Product Information
Registration Status: ActiveSIN14992P
ZOLEDRONIC SANDOZ SOLUTION FOR INFUSION 4MG/100ML is approved to be sold in Singapore with effective from 2016-04-26. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN14992P.
This product contains Zoledronic acid 4mg/100ml in the form of INTRAVENOUS INFUSION, SOLUTION. It is approved for INTRAVENOUS use.
This product is manufactured by Novartis Pharma Stein AG in SWITZERLAND, andFresenius Kabi Austria GmbH (DP and Primary packager) in AUSTRIA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Zoledronate (zoledronic acid, marketed by Novartis under the trade names Zometa and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronate is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.
Indication
For the treatment of hypercalcemia of malignancy. Also for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. In May of 2007, the drug was approved for treatment of Paget’s Disease.
Mechanism of Action
The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.
Pharmacokinetics
- Absorption
- Poorly absorbed (oral absorption is about 1% of what intravenous absorption is).
- Distribution
- Metabolism
- Zoledronate does not inhibit human P450 enzymes in vitro and does not undergo biotransformation in vivo.
- Elimination
Clearance
* Renal cl=3.7 +/- 2.0 L/h
Toxicity
There is no experience of acute overdose. Two patients received zoledronate (32 mg) over 5 minutes in clinical trials. Neither patient experienced any clinical or laboratory toxicity. Overdosage may cause clinically significant hypocalcemia, hypophosphatemia, and hypomagnesemia.
Active Ingredient/Synonyms
(1-hydroxy-2-(1H-imidazol-1-yl)ethylidene)bisphosphonic acid | (1-hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid | Anhydrous Zoledronic Acid | Zol | Zoledronate | Zoledronic Acid Anhydrous | Zoledronic Acid, Anhydrous | Zoledronic acid |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.