What is the mechanism of action for bisphosphonates?

What is the mechanism of action for bisphosphonates?

Mechanism of action — The bisphosphonates inhibit osteoclastic bone resorption via a mechanism that differs from that of other antiresorptive agents [2-4]. Bisphosphonates attach to hydroxyapatite binding sites on bony surfaces, especially surfaces undergoing active resorption.

How do nitrogen bisphosphonates work?

N-BPs have been shown to prevent formation of farnesyl pyrophosphate (FPP) and geranylgeranyl pyrophosphate (GGPP), through inhibition of FPP synthase and GGPP synthase, both enzymes in the mevalonate pathway[13–16]. A major effect of these agents is promotion of apoptosis of mature osteoclasts.

How do bisphosphonates work in hypercalcemia?

Bisphosphonates inhibit osteoclastic bone resorption and are effective in the treatment of hypercalcemia due to conditions causing increased bone resorption and malignancy-related hypercalcemia. Pamidronate and etidronate can be given intravenously, while risedronate and alendronate may be effective as oral therapy.

What is the mechanism of action of alendronate?

Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro – PMC.

What is the mechanism of action of risedronate?

Risedronate is a pyridine-based bisphosphonate that inhibits bone resorption caused by osteoclasts Label. Risedronatic acid binds to bone hydroxyapatite Label. Bone resorption causes local acidification, releasing risedronic acid which is that taken into osteoclasts by fluid-phase endocytosis 1.

What is the mechanism of action of the oral and intravenous bisphosphonates in the treatment of osteoporosis?

In addition to their ability to inhibit calcification, bisphosphonates inhibit hydroxyapatite breakdown, thereby effectively suppressing bone resorption.

What is the mechanism of action of Prolia?

Prolia prevents RANKL from activating its receptor, RANK, on the surface of osteoclasts and their precursors. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function, and survival, thereby decreasing bone resorption and increasing bone mass and strength in both cortical and trabecular bone.

How do bisphosphonates inhibit osteoclast activity?

A, Nitrogen-containing bisphosphonates selectively inhibit farnesyl pyrophosphate synthase (FPPS) within osteoclasts. B, Osteoclast endocytosis of bisphosphonate from the bone surface leads to FPPS inhibition and osteoclast apoptosis.

How do you correct hypercalcemia?


  1. Calcitonin (Miacalcin). This hormone from salmon controls calcium levels in the blood.
  2. Calcimimetics. This type of drug can help control overactive parathyroid glands.
  3. Bisphosphonates.
  4. Denosumab (Prolia, Xgeva).
  5. Prednisone.
  6. IV fluids and diuretics.

What is the first line treatment for hypercalcemia?

Intravenous bisphosphonates are the treatment of first choice for the initial management of hypercalcaemia, followed by continued oral, or repeated intravenous bisphosphonates to prevent relapse.

How do bisphosphonates work in osteoporosis?

In people with osteoporosis, the bones lose minerals faster than they can be regenerated. Bisphosphonates help prevent your bones from losing calcium and other minerals by slowing or stopping the natural processes that dissolve bone tissue. In doing this, they help your bones remain strong and intact.

What is the action of Actonel?

CLINICAL PHARMACOLOGY Actonel Mechanism of Action: Actonel has an affinity for hydroxyapatite crystals in bone and acts as an antiresorptive agent. At the cellular level, Actonel inhibits osteoclasts.

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