Bisphosphonate Mechanism

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.Apr 6, 2022

What is the function of bisphosphonates?

Bisphosphonates are a group of drugs that work by slowing bone loss. They reduce the risk of hip and spine fractures. Bone renewal is a slow process, but in many people an increase in bone density can be measured over five years of treatment.

How do bisphosphonates slow down osteoclasts?

Bisphosphonates are drugs that target areas of higher bone turnover. The osteoclast cells, which break down old bone, absorb the bisphosphonate drug. Their activity is slowed down. This reduces bone breakdown.

What is the mechanism of action of Romosozumab?

Mechanism of Action

Evenity (romosozumab-aqqg) is a humanized monoclonal antibody (IgG2) and inhibits the action of sclerostin, a regulatory factor in bone metabolism. Evenity increases bone formation and, to a lesser extent, decreases bone resorption.

How do bisphosphonates treat 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 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 Prolia?

Denosumab, a recently approved therapy, is a fully human monoclonal antibody that binds the cytokine RANKL (receptor activator of NF?B ligand), an essential factor initiating bone turnover. RANKL inhibition blocks osteoclast maturation, function and survival, thus reducing bone resorption.

How do bisphosphonates decrease calcium?

By inhibiting bone resorption, bisphosphonates reduce calcium efflux from bone into the circulation, leading to the development of hypocalcemia.

What is the role of calcium supplements when patients take bisphosphonates?

Calcium supplementation effectively reduces the rate of bone loss in postmenopausal women, yet most women do not achieve an adequate calcium intake. In fact, use of calcium supplementation appears to have declined as the more effective antiresorptive therapies, such as bisphosphonates, have become available.

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 raloxifene?

The mechanism of action of raloxifene occurs through binding to estrogen receptors. This binding results in activation of estrogenic pathways (estrogen-agonistic effect) and blockade (estrogen-antagonistic effect) in tissues that express estrogen receptors.

How do bisphosphonates inhibit osteoclast activity?

Bisphosphonates also reduce osteoclast activity by decreasing osteoclast progenitor development and recruitment and by promoting osteoclast apoptosis [6]. In addition to their inhibitory effect on osteoclasts, bisphosphonates appear to have a beneficial effect on osteoblasts.

Is Romosozumab the same as denosumab?

The present study revealed that romosozumab treatment is more effective than denosumab treatment in increasing BMD of the lumbar spine at 3 months. Furthermore, the present study suggested that romosozumab treatment has no effects on the disease activity of RA in patients with RA and severe osteoporosis for 6 months.

What are the two main adverse effects of bisphosphonates?

General side effects of bisphosphonates and denosumab

  • Fever and flu-like symptoms. …
  • Low levels of calcium in your blood (hypocalcaemia) …
  • Bone and joint pain. …
  • Changes in bowel movements. …
  • Tiredness and low energy levels. …
  • Feeling sick. …
  • Changes to your kidneys. …
  • Irritation of the food pipe (oesophagus)

What is the action of alendronate?

This medication works by slowing bone loss. This effect helps maintain strong bones and reduce the risk of broken bones (fractures). Alendronate belongs to a class of drugs called bisphosphonates.

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.

Can risedronate cause high blood pressure?

Abdominal pain, back pain, belching, cough, constipation, cramping, diarrhea, difficulty swallowing, headache, heartburn, high blood pressure, skin rash, and urinary tract infections. Risedronate, like other bisphosphonates, may irritate the esophagus and stomach.

Is denosumab an immunosuppressant?

Denosumab is an antibody-based medication, but it doesn’t suppress your immune system. This means it doesn’t increase your risk of complications from the coronavirus. This is unlike other antibody-based medications used to treat diseases like rheumatoid arthritis.

Why does Prolia cause hypocalcemia?

Denosumab is a receptor activator of nuclear factor kappa-B (RANK) ligand inhibitor used in the treatment of osteoporosis. Blockade of RANK ligand prevents osteoclastic resorption of bone, but in doing so impairs the parathyroid hormone (PTH)-driven maintenance of serum calcium.

Is denosumab a biologic?

Objective: Denosumab is a biologic agent used to treat osteoporosis.

Why are bisphosphonates contraindicated in hypocalcemia?

The use of bisphosphonates is contraindicated for the treatment of osteoporosis in patients with hypocalcemia. These agents increase bone mineral density, a process that requires an adequate supply of calcium in the body.

What is IV bisphosphonate treatment?

Background: Intravenous bisphosphonates are widely used for treatment of postmenopausal osteoporosis. They are associated with transient influenza-like symptoms, predominantly after the first zoledronic acid (up to 32 %) or ibandronate (up to 5 %) administration.

What drugs decrease calcium levels?

Bisphosphonates. Intravenous osteoporosis drugs, which can quickly lower calcium levels, are often used to treat hypercalcemia due to cancer. Risks associated with this treatment include breakdown (osteonecrosis) of the jaw and certain types of thigh fractures. Denosumab (Prolia, Xgeva).

Why do bisphosphonates cause osteonecrosis of the jaw?

The mechanism by which BPs cause osteonecrosis is not proven but is probably due to a combination of decreased bone remodelling, poor wound healing, and an antiangiogenic effect leading to ischaemic changes and subsequent necrosis in response to a local traumatic insult.

When do you repeat DEXA after bisphosphonate?

For patients who discontinue bisphosphonates, conduct an annual review of risk factors. A repeat DEXA scan is recommended after two to three years.

Do bisphosphonates build bone?

Standard treatments, drugs called bisphosphonates, stop the loss of bone but do not build it. The alternatives, parathyroid hormone and a derivative, build bone but also break it down, limiting the therapeutic effect.

Why do we give steroids in hypercalcemia?

Corticosteroids are the therapy of choice for cases of 1,25-dihydroxyvitamin D (calcitriol) mediated hypercalcemia. Steroids inhibit 1-?-hydroxylase conversion of 25-hydroxyvitamin D (calcidiol) into 1,25-dihydroxyvitamin D (calcitriol) therefore lessening intestinal calcium absorption.

Can calcitonin be given IV?

The recommended starting dose is 100 IU every 6 to 8 hours by subcutaneous or intramuscular injection. In addition, salmon calcitonin could be administered by intravenous injection after previous rehydration.

What does calcium gluconate do to the heart?

Rapid injection of calcium gluconate may cause vasodilation decreased blood pressure, bradycardia, cardiac arrhythmias, syncope and cardiac arrest.

Is raloxifene an immunosuppressant?

Decreased levels of mRNA for both tumor necrosis factor alpha and RANKL in spleen cells from raloxifene-treated arthritic mice indicated an immunosuppressive action of this SERM.

Is raloxifene an agonist or antagonist?

Raloxifene, a selective estrogen receptor (ER) modulator, is a mixed estrogen agonist/antagonist that has been shown to prevent osteoporosis and breast cancer in women.

Does raloxifene increase estrogen?

Also, raloxifene does not stimulate the breast or uterus as estrogen does. Raloxifene lowers the blood concentrations of total and low-density lipoprotein (LDL) cholesterol, the bad cholesterols, but it does not increase concentrations of high-density lipoprotein (HDL) cholesterol, the good cholesterol, in your blood.

Source : RealOnomics.net

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Tommy E. Junkins

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