Zoledronic acid.
Zoledronic acid (zoledronate) is a new generation bisphosphonate that inhibits osteoclast bone resorption. It was much more potent than other bisphosphonates at inhibiting 1,25-dihydroxyvitamin D3-induced hypercalcaemia in a rat model and calcium release in vitro. A single 5-minute intravenous infusion of zoledronic acid (4 or 8 mg) was significantly more effective than a 2-hour infusion of pamidronic acid (pamidronic acid disodium, pamidronate disodium) [90 mg] in normalising serum calcium levels in patients with hypercalcaemia of malignancy and resulted in a significantly longer median time to relapse (pooled analysis from 2 randomised, double-blind, parallel-group trials). There were no differences in tolerability between zoledronic acid and pamidronic acid in comparative trials; the most common events in pivotal trials were fever, anaemia, nausea, constipation and dyspnoea. Fever, hypophosphataemia and hypocalcaemia were the most common events in a small phase I trial.
Cheer
S M
SM
Adis International Limited, Mairangi Bay, Auckland, New Zealand. demail@adis.co.nz
Noble
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D000818:Animals; D001862:Bone Resorption / Q000517:prevention & control*; D001842:Bone and Bones / Q000187:drug effects / Q000378:metabolism; D002118:Calcium / Q000378:metabolism; D002986:Clinical Trials as Topic; D004164:Diphosphonates / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D006934:Hypercalcemia / Q000188:drug therapy; D007093:Imidazoles / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D009369:Neoplasms / Q000150:complications* / Q000188:drug therapy; D000077211:Zoledronic Acid
D004164:Diphosphonates; D007093:Imidazoles; D000077211:Zoledronic Acid; D002118:Calcium