Description
Clodronate disodium is a bone resorption inhibitor, useful as adjunct therapy in the treatment of osteolytic bone metastases and malignant hypercalcemia.
Chemical Properties
White Solid
Originator
Proctor & Gamble (USA)
Uses
Clodronic Acid Disodium Salt Hydrate is a bisphosphonate antiresorptive agent; bone resorption inhibitor.
Definition
ChEBI: The disodium salt of clodronic acid. It inhibits bone resorption and soft tissue calcification, and is used (generally as the tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteoly
ic lesions and bone pain associated with skeletal metastases.
brand name
Bonefos (Leiras Oy, Finland).
Hazard
Moderately toxic by ingestion.
Biochem/physiol Actions
Analog of pyrophosphate ion that inhibits the osteoclastic activity leading to bone resorption and osteoporosis. The compound is used in cancer research, especially in skeletal metastases and breast carcinoma. When entrapped in liposomes, it is used for macrophage-selective depletion (macrophage "suicide" technique), especially in spleen and liver. Found also to inhibit collagenase and matrix metalloproteinase1.
Clinical Use
Bisphosphonate:
Management of osteolytic lesions, hypercalcaemia and
bone pain associated with skeletal metastases in patients
with breast cancer or multiple myeloma
Safety Profile
A poison by intravenous route. Moderately toxic by ingestion, intraperitoneal routes. When heated to decomposition it emits toxic vapors of PO, and Cl-
Drug interactions
Potentially hazardous interactions with other drugs
Cytotoxics: concentration of estramustine increased.
Metabolism
Clodronate is not metabolised.
Over 70% of an intravenous dose is excreted unchanged
in the urine within 24 hours, the remainder being
sequestered to bone tissue. The substance which is bound
to bone is excreted more slowly, and the renal clearance is
about 75% of the plasma clearance.
