Zoledronic Acid

Products

Zoledronic acid is commercially available as an infusion preparation (Zometa, Aclasta, generics). It has been approved in many countries since 2000.

Structure and properties

Zoledronic acid (C5H10N2O7P2, Mr = 272.1 g/mol) is present in drugs as zoledronic acid monohydrate, a white crystalline powder that is sparingly soluble in water. It is an imidazole derivative and is not present in the drug as a salt, unlike other bisphosphonates such as alendronate.

Effects

Zoledronic acid (ATC M05BA08) inhibits bone resorption by osteoclasts. It accumulates in bone, where it remains for years.

Indications

  • Patients with bone metastases from solid tumors and in multiple myeloma in combination with standard antineoplastic therapy.
  • Treatment of malignant hypercalcemia.
  • Osteoporosis in postmenopausal women and in men.
  • Osteopenia in postmenopausal women with at least one risk factor.
  • Prevention of clinical fractures after femoral neck fracture in men and women.
  • Prevention and treatment of osteoporosis caused by glucocorticoids in women and men.
  • Paget’s disease of the bone (osteodystrophia deformans).

Dosage

According to the professional information. The drug is administered as an intravenous infusion. For the treatment of postmenopausal osteoporosis, it needs to be injected only once a year. For some indications, even a single dose is sufficient.

Contraindications

  • Hypersensitivity
  • Severe renal dysfunction
  • Hypocalcemia
  • Pregnancy and lactation

Full precautions can be found in the drug label.

Interactions

Drug-drug interactions are possible with drugs that may affect renal function, such as aminoglycosides and diuretics.

Adverse effects

The most common possible adverse effects include fever, muscle pain, joint pain, and flu-like symptoms.