CH 42 Drugs Affecting Bone Mineral Metabolism Drug Summary Table

Vitamin D metabolites, analogs?

1. cholecalciferol, ergocalciferol

2. calcitrol

3. doxercalciferol (1-hydroxyvitamin D3)

4. paricalcitrol

5. calcipotriene

MOA of cholecalciferol, ergocalciferol?

regulates gene transcription via the vitamin D receptor

Clinical applications of cholecalciferol, ergocalciferol

1. vitamin D deficiency

2. osteoporosis

3. osteomalacia

4. psoriasis

Clinical applications of Calcitrol (active form)?

1. secondary hyperparathyroidism in patients with CKD

2. hypocalcemia in patients with hypoparathyroidism

Clinical applications of doxercalciferol (1-hydroxyvitamin D3)?

secondary hyperparathyroidism in patients with CKD

An analog of Calcitrol used for management of secondary hyperparathyroidism in patients with CKD?

paricalcitrol

An analog of Calcitrol approved for psoriasis?

calcipotriene

Bisphosphonates?

1. alendronate

2. risendronate

3. ibandronate

4. pamidronate

5. zolendronate

MOA of Alendronate (& other Bisphosphonates)?

suppresses the activity of osteoclasts & inhibits bone resorption

Clinical Applications of Alendronate (& other Bisphosphonates)?

1. osteoporosis

2. Paget's disease

Parathyroid hormone (PTH) analogs?

1. teriparatide

2. naptara

MOA of Teriparatide?

acts through PTH receptors to produce a net increase in bone formation

Clinical applications of Teriparatide?

osteoporosis

Full length rhPTH used for hypoparathyroidism?

Naptara

MOA of calcitonin?

acts through calcitonin receptors to inhibit bone resorption

Clinical applications of Calcitonin?

osteoporosis

Selective estrogen-receptor modulator (SERMs)?

Raloxifene

MOA of Raloxifene (SERMs)?

1. estrogen agonist effect in bone

2. estrogen antagonist effects in breast & endometrium

Clinical applications of Raloxifene (SERMs)?

osteoporosis in postmenopausal women

RANK ligand (RANKL inhibitor)?

Denosumab

MOA of Denosumab?

binds to RANKL and prevents it from stimulating osteoclast differentiation and function

Clinical applications of Denosumab?

osteoporosis

Calcimimetic?

Cinacalcet

MOA of Cinacalcet?

activates the calcium-sensing receptor

Clinical applications of Cinacalcet?

hyperparathyroidism

Minerals?

1. calcium

2. phosphate

3. strontium

MOA of Calcium and phosphate?

bone mineralization

MOA of Strontium?

suppresses bone resorption

Clinical applications of Calcium, Phosphate and/or Strontium?

1. osteoporosis

2. osteomalacia

3. calcium or phosphate deficiencies