Reclast (Novartis)
Reclast (Novartis) - General Information
Reclast (Novartis) (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 Reclast (Novartis) may also prevent recurring fractures in patients with a previous hip fracture.
Reclast (Novartis) 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.
Pharmacology of Reclast (Novartis)
Reclast (Novartis) is a bisphosphonic acid which is an inhibitor of osteoclastic bone resorption. Reclast (Novartis) 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.
Reclast (Novartis) for patients
Reclast (Novartis) Interactions
In vitro studies indicate that zoledronic acid is approximately 22% bound to plasma proteins. In vitro studies also indicate that zoledronic acid does not inhibit microsomal CYP450 enzymes. In vivo studies showed that zoledronic acid is not metabolized, and is excreted into the urine as the intact drug. However, no in vivo drug interaction studies have been performed.
Caution is advised when bisphosphonates are administered with aminoglycosides, since these agents may have an additive effect to lower serum calcium level for prolonged periods. This has not been reported in Zometa clinical trials. Caution should also be exercised when Zometa is used in combination with loop diuretics due to an increased risk of hypocalcemia. Caution is indicated when Zometa is used with other potentially nephrotoxic drugs.
In multiple myeloma patients, the risk of renal dysfunction may be increased when Zometa is used in combination with thalidomide.
Reclast (Novartis) Contraindications
Zometa (zoledronic acid) Injection is contraindicated in patients with clinically significant hypersensitivity to zoledronic acid or other bisphosphonates, or any of the excipients in the formulation of Zometa.
Additional information about Reclast (Novartis)
Reclast (Novartis) 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. Reclast (Novartis) 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Zoledronate
Synonyms: Zoledronic acid; ZOL
Drug Category: Antiresorptives; Bisphosphonates; Antihypocalcemic Agents; Bone Density Conservation Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Zoledronate: Zometa (Novartis); Reclast (Novartis);
Absorption: Poorly absorbed (oral absorption is about 1% of what intravenous absorption is).
Toxicity (Overdose): 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.
Protein Binding: Approximately 22% bound in human plasma, independent of the concentration. However, Canadian product information states binding to human plasma protein is approximately 56%.
Biotransformation: Zoledronate does not inhibit human P450 enzymes in vitro and does not undergo biotransformation in vivo.
Half Life: 146 hours
Dosage Forms of Reclast (Novartis): Powder, for solution Intravenous
Solution Intravenous
Chemical IUPAC Name: (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid
Chemical Formula: C5H10N2O7P2
Zoledronate on Wikipedia: https://en.wikipedia.org/wiki/Zoledronate
Organisms Affected: Humans and other mammals
