Zoledronic Acid

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Aclasta, Zometa; Belgium: Aclasta, Zometa; Bulgaria: Aclasta, Zometa; Czech Republic: Aclasta, Zometa; Denmark: Aclasta, Zometa; Estonia: Aclasta, Zometa; Finland: Aclasta, Zometa; France: Aclasta, Zometa; Germany: Aclasta, Zometa; Greece: Aclasta, Zometa; Hungary: Aclasta, Zometa; Ireland: Aclasta, Zometa; Italy: Aclasta, Zometa; Latvia: Aclasta, Zometa; Lithuania: Aclasta, Zometa; Luxembourg: Aclasta, Zometa; Malta: Aclasta, Zometa; Netherlands: Aclasta, Zometa; Poland: Aclasta, Zometa; Portugal: Aclasta, Zometa; Romania: Aclasta, Zometa; Slovakia: Aclasta, Zometa; Slovenia: Aclasta, Zometa; Spain: Aclasta, Zometa; Sweden: Aclasta, Zometa; UK: Aclasta, Zometa.

North America

Canada: Aclasta, Zometa; USA: Reclast, Zometa.

Latin America

Argentina: Ácido Zoledrónico, Aclasta, Dreico, Rionit, Sinresor, Varidrónico, Xedrón, Zometa; Brazil: Aclasta, Zometa; Mexico: Zometa.

Asia

Japan: Zometa.

Drug combinations

Chemistry

Zoledronic Acid: C~5~H~10~N~2~O~7~P~2~ H~2~O. Mw: 290.10. (1) Phosphonic acid, [1-hydroxy-2-(1H-imidazol-1-yl)ethylidene]bis-, monohydrate; (2)(1-Hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid, monohydrate. CAS-165800-06-6 (1996).

Pharmacologic Category

Bone Resorption Inhibitors; Bisphosphonate Derivative. Antidotes. (ATC-Code: M05BA08).

Mechanism of action

Inhibits bone resorption via actions on osteoclasts or on osteoclast precursors. Inhibits osteoclastic activity and skeletal calcium release induced by tumors. Decreases serum calcium and phosphorus, and increases their elimination. In osteoporosis, zoledronic acid inhibits osteoclast-mediated resorption, therefore reducing bone turnover.

Therapeutic use

Treatment of hypercalcemia of malignancy. Treatment of multiple myeloma. Treatment of bone metastases of solid tumors. Treatment of Paget’s disease of bone. Treatment of osteoporosis in postmenopausal women (to reduce incidence of fractures or of new clinical fractures in low-trauma hip fracture). Treatment of osteoporosis in men (to increase bone mass).

Pregnancy and lactiation implications

Should not be used during pregnancy (may cause fetal harm if administered to a pregnant woman). As it binds to bone long-term, use not recommended in nursing women.

Unlabeled use

Prevention of bone loss associated with aromatase inhibitor therapy in postmenopausal women with breast cancer. Prevention of bone loss associated with androgen deprivation therapy in prostate cancer.

Contraindications

Hypersensitivity to zoledronic acid, other bisphosphonates, or any component of the formulation. Hypocalcemia.

Warnings and precautions

Infrequently, severe (and occasionally debilitating) bone, joint, and/or muscle pain reported during bisphosphonate treatment (avoid use in history of symptoms in association with bisphosphonate therapy). Bisphosphonate therapy associated with osteonecrosis, primarily of jaw. Use with caution in aspirin-sensitive asthma (may cause bronchoconstriction). May cause hypocalcemia in Paget’s disease (use caution in disturbances of calcium and mineral metabolism (e.g. hypoparathyroidism, thyroid surgery, malabsorption syndromes)). Use with caution in renal impairment, and in the elderly (possible decreased renal function). Not approved for use in children. Women of childbearing age should avoid becoming pregnant.

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