Showing posts with label Bisphosphonate. Show all posts
Showing posts with label Bisphosphonate. Show all posts

Alendronate (Fosamax)

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Name: Alendronate (Fosamax)

Class: Bisphosphonate

Mechanism: Structure sim. to inorganic pyrophosphate. Impairs formation and dissolution of calcium phosphate crystals. Alters number/activity of osteoclasts (1° effect) ® slowed bone resorption. Slows formation and dissolution of hydroxyapatite crystals.

Absorption:

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s:

Utility: Increases bone mass in spines and hips of postmenopausal women ® ¯ incidence of fractures.

Special Features: Efficacy maintained over at least 3 yr.

 

Pamidronate (Aredia)

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Name: Pamidronate (Aredia)

Class: Bisphosphonate

Mechanism: Structure sim. to inorganic pyrophosphate. Impairs formation and dissolution of calcium phosphate crystals. Alters number/activity of osteoclasts (1° effect) ® slowed bone resorption. Slows formation and dissolution of hydroxyapatite crystals.

Absorption: IV admin. only

Dist.:

Metabolism.:

Excretion, :

Toxicity/S.E.s:

Utility: DOC for mod.-severe hypercalcemia assoc. w/malignant neoplasms. Treat Paget’s disease of bone. Must be used in conjnxn w/adequate hydration and urinary output.

Special Features: 100x more potent than etidronate, more efficacious, and does not affect normal bone mineralization at normal therapeutic concentrations.

 

Sodium etidronate (Didronel)

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Name: Sodium etidronate (Didronel)

Class: Bisphosphonate

Mechanism: Structure sim. to inorganic pyrophosphate. Impairs formation and dissolution of calcium phosphate crystals. Alters number/activity of osteoclasts (1° effect) ® slowed bone resorption. Slows formation and dissolution of hydroxyapatite crystals.

Absorp.: Oral ® very little absorp., but still effective. Oral absorp. varies w/dose. Further reduced by food or divalent cations. IV ® much higher blood levels.

Dist.: 50% of absorbed drug accum. in bone and turns over w/t½ of weeks.

Metabolism.:

Excretion, : 50% rapidly excreted unchanged by kidney.

Toxicity/S.E.s: Protracted or high-dose therapy ® osteomalacia.

Utility: Treat Paget’s disease of bone as well as or better than calcitonin—oral efficacy, lower cost, no antigenicity, longer remissions. However, chronic use ® osteomalacia w/­risk of bone pain & fractures. Treat heterotopic ossification—given orally after total hip replacement or spinal injury. Treat hypercalcemia of malignancy (IV). Under testing for long-term intermittent therapy for vertebral osteoporosis (+ calcium and vit. D).

Special Features: Unlike pyrophosphate, resistant to enzymatic hydrolysis. Clinical failure of therapy often due to coadmin. w/calcium tablets or food