~Teachingcenter的醫學筆記~

治療骨礦物動態平衡異常之用藥
Durgs Used in Diseases of Bone Mineral Homeostasis

Vitamin D, Metabolites, Analogs

1. Medication(s)
   • Cholecalciferol
   • Ergocalciferol
   • Calcitriol
   • Doxercalciferol
   • Paricalcitol
   • Calcipotriene
2. Mechanism of Action
   • Regulate gene transcription via the vitamin D receptor.
3. Effects
   • Stimulate intestinal calcium absorption, bone resorption, renal calcium and phosphate reabsorption.
   • Decrease parathyroid hormone (PTH).
   • Promote innate immunity.
   • Inhibit adaptive immunity.
4. Clinical Applications
   • Osteoporosis
   • Osteomalacia
   • Renal failure
   • Malabsorption
   • Psoriasis
5. Toxicites
   • Hypercalcemia, hypercalciuria
   • The vitamin D preparations have much longer half-life than the metabolites and analogs

Bisphosphonates

1. Medication(s)
   • Alendronate
   • Risedronate
   • Ibandronate
   • Pamidronate
   • Zoledronate
2. Mechanism of Action
   • Suppress the activity of osteoclasts in part via inhibition of famesyl pyrophosphate synthesis.
3. Effects
   • Inhibit bone resorption and secondarily bone formation.
4. Clinical Applications
   • Osteoporosis
   • Bone metastases
   • Hypercalcemia
5. Toxicites
   • Adynamic bone
   • Possible renal failure
   • Rare osteonecrosis of the jaw
   • Rare subtrochanteric (femur) fractures

Hormones

1. Medication(s)
   • Teriparatide
   • Calcitonin
2. Mechanism of Action
   • These hormones act via their cognate G protein-coupled receptors.
3. Effects
   • Teriparatide stimulates bone turnover.
   • Calcitonin suppresses bone resorption.
4. Clinical Applications
   • Both are used in osteoporosis.
   • Calcitonin is used for hypercalcemia.
5. Toxicites
   • Teriparatide may cause hypercalcemia and hypercalciuria.

Selective estrogen receptor modulators, SERMs

1. Medication(s)
   • Raloxifene
2. Mechanism of Action
   • Interacts selectively with estrogen receptors.
3. Effects
   • Inhibits bone resorption without stimulating breast or endometrial hyperplasia.
4. Clinical Applications
   • Osteoporosis
5. Toxicites
   • (Does not prevent hot flashes.)
   • Increased risk of venous thromboembolism.

Rank ligand (RANKL) inhibitor

1. Medication(s)
   • Denosumab
2. Mechanism of Action
   • Monoclonal antibody
   • Binds to RANKL and prevents it from stimulating osteoclast differentiation and function.
3. Effects
   • Blocks bone resorption.
4. Clinical Applications
   • Osteoporosis
5. Toxicites
   • May increase risk of infections.

Calcium receptor agonist

1. Medication(s)
   • Cinacalcet
2. Mechanism of Action
   • Activates the calcium-sensing receptor.
3. Effects
   • Inhibits PTH secretion.
4. Clinical Applications
   • Hyperparathyroidism
5. Toxicites
   • Nausea

Minerals

1. Medication(s)
   • Calcium
   • Phosphate
   • Strontium
2. Mechanism of Action
   • Multiple physiologic actions through regulation of multiple enzymatic pathways.
3. Effects
   • Strontium suppresses bone resorption and increases bone formation.
   • Calcium and phosphate required for bone mineralization.
4. Clinical Applications
   • Osteoporosis
   • Osteomalacia
   • Deficiencies in calcium or phosphate
5. Toxicites
   • Ectopic calcification