How does SERM help osteoporosis?

Some SERMs, such as raloxifene and bazedoxifene, have estrogen activity in bone and, therefore, prevent bone loss, improve bone mineral density (BMD), and decrease the risk of vertebral fracture. The use of SERMs for the prevention and treatment of osteoporosis will be discussed here.

How does a SERM work?

A: SERMs stands for “selective estrogen receptor modulators,” also called estrogen agonists/antagonists, which describes what these drugs do. They activate or block the estrogen receptors only in certain areas of the body and not others. That can make them safer than estrogen alone or result in fewer side effects.

Why do aromatase inhibitors cause bone loss?

—Estrogen regulates physiologic bone remodeling by suppressing osteoclast-mediated bone resorption. During aromatase inhibitor–associated or postmenopausal estrogen deficiency, bone resorption and osteoblast-mediated bone formation are imbalanced, leading to net bone loss.

What is raloxifene mechanism of action?

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 does 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.

How does raloxifene treat osteoporosis?

Raloxifene is used to help prevent and treat thinning of the bones (osteoporosis) only in postmenopausal women. It works like an estrogen to stop the bone loss that can develop in women after menopause, but it does not increase the bone density as much as daily 0.625 mg doses of conjugated estrogens.

What are examples of SERMs?

Two of the most common SERMs are tamoxifen (Nolvadex, Soltamox) and raloxifene (Evista). There are several others as well, including lasofoxifene, bazedoxifene, and clomiphene citrate. Keep reading to learn more about the types of SERMs and how they work to treat different conditions.

Can aromatase inhibitors cause osteoporosis?

However, some of these therapies affect bone metabolism, resulting in osteoporosis. Aromatase inhibitors lower circulating oestrogen levels to almost unrecordable levels in postmenopausal women, predisposing them to bone loss with an increase in fracture risk.

Why does letrozole cause osteoporosis?

Aromatase inhibitors (such as anastrozole, exemestane and letrozole) reduce the amount of oestrogen made in the body, which can reduce bone density and cause fractures.

How does raloxifene work in osteoporosis?

Descriptions. Raloxifene is used to help prevent and treat thinning of the bones (osteoporosis) only in postmenopausal women. It works like an estrogen to stop the bone loss that can develop in women after menopause, but it does not increase the bone density as much as daily 0.625 mg doses of conjugated estrogens.

What are the side effects of raloxifene?

What side effects can this medication cause?

• hot flashes (more common in the first 6 months of raloxifene therapy)
• leg cramps.
• swelling of the hands, feet, ankles, or lower legs.
• flu-like syndrome.
• joint pain.
• sweating.
• difficulty falling asleep or staying asleep.

What is the effect of SERMs on bone homeostasis?

With regards to bone loss and osteoporosis, the action of SERMs on the estrogen receptor affects bone homeostasis by downmodulating the activity of osteoclasts in a transforming growth factor-β3-dependent manner and reducing bone resorption. This affect allows in preventing and treating osteoporosis.

What is the mechanism of action of SERM drugs?

Mechanism of Action The mechanism of action of SERM class of compounds relies on their tissue-selective estrogen receptor agonist or antagonist activity in their interaction with the estrogen receptor, and these properties encompass a certain level of molecular and functional complexity.

Who should use SERMs for osteoporosis?

Abstract. Compared to bisphosphonate drug formulations for osteoporosis, SERMs are to be used primarily in postmenopausal women of younger age and are particularly recommended if there is a family history of invasive breast cancer, as their use greatly reduces the incidence of this type of cancer in women.

Is raloxifene an effective SERM for osteoporosis?

Among the above mentioned SERMs, raloxifene has been widely used in prevention and treatment of postmenopausal osteoporosis and vertebral compression fractures, and clinical studies are now underway to test the comparative advantages of raloxifene with those of bazedoxifene, a more recently developed SERM.