Role of Bisphosphonates in Osteoporosis

1. BISPHOSPHONATES IN
OSTEOPOROSIS

2. Specific learning objectives
Students will be able to understand
• What are bisphosphonates (BPNs) ?
• Role of BPNs in osteoporosis
• Uses and contraindications
• Adverse effects

3. Osteoporosis
• Systemic skeletal disease
• Characterized by:
• Low bone density
• Micro-architectural
deterioration of bone
• Enhanced bone fragility
and risk of fracture

4. Pharmacotherapy of Osteoporosis
Antiresorptive drugs
• BISPHOSPHONATES
• Raloxifene
• HRT
• Denosumab
Bone forming drugs
• Teriparatide
• Calcium
• Vitamin D
• Strontium ranelate

5. Source: Google images

6. Analogues of pyrophosphate: carbon atom replacing
oxygen in the P-O-P skeleton

7. Classification
BISPHOSPHONATES
First generation BPNs Etidronate
*Tiludronate
Second generation BPNs Pamidronate
Alendronate
Ibandronate
Third generation BPNs Risedronate
Zoledronate
*Not available in India

8. Mechanism(s) of action
Source: Google images

9. MECHANISM OF ACTION
Source: Google images

10. • Oral drugs:
• Alendronate (5-10 mg daily; 35-70 mg weekly)
• Ibandronate
• Risedronate
• Drugs given through i.v. infusion:
• Pamidronate
• Zoledronate (4 mg in 100 ml NS/D5 over 15 min)

11. • Poorly absorbed
• Gastric irritation, esophagitis
• Taken on empty stomach with full glass of water
• Not to lie down or take food for at least 30 min
• Should not be chewed

12. • Bisphosphonates should be avoided with:
• Iron, calcium supplements
• Antacids
• Tea, coffee, fruit juice
• 50% of the absorbed / injected drug is sequestrated
in bones
• 50% is excreted unchanged in urine
Non-absorbable
complex

13. Adverse effects
• Fever, chills or flushing
• Musculoskeletal pain
• Nausea, vomiting or diarrhoea
• Fatigue, dyspnoea, dizziness
• OSTEONECROSIS OF JAW
• CHALKSTICK FRACTURE
Acute
phase
response

14. Contraindications
• Renal failure
• Esophageal motility disorders
• Hypersensitivity

15. Other uses of BPNs
• Paget’s disease
• Hypercalcaemia of malignancy
• Osteolytic bone metastasis
• Breast and prostate cancer

16. Thank you!