ZOLIDIN CONCENTRATE FOR SOLUTION FOR INFUSION 4 MG/ 5 ML

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.

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 |

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.

Pharmacodynamics

Zoledronate is a bisphosphonic acid which is an inhibitor of osteoclastic bone resorption. Zoledronate is used to prevent osteoporosis and skeletal fractures, particularly in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia, particularly hypercalcemia of malignancy. It can also be helpful for treating pain from bone metastases.

Pharmacokinetics

Absorption:

Poorly absorbed (oral absorption is about 1% of what intravenous absorption is).

Distribution:

Not Available

Metabolism:

Zoledronate does not inhibit human P450 enzymes in vitro and does not undergo biotransformation in vivo.

Elimination:

In 64 patients with cancer and bone metastases, on average (± s.d.) 39 ± 16% of the administered zoledronic acid dose was recovered in the urine within 24 hours, with only trace amounts of drug found in urine post-Day 2.

Half-life

146 hours

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.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

ZOLIDIN CONCENTRATE FOR SOLUTION FOR INFUSION 4 MG/ 5 ML was registered with Health Science Authority of Singapore by ACCORD HEALTHCARE PTE LTD. It is marketed with the registration number of SIN15707P with effective from 2019-06-03.

This product contains 4 mg/vial of Zoledronic Acid in the form of INFUSION, SOLUTION CONCENTRATE.

The medicine was manufactured by INTAS PHARMACEUTICALS LIMITED in INDIA

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: M05BA08

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