Bisphosphonates

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Contents 1 Mechanism of Action 2 Medical Uses 3 Important Safety Information 4 Available Medications in this Class 5 References 6 External Links

Mechanism of Action

Bisphosphonates are antiresorptive agents. They prevent the transformation of calcium phosphate into hydroxyapatite. In addition, bisphosphonates inhibits osteoclast mediated bone reabsorption through an unknown mechanism. Current theories suggest that alendronate is incorporated into osteoclasts and disrupts the cellular ruffed border. As a result, active bone resorption is reduced. ^[1].

Medical Uses

FDA Approved Indications:

• Treatment and prevention of osteoporosis in postmenopausal females(Alendronate^[2], Alendronate;Cholecalciferol^[3], Etidronate;Calcium^[4], Ibandronate^[5], Risedronate^[6], Risedronate;Calcium^[7]
• Treatment of osteoporosis in males (Alendronate^[2], Risedronate^[6])
• Increase bone mass in males with osteoporosis (Alendronate;Cholecalciferol^[3])
• Paget's disease of the bone (Alendronate^[2], Etidronate^[4], Pamidronate^[8], Risedronate^[6], Tiludronate^[9])
• Prevention of corticosteroid-induced osteoporosis (Etidronate;Calcium^[4], Risedronate^[6])
• Treatment of corticosteroid-induced osteoporosis in males and females with low bone mineral density who are receiving a daily dosage ≥7.5 mg of prednisone (or equivalent)(Alendronate^[2], Risedronate^[6])
• Management of hypercalcemia of malignancy(Clodronate^[10], Pamidronate^[8], Zoledronic Acid^[11])
• Prevention and treatment of heterotopic ossification due to spinal cord injury or after total hip replacement (Etidronate^[4])
• Treatment of osteolytic bone lesions associated with multiple myeloma or metastatic breast cancer (Pamidronate^[8])

Non FDA Approved Indications^[12]:

• Postmenopausal osteoporosis (Etidronate)
• Hypercalcemia of malignancy (Ibandronate)
• Corticosteroid-induced osteoporosis (Ibandronate)
• Paget's disease (Ibandronate)
• Reduction of bone pain and skeletal complications from metastatic bone disease (Ibandronate)
• Treatment of pediatric osteoporosis (Pamidronate)
• Treatment of osteogenesis imperfecta (Pamidronate)
• Treatment of metabolic bone diseases (Zoledronic Acid)

Important Safety Information

Patients may experience signs of serious upper digestive problems after taking bisphosphonates. Symptoms include difficult or painful swallowing, chest pain, or severe or continuing heartburn. Treatment with bisphosphonates may need to be stopped if these occur.

Available Medications in this Class

• Alendronate
• Alendronate;Cholecalciferol
• Risedronate
• Risedronate;Calcium
• Ibandronate
• Pamidronate
• Etidronate
• Etidronate;Calcium
• Tiludronate
• Zoledronic acid
• Clodronate(Not available in U.S.)

Complete Medication Classification List

References

1. ↑ Dipiro JT, Talbert RL, Yee GC, Matzke GR, Wells BG, Posey LM. Pharmacotherapy: A Pathophysiologic Approach. 5th Edition ed. New York, NY: The McGraw-Hill Companies, Inc 2002.
2. ↑ ^{2.0 2.1 2.2 2.3} Fosamax® (alendronate sodium) package insert. Whitehouse Station, NJ; Merck & Co.Inc; 2006 Nov.
3. ↑ ^3.0 3.1 Fosamax Plus D® (alendronate sodium and cholecalciferol) package insert. Whitehouse Station, NJ; Merck & Co.Inc; 2006 Nov.
4. ↑ ^{4.0 4.1 4.2 4.3} Didronel® (etidronate sodium) package insert.Cincinnati, OH; Procter & Gamble Pharmaceuticals; 2005 May.
5. ↑ Boniva® (ibandronate sodium) package insert.Research Triangle Park, NC; GlaxoSmith Kline; 2006 Aug.
6. ↑ ^{6.0 6.1 6.2 6.3 6.4} Actonel® (risedronate sodium) package insert. Bridgewate, NJ; sanofi-aventis U.S.; 2006 Aug.
7. ↑ Actonel with Calcium® (risedronate sodium with calcium carbonate) package insert.Bridgewate, NJ; sanofi-aventis U.S.; 2006 Aug.
8. ↑ ^{8.0 8.1 8.2} Aredia® (pamidronate disodium) package insert.East Hanover, NJ; Novartis Pharmaceutical Corporation; 1998 May.
9. ↑ Skelid® (tiludronate sodium) package insert.Bridgewater, NJ; Sanofi-aventis U.S.; 2006 April.
10. ↑ Lexi-Comp (2003). Drug Information Handbook. 11th Edition., APhA.
11. ↑ Zometa® (zoledronic acid) package insert.East Hanover, NJ; Novartis Pharmaceuticals.
12. ↑ Lacy C, Armstrong L, Goldman M, Lance L. Drug Information Handbook 11th edition: APhA 2003.

External Links

• Package Inserts
  • Fosamax Package Insert
  • Fosamax Plus D Package Insert
  • Actonel Package Insert
  • Actonel with Calcium Package Insert
  • Boniva Package Insert
  • Didronel Package Insert
  • Aredia Package Insert
  • Skelid Package Insert
  • Zometa Package Insert

• Clinical treatment guidelines
  • National Institutes of Health (NIH)
  • American Association of Clinical Endocrinologist (AACE)
  • National Osteoporosis Foundation
  • The 2004 Surgeon General’s Report on Bone Health and Osteoporosis

• Other resources
  • Osteoporosis Risk Assessment
  • American Association of Clinical Endocrinologist (AACE)
  • National Osteoporosis Foundation
  • Nonpharmacologic Prevention and Treatment of Osteoporosis
  • BoneBalance™
  • Foundation for Osteoporosis Research and Education (FORE)
  • International Osteoporosis Foundation
  • National Institutes of Health Osteoporosis and Related Bone Diseases-National Resource Center
  • National Institute on Aging (NIA)