rate. The infusion time must not be less than 15 minutes. Two glasses of fluid (such as water) before and after the infusion are usually enough. The infusion rate should be adjusted by the patient’s response on the day you are treated with Zoledronic Acid.
Zoledronic Acid must not be mixed or given intravenously with any other medication or drug. If given intravenously, Zoledronic Acid is a constant infusion rate. If refrigerated, allow the refrigerated solution to reach room temperature before administration. Aseptic techniques must be followed during the administration of Zoledronic Acid. If given intravenously, Zoledronic Acid should be discarded. Only clear solution free from particles and discoloration should be used. After the operation, Zoledronic Acid is physically stable for at least 24 hours at 2°C to 4°C. From a microbiology point of view, the product should be used immediately. Zoledronic Acid should be used only for infusion and not for oral administration. Consult with any Calcium or other divalent cation-containing solutions.
Special drug-drug interaction studies have not been conducted with Zoledronic Acid. Zoledronic Acid is eliminated by renal excretion. Caution is indicated when Zoledronic Acid is administered in conjunction with drugs that can significantly impact renal function (e.g. aminoglycosides or diuretics that may cause dehydration).
Over dosage: Clinical experience with acute over dosage is limited. Patients who have received dosage higher than those recommended should be carefully monitored. In the event of overdose leading to clinically significant hypocalcaemia, reversal may be achieved with supplemental oral Calcium and/or an infusion to Calcium.
Pregancy and Lactation: Pregnant women and lactating mother should not take this medicine.
Patients must be appropriately hydrated prior to administration of Zoledronic Acid. This is especially important in the elderly and for patients receiving diuretic therapy. Adequate hydration can be achieved by the patient drinking two glasses of fluid (such as water) before and after the infusion. Preexisting hypocalcaemia must be treated by adequate intake of Calcium and Vitamin-D before initiating therapy with Zoledronic Acid. Other disturbances of mineral metabolism must be effectively treated (e.g. diminished parathyroid reserve, thyroid surgery and Intestinal Calcium malabsorption). Physicians should consider clinical monitoring for these patients.