How does raloxifene work in the body?

Raloxifene prevents and treats osteoporosis by mimicking the effects of estrogen (a female hormone produced by the body) to increase the density (thickness) of bone. Raloxifene decreases the risk of developing invasive breast cancer by blocking the effects of estrogen on breast tissue.

How does raloxifene help 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.

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.

Is raloxifene a partial agonist?

Raloxifene acts as a partial agonist of the ERα and as a pure antagonist of the ERβ. In contrast to the classical ERs, raloxifene is an agonist of the G protein-coupled estrogen receptor (GPER) ( EC50 = 10–100 nM), a membrane estrogen receptor.

What are the benefits of raloxifene?

Raloxifene is used by women to prevent and treat bone loss (osteoporosis) after menopause. It slows down bone loss and helps to keep bones strong, making them less likely to break. Raloxifene may also lower the chance of getting a certain type of breast cancer (invasive breast cancer) after menopause.

Is raloxifene a hormone blocker?

Raloxifene is not an estrogen hormone, but it acts like estrogen in some parts of the body, like your bones. In other parts of the body (uterus and breasts), raloxifene acts like an estrogen blocker.

When is the best time to take raloxifene?

You can take raloxifene at whatever time of day you find easiest to remember but try to take your doses at the same time of day, each day. This will help you to remember to take your doses regularly. You can take the tablet either before or after a meal. If you forget to take a dose, take it as soon as you remember.

What are contraindications of Raloxifene?

Contraindications to raloxifene include past medical history of deep venous thrombosis, renal vein thrombosis, pulmonary embolism, malignancy, active smoking, or any thrombophilia (factor V Leiden deficiency, prothrombin gene mutation G20210A, antiphospholipid syndrome, deficiency of antithrombin, protein c and s …

Does Raloxifene reduce estrogen?

Conclusion(s): In postmenopausal women, raloxifene (60 mg/d) did not increase serum estrogen levels; however, it increased levels of sex steroid-binding globulin and thyroxine-binding globulin and decreased FSH levels.

What is the precautions to be taken before administering the ibandronate?

Before using this medication, tell your doctor or pharmacist your medical history, especially of: esophagus problems (such as heartburn, narrowing of the esophagus, achalasia), low blood calcium levels (hypocalcemia), inability to sit upright or stand for 60 minutes, difficult or painful swallowing, stomach/intestinal …

What is a serious adverse effect that may occur with use of raloxifene?

Seek immediate medical attention if any of these unlikely but serious side effects occur: leg swelling/pain, trouble breathing, chest pain, sudden vision changes, severe headache, weakness on one side of the body, confusion. A very serious allergic reaction to this drug is rare.

What is raloxifene used for?

Raloxifene: mechanism of action, effects on bone tissue, and applicability in clinical traumatology practice Raloxifene, a member of the class of selective estrogen receptor modulators (SERM), reproduces the beneficial effects of estrogens on the skeletal systems, without the negative effects estrogens on breast and endometrium.

How does raloxifene affect the skeletal system?

Raloxifene, a member of the class of selective estrogen receptor modulators (SERM), reproduces the beneficial effects of estrogens on the skeletal systems, without the negative effects estrogens on breast and endometrium. This is a review article summarizing its mechanism, effects on bone and its applicability in traumatology clinical practice.

What is the mechanism of action of raloxifene in breast cancer?

Label In breast tissues, raloxifene acts as an estrogen receptor antagonist to attenuate the estrogen-dependent proliferative effects of epithelial cell expansion. In addition to the antiproliferative effects, raloxifene prevents the production of cytokines and recruitment of macrophages and lymphocytes into tumor mass. 10

Is raloxifene an antagonist or an agonist?

Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect.