Drug reference

Zoledronic acid

Bisphosphonate · Agent for Disorders of Bone Metabolism

BisphosphonateAgent for Disorders of Bone Metabolism

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

CidofovirSevereDatabaseDDInter
DeferasiroxSevereDatabaseDDInter
DiatrizoateSevereDatabaseDDInter
EtelcalcetideSevereDatabaseDDInter

Mechanism

Zoledronic acid is the most potent bisphosphonate available, with approximately 100-fold greater antiresorptive activity than pamidronate. It binds avidly to hydroxyapatite in bone and is internalized by osteoclasts during bone resorption, where it inhibits farnesyl pyrophosphate synthase in the mevalonate pathway — preventing prenylation of small GTPases (Ras, Rho, Rac) essential for osteoclast cytoskeletal organization, membrane ruffling, and survival. Intravenous administration of 5 mg once yearly is sufficient for osteoporosis treatment due to its avid skeletal binding and persistent activity.

Indications

Glucocorticoid-induced osteoporosis (as an alternative in patients intolerant of oral bisphosphonates or in whom they are contra-indicated)Osteoporosis in men (as an alternative in patients intolerant of oral bisphosphonates or in whom they are contra-indicated)Osteoporosis in postmenopausal women (as an alternative in patients intolerant of oral bisphosphonates or in whom they are contra-indicated)

Dosing

Geriatric: Treatment can be continued beyond 3 years in patients over 75 years of age, or with a history of previous hip or vertebral fracture, or patients who have had one or more fragility fractures during treatment, or who are taking long-term glucocorticoid therapy.